| Patent(s) and the Corresponding Patented Drug(s) |
Top |
| World Intellectual Property Organization (WIPO) |
| Patent ID |
WO2014128591 |
| Title |
Pyrrolo [2, 3 -D]Pyrimidine Derivatives As Inhibitors of Janus- Related Kinases (Jak). |
| Abstract |
Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them. |
| Applicant(s) |
Pfizer Inc |
| Representative Drug(s) |
D0FQ4Z |
Drug Info
|
IC50 > 10000 nM |
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[1] |
|
2
|
D0KL3B
|
Drug Info
|
IC50 > 10000 nM
|
[1] |
| Patent ID |
WO2014101295 |
| Title |
Isoxazole Derivative That Inhibits Activity of Janus Kinases (Jaks). |
| Abstract |
Disclosed is an isoxazole derivative that inhibits the activity of the Janus kinases (JAKs), the structure thereof as presented in formula I, formula II, formula IX, and formula XI. The substituent groups in the formulas are described in the description. Also disclosed are the pharmaceutical composition of the compound and a related use in medicine preparation. |
| Applicant(s) |
Zhejiang Dtrm Biopharma |
| Representative Drug(s) |
D0TX2G |
Drug Info
|
IC50 = 7 nM |
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[1] |
|
2
|
D0G9MM
|
Drug Info
|
IC50 = 81 nM
|
[1] |
| Patent ID |
WO2014081732 |
| Title |
Azaindole Derivatives As Jak3 Inhibitors. |
| Abstract |
The present disclosure provides compounds that are JAK3 inhibitors and therefore useful for the treatment of diseases treatable by inhibition of JAK3 such as cancer and inflammatory diseases. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds. |
| Applicant(s) |
Principia Biopharma Inc |
| Representative Drug(s) |
D0HL5C |
Drug Info
|
IC50 = 0.0025 nM |
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[1] |
|
2
|
D09JLL
|
Drug Info
|
IC50 = 0.0035 nM
|
[1] |
| Patent ID |
WO2014039595 |
| Title |
Imidazopyridazine Jak3 Inhibitors and Their Use for The Treatment of Inflammatory and Autoimmune Diseases. |
| Abstract |
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases. |
| Applicant(s) |
Bristol-Myers Squibb Company |
| Representative Drug(s) |
D00PTE |
Drug Info
|
IC50 = 0.7 nM |
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[2] |
|
2
|
D07BND
|
Drug Info
|
IC50 = 1.3 nM
|
[2] |
| Patent ID |
WO2013092854 |
| Title |
Pyrimidine-2,4-Diamine Derivatives As Kinase Inhibitors. |
| Abstract |
The present invention relates to compounds of formula (I) wherein X, R, Y0, T0A, T0B have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immuno logically-mediated diseases. The invention also relates to pharmaceutical compositions including said compoundsand their use as medicaments. |
| Applicant(s) |
Cellzome Limited |
| Representative Drug(s) |
D0LR6J |
Drug Info
|
IC50 = 100 to 1000 nM |
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[2] |
|
2
|
D0S6XT
|
Drug Info
|
IC50 < 100 nM
|
[2] |
|
3
|
D0SJ1Q
|
Drug Info
|
IC50 = 1000 to 10000 nM
|
[2] |
| Patent ID |
WO2013085802 |
| Title |
Pyrrolopyrimidines As Janus Kinase Inhibitors. |
| Abstract |
The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I. |
| Applicant(s) |
Merck Sharp & Dohme Corp |
| Representative Drug(s) |
D0E2WK |
Drug Info
|
IC50 = 5.5 nM |
[1] |
| Patent ID |
WO2013070606 |
| Title |
Methods for Treating Inflammatory Diseases and Pharmaceutical Combinations Useful Therefor. |
| Abstract |
The present invention provides method of treating or lessening the severity of a disease selected from spondyloarthropathy, systemic lupus erythematosus, rheumatoid arthritis, or any combination thereof comprising the administration of a compound of Formula I and an optional co-therapy (e.g., chemotherapy agent, DMARD, or any combination thereof). The present invention also provides a pharmaceutical composition comprising a compound of Formula I, a method of manufacturing a pharmaceutical composition comprising a compound of Formula I, and a method of administering a pharmaceutical composition comprising a solid form of a compound of Formula I. |
| Applicant(s) |
Vertex Pharmaceuticals Incorporated |
| Representative Drug(s) |
D0GH8D |
Drug Info
|
IC50 = 3 nM |
[1] |
| Patent ID |
WO2013030138 |
| Title |
Pyrrolopyrazine Kinase Inhibitors. |
| Abstract |
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases. |
| Applicant(s) |
F. Hoffmann-La Roche Ag |
| Representative Drug(s) |
D0JU1R |
Drug Info
|
IC50 = 0.8 nM |
[1] |
| Patent ID |
WO2013025628 |
| Title |
Janus Kinase Inhibitor Compounds and Methods. |
| Abstract |
The present invention relates to Janus kinase inhibitor compounds, prodrugs, and compositions thereof. Some embodiments include the use of such compounds and compositions for the treatment or prevention of skin and/or eye disorders. Claimed are prodrug compounds of Formula I, II, III: (Formula I, II, III) wherein: A is selected from the group consisting of phosphono, phosphonomethyl, phosphonooxymethyl, alkylaminocarbonyl, and acetyl; wherein the acetyl is optionally substituted with methyl, ethyl, propyl, isopropyl, amino, methylamino, dimethylamino, benzyl, pyrrolidinyl, hydroxylcarbonylmethyl, and hydroxylated tetrahydropyranyl; The other variables are as defined in the claims. |
| Applicant(s) |
LIGAND PHARMACEUTICALS INCORPORATED COLE, Andrew, G. JAMES, Ray, A. SHAO, Yuefei LETOURNEAU, Jeffrey, J. QUINTERO, Jorge, G. RIVIELLO, Christopher, Mark ZHI, Lin |
| Representative Drug(s) |
D0SX1B |
Drug Info
|
IC50 = 0.18 nM |
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[1] |
|
2
|
D00ZVY
|
Drug Info
|
IC50 = 1.4 nM
|
[1] |
| Patent ID |
WO2015173683 |
| Title |
Pyrazolopyridines and Pyrazolopyrimidines. |
| Abstract |
A compound having the structure: A compound having the structure (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein A and A' are independently C or N, where C may be unsubstituted or substituted by halo or C1-C6 alkyl; R and R0 are independently selected from the group consisting of H, C1-C6 alkyl, hydroxy(C1-C6 alkyl), phenyl(C1-C6 alkyl), and -(CH2)n-W, where W is C3-C8 cycloalkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic containing 1 -3 N, S and/or 0 atoms, -SO2-R', -NHSO2-R', -NR"SO2-R' and SR', where R' and R" are independently C1-C6 alkyl or C3-C8 cycloalkyl, etc.; wherein each of said alkyl, cycloalkyl, heterocyclic, phenyl, naphthyl or heteroaryl may be unsubstituted or substituted by phenyl, heteroaryl, etc.; or, R and R0 and the N atom to which they are bonded together form a monocyclic or bicyclic heterocyclic ring which may be unsubstituted or substituted by (a) halo, hydroxy, heteroaryl, C1-C6 alkyl, C1-C6 alkoxy, etc., or (b) -(CH2)n-W, where W is C3-C8cycloalkyl, phenyl, etc.; R1 is H, halo or cyano; R2 and R2' are independently H, C1-C6 alkyl, cyano, C1-C6 alkoxy, C1-C6 alkylthio, or C3-C8 cycloalkyl where alkyl, alkoxy, or cycloalkyl is optionally substituted by one or more fluorine atoms; X is a bond, -CO-, -CONH-, -S02-, -SONH-, or -(CH2)m-; R3 is H, C1-C4 alkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic containing 1 -3 N atoms, a 5-membered heteroaryl or heterocyclic, etc., or (c) 2 O or S atoms and 0-2 N atoms; wherein each of said phenyl, naphthyl, heteroaryl or heterocyclic is optionally substituted by alkyl, 1 substituent -Y-R4 and/or 1 -4 substituents each independently selected from R5; with the proviso that when X is -CO- or -SO2-, R3 is not H; Y is a bond, -(CH2)m- or -O-; R4 is (a) H, C1-C6 alkyl, C3-C8 cycloalkl, halo, oxo, -OR6, -NR7R8, -SR6, -SOR9, -SO2R9, -COR6, -OCOR6, -COOR6, -NR6COR6, -CONR7R8, etc.; (b) phenyl or naphthyl, said phenyl and naphthyl being optionally substituted with 1 -5 substituents selected from C1-C6 alkyl, C3-C8 cycloalkyl, halo, cyano, -OR6, -NR7R8, etc.; or (c) a 3 to 8-membered saturated or partially unsaturated monocyclic heteroaryl, etc.; R6 is H, C1-C6 alkyl or C3-C8 cycloalkyl, etc.; R7 and R8 are each independently H, C1-C6 alkyl or C3-C8 cycloalkyl or are taken together with the nitrogen atom to which they are attached to form a 4-, 5- or 6-membered saturated heterocyclic ring containing 1 -2 nitrogen atoms or 1 nitrogen and 1 oxygen atom, said C1-C6 alkyl is optionally substituted by C3-C8 cycloalkyl, ha lo, etc., and said heterocyclic ring being optionally substituted by one or more C1-C6 alkyl or C3-C8 cycloalkyli groups; R9 is C1-C6 alkyl or C3-C8 cycloalkyl; and, m and n are independently 0, 1, 2 or 3. The invention also relates to pharmaceutically acceptable salts of these compounds and to pharmaceutically acceptable solvates thereof; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly asthma and COPD. |
| Applicant(s) |
Pfizer Inc |
| Representative Drug(s) |
D03QAY |
Drug Info
|
IC50 = 10 nM |
[1] |
| Patent ID |
WO2015164614 |
| Title |
Janus Kinase Inhibitors and Uses Thereof. |
| Abstract |
The present invention provides kinase inhibitors, such as compounds of Formula (I) and Formula (II). The compounds may covalently or non-covalently bind a kinase (e.g., Janus kinase 3 (JAK3)). Also provided are pharmaceutical compositions, kits, methods, and uses that involve the compounds for reducing the activity of a kinase and/or treating and/or preventing a condition associated with aberrant activity of a kinase (e.g., a proliferative disease, inflammatory disorder, autoimmune disorder, painful condition, and/or viral infection). (I) (II). |
| Applicant(s) |
DANA-FARBER CANCER INSTITUTE, INC. |
| Representative Drug(s) |
D01DBB |
Drug Info
|
IC50 = 5 nM |
[2] |
| Patent ID |
WO2015164604 |
| Title |
Hydrophobically Tagged Janus Kinase Inhibitors and Uses Thereof. |
| Abstract |
The present invention provides Janus kinase inhibitors, such as compounds of Formula (I) and Formula (II) wherein RY1 and RY2 comprise a tagged hydrophobic moiety RH. The compounds may covalently or non-covalently bind a kinase (e.g., Janus kinase 3 (JAK3)). The hydrophobic moiety RH may signal to the intracellular protein homeostasis machinery to induce degradation of the targeted kinase. Also provided are pharmaceutical compositions, kits, methods, and uses that involve the compounds for reducing the activity of a kinase and/or treating and/or preventing a condition associated with aberrant activity of a kinase (e.g., a proliferative disease, inflammatory disorder, autoimmune disorder, painful condition, and/or viral infection). |
| Applicant(s) |
Dana-Farber Cancer Institute, Inc |
| Patent ID |
WO2015148867 |
| Title |
Substituted Heteroaryl Compounds and Methods of Use. |
| Abstract |
The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof useful in preventing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease. |
| Applicant(s) |
Calitor Sciences, Llc |
| Representative Drug(s) |
D0GB7G |
Drug Info
|
IC50 = 360 nM |
[2] |
| Patent ID |
WO2015144773 |
| Title |
New Compounds. |
| Abstract |
The invention relates to a compound of formula (I) wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful as therapeutic agent for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, inflammatory bowel diseases, Crohn's disease, Alzheimer's disease, leukemia, osteoarthritis, control of pruritus, chronic respiratory disease or keratoconjunctivitis in mammals. |
| Applicant(s) |
Novartis Tiergesundheit Ag |
| Patent ID |
WO2015123453 |
| Title |
Pyridazine Compounds As Jak Inhibitors. |
| Abstract |
In one aspect, the invention provides a compound according to formula I, as well as tautomers, pharmaceutically acceptable salts, and hydrates thereof. Pharmaceutical compositions, methods of inhibiting Janus kinases (JAKs), and methods for treating a condition or disorder mediated at least in part by JAK kinase activity are also described. |
| Applicant(s) |
Portola Pharmaceuticals, Inc |
| Patent ID |
WO2015119126 |
| Title |
Azaindole Derivative. |
| Abstract |
The purpose of the present invention is to provide a novel compound having a selective JAK3-inhibiting effect and excellent oral absorption. Moreover, the purpose of the present invention is to provide a medical drug useful, on the basis of a JAK3-inhibiting effect, for the prevention and/or treatment of JAK3-associated disease, particularly rheumatoid arthritis or multiple sclerosis. Provided is an azaindole derivative, or a salt thereof, having a cycloalkenyl group that is represented by formula (I) [where R1-R4, m and n are as defined in the Specification], and a medical drug composition comprising the azaindole derivative or salt thereof. |
| Applicant(s) |
Taiho Pharmaceutical Industry Co., Ltd |
| Patent ID |
WO2015110378 |
| Title |
Benzimidazole Derivatives and Pharmaceutical Compositions Thereof for The Treatment of Inflammatory Disorders. |
| Abstract |
The present invention discloses compounds according to Formula (I) wherein Cy, R1, L1 R3, R4, R5, La, and Ra are as defined herein. Novel benzimidazoles according to Formula (I), able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons. |
| Applicant(s) |
Galapagos Nv |
| Representative Drug(s) |
D01CRX |
Drug Info
|
IC50 > 500 nM |
[2] |
| Patent ID |
WO2015110092 |
| Title |
4-Substituted Pyrrolo[2,3-D]Pyrimidine Compound and Use Thereof. |
| Abstract |
The present invention relates to a 4-substituted pyrrolo[2,3-d]pyrimidine compound and the use thereof in preparing medications for treating JAK-targeted diseases such as rheumatoid, immune system dis. |
| Applicant(s) |
Jiangsu Carefree Pharmaceutical Co., Ltd |
| Representative Drug(s) |
D0M3CB |
Drug Info
|
IC50 = 28 nM |
[1] |
| Patent ID |
WO2015091531 |
| Title |
Imidazolopyrimidin-2-Yl Derivatives As Jak Inhibitors. |
| Abstract |
New imidazopyridmin-2-yl derivatives are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use as inhibitors of Janus Kinases (JAK) for the treatment of myeloproliferative disorders, leukemia, lymphoid malignancies and solid tumors; bone marrow and organ transplant rejection; immune-mediated diseases and inflammatory diseases. |
| Applicant(s) |
Almirall, Sa |
| Patent ID |
WO2015089153 |
| Title |
Treatment of Multiple Sclerosis with A 1,2,4-Triazolo [1,5A] Pyridine Derivative. |
| Abstract |
The present disclosure provides methods and compositions for treating chronic autoimmune diseases, such as multiple sclerosis, using [8-(4-methanesulfonyl-phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]-[3-(4-methyl-piperazin-1-yl)-phenyl]-amine or a pharmaceutically acceptable salt thereof. |
| Applicant(s) |
Cephalon, Inc |
| Representative Drug(s) |
D07XYI |
Drug Info
|
IC50 = 63 nM |
[2] |
| Patent ID |
WO2015086693 |
| Title |
Pyrazolopyrimidin-2-Yl Derivatives As Jak Inhibitors. |
| Abstract |
New pyrazolopyridmiin-2-yl derivatives are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK). |
| Applicant(s) |
Almirall, Sa |
| Representative Drug(s) |
D0G0FK |
Drug Info
|
IC50 < 100 nM |
[2] |
| Patent ID |
WO2015083028 |
| Title |
Pyrrolo[2,3-D]Pyrimidinyl, Pyrrolo[2,3-B]Pyrazinyl and Pyrrolo[2,3-D]Pyridinyl Acrylamides. |
| Abstract |
The present invention provides pharmaceutically active pyrrolo[2,3- d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylamides and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK. |
| Applicant(s) |
Pfizer Inc |
| Representative Drug(s) |
D0EX5C |
Drug Info
|
IC50(1000nM ATP) = 7.5 nM; IC50(4000nM ATP) = 0.2 nM |
[1] |
| Patent ID |
WO2015057695 |
| Title |
Novel Compositions, Uses and Methods for Their Preparation. |
| Abstract |
The present invention relates to novel compunds and pharmaceutical compositions thereof which may be useful in the treatment and/or prevention of various conditions. The present invention also provides methods of prearing such compounds and compositions, and methods of using the same. |
| Applicant(s) |
Bohan Jin |
| Representative Drug(s) |
D01EYJ |
Drug Info
|
IC50 > 100 nM |
[2] |
| Patent ID |
WO2015039613 |
| Title |
Compound Inhibiting Kinase Activities of Btk and/or Jak3. |
| Abstract |
A compound capable of inhibiting kinase activities of BTK and/or JAK3, a pharmaceutical composition, and applications in preparing a medicament. The compound is as represented by structural formula I,. |
| Applicant(s) |
Beijing Hanmi Pharmaceutical Co., Ltd |
| Patent ID |
WO2015039612 |
| Title |
Compound Inhibiting Kinase Activities of Btk and/or Jak3. |
| Abstract |
The present invention relates to a compound inhibiting the kinase activities of Bruton's tyrosine kinase (BTK) and/or Janus kinase 3 (JAK3), a pharmaceutical composition of the compound, pharmaceutica. |
| Applicant(s) |
Beijing Hanmi Pharmaceutical Co., Ltd |
| Representative Drug(s) |
D00BYK |
Drug Info
|
IC50 < 10 nM |
[1] |
| Patent ID |
WO2015032423 |
| Title |
Pharmaceutical Compounds. |
| Abstract |
The invention provides a compound which is an amide of the formula (2): or a salt or stereoisomer thereof; wherein: R7 is selected from chlorine and fluorine; R3, R4, R5 and R6 are each independently selected from hydrogen, fluorine and chlorine; n is 0, 1 or 2; Q1 is selected from C(=O), S(=O) and SO2; A is absent or is NR2; R1 is selected from: - hydrogen; - an optionally substituted C1-6 non-aromatic hydrocarbon group; and - 3- to 7-membered non-aromatic carbocyclic and heterocyclic rings containing one or two heteroatom ring members selected from O, N and S, and bridged bicyclic heterocyclic rings of seven to nine ring members of which one or two are nitrogen atoms, the carbocyclic and heterocyclic rings and bridged bicyclic heterocyclic rings being optionally substituted; R2 is selected from hydrogen and C1-4 alkyl; or NR1R2 forms an optionally substituted 4- to 7-membered non-aromatic nitrogen- containing heterocyclic ring optionally containing a second heteroatom ring member selected from nitrogen and oxygen; with the provisos that: (i) no more than two of R3 to R6 are other than hydrogen; and (ii) when R7 and R6 are both fluorine, then one of R3 to R5 is chlorine or fluorine and/or R1-A-Q1 is selected from ethylsulfonyl and isopropylsulfonyl. Also provided are pharmaceutical compositions containing the compounds and their therapeutic uses. |
| Applicant(s) |
Sareum Limited |
| Representative Drug(s) |
D05AXE |
Drug Info
|
IC50 = 43 nM |
[1] |
| Patent ID |
WO2015019365 |
| Title |
N-Cyanomethylamides As Inhibitors of Janus Kinase. |
| Abstract |
The present invention relates to compounds of general formula (1) that are inhibitors of Janus Kinase (JAK), a family of tyrosine kinases that are involved in inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. In particular, the compound of the invention inhibits JAK1 and/or JAK2 and/or JAK3 sub families. The present invention also provides methods for the production of the compounds of the invention, pharmaceutical compositions comprising the compounds of the invention, their tautomeric forms, and their pharmaceutically acceptable salts. |
| Applicant(s) |
Cadila Healthcare Limited |
| Patent ID |
WO2014172513 |
| Title |
3,5-(Un)Substituted-1H-Pyrrolo[2,3-B]Pyridine, 1H-Pyrazolo[3,4-B]Pyridine and 5H-Pyrrolo [2-,3-B]Pyrazine Dual Itk and Jak3 Kinase Inhibitors. |
| Abstract |
The present invention relates to compounds described by Formula: (I) salts thereof, their synthesis, and their use as ITK and JAK3 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and or disorders such disease associated with abnormal cell growth such as autoimmune, inflammation, rheumatoid arthritis, systemic lupus erythematosus, atherosclerosis, ulcerative colitis, psoriatic arthritis, psoriasis, Crohn's, metabolic and cancer diseases. The present invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions and processes for preparing the compounds of the invention. |
| Applicant(s) |
Arrien Pharmaceuticals Llc |
| Representative Drug(s) |
D02IET |
Drug Info
|
IC50 < 100 nM |
[2] |
| Patent ID |
WO2014123167 |
| Title |
Tricyclic Pyrrolopyridine Compound, and Jak Inhibitor. |
| Abstract |
The present invention addresses the problem of providing a novel tricyclic pyrrolopyridine compound which has a JAK inhibitory activity, and is particularly useful for preventing, treating and/or alleviating autoimmune diseases, inflammatory diseases, or allergic diseases. Provided is a novel tricyclic pyrrolopyridine compound represented by formula (I) (the substituents in the formula are defined in detail in the description, however R1 represents a C1-6 alkyl group, or the like, R2 represents a hydrogen atom, or the like, R3 represents a hydrogen atom, or the like, ring A represents a C3-11 cycloalkane, or the like, L1 represents a C1-6 alkylene group, or the like, and R4 represents NRaRb, or the like), a tautomer of said compound or a pharmaceutically acceptable salt thereof, or a solvate of the compound, the tautomer, or the pharmaceutically acceptable salt. |
| Applicant(s) |
Nissan Chemical Industries, Ltd |
| Representative Drug(s) |
D04BOW |
Drug Info
|
IC50 = 28 nM |
[1] |
| Patent ID |
WO2014111037 |
| Title |
Five-and-Six-Membered Heterocyclic Compound, and Preparation Method, Pharmaceutical Composition and Use Thereof. |
| Abstract |
A five-and-six-membered heterocyclic compound as represented by general formula I, pharmaceutically acceptable salt, metabolite, metabolic precursors or drug precursors thereof, preparation method, ph. |
| Applicant(s) |
Shanghai Yunyi Healthcare Management Co., Ltd |
| Representative Drug(s) |
D08WPB |
Drug Info
|
IC50 < 50 nM |
[1] |
| Patent ID |
WO2014058921 |
| Title |
Substituted Pyrimidinyl Kinase Inhibitors. |
| Abstract |
Provided are substituted pyrimidinyl compounds for inhibition of JAK and/or Syk kinase, pharmaceutical compositions thereof, methods for inhibiting JAK and/or Syk kinase activity, and methods for treating conditions mediated at least in part by JAK and/or Syk kinase activity. |
| Applicant(s) |
Portola Pharmaceuticals, Inc |
| Patent ID |
WO2014000032 |
| Title |
Phenyl Amino Pyrimidine Bicyclic Compounds and Uses Thereof. |
| Abstract |
The present invention relates to phenyl amino pyrimidine bicyclic compounds formula (I) which are inhibitors of protein kinases including JAK kinases. In particular the compounds are active against JAK1, JAK2, JAK3 and TYK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases. |
| Applicant(s) |
Ym Biosciences Australia Pty Ltd |
| Representative Drug(s) |
D0RJ3W |
Drug Info
|
IC50 = 61 nM |
[1] |
| Patent ID |
WO2013189771 |
| Title |
Aminotriazolopyridine for Use In The Treatment of Inflammation, and Pharmaceutical Compositions Thereof. |
| Abstract |
The present invention relates to the novel medical use of the compound according to Formula I, in particular in the treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. In particular, the compound inhibits JAK a family of tyrosine kinases, and more particularly JAK1. The present invention also provides pharmaceutical compositions comprising the compound, methods for the prophylaxis and/or treatment of diseases involving inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons by administering the compound. |
| Applicant(s) |
Galapagos Nv |
| Representative Drug(s) |
D09ALF |
Drug Info
|
IC50 > 3600 nM |
[2] |
| Patent ID |
WO2013118986 |
| Title |
Triazolopyridine Derivatives As A Tyrosine Kinase Inhibitor. |
| Abstract |
Provided is a novel triazolopyridine derivative having irreversible tyrosine kinase inhibiting activities, and a pharmaceutical composition comprising the same which can be useful for prevention or treatment of inflammatory diseases, autoimmune diseases, proliferative diseases or hyperproliferative diseases, immunologically mediated diseases, cancers or tumors. |
| Applicant(s) |
Hanmi Pharm Co., Ltd |
| Representative Drug(s) |
D0NK1R |
Drug Info
|
IC50 = 9 nM |
[2] |
| Patent ID |
WO2013117649 |
| Title |
Imidazo [4, 5 -C] Pyridine Derivatives Useful for The Treatment of Degenerative and Inflammatory Diseases. |
| Abstract |
Novel imidazolopyridines according to Formula I, able to inhibit JAK are disclosed, wherein R1 and Cy are as disclosed herein. These compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. |
| Applicant(s) |
Galapagos Nv |
| Patent ID |
WO2013117646 |
| Title |
Novel Compound Useful for The Treatment of Degenerative and Inflammatory Diseases. |
| Abstract |
A novel imidazolopyridine according to Formula I, able to inhibit JAK as disclosed, this compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. |
| Applicant(s) |
Galapagos Nv |
| Patent ID |
WO2013117645 |
| Title |
Imidazo [4, 5 -C] Pyridine Derivatives Useful for The Treatment of Degenerative and Inflammatory Diseases. |
| Abstract |
Wherein R1, L1, R3, R4, Cy, L2 and R5 are as defined herein. Novel imidazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. |
| Applicant(s) |
Galapagos Nv |
| Representative Drug(s) |
D07PTU |
Drug Info
|
IC50 = 0.01 to 100 nM |
[2] |
| Patent ID |
WO2013100631 |
| Title |
Novel Imidazopyridine Derivatives As A Tyrosine Kinase Inhibitor. |
| Abstract |
Provided is a novel imidazopyridine derivative having irreversible tyrosine kinase inhibiting activities, and a pharmaceutical composition comprising the same which can be useful for prevention or treatment of inflammatory diseases, autoimmune diseases, proliferative diseases or hyperproliferative diseases, immunologically mediated diseases, cancers or tumors. |
| Applicant(s) |
Hanmi Pharm. Co., Ltd |
| Representative Drug(s) |
D0P3UH |
Drug Info
|
IC50 < 50 nM |
[2] |
| Patent ID |
WO2013091539 |
| Title |
Pyrrole Six-Membered Heteroaryl Ring Derivative, Preparation Method Therefor, and Medicinal Uses Thereof. |
| Abstract |
The present invention relates to a pyrrole six-membered heteroaryl ring derivative, the preparation method therefor, and the medicinal uses thereof. Specifically, the present invention relates to a new pyrrole six-membered heteroaryl ring derivative as represented in formula (I), the preparation method therefor, a medicinal composition comprising the derivative, and a therapeutic agent using same, and, in particular, the uses as a JAK inhibitor and an immunosuppressor. Substituents in formula (I) have the same definitions as in description. |
| Applicant(s) |
Jiangsu Hengrui Medicine Co |
| Representative Drug(s) |
D09UBE |
Drug Info
|
IC50 = 11 nM |
[1] |
| Patent ID |
WO2013055645 |
| Title |
5,7-Substituted-Imidazo[1,2-C]Pyrimidines. |
| Abstract |
Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities. |
| Applicant(s) |
Array Biopharma Inc |
| Representative Drug(s) |
D0U1HA |
Drug Info
|
IC50 = 100 to 1000 nM |
[2] |
| Patent ID |
WO2013054351 |
| Title |
Heterocyclic Compounds. |
| Abstract |
The present invention relates to novel pyrimidine class of compounds, their pharmaceutically acceptable salts, and pharmaceutically acceptable compositions containing them and their use in medicine. |
| Applicant(s) |
Cadila Healthcare Limited |
| Representative Drug(s) |
D0T5AF |
Drug Info
|
IC50 = 2.9 nM |
[2] |
| Patent ID |
WO2013052355 |
| Title |
Azaindoles As Janus Kinase Inhibitors. |
| Abstract |
The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer. |
| Applicant(s) |
Merck Sharp & Dohme Corp |
| Representative Drug(s) |
D0IQ6G |
Drug Info
|
IC50 < 10 nM |
[1] |
| Patent ID |
WO2013043826 |
| Title |
Tricyclic Compounds Useful As Protein Kinase Inhibitors. |
| Abstract |
The invention provides compounds of Formula (I), pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions. |
| Applicant(s) |
Abbvie Inc |
| Representative Drug(s) |
D0QL7J |
Drug Info
|
IC50 < 1000 nM |
[2] |
| Patent ID |
WO2013041605 |
| Title |
Pyrazolo[4,3-C]Pyridine Derivatives As Kinase Inhibitors. |
| Abstract |
The present invention relates to compounds of formula (I) wherein X1 to X5, Y, ZA, ZB, R and A have the meaning as cited in the description and the claims. Said compounds are useful as kinase inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically- mediated diseases. The invention also relates to pharmaceutical compositions including said compounds as well as the use as medicaments. |
| Applicant(s) |
Cellzome Limited |
| Representative Drug(s) |
D09PIS |
Drug Info
|
IC50 = 5 nM |
[2] |
| Patent ID |
WO2013024895 |
| Title |
Tricyclic Heterocyclic Compounds and Jak Inhibitors. |
| Abstract |
Novel tricyclic pyrimidine compounds and tricyclic pyridine compounds having JAK inhibitory activities are provided. A tricyclic heterocyclic compound represented by the formula (Ia): wherein the rings Aa and Ba, Xa, Ya, R1a, R2a, R3a, L1a, L2a, L3a and na are as defined in the description. |
| Applicant(s) |
Nissan Chemical Industries, Ltd |
| Patent ID |
WO2013017480 |
| Title |
Pyrazolo[4,3-C]Pyridine Derivatives As Jak Inhibitors. |
| Abstract |
The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z5, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments. |
| Applicant(s) |
Cellzome Limited |
| Representative Drug(s) |
D0D1QH |
Drug Info
|
IC50 = 1000 to 10000 nM |
[2] |
| Patent ID |
WO2013017479 |
| Title |
Pyrazolo[4,3-C]Pyridine Derivatives As Jak Inhibitors. |
| Abstract |
The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z4, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically- mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments. |
| Applicant(s) |
Cellzome Limited |
| Representative Drug(s) |
D02VGC |
Drug Info
|
IC50 < 100 nM |
[2] |
| Patent ID |
WO2013017461 |
| Title |
Pyridin-2(1H)-One Derivatives As Jak Inhibitors. |
| Abstract |
New pyridin-2(1H)-one derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK). |
| Applicant(s) |
Almirall Sa |
| Representative Drug(s) |
D0A6RG |
Drug Info
|
IC50 < 100 nM |
[2] |
| Patent ID |
WO2013014162 |
| Title |
Heterocyclyl Pyrimidine Analogues As Jak Inhibitors. |
| Abstract |
The present invention relates to compounds of formula (I), wherein X1 to X5, Z1 to Z3, Y0, RY1, RY2 and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically- mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments. |
| Applicant(s) |
Cellzome Limited |
| Representative Drug(s) |
D01FVC |
Drug Info
|
IC50 < 100 nM |
[2] |
| Patent ID |
WO2013007768 |
| Title |
Tricyclic Heterocyclic Compounds, Compositions and Methods of Use Thereof As Jak Inhibitors. |
| Abstract |
The invention provides novel compounds of formula I having the general formula:(I) wherein Rl s R2, R3, X and Y are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders. |
| Applicant(s) |
F. Hoffmann-La Roche Ag |
| Representative Drug(s) |
D0M2WA |
Drug Info
|
IC50 = 32 nM |
[1] |
| Patent ID |
WO2013007765 |
| Title |
Fused Tricyclic Compounds for Use As Inhibitors of Janus Kinases. |
| Abstract |
The invention provides novel compounds of formula (I) having the general formula (I) wherein R1, V, W, X, Y and Z are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders. |
| Applicant(s) |
F. Hoffmann-La Roche Ag |
| Representative Drug(s) |
D0LS1O |
Drug Info
|
IC50 = 240 nM |
[1] |
| Patent ID |
WO2008079521 |
| Title |
Tricyclic Heteroaryl Compounds Useful As Inhibitors of Janus Kinase. |
| Abstract |
The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. |
| Applicant(s) |
Vertex Pharmaceuticals Incorporated |
| Representative Drug(s) |
D03TEE |
Drug Info
|
Ki < 250 nM |
[2] |
| Patent ID |
WO2014157569 |
| Title |
Heterocyclic Compound. |
| Abstract |
Provided is a compound having an excellent JAK-inhibiting effect, the compound being is useful as an agent for the prevention or treatment of autoimmune diseases (rheumatoid arthritis, psoriasis, infl. |
| Applicant(s) |
Takeda Pharmaceutical Company Limited |
| Representative Drug(s) |
D09RUN |
Drug Info
|
N.A. |
[1] |
| Patent ID |
WO2013148638 |
| Title |
Compositions and Methods Related To Inhibitors of Jak Kinase. |
| Abstract |
Embodiments are directed to JAK kinase inhibiting prodrug compounds of Formula lb, containing a promoiety that results in alcohol derivative of the parent compound upon removal and methods of using an effective amount of said prodrug compounds in the treatment of a JAK-mediated disease or disorder in a subject. Preferred promoieties include phosphate, phosphonate, phosphate salt, sulfate, or sulfate salt. |
| Applicant(s) |
Ep Pharma, Inc |
| Patent ID |
WO2011075334 |
| Title |
Pyrrolo[2,3-D]Pyrimidine Compounds. |
| Abstract |
Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation. (Formula (I)). |
| Applicant(s) |
Pfizer Inc |
| Patent ID |
WO2010141796 |
| Title |
Preparation and Uses of 1,2,4-Triazolo [1,5A] Pyridine Derivatives. |
| Abstract |
This application relates to compounds of the general Formula I and salts thereof, wherein X, R1A, R1B, R2, R3, R4, and R5 are as defined herein. The application also relates to compositions and methods of treatment of hyperproliferative diseases or disorders. |
| Applicant(s) |
Cephalon, Inc |
