Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T11241 Target Info
Target Name Sphingosine-1-phosphate receptor 3 (S1PR3)
Synonyms Sphingosine 1-phosphate receptor Edg-3; S1PR3; S1P3; S1P receptor Edg-3; S1P receptor 3; Endothelial differentiation G-protein coupled receptor 3
Target Type Patented-recorded Target
Gene Name S1PR3
Biochemical Class GPCR rhodopsin
UniProt ID
S1PR3_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
United States Patent and Trademark Office (USPTO)
Patent ID US9707205
Title S1P receptors modulators and their use thereof
Abstract The invention relates to novel compounds that have S1P receptor modulating activity. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, autoimmune response. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as autoimmune response.
Applicant(s) AKAAL PHARMA PTY LTD.
Patent ID US9670220
Title Fused heterocyclic derivatives as S1P modulators
Abstract The present invention relates to a fused heterocyclic derivative of the formula (I) The variables R1-R4, z, A, Q, X and Y are as defined in the claims. The following heterocycles are exemplified sub-structures of formula (I): The compounds of formula (I) are modulators of the S1P receptor (Sphingosine-1-phosphate receptor), More specifically, they are agonists of S1P5. The compounds have therapeutic use in treatment of cognitive disorders, age-relate cognitive decline and dementia.
Applicant(s) Abbvie B.V.; AbbiVie Inc.
Representative Drug(s) D0Q4XE Drug Info N.A. Click to Show More [2]
2 D07JOR Drug Info N.A. [2]
Patent ID US9670220
Title Fused heterocyclic derivatives as S1P modulators
Abstract The present invention relates to a fused heterocyclic derivative of the formula (I) The variables R1-R4, z, A, Q, X and Y are as defined in the claims. The following heterocycles are exemplified sub-structures of formula (I): The compounds of formula (I) are modulators of the S1P receptor (Sphingosine-1-phosphate receptor), More specifically, they are agonists of S1P5. The compounds have therapeutic use in treatment of cognitive disorders, age-relate cognitive decline and dementia.
Applicant(s) Abbvie B.V.; AbbiVie Inc.
Representative Drug(s) D0Q4XE Drug Info N.A. Click to Show More [2]
2 D07JOR Drug Info N.A. [2]
Patent ID US9670220
Title Fused heterocyclic derivatives as S1P modulators
Abstract The present invention relates to a fused heterocyclic derivative of the formula (I) The variables R1-R4, z, A, Q, X and Y are as defined in the claims. The following heterocycles are exemplified sub-structures of formula (I): The compounds of formula (I) are modulators of the S1P receptor (Sphingosine-1-phosphate receptor), More specifically, they are agonists of S1P5. The compounds have therapeutic use in treatment of cognitive disorders, age-relate cognitive decline and dementia.
Applicant(s) Abbvie B.V.; AbbiVie Inc.
Representative Drug(s) D0Q4XE Drug Info N.A. Click to Show More [2]
2 D07JOR Drug Info N.A. [2]
Patent ID US9617250
Title Pyridin-4-yl derivatives
Abstract The invention relates to compounds of the Formula (I), Formula (I) wherein R1 and R2 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
Applicant(s) ACTELION PHARMACEUTICALS LTD.
Representative Drug(s) D0R7ED Drug Info N.A. Click to Show More [3]
2 D0EP8Y Drug Info N.A. [3]
3 D0HW8T Drug Info N.A. [3]
4 D04NEO Drug Info N.A. [3]
Patent ID US9617250
Title Pyridin-4-yl derivatives
Abstract The invention relates to compounds of the Formula (I), Formula (I) wherein R1 and R2 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
Applicant(s) ACTELION PHARMACEUTICALS LTD.
Representative Drug(s) D0R7ED Drug Info N.A. Click to Show More [3]
2 D0EP8Y Drug Info N.A. [3]
3 D0HW8T Drug Info N.A. [3]
4 D04NEO Drug Info N.A. [3]
Patent ID US9617250
Title Pyridin-4-yl derivatives
Abstract The invention relates to compounds of the Formula (I), Formula (I) wherein R1 and R2 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
Applicant(s) ACTELION PHARMACEUTICALS LTD.
Representative Drug(s) D0R7ED Drug Info N.A. Click to Show More [3]
2 D0EP8Y Drug Info N.A. [3]
3 D0HW8T Drug Info N.A. [3]
4 D04NEO Drug Info N.A. [3]
Patent ID US9617250
Title Pyridin-4-yl derivatives
Abstract The invention relates to compounds of the Formula (I), Formula (I) wherein R1 and R2 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
Applicant(s) ACTELION PHARMACEUTICALS LTD.
Representative Drug(s) D0R7ED Drug Info N.A. Click to Show More [3]
2 D0EP8Y Drug Info N.A. [3]
3 D0HW8T Drug Info N.A. [3]
4 D04NEO Drug Info N.A. [3]
Patent ID US9522888
Title Substituted bicyclic compounds
Abstract Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is OH or OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D02WVW Drug Info N.A. Click to Show More [4]
2 D0IL0J Drug Info N.A. [4]
Patent ID US9522888
Title Substituted bicyclic compounds
Abstract Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is OH or OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D02WVW Drug Info N.A. Click to Show More [4]
2 D0IL0J Drug Info N.A. [4]
Patent ID US9216972
Title Tricyclic heterocyclic compounds
Abstract Disclosed are compounds of Formula (I) or stereoisomers or salts thereof, wherein: X1, X2, X3, W, Q1, Q2, and G2 are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D06DRH Drug Info N.A. Click to Show More [5]
2 D09RDP Drug Info N.A. [5]
3 D0T4SV Drug Info N.A. [5]
Patent ID US9216972
Title Tricyclic heterocyclic compounds
Abstract Disclosed are compounds of Formula (I) or stereoisomers or salts thereof, wherein: X1, X2, X3, W, Q1, Q2, and G2 are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D06DRH Drug Info N.A. Click to Show More [5]
2 D09RDP Drug Info N.A. [5]
3 D0T4SV Drug Info N.A. [5]
Patent ID US9216972
Title Tricyclic heterocyclic compounds
Abstract Disclosed are compounds of Formula (I) or stereoisomers or salts thereof, wherein: X1, X2, X3, W, Q1, Q2, and G2 are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D06DRH Drug Info N.A. Click to Show More [5]
2 D09RDP Drug Info N.A. [5]
3 D0T4SV Drug Info N.A. [5]
Patent ID US9216972
Title Tricyclic heterocyclic compounds
Abstract Disclosed are compounds of Formula (I) or stereoisomers or salts thereof, wherein: X1, X2, X3, W, Q1, Q2, and G2 are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D06DRH Drug Info N.A. Click to Show More [5]
2 D09RDP Drug Info N.A. [5]
3 D0T4SV Drug Info N.A. [5]
Patent ID US9187437
Title Substituted oxadiazole compounds
Abstract Disclosed are compounds of Formula (I): or stereoisomers, N-oxides, salts, or prodrugs thereof; wherein: Ring A is phenyl or 5- to 6-membered heteroaryl; (i) R1 and R2 are independently C1-C4 alkyl; or (ii) R1 and R2 together with the carbon atom to which they are attached, form a cyclic group; Q is phenyl or 5- to 6-membered heteroaryl substituted with zero to 3 substituents; and R3, L1, L2, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Applicant(s) BRISTOL-MYERS SQUIBB COMPANY
Representative Drug(s) D0OW3S Drug Info N.A. Click to Show More [6]
2 D0AK7K Drug Info N.A. [6]
3 D0RQ0B Drug Info N.A. [6]
Patent ID US9187437
Title Substituted oxadiazole compounds
Abstract Disclosed are compounds of Formula (I): or stereoisomers, N-oxides, salts, or prodrugs thereof; wherein: Ring A is phenyl or 5- to 6-membered heteroaryl; (i) R1 and R2 are independently C1-C4 alkyl; or (ii) R1 and R2 together with the carbon atom to which they are attached, form a cyclic group; Q is phenyl or 5- to 6-membered heteroaryl substituted with zero to 3 substituents; and R3, L1, L2, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Applicant(s) BRISTOL-MYERS SQUIBB COMPANY
Representative Drug(s) D0OW3S Drug Info N.A. Click to Show More [6]
2 D0AK7K Drug Info N.A. [6]
3 D0RQ0B Drug Info N.A. [6]
Patent ID US9187437
Title Substituted oxadiazole compounds
Abstract Disclosed are compounds of Formula (I): or stereoisomers, N-oxides, salts, or prodrugs thereof; wherein: Ring A is phenyl or 5- to 6-membered heteroaryl; (i) R1 and R2 are independently C1-C4 alkyl; or (ii) R1 and R2 together with the carbon atom to which they are attached, form a cyclic group; Q is phenyl or 5- to 6-membered heteroaryl substituted with zero to 3 substituents; and R3, L1, L2, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Applicant(s) BRISTOL-MYERS SQUIBB COMPANY
Representative Drug(s) D0OW3S Drug Info N.A. Click to Show More [6]
2 D0AK7K Drug Info N.A. [6]
3 D0RQ0B Drug Info N.A. [6]
Patent ID US9181182
Title S1P receptors modulators
Abstract The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.
Applicant(s) Akaal Pharma PTY LTD
Representative Drug(s) D0MH3Y Drug Info N.A. Click to Show More [7]
2 D0A0VI Drug Info N.A. [7]
Patent ID US9181182
Title S1P receptors modulators
Abstract The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.
Applicant(s) Akaal Pharma PTY LTD
Representative Drug(s) D0MH3Y Drug Info N.A. Click to Show More [7]
2 D0A0VI Drug Info N.A. [7]
Patent ID US9181182
Title S1P receptors modulators
Abstract The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.
Applicant(s) Akaal Pharma PTY LTD
Representative Drug(s) D0MH3Y Drug Info N.A. Click to Show More [7]
2 D0A0VI Drug Info N.A. [7]
Patent ID US9150519
Title 6-amino-pyrimidine-4-carboxamide derivatives and related compounds which bind to the sphingosine 1-phosphate (S1P) receptor for the treatment of multiple sclerosis
Abstract The invention relates to compounds of formula (I): wherein X, W, Q, R, R1 and R2 have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
Applicant(s) MERCK SERONO SA
Representative Drug(s) D09LDU Drug Info N.A. Click to Show More [8]
2 D0I5TH Drug Info N.A. [8]
3 D0LT2N Drug Info N.A. [8]
4 D04UXN Drug Info N.A. [8]
Patent ID US9150519
Title 6-amino-pyrimidine-4-carboxamide derivatives and related compounds which bind to the sphingosine 1-phosphate (S1P) receptor for the treatment of multiple sclerosis
Abstract The invention relates to compounds of formula (I): wherein X, W, Q, R, R1 and R2 have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
Applicant(s) MERCK SERONO SA
Representative Drug(s) D09LDU Drug Info N.A. Click to Show More [8]
2 D0I5TH Drug Info N.A. [8]
3 D0LT2N Drug Info N.A. [8]
4 D04UXN Drug Info N.A. [8]
Patent ID US9150519
Title 6-amino-pyrimidine-4-carboxamide derivatives and related compounds which bind to the sphingosine 1-phosphate (S1P) receptor for the treatment of multiple sclerosis
Abstract The invention relates to compounds of formula (I): wherein X, W, Q, R, R1 and R2 have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
Applicant(s) MERCK SERONO SA
Representative Drug(s) D09LDU Drug Info N.A. Click to Show More [8]
2 D0I5TH Drug Info N.A. [8]
3 D0LT2N Drug Info N.A. [8]
4 D04UXN Drug Info N.A. [8]
Patent ID US9150519
Title 6-amino-pyrimidine-4-carboxamide derivatives and related compounds which bind to the sphingosine 1-phosphate (S1P) receptor for the treatment of multiple sclerosis
Abstract The invention relates to compounds of formula (I): wherein X, W, Q, R, R1 and R2 have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
Applicant(s) MERCK SERONO SA
Representative Drug(s) D09LDU Drug Info N.A. Click to Show More [8]
2 D0I5TH Drug Info N.A. [8]
3 D0LT2N Drug Info N.A. [8]
4 D04UXN Drug Info N.A. [8]
Patent ID US8563594
Title S1P3 receptor inhibitors for treating pain
Abstract Disclosed herein are compositions and methods for treating pain using S1P3 receptor inhibitors.
Applicant(s) Allergan, Inc.
Representative Drug(s) D0K8FK Drug Info IC50 = 5 nM Click to Show More [9]
2 D0CV8R Drug Info IC50 = 6 nM [9]
3 D0F4TB Drug Info IC50 = 1600 nM [9]
Patent ID US8563594
Title S1P3 receptor inhibitors for treating pain
Abstract Disclosed herein are compositions and methods for treating pain using S1P3 receptor inhibitors.
Applicant(s) Allergan, Inc.
Representative Drug(s) D0K8FK Drug Info IC50 = 5 nM Click to Show More [9]
2 D0CV8R Drug Info IC50 = 6 nM [9]
3 D0F4TB Drug Info IC50 = 1600 nM [9]
Patent ID US8563594
Title S1P3 receptor inhibitors for treating pain
Abstract Disclosed herein are compositions and methods for treating pain using S1P3 receptor inhibitors.
Applicant(s) Allergan, Inc.
Representative Drug(s) D0K8FK Drug Info IC50 = 5 nM Click to Show More [9]
2 D0CV8R Drug Info IC50 = 6 nM [9]
3 D0F4TB Drug Info IC50 = 1600 nM [9]
Patent ID US8524917
Title 6-substituted indole-3-carboxylic acid amide compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
Abstract The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, o, A, A1, A2, X, Z, R1, R3, R2, p, q and r are as defined in the specification. These compounds are useful for treating a disease or condition selected from the group consisting of glaucoma, dry eye, angiogenesis, cardiovascular conditions and diseases, and wound healing.
Applicant(s) Allergan, Inc.
Representative Drug(s) D0S0MC Drug Info IC50 = 19 nM Click to Show More [10]
2 D0RL7G Drug Info IC50 = 59 nM [10]
Patent ID US8524917
Title 6-substituted indole-3-carboxylic acid amide compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
Abstract The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, o, A, A1, A2, X, Z, R1, R3, R2, p, q and r are as defined in the specification. These compounds are useful for treating a disease or condition selected from the group consisting of glaucoma, dry eye, angiogenesis, cardiovascular conditions and diseases, and wound healing.
Applicant(s) Allergan, Inc.
Representative Drug(s) D0S0MC Drug Info IC50 = 19 nM Click to Show More [10]
2 D0RL7G Drug Info IC50 = 59 nM [10]
Patent ID US10179791
Title Spiro-cyclic amine derivatives as S1P modulators
Abstract The present invention relates to spiro-cyclic amine derivatives of the formula (I) whereinR1 is selected from cyano,(2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl each optionally substituted with CN or one or more fluoro atoms,(3-6C)cycloalkyl, (4-6C)cycloalkenyl or a (8-10C)bicyclic group, each optionally substituted with halogen or (1-4C)alkyl,phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, cyano, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-6C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino and (3-6C)cycloalkyl optionally substituted with phenyl which may be substituted with (1-4C)alkyl or halogen,phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms,monocyclic heterocycle optionally independently substituted with halogen, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (3-6C)cycloalkyl, or phenyl optionally substituted with (1-4C)alkyl or halogen,andbicyclic heterocycle optionally substituted with halogen or (1-4C)alkyl optionally substituted with one or more fluoro atoms; Y(Cn-alkylene)-X is a linking group wherein Y is attached to R1 and selected from a bond, O, CO, S, SO, SO2, NH, CHCH, C(CF3)CH, CC, CH2O, OCO, COO, CONH, NHCO, and trans-cyclopropylene;n is an integer from 0 to 10; andX is attached to the phenylene/pyridyl moiety and selected from a bond, O, S, SO, SO2, NH, CO, CHCH, and trans-cyclopropylene; R2 is H or independently selected from one or more substituents selected from halogen, (1-4C)alkoxy and (1-4C)alkyl optionally substituted with one or more fluor atoms; andR3 is (1-4C)alkylene-R4 wherein the alkylene group may be substituted with one or more halogen atoms or with (CH2)2 to form a cyclopropyl moiety, or R3 is (3-6C)cycloalkylene-R4, CH2-(3-6C)cycloalkylene-R4, (3-6C)cycloalkylene-CH2R4 or COCH2R4, wherein R4 is OH, PO3H2, OPO3H2, COOH, COO(1-4C)alkyl or tetrazol-5-yl;Q is a bond or O;W-T- is selected from CHCH, CH2CH2, CH2O, OCH2, OCH2CH2, and COO;R5 is H or independently selected from one or more halogens;Z is CH, CR2 or N; andA represents a morpholine ring structure or a 5-, 6- or 7-membered cyclic amine;or a pharmaceutically acceptable salt, a solvate or hydrate thereof or one or more N-oxides thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of diseases and conditions in which (a) S1P receptor(s) is (are) involved.
Applicant(s) AbbVie B.V.; AbbVie, Inc.
Representative Drug(s) D0LT5U Drug Info N.A. Click to Show More [11]
2 D0O4RX Drug Info N.A. [11]
3 D08BFF Drug Info N.A. [11]
Patent ID US10179791
Title Spiro-cyclic amine derivatives as S1P modulators
Abstract The present invention relates to spiro-cyclic amine derivatives of the formula (I) whereinR1 is selected from cyano,(2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl each optionally substituted with CN or one or more fluoro atoms,(3-6C)cycloalkyl, (4-6C)cycloalkenyl or a (8-10C)bicyclic group, each optionally substituted with halogen or (1-4C)alkyl,phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, cyano, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-6C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino and (3-6C)cycloalkyl optionally substituted with phenyl which may be substituted with (1-4C)alkyl or halogen,phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms,monocyclic heterocycle optionally independently substituted with halogen, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (3-6C)cycloalkyl, or phenyl optionally substituted with (1-4C)alkyl or halogen,andbicyclic heterocycle optionally substituted with halogen or (1-4C)alkyl optionally substituted with one or more fluoro atoms; Y(Cn-alkylene)-X is a linking group wherein Y is attached to R1 and selected from a bond, O, CO, S, SO, SO2, NH, CHCH, C(CF3)CH, CC, CH2O, OCO, COO, CONH, NHCO, and trans-cyclopropylene;n is an integer from 0 to 10; andX is attached to the phenylene/pyridyl moiety and selected from a bond, O, S, SO, SO2, NH, CO, CHCH, and trans-cyclopropylene; R2 is H or independently selected from one or more substituents selected from halogen, (1-4C)alkoxy and (1-4C)alkyl optionally substituted with one or more fluor atoms; andR3 is (1-4C)alkylene-R4 wherein the alkylene group may be substituted with one or more halogen atoms or with (CH2)2 to form a cyclopropyl moiety, or R3 is (3-6C)cycloalkylene-R4, CH2-(3-6C)cycloalkylene-R4, (3-6C)cycloalkylene-CH2R4 or COCH2R4, wherein R4 is OH, PO3H2, OPO3H2, COOH, COO(1-4C)alkyl or tetrazol-5-yl;Q is a bond or O;W-T- is selected from CHCH, CH2CH2, CH2O, OCH2, OCH2CH2, and COO;R5 is H or independently selected from one or more halogens;Z is CH, CR2 or N; andA represents a morpholine ring structure or a 5-, 6- or 7-membered cyclic amine;or a pharmaceutically acceptable salt, a solvate or hydrate thereof or one or more N-oxides thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of diseases and conditions in which (a) S1P receptor(s) is (are) involved.
Applicant(s) AbbVie B.V.; AbbVie, Inc.
Representative Drug(s) D0LT5U Drug Info N.A. Click to Show More [11]
2 D0O4RX Drug Info N.A. [11]
3 D08BFF Drug Info N.A. [11]
Patent ID US10179791
Title Spiro-cyclic amine derivatives as S1P modulators
Abstract The present invention relates to spiro-cyclic amine derivatives of the formula (I) whereinR1 is selected from cyano,(2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl each optionally substituted with CN or one or more fluoro atoms,(3-6C)cycloalkyl, (4-6C)cycloalkenyl or a (8-10C)bicyclic group, each optionally substituted with halogen or (1-4C)alkyl,phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, cyano, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-6C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino and (3-6C)cycloalkyl optionally substituted with phenyl which may be substituted with (1-4C)alkyl or halogen,phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms,monocyclic heterocycle optionally independently substituted with halogen, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (3-6C)cycloalkyl, or phenyl optionally substituted with (1-4C)alkyl or halogen,andbicyclic heterocycle optionally substituted with halogen or (1-4C)alkyl optionally substituted with one or more fluoro atoms; Y(Cn-alkylene)-X is a linking group wherein Y is attached to R1 and selected from a bond, O, CO, S, SO, SO2, NH, CHCH, C(CF3)CH, CC, CH2O, OCO, COO, CONH, NHCO, and trans-cyclopropylene;n is an integer from 0 to 10; andX is attached to the phenylene/pyridyl moiety and selected from a bond, O, S, SO, SO2, NH, CO, CHCH, and trans-cyclopropylene; R2 is H or independently selected from one or more substituents selected from halogen, (1-4C)alkoxy and (1-4C)alkyl optionally substituted with one or more fluor atoms; andR3 is (1-4C)alkylene-R4 wherein the alkylene group may be substituted with one or more halogen atoms or with (CH2)2 to form a cyclopropyl moiety, or R3 is (3-6C)cycloalkylene-R4, CH2-(3-6C)cycloalkylene-R4, (3-6C)cycloalkylene-CH2R4 or COCH2R4, wherein R4 is OH, PO3H2, OPO3H2, COOH, COO(1-4C)alkyl or tetrazol-5-yl;Q is a bond or O;W-T- is selected from CHCH, CH2CH2, CH2O, OCH2, OCH2CH2, and COO;R5 is H or independently selected from one or more halogens;Z is CH, CR2 or N; andA represents a morpholine ring structure or a 5-, 6- or 7-membered cyclic amine;or a pharmaceutically acceptable salt, a solvate or hydrate thereof or one or more N-oxides thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of diseases and conditions in which (a) S1P receptor(s) is (are) involved.
Applicant(s) AbbVie B.V.; AbbVie, Inc.
Representative Drug(s) D0LT5U Drug Info N.A. Click to Show More [11]
2 D0O4RX Drug Info N.A. [11]
3 D08BFF Drug Info N.A. [11]
Patent ID US10166249
Title Substituted bicyclic compounds
Abstract Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is OH or OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D09SKG Drug Info N.A. Click to Show More [12]
2 D0E5OA Drug Info N.A. [12]
3 D0OH0T Drug Info N.A. [12]
Patent ID US10166249
Title Substituted bicyclic compounds
Abstract Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is OH or OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D09SKG Drug Info N.A. Click to Show More [12]
2 D0E5OA Drug Info N.A. [12]
3 D0OH0T Drug Info N.A. [12]
Patent ID US10166249
Title Substituted bicyclic compounds
Abstract Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is OH or OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D09SKG Drug Info N.A. Click to Show More [12]
2 D0E5OA Drug Info N.A. [12]
3 D0OH0T Drug Info N.A. [12]
References  Top
REF 1 S1P receptors modulators and their use thereof. US9707205.
REF 2 Fused heterocyclic derivatives as S1P modulators. US9670220.
REF 3 Pyridin-4-yl derivatives. US9617250.
REF 4 Substituted bicyclic compounds. US9522888.
REF 5 Tricyclic heterocyclic compounds. US9216972.
REF 6 Substituted oxadiazole compounds. US9187437.
REF 7 S1P receptors modulators. US9181182.
REF 8 6-amino-pyrimidine-4-carboxamide derivatives and related compounds which bind to the sphingosine 1-phosphate (S1P) receptor for the treatment of multiple sclerosis. US9150519.
REF 9 S1P3 receptor inhibitors for treating pain. US8563594.
REF 10 6-substituted indole-3-carboxylic acid amide compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity. US8524917.
REF 11 Spiro-cyclic amine derivatives as S1P modulators. US10179791.
REF 12 Substituted bicyclic compounds. US10166249.

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