Patent(s) and the Corresponding Patented Drug(s) |
Top |
World Intellectual Property Organization (WIPO) |
Patent ID |
WO2017087863 |
Title |
Pyrazole Compounds and Methods of Making and Using Same. |
Abstract |
Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL and/or FAAH. Furthermore, the subject compounds and compositions are useful for the treatment of, for example, pain. |
Applicant(s) |
Abide Therapeutics, Inc |
Representative Drug(s) |
D0S2JF |
Drug Info
|
IC50 = 1000 to 10000 nM |
[1] |
Patent ID |
WO2016014975 |
Title |
Urea/Carbamates Faah Magl or Dual Faah/Magl Inhibitors and Uses Thereof. |
Abstract |
Disclosed are compounds that may be used to inhibit the action of fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL) or dual FAAH/MAGL. |
Applicant(s) |
Northeastern University |
Representative Drug(s) |
D00IPI |
Drug Info
|
IC50 = 0.01 to 0.1 nM |
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[1] |
2
|
D02ZUW
|
Drug Info
|
IC50 = 0.01 to 0.1 nM
|
[1] |
3
|
D09RGE
|
Drug Info
|
IC50 = 0.01 to 0.1 nM
|
[1] |
4
|
D08SMT
|
Drug Info
|
IC50 = 10 to 100 nM
|
[1] |
Patent ID |
WO2015179559 |
Title |
Pyrazole Compounds and Methods of Making and Using Same. |
Abstract |
Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of one or more of MAGL, ABHD6, and FAAH. Furthermore, the subject compounds and compositions are useful for the treatment of, for example, pain, solid tumors and/or obesity. |
Applicant(s) |
Abide Therapeutics, Inc |
Representative Drug(s) |
D0LL0X |
Drug Info
|
IC50 > 1000 nM |
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[1] |
2
|
D0O9DS
|
Drug Info
|
IC50 > 1000 nM
|
[1] |
Patent ID |
WO2012145737 |
Title |
Fatty Acid Amide Hydrolase Inhibitors for Treating Pain. |
Abstract |
Compounds of Formula 1 are described herein. These compounds may be administered to a patient for treatment of suffering from pain or other FAAH mediated conditions. |
Applicant(s) |
Allergan, Inc |
Representative Drug(s) |
D0HZ7J |
Drug Info
|
IC50 = 20 nM |
Click to Show More |
[2] |
2
|
D05FQX
|
Drug Info
|
IC50 = 180 nM
|
[2] |
Patent ID |
WO2010141809 |
Title |
Aryl-Substituted Heterocyclic Urea Modulators of Fatty Acid Amide Hydrolase. |
Abstract |
Certain aryl-substituted heterocyclic urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). |
Applicant(s) |
Janssen Pharmaceutica Nv |
Representative Drug(s) |
D05MKN |
Drug Info
|
IC50 = 3 nM |
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[2] |
2
|
D0J1KT
|
Drug Info
|
IC50 = 5 nM
|
[2] |
Patent ID |
WO2010135360 |
Title |
Isoxazolines As Inhibitors of Fatty Acid Amide Hydrolase. |
Abstract |
The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof. |
Applicant(s) |
Infinity Pharmaceuticals, Inc |
Representative Drug(s) |
D0OI8P |
Drug Info
|
Ki < 100 nM |
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[2] |
2
|
D0Q6GP
|
Drug Info
|
Ki < 100 nM
|
[2] |
3
|
D0R3JK
|
Drug Info
|
Ki < 100 nM
|
[2] |
Patent ID |
WO2010118155 |
Title |
Inhibitors of Fatty Acid Amide Hydrolase. |
Abstract |
Provided herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof, or mixtures thereof, wherein Z1, Z2, X1, X2, X3, R1, R2 R3, m and n are defined herein. Also provided are pharmaceutically acceptable compositions that include a compound of formula I and a pharmaceutically acceptable excipient. Also provided are methods for treating FAAH-mediated disorders comprising administering to a subject in need thereof a therapeutically effective amount of a compound or composition of the present invention. |
Applicant(s) |
Infinity Pharmaceuticals, Inc |
Representative Drug(s) |
D05HJF |
Drug Info
|
Ki < 10 nM |
Click to Show More |
[2] |
2
|
D07JMG
|
Drug Info
|
Ki < 10 nM
|
[2] |
Patent ID |
WO2009126691 |
Title |
Inhibitors of Fatty Acid Amide Hydrolase. |
Abstract |
The present invention provides compounds, and pharmaceutically acceptable compositions thereof, encompassed by any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof. The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof. |
Applicant(s) |
Infinity Pharmaceuticals, Inc |
Representative Drug(s) |
D0P3MU |
Drug Info
|
Ki < 10 nM |
Click to Show More |
[2] |
2
|
D0PU2A
|
Drug Info
|
Ki < 10 nM
|
[2] |
Patent ID |
WO2010007966 |
Title |
Azole Compound. |
Applicant(s) |
Astellas Pharma Inc |
Representative Drug(s) |
D00RKV |
Drug Info
|
IC50human FAAH in a bladder-derived cell line (HTB-9) = 0.047 nM |
[2] |
Patent ID |
WO2012106569 |
Title |
Alpha-Ketoheterocycles and Methods of Making and Using. |
Abstract |
Compounds are disclosed that are effective in inhibition of fatty acid amide hydrolase, an enzyme responsible for catabolism of endogenous cannabinoids such as anandamide. The compounds are useful as analgesic compounds and as sleep-inducing compounds, that can be orally administered, and that can have a relatively long duration of effect. Methods of preparation of the compounds are also provided. The compounds are conformationally constrained analogs of heterocyclylketones such as oxazolylketones. |
Applicant(s) |
The Scripps Research Institute |
Representative Drug(s) |
D03MCC |
Drug Info
|
N.A. |
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[2] |
2
|
D0LZ8I
|
Drug Info
|
N.A.
|
[2] |
Patent ID |
WO2010141817 |
Title |
Heteroaryl-Substituted Spirocyclic Diamine Urea Modulators of Fatty Acid Amide Hydrolase. |
Abstract |
Certain heteroaryl-substituted spirocyclic diamine urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). |
Applicant(s) |
Janssen Pharmaceutica Nv |
Representative Drug(s) |
D09VEY |
Drug Info
|
N.A. |
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[2] |
2
|
D0GI7I
|
Drug Info
|
N.A.
|
[2] |
Patent ID |
WO2010074588 |
Title |
Pharmaceutical Compounds. |
Abstract |
The invention relates to compounds and compositions for inhibiting the enzyme fatty acid amide hydrolase (FAAH), the use of the compounds in therapy and, in particular, for treating or preventing conditions whose development or symptoms are linked to substrates of the FAAH enzyme, and methods of treatment or prevention using the compounds and compositions. |
Applicant(s) |
Bial Portela & Ca Sa |
Representative Drug(s) |
D02JER |
Drug Info
|
N.A. |
Click to Show More |
[2] |
2
|
D0U0QQ
|
Drug Info
|
N.A.
|
[2] |
Patent ID |
WO2010068453 |
Title |
Heteroaryl-Substituted Urea Modulators of Fatty Acid Amide Hydrolase. |
Abstract |
Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis). |
Applicant(s) |
Janssen Pharmaceutica Nv |
Representative Drug(s) |
D04USU |
Drug Info
|
N.A. |
Click to Show More |
[2] |
2
|
D0LB8Y
|
Drug Info
|
N.A.
|
[2] |
Patent ID |
WO2010068452 |
Title |
Heteroaryl-Substituted Urea Modulators of Fatty Acid Amide Hydrolase. |
Abstract |
Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis). |
Applicant(s) |
Janssen Pharmaceutica Nv |
Representative Drug(s) |
D04USU |
Drug Info
|
N.A. |
Click to Show More |
[2] |
2
|
D0LB8Y
|
Drug Info
|
N.A.
|
[2] |
Patent ID |
WO2010005572 |
Title |
Alpha-Keto Heterocycles As Faah Inhibitors. |
Abstract |
The invention provides a series of -alphaketoheterocyclic compounds, for example, compounds of formula (I). The compounds can inhibit fatty acid amide hydrolase and can be useful for treatment of malconditions modulated by fatty acid amide hydrolase. The invention further provides methods of making compounds of formula (I), useful intermediates for the preparation of compounds of formula (I), and methods of using compounds of formula (I) and compositions thereof. |
Applicant(s) |
The Scripps Research Institute |
Patent ID |
WO2009117444 |
Title |
Inhibitors of Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase for Modulation of Cannabinoid Receptors. |
Abstract |
Disclosed are compounds and compositions that inhibit the action of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), methods of inhibiting FAAH and MGL, methods of modulating cannabinoid receptors, and methods of treating various disorders related to modulation of cannabinoid receptors. |
Applicant(s) |
Northeastern University |
Representative Drug(s) |
D09AAB |
Drug Info
|
N.A. |
Click to Show More |
[2] |
2
|
D0RZ5O
|
Drug Info
|
N.A.
|
[2] |
Patent ID |
WO2012088469 |
Title |
Faah Inhibitors. |
Abstract |
The present disclosure relates to compounds useful as inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment or prevention of various disorders. Compounds of the invention are described in Table 1. |
Applicant(s) |
Ironwood Pharmaceuticals, Inc |
Representative Drug(s) |
D00PFD |
Drug Info
|
IC50 = 4 nM |
[2] |
Patent ID |
WO2011139951 |
Title |
Modulators of Fatty Acid Amide Hydrolase. |
Abstract |
4-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1 -carboxylic acid (4-chloro-pyridin-3-yl)-amide is described, which is useful as a FAAH modulator. 4-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1 -carboxylic acid (4-chloro-pyridin-3-yl)-amide may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). A method of synthesizing 4- (2,2-difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1 -carboxylic acid (4- chloro-pyridin-3-yl)-amide is also disclosed. |
Applicant(s) |
Janssen Pharmaceutica Nv |
Representative Drug(s) |
D0IA7Z |
Drug Info
|
IC50 = 75 nM |
[2] |
Patent ID |
WO2011071996 |
Title |
Faah Inhibitors. |
Abstract |
The present disclosure relates to N-benzyl pyrrole compounds of formula (I) useful as inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment or prevention of various disorders. |
Applicant(s) |
Ironwood Pharmaceuticals, Inc |
Representative Drug(s) |
D00PFD |
Drug Info
|
IC50 = 4 nM |
[2] |
Patent ID |
WO2011022348 |
Title |
Ethylene Diamine Modulators of Fatty Acid Amide Hydrolase. |
Abstract |
Certain ethylene diamine compounds of Formula (I) are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed. |
Applicant(s) |
Janssen Pharmaceutica Nv |
Representative Drug(s) |
D0M1ND |
Drug Info
|
IC50 = 20 nM |
[2] |
Patent ID |
WO2010118159 |
Title |
Inhibitors of Fatty Acid Amide Hydrolase. |
Abstract |
Provided herein are compounds of formula (I): or pharmaceutically acceptable salts, solvates or prodrugs thereof or mixtures thereof, wherein Z1, Z2, X1, X2, X3, R1, R2 R3, R4, m and n are defined herein. Also provided are pharmaceutically acceptable compositions that include a compound of formula I and a pharmaceutically acceptable excipient. Also provided are methods for treating an FAAH-mediated disorder comprising administering to a subject in need thereof a therapeutically effective amount of a compound or composition of the present invention. |
Applicant(s) |
Infinity Pharmaceuticals, Inc |
Representative Drug(s) |
D0H8LZ |
Drug Info
|
Ki < 100 nM |
[2] |
Patent ID |
WO2010058318 |
Title |
1-Oxa-8-Azaspiro [4, 5 ] Decane- 8 -Carboxamide Compounds As Faah Inhibitors. |
Abstract |
Provided herein are 1-oxa-8-azaspiro[4.5]decane-8-carboxamide compounds of formula I wherein Ar1, Ar2, R1, R2, R3 and R4 are as defined herein and the pharmaceutically acceptable salts of such compounds useful in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, conditions including acute pain, chronic pain, neuropathic pain, nociceptive pain, inflammatory pain, fibromyalgia, rheumatoid arthritis, inflammatory bowel disease, lupus, diabetes, allergic asthma, vascular inflammation, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease. |
Applicant(s) |
Pfizer Inc |
Representative Drug(s) |
D0DD7K |
Drug Info
|
kinact/Ki = 30800 M-1s-1 |
[2] |
Patent ID |
WO2010049841 |
Title |
7-Azaspiro [3.5] Nonane-7-Carboxamide Compounds As Modulators of Fatty Acid Amide Hydrolase. |
Abstract |
Provided herein are 7-azaspiro[3.5]nonane-7-carboxamide compounds and the pharmaceutically acceptable salts of such compounds useful in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, conditions including including acute pain, chronic pain, neuropathic pain, nociceptive pain, inflammatory pain, cancer and cancer pain, fibromyalgia, rheumatoid arthritis, inflammatory bowel disease, lupus, diabetes, allergic asthma, vascular inflammation, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease. |
Applicant(s) |
Pfizer Inc |
Patent ID |
WO2010039186 |
Title |
Benzoxazoles Useful As Faah Modulators and Uses Thereof. |
Abstract |
Compounds are disclosed that have formula I: wherein X, R1, R2, R3, R4 and n are as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, anxiety, depression, inflammation, cognitive disorders, weight and eating disorders, Parkinson's disease, Alzheimer's disease, spasticity, addiction, glaucoma, and others. |
Applicant(s) |
Renovis, Inc |
Representative Drug(s) |
D05RQF |
Drug Info
|
IC50 = 1.3 nM |
[2] |
Patent ID |
WO2009127949 |
Title |
4- [3- (Aryloxy) Benzylidene] -3-Methyl Piperidine Aryl Carboxamide Compounds Useful As Faah Inhibitors. |
Abstract |
The present invention relates to compounds of Formula (I), wherein Ar is optionally substituted phenyl or heteroaryl and X, Y and Z are independently N or CH; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity. |
Applicant(s) |
Pfizer Inc |
Representative Drug(s) |
D0K2WP |
Drug Info
|
kinact/Ki = 40000 M-1s-1 |
[2] |
Patent ID |
WO2009127948 |
Title |
4- [3- (Aryloxy) Benzylidene] -3-Methyl Piperidine 5-Membered Aryl Carboxamide Compounds Useful As Faah Inhibitors. |
Abstract |
The present invention relates to compounds of Formula (I), wherein Ar is a 5-membered heteroaryl moiety and X, Y and Z are independently N or CH; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity. |
Applicant(s) |
Pfizer Inc |
Representative Drug(s) |
D07MIY |
Drug Info
|
kinact/Ki = 40000 M-1s-1 |
[2] |
Patent ID |
WO2009127944 |
Title |
Ether Benzylidene Piperidine Aryl Carboxamide Compounds Useful As Faah Inhibitors. |
Abstract |
The present invention relates to compounds of Formula (I) wherein Ar is optionally substituted phenyl or 6-membered heteroaryl moiety, or a benzisoxazole, pyrrolopyridine, or benzotriazole group; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, including pain, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease. |
Applicant(s) |
Pfizer Inc |
Representative Drug(s) |
D02ZPG |
Drug Info
|
kinact/Ki = 40000 M-1s-1 |
[2] |
Patent ID |
WO2009109743 |
Title |
Azetidine Derivatives. |
Abstract |
Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Formula (I) Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms. |
Applicant(s) |
Vernalis (R & D) Ltd |
Representative Drug(s) |
D0BN7S |
Drug Info
|
IC50 = 38 nM |
[2] |
Patent ID |
WO2009105220 |
Title |
Aryl-Hydroxyethylamino-Pyrimidines and Triazines As Modulators of Fatty Acid Amide Hydrolase. |
Abstract |
Certain aryl-hydroxyethylamino-pyrimidine and triazine compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed. |
Applicant(s) |
Janssen Pharmaceutica Nv |
Representative Drug(s) |
D01THA |
Drug Info
|
IC50 = 1 nM |
[2] |
Patent ID |
WO2009011904 |
Title |
Compounds Useful As Faah Modulators and Uses Thereof. |
Abstract |
Compounds are disclosed that have formula (I): where A, B, L1, X, W, Y, R1, R3, and nlare as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, anxiety, depression, inflammation, cognitive disorders, weight and eating disorders, Parkinson's disease, Alzheimer's disease, spasticity, addiction, glaucoma, and others. |
Applicant(s) |
Renovis, Inc |
Representative Drug(s) |
D05KXF |
Drug Info
|
IC50 < 100 nM |
[2] |
Patent ID |
WO2015003002 |
Title |
Pyrrolo-Pyrrole Carbamate and Related organic Compounds, Pharmaceutical Compositions, and Medical Uses Thereof. |
Abstract |
The invention provides pyrrolo-pyrrole carbamate and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., solid tumor cancer, obesity, Down's syndrome, Alzheimer's disease, or pain, in a patient. The octahydropyrrolo pyrrole carbamates could be derived from hexafluoroisopropanol, ,-disuccinimide and such. The activity of carbamates in MAGL, FAAH, and ABHD6 assays are also described. |
Applicant(s) |
Abide Therapeutics, Inc |
Representative Drug(s) |
D0GT0I |
Drug Info
|
N.A. |
[1] |
Patent ID |
WO2014004676 |
Title |
Use of Faah Inhibitors As Neuroprotective Agents In The Cns. |
Abstract |
The present disclosure relates to methods of using a fatty acid amide hydrolase (FAAH) inhibitor of Formula I alone or in combination with one or more additional therapeutic agents for the treatment or prevention of neuronal injury or neurodegeneration in a patient in need thereof. |
Applicant(s) |
Ironwood Pharmaceuticals, Inc |
Representative Drug(s) |
D04VYE |
Drug Info
|
N.A. |
[2] |
Patent ID |
WO2012015704 |
Title |
Peripherally Restricted Faah Inhibitors. |
Abstract |
Peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH) are provided. The compounds can suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). Despite their relative inability to access brain and spinal cord, the compounds attenuate behavioral responses indicative of persistent pain in rodent models of inflammation and peripheral nerve injury, and suppresses noxious stimulus-evoked neuronal activation in spinal cord regions implicated in nociceptive processing. CBi receptor blockade prevents these effects. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the inhibition of peripheral FAAH would be of benefit. The compounds of the invention are according to the formula (I): in which R1 is a polar group. In some embodiments, R1 is selected from the group consisting of hydroxy and the physiologically hydro lysable esters thereof. R2 and R3 are independently selected from the group consisting of hydrogen and substituted or unsubstituted hydrocarbyl; each R4 is independently selected from the group consisting of halogen and substituted or unsubstituted hydrocarbyl and n is an integer from 0 to 4; each R5 is independently selected from the group consisting of halo and substituted or unsubstituted hydrocarbyl and m is an integer from 0 to 3; and R6 is substituted or unsubstituted cyclohexyl; and the pharmaceutically acceptable salts thereof. |
Applicant(s) |
The Regents of the University of California |
Representative Drug(s) |
D0LR7Z |
Drug Info
|
N.A. |
[2] |
Patent ID |
WO2011140164 |
Title |
Aza-Indole Derivatives Useful As Modulators of Faah. |
Abstract |
The present invention is directed to certain Aza-Indole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease. |
Applicant(s) |
Merck Sharp & Dohme Corp |
Representative Drug(s) |
D05IZN |
Drug Info
|
N.A. |
[2] |
Patent ID |
WO2011126960 |
Title |
Oxazole Derivatives Useful As Modulators of Faah. |
Abstract |
The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease. |
Applicant(s) |
Merck Sharp & Dohme Corp |
Representative Drug(s) |
D0P2AB |
Drug Info
|
N.A. |
[2] |
Patent ID |
WO2011097233 |
Title |
Fatty Acid Amide Hydrolase Inhibitors. |
Abstract |
The present invention provides fatty acid amide hydrolase inhibitors, solid forms thereof, compositions thereof, and methods of making and using the same. |
Applicant(s) |
Infinity Pharmaceuticals, Inc |
Representative Drug(s) |
D02LJQ |
Drug Info
|
N.A. |
[2] |
Patent ID |
WO2011085216 |
Title |
Use of Faah Inhibitors for Treating Parkinson'S Disease and Restless Legs Syndrome. |
Abstract |
The present disclosure relates to methods of using fatty acid amide hydrolase (FAAH) inhibitors to treat aspects of Parkinson's disease (PD), restless legs syndrome (RLS) and periodic limb movement disorder (PLMD), the use of FAAH inhibitors for the manufacture of medicaments for use in the treatment of PD, RLS and PLMD, as well as pharmaceutically acceptable compositions comprising FAAH inhibitors for use in the treatment of PD, RLS and PLMD. |
Applicant(s) |
Ironwood Pharmaceuticals, Inc |
Representative Drug(s) |
D04VYE |
Drug Info
|
N.A. |
[2] |
Patent ID |
WO2010105930 |
Title |
Carbamate Derivatives In Particular for The Treatment of Neurological Disorders. |
Abstract |
The present invention relates to new carbamate derivatives of formula I, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders, such as neuropathic pain and anxiety. |
Applicant(s) |
Sigma-Tau Industrie Farmaceutiche Riunite Spa |
Representative Drug(s) |
D0KE8U |
Drug Info
|
N.A. |
[2] |
Patent ID |
WO2010101724 |
Title |
Imidazole Derivatives Useful As Modulators of Faah and As Faah Imaging Agents. |
Abstract |
The present invention is directed to certain Inidazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease. |
Applicant(s) |
Merck Sharp & Dohme Corp |
Representative Drug(s) |
D05LBM |
Drug Info
|
N.A. |
[2] |
Patent ID |
WO2009152025 |
Title |
Imidazole Derivatives Useful As Inhibitors of Faah. |
Abstract |
The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease. |
Applicant(s) |
Merck Sharp & Dohme Corp |
Representative Drug(s) |
D00ZGG |
Drug Info
|
N.A. |
[2] |
Patent ID |
WO2009151991 |
Title |
Pyrazole Derivatives Useful As Inhibitors of Faah. |
Abstract |
The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer disease, and Parkinson's disease. |
Applicant(s) |
Merck Sharp & Dohme Corp |
Representative Drug(s) |
D09SWG |
Drug Info
|
N.A. |
[2] |
Patent ID |
WO2009109504 |
Title |
Enol Carbamate Derivatives As Modulators of Fatty Acid Amide Hydrolase. |
Abstract |
The invention provides novel enol carbamate derivatives of formula (I) for inhibiting Fatty Acid Amide Hydrolase (FAAH), compositions that include such compounds as well as methods of treating diseases of energy metabolism, central nervous system disorders, cardiovascular and respiratory disorders, retinopathy, cancer, gastrointestinal and liver disorders and/or musculoskeletal disorders. The compounds of the present invention proved particularly efficacious in animal models of anxiety and pain. |
Applicant(s) |
Sigma-Tau Industrie Farmaceutiche Riunite Spa |
Representative Drug(s) |
D07VNW |
Drug Info
|
N.A. |
[2] |
Patent ID |
WO2009084970 |
Title |
5-O-Substituted 3-N-Phenyl-1,3,4-Oxadiazolones for Medical Use. |
Abstract |
The present invention relates to compounds having a 5-O-substituted 3-N-phenyl-1,3,4-oxadiazolone structural unit which have unexpectedly high level of inhibition of FAAH (fatty acid amide hydrolase). (I). |
Applicant(s) |
Bial-Portela & Ca., Sa |
Representative Drug(s) |
D0B7CW |
Drug Info
|
N.A. |
[2] |
Patent ID |
WO2006054652 |
Title |
Amide Compound. |
Abstract |
An FAAH inhibitor; and a preventive/therapeutic agent for cerebrovascular disorders and a preventive/therapeutic agent for sleep disorders which each contains the inhibitor. The FAAH inhibitor is a compound represented by the formula (I0): (wherein Z represents oxygen or sulfur; R1 represents optionally substituted aryl or an optionally substituted heterocyclic group; R1a represents hydrogen, an optionally substituted hydrocarbon group, hydroxy, etc.; R2 represents optionally substituted piperidine-1,4-diyl or optionally substituted piperazine-1,4-diyl; R3 represents an optionally substituted group formed by removing two hydrogen atoms from a 5-membered aromatic heterocycle having 1-3 heteroatoms selected among nitrogen, oxygen, and sulfur, or represents -CO-, etc.; and R4 represents an optionally substituted hydrocarbon group or optionally substituted heterocyclic group) or a salt of the compound. |
Applicant(s) |
Takeda Pharmaceutical Company Limited |
Representative Drug(s) |
D08JES |
Drug Info
|
N.A. |
[2] |
Patent ID |
WO2010151160 |
Title |
O-Substituted 3-N-Heteroaryl-1,3,4-Oxadiazolones for Medical Use. |
Abstract |
The present invention relates to compound of formula (I), wherein A represents a 5- or 6-membered heteroaromatic ring system containing up to 4 heteroatoms selected from O, S and N, which is optionally substituted, and to a stereoisomer, pharmaceutically acceptable salt or ester, or prodrug thereof. |
Applicant(s) |
Bial Portela & Ca Sa |
Patent ID |
WO2010074587 |
Title |
5-O-Substituted 3-N-Aryl-1,3,4-Oxadiazolones for Medical Use. |
Abstract |
The present invention relates to a compound of formula (I), wherein A represents an optionally substituted phenyl or a 5- or 6-membered heteroaromatic ring system containing up to 4 heteroatoms selected from O, S and N, B represents a single bond, O, S or NR1, wherein R1 is selected from hydrogen or a C1-C6-alkyl group; L represents a linker; C represents an amino moiety; n represents 0 or 1; m represents 0, 1, 2, 3, 4, 5 or 6; X represents O or S; and Y represents hydrogen or an optionally substituted carbon moiety; and to stereoisomers, pharmaceutically acceptable salts or esters, or prodrugs thereof. The compounds of the invention are potent FAAH inhibitors. |
Applicant(s) |
Bial-Portela & Ca., Sa |
Patent ID |
WO2008063300 |
Title |
Boronic Acids and Esters As Inhibitors of Fatty Acid Amide Hydrolase. |
Abstract |
The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). The present invention also provides methods for treating FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a provided compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH in a patient by administering a therapeutically effective amount of a compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof. |
Applicant(s) |
Infinity Pharmaceuticals, Inc |
United States Patent and Trademark Office (USPTO) |
Patent ID |
US2009062294 |
Title |
Heteroaryl-Substituted Urea Modulators of Fatty Acid Amide Hydrolase. |
Applicant(s) |
Janssen Pharmaceutica Nv |
Representative Drug(s) |
D04USU |
Drug Info
|
N.A. |
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[2] |
2
|
D0LB8Y
|
Drug Info
|
N.A.
|
[2] |
Patent ID |
US20100292266 |
Title |
Oxazolyl Piperidine Modulators of Fatty Acid Amide Hydrolase. |
Applicant(s) |
Apodaca Richard et al |
Patent ID |
US20090111778 |
Title |
2-Keto-Oxazoles As Modulators of Fatty Acid Amide Hydrolase. |
Applicant(s) |
Janssen Pharmaceutica Nv |
Representative Drug(s) |
D0IK9V |
Drug Info
|
IC50 = 0.4 nM |
[2] |