| Patent(s) and the Corresponding Patented Drug(s) |
Top |
| World Intellectual Property Organization (WIPO) |
| Patent ID |
WO2014023643 |
| Title |
Multitarget Faah and Cox Inhibitors and Therapeutical Uses Thereof. |
| Abstract |
The invention provides novel multitarget inhibitors of the enzymes Fatty Acid Amide Hydrolase (FAAH), Cyclooxygenase-1 (COX-1) and/or Cyclooxygenase-2 (COX-2) having a specific carbamate moiety on the meta or ortho position of the A ring of a substituted biphenyl core and having an halogen in the ortho position of the B ring of the biphenyl core. The invention concerns also with therapeutical application of the multitarget inhibitors in particular in the prevention and treatment of cancer. |
| Applicant(s) |
Fondazione Istituto Italiano Di Tecnologia |
| Representative Drug(s) |
D0S8TB |
Drug Info
|
IC50 = 31 nM |
[1] |
| 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 = 320 nM |
[1] |
| Patent ID |
WO2011060026 |
| Title |
Piperazinecarboxamide Derivative Useful As A Modulator of Fatty Acid Amide Hydrolase (Faah). |
| Abstract |
N-Pyridin-3-yl-4-{3-[4-(trifluoromethyl)phenoxy]benzyl}piperazine-1- carboxamide is described, which is useful as a FAAH inhibitor. N-Pyridin-3-yl- 4-{3-[4-(trifluoromethyl)phenoxy]benzyl}piperazine-1-carboxamide 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 N-pyridin-3-yl-4-{3-[4- (trifluoromethyl)phenoxy]benzyl}piperazine-1 -carboxamide is also disclosed. |
| Applicant(s) |
Jansen Pharmaceutica Nv Hawryluk, Natalie, A |
| Representative Drug(s) |
D00ZCD |
Drug Info
|
IC50 = 18 nM |
[1] |
| 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 = 60 nM |
[1] |
| Patent ID |
WO2010130945 |
| Title |
7-Aza-Spiro[3.5]Nonane-7-Carboxylate Derivatives, Preparation Thereof, and Therapeutic Use Thereof. |
| Abstract |
The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m, n, o and p independently are a number from 0 to 3, provided that m+n 7 and that o+p 7; A is a covalent bond, an oxygen atom, a C1-6-alkylene group or a -O-C1-6-alkylene group in which the end that is an oxygen atom is bonded to the R1 group and the end that is an alkylene group is bonded to the carbon of the bicyclic compound; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl or trifluoromethyl group; R4 is an optionally substituted 5-membered heterocyclic compounds; wherein the compounds can be in the state of a base or an acid addition salt. The invention can be used in therapeutics. |
| Applicant(s) |
Sanofi |
| Representative Drug(s) |
D0I6VK |
Drug Info
|
IC50 = 0.46 nM |
[1] |
| Patent ID |
WO2010055267 |
| Title |
Carbamate Derivatives of Alkyl-Heterocycles, Preparation Thereof and Therapeutic Use Thereof. |
| Abstract |
Compound corresponding to general formula (I): in which R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6- alkoxy or NR8R9 group; n is an integer equal to 1, 2 or 3 and m is an integer equal to 1 or 2; A is a covalent bond or a C1-8-alkylene group; R1 is a phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, naphthyl, quinolinyl, isoquinolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, cinnolinyl or naphthyridinyl group, this group being optionally substituted; R3 is a hydrogen or fluorine atom, a C1-6-alkyl group or a trifluoromethyl group; R4 is a group selected from furanyl, pyrrolyl, thienyl, isothiazolyl, oxazolyl, isoxazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, imidazole, triazolyl, tetrazolyl, oxazolone, oxazolidinone, isoxazolone, isoxazolidinone, isothiazolone, isothiazolidinone, imidazolone, imidazolidinone, pyrazolone, pyrazolidinone, oxadiazolone, thiadiazolone and triazolone, this group being optionally substituted; in the form of a base or of an addition salt with an acid. Therapeutic use. |
| Applicant(s) |
Sanofi-Aventis |
| Patent ID |
WO2010010288 |
| Title |
Alkyl Thiazole Carbamate Derivatives, Preparation Thereof, and Use Thereof As Faah Enzyme Inhibitors. |
| Abstract |
Compound of general formula (I), in which R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or NR8R9 group, n is an integer equal to 1, 2 or 3, and m is an integer equal to 1 or 2, A is a covalent bond or a C1-8-alkylene group; R1 is an optionally substituted aryl or heteroaryl group, R3 is a hydrogen or fluorine atom, a C1-6-alkyl group or a trifluoromethyl group, and R4 is an optionally substituted thiazole, in the form of a base or of an acid addition salt. Therapeutic use. |
| Applicant(s) |
Sanofi-Aventis |
| Patent ID |
WO2009138416 |
| Title |
Oxime Carbamoyl Derivatives As Modulators of Fatty Acid Amides Hydrolase. |
| Abstract |
The present invention relates to new oxime carbamoyl 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) |
D0C3OH |
Drug Info
|
IC50 < 10 nM |
[1] |
| 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 = 3 nM |
[1] |
| 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
|
IC50 < 100 nM |
[1] |
