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Organic compounds

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Organic compounds


Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy. Finally, the present invention also provides a pharmaceutical composition. The present invention provides a compound of formula I:
Related Terms: Aldosterone Endometrial

Inventors: Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
USPTO Applicaton #: #20120277215 - Class: 51421402 (USPTO) - 11/01/12 - Class 514 
Drug, Bio-affecting And Body Treating Compositions > Designated Organic Active Ingredient Containing (doai) >Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai >Hetero Ring Is Seven-membered Consisting Of One Nitrogen And Six Carbons >Polycyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos >Ring Nitrogen Of The Seven-membered Hetero Ring Is Shared By An Additional Cyclo Of The Polycyclo Ring System >Plural Ring Nitrogens In The Polycyclo Ring System

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The Patent Description & Claims data below is from USPTO Patent Application 20120277215, Organic compounds.

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The present invention relates to novel imidazole derivatives that are used as aldosterone synthase and aromatase inhibitors, as well as for treatment of a disorder or disease mediated by aldosterone synthase or aromatase.

The present invention provides a compound of formula (I)

wherein n is 1, or 2, or 3; R is hydrogen, (C1-C7) alkyl, or (C1-C7) alkenyl, said (C1-C7) alkyl and (C1-C7) alkenyl being optionally substituted by one to five substituents independently selected from the group consisting of —O—R8 and —N(R8)(R9), wherein R8 and R9 are independently selected from the group consisting of hydrogen, (C1-C7) alkyl, acyl, aryl and heteroaryl, each of which is further optionally substituted by one to four substituents independently selected from the group consisting of halo, (C1-C7) alkoxy and (C1-C7) alkyl; or R is —C(O)O—R10, or —C(O)N(R11)(R12), wherein R10, R11 and R12 are selected independently from the group consisting of hydrogen, (C1-C7) alkyl, (C3-C8) cycloalkyl, aryl, aryl-(C1-C7) alkyl, (C1-C7) haloalkyl and heteroaryl, each of which is further optionally substituted by one to four substituents independently selected from the group consisting of halo, hydroxyl, (C1-C7) alkoxy, (C1-C7) alkyl, and aryl, wherein R11 and R12 taken together with the nitrogen atom to which they are attached optionally form a 3-8-membered ring; R1, R2, R3, R4, and R5 are selected independently from the group consisting of hydrogen, (C1-C7) alkenyl, (C1-C7) alkyl, (C3-C8) cycloalkyl, halo, cyano, nitro, H2N—, (C1-C7) haloalkyl, (C1-C7) alkoxy, (C3-C8) cycloalkoxy, aryloxy, aryl, heretoaryl, —C(O)OR10, and —N(R13)(R14), said (C1-C7) alkyl, (C1-C7) alkenyl, (C1-C7) alkoxy, aryl and heteroaryl being further optionally substituted by one to three substituents selected from (C1-C7) alkyl, hydroxyl, halo, (C1-C7) alkoxy, nitro, cyano, (C1-C7) dialkylamino, (C1-C7) alkoxy-(C1-C7) alkyl-, and (C1-C7) haloalkyl, said R10 having the same meanings as defined above, said R13 and R14 are independently selected from the group consisting of hydrogen, (C1-C7) alkyl, (C3-C8) cycloalkyl, (C1-C7) haloalkyl, (C1-C7) haloalkoxy, aryl and cyano, with the proviso that no more than three of R1, R2, R3, R4, and R5 are simultaneously hydrogen; R13 and R14 taken together with the nitrogen atom to which they are attached optionally form a 3-8-membered ring; R and R1 taken together optionally form a 5-6-membered ring containing 0 or 1 heteroatom selected from O, N, or S; R6 and R7 are independently hydrogen, hydroxyl, (C1-C7) alkyl, (C1-C7) alkoxy, phenyl, or benzyl, wherein phenyl and benzyl are optionally substituted by one to four substituents independently selected from the group consisting of halo, (C1-C7) alkoxy and (C1-C7) alkyl; when R6 and R7 are attached to the same carbon atom, they optionally form a moiety (A) represented by the following structure:



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stats Patent Info
Application #
US 20120277215 A1
Publish Date
11/01/2012
Document #
13540113
File Date
07/02/2012
USPTO Class
51421402
Other USPTO Classes
5483027, 514393, 544139, 5142332, 546199, 514322, 5483011, 546121, 514300, 540579
International Class
/
Drawings
0


Aldosterone
Endometrial


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