http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-068635-A1
Outgoing Links
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|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_966a6c1f382ec9bcb5e3839dfd73e5b8 |
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| filingDate | 2008-09-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2009-11-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-068635-A1 |
| titleOfInvention | DERIVATIVES OF 1, 1, 1 - TRIFLUOR - 2 - HIDROXI - 3 - PHENYLPROPANE, A METHOD FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS CONTAINING AND THEIR USE IN THE MANUFACTURE OF A MEDICINAL PRODUCT FOR THE TREATMENT OF DISEASES ASSOCIATED WITH THE MODULATION OF RECEPTION GLUCOCORTICOIDS. |
| abstract | The compounds are useful as glucocorticoid receptor antagonists for the treatment and / or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression. In addition, pharmaceutical compositions containing them are provided. Claim 1: Compounds of the general formula (1) wherein A is C-R1b or N; R1a, R1b, R1c, R1d and R1e independently from each other are chosen from the group consisting of hydrogen, C1-7 alkyl, (C3-7 cycloalkyl) -C1-7 alkyl, halogen, halogen-C1-7 alkyl, halogen- C1-7 alkoxy, halogen- (C1-7 alkyl) -sulfonyloxy, hydroxy, hydroxy-C1-7 alkyl, C1-7 alkoxy, (C1-7 alkoxy) -C 1-7 alkoxy, hydroxy-C1-7 alkoxy, amino -C 1-7 alkoxy, cyano, carboxyl, carboxy-C 1-7 alkyl, carboxy-C 1-7 alkoxy, (C 1-7 alkoxy) -carbonyl, (C 1-7 alkoxy) -C 1-7 alkoxycarbonyl, (C 1 alkoxy -7) -C1-7 carbonylamino-alkoxy, (C1-7 alkyl) -carbonyloxy-C1-7 alkoxy, aminocarbonyl-C1-7 alkoxy, di (C1-7 alkyl) -amino, di (C2-7 alkenyl) - amino, (C1-7 alkyl) -sulfonyl-amino, phenylcarbonylamino, phenylsulfonyloxy, heteroaryl-C1-7 alkoxy, said heteroaryl ring is selected from the group consisting of oxadiazolyl, isoxazolyl, thiadiazolyl and tetrazolyl and is unsubstituted or substituted by C1 alkyl -7, phenyloxy and phenyl-C1-7 alkoxy, said phenyl ring is unsubstituted or substituted once, twice or three times by its stituuents chosen from the group consisting of halogen, halogen-C1-7 alkyl, C1-7 alkyl, hydroxy, cyano, (C1-7 alkyl) -sulfonyl, C1-7 alkoxy and halogen-C1-7 alkoxy; or R1c and R1d or R1d and R1e together are -CH = CH-CH = CH- to form a phenyl ring together with the carbon atoms to which they are attached; R2 is selected from the group consisting of C1-7 alkyl, (C3-7 cycloalkyl) -C1-7 alkyl, carboxy-C1-7 alkyl, (C1-7 alkoxy) -carbonyl-C1-7 alkyl, triazolyl-C1 alkyl -7 and phenyl, said phenyl is unsubstituted or substituted by one, two or three halogen groups; R3 is hydrogen or C1-7 alkyl; or R2 and R3 together with the carbon atom to which they are attached form a C3-5 cycloalkyl ring; R4 is a heteroaryl ring selected from the group consisting of pyridyl, pyrazinyl, pyrimidinyl, pyridazinyl, 2-oxo-1,2-dihydropyridinyl, quinolinyl, isoquinolinyl, cinolinyl, pyrazolyl, imidazolyl, thiazolyl, pyrazolo [1,5-a] pyridyl , imidazo [1,2-a] pyridyl, quinoxalinyl, benzothiazolyl, benzotriazolyl, indolyl, indazolyl, 3,4-dihydro-1H-isoquinolinyl and 3,4-dihydro-2H-pyrido [3,2-b] [1, 4] oxazinyl, said heteroaryl ring is unsubstituted or substituted by one, two or three substituents selected from the group consisting of halogen, halogen-C1-7 alkyl, cyano, C1-7 alkyl, (C3-7 cycloalkyl) -C1 alkyl -7, C 1-7 alkoxy, (C 1-7 alkoxy) -C 1-7 alkoxy, C 1-7 alkoxy, C 1-7 hydroxy-alkoxy, halogen-C 1-7 alkoxy carboxyl, carboxy-C 1-7 alkyl, carboxy -C1-7 alkoxy, (C1-7 alkoxy) -carbonyl, (C1-7 alkoxy) -carbonyl-C1-7 alkyl, (C1-7 alkoxy) -carbonyl-C1-7 alkoxy, R6R7N-carbonyl-C1- alkoxy 7, wherein R6 and R7 are independently selected from hydrogen or C1-7 alkyl or R6 and R7 together with the nitrogen atom to which they are attached they form a heterocyclic ring chosen from pyrrolidine, piperidine, morpholine and thiomorpholine, phenyl, said phenyl is unsubstituted or substituted by one, two or three substituents chosen from the group consisting of halogen, halogen- C1-7 alkyl, C1-7 alkyl, hydroxy, cyano, carboxyl, (C1-7 alkoxy) -carbonyl and C1-7 alkoxy; pyridyl, heterocyclyl selected from the group consisting of pyrrolidine and piperidine, said heterocyclyl ring is unsubstituted or substituted by carboxyl or (C1-7 alkoxy) -carbonyl, phenyl-C1-7 alkyl, phenyloxy and phenyl-C1-7 alkoxy; R5 is hydrogen or methyl; n is the number 0 or 1; and its pharmaceutically acceptable salts. Claim 21: A process for obtaining the compounds of the formula (1) according to any one of claims 1 to 20, said process consists in: treating a compound of the formula (2) in which A, n, from R1a to R1e , R2, R3 and R4 have the meanings defined above, with trifluoromethyltrimethylsilane and a suitable fluoride to obtain a compound of the formula (3), in which R5 is hydrogen, and, if desired, rent the compound of the formula (3 ) with a methyl iodide in the presence of a base, for example NaH, obtaining a compound of the formula (4), in which R5 is methyl, and, if desired, converting the compound obtained into a pharmaceutically acceptable salt. |
| priorityDate | 2007-09-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 64.