http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-043355-A1
Outgoing Links
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| filingDate | 2004-01-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2005-07-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-043355-A1 |
| titleOfInvention | COMPOUNDS DERIVED FROM AMIDA, PREPARATION OF DRUGS THAT CONTAIN THEM FOR THE TREATMENT AND PREVENTION OF DISORDERS ASSOCIATED WITH GLUCOCORTICOIDS |
| abstract | Esulin in muscle and adipose tissue, and reduce lipolysis and the production of free fatty acids in adipose tissue, also reduce the concentration of hepatic glucocorticoid in mammals, in particular, the concentration of hepatic cortisol in humans, resulting in the inhibition of hepatic gluconeogenesis and the reduction of plasma glucose levels. In this way, they can be particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions where hyperglycermia and / or insulin resistance, such as type 2 diabetes, are involved, and can also be used to treat other disorders associated with glucocorticoids. , such as syndrome X, dyslipidemia, hypertension and central obesity. In addition, being refers to the use of these compounds for the preparation of medicaments, in particular useful medicaments for the treatment and prevention of disorders associated with glucocorticoid, improving insulin sensitivity, reducing plasma glucose levels, reducing lipolysis and production of free fatty acids, and decreasing the formation of visceral adipose tissue. Claim 1: A compound according to formula (1), wherein: R1 and R2 are independently hydrogen, cyano, halogen, nitro, trifluoromethyl, optionally substituted amino, alkyl, alkoxy, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; or r1 and R2 combined together the carbon atoms to which they are attached form an optionally substituted 5- to 7-membered aromatic or heteroaromatic ring; R3 is optionally substituted lower alkyl; or R3 and R2 combined together with the amide group to which R3 is attached and the carbon atoms to which R2 and the amide are attached form an optionally substituted 5- to 7-membered carbocyclic or heterocyclic ring; R4 is optionally substituted alkyl, cycloalkyl, heterocyclic, aryl, arylalkyl or heteroarylalkyl; or R4 and R3 taken together with the atom to which they are attached form a 5 to 8 member ring, which may be optionally substituted or may contain another heterogeneous atom selected from oxygen, nitrogen and sulfur; or R4 and R3 taken together with the nitrogen atom to which they are attached form a fused bicyclic ring of 8 to 12 members, which may optionally be substituted or may contain another heterogeneous atom selected from oxygen, nitrogen and sulfur; W is -NR5C (O) R6, -NR5C (O) OR6, -NR5C (O) NR6R7, -NR5C (S) NR6R7, -NR5S (O) 2R6, -NR5R8, -C (O) NR6R7, -OR9 or -OC (O) NR6R7, wherein: R5 and R7 are independently hydrogen, optionally substituted alkyl or aralkyl; or R5 and R1 are optionally substituted alkylene which combined with the nitrogen atom to which R5 is attached and the carbon atoms to which W and R1 are attached form a 5 or 6 membered ring; R6 is optionally substituted alkyl, cycloalkyl, heterocyclyl, aryl, aralkyl or heteroaralkyl; R8 is optionally substituted alkyl, aralkyl or heteroaralkyl; R9 is hydrogen, optionally substituted alkyl, cycloalkyl, heterocyclyl, heterocycloalkyl, aralkyl, heteroaralkyl, alkanoyl, aroyl or heteroaroyl; or W is aryl or heteroaryl; or W is hydrogen provided that R1 is -NR5Z, where Z is -C (O) R6, -C (O) OR6, -C (O) NR6R7, -C (S) NR6R7, -S (O) R6, or R8; or W and R1 combined together the carbon atoms to which they are attached form a 6-membered aromatic or heteroaromatic ring optionally substituted with alkyl, alkoxy, aryl, heteroaryl, halogen, -NR5Z, -C (O) NR6R7, -OR9 or -OC (O) NR6R7; X and Y are independently CH or nitrogen; or -X = Y is -CH2-, oxygen, sulfur or -NR10-, wherein R10 is hydrogen or lower alkyl; or a pharmaceutically acceptable salt thereof. |
| priorityDate | 2003-01-24-04:00^^<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: 171.