- AZAINDOLE INHIBITORS OF IAP
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The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: I wherein X1, X2, Y, Z1, Z2, Z3, Z4, R1, R2, R3, R3', R4, R4', R5, R6, R6' and R9 are as described herein.
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Page/Page column 39
(2010/04/03)
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- INHIBITORS OF IAP
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The invention provides novel compounds that are inhibitors of IAPs having the general formula: wherein X1, X2, X3, Y, A, R1, R2, R3, R4, R4', R5, R5'/
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Page/Page column 43
(2010/04/03)
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- IMIDAZOPYRIDINE INHIBITORS OF IAP
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The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein Q, X1, X2, Y, Z R1, R2, R3, R3', R4, R4', R5, R6, R6' and n are as described herein.
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- INHIBITORS OF IAP
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The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds having the general formula U1 - M - U2 wherein M is a linking group covalently joining R2, R3, R4 or R5 of U1 to an R2, R3, R4 or R5 group of U2; U1 and U2 have the general formula (I) and G, X1, X2, R2, R3, R3', R4, R4' and R5, are as described herein.
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Page/Page column 72
(2008/12/08)
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- INHIBITORS OF IAP
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The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula (I): wherein Q, X1, X2, Y, Z1, Z2, Z3, Z4, R1, R2, R3, R3', R4, R4', R5, R6, R6' and n are as described herein.
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Page/Page column 48; 49
(2008/06/13)
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- ALPHA-AMINO ACID DERIVATIVES AND USE THEREOF AS MEDICINES
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Compounds represented by the α-amino acid derivative or a pharmaceutically acceptable salt thereof of the present invention have a therapeutic effect due to a DPP-IV inhibitory action and useful as pharmaceutical agents for the treatment and/or prophylaxi
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Page/Page column 17-18
(2008/06/13)
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- Dipeptidyl peptidase-IV inhibitors
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The invention provides compounds of Formula (I) or prodrugs thereof, or pharmaceutically acceptable salts of said compounds or prodrugs, or solvates of said compounds, prodrugs or salts, wherein A, N, X and R1 are as defined herein; pharmaceutical compositions thereof; and methods of using the pharmaceutical compositions for the treatment of diseases, including Type 2 diabetes, Type 1 diabetes, impaired glucose tolerance, hyperglycemia, metabolic syndrome (syndrome X and/or insulin resistance syndrome), glucosuria, metabolic acidosis, arthritis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, obesity, conditions exacerbated by obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, short stature due to growth hormone deficiency, infertility due to polycystic ovary syndrome, anxiety, depression, insomnia, chronic fatigue, epilepsy, eating disorders, chronic pain, alcohol addiction, diseases associated with intestinal motility, ulcers, irritable bowel syndrome, inflammatory bowel syndrome; short bowel syndrome; and the prevention of disease progression in Type 2 diabetes.
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Page/Page column 24
(2010/02/14)
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- Heterocycle fused cyclohexylglycine derivatives as novel dipeptidyl peptidase-IV inhibitors
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A new class of potent inhibitors of dipeptidyl peptidase IV (DP-IV) for the treatment of type II diabetes are described. Presented herein is the synthesis of indole-fused and thiazole-fused cyclohexylglycines. Pyrrolidine-derived amides of these novel heterocycles led to the discovery of thiazole derivatives (3f) and (11a), both low nanomolar inhibitors of DP-IV (IC50 = 6 nM).
- Mastracchio, Anthony,Parmee, Emma R.,Leiting, Barbara,Marsilio, Frank,Patel, Reshma,Thornberry, Nancy A.,Weber, Ann E.,Edmondson, Scott D.
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p. 203 - 206
(2007/10/03)
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- FUSED INDOLES AS DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
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The present invention is directed to fused indole derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is in
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