公开(公告)号：WO2007027651A2

公开(公告)日：2007-03-08

申请号：PCT/US2006033620

申请日：2006-08-25

Applicant: ABBOTT LAB ,  PEI ZHONGHUA ,  VON GELDERN THOMAS ,  MADAR DAVID J ,  LI XIAOFENG ,  BASHA FATIMA ,  YONG HONG ,  LONGENECKER KENTON L ,  BACKES BRADLEY J ,  JUDD ANDREW S ,  MULHERN MATHEW M ,  STEWART KENT D

Inventor： PEI ZHONGHUA ,  VON GELDERN THOMAS ,  MADAR DAVID J ,  LI XIAOFENG ,  BASHA FATIMA ,  YONG HONG ,  LONGENECKER KENTON L ,  BACKES BRADLEY J ,  JUDD ANDREW S ,  MULHERN MATHEW M ,  STEWART KENT D

IPC: C07C217/54 ,  C07C211/40 ,  C07D213/38 ,  C07D213/68 ,  C07D317/64

CPC classification number: C07C211/48 ,  C07C211/40 ,  C07C217/52 ,  C07C217/54 ,  C07C217/74 ,  C07C217/84 ,  C07C217/86 ,  C07C225/22 ,  C07C229/42 ,  C07C229/48 ,  C07C229/60 ,  C07C233/43 ,  C07C233/78 ,  C07C235/46 ,  C07C237/24 ,  C07C237/30 ,  C07C237/42 ,  C07C255/54 ,  C07C255/58 ,  C07C311/22 ,  C07C311/36 ,  C07C317/22 ,  C07C317/36 ,  C07C2601/14 ,  C07C2601/16 ,  C07D207/16 ,  C07D209/08 ,  C07D209/48 ,  C07D211/46 ,  C07D211/60 ,  C07D211/62 ,  C07D213/30 ,  C07D213/38 ,  C07D213/64 ,  C07D213/68 ,  C07D213/74 ,  C07D213/82 ,  C07D217/04 ,  C07D263/56 ,  C07D263/60 ,  C07D277/04 ,  C07D277/64 ,  C07D295/135 ,  C07D295/185 ,  C07D295/205 ,  C07D317/66 ,  C07D319/18 ,  C07D333/34 ,  C07D333/38 ,  C07D409/04 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention relates to compounds, which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, metabolic syndrome , hyperinsulinemia, obesity, atherosclerosis, various immunomodulatory diseases, and other diseases.

Abstract translation: 本发明涉及抑制二肽基肽酶IV（DPP-IV）的化合物，其可用于预防或治疗糖尿病，特别是II型糖尿病，以及高血糖症，代谢综合征，高胰岛素血症，肥胖症，动脉粥样硬化，各种免疫调节疾病 ，等疾病。

公开(公告)号：WO1990015056A1

公开(公告)日：1990-12-13

申请号：PCT/US1990002864

申请日：1990-05-22

Applicant: ABBOTT LABORATORIES ,  SCHOENLEBER, Robert, W. ,  KEBABIAN, John, W. ,  MARTIN, Yvonne, C. ,  DeNINNO, Michael, P. ,  PERNER, Richard, J. ,  STOUT, David, M. ,  HSIAO, Chi-Nung, W. ,  DiDOMENICO, Stanley, Jr. ,  DeBERNARDIS, John, F. ,  BASHA, Fatima, Z. ,  MEYER, Micheal, D. ,  DE, Biswanath ,  EHRLICH, Paul, P. ,  CAMPBELL, James, R. ,  MORTON, Howard, E. ,  LIJEWSKI, Linda, M.

Inventor： ABBOTT LABORATORIES

IPC: C07D409/04

CPC classification number: C07D207/08 ,  A61K38/00 ,  C07C215/64 ,  C07C217/74 ,  C07C219/28 ,  C07C233/18 ,  C07C237/08 ,  C07C271/16 ,  C07C271/44 ,  C07C309/65 ,  C07C323/60 ,  C07C2601/14 ,  C07C2602/10 ,  C07C2602/28 ,  C07C2603/28 ,  C07C2603/74 ,  C07C2603/93 ,  C07D209/62 ,  C07D221/10 ,  C07D221/20 ,  C07D311/76 ,  C07D311/78 ,  C07D311/96 ,  C07D313/08 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D407/04 ,  C07D407/12 ,  C07D493/10 ,  C07K5/06026

Abstract: Novel compounds are provided of formula (I), or a pharmaceutically acceptable salt, ester or amide thereof, wherein A is O, S, CHR2, CR2 or C when n is 0 and A and R6 taken together form a nitrogen-containing 5-, 6- or 7-membered ring, and n is zero or 1. The dotted lines represent optional double bonds. R1 is selected from hydrogen and a readily cleavable group. R2 is selected from hydrogen, alkyl, substituted alkyl, alkenyl and alkynyl. R3 is selected from alkyl, substituted alkyl, alkenyl, alkynyl, cycloalkyl, carbocyclic aryl, carbocyclic arylalkyl and heterocycle. R4 is selected from hydrogen and alkyl or, taken together with R3 and the carbon atom to which they are attached, forms a spirocycloalkyl ring of from 3 to 7 carbons. R5 is selected from hydrogen, alkyl and substituted alkyl or, taken together with R3 and the carbon atoms to which they are attached forms a cycloalkyl ring of from 5 to 7 carbons. R6 is selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, carbocyclic arylalkyl, alkanoyl of from 1 to 8 carbons, amino acid and dipeptide or, taken together with A when A is C and when n is 0, forms a nitrogen-containing 5-, 6-, or 7-membered ring. R7 is hydrogen or alkyl or, taken together with R6 or R8, forms a nitrogen-containing 5-, 6- or 7-membered ring, provided that when R6 is carbocyclic arylalkyl, R7 is not alkyl. R8 is hydrogen or alkyl or, taken together with R6 or R7, forms a nitrogen-containing 5-, 6-, or 7-membered ring or, taken together with the catechol ring at the 8-position and the carbon atoms to which they are attached, forms a 5-, 6- or 7-membered ring. The compounds of the invention are useful for treating dopamine-related neurological, psychological and cardiovascular disorders as well as in the treatment of cognitive impairment, attention deficit disorder, and substance abuse and other addictive behavior disorders.

公开(公告)号：WO1989006645A1

公开(公告)日：1989-07-27

申请号：PCT/US1989000140

申请日：1989-01-13

Applicant: ABBOTT LABORATORIES ,  DEBERNARDIS, John, Francis ,  ZELLE, Robert, Edward ,  BASHA, Fatima, Zehra

Inventor： ABBOTT LABORATORIES

IPC: C07C91/28

CPC classification number: C07D207/08 ,  C07C45/004 ,  C07C45/46 ,  C07C45/63 ,  C07C45/71 ,  C07C49/577 ,  C07C49/697 ,  C07C49/747 ,  C07C49/753 ,  C07C62/32 ,  C07C62/34 ,  C07C211/30 ,  C07C215/50 ,  C07C217/74 ,  C07C229/50 ,  C07C233/18 ,  C07C255/47 ,  C07C259/08 ,  C07C323/22 ,  C07C2601/08 ,  C07C2602/10 ,  C07D207/06 ,  C07D207/335 ,  C07D213/38 ,  C07D307/52 ,  C07D317/70 ,  C07D319/20 ,  C07D319/22 ,  C07D333/20 ,  C07D333/24 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07C49/755

Abstract: The present invention includes compounds represented by formula (I), wherein n is 0 or 1; R1, R2, R3 and R4 are independently selected from hydrogen, hydroxyl, amino, alkylamino, alkylsulfonylamino, loweralkyl, loweralkoxy, halo, and thioalkoxy; R1 and R2 or R2 and R3 taken together can form a methylenedioxy or ethylenedioxy bridge; R10 is independently selected from hydrogen, loweralkyl, phenyl, and substituted phenyl; R5 is loweralkyl; R9 is hydrogen or loweralkyl; R6 and R8 are hydrogen; and R7 is (II), wherein m is 0, 1 or 2; X is CH2, O, S or N-CH3; or R7 is (III), wherein s is 0, 1, or 2; Z is C or N; R11 and R12 are independently selected from hydrogen, halo, hydroxy, methoxy, thiomethoxy, amino and loweralkyl, or R11 and R12 taken together can form a methylenedioxy or ethylenedioxy bridge; or R7 is (IV), wherein t is 0 or 1; or R5 and R9 taken together form a pyrrolidine ring and then R6 and R8 are hydrogen and R7 is as described above; or R5 and R9 taken together form a pyrrolidine ring and then R6 is hydrogen and R7 and R8 taken together may form a phenyl, substituted phenyl, thienyl or furyl ring; or R5 and R8 taken together form a pyrrolidine ring and then R9 and R6 are hydrogen and R7 is phenyl, substituted phenyl, thienyl, or furyl; or R7 and R9 are hydrogen and R6 is benzyl, substituted benzyl, thienylmethyl, or furylmethyl; or a pharmaceutically acceptable salt thereof.

公开(公告)号：WO2007027651A3

公开(公告)日：2007-03-08

申请号：PCT/US2006/033620

申请日：2006-08-25

Applicant: ABBOTT LABORATORIES ,  PEI, Zhonghua ,  VON GELDERN, Thomas ,  MADAR, David, J. ,  LI, Xiaofeng ,  BASHA, Fatima ,  YONG, Hong ,  LONGENECKER, Kenton, L. ,  BACKES, Bradley, J. ,  JUDD, Andrew, S. ,  MULHERN, Mathew, M. ,  STEWART, Kent, D.

Inventor： PEI, Zhonghua ,  VON GELDERN, Thomas ,  MADAR, David, J. ,  LI, Xiaofeng ,  BASHA, Fatima ,  YONG, Hong ,  LONGENECKER, Kenton, L. ,  BACKES, Bradley, J. ,  JUDD, Andrew, S. ,  MULHERN, Mathew, M. ,  STEWART, Kent, D.

IPC: C07C211/40 ,  C07C211/54 ,  C07C211/62 ,  C07D213/38 ,  C07D213/68 ,  C07D317/64 ,  C07D487/04 ,  A61K31/137

Abstract: The present invention relates to compounds, which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, metabolic syndrome , hyperinsulinemia, obesity, atherosclerosis, various immunomodulatory diseases, and other diseases.

公开(公告)号：CA2050723A1

公开(公告)日：1992-03-11

申请号：CA2050723

申请日：1991-09-05

Applicant: WINN MARTIN ,  BISWANATH DE ,  ZYDOWSKY THOMAS M ,  KERKMAN DANIEL J ,  DEBERNARDIS JOHN F ,  ROSENBERG SAUL H ,  SHIOSAKI KAZUMI ,  BASHA FATIMA Z ,  TASKER ANDREW S ,  VON GELDERN THOMAS W ,  KESTER JEFFREY A ,  HOLLEMAN WILLIAM H

Inventor： WINN MARTIN ,  DE BISWANATH ,  ZYDOWSKY THOMAS M ,  KERKMAN DANIEL J ,  DEBERNARDIS JOHN F ,  ROSENBERG SAUL H ,  SHIOSAKI KAZUMI ,  BASHA FATIMA Z ,  TASKER ANDREW S ,  VON GELDERN THOMAS W ,  KESTER JEFFREY A ,  HOLLEMAN WILLIAM H

IPC: A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/495 ,  A61K31/50 ,  A61K31/505 ,  A61K31/53 ,  A61P1/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P27/02 ,  A61P43/00 ,  C07D213/64 ,  C07D213/70 ,  C07D213/71 ,  C07D213/72 ,  C07D213/74 ,  C07D213/80 ,  C07D239/26 ,  C07D239/34 ,  C07D239/42 ,  C07D257/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

Abstract: Novel pyrimidine, pyridine, pyridazine, pyrazine and triazine compounds are provided of the formula (I). (I) The compounds of the invention are useful for treating hypertension, edema, renal failure, congestive heart failure, psoriasis and glaucoma, and in the prevention and treatment of atherosclerosis or to treat gastrointestinal disorders associated with enhanced contractility and/or motility of intestinal smooth muscle or to treat contractile disorders of the uterus.