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1. 发明专利

DE60010855D1 未知
公开(公告)号：DE60010855D1
公开(公告)日：2004-06-24
申请号：DE60010855
申请日：2000-01-11
申请人： MERCK SHARP & DOHME
发明人： BLURTON PETER , BURKAMP FRANK , CHENG KOON-FUNG , FLETCHER ROBERT , MACLEOD MURRAY , VAN NIEL BODIL , SPINKS DANIEL
IPC分类号： A61K31/445 , A61K31/454 , A61P1/14 , A61P25/00 , A61P25/04 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/30 , A61P27/06 , A61P43/00 , C07D211/54 , C07D401/10 , C07D401/12 , C07D521/00
摘要： A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted azetidine, pyrrolidine or piperidine ring are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and depression.

2. 发明专利

DE69807074T2 未知
公开(公告)号：DE69807074T2
公开(公告)日：2003-04-03
申请号：DE69807074
申请日：1998-05-06
申请人： MERCK SHARP & DOHME
发明人： CARLING ROBERT , LADDUWAHETTY TAMARA , MACLEOD MURRAY , MERCHANT JOHN , MOORE WILLIAM , STERNFELD FRANCINE , STREET JOSEPH
IPC分类号： A61K31/5025 , A61P25/28 , A61P43/00 , C07D487/04 , A61K31/50
摘要： Substituted 1,2,4-Triazolo[3,4-A]phthalazine derivatives are GABA Alpha 5 ligands and are represented by the formula

3. 发明专利

DE69428913T2 未知
公开(公告)号：DE69428913T2
公开(公告)日：2002-05-29
申请号：DE69428913
申请日：1994-12-23
申请人： MERCK SHARP & DOHME
发明人： BAKER RAYMOND , HARRISON TIMOTHY , MACLEOD MURRAY , OWENS PATE , SEWARD MARY , SWAIN JOHN , TEALL RICHARD
IPC分类号： C07D487/08 , A61K31/535 , A61K31/5377 , A61K31/541 , A61P1/08 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/28 , A61P29/00 , A61P43/00 , C07D413/06 , C07D413/14 , C07D417/14 , C07F9/6533 , C07F9/6558
摘要： The present invention relates to compounds of the formula (I): wherein R is hydrogen, halogen, C1-6alkyl, C1-6alkoxy, CF3, NO2, CN, SR , SOR , SO2R , CO2R , CONR R , C2-6alkenyl, C2-6alkynyl or C1-4alkyl substituted by C1-4alkoxy, where R and R are hydrogen or C1-4alkyl; R is hydrogen, halogen, C1-6alkyl, C1-6alkoxy substituted by C1-4alkoxy or CF3; R is hydrogen, halogen or CF3; R is selected from the definitions of R ; R is selected from the definitions of R ; R is a 5-membered or 6-membered heterocyclic ring containing 2 or 3 nitrogen atoms optionally substituted by =O or =S and optionally substituted by an aminoalkyl group; R and R are hydrogen or C1-4alkyl, or R and R are joined to form a C5-7 ring; X is C1-4alkylene optionally substituted by oxo; and Y is a C1-4alkyl group substituted by hydroxyl; and pharmaceutically acceptable salts and prodrugs thereof. The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.

4. 发明专利

DE69807074D1 未知
公开(公告)号：DE69807074D1
公开(公告)日：2002-09-12
申请号：DE69807074
申请日：1998-05-06
申请人： MERCK SHARP & DOHME
发明人： CARLING ROBERT , LADDUWAHETTY TAMARA , MACLEOD MURRAY , MERCHANT JOHN , MOORE WILLIAM , STERNFELD FRANCINE , STREET JOSEPH
IPC分类号： A61K31/5025 , A61P25/28 , A61P43/00 , C07D487/04 , A61K31/50
摘要： Substituted 1,2,4-Triazolo[3,4-A]phthalazine derivatives are GABA Alpha 5 ligands and are represented by the formula

5. 发明专利

DE69709950D1 未知
公开(公告)号：DE69709950D1
公开(公告)日：2002-02-28
申请号：DE69709950
申请日：1997-10-28
申请人： MERCK SHARP & DOHME
发明人： BROUGHTON BARFF , CHAMBERS STUART , HOBBS CHRISTINE , MACLEOD MURRAY , REEVE JOHN
IPC分类号： A61K31/381 , A61K31/4025 , A61K31/41 , A61K31/4155 , A61K31/4178 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/4436 , A61K31/4439 , A61K31/496 , A61K31/497 , A61K31/506 , A61P25/22 , A61P25/26 , A61P25/28 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04 , C07D417/14 , A61K31/38
摘要： A pharamceutical composition comprises a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein A is C1-6alkyl, C2-6alkenyl, C2-6-alkynyl, C3-6-cycloalkyl, arylC1-6alkyl, aryl, S(O)pR1.

6. 发明专利

DE60010855T2 未知
公开(公告)号：DE60010855T2
公开(公告)日：2005-06-16
申请号：DE60010855
申请日：2000-01-11
申请人： MERCK SHARP & DOHME
发明人： BLURTON PETER , BURKAMP FRANK , CHENG KOON-FUNG , FLETCHER ROBERT , MACLEOD MURRAY , VAN NIEL BODIL , SPINKS DANIEL
IPC分类号： A61K31/445 , A61K31/454 , A61P1/14 , A61P25/00 , A61P25/04 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/30 , A61P27/06 , A61P43/00 , C07D211/54 , C07D401/10 , C07D401/12 , C07D521/00
摘要： A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted azetidine, pyrrolidine or piperidine ring are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and depression.

7. 发明专利

DE69709950T2 未知
公开(公告)号：DE69709950T2
公开(公告)日：2002-08-29
申请号：DE69709950
申请日：1997-10-28
申请人： MERCK SHARP & DOHME
发明人： BROUGHTON BARFF , CHAMBERS STUART , HOBBS CHRISTINE , MACLEOD MURRAY , REEVE JOHN
IPC分类号： A61K31/381 , A61K31/4025 , A61K31/41 , A61K31/4155 , A61K31/4178 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/4436 , A61K31/4439 , A61K31/496 , A61K31/497 , A61K31/506 , A61P25/22 , A61P25/26 , A61P25/28 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04 , C07D417/14 , A61K31/38
摘要： A pharamceutical composition comprises a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein A is C1-6alkyl, C2-6alkenyl, C2-6-alkynyl, C3-6-cycloalkyl, arylC1-6alkyl, aryl, S(O)pR1.

8. 发明专利

DE69428913D1 未知
公开(公告)号：DE69428913D1
公开(公告)日：2001-12-06
申请号：DE69428913
申请日：1994-12-23
申请人： MERCK SHARP & DOHME
发明人： BAKER RAYMOND , HARRISON TIMOTHY , MACLEOD MURRAY , OWENS PATE , SEWARD MARY , SWAIN JOHN , TEALL RICHARD
IPC分类号： C07D487/08 , A61K31/535 , A61K31/5377 , A61K31/541 , A61P1/08 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/28 , A61P29/00 , A61P43/00 , C07D413/06 , C07D413/14 , C07D417/14 , C07F9/6533 , C07F9/6558
摘要： The present invention relates to compounds of the formula (I): wherein R is hydrogen, halogen, C1-6alkyl, C1-6alkoxy, CF3, NO2, CN, SR , SOR , SO2R , CO2R , CONR R , C2-6alkenyl, C2-6alkynyl or C1-4alkyl substituted by C1-4alkoxy, where R and R are hydrogen or C1-4alkyl; R is hydrogen, halogen, C1-6alkyl, C1-6alkoxy substituted by C1-4alkoxy or CF3; R is hydrogen, halogen or CF3; R is selected from the definitions of R ; R is selected from the definitions of R ; R is a 5-membered or 6-membered heterocyclic ring containing 2 or 3 nitrogen atoms optionally substituted by =O or =S and optionally substituted by an aminoalkyl group; R and R are hydrogen or C1-4alkyl, or R and R are joined to form a C5-7 ring; X is C1-4alkylene optionally substituted by oxo; and Y is a C1-4alkyl group substituted by hydroxyl; and pharmaceutically acceptable salts and prodrugs thereof. The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.

9. 发明专利

DE69516853T2 未知
公开(公告)号：DE69516853T2
公开(公告)日：2000-11-16
申请号：DE69516853
申请日：1995-02-06
申请人： MERCK SHARP & DOHME
发明人： BAKER RAYMOND , MACLEOD MURRAY , SEWARD MARY , SWAIN JOHN
IPC分类号： A61K31/4427 , A61K31/445 , A61K31/451 , A61P1/00 , A61P1/08 , A61P9/00 , A61P11/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P29/00 , A61P35/02 , A61P37/00 , A61P37/08 , A61P43/00 , C07D211/42 , C07D211/54 , C07D401/06
摘要： PCT No. PCT/GB95/00228 Sec. 371 Date Sep. 26, 1996 Sec. 102(e) Date Sep. 26, 1996 PCT Filed Feb. 6, 1995 PCT Pub. No. WO95/21819 PCT Pub. Date Aug. 17, 1995 (I) The present invention relates to compounds of formula (I) wherein n is 3 and where any carbon atom of (CH2)n may be substituted by R4 and/or R5; X represents O or S; R1 represents (CH2)qphenyl, wherein q is 0, 1 , 2 or 3 which may be optionally substituted in the phenyl ring; R2 represents aryl selected from phenyl and naphthyl; heteroaryl selected from indazolyl, thienyl, furyl, pyridyl, thiazolyl, tetrazolyl and quinolyl; benzhydryl; or benzyl; wherein each aryl or heteroaryl moiety may be substituted; R4 and R5 each independently represent H, halo, C1-6alkyl, oxo, CO2Ra or CONRaRb; R6 represents H or C1-6alkyl; R7 represents trifluoromethyl, C2-6alkenyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, (CH2)pNR9R10, CO2R16, CONR9R10, (CH2)pCO2R16, (CH2)pCONR9R10, (CH2)pNR9COR16, (CH2)pNHSO2R11, (CH2)pOR16, (CH2)pOC(O)R9 or (CH2)pOC1-4alkylCOR17 or C1-6alkyl substituted by a hydroxy group; R8 repents H, CORa, CO2Ra, COCONRaRb, COCO2Ra, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, C1-6alkyl optionally substituted by a group selected from (CO2Ra, CONRaRb, hydroxy, cyano, CORa, NRaRb, C(NOH)NRaRb, CONHphenyl(C1-4alkyl), COCO2Ra, CONHNRaRb, C(S)NRaRb, CONRaC1-6alkylR12, CONR13C2-6alkynyl, CONR13C2-6alkenyl, COCONRaRb, CONRaC(NRb)NRaRb, CONRaheteroaryl, and optionally substituted phenyl or C1-6alkyl, optionally substituted by oxo, substituted by an optionally substituted aromatic heterocycle; Ra and Rb each independently represent H, C1-6alkyl, trifluoromethyl or phenyl optionally substituted by C1-6alkyl, halo or trifluoromethyl. The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.

10. 发明专利

DE69516853D1 未知
公开(公告)号：DE69516853D1
公开(公告)日：2000-06-15
申请号：DE69516853
申请日：1995-02-06
申请人： MERCK SHARP & DOHME
发明人： BAKER RAYMOND , MACLEOD MURRAY , SEWARD MARY , SWAIN JOHN
IPC分类号： A61K31/4427 , A61K31/445 , A61K31/451 , A61P1/00 , A61P1/08 , A61P9/00 , A61P11/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P29/00 , A61P35/02 , A61P37/00 , A61P37/08 , A61P43/00 , C07D211/42 , C07D211/54 , C07D401/06
摘要： PCT No. PCT/GB95/00228 Sec. 371 Date Sep. 26, 1996 Sec. 102(e) Date Sep. 26, 1996 PCT Filed Feb. 6, 1995 PCT Pub. No. WO95/21819 PCT Pub. Date Aug. 17, 1995 (I) The present invention relates to compounds of formula (I) wherein n is 3 and where any carbon atom of (CH2)n may be substituted by R4 and/or R5; X represents O or S; R1 represents (CH2)qphenyl, wherein q is 0, 1 , 2 or 3 which may be optionally substituted in the phenyl ring; R2 represents aryl selected from phenyl and naphthyl; heteroaryl selected from indazolyl, thienyl, furyl, pyridyl, thiazolyl, tetrazolyl and quinolyl; benzhydryl; or benzyl; wherein each aryl or heteroaryl moiety may be substituted; R4 and R5 each independently represent H, halo, C1-6alkyl, oxo, CO2Ra or CONRaRb; R6 represents H or C1-6alkyl; R7 represents trifluoromethyl, C2-6alkenyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, (CH2)pNR9R10, CO2R16, CONR9R10, (CH2)pCO2R16, (CH2)pCONR9R10, (CH2)pNR9COR16, (CH2)pNHSO2R11, (CH2)pOR16, (CH2)pOC(O)R9 or (CH2)pOC1-4alkylCOR17 or C1-6alkyl substituted by a hydroxy group; R8 repents H, CORa, CO2Ra, COCONRaRb, COCO2Ra, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, C1-6alkyl optionally substituted by a group selected from (CO2Ra, CONRaRb, hydroxy, cyano, CORa, NRaRb, C(NOH)NRaRb, CONHphenyl(C1-4alkyl), COCO2Ra, CONHNRaRb, C(S)NRaRb, CONRaC1-6alkylR12, CONR13C2-6alkynyl, CONR13C2-6alkenyl, COCONRaRb, CONRaC(NRb)NRaRb, CONRaheteroaryl, and optionally substituted phenyl or C1-6alkyl, optionally substituted by oxo, substituted by an optionally substituted aromatic heterocycle; Ra and Rb each independently represent H, C1-6alkyl, trifluoromethyl or phenyl optionally substituted by C1-6alkyl, halo or trifluoromethyl. The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.

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