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1. 发明申请

WO2004039803A2 HIV-INTEGRASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS FOR THEIR USE 审中-公开
标题翻译： HIV整合酶抑制剂，药物组合物及其使用方法
公开(公告)号：WO2004039803A2
公开(公告)日：2004-05-13
申请号：PCT/IB2003/004735
申请日：2003-10-27
申请人： PFIZER INC. , HU, Qiyue , KUKI, Atsuo , NOWLIN, Dawn, Marie , PLEWE, Michael, Bruno , WANG, Hai , ZHANG, Junhu
发明人： HU, Qiyue , KUKI, Atsuo , NOWLIN, Dawn, Marie , PLEWE, Michael, Bruno , WANG, Hai , ZHANG, Junhu
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D471/12 , C07D471/14
摘要： Bicyclic hydroxamate compounds represented by the Formula I are described. The bicyclic hydroxamate compounds and compositions containing those compounds may be used to inhibit or modulate an enzyme activity of HIV Integrase and to treat HIV mediated diseases and conditions.
摘要翻译：描述了由式I表示的双环异羟肟酸酯化合物。双环异羟肟酸酯化合物和含有这些化合物的组合物可用于抑制或调节HIV整合酶的酶活性并治疗HIV介导的疾病和病症。

2. 发明申请

WO9901423A8 GLUCAGON ANTAGONISTS/INVERSE AGONISTS 审中-公开
标题翻译： GLUCAGON ANTAGONISTS / INVERSE AGONISTS
公开(公告)号：WO9901423A8
公开(公告)日：2001-05-17
申请号：PCT/DK9800287
申请日：1998-06-30
申请人： NOVO NORDISK AS , ALANEX CORP , LING ANTHONY , GREGOR VLAD , GONZALES JAVIER , HONG YUFENG , KIEL DAN , KUKI ATSUO , SHI SHENGHUA , NAERUM LARS , MADSEN PETER , SAMS CHRISTIAN , LAU JESPER , PLEWE MICHAEL BRUNO , FENG JUN , TENG MIN , JOHNSON MICHAEL DAVID , TESTON KIMBERLY ANN , SIDELMANN ULLA GROVE , KNUDSEN LOTTE BJERRE
发明人： LING ANTHONY , GREGOR VLAD , GONZALES JAVIER , HONG YUFENG , KIEL DAN , KUKI ATSUO , SHI SHENGHUA , NAERUM LARS , MADSEN PETER , SAMS CHRISTIAN , LAU JESPER , PLEWE MICHAEL BRUNO , FENG JUN , TENG MIN , JOHNSON MICHAEL DAVID , TESTON KIMBERLY ANN , SIDELMANN ULLA GROVE , KNUDSEN LOTTE BJERRE
IPC分类号： C07C251/86 , C07C255/29 , C07C309/65 , C07C311/49 , C07C317/28 , C07C323/45 , C07D209/48 , C07D209/86 , C07D213/30 , C07D213/80 , C07D215/12 , C07D231/12 , C07D295/185 , C07D307/12 , C07D307/52 , C07D309/06 , C07D317/58 , C07C243/18 , A61K31/15 , A61K31/40 , C07D209/04
CPC分类号： C07D209/48 , C07C251/86 , C07C255/29 , C07C309/65 , C07C311/49 , C07C317/28 , C07C323/45 , C07C2601/02 , C07C2601/14 , C07D209/86 , C07D213/30 , C07D213/80 , C07D215/12 , C07D231/12 , C07D295/185 , C07D307/12 , C07D307/52 , C07D309/06 , C07D317/58
摘要： Non-peptide compounds comprising a central hydrazide motif and methods for the synthesis thereof. The compounds act to antagonize the action of the glucagon peptide hormone.
摘要翻译：包含中心酰肼基序的非肽化合物及其合成方法。该化合物起拮抗胰高血糖素肽激素的作用。

3. 发明申请

WO0236554A3 AMIDINO-UREA SEROTONIN RECEPTOR LIGANDS AND COMPOSITIONS, THEIR PHARMACEUTICAL USES, AND METHODS FOR THEIR SNYTHESIS 审中-公开
标题翻译：氨基酸尿嘧啶受体配体和组合物，其药物用途及其SNYTHESIS的方法
公开(公告)号：WO0236554A3
公开(公告)日：2003-03-13
申请号：PCT/IB0102022
申请日：2001-10-26
申请人： WARNER LAMBERT CO , HONG YUFENG , KUKI ATSUO , TOMPKINS EILEEN VALENZUELA , PENG ZHENGWEI , LUTHIN DAVID ROBERT
发明人： HONG YUFENG , KUKI ATSUO , TOMPKINS EILEEN VALENZUELA , PENG ZHENGWEI , LUTHIN DAVID ROBERT
IPC分类号： C07D295/20 , A61K31/175 , A61K31/381 , A61K31/40 , A61K31/4045 , A61K31/4164 , A61K31/437 , A61K31/4402 , A61K31/4406 , A61K31/445 , A61K31/4465 , A61K31/4468 , A61K31/4525 , A61K31/454 , A61K31/472 , A61K31/495 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P43/00 , C07C279/22 , C07C279/24 , C07C323/48 , C07D207/09 , C07D209/14 , C07D209/16 , C07D211/16 , C07D211/26 , C07D211/58 , C07D211/60 , C07D211/62 , C07D213/36 , C07D213/40 , C07D217/06 , C07D233/61 , C07D233/64 , C07D235/30 , C07D295/215 , C07D333/20 , C07D405/06 , C07D413/06 , C07D471/10 , C07D521/00 , A61K31/155
CPC分类号： C07D213/40 , C07C279/22 , C07C279/24 , C07C2602/08 , C07C2602/42 , C07D207/09 , C07D209/14 , C07D211/16 , C07D211/26 , C07D211/58 , C07D211/60 , C07D211/62 , C07D217/06 , C07D231/12 , C07D233/56 , C07D235/30 , C07D249/08 , C07D295/215 , C07D333/20 , C07D405/06 , C07D413/06 , C07D471/10
摘要： Novel amidino-urea 5-HT7 receptor ligands, methods of preparing such ligands, intermediate compounds useful in the preparation of the receptor ligands, pharmaceutical compositions comprising the receptor ligands, and methods of treating sleep disorders, pain, depression, and schizophrenia employing the receptor ligands are disclosed. The receptor ligands have formula (1): wherein the formula variables are as defined herein, and pharmaceutically acceptable salts, solvates, active metabolites, or prodrugs thereof.
摘要翻译：新型脒基 - 尿素5-HT7受体配体，制备这种配体的方法，可用于制备受体配体的中间体化合物，包含受体配体的药物组合物，以及使用受体的治疗睡眠障碍，疼痛，抑郁症和精神分裂症的方法配体。受体配体具有式（1）：其中式变量如本文所定义，及其药学上可接受的盐，溶剂合物，活性代谢物或前药。

4. 发明申请

WO0033839B1 NON-PEPTIDE ANTAGONISTS OF GLP-1 RECEPTOR AND METHODS OF USE 审中-公开
标题翻译： GLP-1受体的非肽拮抗剂及其使用方法
公开(公告)号：WO0033839B1
公开(公告)日：2000-09-28
申请号：PCT/US9929065
申请日：1999-12-08
申请人： AGOURON PHARMA , TRUESDALE LARRY KENNETH , BYCHOWSKI RICHARD A , GONZALEZ JAVIER , KUKI ATSUO , RAJAPAKSE RANJAN JAGATH , TENG MIN , KIEL DAN , DHANOA DALJIT S , HONG YUFENG , CHOU TSO SHENG , LING ANTHONY L , JOHNSON MICHAEL DAVID , GREGOR VLAD EDWARD
发明人： TRUESDALE LARRY KENNETH , BYCHOWSKI RICHARD A , GONZALEZ JAVIER , KUKI ATSUO , RAJAPAKSE RANJAN JAGATH , TENG MIN , KIEL DAN , DHANOA DALJIT S , HONG YUFENG , CHOU TSO-SHENG , LING ANTHONY L , JOHNSON MICHAEL DAVID , GREGOR VLAD EDWARD
IPC分类号： C07D491/147 , A61K31/437 , A61K31/519 , A61P5/48 , A61P43/00 , C07D471/04 , C07D471/10 , C07D471/14 , C07D491/04 , C07D491/14 , C07D521/00 , A61K31/4985 , A61K31/5377 , C07D237/00 , C07D413/14 , C07D471/12
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D471/04 , C07D471/14 , C07D491/04 , C07D491/14
摘要： Non-peptide compounds that act as antagonists of the intestinal hormone glucagon-like peptide 1 (GLP-1) have a 9H- beta -carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding to the GLP-1 receptor and/or prevent activation of the receptor by bound GLP-1. The invention further relates to a method of inhibiting the binding of GLP-1 to the GLP-1 receptor and a method of inhibiting the activation of the GLP-1 receptor. Intermediate compounds useful for making non-peptide GLP-1 receptor antagonists are also described.
摘要翻译：作为肠激素胰高血糖素样肽1（GLP-1）的拮抗剂的非肽化合物具有9H-β-咔啉中心基序。该化合物表现出有利的物理，化学和生物学特性，并且抑制GLP-1肽与GLP-1受体的结合和/或通过结合的GLP-1阻止受体活化。本发明还涉及抑制GLP-1与GLP-1受体结合的方法以及抑制GLP-1受体活化的方法。还描述了可用于制备非肽GLP-1受体拮抗剂的中间体化合物。

5. 发明申请

WO2004039803A3 HIV-INTEGRASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS FOR THEIR USE 审中-公开
标题翻译： HIV-INTEGRASE INHIBITORS，PHARMACEUTICAL COMPOSITIONS及其使用方法
公开(公告)号：WO2004039803A3
公开(公告)日：2004-09-16
申请号：PCT/IB0304735
申请日：2003-10-27
申请人： PFIZER , HU QIYUE , KUKI ATSUO , NOWLIN DAWN MARIE , PLEWE MICHAEL BRUNO , WANG HAI , ZHANG JUNHU
发明人： HU QIYUE , KUKI ATSUO , NOWLIN DAWN MARIE , PLEWE MICHAEL BRUNO , WANG HAI , ZHANG JUNHU
IPC分类号： A61K31/435 , A61P31/18 , C07D471/04 , C07D471/12 , C07D471/14
CPC分类号： C07D471/04 , C07D471/12 , C07D471/14
摘要： Bicyclic hydroxamate compounds represented by the Formula I are described. The bicyclic hydroxamate compounds and compositions containing those compounds may be used to inhibit or modulate an enzyme activity of HIV Integrase and to treat HIV mediated diseases and conditions.
摘要翻译：描述由式I表示的双环氧肟酸盐化合物。双环异羟肟酸酯化合物和含有这些化合物的组合物可用于抑制或调节HIV整合酶的酶活性并治疗HIV介导的疾病和病症。

6. 发明申请

WO2004067531A1 HIV-INTEGRASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS FOR THEIR USE 审中-公开
标题翻译： HIV-INTEGRASE INHIBITORS，PHARMACEUTICAL COMPOSITIONS及其使用方法
公开(公告)号：WO2004067531A1
公开(公告)日：2004-08-12
申请号：PCT/IB2004/000259
申请日：2004-01-23
申请人： PFIZER INC. , KUKI, Atsuo , LI, Xinqiang , PLEWE, Michael, Bruno , WANG, Hai , ZHANG, Junhu
发明人： KUKI, Atsuo , LI, Xinqiang , PLEWE, Michael, Bruno , WANG, Hai , ZHANG, Junhu
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Beta-carboline hydroxamic acid compounds represented by formula (I) and formula (lb) are described, wherein: R 1, R 2 , R 3 , R 4 , R 5 , and R 6 are independently selected from hydrogen, halogen, C 1 _C 6 alkyl, aikoxy C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, -OR c , -NO 2 , and -N(R c ) 2 , each R c is Independently selected from hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, and C 2 -C a alkynyl; R 7 Is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, or C 2 -C 6 alkynyl, all of which are optionally substituted by one or more substituents independently selected from halogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl; C 2 -C 6 alkynyl, aryl, cycloalkyl, heterocycioalkyl, and heteroaryl, wherein said aryl, cydoalkyi, and heterocycloalkyl are optionally substituted with one or more substituents independently selected from halogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, and C 2 -C 6 alkynyl; R 8 and R 9 are independently selected from hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, and C 2 -C 6 aikynyl, wherein said alkyl, alkenyl, and alkynyl are optionally substituted with one or more substituents independently selected from halogen, aryl, cycloalkyl, heterocycloalkyl, and heteroaryl group, wherein said aryl, cycloalkyl, and heterocycloalkyl are optionally substituted with one or more substituents independently selected from halogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, and C 2 -C 6 alkynyl. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity of HIV integrase enzyme and to treat HIV integrase-mediated diseases and conditions.
摘要翻译：描述了由式（I）和式（Ib）表示的β-咔啉异羟肟酸化合物，其中：R1，R2，R3，R4，R5和R6独立地选自氢，卤素，C1-C6烷基，烷氧基C1-C6烷基，C 2 -C 6烯基，C 2 -C 6炔基，-OR c，-NO 2和-N（R c）2，每个R c独立地选自氢，C 1 -C 6烷基，C 2 -C 6烯基和C 2 -C 5炔基; R 7是C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基，它们全部被一个或多个独立地选自卤素，C 1 -C 6烷基，C 2 -C 6烯基， C 2 -C 6炔基，芳基，环烷基，杂环烷基和杂芳基，其中所述芳基，环烷基和杂环烷基任选被一个或多个独立地选自卤素，C 1 -C 6烷基，C 2 -C 6烯基和C 2 -C 6炔基的取代基取代 ; R 8和R 9独立地选自氢，C 1 -C 6烷基，C 2 -C 6烯基和C 2 -C 6炔基，其中所述烷基，烯基和炔基任选地被一个或多个独立地选自卤素，芳基，环烷基，杂环烷基和杂芳基，其中所述芳基，环烷基和杂环烷基任选地被一个或多个独立地选自卤素，C 1 -C 6烷基，C 2 -C 6烯基和C 2 -C 6炔基的取代基取代。含有这些化合物的β-咔啉异羟肟酸化合物和组合物可用于抑制或调节HIV整合酶的活性并且用于治疗HIV整合酶介导的疾病和病症。

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