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1. 发明申请

WO1998014192A1 VITRONECTIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：维生素受体拮抗剂
公开(公告)号：WO1998014192A1
公开(公告)日：1998-04-09
申请号：PCT/US1997018001
申请日：1997-10-01
申请人： SMITHKLINE BEECHAM CORPORATION , CALLAHAN, James, Francis , COUSINS, Russell, Donovan , KEENAN, Richard, McCullock , KWON, Chet , MILLER, William, Henry , UZINKAS, Irene, Nijole
发明人： SMITHKLINE BEECHAM CORPORATION
IPC分类号： A61K31/44
CPC分类号： C07D223/16 , A61K31/55 , A61K33/24 , A61K45/06 , C07D401/12 , C07D403/12 , C07D417/12 , Y02P20/55 , Y02P20/582 , A61K31/47 , A61K2300/00
摘要： Compounds having a benzodiazepinyl core structure are disclosed which are vitronectin receptor antagonists useful in the treatment of osteoporosis, angiogenesis, tumor growth and metastasis, atherosclerosis, restenosis and inflammation.
摘要翻译：公开了具有苯并二氮杂环核心结构的化合物，其是可用于治疗骨质疏松症，血管生成，肿瘤生长和转移，动脉粥样硬化，再狭窄和炎症的玻连蛋白受体拮抗剂。

2. 发明申请

WO1996000730A1 VITRONECTIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：维生素受体拮抗剂
公开(公告)号：WO1996000730A1
公开(公告)日：1996-01-11
申请号：PCT/US1995008306
申请日：1995-06-29
申请人： SMITHKLINE BEECHAM CORPORATION , ALI, Fadia , BONDINELL, William , HUFFMAN, William, Francis , LAGO, M., Amparo , KEENAN, Richard, McCulloch , KWON, Chet , MILLER, William, Henry , NGUYEN, Thomas , TAKATA, Dennis, T.
发明人： SMITHKLINE BEECHAM CORPORATION
IPC分类号： C07D519/00
CPC分类号： C07D223/16 , C07D235/14 , C07D243/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/04
摘要： Compounds are disclosed which are vitronectin receptor antagonists useful in the treatment of osteoporosis. These compounds comprise a fibrinogen receptor antagonist template linked to a heterocyclic moiety.
摘要翻译：公开了可用于治疗骨质疏松症的玻连蛋白受体拮抗剂的化合物。这些化合物包含与杂环部分连接的纤维蛋白原受体拮抗剂模板。

3. 发明申请

WO1997024119A1 VITRONECTIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：维生素受体拮抗剂
公开(公告)号：WO1997024119A1
公开(公告)日：1997-07-10
申请号：PCT/US1996020748
申请日：1996-12-20
申请人： SMITHKLINE BEECHAM CORPORATION , MILLER, William, Henry , BONDINELL, William, Edward , KU, Thomas, Wen-Fu , KEENAN, Richard, McCulloch , SAMANEN, James, Martin , KWON, Chet , ALI, Fadia, El-Fehail , LAGO, Maria, A.
发明人： SMITHKLINE BEECHAM CORPORATION
IPC分类号： A61K31/40
CPC分类号： C07D401/12 , C07D235/14 , C07D235/16 , C07D235/30 , C07D243/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/06 , C07D471/04 , C07D487/04
摘要： Compounds of formulae (I-V) are disclosed which are vitronectin receptor antagonists and are useful in the treatment of osteoporosis.
摘要翻译：公开了式（I-V）化合物，其是玻连蛋白受体拮抗剂，并且可用于治疗骨质疏松症。

4. 发明申请

WO2005035533A8 MODULATORS OF SEROTONIN RECEPTORS 审中-公开
标题翻译：调节血清素受体
公开(公告)号：WO2005035533A8
公开(公告)日：2005-06-30
申请号：PCT/US2004032849
申请日：2004-10-06
申请人： SQUIBB BRISTOL MYERS CO , WACKER DEAN A , ZHAO GUOHUA , KWON CHET , VARNES JEFFREY G , STEIN PHILIP D
发明人： WACKER DEAN A , ZHAO GUOHUA , KWON CHET , VARNES JEFFREY G , STEIN PHILIP D
IPC分类号： A61P25/24 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04 , A61K31/4985
CPC分类号： C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention provides modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impared glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using such compounds and compositions.
摘要翻译：本发明提供了5-羟色胺受体调节剂，含有这种调节剂的药物组合物以及治疗与血清素受体调节有关的各种疾病，病症和病症的方法，例如代谢疾病，包括但不限于肥胖症，糖尿病，糖尿病并发症，动脉粥样硬化，葡萄糖耐量降低和血脂异常; 包括但不限于焦虑症，抑郁症，强迫症，恐慌症，精神病，精神分裂症，睡眠障碍，性障碍和社交恐怖症的中枢神经系统疾病; 头痛; 偏头痛; 和使用这些化合物和组合物的胃肠疾病。

5. 发明申请

WO2005035533A1 MODULATORS OF SEROTONIN RECEPTORS 审中-公开
标题翻译： SEROTONIN受体的调节剂
公开(公告)号：WO2005035533A1
公开(公告)日：2005-04-21
申请号：PCT/US2004/032849
申请日：2004-10-06
申请人： BRISTOL-MYERS SQUIBB COMPANY , WACKER, Dean A. , ZHAO, Guohua , KWON, Chet , VARNES, Jeffrey G. , STEIN, Philip D.
发明人： WACKER, Dean A. , ZHAO, Guohua , KWON, Chet , VARNES, Jeffrey G. , STEIN, Philip D.
IPC分类号： C07D487/04
CPC分类号： C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention provides modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impared glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using such compounds and compositions.
摘要翻译：本发明提供5-羟色胺受体的调节剂，含有这样的调节剂的药物组合物和用于治疗与调节血清素受体相关的各种疾病，病症和病症的方法，所述调节剂包括但不限于肥胖症，糖尿病，糖尿病并发症，动脉粥样硬化，葡萄糖耐量异常和血脂异常; 包括但不限于焦虑，抑郁，强迫症，恐慌症，精神病，精神分裂症，睡眠障碍，性障碍和社交恐惧症的中枢神经系统疾病; 头痛偏头痛; 和使用这些化合物和组合物的胃肠道疾病。

6. 发明申请

WO1996018602A1 BICYCLIC FIBRINOGEN ANTAGONISTS 审中-公开
标题翻译：双相纤维蛋白拮抗剂
公开(公告)号：WO1996018602A1
公开(公告)日：1996-06-20
申请号：PCT/US1995015937
申请日：1995-12-07
申请人： SMITHKLINE BEECHAM CORPORATION , CALLAHAN, James, Francis , KEENAN, Richard, McCulloch , KWON, Chet , SAMANEN, James, Martin
发明人： SMITHKLINE BEECHAM CORPORATION
IPC分类号： C07C245/04
CPC分类号： C07D217/06 , C07C233/32 , C07C257/18 , C07C2602/10
摘要： This invention relates to compound of formula (I) which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.
摘要翻译：本发明涉及有效抑制血小板聚集的式（I）化合物，用于实现这种活性的药物组合物和抑制血小板聚集的方法。

7. 发明申请

WO1996006087A1 BICYCLIC COMPOUNDS 审中-公开
标题翻译：双酚化合物
公开(公告)号：WO1996006087A1
公开(公告)日：1996-02-29
申请号：PCT/US1995010670
申请日：1995-08-22
申请人： SMITHKLINE BEECHAM CORPORATION , KWON, Chet , MILLER, William, Henry
发明人： SMITHKLINE BEECHAM CORPORATION
IPC分类号： C07D243/14
CPC分类号： C07D223/16 , C07D243/14 , C07D267/14 , C07D281/10 , C07D401/14
摘要： This invention relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof, which are effective for inhibiting platelet aggregation and bone resorption, pharmaceutical compositions for effecting such activity, and a method for using these compounds.
摘要翻译：本发明涉及有效抑制血小板聚集和骨吸收的式（I）化合物或其药学上可接受的盐，用于实现这种活性的药物组合物以及使用这些化合物的方法。

8. 发明申请

WO1996000574A1 VITRONECTIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：维生素受体拮抗剂
公开(公告)号：WO1996000574A1
公开(公告)日：1996-01-11
申请号：PCT/US1995008146
申请日：1995-06-29
申请人： SMITHKLINE BEECHAM CORPORATION , COUSINS, Russell, Donovan , KEENAN, Richard, McCulloch , KWON, Chet , MILLER, William, Henry , UZINSKAS, Irene, Nijole
发明人： SMITHKLINE BEECHAM CORPORATION
IPC分类号： A61K31/55
CPC分类号： C07D223/16 , C07D235/14 , C07D243/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/04
摘要： Compounds of formula (I) are disclosed which are inhibitors of the vitronectin receptor, wherein X-X' is NR -CH, NC(O)R -CH, N=C, CR =C, CHR -CH, O-CH or S-CH; R is H, C1-6alkyl or benzyl; R is (CH2)nCO2H; R is H, C1-6alkyl, Ar-C0-6alkyl, Het-C0-6 alkyl, or C3-6cycloalkyl-C0-6alkyl; R is W-U, Y-(CHR )m-U or Z-C(O); R and R are independently chosen from H, C1-6alkyl, Ar-C0-6alkyl;, Het-C0-6alkyl and C3-6cycloalkyl-C0-6alkyl; m is 1 or 2; n is 1 or 2; U is NR C(O), C(O)NR , CH=CH, CC, CH2-CH2, O-CH2, CH2-O or CH2OCONR ; W is (a), (b) or (c); R is H, OH, NO2, N(R )2, CON(R )2, CH2N(R )2, or R HN-C(=NH); Y is NH2, NHR , N(R )2, C(O)N(R )2, OH, =N-OR , (d), (e) or (f); Z is (g) or (h); R is H, N(R )2, C1-4alkyl, CON(R )2, OH, OR , or Ar-C0-4alkyl; R is H, C1-4alkyl, 2- or 3-pyridinyl, 1-, 2- or 3-piperidinyl, or 2- or 4-pyrimidinyl; and pharmaceutically acceptable salts thereof.
摘要翻译：公开了式（I）化合物，其为玻连蛋白受体的抑制剂，其中XX'为NR 1 -CH，NC（O）R 3 -CH，N = C，CR 1 = C，CHR -CH，O-CH或S-CH; R 1是H，C 1-6烷基或苄基; R 2是（CH 2）n CO 2 H; R 3是H，C 1-6烷基，Ar-C 0-6烷基，Het-C 0-6烷基或C 3-6环烷基-C 0-6烷基; R 4是W-U，Y-（CHR 5）m-U或Z-C（O）; R 5和R 6独立地选自H，C 1-6烷基，Ar-C 0-6烷基，Het-C 0-6烷基和C 3-6环烷基-C 0-6烷基; m为1或2; n为1或2; U是NR 1 C（O），C（O）NR 1，CH = CH，CC，CH 2 -CH 2，O-CH 2，CH 2 -O或CH 2 OCONR 1; W是（a），（b）或（c）; R a是H，OH，NO 2，N（R 6）2，CON（R 6）2，CH 2 N（R 6）2或R 6 HN-C（= NH） ; Y是NH 2，NHR 6，N（R 6）2，C（O）N（R 6）2，OH，= N-OR 6，（d），（e） F）; Z是（g）或（h）; R d是H，N（R 1）2，C 1-4烷基，CON（R 1）2，OH，OR 1或Ar-C 0-4烷基; R e是H，C 1-4烷基，2-或3-吡啶基，1-，2-或3-哌啶基，或2-或4-嘧啶基; 及其药学上可接受的盐。

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