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21. 发明授权

US6017944A Antagonists of gonadotropin releasing hormone 失效
公开(公告)号：US6017944A
公开(公告)日：2000-01-25
申请号：US178689
申请日：1998-10-26
申请人： Lin Chu , Thomas F. Walsh , Mark Goulet , Matthew J. Wyvratt , Stephanie L. Witkin
发明人： Lin Chu , Thomas F. Walsh , Mark Goulet , Matthew J. Wyvratt , Stephanie L. Witkin
IPC分类号： A61P15/08 , C07D453/06 , C07D487/08 , A61K31/40 , A61K31/405 , C07D209/02 , C07D209/12 , C07D403/10
CPC分类号： C07D487/08 , C07D453/06
摘要： There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

22. 发明授权

US5208228A Aminomacrolides and derivatives having immunosuppressive activity 失效
标题翻译：具有免疫抑制活性的氨基马来酰胆碱和衍生物
公开(公告)号：US5208228A
公开(公告)日：1993-05-04
申请号：US698888
申请日：1991-05-13
申请人： Hyun O. Ok , Thomas R. Beattie , Michael H. Fisher , Matthew J. Wyvratt , Mark Goulet
发明人： Hyun O. Ok , Thomas R. Beattie , Michael H. Fisher , Matthew J. Wyvratt , Mark Goulet
IPC分类号： C07H19/01
CPC分类号： C07H19/01
摘要： Aminomacrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by incorporation of a nitrogen substituent at C-3" and/or C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma.
摘要翻译：通过在环己基环的C-3“和/或C-4”处引入氮取代基，由合适的前体制备了通式结构式I的氨基马来酰氯：。这些大环内酯类免疫抑制剂可用于哺乳动物宿主用于治疗自身免疫性疾病，感染性疾病和/或预防外来器官移植排斥反应。此外，这些大环内酯类免疫抑制剂可用于局部治疗炎性和过度增生性皮肤病以及免疫介导疾病的皮肤表现。此外，这些大环内酯可用于治疗可逆性阻塞性气道疾病，特别是哮喘。

23. 发明授权

US5162334A Amino O-alkyl, O-alkenyl and O-alkynlmacrolides having immunosuppressive activity 失效
标题翻译：具有免疫抑制活性的氨基O-烷基，O-链烯基和O-炔炔基大环内酯
公开(公告)号：US5162334A
公开(公告)日：1992-11-10
申请号：US698886
申请日：1991-05-13
申请人： Mark Goulet , Matthew J. Wyvratt
发明人： Mark Goulet , Matthew J. Wyvratt
IPC分类号： C07D498/18
CPC分类号： C07D498/18
摘要： Amino O-alkyl, O-alkenyl and O-alkynylmacrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and amination at C-3"/C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma.
摘要翻译：一般结构式I的氨基O-烷基，O-烯基和O-炔基丙烯酰氧化物：通过在环己基环的C-3“/ C-4”处的烷基化和胺化由合适的前体制备。这些大环内酯类免疫抑制剂可用于哺乳动物宿主用于治疗自身免疫性疾病，感染性疾病和/或预防外来器官移植排斥反应。此外，这些大环内酯类免疫抑制剂可用于局部治疗炎性和过度增生性皮肤病以及免疫介导疾病的皮肤表现。此外，这些大环内酯可用于治疗可逆性阻塞性气道疾病，特别是哮喘。

24. 发明授权

US5726319A Biphenyl substituted dipeptide analogs promote release of growth hormone 失效
标题翻译：联苯取代的二肽类似物促进生长激素的释放
公开(公告)号：US5726319A
公开(公告)日：1998-03-10
申请号：US510026
申请日：1995-08-01
申请人： Peter Lin , William R. Schoen , Judith M. Pisano , Matthew J. Wyvratt
发明人： Peter Lin , William R. Schoen , Judith M. Pisano , Matthew J. Wyvratt
IPC分类号： A61K38/00 , C07C275/24 , C07D257/04 , C07K5/06 , C07D257/00
CPC分类号： C07D257/04 , C07C275/24 , C07K5/06026 , C07K5/06191 , A61K38/00
摘要： There are disclosed certain compounds identified as substituted dipeptide analogs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such substituted dipeptide analogs as the active ingredient thereof are also disclosed.
摘要翻译：公开了鉴定为取代的二肽类似物的某些化合物，其促进人和动物中生长激素的释放。该物质可用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人体中，增加受缺乏正常分泌天然生长激素影响的人的身高。还公开了含有这种取代的二肽类似物作为其活性成分的生长促进组合物。

25. 发明授权

US5030640A Novel .beta.-adrenergic agonists and pharmaceutical compositions thereof 失效
标题翻译：新型β-肾上腺素能激动剂及其药物组合物
公开(公告)号：US5030640A
公开(公告)日：1991-07-09
申请号：US293785
申请日：1989-01-05
申请人： Michael H. Fisher , Matthew J. Wyvratt
发明人： Michael H. Fisher , Matthew J. Wyvratt
IPC分类号： A23K1/16 , A61K31/41 , A61K31/44 , A61K31/4427 , A61K31/505 , A61P3/04 , A61P11/08 , A61P25/24 , A61P25/26 , C07D401/12 , C07D403/12 , C07D487/04
CPC分类号： C07D401/12 , C07D403/12
摘要： .alpha.-Heterocyclic ethanolamino alkylindole derivatives and compositions made therefrom are potent .beta.-agonists having utility as growth promotion agents for animals, bronchodilators, antidepressants and antiobesity agents.

26. 发明授权

US07834062B2 Aminoalkylphenols, methods of using and making the same 有权
标题翻译：氨基烷基苯酚，使用和制造方法
公开(公告)号：US07834062B2
公开(公告)日：2010-11-16
申请号：US12540445
申请日：2009-08-13
申请人： Conrad P. Dorn , Mary Ann Powles , Thomas F. Walsh , Matthew J. Wyvratt
发明人： Conrad P. Dorn , Mary Ann Powles , Thomas F. Walsh , Matthew J. Wyvratt
IPC分类号： A61K31/135
CPC分类号： C07C233/18 , C07C215/50 , C07C215/52 , C07C217/58 , C07C229/14 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/28 , C07D213/38 , C07D241/12 , C07D249/12 , C07D295/096 , C07D307/52 , C07D309/04 , C07D309/14 , C07D319/12 , C07D333/48
摘要： The present invention relates to Mannich base antimalarial aminoalkylphenol compounds and their use against protozoa of the genus Plasmodium, particularly emerging strains of drug-resistant Plasmodia. This invention further relates to compositions containing such compounds and a process for making the compounds. This and other aspects of the invention are realized upon review of the entire specification.
摘要翻译：本发明涉及曼尼希碱抗疟氨基烷基苯酚化合物及其抗疟原虫的原生动物的用途，特别是新出现的抗药性血浆的菌株。本发明还涉及含有这些化合物的组合物和制备该化合物的方法。本发明的这个和其它方面在整个说明书的审查之后实现。

27. 发明授权

US06432980B1 Aliphatic amine substituted piperidyl diaryl pyrrole derivatives as antiprotozoal agents 失效
标题翻译：脂肪族胺取代的哌啶基二芳基吡咯衍生物作为抗原虫剂
公开(公告)号：US06432980B1
公开(公告)日：2002-08-13
申请号：US09710165
申请日：2000-11-10
申请人： Tesfaye Biftu , Danqing D. Feng , Gui-Bai Liang , Mitree M. Ponpipom , Xiaoxia Qian , Narindar Girotra , Michael H. Fischer , Matthew J. Wyvratt
发明人： Tesfaye Biftu , Danqing D. Feng , Gui-Bai Liang , Mitree M. Ponpipom , Xiaoxia Qian , Narindar Girotra , Michael H. Fischer , Matthew J. Wyvratt
IPC分类号： A61K314523
CPC分类号： C07D401/14 , A61K31/4545 , C07D413/14 , Y02A50/491
摘要： Trisubstituted pyrroles are antiprotozoal agents useful in the treatment and prevention of protozoal diseases in human and animals, including the control of coccidiosis in poultry.
摘要翻译：三取代吡咯是可用于治疗和预防人类和动物中的原生动物疾病的抗原虫剂，包括控制家禽中的球虫病。

28. 发明授权

US06211174B1 Naphtho-fused lactams promote release of growth hormone 失效
标题翻译：萘普生内含物促进生长激素的释放
公开(公告)号：US06211174B1
公开(公告)日：2001-04-03
申请号：US09159451
申请日：1998-09-24
申请人： Robert J. Devita , Matthew J. Wyvratt
发明人： Robert J. Devita , Matthew J. Wyvratt
IPC分类号： C07D22314
CPC分类号： C07D281/08 , A61K31/66 , C07D223/14 , C07D267/10 , A61K31/55 , A61K2300/00
摘要： The present invention is directed to certain naphtho-fused lactams of the general structural formula: wherein and R1, R1a, R1b, R2a, R2b, R3a, R4, R5, R6, A, L, X, n, p and w are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone.
摘要翻译：本发明涉及以下通式的某些萘并稠合内酰胺：其中R1，R1a，R1b，R2a，R2b，R3a，R4，R5，R6，A，L，X，n，p和w分别为本文定义。这些化合物促进人和动物中生长激素的释放。这种性质可以用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人类中，用于治疗以生长激素分泌不足为特征的生理或医学病症，例如生长激素缺乏的身材矮小儿童，并且治疗通过生长激素的合成代谢作用改善的医疗状况。

29. 发明授权

US5726307A Benzo-fused lactams promote release of growth hormone 失效
公开(公告)号：US5726307A
公开(公告)日：1998-03-10
申请号：US356935
申请日：1994-12-15
申请人： William R. Schoen , Matthew J. Wyvratt
发明人： William R. Schoen , Matthew J. Wyvratt
IPC分类号： A61K31/55 , A61P3/00 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D417/06 , C07D285/36 , C07D267/14
CPC分类号： C07D403/06 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/06
摘要： There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.

30. 发明授权

US5077290A Morpholine derivatives compositions and use 失效
标题翻译：吗啉衍生物组合物和用途
公开(公告)号：US5077290A
公开(公告)日：1991-12-31
申请号：US597976
申请日：1990-10-11
申请人： Michael H. Fisher , Matthew J. Wyvratt
发明人： Michael H. Fisher , Matthew J. Wyvratt
IPC分类号： C07D413/04 , C07D413/14 , C07D471/04
CPC分类号： C07D471/04 , C07D413/04 , C07D413/14
摘要： N-Substituted-2-heterocyclic morpholine derivatives and compositions made therefrom are highly active compounds having utility as growth promotion agents for animals, bronchodilators, antidepressants and antiobesity agents.
摘要翻译： N-取代的2-杂环吗啉衍生物和由其制备的组合物是具有用作动物，支气管扩张剂，抗抑郁药和抗肥胖剂的生长促进剂的高活性化合物。

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