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21. 发明授权

US5310903A Imidazolidyl rapamycin derivatives 失效
标题翻译：咪唑烷雷怕霉素衍生物
公开(公告)号：US5310903A
公开(公告)日：1994-05-10
申请号：US26925
申请日：1993-03-05
申请人： Mark Goulet , William H. Parsons , Matthew J. Wyvratt
发明人： Mark Goulet , William H. Parsons , Matthew J. Wyvratt
IPC分类号： C07D498/18 , A61K31/395
CPC分类号： C07D498/18
摘要： Imidazolidyl rapamycin derivatives of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-42 and/or C-31. These compounds are useful in a mammalian host for the treatment of autoimmune diseases and diseases of inflammation, infectious diseases, the prevention of rejection of foreign organ transplants and the treatment of solid tumors.
摘要翻译：一般结构式I的咪唑烷基雷帕霉素衍生物：通过C-42和/或C-31的烷基化和/或芳基化从合适的前体制备。这些化合物可用于哺乳动物宿主用于治疗自身免疫性疾病和炎症疾病，感染性疾病，预防外来器官移植排斥和治疗实体瘤。

22. 发明授权

US5147877A Semi-synthetic immunosuppressive macrolides 失效
标题翻译：半合成免疫抑制大环内酯类
公开(公告)号：US5147877A
公开(公告)日：1992-09-15
申请号：US759746
申请日：1991-09-12
申请人： Mark Goulet
发明人： Mark Goulet
IPC分类号： C07D498/18 , C07H19/01
CPC分类号： C07D498/18 , C07H19/01
摘要： Macrolides of the general structural Formula I: ##STR1## have been prepared. These macrolides are antagonists of FK-506-type immunosuppressants and are useful for modifying dosages of FK-506-type immunosuppressants in the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. Furthermore, the compounds of the present invention may have utility as antidotes for overdoses of FK-506-type immunosuppressants. In addition, 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.
摘要翻译：一般结构式I的大环内酯类：我已经准备好了。这些大环内酯类是FK-506型免疫抑制剂的拮抗剂，可用于修饰FK-506型免疫抑制剂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的剂量。此外，本发明的化合物可用作FK-506型免疫抑制剂过量的解毒剂。此外，这些大环内酯类免疫抑制剂可用于哺乳动物宿主中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。

23. 发明授权

US06200957B1 Antagonists of gonadotropin releasing hormone 失效
公开(公告)号：US06200957B1
公开(公告)日：2001-03-13
申请号：US09115497
申请日：1998-07-14
申请人： Mark Goulet , Wallace T. Ashton , Lin Chu , Michael H. Fisher , Peter Lin , Mitree M. Ponpipom , Matthew J. Wyvratt , Narindar N. Girotra , Jonathan Young
发明人： Mark Goulet , Wallace T. Ashton , Lin Chu , Michael H. Fisher , Peter Lin , Mitree M. Ponpipom , Matthew J. Wyvratt , Narindar N. Girotra , Jonathan Young
IPC分类号： C07D20910
CPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , C07D487/08
摘要： There are disclosed compounds of formula (I) 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.

24. 发明授权

US5349061A O-heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroarylmacrolides having immunosuppressive activity 失效
标题翻译：具有免疫抑制活性的O-杂芳基，O-烷基杂芳基，O-烯基杂芳基和O-炔基杂芳基大环内酯
公开(公告)号：US5349061A
公开(公告)日：1994-09-20
申请号：US135200
申请日：1993-10-12
申请人： Peter J. Sinclair , Joung Goulet , Frederick Wong , Mark Goulet , William H. Parsons , Matthew J. Wyvratt
发明人： Peter J. Sinclair , Joung Goulet , Frederick Wong , Mark Goulet , William H. Parsons , Matthew J. Wyvratt
IPC分类号： A61K31/40 , A61K31/445 , A61K31/495 , A61K31/70 , A61P37/06 , C07D498/18 , C07H19/01 , A61K31/345 , C07D491/16
CPC分类号： C07H19/01
摘要： O-Heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroaryl-macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation 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, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.
摘要翻译：通式I的O-杂芳基，O-烷基杂芳基，O-链烯基杂芳基和O-炔基杂芳基 - 大环内酯：通过C-3“和/或C的烷基化和/或芳基化从合适的前体制备 -4“。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疾病，感染性疾病，预防外来器官移植排斥和/或相关疾病，疾病和疾病。

25. 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。

26. 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。

27. 发明申请

US20050239828A1 Spirocyclic amides as cannabinoid receptor modulators 失效
标题翻译：螺环酰胺作为大麻素受体调节剂
公开(公告)号：US20050239828A1
公开(公告)日：2005-10-27
申请号：US10507864
申请日：2003-03-21
申请人： William Hagmann , Linus Lin , Shrenik Shah , Mark Goulet , James Jewell
发明人： William Hagmann , Linus Lin , Shrenik Shah , Mark Goulet , James Jewell
IPC分类号： C07D307/24 , A61K31/165 , A61K31/27 , A61K31/275 , A61K31/341 , A61K31/351 , A61K31/397 , A61K31/40 , A61K31/401 , A61K31/4015 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4425 , A61K31/445 , A61K31/4545 , A61K31/5375 , A61P1/10 , A61P1/14 , A61P1/16 , A61P3/04 , A61P9/10 , A61P11/06 , A61P25/00 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , A61P29/00 , A61P43/00 , C07C233/59 , C07C235/40 , C07C235/82 , C07C237/24 , C07C255/60 , C07C271/24 , C07C317/44 , C07D205/04 , C07D207/16 , C07D207/28 , C07D207/38 , C07D207/48 , C07D211/60 , C07D211/62 , C07D213/40 , C07D213/56 , C07D213/61 , C07D213/82 , C07D213/89 , C07D265/30 , C07D307/68 , C07D309/08 , C07D401/04 , C07D41/02
CPC分类号： C07D207/38 , C07C233/59 , C07C235/40 , C07C235/82 , C07C237/24 , C07C255/60 , C07C271/24 , C07C317/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/16 , C07D207/48 , C07D211/60 , C07D211/62 , C07D213/56 , C07D213/61 , C07D213/82 , C07D213/89 , C07D265/30 , C07D307/24 , C07D307/68 , C07D309/08 , C07D401/04
摘要： Novel compounds of structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as psychotropic drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinsons disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as, the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要翻译：结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管意外的精神药物，头部创伤，焦虑障碍，压力，癫痫，帕金森病，运动障碍和精神分裂症。这些化合物也可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

28. 发明授权

US5780437A Antagonists of gonadotropin releasing hormone 失效
标题翻译：促性腺激素释放激素的拮抗剂
公开(公告)号：US5780437A
公开(公告)日：1998-07-14
申请号：US760816
申请日：1996-12-05
申请人： Mark Goulet , Wallace T. Ashton , Lin Chu , Michael H. Fisher , Narindar N. Girotra , Peter Lin , Matthew J. Wyvratt
发明人： Mark Goulet , Wallace T. Ashton , Lin Chu , Michael H. Fisher , Narindar N. Girotra , Peter Lin , Matthew J. Wyvratt
IPC分类号： C07D20060101 , C07D401/12 , C07D401/14 , C07D413/14 , C07D487/08 , A61K38/00 , A61K31/40 , A61K31/54
CPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , C07D487/08
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.
摘要翻译：公开了式（I）的化合物及其药学上可接受的盐，其可用作GnRH的拮抗剂，因此可用于治疗两种男性中各种性激素相关和其他病症和妇女。

29. 发明授权

US5532248A O-aryl,O-alkyl, and O-alkenyl-macrolides having immunosuppressive activity 失效
标题翻译：具有免疫抑制活性的O-芳基，O-烷基和O-烯基 - 大环内酯类
公开(公告)号：US5532248A
公开(公告)日：1996-07-02
申请号：US440180
申请日：1995-05-12
申请人： Mark Goulet , William H. Parsons , Helen M. Organ , Peter J. Sinclair , Frederick Wong , Matthew J. Wyvratt
发明人： Mark Goulet , William H. Parsons , Helen M. Organ , Peter J. Sinclair , Frederick Wong , Matthew J. Wyvratt
IPC分类号： A61K31/41 , A61K31/40 , A61K31/435 , A61K31/445 , A61P17/00 , A61P29/00 , A61P31/12 , A61P37/06 , C07D498/18 , C07D491/16
CPC分类号： C07D498/18
摘要： O-Aryl, O-alkyl, O-alkenyl and O-alkynyl-macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation 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 and/or related afflictions, diseases and illnesses.
摘要翻译：一般结构式I的O-芳基，O-烷基，O-链烯基和O-炔基 - 大环内酯类：已经通过C-3“和/或C的烷基化和/或芳基化由合适的前体制备 -4“。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和/或相关疾病，疾病和疾病。

30. 发明授权

US5344925A Imidazolidyl macrolides having immunosuppressive activity 失效
标题翻译：具有免疫抑制活性的咪唑烷基大环内酯类
公开(公告)号：US5344925A
公开(公告)日：1994-09-06
申请号：US124137
申请日：1993-09-20
申请人： Mark Goulet , Peter J. Sinclair , Frederick Wong , Matthew J. Wyvratt
发明人： Mark Goulet , Peter J. Sinclair , Frederick Wong , Matthew J. Wyvratt
IPC分类号： C07H19/01 , A61K20060101 , A61K31/395 , A61K31/4178 , A61K31/4184 , A61K31/422 , A61K31/423 , A61K31/427 , A61K31/428 , A61K31/435 , A61K31/436 , A61K31/70 , A61K31/7056 , A61P37/06 , C07D20060101 , C07D498/12 , C07D498/18 , C07H7/06 , C07H15/04 , C07H19/02 , C07D491/16
CPC分类号： C07H19/01
摘要： Imidazolidyl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation 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 the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.
摘要翻译：一般结构式I的咪唑烷基大环内酯：通过在环己基环的C-3“和/或C-4”进行烷基化和/或芳基化，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，预防外来器官移植排斥和/或相关疾病，疾病和疾病。

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