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公开(公告)号：US09315475B2
公开(公告)日：2016-04-19
申请号：US14021930
申请日：2013-09-09
申请人： Christian Beaulieu , David J. Bennett , Christopher J. Bungard , Ronald K. Chang , Sheldon Crane , Thomas J. Greshock , Li Hao , Kate Holloway , Jesse J. Manikowski , John A. McCauley , Daniel McKay , Carmela Molinaro , Oscar Miguel Moradei , Philippe G. Nantermet , Christian Nadeau , Satyanarayana Tummanapalli , William Shipe , Sanjay Kumar Singh , Vouy Linh Truong , Sivalenka Vijayasaradhi , Peter D. Williams , Catherine M. Wiscount
发明人： Christian Beaulieu , David J. Bennett , Christopher J. Bungard , Ronald K. Chang , Sheldon Crane , Thomas J. Greshock , Li Hao , Kate Holloway , Jesse J. Manikowski , John A. McCauley , Daniel McKay , Carmela Molinaro , Oscar Miguel Moradei , Philippe G. Nantermet , Christian Nadeau , Satyanarayana Tummanapalli , William Shipe , Sanjay Kumar Singh , Vouy Linh Truong , Sivalenka Vijayasaradhi , Peter D. Williams , Catherine M. Wiscount
IPC分类号： C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D265/30 , C07D487/04 , C07D493/04 , A61K31/5375 , A61K31/5377 , A61K31/695 , A61K45/06 , C07F7/08
CPC分类号： C07D265/30 , A61K31/5375 , A61K31/5377 , A61K31/695 , A61K45/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/04 , C07D493/04 , C07F7/0814
摘要： The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译： 式I所包括的化合物包括可以在体内代谢为HIV蛋白酶抑制剂的HIV蛋白酶抑制剂和其它化合物的化合物。 化合物及其药学上可接受的盐可用于预防或治疗HIV感染以及预防，治疗或延迟艾滋病的发病。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。
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公开(公告)号：US08642799B2
公开(公告)日：2014-02-04
申请号：US13861046
申请日：2013-04-11
IPC分类号： C07C255/04 , A61K31/275
CPC分类号： C07C255/60 , A61K31/277 , A61K31/4418 , A61K31/5375 , A61K45/06 , C07C255/44 , C07C255/46 , C07C311/37 , C07C317/32 , C07C323/32 , C07C2601/02 , C07D207/335 , C07D213/36 , C07D213/38 , C07D213/57 , C07D213/89 , C07D271/06 , C07D295/135 , C07D295/185 , C07D295/192 , Y02A50/486
摘要： Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, stronglyoidiasis, trichostrongyliasis, trichomoniasis or cestodiasis.
摘要翻译： 负责哺乳动物疾病的几种寄生虫依赖于各种生命周期功能的半胱氨酸蛋白酶。 这些蛋白酶的抑制或降低功能可用于治疗和/或预防这些寄生虫病，包括： 弓形虫病，疟疾，非洲锥虫病，恰加斯病，利什曼病，血吸虫病，阿米巴病，贾第鞭毛虫病，鞭毛虫病，op病，疟原虫病，筋膜ias病，淋巴丝虫病，盘尾丝虫病，麦地那龙线虫病，蛔虫病，绦虫病，强类病，毛滴虫病，毛滴虫病或绦虫病。
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3.发明申请CYSTEINE PROTEASE INHIBITORS FOR THE TREATMENT OF PARASITIC DISEASES 有权CYSTEINE PROTEASE抑制剂治疗PARASITIC疾病公开(公告)号：US20130244962A1
公开(公告)日：2013-09-19
申请号：US13861046
申请日：2013-04-11
IPC分类号： C07C255/60 , A61K45/06 , A61K31/5375 , C07D295/192 , A61K31/4418 , A61K31/277 , C07D213/36
CPC分类号： C07C255/60 , A61K31/277 , A61K31/4418 , A61K31/5375 , A61K45/06 , C07C255/44 , C07C255/46 , C07C311/37 , C07C317/32 , C07C323/32 , C07C2601/02 , C07D207/335 , C07D213/36 , C07D213/38 , C07D213/57 , C07D213/89 , C07D271/06 , C07D295/135 , C07D295/185 , C07D295/192 , Y02A50/486
摘要： Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, stronglyoidiasis, trichostrongyliasis, trichomoniasis or cestodiasis.
摘要翻译： 负责哺乳动物疾病的几种寄生虫依赖于各种生命周期功能的半胱氨酸蛋白酶。 这些蛋白酶的抑制或降低功能可用于治疗和/或预防这些寄生虫病，包括： 弓形虫病，疟疾，非洲锥虫病，恰加斯病，利什曼病，血吸虫病，阿米巴病，贾第鞭毛虫病，鞭毛虫病，op病，疟原虫病，筋膜ias病，淋巴丝虫病，盘尾丝虫病，麦地那龙线虫病，蛔虫病，绦虫病，强类病，毛滴虫病，毛滴虫病或绦虫病。
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4.发明申请CATHEPSIN CYSTEINE PROTEASE INHIBITORS FOR THE TREATMENT OF VARIOUS DISEASES 审中-公开用于治疗各种疾病的CATHEPSIN CYSTEINE蛋白酶抑制剂公开(公告)号：US20120101053A1
公开(公告)日：2012-04-26
申请号：US13379200
申请日：2010-06-16
申请人： Cameron Black , Christian Beaulieu
发明人： Cameron Black , Christian Beaulieu
IPC分类号： A61K31/7048 , A61K31/4168 , A61K31/522 , A61K31/351 , A61K31/497 , A61K31/661 , A61K31/663 , A61K31/675 , A61K31/4706 , A61K31/4709 , A61K31/506 , A61K31/65 , A61K31/4355 , A61K31/366 , A61K31/29 , A61K31/4985 , A61K31/47 , A61K31/53 , A61K31/165 , A61K31/429 , A61K31/433 , C07C233/40 , C07D277/76 , C07D285/125 , A61P33/02 , A61P33/06 , A61K31/541
CPC分类号： C07D277/76 , C07C255/29 , C07C255/41 , C07C317/32 , C07C317/48 , C07C323/60 , C07C2601/02 , C07C2601/10 , C07D277/36 , C07D285/125 , C07D333/28 , Y02A50/488
摘要： The present invention relates to compounds capable of inhibiting and/or decreasing the activity of one or more cathepsins, thereby treating and/or preventing various disease states associated with one or more cysteine proteases including, but not limited to, cathepsins and papain-like cysteine proteases. Disease states treated and/or prevented by the compounds of the invention include, but are not limited to, mammalian parasitic diseases in which the parasite utilizes a critical cysteine protease from the papain family. Examples of parasitic diseases to be treated or prevented by the compounds of the invention include, but are not limited to, toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, coccidiosis, giardiosis, cryptosporidiosis or schistosomiasis.
摘要翻译： 本发明涉及能够抑制和/或降低一种或多种组织蛋白酶的活性的化合物，从而治疗和/或预防与一种或多种半胱氨酸蛋白酶相关的各种疾病状态，包括但不限于组织蛋白酶和木瓜蛋白酶样半胱氨酸 蛋白酶。 本发明化合物治疗和/或预防的疾病状态包括但不限于哺乳动物寄生虫病，其中寄生虫利用来自木瓜蛋白酶家族的关键半胱氨酸蛋白酶。 本发明化合物治疗或预防的寄生虫病的实例包括但不限于弓形虫病，疟疾，非洲锥虫病，恰加斯病，利什曼病，球虫病，流感病，隐孢子虫病或血吸虫病。
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公开(公告)号：US20050154044A1
公开(公告)日：2005-07-14
申请号：US11007009
申请日：2004-12-08
申请人： Christian Beaulieu , Daniel Guay , Zhaoyin Wang , Robert Zamboni
发明人： Christian Beaulieu , Daniel Guay , Zhaoyin Wang , Robert Zamboni
IPC分类号： A61K31/403 , A61P11/02 , A61P11/06 , A61P29/00 , C07D209/88 , C07D209/94
CPC分类号： C07D209/94 , C07D209/88
摘要： The present invention provides substituted tetrahydrocarbazole and cyclopentanoindole derivatives as antagonists of DP receptor, and as such are useful for the treatment of prostaglandin D2 mediated diseases such as rhinitis, asthma and nasal congestion.
摘要翻译： 本发明提供取代的四氢咔唑和环戊烯吲哚衍生物作为DP受体的拮抗剂，因此可用于治疗前列腺素D2介导的疾病如鼻炎，哮喘和鼻塞。
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公开(公告)号：US09586931B2
公开(公告)日：2017-03-07
申请号：US14431895
申请日：2013-09-24
申请人： Michelle R. Machacek , Eric T. Romeo , Solomon D. Kattar , Matthew Christopher , Michael D. Altman , Alan B. Northrup , John Michael Ellis , Brendan O'Boyle , Anthony Donofrio , Jonathan Grimm , Michael H. Reutershan , Kaleen Konrad Childers , Ryan D. Otte , Brandon Cash , Yves Ducharme , Andrew M. Haidle , Kerrie Spencer , Dilrukshi Vitharana , Lingyun Wu , Li Zhang , Peng Zhang , Christian Beaulieu , Daniel Guay
发明人： Michelle R. Machacek , Eric T. Romeo , Solomon D. Kattar , Matthew Christopher , Michael D. Altman , Alan B. Northrup , John Michael Ellis , Brendan O'Boyle , Anthony Donofrio , Jonathan Grimm , Michael H. Reutershan , Kaleen Konrad Childers , Ryan D. Otte , Brandon Cash , Yves Ducharme , Andrew M. Haidle , Kerrie Spencer , Dilrukshi Vitharana , Lingyun Wu , Li Zhang , Peng Zhang , Christian Beaulieu , Daniel Guay
IPC分类号： A61K9/10 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D498/04 , C07D413/14 , C07D239/42 , A61K9/00 , A61K9/20 , A61K9/48 , C07D403/12 , C07D405/12 , C07D409/12 , C07D471/04
CPC分类号： C07D401/14 , A61K9/0019 , A61K9/0073 , A61K9/0075 , A61K9/10 , A61K9/2027 , A61K9/4858 , C07D239/42 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04
摘要： Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
摘要翻译： 提供式I的三唑衍生物，其是脾脏酪氨酸激酶和药物组合物的有效抑制剂。 三唑衍生物可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。
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公开(公告)号：US20150239866A1
公开(公告)日：2015-08-27
申请号：US14431895
申请日：2013-09-24
申请人： Michelle R. MACHACEK , Eric T. ROMEO , Solomon D. KATTAR , Matthew CHRISTOPHER , Michael D. ALTMAN , Alan B. NORTHRUP , John Michael ELLIS , Brendan O BOYLE , Anthony DONOFRIO , Jonathan GRIMM , Michael H. REUTERSHAN , Kaleen Konrad CHILDERS , Ryan D. OTTE , Brandon CASH , Yves DUCHARME , Andrew M. HAIDLE , Kerrie SPENCER , Dilrukshi VITHARANA , Lingyun WU , Li ZHANG , Peng ZHANG , Christian BEAULIEU , Daniel GUAY
发明人： Michelle R. Machacek , Eric T. Romeo , Solomon D. Kattar , Matthew Christopher , Michael D. Altman , Alan B. Northrup , John Michael Ellis , Brendan O'Boyle , Anthony Donofrio , Jonathan Grimm , Michael H. Reutershan , Kaleen Konrad Childers , Ryan D. Otte , Brandon Cash , Yves Ducharme , Andrew M. Haidle , Kerrie Spencer , Dilrukshi Vitharana , Lingyun Wu , Li Zhang , Peng Zhang , Christian Beaulieu , Daniel Guay
IPC分类号： C07D401/14 , C07D471/04 , C07D405/14 , C07D413/14 , C07D498/04 , C07D409/14 , C07D417/14
CPC分类号： C07D401/14 , A61K9/0019 , A61K9/0073 , A61K9/0075 , A61K9/10 , A61K9/2027 , A61K9/4858 , C07D239/42 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04
摘要： Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
摘要翻译： 提供式I的三唑衍生物，其是脾脏酪氨酸激酶和药物组合物的有效抑制剂。 三唑衍生物可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。
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公开(公告)号：US20140200197A1
公开(公告)日：2014-07-17
申请号：US14021930
申请日：2013-09-09
申请人： JOHN A. MCCAULEY , CHRISTIAN BEAULIEU , DAVID J. BENNETT , CHRISTOPHER J. BUNGARD , RONALD K. CHANG , SHELDON CRANE , THOMAS J. GRESHOCK , LI HAO , KATE HOLLOWAY , JESSE J. MANIKOWSKI , DANIEL MCKAY , CARMELA MOLINARO , OSCAR MIGUEL MORADEI , PHILIPPE G. NANTERMET , CHRISTIAN NADEAU , TUMMANAPALLI SATYANARAYANA , WILLIAM SHIPE , SANJAY KUMAR SINGH , VOUY LINH TRUONG , SIVALENKA VIJAYARADHI , PETER D. WILLIAMS , CATHERINE M. WISCOUNT
发明人： JOHN A. MCCAULEY , CHRISTIAN BEAULIEU , DAVID J. BENNETT , CHRISTOPHER J. BUNGARD , RONALD K. CHANG , SHELDON CRANE , THOMAS J. GRESHOCK , LI HAO , KATE HOLLOWAY , JESSE J. MANIKOWSKI , DANIEL MCKAY , CARMELA MOLINARO , OSCAR MIGUEL MORADEI , PHILIPPE G. NANTERMET , CHRISTIAN NADEAU , TUMMANAPALLI SATYANARAYANA , WILLIAM SHIPE , SANJAY KUMAR SINGH , VOUY LINH TRUONG , SIVALENKA VIJAYARADHI , PETER D. WILLIAMS , CATHERINE M. WISCOUNT
IPC分类号： C07D265/30 , A61K45/06 , C07D413/12 , A61K31/695 , C07D413/06 , C07D417/12 , C07D487/04 , C07F7/08 , A61K31/5375 , A61K31/5377
CPC分类号： C07D265/30 , A61K31/5375 , A61K31/5377 , A61K31/695 , A61K45/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/04 , C07D493/04 , C07F7/0814
摘要： The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译： 式I所包括的化合物包括可以在体内代谢为HIV蛋白酶抑制剂的HIV蛋白酶抑制剂和其它化合物的化合物。 化合物及其药学上可接受的盐可用于预防或治疗HIV感染以及预防，治疗或延迟艾滋病的发病。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。
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![Dihydropyrrolo[1,2-a]indole and tetrahydropyrido[1,2-a]-indole derivatives as prostaglandin d2 receptor antagonists](/abs-image/US/2006/12/05/US07144913B2/abs.jpg.150x150.jpg)
9.发明授权Dihydropyrrolo[1,2-a]indole and tetrahydropyrido[1,2-a]-indole derivatives as prostaglandin d2 receptor antagonists 有权二氢吡咯并[1,2-a]吲哚和四氢吡啶并[1,2-a] - 吲哚衍生物作为前列腺素d2受体拮抗剂公开(公告)号：US07144913B2
公开(公告)日：2006-12-05
申请号：US10474929
申请日：2002-05-22
申请人： Zhaoyin Wang , Christian Beaulieu , Claude Dufresne , Daniel Guay , Yves LeBlanc
发明人： Zhaoyin Wang , Christian Beaulieu , Claude Dufresne , Daniel Guay , Yves LeBlanc
IPC分类号： A61K31/40 , C07D487/00
CPC分类号： C07D471/04 , C07D487/04
摘要： Dihydropyrroloindoles and tetrahydropyridoindoles are prostaglandin receptor antagonists useful for the treatment of prostaglandin-mediated diseases such as allergic rhinitis, nasal congestion and asthma.
摘要翻译： 二氢吡咯并吲哚和四氢吡啶并吲哚是用于治疗前列腺素介导的疾病如过敏性鼻炎，鼻塞和哮喘的前列腺素受体拮抗剂。
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10.发明申请公开(公告)号：US20100179173A1
公开(公告)日：2010-07-15
申请号：US12663556
申请日：2008-06-26
申请人： Daniel Guay , Christian Beaulieu , Michel Belley , Sheldon N. Crane , Jeancarlo De Luca , Rejean Fortin , Yves Gareau , Lianhai Li , Michel Therien , Geoffrey K. Tranmer , Vouy Linh Truong , Zhaoyin Wang
发明人： Daniel Guay , Christian Beaulieu , Michel Belley , Sheldon N. Crane , Jeancarlo De Luca , Rejean Fortin , Yves Gareau , Lianhai Li , Michel Therien , Geoffrey K. Tranmer , Vouy Linh Truong , Zhaoyin Wang
IPC分类号： A61K31/519 , C07D471/04 , A61P3/10
CPC分类号： C07D471/04
摘要： Fused pyrimidine compounds of structural formula (I) are effective as antagonists of the biological activity of the GPR105 protein. They are useful for the treatment, control or prevention of disorders responsive to antagonism of this receptor, such as diabetes, particularly, Type 2 diabetes, insulin resistance, hyperglycemia, lipid disorders, obesity, atherosclerosis, and Metabolic Syndrome.
摘要翻译： 结构式（I）的稠合嘧啶化合物作为GPR105蛋白质的生物活性的拮抗剂是有效的。 它们可用于治疗，控制或预防对该受体的拮抗作用有响应的病症，例如糖尿病，特别是2型糖尿病，胰岛素抵抗，高血糖症，脂质障碍，肥胖，动脉粥样硬化和代谢综合征。
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