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公开(公告)号：US20130225578A1
公开(公告)日：2013-08-29
申请号：US13819688
申请日：2011-08-31
IPC分类号： A61K31/517 , C07D403/14 , A61K31/5377 , C07D403/12 , C07D413/14 , A61K45/06 , C07D405/14
CPC分类号： A61K31/517 , A61K31/5377 , A61K45/06 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/14
摘要： Provided herein are 7-cyclylquinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
摘要翻译： 本文提供了用于治疗JAK激酶介导的疾病的7-环基喹唑啉化合物，包括JAK2激酶，JAK3激酶或TYK2激酶介导的疾病。 还提供了包含该化合物的药物组合物和使用该化合物和组合物的方法。
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公开(公告)号：US20130035326A1
公开(公告)日：2013-02-07
申请号：US13390911
申请日：2010-08-18
申请人： Sunny Abraham , Mark W. Holladay , Gang Liu , Shimin Xu
发明人： Sunny Abraham , Mark W. Holladay , Gang Liu , Shimin Xu
IPC分类号： C07D413/12 , C07D498/04 , A61K31/5383 , A61K31/4375 , C07D471/04 , C07D413/14 , A61K31/444 , A61K31/553 , A61K31/4545 , A61K31/506 , A61K31/5377 , A61K31/505 , C07D401/12 , A61K31/497 , A61K31/437 , A61K31/5513 , C07D239/42 , C07D401/04 , A61P29/00 , A61P37/00 , A61P35/00 , A61P35/02 , A61P37/06 , A61P17/02 , A61P13/12 , A61P17/06 , A61P37/08 , A61P11/00 , A61P19/02 , A61P25/00 , A61P19/10 , A61P11/06 , A61P37/02 , A61P31/00 , A61P3/10 , A61P1/00 , A61P1/04 , A61P19/04 , A61K31/4439
CPC分类号： C07D239/42 , A61K31/4353 , A61K31/4375 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/501 , A61K31/506 , A61K31/5375 , A61K31/5377 , A61K31/553 , C07D401/04 , C07D401/12 , C07D413/12 , C07D413/14 , C07D471/04 , C07D498/04
摘要： Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
摘要翻译： 本文提供了用于治疗KIT，CSF-1R和/或FLT3激酶介导的疾病的化合物。 还提供了包含该化合物的药物组合物和使用该化合物和组合物的方法。
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公开(公告)号：US20110118245A1
公开(公告)日：2011-05-19
申请号：US12933402
申请日：2009-03-17
申请人： Sunny Abraham , Shripad S. Bhagwat , Brian T. Campbell , Qi Chao , Raffaella Faraoni , Mark W. Holladay , Andiliy G. Lai , Martin W. Rowbottom , Eduardo Setti , Kelly G. Sprankle
发明人： Sunny Abraham , Shripad S. Bhagwat , Brian T. Campbell , Qi Chao , Raffaella Faraoni , Mark W. Holladay , Andiliy G. Lai , Martin W. Rowbottom , Eduardo Setti , Kelly G. Sprankle
IPC分类号： A61K31/517 , C07D413/12 , C07D491/056 , A61K31/519 , C07D413/14 , A61K31/5377 , C07D417/14 , A61K31/541 , C07D403/12 , C07D239/88 , C07D401/12 , A61P19/10 , A61P29/00 , A61P3/10 , A61P1/00 , A61P19/02 , A61P37/00 , A61P35/04
CPC分类号： C07D239/88 , A61K9/20 , A61K9/48 , A61K31/517 , A61K45/06 , C07D239/93 , C07D261/14 , C07D413/12
摘要： Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.
摘要翻译： 提供根据式（I）的化合物，组合物和方法用于调节RAF激酶（包括BRAF激酶）的活性，并用于治疗，预防或改善由RAF激酶介导的疾病或病症的一种或多种症状。 式（I）：或其药学上可接受的盐，溶剂合物，其水合物的包合物，其中X为O或S（O）t; Ra是O或S.
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公开(公告)号：US07919484B2
公开(公告)日：2011-04-05
申请号：US11815739
申请日：2006-02-08
申请人： Rajender Kamboj , Michael D. Winther , Robert Fraser , Mikhail Chafeev , Sultan Chowdhury , Jian-Min Fu , Duanjie Hou , Shifeng Liu , Vandna Raina , Mehran Seid Bagherzadeh , Serguei Sviridov , Kashinath Sadalapure , Shaoyi Sun , Vishnumurthy Kodumuru , Nagasree Chakka , Zaihui Zhang , Melwyn Abreo , Mikhail A. Kondratenko , Daniel F. Harvey , Cindy J. Hudson , Wenbao Li , Chi Tu , Sengen Sun , Mark W. Holladay , Heinz W. Gschwend
发明人： Rajender Kamboj , Michael D. Winther , Robert Fraser , Mikhail Chafeev , Sultan Chowdhury , Jian-Min Fu , Duanjie Hou , Shifeng Liu , Vandna Raina , Mehran Seid Bagherzadeh , Serguei Sviridov , Kashinath Sadalapure , Shaoyi Sun , Vishnumurthy Kodumuru , Nagasree Chakka , Zaihui Zhang , Melwyn Abreo , Mikhail A. Kondratenko , Daniel F. Harvey , Cindy J. Hudson , Wenbao Li , Chi Tu , Sengen Sun , Mark W. Holladay , Heinz W. Gschwend
IPC分类号： A61K31/501 , C07D211/34
CPC分类号： A61K31/64 , A61K31/00 , A61K31/4439 , A61K38/28 , A61K45/06 , A61K2300/00
摘要： This invention is directed to the use of SCD-1 inhibitors of the formula (I): where x, y, V, W, G, J, L, M, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein, in combination with other drug therapies to treat adverse weight gain.
摘要翻译： 本发明涉及式（I）的SCD-1抑制剂的用途：其中x，y，V，W，G，J，L，M，R2，R3，R5，R5a，R6，R6a，R7， 本文定义R7a，R8和R8a与其他药物治疗组合以治疗不利的体重增加。
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公开(公告)号：US20090030008A1
公开(公告)日：2009-01-29
申请号：US12247792
申请日：2008-10-08
申请人： Serguei Sviridov , Vishnumurthy Kodumuru , Shifeng Liu , Melwyn Abreo , Michael D. Winther , Heinz W. Gschwend , Rajender Kamboj , Shaoyi Sun , Mark W. Holladay , Wenbao Li , Chi Tu
发明人： Serguei Sviridov , Vishnumurthy Kodumuru , Shifeng Liu , Melwyn Abreo , Michael D. Winther , Heinz W. Gschwend , Rajender Kamboj , Shaoyi Sun , Mark W. Holladay , Wenbao Li , Chi Tu
IPC分类号： A61K31/496 , C07D403/04 , A61P3/04 , A61P3/10
CPC分类号： A61K31/551 , A61K31/00 , A61K31/501 , C07D237/20 , C07D403/08 , C07D405/08 , C07D409/12 , C07D413/08
摘要： Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where G, J, L, M, x, y, W, V, R2, R3, R4, R5, R6, R7, R8, R8a, R9, R9a, R10, R10a, R11 and R11a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
摘要翻译： 公开了在哺乳动物，优选人中治疗SCD介导的疾病或病症的方法，其中所述方法包括向有需要的哺乳动物施用式（I）化合物：其中G，J，L，M，x ，Y，W，V，R2，R3，R4，R5，R6，R7，R8，R8a，R9，R9a，R10，R10a，R11和R11a。 还公开了包含式（I）化合物的药物组合物。
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公开(公告)号：US07335658B2
公开(公告)日：2008-02-26
申请号：US10901563
申请日：2004-07-29
申请人： Nagasree Chakka , Mikhail Chafeev , Sultan Chowdhury , Jian-Min Fu , Duanjie Hou , Rajender Kamboj , Vishnumurthy Kodumuru , Shifeng Liu , Vandna Raina , Shaoyi Sun , Serguei Sviridov , Michael D Winther , Zaihui Zhang , Melwyn Abreo , Mark W Holladay , Wenbao Li , Sengen Sun , Chi Tu , Heinz W Gschwend
发明人： Nagasree Chakka , Mikhail Chafeev , Sultan Chowdhury , Jian-Min Fu , Duanjie Hou , Rajender Kamboj , Vishnumurthy Kodumuru , Shifeng Liu , Vandna Raina , Shaoyi Sun , Serguei Sviridov , Michael D Winther , Zaihui Zhang , Melwyn Abreo , Mark W Holladay , Wenbao Li , Sengen Sun , Chi Tu , Heinz W Gschwend
IPC分类号： C07D403/04 , C07D403/14 , A61K31/497
CPC分类号： A61K31/00 , A61K31/501 , A61K31/551 , C07D237/20 , C07D237/24
摘要： Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
摘要翻译： 公开了在哺乳动物，优选人中治疗SCD介导的疾病或病症的方法，其中所述方法包括向有需要的哺乳动物施用式（I）化合物：其中x，y，W，V，R R 2，R 3，R 4，R 5，R 6，R 6，R 4， R 6a，R 7，R 7a，R 8，R 8a，R 8，R 7， 本文定义了9和9和9 9。 还公开了包含式（I）化合物的药物组合物。
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公开(公告)号：US06645968B2
公开(公告)日：2003-11-11
申请号：US09777217
申请日：2001-02-05
申请人： Robert J. Altenbach , Hao Bai , Jorge D. Brioni , William A. Carroll , Murali Gopalakrishnan , Robert J. Gregg , Mark W. Holladay , Peggy P. Huang , John F. Kincaid , Michael E. Kort , Philip R. Kym , John K. Lynch , Arturo Perez-Medrano , Henry Q. Zhang
发明人： Robert J. Altenbach , Hao Bai , Jorge D. Brioni , William A. Carroll , Murali Gopalakrishnan , Robert J. Gregg , Mark W. Holladay , Peggy P. Huang , John F. Kincaid , Michael E. Kort , Philip R. Kym , John K. Lynch , Arturo Perez-Medrano , Henry Q. Zhang
IPC分类号： A61K314406
CPC分类号： C07D213/40 , A61K31/17 , A61K31/275 , A61K31/4406 , C07C233/78 , C07C233/83 , C07C271/22 , C07C275/28 , C07C275/30 , C07C279/28 , C07C279/36 , C07C335/16 , C07C335/18 , C07D209/08 , C07D213/74 , C07D213/75 , C07D213/82 , C07D215/38 , C07D233/42 , C07D233/84 , C07D235/06 , C07D239/42 , C07D333/20 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12
摘要： Compounds of formula I: are useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of opening potassium channels in a mammal.
摘要翻译： 式I化合物可用于治疗用钾通道开放剂预防或改善的疾病。 还公开了钾通道开放组合物和在哺乳动物中开放钾通道的方法。
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公开(公告)号：US06503935B1
公开(公告)日：2003-01-07
申请号：US09364901
申请日：1999-07-29
申请人： Robert J. Altenbach , Michael D. Meyer , James F. Kerwin, Jr. , Mark W. Holladay , Albert Khilevich , Teodozyj Kolasa , Jeffrey Rohde , William A. Carroll
发明人： Robert J. Altenbach , Michael D. Meyer , James F. Kerwin, Jr. , Mark W. Holladay , Albert Khilevich , Teodozyj Kolasa , Jeffrey Rohde , William A. Carroll
IPC分类号： A61K31425
CPC分类号： C07D233/64 , C07D233/84 , C07D401/12 , C07D403/12 , C07D405/04 , C07D409/12 , C07D417/12
摘要： Compounds having formula I: are useful in treating diseases prevented by or ameliorated with &agr;1A agonists. Also disclosed are &agr;1A agonist compositions and a method of activating &agr;1 adrenoceptors in a mammal.
摘要翻译： 具有式I的化合物可用于治疗由α1A激动剂预防或改善的疾病。 还公开了α1A激动剂组合物和在哺乳动物中激活α1肾上腺素受体的方法。
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公开(公告)号：US08633207B2
公开(公告)日：2014-01-21
申请号：US13222937
申请日：2011-08-31
IPC分类号： A01N43/54 , A61K31/517 , C07D239/72 , C07D401/00
CPC分类号： C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： Provided herein are quinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
摘要翻译： 本文提供了用于治疗JAK激酶介导的疾病的喹唑啉化合物，包括JAK2激酶，JAK3激酶或TYK2激酶介导的疾病。 还提供了包含该化合物的药物组合物和使用该化合物和组合物的方法。
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公开(公告)号：US08618289B2
公开(公告)日：2013-12-31
申请号：US12933402
申请日：2009-03-17
申请人： Sunny Abraham , Shripad S. Bhagwat , Brian T. Campbell , Qi Chao , Raffaella Faraoni , Mark W. Holladay , Andiliy G. Lai , Martin W. Rowbottom , Eduardo Setti , Kelly G. Sprankle
发明人： Sunny Abraham , Shripad S. Bhagwat , Brian T. Campbell , Qi Chao , Raffaella Faraoni , Mark W. Holladay , Andiliy G. Lai , Martin W. Rowbottom , Eduardo Setti , Kelly G. Sprankle
IPC分类号： C07D239/70 , A01N43/54
CPC分类号： C07D239/88 , A61K9/20 , A61K9/48 , A61K31/517 , A61K45/06 , C07D239/93 , C07D261/14 , C07D413/12
摘要： Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.
摘要翻译： 提供根据式（I）的化合物，组合物和方法用于调节RAF激酶（包括BRAF激酶）的活性，并用于治疗，预防或改善由RAF激酶介导的疾病或病症的一种或多种症状。 式（I）：或其药学上可接受的盐，溶剂合物，其水合物的包合物，其中X为O或S（O）t; Ra是O或S.
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