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11.发明授权
公开(公告)号：US5914328A
公开(公告)日：1999-06-22
申请号：US485537
申请日：1995-06-07
申请人： Nan-Horng Lin , Mark W. Holladay , Melwyn A. Abreo , David E. Gunn , Suzanne A. Lebold , Richard L. Elliott , Yun He
发明人： Nan-Horng Lin , Mark W. Holladay , Melwyn A. Abreo , David E. Gunn , Suzanne A. Lebold , Richard L. Elliott , Yun He
IPC分类号： C07D401/12 , C07D403/12 , C07D417/12 , A61K31/425 , A61K31/495 , A61K31/50 , A61K31/505
CPC分类号： C07D401/12 , C07D403/12 , C07D417/12
摘要： Novel heterocyclic ether compounds of the formula: ##STR1## wherein *, A,B, n, R.sup.1, R.sup.2 and X are specifically defined, or pharmaceutically-acceptable salts or prodrugs thereof, which are useful in selectively activating or inhibiting neurotransmitter release; to therapeutically-effective pharmaceutical compositions of these compounds; and to the use of said compositions to activate or inhibit neurotransmitter release in mammals.
摘要翻译： 具有下式的新型杂环醚化合物：其中*，A，B，n，R 1，R 2和X具体定义，或其药学上可接受的盐或前药，其可用于选择性活化或抑制神经递质释放; 到这些化合物的治疗有效的药物组合物; 以及使用所述组合物来激活或抑制哺乳动物中的神经递质释放。
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公开(公告)号：US06593335B1
公开(公告)日：2003-07-15
申请号：US09338889
申请日：1999-06-23
申请人： William A. Carroll , Yiyuan Chen , Mark W. Holladay , Michael E. Kort , Philip R. Kym , James P. Sullivan , Rui Tang , Lin Yi , Henry Q. Zhang , Irene Drizin
发明人： William A. Carroll , Yiyuan Chen , Mark W. Holladay , Michael E. Kort , Philip R. Kym , James P. Sullivan , Rui Tang , Lin Yi , Henry Q. Zhang , Irene Drizin
IPC分类号： A61K314365
CPC分类号： C07D221/04 , C07C45/00 , C07C45/298 , C07C45/41 , C07C45/63 , C07C45/71 , C07C205/44 , C07D215/36 , C07D495/04 , C07D495/14 , C07C47/565 , C07C47/55 , C07C49/753
摘要： Compounds having the 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： 具有式I的化合物可用于治疗由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：US06265417B1
公开(公告)日：2001-07-24
申请号：US09206055
申请日：1998-12-04
IPC分类号： A61K3147
CPC分类号： C07D221/04 , C07C45/298 , C07D215/36 , C07D495/04 , C07D495/14 , C07C47/55
摘要： Compounds having the formula 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： 具有该化学式的化合物可用于治疗由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：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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16.发明申请OPTICALLY ACTIVE PYRAZOLYLAMINOQUINAZOLINE, AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF 有权光学活性的吡唑啉氨基胆碱和药物组合物及其使用方法公开(公告)号：US20120053193A1
公开(公告)日：2012-03-01
申请号：US13222963
申请日：2011-08-31
申请人： Mark W. Holladay , Eduardo Setti
发明人： Mark W. Holladay , Eduardo Setti
IPC分类号： A61K31/517 , A61P35/00 , A61P35/02 , C07D401/12
CPC分类号： A61K31/517 , B01D15/3833 , C07D403/12
摘要： Provided herein is an optically active pyrazolylaminoquinazoline, and pharmaceutical compositions thereof. Also provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a JAK-mediated condition, disorder, or disease. Further provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a proliferative disease, inflammatory disease, or renal disease.
摘要翻译： 本文提供光学活性吡唑基氨基喹唑啉及其药物组合物。 本文还提供了治疗，预防或改善JAK介导的病症，病症或疾病的一种或多种症状的方法。 本文还提供了治疗，预防或改善增殖性疾病，炎性疾病或肾脏疾病的一种或多种症状的方法。
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公开(公告)号：US20120053174A1
公开(公告)日：2012-03-01
申请号：US13222937
申请日：2011-08-31
IPC分类号： A61K31/5377 , A61K31/517 , C07D403/14 , C07D405/14 , A61P37/02 , C07D413/14 , A61P35/00 , A61P29/00 , A61P37/06 , C07D401/14 , C07D417/14
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：US07749980B2
公开(公告)日：2010-07-06
申请号：US10576859
申请日：2004-10-21
申请人： Robert Plourde, Jr. , Sammy R. Shaver , Melwyn Anthony Abreo , Lorenzo Josue Alfaro-Lopez , Yangbo Feng , Tatyana V. Khasanova , Mark W. Holladay , Christopher S. Crean
发明人： Robert Plourde, Jr. , Sammy R. Shaver , Melwyn Anthony Abreo , Lorenzo Josue Alfaro-Lopez , Yangbo Feng , Tatyana V. Khasanova , Mark W. Holladay , Christopher S. Crean
CPC分类号： A61K31/519 , A61K31/52
摘要： The present invention is directed to a method of treating pain. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a P2X receptor antagonist. The methods of the present invention are useful in reducing pain, such as traumatic pain, neuropathic pain, organ pain and/or pain associated with diseases. The P2X receptor antagonists useful for this invention are non-nucleotide compounds of general Formula I. Compounds of Formula I can be used alone to treat pain. Compounds of Formula I can also be used in conjunction with other therapeutic agents or adjunctive therapies commonly used to treat pain, thus enhancing the therapeutic effect of pain reduction.
摘要翻译： 本发明涉及治疗疼痛的方法。 该方法包括向受试者施用包含有效量的P2X受体拮抗剂的药物组合物。 本发明的方法可用于减少疼痛，例如创伤性疼痛，神经性疼痛，器官疼痛和/或与疾病相关的疼痛。 可用于本发明的P2X受体拮抗剂是通式I的非核苷酸化合物。式I化合物可单独用于治疗疼痛。 式I化合物也可以与通常用于治疗疼痛的其它治疗剂或辅助疗法结合使用，从而增强疼痛减轻的治疗效果。
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公开(公告)号：US07456180B2
公开(公告)日：2008-11-25
申请号：US10567009
申请日：2004-07-29
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： A61K31/497 , C07D241/02
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，R 2，R 3，R 4，R 5，R SUP > 6，R 7，R 8，R 8a，R 9，R SUP， > 9a，R 10，R 10a，R 11和R 11是本文定义的 。 还公开了包含式（I）化合物的药物组合物。
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20.发明授权Optically active pyrazolylaminoquinazoline, and pharmaceutical compositions and methods of use thereof 有权光学活性吡唑基氨基喹唑啉，及其药物组合物及其使用方法公开(公告)号：US08912324B2
公开(公告)日：2014-12-16
申请号：US13222963
申请日：2011-08-31
申请人： Mark W. Holladay , Eduardo Setti
发明人： Mark W. Holladay , Eduardo Setti
IPC分类号： C07D417/00 , C07D419/00 , C07D403/12 , A61K31/517
CPC分类号： A61K31/517 , B01D15/3833 , C07D403/12
摘要： Provided herein is an optically active pyrazolylaminoquinazoline, and pharmaceutical compositions thereof. Also provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a JAK-mediated condition, disorder, or disease. Further provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a proliferative disease, inflammatory disease, or renal disease.
摘要翻译： 本文提供光学活性吡唑基氨基喹唑啉及其药物组合物。 本文还提供了治疗，预防或改善JAK介导的病症，病症或疾病的一种或多种症状的方法。 本文还提供了治疗，预防或改善增殖性疾病，炎性疾病或肾脏疾病的一种或多种症状的方法。
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