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公开(公告)号:US07105682B2
公开(公告)日:2006-09-12
申请号:US10046622
申请日:2002-01-10
Applicant: Guoqing Chen , Jeffrey Adams , Jean Bemis , Lucian Di Pietro , Celia Dominguez , Daniel Elbaum , Julie Germain , Qi Huang , Joseph L. Kim , Xiaohu Ouyang , Vinod F. Patel , Leon M. Smith , Andrew Tasker , Ning Xi , Shimin Xu , Chester Chenguang Yuan , Michael Croghan , Tae-Seong Kim
Inventor: Guoqing Chen , Jeffrey Adams , Jean Bemis , Lucian Di Pietro , Celia Dominguez , Daniel Elbaum , Julie Germain , Qi Huang , Joseph L. Kim , Xiaohu Ouyang , Vinod F. Patel , Leon M. Smith , Andrew Tasker , Ning Xi , Shimin Xu , Chester Chenguang Yuan , Michael Croghan , Tae-Seong Kim
IPC: C07D401/02 , A61K31/44
CPC classification number: C07D401/14 , A61K31/00 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , Y02A50/401
Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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公开(公告)号:US10357481B2
公开(公告)日:2019-07-23
申请号:US15579878
申请日:2016-06-27
Applicant: MERCK SHARP & DOHME CORP. , Gregori J. Morriello , Lehua Chang , Ashley Forster , Yili Chen , Michael P. Dwyer , Zack Zhiqiang Guo , Ming Wang , Shimin Xu , Yingjian Bo , Jianmin Fu
Inventor: Gregori J. Morriello , Lehua Chang , Ashley Forster , Yili Chen , Michael P. Dwyer , Zack Zhiqiang Guo , Ming Wang , Shimin Xu , Yingjian Bo , Jianmin Fu
IPC: A61K31/4196 , C07D471/04 , C07D487/04 , A61P25/28 , A61P25/22 , A61P25/18 , A61P25/16 , A61P25/06 , A61K31/52
Abstract: The present invention is directed to substituted triazolo bicyclic compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
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公开(公告)号:US10287293B2
公开(公告)日:2019-05-14
申请号:US15736202
申请日:2016-06-27
Applicant: Merck Sharp & Dohme Corp. , Shawn J. Stachel , Christopher J. Sinz , Yili Chen , Jonathan E. Wilson , Michael P. Dwyer , Daniel V. Paone , Shimin Xu
Inventor: Shawn J. Stachel , Michael P. Dwyer , Christopher J. Sinz , Jonathan E. Wilson , Daniel V. Paone , Yili Chen , Shimin Xu
Abstract: The present invention is directed to dihydropyrazolopyrimidinone compounds of formulas (I) and (II) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
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公开(公告)号:US20180169072A1
公开(公告)日:2018-06-21
申请号:US15579878
申请日:2016-06-27
Applicant: Gregori J. MORRIELLO , Lehua CHANG , Ashley FORSTER , Yili CHEN , Michael P. DWYER , Zack Zhiqiang GUO , Ming WANG , Shimin XU , Yingjian BO , Jianmin FU , MERCK SHARP & DOHME CORP.
Inventor: Gregori J. MORRIELLO , Lehua CHANG , Ashley FORSTER , Yili CHEN , Michael P. DWYER , Zack Zhiqiang GUO , Ming WANG , Shimin XU , Yingjian BO , Jianmin FU
CPC classification number: A61K31/4196 , A61K31/52 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , C07D471/04 , C07D487/04
Abstract: The present invention is directed to substituted triazolo bicyclic compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
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25.
公开(公告)号:US20120065185A1
公开(公告)日:2012-03-15
申请号:US13297213
申请日:2011-11-15
Applicant: Guoqing CHEN , Jeffrey Adams , Jean Bemis , Shon Booker , Guolin Cai , Lucian Di Pietro , Celia Dominguez , Daniel Elbaum , Julie Germain , Stephanie Geuns-Meyer , Michael Handley , Qi Huang , Joseph L. Kim , Tae-Seong Kim , Alexander Kiselyov , Xiaohu Ouyang , Vinod F. Patel , Leon M. Smith , Markian Stec , Andrew Tasker , Ning Xi , Shimin Xu , Chester Chenguang Yuan , Michael Croghan
Inventor: Guoqing CHEN , Jeffrey Adams , Jean Bemis , Shon Booker , Guolin Cai , Lucian Di Pietro , Celia Dominguez , Daniel Elbaum , Julie Germain , Stephanie Geuns-Meyer , Michael Handley , Qi Huang , Joseph L. Kim , Tae-Seong Kim , Alexander Kiselyov , Xiaohu Ouyang , Vinod F. Patel , Leon M. Smith , Markian Stec , Andrew Tasker , Ning Xi , Shimin Xu , Chester Chenguang Yuan , Michael Croghan
IPC: A61K31/4436 , A61K31/4709 , A61K31/4725 , A61P3/00 , A61P7/00 , A61P35/00 , A61P31/00 , A61K31/444 , A61K31/5377
CPC classification number: C07D213/82 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/538 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/00 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
Abstract: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like.
Abstract translation: 所选择的杂环化合物对于预防和治疗诸如血管生成介导的疾病等疾病是有效的。 本发明包括新型化合物,类似物,前药及其药学上可接受的衍生物,用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。
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26.
公开(公告)号:US08026241B2
公开(公告)日:2011-09-27
申请号:US12367352
申请日:2009-02-06
Applicant: Chenera Balan , Yunxin Bo , Celia Dominguez , Christopher H. Fotsch , Vijay K. Gore , Vu Van Ma , Mark H. Norman , Vassil I. Ognyanov , Yi-xin Qian , Xianghong Wang , Ning Xi , Shimin Xu
Inventor: Chenera Balan , Yunxin Bo , Celia Dominguez , Christopher H. Fotsch , Vijay K. Gore , Vu Van Ma , Mark H. Norman , Vassil I. Ognyanov , Yi-xin Qian , Xianghong Wang , Ning Xi , Shimin Xu
IPC: A61K31/497 , C07D403/04 , C07D401/04
CPC classification number: C07D401/04 , C07D235/30 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14 , C07D471/04
Abstract: Therapeutic benzimidazoles and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotizing agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
Abstract translation: 治疗性苯并咪唑和含有它们的组合物,用于治疗急性,炎性和神经性疼痛,牙痛,一般头痛,偏头痛,丛集性头痛,混合血管和非血管综合征,紧张性头痛,一般炎症,关节炎,风湿性疾病,骨关节炎 ,炎症性肠病,炎症性眼病,炎症性或不稳定性膀胱病,银屑病,皮肤炎症成分炎症,慢性炎性病症,炎性疼痛及相关的痛觉过敏和异常性疼痛,神经性疼痛及相关的痛觉过敏和异常性疼痛,糖尿病性神经病疼痛,灼痛,交感神经痛 维持疼痛,输血综合征,哮喘,上皮组织损伤或功能障碍,单纯疱疹,呼吸道,泌尿生殖道,胃肠道或血管区内脏运动紊乱,伤口,烧伤,过敏性皮肤反应,瘙痒,白癜风,一般胃肠道疾病,胃溃疡 十二指肠溃疡,腹泻,坏死因子诱发的胃损伤,毛发生长,血管舒缩或过敏性鼻炎,支气管疾病或膀胱疾病。
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27.
公开(公告)号:US20110105498A1
公开(公告)日:2011-05-05
申请号:US12150158
申请日:2008-04-24
Applicant: Liping H. Pettus , Andrew Tasker , Shimin Xu , Ryan Wurz
Inventor: Liping H. Pettus , Andrew Tasker , Shimin Xu , Ryan Wurz
IPC: A61K31/5377 , C07D471/04 , A61K31/437 , A61P19/02 , A61P19/10 , A61P35/02 , A61P17/00 , A61P3/10 , A61P9/10 , A61P37/06 , A61P11/06 , A61P31/18 , A61P31/16 , A61P31/22 , A61P17/06 , A61P29/00 , C07D487/04 , A61K31/4985 , A61K31/496
CPC classification number: C07D471/04 , C07D487/04
Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R4, R5, R6 and Z are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of P38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
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公开(公告)号:US07759337B2
公开(公告)日:2010-07-20
申请号:US11367123
申请日:2006-03-02
Applicant: Andrew Tasker , Dawei Zhang , Guo-Qiang Cao , Partha Pratim Chakrabarti , James Richard Falsey , Bradley J. Herberich , Randall W. Hungate , Liping H. Pettus , Anthony Reed , Robert M. Rzasa , Kelvin K. C. Sham , Maya C. Thaman , Shimin Xu
Inventor: Andrew Tasker , Dawei Zhang , Guo-Qiang Cao , Partha Pratim Chakrabarti , James Richard Falsey , Bradley J. Herberich , Randall W. Hungate , Liping H. Pettus , Anthony Reed , Robert M. Rzasa , Kelvin K. C. Sham , Maya C. Thaman , Shimin Xu
IPC: C07D237/34 , C07D413/12 , C07D498/08 , C07D279/12 , C07D243/08 , A61K31/498 , A61K31/5355 , A61K31/537 , A61K31/541 , A61K31/551 , A61P29/00 , A61P23/00 , C07D487/04 , A61K31/4985
CPC classification number: C07D409/04 , C07D237/30 , C07D237/32 , C07D237/34 , C07D403/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D487/08 , C07D491/10
Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein B, R1, R2, R3, R4 and R5 are d.efined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
Abstract translation: 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病,包括炎症和相关病症的化合物。 该化合物具有通式I,其中B,R 1,R 2,R 3,R 4和R 5在本文中定义。 本发明还包括药物组合物,其包含一种或多种式I化合物,这些化合物和组合物用于治疗激酶介导的疾病包括类风湿性关节炎,牛皮癣和其它炎症疾病的用途,以及可用于制备 一级方程式
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29.
公开(公告)号:US20090012299A1
公开(公告)日:2009-01-08
申请号:US12151478
申请日:2008-05-06
Applicant: Liping Pettus , Andrew Tasker , Shimin Xu , Ryan Wurz
Inventor: Liping Pettus , Andrew Tasker , Shimin Xu , Ryan Wurz
IPC: C07D487/04
CPC classification number: C07D471/04
Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, A3, A4, B, R1, R2, R3, R4 and R5 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of P38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
Abstract translation: 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病,包括炎症和相关病症的化合物。 化合物具有通式I,其中A1,A2,A3,A4,B,R1,R2,R3,R4和R5如本文所定义。 本发明还包括药物组合物,其包含一种或多种式I化合物,用于治疗P38地图激酶介导的疾病(包括类风湿性关节炎,牛皮癣,慢性阻塞性肺病,疼痛和其它炎症性疾病)的这些化合物和组合物的用途以及中间体 和可用于制备式I化合物的方法。
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公开(公告)号:US07435823B2
公开(公告)日:2008-10-14
申请号:US11042634
申请日:2005-01-24
Applicant: Michele Potashman , Tae-Seong Kim , Steven Bellon , Shon Booker , Yuan Cheng , Joseph L. Kim , Andrew Tasker , Ning Xi , Shimin Xu , Jean-Christophe Harmange , George Borg , Matthew Weiss , Brian L. Hodous , Russell Graceffa , William H. Buckner , Craig E. Masse , Deborah Choquette , Matthew W. Martin , Julie Germain , Lucian V. DiPietro , Stuart C. Chaffee , Joseph J. Nunes , John L. Buchanan , Gregory J. Habgood , David C. McGowan , Douglas A. Whittington , Daniel La , Vinod F. Patel
Inventor: Michele Potashman , Tae-Seong Kim , Steven Bellon , Shon Booker , Yuan Cheng , Joseph L. Kim , Andrew Tasker , Ning Xi , Shimin Xu , Jean-Christophe Harmange , George Borg , Matthew Weiss , Brian L. Hodous , Russell Graceffa , William H. Buckner , Craig E. Masse , Deborah Choquette , Matthew W. Martin , Julie Germain , Lucian V. DiPietro , Stuart C. Chaffee , Joseph J. Nunes , John L. Buchanan , Gregory J. Habgood , David C. McGowan , Douglas A. Whittington , Daniel La , Vinod F. Patel
IPC: C07D215/38 , C07D265/34
CPC classification number: C07D213/64 , C07D213/81 , C07D215/233 , C07D215/38 , C07D215/48 , C07D215/54 , C07D237/34 , C07D239/34 , C07D239/47 , C07D239/84 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Abstract translation: 所选化合物对于预防和治疗诸如HGF介导的疾病等疾病是有效的。 本发明包括新颖的化合物,类似物,前药和药学上可接受的盐,用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。
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