专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US08232293B2 Crystalline forms of a potent HCV inhibitor 有权
标题翻译：有效的HCV抑制剂的结晶形式
公开(公告)号：US08232293B2
公开(公告)日：2012-07-31
申请号：US12559927
申请日：2009-09-15
申请人： Thilo Berkenbusch , Carl Alan Busacca , Burkhard Jaeger , Richard J. Varsolona
发明人： Thilo Berkenbusch , Carl Alan Busacca , Burkhard Jaeger , Richard J. Varsolona
IPC分类号： A61K31/4709 , A61K31/427 , A61K31/4025 , C07D215/233 , C07D417/14 , C07D207/12
CPC分类号： C07D417/14
摘要： This invention relates to novel crystalline forms of the following Compound (1), and the sodium salt thereof, and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection:
摘要翻译：本发明涉及以下化合物（1）的新型结晶形式及其钠盐及其制备方法，其药物组合物及其在治疗丙型肝炎病毒（HCV）感染中的用途：

2. 发明授权

US08362035B2 Crystalline forms of a potent HCV inhibitor 有权
标题翻译：有效的HCV抑制剂的结晶形式
公开(公告)号：US08362035B2
公开(公告)日：2013-01-29
申请号：US13541158
申请日：2012-07-03
申请人： Thilo Berkenbusch , Carl Alan Busacca , Burkhard Jaeger , Richard J. Varsolona
发明人： Thilo Berkenbusch , Carl Alan Busacca , Burkhard Jaeger , Richard J. Varsolona
IPC分类号： A61K31/4709 , A61K31/427 , A61K31/4025 , C07D215/233 , C07D417/14 , C07D207/12
CPC分类号： C07D417/14
摘要： This invention relates to novel crystalline forms of the following Compound (1), and the sodium salt thereof, and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection:
摘要翻译：本发明涉及以下化合物（1）的新型结晶形式及其钠盐及其制备方法，其药物组合物及其在治疗丙型肝炎病毒（HCV）感染中的用途：

3. 发明授权

US5693803A Process for making HIV protease inhibitors 失效
公开(公告)号：US5693803A
公开(公告)日：1997-12-02
申请号：US474800
申请日：1995-06-07
申请人： David Askin , Kai Rossen , Paul Reider , Richard J. Varsolona , Ralph P. Volante , Kenneth M. Wells
发明人： David Askin , Kai Rossen , Paul Reider , Richard J. Varsolona , Ralph P. Volante , Kenneth M. Wells
IPC分类号： A61K31/42 , A61K31/423 , A61K31/44 , A61K31/495 , A61K31/496 , A61P31/12 , A61P37/04 , A61P43/00 , C07D241/04 , C07D263/52 , C07D303/36 , C07D401/06 , C07D405/06 , C07D413/06 , C07D405/14
CPC分类号： C07D303/36 , C07D241/04 , C07D263/52 , C07D401/06 , C07D405/06 , C07D413/06
摘要： Intermediates of structural formula ##STR1## can be made by reacting a primary or secondary amine with glycosidol or an activated derivative thereof. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.

4. 发明授权

US5866573A Pyrazinone thrombin inhibitors 失效
标题翻译：吡嗪酮凝血酶抑制剂
公开(公告)号：US5866573A
公开(公告)日：1999-02-02
申请号：US837682
申请日：1997-04-21
申请人： Philip E.. Sanderson , Terry A.. Lyle , Bruce D. Dorsey , Richard J. Varsolona
发明人： Philip E.. Sanderson , Terry A.. Lyle , Bruce D. Dorsey , Richard J. Varsolona
IPC分类号： C07D241/20 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , A61K31/495 , C07D403/12 , C07D413/12
CPC分类号： C07D401/12 , C07D241/20 , C07D401/14 , C07D405/14 , C07D409/14
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## for example: ##STR2##
摘要翻译：本发明的化合物可用于抑制具有以下结构的凝血酶和相关的血栓形成闭塞：例如：

5. 发明授权

US11306080B2 Crystalline form of a BACE inhibitor, compositions, and use 有权
公开(公告)号：US11306080B2
公开(公告)日：2022-04-19
申请号：US16622323
申请日：2018-06-08
申请人： Merck Sharp & Dohme Corp. , Laura M. Artino , William Morris , Eric Sirota , Richard J. Varsolona
发明人： Laura M. Artino , William Morris , Eric Sirota , Richard J. Varsolona
IPC分类号： C07D417/12
摘要： The present invention provides a novel crystalline form of verubecestat (Crystalline Form II of Verubecestat) and pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an Aβ pathology and/or a symptom or symptoms thereof. Non-limiting examples of such Aβ pathologies, including Alzheimer's disease and mild cognitive impairment, are disclosed herein.

6. 发明申请

US20180179223A1 PROCESS FOR PREPARING SUBSTITUTED TETRACYCLIC HETEROCYCLE COMPOUNDS 审中-公开
公开(公告)号：US20180179223A1
公开(公告)日：2018-06-28
申请号：US15578777
申请日：2016-06-03
申请人： Jingjun Yin , Tetsuji Itoh , Jianguo Yin , Bangping Xiang , Kevin R. Campos , Alexei Kalinin , Zhuqing Liu , Melodie Deniz Christensen , Kevin M. Belyk , Richard J. Varsolona , Andrew Brunskill
发明人： Jingjun Yin , Tetsuji Itoh , Jianguo Yin , Bangping Xiang , Kevin R. Campos , Alexei Kalinin , Zhuqing Liu , Melodie Deniz Christensen , Kevin M. Belyk , Richard J. Varsolona , Andrew Brunskill
IPC分类号： C07D498/04 , C07F5/02 , C07D403/04 , B01J31/04
CPC分类号： C07D498/04 , B01J31/04 , C07D403/04 , C07F5/025
摘要： The present invention is directed to processes for preparing Substituted Tetracyclic Heterocycle Compounds of formula (I): (I) which may be useful as HCV NS5A inhibitors. The present invention is also directed to compounds that may be useful as synthetic intermediates and catalysts in the processes of the invention.

7. 发明授权

US06642237B1 Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides and uses thereof 失效
标题翻译： γ-羟基-2-（氟烷基氨基羰基）-1-哌嗪烷酰胺及其用途
公开(公告)号：US06642237B1
公开(公告)日：2003-11-04
申请号：US09718223
申请日：2000-11-21
申请人： James R. Tata , Kevin T. Chapman , Joseph Leslie Duffy , Nancy J. Kevin , Yuan Cheng , Thomas A. Rano , Fengqi Zhang , Tracy Huening , Brian Anthony Kirk , Zhijian Lu , Subharekha Raghavan , Fred J. Fleitz , Daniel E. Petrillo , Joseph D. Armstrong, III , Richard J. Varsolona , David Askin , R. Scott Hoerrner , Robert Purick
发明人： James R. Tata , Kevin T. Chapman , Joseph Leslie Duffy , Nancy J. Kevin , Yuan Cheng , Thomas A. Rano , Fengqi Zhang , Tracy Huening , Brian Anthony Kirk , Zhijian Lu , Subharekha Raghavan , Fred J. Fleitz , Daniel E. Petrillo , Joseph D. Armstrong, III , Richard J. Varsolona , David Askin , R. Scott Hoerrner , Robert Purick
IPC分类号： C07D491048
CPC分类号： C07D401/06 , A61K31/00 , A61K45/06 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/04 , C07D495/04 , A61K2300/00
摘要： &ggr;-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.
摘要翻译： γ-羟基-2-（氟烷基氨基羰基）-1-哌嗪戊酰胺化合物是HIV蛋白酶和HIV复制抑制剂的抑制剂。这些化合物可用于预防或治疗HV的感染和治疗AIDS，无论是化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒剂，免疫调节剂，抗生素或疫苗结合使用。还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。这些化合物对HIV病毒突变体有效，其对目前用于治疗AIDS和HIV感染的HIV蛋白酶抑制剂具有抗性。

8. 发明授权

US5886184A Finasteride processes 失效
标题翻译：非那雄胺加工
公开(公告)号：US5886184A
公开(公告)日：1999-03-23
申请号：US824426
申请日：1997-03-26
申请人： Ulf H. Dolling , James A. McCauley , Richard J. Varsolona
发明人： Ulf H. Dolling , James A. McCauley , Richard J. Varsolona
IPC分类号： A61K31/58 , C07F3/00 , C07J9/00 , C07J73/00 , C07J75/00 , H04N5/74 , C07D221/18 , A61K31/435
CPC分类号： C07F3/003 , C07J73/005 , H04N5/7458
摘要： Disclosed is a new process for producing finasteride which involves reacting the magnesium halide salt of 17.beta.-carboalkoxy-4-aza-5.alpha.-androst-1-en-3-one with t-butylamino magnesium halide, present in at least a 2:1 molar ratio to the ester, formed from t-butyl amine and an aliphatic/aryl magnesium halide at ambient temperature in an inert organic solvent under an inert atmosphere followed by heating and recovering the product finasteride.Also disclosed are two polymorphic crystalline Forms I and II of finasteride, and methods of their production.
摘要翻译：公开了一种生产非那雄胺的新方法，其包括使17β-烷氧基-4-氮杂-5α-雄甾-1-烯-3-酮的卤化镁盐与叔丁基氨基卤化镁反应，其存在于至少2 ：在惰性气氛下，在环境温度下，在惰性有机溶剂中，由叔丁胺和脂族/芳基卤化镁形成1摩尔比，然后加热和回收非那雄胺产物。还公开了非那雄胺的两种多晶型晶型I和II及其生产方法。

9. 发明授权

US5767124A Polymorphic forms of a growth hormone secretagogue 失效
标题翻译：多形态的生长激素促分泌素
公开(公告)号：US5767124A
公开(公告)日：1998-06-16
申请号：US736170
申请日：1996-10-23
申请人： Jerome P. Draper , Michael J. Kaufman , David C. Dubost , James A. McCauley , Jennifer L. Vandrilla , Richard J. Varsolona
发明人： Jerome P. Draper , Michael J. Kaufman , David C. Dubost , James A. McCauley , Jennifer L. Vandrilla , Richard J. Varsolona
IPC分类号： A61K45/06 , C07D20060101 , C07D471/10 , A61K31/445 , C07D401/02
CPC分类号： A61K45/06 , C07D471/10
摘要： This invention is concerned with polymorphic forms of the compound N-�1(R)-�(1,2-dihydro-1-methanesulfonylspiro�3H-indole-3,4'-piperdin!-1'-yl)carbonyl!-2-(phenylmethyloxy)ethyl!-2-amino-2-methylpropanamide methanesulfonate which is a growth hormone secretagogue that is useful in food animals to promote their growth thereby rendering the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, and to treat medical conditions which are improved by the anabolic effects of growth hormone. The instant polymorphic forms have advantages over the other known forms of N-�1(R)-�(1,2-dihydro-1-methanesulfonylspiro�3H-indole-3,4'-piperdin!-1'-yl)carbonyl!-2-(phenylmethyloxy)-ethyl!-2-amino-2-methylpropanamide methanesulfonate in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations. The present invention is also concerned with processes for preparing these polymorphic forms, pharmaceutical formulations comprising these polymorphic forms as active ingredients and the use of the polymorphic form of the compound and their formulations in the treatment of certain disorders.
摘要翻译：本发明涉及化合物N- [1（R） - [（1,2-二氢-1-甲磺酰基螺[3H-吲哚-3,4'-哌啶] -1'-基）羰基] - 2-（苯基甲氧基）乙基] -2-氨基-2-甲基丙酰胺甲磺酸盐，其是生物激素促分泌素，其可用于食用动物以促进其生长，从而使食用肉制品的生产更有效，并且在人类中，或以生长激素分泌不足为特征的医疗状况，以及治疗由生长激素的合成代谢作用改善的医疗状况。本发明的多晶型物质具有优于其他已知形式的N- [1（R） - [（1,2-二氢-1-甲磺酰基螺[3H-吲哚-3,4'-哌啶] -1'-基）羰基 ] -2-（苯基甲氧基） - 乙基] -2-氨基-2-甲基丙酰胺甲磺酸盐的热力学稳定性和药物制剂中的适用性。本发明还涉及制备这些多晶型形式的方法，包含这些多晶型形式作为活性成分的药物制剂以及化合物的多晶形式及其制剂在治疗某些疾病中的用途。

10. 发明授权

US5637711A Process for making HIV protease inhibitors 失效
标题翻译：制造HIV蛋白酶抑制剂的方法
公开(公告)号：US5637711A
公开(公告)日：1997-06-10
申请号：US474626
申请日：1995-06-07
申请人： David Askin , Paul Reider , Kai Rossen , Richard J. Varsolona , Ralph P. Volante , Kenneth M. Wells
发明人： David Askin , Paul Reider , Kai Rossen , Richard J. Varsolona , Ralph P. Volante , Kenneth M. Wells
IPC分类号： A61K31/42 , A61K31/423 , A61K31/44 , A61K31/495 , A61K31/496 , A61P31/12 , A61P37/04 , A61P43/00 , C07D241/04 , C07D263/52 , C07D303/36 , C07D401/06 , C07D405/06 , C07D413/06
CPC分类号： C07D303/36 , C07D241/04 , C07D263/52 , C07D401/06 , C07D405/06 , C07D413/06
摘要： Intermediates of structural formula ##STR1## can be made by reacting a primary or secondary amine with glycosidol or an activated derivative thereof. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.
摘要翻译：通过使伯胺或仲胺与糖苷或其活化衍生物反应，可以制备结构式“IMAGE”的中间体。该方法和中间体可用于合成HIV蛋白酶抑制剂化合物。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式