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1. 发明授权

US06720331B2 1-substituted 1,2,3,4-tetrahydro-&bgr;-carboline and 3,4-dihydro-&bgr;-carboline and analogs as antitumor agents 失效
标题翻译： 1-取代的1,2,3,4-四氢-β-咔啉和3,4-二氢-β-咔啉及类似物作为抗肿瘤剂
公开(公告)号：US06720331B2
公开(公告)日：2004-04-13
申请号：US10115312
申请日：2002-04-03
申请人： Sheau Farn Yeh , Ya-Ching Shen
发明人： Sheau Farn Yeh , Ya-Ching Shen
IPC分类号： A61K31437
CPC分类号： C07D471/04
摘要： A composition includes a substituted dihydro- or tetrahydro-&bgr;-carboline of formula (II) or (III), wherein the aromatic ring of the carboline may include one or more substituents selected from the group consisting of hydroxy, C1-6 alkoxy, benzyloxy, C1-6 acyloxy, amino, C1-6 alkyl, C1-6 dialkylamino, halogen, and carboxy, and the C-1 position of the carboline may include a substitutent selected from the group consisting of a carbocyclic group and a heterocyclic group. The composition may include a salt or a prodrug of the substituted dihydro- or tetrahydro-&bgr;-carboline. The composition may further includes a pharmaceutically acceptable carrier, diluent, or excipient.
摘要翻译：组合物包括式（II）或（III）的取代的二氢或四氢-β-咔啉，其中咔啉的芳环可以包括一个或多个选自羟基，C 1-6烷氧基，苄氧基，C 1-6酰氧基，氨基，C 1-6烷基，C 1-6二烷基氨基，卤素和羧基，咔啉的C-1位可以包括选自碳环基和杂环基的取代基。组合物可以包括取代的二氢或四氢-β-咔啉的盐或前药。组合物还可以包含药学上可接受的载体，稀释剂或赋形剂。

2. 发明授权

US06703404B2 Tert -butyl-(7-methyl-imidazol [1,2-a]pyridin-3-yl)-amine derivatives 失效
标题翻译：叔丁基 - （7-甲基 - 咪唑并[1,2-a]吡啶-3-基） - 胺衍生物
公开(公告)号：US06703404B2
公开(公告)日：2004-03-09
申请号：US10117339
申请日：2002-04-08
申请人： Corinna Maul , Bernd Sundermann , Hagen-Heinrich Hennies , Johannes Schneider , Matthias Gerlach
发明人： Corinna Maul , Bernd Sundermann , Hagen-Heinrich Hennies , Johannes Schneider , Matthias Gerlach
IPC分类号： A61K31437
CPC分类号： C07D471/04 , C07D487/04 , C07D513/04 , C07F9/6561 , C40B40/00
摘要： A Tert.-butyl-(7-methyl-imidazo[1,2-a]pyridin-3-yl)-amine derivatives of Formula I: wherein the pharmaceutically acceptable salts, methods of making and method of use, in particular for the treatment of migraine.
摘要翻译：式I的叔丁基 - （7-甲基 - 咪唑并[1,2-a]吡啶-3-基） - 胺衍生物：其中药学上可接受的盐，制备方法和使用方法，特别是治疗偏头痛。

3. 发明授权

US06613775B1 Imidazo[1,2-a]pyridine compounds 有权
标题翻译：咪唑并[1,2-a]吡啶化合物
公开(公告)号：US06613775B1
公开(公告)日：2003-09-02
申请号：US09403510
申请日：1999-10-22
申请人： Kosrat Amin , Mikael Dahlström , Peter Nordberg , Ingemar Starke
发明人： Kosrat Amin , Mikael Dahlström , Peter Nordberg , Ingemar Starke
IPC分类号： A61K31437
CPC分类号： C07D471/04
摘要： The present invention relates to novel compounds, and therapeutically acceptable salts thereof of the formula (I), which inhibit exogenously or endogenously stimulated gastric acid secretion and thus can be used in the prevention and treatment of gastrointestinal inflammatory diseases.
摘要翻译：本发明涉及抑制外源性或内源性刺激的胃酸分泌的式（I）的新化合物及其治疗上可接受的盐，因此可用于预防和治疗胃肠炎性疾病。

4. 发明授权

US06538004B2 Tricyclic dihydropyrazolone and tricyclic dihydroisoxazolone potassium channel openers 失效
标题翻译：三环二氢吡唑酮和三环二氢异恶唑酮钾通道开放剂
公开(公告)号：US06538004B2
公开(公告)日：2003-03-25
申请号：US09778551
申请日：2001-02-07
申请人： Irene Drizin , Robert J. Altenbach , William A. Carroll
发明人： Irene Drizin , Robert J. Altenbach , William A. Carroll
IPC分类号： A61K31437
CPC分类号： C07D471/04 , C07C45/298 , C07C45/41 , C07C45/63 , C07C205/44 , C07D491/14 , C07D495/14 , C07C47/55
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。

5. 发明授权

US06498166B1 Pyrazolopyridines 失效
标题翻译：吡唑并吡啶类
公开(公告)号：US06498166B1
公开(公告)日：2002-12-24
申请号：US09890925
申请日：2001-08-30
申请人： Ian Baxter Campbell , Paul Francis Lambeth , Alan Naylor , Neil Anthony Pegg
发明人： Ian Baxter Campbell , Paul Francis Lambeth , Alan Naylor , Neil Anthony Pegg
IPC分类号： A61K31437
CPC分类号： C07D471/04
摘要： The invention provides the compounds of formula (I) wherein: R0 and R1 are independently selected from H, halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms; R2 is halogen, CN, CONR4R5, CO2H, CO2C1-6alkyl, or NHSO2R4; R3 is C1-6alkyl or NH2; and R4 and R5 are independently selected from H, C1-6alkyl, phenyl, phenyl substituted by one or more atoms or groups (selected from halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms), or together with the nitrogen atom to which they are attached form a saturated 4 to 8 membered ring; and pharmaceutically acceptable derivatives thereof. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.
摘要翻译：本发明提供式（I）化合物，其中：R 0和R 1独立地选自H，卤素，C 1-6烷基，C 1-6烷氧基或被一个或多个氟原子取代的C 1-6烷氧基; R 2是卤素，CN，CONR 4 R 5 ，CO 2 H，CO 2 C 1-6烷基或NHSO 2 R 4; R 3是C 1-6烷基或NH 2; R 4和R 5独立地选自H，C 1-6烷基，苯基，被一个或多个原子或基团取代的苯基（选自卤素，C 1-6烷基，C 1-6烷氧基或被一个或多个氟原子取代的C 1-6烷氧基），或与它们所连接的氮原子一起形成饱和的4至8元环; 其药学上可接受的衍生物。式（I）化合物是COX-2的有效和选择性抑制剂，可用于治疗疼痛，发热，多种病症和疾病的炎症。

6. 发明授权

US06492384B1 Imidazo (4,5-C) pyridine-4-one derivatives with factor XA inhibiting effect 失效
标题翻译：咪唑（4,5-C）吡啶-4-酮衍生物，具有因子XA抑制作用
公开(公告)号：US06492384B1
公开(公告)日：2002-12-10
申请号：US09806418
申请日：2001-12-13
申请人： Werner Mederski , Horst Juraszyk , Hanns Wurziger , Joachim Gante , Dieter Dorsch , Hans-Peter Buchstaller , Sabine Bernotat-Danielowski , Guido Melzer , Soheila Anzali
发明人： Werner Mederski , Horst Juraszyk , Hanns Wurziger , Joachim Gante , Dieter Dorsch , Hans-Peter Buchstaller , Sabine Bernotat-Danielowski , Guido Melzer , Soheila Anzali
IPC分类号： A61K31437
CPC分类号： C07D471/04
摘要： The invention relates to novel compounds of formula (I), wherein R, R1, R2, R3, n and p have the meaning defined in claim 1. Compounds are inhibitors of clotting factor Xa and can be used for the prophylaxis and/or therapy of thrombo-embolic disorders.
摘要翻译：本发明涉及式（I）的新化合物，其中R，R 1，R 2，R 3，n和p具有权利要求1中定义的含义。化合物是凝血因子Xa的抑制剂，可用于预防和/或治疗的血栓栓塞障碍。

7. 发明授权

US06469021B1 Non-peptide antagonists of GLP-1 receptor and methods of use 失效
标题翻译： GLP-1受体的非肽拮抗剂和使用方法
公开(公告)号：US06469021B1
公开(公告)日：2002-10-22
申请号：US09831572
申请日：2001-10-26
申请人： Larry Kenneth Truesdale , Richard A. Bychowski , Javier Gonzalez , Atsuo Kuki , Ranjan Jagath Rajapakse , Min Teng , Dan Kiel , Daljit S. Dhanoa , Yufeng Hong , Tso-sheng Chou , Anthony L. Ling , Michael David Johnson , Vlad Edward Gregor
发明人： Larry Kenneth Truesdale , Richard A. Bychowski , Javier Gonzalez , Atsuo Kuki , Ranjan Jagath Rajapakse , Min Teng , Dan Kiel , Daljit S. Dhanoa , Yufeng Hong , Tso-sheng Chou , Anthony L. Ling , Michael David Johnson , Vlad Edward Gregor
IPC分类号： A61K31437
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D471/04 , C07D471/14 , C07D491/04 , C07D491/14
摘要： Non-peptide compounds that act as antagonists of the intestinal hormone glucagons-like peptide 1 (GLP-1) have a 9H-b-carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding to the GLP-1 receptor and/or prevent activation of the receptor by bound GLP-1. The invention further relates to a method of inhibiting the binding of GLP-1 to the GLP-1 receptor and a method of inhibiting the activation of the GLP-1 receptor. Intermediate compounds useful for making non-peptide GLP-1 receptor antagonists are also described.
摘要翻译：作为肠激素胰高血糖素样肽1（GLP-1）的拮抗剂的非肽化合物具有9H-b-咔啉中心基序。该化合物表现出有利的物理，化学和生物学特性，并且抑制GLP-1肽与GLP-1受体的结合和/或通过结合的GLP-1阻止受体活化。本发明还涉及抑制GLP-1与GLP-1受体结合的方法以及抑制GLP-1受体活化的方法。还描述了可用于制备非肽GLP-1受体拮抗剂的中间体化合物。

8. 发明授权

US06436955B1 Crystal modification A of 8-cyano-1-cyclopropyl-7-(is,6s-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid 有权
标题翻译： 8-氰基-1-环丙基-7-（is，6s-2,8-二氮杂双环[4.3.0]壬烷-8-基）-6-氟-1,4-二氢-4-氧代 - 3-喹啉羧酸
公开(公告)号：US06436955B1
公开(公告)日：2002-08-20
申请号：US09856669
申请日：2001-05-23
申请人： Thomas Himmler , Werner Hallenbach , Hubert Rast
发明人： Thomas Himmler , Werner Hallenbach , Hubert Rast
IPC分类号： A61K31437
CPC分类号： C07D471/04
摘要： The present invention relates to a defined crystal modification of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0] nonan-8-yl)-6-fluoro-1, 4-dihydro-4-oxo-3-quinolinecarboxylic acid of the formula (I), to processes for its preparation and to its use in pharmaceutical preparations. The crystal modification can be distinguished from other crystal modifications of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl )-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid of the formula (I) by its characteristic X-ray powder diffractogram and its differential thermodiagram (see description).
摘要翻译：本发明涉及8-氰基-1-环丙基-7-（1S，6S-2,8-二氮杂双环[4.3.0]壬烷-8-基）-6-氟-1,4- 式（I）的二氢-4-氧代-3-喹啉羧酸，其制备方法及其在药物制剂中的应用。晶体修饰可以区别于8-氰基-1-环丙基-7 - （1S，6S-2,8-二氮杂双环[4.3.0]壬烷-8-基）-6-氟-1,4-二氢-4-氧代-3-喹啉羧酸其特征 X射线粉末衍射图及其差示热图（见说明）。

9. 发明授权

US06365598B1 Pyrroloquinolines for treatment of obesity 失效
标题翻译：吡咯喹啉类治疗肥胖症
公开(公告)号：US06365598B1
公开(公告)日：2002-04-02
申请号：US09786159
申请日：2001-03-01
申请人： David Reginald Adams , Jonathan Mark Bentley , Jonathan Richard Anthony Roffey , Corinna Dagmar Bodkin , Howard Langham Mansell , Ashley Roger George , Ian Anthony Cliffe
发明人： David Reginald Adams , Jonathan Mark Bentley , Jonathan Richard Anthony Roffey , Corinna Dagmar Bodkin , Howard Langham Mansell , Ashley Roger George , Ian Anthony Cliffe
IPC分类号： A61K31437
CPC分类号： C07D471/04
摘要： A chemical compound of formula (I), wherein R1 to R3 are independently selected from hydrogen and alkyl; R4 is selected from hydrogen, alkyl, alkoxy, formyl and cyano; X1 is selected from N and C—R7; X2 is selected from N and C—R8; X3 is selected from N and C—R9; X4 is selected from N and C—R10; wherein at least one of X1, X2, X3 and X4 is N; and R5 to R10 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus; and sleep apnea, and particularly for the treatment of obesity.

10. 发明授权

US06313139B1 Benzylamine derivatives which are useful in treating psychiatric disorders 有权
标题翻译：可用于治疗精神疾病的苄胺衍生物
公开(公告)号：US06313139B1
公开(公告)日：2001-11-06
申请号：US09359284
申请日：1999-07-22
申请人： Fredericus Antonius Dijcks , Dirk Leysen , Joannes Theodorus Maria Linders , Gerardus Stephanus Franciscus Ruigt , Ian Craig Carlyle , Simon James Anthony Grove , Duncan Robertson Rae , Simon N. Thorn
发明人： Fredericus Antonius Dijcks , Dirk Leysen , Joannes Theodorus Maria Linders , Gerardus Stephanus Franciscus Ruigt , Ian Craig Carlyle , Simon James Anthony Grove , Duncan Robertson Rae , Simon N. Thorn
IPC分类号： A61K31437
CPC分类号： C07D413/04 , A61K31/00 , A61K31/085 , A61K31/121 , A61K31/137 , A61K31/15 , A61K31/381 , A61K31/416 , A61K31/423 , A61K31/426 , A61K31/437 , A61K31/472 , C07C211/28 , C07C211/29 , C07C217/56 , C07C255/58 , C07D213/61 , C07D215/12 , C07D217/14 , C07D231/56 , C07D239/26 , C07D261/08 , C07D261/20 , C07D263/57 , C07D277/28 , C07D277/66 , C07D307/52 , C07D307/80 , C07D307/81 , C07D333/20 , C07D333/28 , C07D333/58
摘要： The present invention relates to certain novel benzylamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.
摘要翻译：本发明涉及某些新的苄胺衍生物，其制备方法，含有它们的药物制剂及其在药物治疗中的用途，特别是治疗抑郁症。

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