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1. 发明授权

US09006237B2 Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases 有权
公开(公告)号：US09006237B2
公开(公告)日：2015-04-14
申请号：US13411450
申请日：2012-03-02
申请人： Martin James Inglis Andrews , Mark Stuart Chambers , Wolfgang Schmidt , Giovanni Alessandro Tricarico , Grégory Louis Joseph Bar , Kim Louise Hirst , Olga Raquel Pinto Santos Oliveira Roussel , Juha Andrew Clase
发明人： Martin James Inglis Andrews , Mark Stuart Chambers , Wolfgang Schmidt , Giovanni Alessandro Tricarico , Grégory Louis Joseph Bar , Kim Louise Hirst , Olga Raquel Pinto Santos Oliveira Roussel , Juha Andrew Clase
IPC分类号： A61K31/503 , A61K31/4985 , C07D403/12 , C07D407/04 , C07D487/04
CPC分类号： C07D487/04
摘要： Novel fused pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammation, rheumatoid arthritis and others.

2. 发明授权

US07402682B2 3-heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-B]indole-1-carboxamide derivatives, their preparation and therapeutic use 有权
标题翻译： 3-杂芳基-3,5-二氢-4-氧代-4H-哒嗪并[4,5-B]吲哚-1-甲酰胺衍生物，其制备和治疗用途
公开(公告)号：US07402682B2
公开(公告)日：2008-07-22
申请号：US11427508
申请日：2006-06-29
申请人： Philippe Burnier , Jacques Froissant , Benoit Marabout , Frank Marguet , Frederic Puech
发明人： Philippe Burnier , Jacques Froissant , Benoit Marabout , Frank Marguet , Frederic Puech
IPC分类号： C07D487/02 , C07D209/42 , A61K31/503
CPC分类号： C07D487/04 , C07D209/42
摘要： A subject-matter of the invention is the compounds of general formula (I) in which X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 and R3 each represent, independently of one another, a hydrogen atom or a (C1-C4)alkyl group or else R2 and R3 form, with the nitrogen atom which carries them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type, it being possible for the heteroaromatic group to carry one or more halogen atoms and/or one or more (C1-C4)alkyl or (C1-C4)alkoxy groups; in the form of bases, of addition salts with acids, of solvates or of hydrates, the pharmaceutical compositions comprising them, processes for their preparation and synthetic intermediates.
摘要翻译：本发明的主题是通式（I）的化合物，其中X表示氢或卤素原子; R 1表示氢原子或（C 1 -C 4 -C 4）烷基; R 2和R 3各自独立地表示氢原子或（C 1 -C 4）烷基，或者R 2和R 3形式，与携带它们的氮原子一起形成吡咯烷基，哌啶基，吗啉基或4-烷基哌嗪基; 并且Het表示吡啶基，1-氧化吡啶基，喹啉基，异喹啉基，嘧啶基，吡嗪基或哒嗪基的杂芳族基团，杂芳基可以携带一个或多个卤素原子和/或一个或多个（C 1 C 1 -C 4烷基或（C 1 -C 4 -C 4）烷氧基; 以碱的形式，与酸，溶剂合物或水合物的加成盐，包含它们的药物组合物，其制备方法和合成中间体。

3. 发明申请

US20080139569A1 NOVEL CRYSTALLINE FORM 有权
标题翻译：新型结晶形式
公开(公告)号：US20080139569A1
公开(公告)日：2008-06-12
申请号：US12031243
申请日：2008-02-14
申请人： William L. ROCCO , John D. HIGGINS
发明人： William L. ROCCO , John D. HIGGINS
IPC分类号： A61K31/503 , C07D487/02
CPC分类号： C07D487/04
摘要： Disclosed are a novel crystalline form of 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide, processes of preparing said crystalline form of 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide, compositions comprising said form in admixture with one or more pharmaceutically acceptable excipients, and uses for the same.
摘要翻译：公开了7-氯-N，N，5-三甲基-4-氧代-3-苯基-3,5-二氢-4H-哒嗪并[4,5-b]吲哚-1-乙酰胺的新型结晶形式，方法制备所述结晶形式的7-氯-N，N，5-三甲基-4-氧代-3-苯基-3,5-二氢-4H-哒嗪并[4,5-b]吲哚-1-乙酰胺，其组合物包含所述形式与一种或多种药学上可接受的赋形剂混合，及其用途。

4. 发明申请

US20070088036A1 Piperidine derivatives and methods of use 有权
标题翻译：哌啶衍生物和使用方法
公开(公告)号：US20070088036A1
公开(公告)日：2007-04-19
申请号：US11546938
申请日：2006-10-11
申请人： Penglie Zhang , Andrew Pennell , Wei Chen , Kevin Greenman , Lianfa Li , Edward Sullivan
发明人： Penglie Zhang , Andrew Pennell , Wei Chen , Kevin Greenman , Lianfa Li , Edward Sullivan
IPC分类号： A61K31/519 , A61K31/498 , A61K31/503 , C07D498/02 , C07D491/02 , C07D487/02
CPC分类号： C07D401/06 , C07D211/42 , C07D211/52 , C07D211/56 , C07D211/60 , C07D211/64 , C07D401/14 , C07D413/14 , C07D471/04
摘要： Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
摘要翻译：提供了作为CCR1受体的有效拮抗剂并具有体内抗炎活性的化合物。化合物通常是单环和双环化合物，并且可用于药物组合物，用于治疗CCR1介导的疾病的方法，以及用于鉴定竞争性CCR1拮抗剂的测定中的对照。

5. 发明申请

US20070066618A1 Use of EP4 Receptor Ligands in the Treatment of IL-6 Involved Diseases 失效
标题翻译：使用EP4受体配体治疗IL-6相关疾病
公开(公告)号：US20070066618A1
公开(公告)日：2007-03-22
申请号：US11556414
申请日：2006-11-03
申请人： Masato Shimojo , Kana Taniguchi
发明人： Masato Shimojo , Kana Taniguchi
IPC分类号： A61K31/53 , A61K31/52 , A61K31/503 , A61K31/498 , A61K31/4745 , A61K31/4184
CPC分类号： A61K31/426 , A61K31/00 , A61K31/4178 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/437 , A61K31/4745 , A61K31/498 , A61K31/502 , A61K31/52 , A61K31/522 , A61K31/53
摘要： Methods of treating IL-6 involved diseases with EP4 receptor ligands, including EP4 receptor antagonists. Assays to determine the effect of test compounds on PGE2-induced whole blood cells activation.
摘要翻译：治疗IL-6的方法涉及具有EP4受体配体的疾病，包括EP4受体拮抗剂。测定化合物对PGE2诱导的全血细胞活化的影响的测定。

6. 发明申请

US20070049593A1 Tetracyclic fused heterocyclic compound and use thereof as HCV polymerase inhibitor 审中-公开
标题翻译：四环稠合杂环化合物及其作为HCV聚合酶抑制剂的用途
公开(公告)号：US20070049593A1
公开(公告)日：2007-03-01
申请号：US11064319
申请日：2005-02-23
申请人： Takahiro Oka , Kazutaka Ikegashira , Shintaro Hirashima , Hiroshi Yamanaka , Satoru Noji , Yasushi Niwa , Yoko Matsumoto , Toshihiro Sato , Izuru Ando , Yukihiro Nomura
发明人： Takahiro Oka , Kazutaka Ikegashira , Shintaro Hirashima , Hiroshi Yamanaka , Satoru Noji , Yasushi Niwa , Yoko Matsumoto , Toshihiro Sato , Izuru Ando , Yukihiro Nomura
IPC分类号： C07D471/02 , A61K31/53 , A61K31/519 , A61K31/498 , A61K31/503 , A61K31/4745
CPC分类号： C07D513/04 , C07D487/04 , C07D487/14 , C07D498/04 , C07D498/14
摘要： The present invention relates to a tetracyclic fused heterocyclic compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.
摘要翻译：本发明涉及由下式[I]表示的四环稠合杂环化合物，其中各符号如说明书中所定义，或其药学上可接受的盐，丙型肝炎病毒（HCV）聚合酶抑制剂和治疗剂含有该化合物的丙型肝炎。本发明化合物基于HCV聚合酶抑制活性显示抗HCV活性，可用作预防或治疗丙型肝炎的药剂。

7. 发明申请

US20060287324A1 Bicyclic heterocycles as cannabinoid-1 receptor modulators 有权
标题翻译：双环杂环作为大麻素-1受体调节剂
公开(公告)号：US20060287324A1
公开(公告)日：2006-12-21
申请号：US11455039
申请日：2006-06-16
申请人： Chongqing Sun , Yanting Huang , Doree Sitkoff , Taekyu Lee , William Ewing
发明人： Chongqing Sun , Yanting Huang , Doree Sitkoff , Taekyu Lee , William Ewing
IPC分类号： A61K31/503 , A61K31/4745 , C07D487/04 , C07D471/02
CPC分类号： C07D471/04 , C07D487/04
摘要： The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formula: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein A, B, R1, R2, R3 and R8 are described herein.
摘要翻译：本申请描述了根据式I的化合物，包含至少一种根据式I的化合物和任选的一种或多种另外的治疗剂的药物组合物和使用根据式I的化合物的治疗方法，其单独和与一种或多种另外的治疗剂。所述化合物具有以下通式：包括所有前药，溶剂化物，药学上可接受的盐和立体异构体，其中A，B，R 1，R 2，R 3 本文描述了本文和/或 8。

8. 发明申请

US20060281750A1 Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors 有权
标题翻译：杂芳基11-β-羟基类固醇脱氢酶I型抑制剂
公开(公告)号：US20060281750A1
公开(公告)日：2006-12-14
申请号：US11448946
申请日：2006-06-07
申请人： James Li , Lawrence Hamann , Haixia Wang
发明人： James Li , Lawrence Hamann , Haixia Wang
IPC分类号： A61K31/503 , A61K31/4745 , A61K31/4192 , C07D471/02
CPC分类号： C07D471/04
摘要： Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: W-L-Z (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, L and Z are defined herein.
摘要翻译：提供了新的化合物，其为11-β-羟基类固醇脱氢酶I型抑制剂。 11-β-羟基类固醇脱氢酶I型抑制剂可用于治疗，预防或减缓需要11-β-羟基类固醇脱氢酶I型抑制剂治疗的疾病进展。这些新化合物具有以下结构：<？in-line-formula description =“In-line Formulas”end =“lead”？> WLZ（I）<？in-line-formula description =“In-line Formulas”end = 或其立体异构体或前药或其药学上可接受的盐，其中W，L和Z在本文中定义。

9. 发明申请

US20060223809A1 Novel compounds 审中-公开
标题翻译：新型化合物
公开(公告)号：US20060223809A1
公开(公告)日：2006-10-05
申请号：US11447343
申请日：2006-06-06
申请人： Martin Cooper , Simon Guile , Anthony Ingall , Rukhsana Rasul
发明人： Martin Cooper , Simon Guile , Anthony Ingall , Rukhsana Rasul
IPC分类号： A61K31/503 , C07D498/02
CPC分类号： C07D495/04
摘要： The invention relates to thienopyridazinones of formula (I): wherein: R1 is C1-6 alkyl, C2-6 alkenyl or C3-6 cycloalkyl which is optionally substituted by C1-6 alkyl, each of the above being optionally substituted by one or more halogen atoms; R2 is C1-6 alkyl; R3 is a group CO-G or SO2-G where G is a 5- or 6-membered ring containing a nitrogen atom and a second heteroatom selected from oxygen and sulphur adjacent to the nitrogen, and optionally substituted by up to 3 groups selected from hydroxyl and C1-4 alkyl; Q is CR5R6 where R5 and R6 are as defined in the specification; and R4 is a 5- to 10-membered mono- or bi-cyclic aromatic ring system, containing 0 to 4 heteroatoms independently selected from nitrogen, oxygen and sulphur, the ring system being optionally substituted as described in the specification, and pharmaceutically acceptable salts and solvates thereof. Processes for their preparation, pharmaceutical compositions containing them and their use in therapy, in particular in the modulation of autoimmune disease are also described.
摘要翻译：本发明涉及式（I）的噻吩并哒嗪酮：其中：R 1是C 1-6烷基，C 2-6链烯基或C 任选被C 1-6烷基取代的，任选被一个或多个卤素原子取代的C 3-6环烷基; R 2是C 1-6烷基; R 3是基团CO-G或SO 2 -G，其中G是含有氮原子的5-或6-元环，和选自氧和/ 硫邻近氮，并且任选地被多至3个选自羟基和C 1-4烷基的基团取代; Q是CR 5，其中R 5和R 6如说明书中所定义; 并且R 4是含有0至4个独立地选自氮，氧和硫的杂原子的5至10元单环或双环芳族环系统，所述环系统如上所述被任选地取代在本说明书及其药学上可接受的盐和溶剂化物中。还描述了其制备方法，含有它们的药物组合物及其在治疗中的用途，特别是在调节自身免疫疾病中。

10. 发明申请

US20060223807A1 Therapeutic methods for type I diabetes 审中-公开
公开(公告)号：US20060223807A1
公开(公告)日：2006-10-05
申请号：US11092099
申请日：2005-03-29
申请人： Roger Davis , Anja Jaeschke
发明人： Roger Davis , Anja Jaeschke
IPC分类号： A61K31/506 , A61K31/502 , A61K31/4745 , A61K31/4439 , A61K31/503 , A61K31/4162
CPC分类号： A61K31/428 , A61K31/18 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/416 , A61K31/42 , A61K31/425 , A61K31/437 , A61K31/445 , A61K31/4535 , A61K31/4725 , A61K31/497 , A61K31/50 , A61K31/506 , A61K31/5377 , A61K31/54 , A61K31/55 , A61K31/70 , Y10S514/866
摘要： The invention relates to the treatment and prevention of type I diabetes. More specifically, the invention relates to compounds that treat or prevent the body's immune system from destroying β-cells (i.e., insulin-producing cells in the pancreatic islets of Langerhans) by inhibition of JNK2, selective inhibition of JNK2, or inhibition of the expression of the MAPK9 gene or gene product. In one embodiment, the present invention contemplates the diagnosis, identification, production, and use of compounds which modulate MAPK9 gene expression or the activity of the MAPK9 gene product including but not limited to, JNK2, the nucleic acid encoding MAPK9 and homologues, analogues, and deletions thereof, as well as antisense, ribozyme, triple helix, antibody, and polypeptide molecules as well as small inorganic molecules. The present invention contemplates a variety of pharmaceutical formulations and routes of administration for such compounds.

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