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1. 发明授权

US06825180B2 Pyridopyrimidine compounds and their uses 失效
公开(公告)号：US06825180B2
公开(公告)日：2004-11-30
申请号：US09859503
申请日：2001-05-18
申请人： Marc J. McKennon , J. Peter Klein , Michael Coon
发明人： Marc J. McKennon , J. Peter Klein , Michael Coon
IPC分类号： C07D47104
CPC分类号： C07D471/04
摘要： Novel pyridopyrimidine-based compounds are found to be useful for the treatment or prevention of symptoms or manifestations associated with diseases or disorders affected by cytokine intracellular signaling.

2. 发明授权

US06693102B2 Pyridine-substituted pyrazolopyridine derivatives 失效
标题翻译：吡啶取代的吡唑并吡啶衍生物
公开(公告)号：US06693102B2
公开(公告)日：2004-02-17
申请号：US10001569
申请日：2001-11-01
申请人： Johannes-Peter Stasch , Achim Feurer , Stefan Weigand , Elke Stahl , Dietmar Flubacher , Cristina Alonso-Alija , Frank Wunder , Dieter Lang , Klaus Dembowsky , Alexander Straub , Elisabeth Perzborn
发明人： Johannes-Peter Stasch , Achim Feurer , Stefan Weigand , Elke Stahl , Dietmar Flubacher , Cristina Alonso-Alija , Frank Wunder , Dieter Lang , Klaus Dembowsky , Alexander Straub , Elisabeth Perzborn
IPC分类号： C07D47104
CPC分类号： C07D471/04 , A61K31/505 , A61K45/06 , A61K2300/00
摘要： The present invention relates to new pyrazolopyridine derivatives of the formula (I) in which R1 represents 4-pyridinyl or 3-pyridinyl; R2 represents H, NH2 or halogen; and salts, isomers and hydrates thereof as stimulators of soluble guanylate cyclase and for use as agents for the treatment of cardiovascular disorders, hypertension, of thromboembolic disorders and ischaemia, sexual dysfunction or inflammation, and for the treatment of disorders of the central nervous system.
摘要翻译：本发明涉及式（I）的新的吡唑并吡啶衍生物，其中R 1表示4-吡啶基或3-吡啶基; R 2表示H，NH 2或卤素; 其盐，异构体和水合物作为可溶性鸟苷酸环化酶的刺激剂，并用作治疗心血管疾病，高血压，血栓栓塞障碍和局部缺血，性功能障碍或炎症以及用于治疗中枢神经系统疾病的药剂。

3. 发明授权

US06670476B2 Resolution of trans-7-(hydroxy-methyl)octa-hydro-2H-pyrido[1,2-a]pyrazine 失效
标题翻译：拆分反式-7-（羟基 - 甲基）八氢-2H-吡啶并[1,2-a]吡嗪
公开(公告)号：US06670476B2
公开(公告)日：2003-12-30
申请号：US10066907
申请日：2001-11-13
申请人： Arthur E. Harms
发明人： Arthur E. Harms
IPC分类号： C07D47104
CPC分类号： C07D471/04
摘要： The invention provides a process for the optical resolution of a racemic mixture, or an optically enriched mixture, of trans-7-(hydroxymethyl)octa-hydro-2H-pyrido-1,2a)pyrazine, a key intermediate for preparing pharmacologically active 2,7-substituted octahydro-1H-pyrido[1,2-a]pyrazine derivatives useful in the treatment of disorders of the dopamine system. The process of the invention involves use of D-(−) or L-(+)naproxen as a resolving agent.
摘要翻译：本发明提供了用于制备反式-7-（羟甲基）八氢-2H-吡啶-1,2a）吡嗪的外消旋混合物或光学富集混合物的光学拆分方法，该吡嗪是制备药理学活性2的关键中间体，7-取代的八氢-1H-吡啶并[1,2-a]吡嗪衍生物，其用于治疗多巴胺系统的病症。本发明的方法涉及使用D - （ - ）或L - （+）萘普生作为分解剂。

4. 发明授权

US06589957B2 Compounds and methods of use for treatment of neurogenic inflammation 失效
公开(公告)号：US06589957B2
公开(公告)日：2003-07-08
申请号：US09944881
申请日：2001-08-31
申请人： Amy E. Wright , Shirley A. Pomponi , Robert S. Jacobs
发明人： Amy E. Wright , Shirley A. Pomponi , Robert S. Jacobs
IPC分类号： C07D47104
CPC分类号： C07D403/14 , A61K31/4178 , A61K31/497 , C07D487/08
摘要： The subject invention pertains to compounds which are useful as anti-inflammatory agents and to compositions containing such compounds as active ingredients. The novel uses of the compounds relate to the anti-neurogenic inflammatory properties of the disclosed bis-heterocyclic compounds. Specifically exemplified herein are dragmacidin f, topsentin d, and topsentin e, and their salts, analogs, and derivatives.

5. 发明授权

US06583285B1 Process for preparing zolpidem 有权
标题翻译：唑吡旦的制备方法
公开(公告)号：US06583285B1
公开(公告)日：2003-06-24
申请号：US10318900
申请日：2002-12-13
申请人： Markus Sauter , Wolfgang Wohlleben
发明人： Markus Sauter , Wolfgang Wohlleben
IPC分类号： C07D47104
CPC分类号： C07D471/04 , C07C235/74 , C07C235/78
摘要： The invention relates to a process for preparing a compound of formula (I) wherein a compound of formula (II), wherein R1 denotes chlorine, bromine, iodine, —O—COCH3, tosylate or mesylate, is reacted with a compound of formula (III), optionally in a suitable diluent and/or in the presence of a suitable added reagent or catalyst, the reaction being carried out in a temperature range from 20 to 80° C.
摘要翻译：本发明涉及一种制备式（I）化合物的方法，其中式（II）化合物（其中R 1表示氯，溴，碘，-O-COCH 3，甲苯磺酸酯或甲磺酸酯）与式（III）化合物反应，，任选地在合适的稀释剂和/或在合适的加入的试剂或催化剂的存在下，反应在20至80℃的温度范围内进行。

6. 发明授权

US06511987B1 Bicyclic and tricyclic heteroaromatic compounds 失效
标题翻译：双环和三环杂芳族化合物
公开(公告)号：US06511987B1
公开(公告)日：2003-01-28
申请号：US09709887
申请日：2000-11-10
申请人： Jun Yuan , Pamela Albaugh , Kenneth Shaw , Alan Hutchinson
发明人： Jun Yuan , Pamela Albaugh , Kenneth Shaw , Alan Hutchinson
IPC分类号： C07D47104
CPC分类号： C07D217/26 , C07D237/30 , C07D471/04 , C07D487/04 , C07D519/00 , G01N2333/70571
摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其中W，Q，X，X 1，Y和Z如本文所定义。这些化合物以高选择性和/或高亲和力结合GABA A受体的苯并二氮杂位点，因此可用于治疗中枢神经系统（CNS）疾病和作为组织样品中GABA A受体定位的探针。还公开了可用于制备这些化合物的中间体。

7. 发明授权

US06492520B1 Substituted pyrido-or pyrimido-containing 6,6- or 6,7-bicyclic derivatives 失效
标题翻译：取代的含吡啶基或嘧啶的6,6-或6,7-双环衍生物
公开(公告)号：US06492520B1
公开(公告)日：2002-12-10
申请号：US09242076
申请日：1999-05-24
申请人： Yuhpyng L. Chen
发明人： Yuhpyng L. Chen
IPC分类号： C07D47104
CPC分类号： C07D471/04
摘要： This invention relates to compounds of formula (I), wherein A, B, D, E, K, G, Z, R3 and R5 are defined as in the specification, and to the pharmaceutically acceptable salts of such compounds. Compounds (I) are corticotropin releasing factor (hormone) CRF (CRH) antagonists.
摘要翻译：本发明涉及式（I）化合物，其中A，B，D，E，K，G，Z，R 3和R 5如说明书中所定义，以及这些化合物的药学上可接受的盐。化合物（I）是促肾上腺皮质激素释放因子（激素）CRF（CRH）拮抗剂。

8. 发明授权

US06486171B2 Piperidine compounds 失效
标题翻译：哌啶化合物
公开(公告)号：US06486171B2
公开(公告)日：2002-11-26
申请号：US10105171
申请日：2002-03-25
申请人： Jean-Louis Peglion , Aimée Dessinges , Christophe Poitevin , Mark Millan , Anne Dekeyne
发明人： Jean-Louis Peglion , Aimée Dessinges , Christophe Poitevin , Mark Millan , Anne Dekeyne
IPC分类号： C07D47104
CPC分类号： C07D471/04 , C07D491/04 , C07D495/04
摘要： A compound selected from those of formula (I): wherein: W represents optionally substituted naphthyl, or a group of formula Y (wherein) as defined in the description, n represents an integer from 1 to 6 inclusive, Z represents a single bond, oxygen, or optionally substituted nitrogen, A and Q each represent CH or nitrogen, it being understood that A or Q must be N and the other CH, M, together with a carbon of the phenyl to which it is bonded, represents thienyl, furyl, pyrrolyl, or oxopyrrolyl, its isomers, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same, which are useful in the treatment of some CNS disorders.
摘要翻译：选自式（I）的化合物：其中：W表示任选取代的萘基，或如说明书中所定义的式Y（其中）的基团，n表示1至6的整数，Z表示单键，氧或任选取代的氮，A和Q各自表示CH或氮，应理解A或Q必须为N，另一个CH，M与其所键合的苯基的碳一起代表噻吩基，呋喃基，吡咯基或氧代吡咯基，其异构体及其药学上可接受的酸或碱加成盐，以及含有它们的药物，其可用于治疗一些CNS障碍。

9. 发明授权

US06388076B1 Protein tyrosine phosphatase-inhibiting compounds 失效
标题翻译：蛋白酪氨酸磷酸酶抑制化合物
公开(公告)号：US06388076B1
公开(公告)日：2002-05-14
申请号：US09645785
申请日：2000-08-24
申请人： Adnan Mjalli , Sepehr Sarshar , Xiaodong Cao , Farid Bakir
发明人： Adnan Mjalli , Sepehr Sarshar , Xiaodong Cao , Farid Bakir
IPC分类号： C07D47104
CPC分类号： C07D471/04
摘要： Y—X—C(R′)═C(R″)COOR′″ (A1) The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phosphotyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryoic cells, whole animals and human beings. R′ and R″ are independently selected from the group consisting of hydrogen, halo, cyano, nitro, trihalomethyl, alkyl, arylalkyl. R′″ is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, arylalkyl, X is aryl, Y is selected from hydrogen or wherein (*) indicates a potential point of attachment to X.
摘要翻译：本发明涉及具有式（A1）所示的一般结构的新型蛋白质酪氨酸磷酸酶调节化合物，其制备方法，包含该化合物的组合物，其用于治疗人和动物病症的用途，用于其纯化的蛋白质或糖蛋白，以及它们在诊断中的用途。本发明涉及在体外系统，微生物，真核细胞，整个动物和人类中调节具有磷酸酪氨酸识别单元的分子的活性，包括蛋白酪氨酸磷酸酶（PTP酶）和具有Src同源性-2结构域的蛋白质。 R'和R“独立地选自氢，卤素，氰基，硝基，三卤代甲基，烷基，芳基烷基。 R“选自氢，烷基，取代的烷基，芳基，芳基烷基，X是芳基，Y选自氢或其中（*）表示与X连接的潜在点。

10. 发明授权

US06358946B1 C-6 ring-substituted pyrido[1,2-a]benzimidazole derivatives useful in treating central nervous system disorders 有权
标题翻译：可用于治疗中枢神经系统疾病的C-6环取代的吡啶并[1,2-a]苯并咪唑衍生物
公开(公告)号：US06358946B1
公开(公告)日：2002-03-19
申请号：US09619804
申请日：2000-07-20
申请人： Allen B. Reitz , Samuel O. Nortey , Pauline Sanfilippo , Malcolm K. Scott
发明人： Allen B. Reitz , Samuel O. Nortey , Pauline Sanfilippo , Malcolm K. Scott
IPC分类号： C07D47104
CPC分类号： C07D471/04
摘要： A C-6 ring-substituted pyrido[1,2-a]benzimidazole derivative of the formula: methods of preparation and pharmaceutical compositions containing a substituted pyrido[1,2-a]benzimidzole derivative as the active ingredient are disclosed. The substituted pyrido[1,2-a]benzimidazole derivatives are useful in the treatment of central nervous system disorders.
摘要翻译：公开了下式的C-6环取代的吡啶并[1,2-a]苯并咪唑衍生物：制备方法和含有取代的吡啶并[1,2-a]苯并咪唑衍生物作为活性成分的药物组合物。取代的吡啶并[1,2-a]苯并咪唑衍生物可用于治疗中枢神经系统疾病。

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