公开(公告)号：US20060223741A1

公开(公告)日：2006-10-05

申请号：US11315354

申请日：2005-12-23

申请人： Maree Smith ,  Bruce Wyse

发明人： Maree Smith ,  Bruce Wyse

IPC分类号： A61K38/17 ,  A61K48/00 ,  A61K31/503 ,  A61K31/519 ,  A61K31/4745 ,  A61K31/495 ,  A61K31/4709

CPC分类号： C07D471/04 ,  A61K31/517 ,  A61K38/08 ,  C07D239/90 ,  C07D401/06 ,  C07D403/10 ,  C07D403/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/12 ,  G01N33/74 ,  G01N2500/00

摘要： The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of neuropathic pain, including mechanical hyperalgesia, thermal or mechanical allodynia, diabetic pain and entrapment pain, in vertebrate animals and particularly in human subjects. The AT2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of neuropathic conditions.

摘要翻译： 本发明涉及可用于预防和改善与神经病变相关的体征和症状的方法和试剂。 更具体地，本发明公开了血管紧张素II受体2（AT2受体）拮抗剂用于神经性疼痛的治疗，预防，逆转和/或症状缓解的用途，包括机械痛觉过敏，热或机械 异常性疼痛，糖尿病疼痛和包埋疼痛，在脊椎动物中，特别是在人类受试者中。 AT 2受体拮抗剂可以单独提供或与其它化合物组合提供，例如可用于控制神经病症状况的那些。

公开(公告)号：US07087612B2

公开(公告)日：2006-08-08

申请号：US10734949

申请日：2003-12-13

申请人： Rosa Maria Rodriguez Sarmiento ,  Andrew William Thomas ,  Rene Wyler

发明人： Rosa Maria Rodriguez Sarmiento ,  Andrew William Thomas ,  Rene Wyler

IPC分类号： A61K31/517 ,  A01N43/54 ,  C07D239/72 ,  A61P25/28 ,  C07C43/20 ,  C07C63/04

CPC分类号： C07D239/90

摘要： This invention relates to 3H-quinazolin-4-one derivatives as defined in the specification and claims, to a process for their preparation, to pharmaceutical compositions comprising them and to their use as selective monoamine oxidase B inhibitors.

摘要翻译： 本发明涉及如说明书和权利要求书中定义的3H-喹唑啉-4-酮衍生物及其制备方法，包含它们的药物组合物及其作为选择性单胺氧化酶B抑制剂的用途。

公开(公告)号：US20060172994A1

公开(公告)日：2006-08-03

申请号：US11320414

申请日：2005-12-28

申请人： Kenneth Carson ,  Prakash Raman ,  Francois Soucy ,  Qing Ye ,  Shomir Ghosh

发明人： Kenneth Carson ,  Prakash Raman ,  Francois Soucy ,  Qing Ye ,  Shomir Ghosh

IPC分类号： A61K31/55 ,  A61K31/496 ,  A61K31/551 ,  A61K31/454 ,  C07D403/02

CPC分类号： C07D207/12 ,  A61K31/454 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/517 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D207/14 ,  C07D211/46 ,  C07D239/30 ,  C07D239/86 ,  C07D239/90 ,  C07D295/073 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/14 ,  C07D473/32

摘要： The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders.

摘要翻译： 本发明涉及可用作趋化因子受体拮抗剂的化合物。 提供通式I的化合物：或其药学上可接受的盐。 本发明还提供包含所述化合物的药学上可接受的组合物和使用化合物和组合物抑制趋化因子受体的方法，还用于治疗各种疾病，病症或病症，包括急性或慢性炎性疾病，癌症或溶骨性骨骼疾病 。

公开(公告)号：US20060089500A1

公开(公告)日：2006-04-27

申请号：US11296749

申请日：2005-12-07

申请人： Ranga Gurram ,  Venkateswarlu Akella ,  Rajagopalan Ramanujam ,  Ranjan Chakrabarti ,  Parimal Misra ,  Vidya Lohray ,  Braj Lohray ,  Rao Paraselli

发明人： Ranga Gurram ,  Venkateswarlu Akella ,  Rajagopalan Ramanujam ,  Ranjan Chakrabarti ,  Parimal Misra ,  Vidya Lohray ,  Braj Lohray ,  Rao Paraselli

IPC分类号： A61K31/513 ,  C07D239/02

CPC分类号： C07D239/36 ,  C07C217/22 ,  C07C237/32 ,  C07C247/04 ,  C07D239/90

摘要： The present invention relates to novel antiobesity and hypocholesterolemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel β-aryl-α-oxysubstituted alkylcarboxylic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. The present invention also relates to a process for the preparation of the above said novel compounds, their analogs, their derivatives, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them. The present invention also relates to novel intermediates, processes for their preparation and their use in the preparation of compounds of formula (I).

公开(公告)号：US20050277631A1

公开(公告)日：2005-12-15

申请号：US11195134

申请日：2005-08-01

申请人： Elizabeth Doherty ,  Jiawang Zhu ,  Markian Stec ,  Mark Norman ,  Hui-Ling Wang ,  Christopher Fotsch ,  Ning Chen ,  Partha Chakrabarti ,  Celia Dominguez ,  James Falsey ,  Christopher Hulme ,  Jodie Katon ,  Thomas Nixey ,  Vassil Ognyanov ,  Liping Pettus ,  Robert Rzasa

发明人： Elizabeth Doherty ,  Jiawang Zhu ,  Markian Stec ,  Mark Norman ,  Hui-Ling Wang ,  Christopher Fotsch ,  Ning Chen ,  Partha Chakrabarti ,  Celia Dominguez ,  James Falsey ,  Christopher Hulme ,  Jodie Katon ,  Thomas Nixey ,  Vassil Ognyanov ,  Liping Pettus ,  Robert Rzasa

IPC分类号： A61P29/00 ,  C07D209/08 ,  C07D209/12 ,  C07D209/42 ,  C07D209/48 ,  C07D213/26 ,  C07D213/64 ,  C07D213/643 ,  C07D213/74 ,  C07D213/75 ,  C07D215/22 ,  C07D215/227 ,  C07D215/38 ,  C07D217/04 ,  C07D231/40 ,  C07D231/56 ,  C07D233/38 ,  C07D239/42 ,  C07D239/90 ,  C07D241/42 ,  C07D263/56 ,  C07D265/36 ,  C07D277/62 ,  C07D277/82 ,  C07D307/79 ,  C07D319/20 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  A61K31/549 ,  A61K31/501 ,  C07D417/02 ,  C07D43/02

CPC分类号： C07D231/40 ,  C07D209/08 ,  C07D209/12 ,  C07D209/42 ,  C07D209/48 ,  C07D213/26 ,  C07D213/643 ,  C07D213/74 ,  C07D213/75 ,  C07D215/227 ,  C07D215/38 ,  C07D217/04 ,  C07D231/56 ,  C07D233/38 ,  C07D239/42 ,  C07D239/90 ,  C07D241/42 ,  C07D263/56 ,  C07D265/36 ,  C07D277/62 ,  C07D277/82 ,  C07D307/79 ,  C07D319/20 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

摘要： Compounds having the general structure 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 necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

公开(公告)号：US06831085B1

公开(公告)日：2004-12-14

申请号：US09724941

申请日：2000-11-28

申请人： Gustave Bergnes ,  Whitney W. Smith ,  John C. Chabala

发明人： Gustave Bergnes ,  Whitney W. Smith ,  John C. Chabala

IPC分类号： A61K31517

CPC分类号： C07D239/90 ,  C07D239/91

摘要： Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.

摘要翻译： 公开了式1a，1b，1c和1d的喹唑啉酮。 它们可用于治疗与KSP驱动蛋白活性相关的细胞增殖性疾病和病症。

公开(公告)号：US20040067969A1

公开(公告)日：2004-04-08

申请号：US10366828

申请日：2003-02-14

发明人： Gustave Bergnes ,  Edward Ha ,  George Yiannikouros ,  Panos Kalaritis ,  Brandon E. Yonce ,  Kurt Alan Welday JR.

IPC分类号： A61K031/517 ,  C07D239/72

CPC分类号： C07D239/90 ,  C07B2200/07 ,  C07D239/91

摘要： The present invention provides intermediates, synthetic methods and novel quinazolinone compositions of matter.

摘要翻译： 本发明提供了物质的中间体，合成方法和新颖的喹唑啉酮组合物。

公开(公告)号：US20040048797A1

公开(公告)日：2004-03-11

申请号：US10419327

申请日：2003-04-17

发明人： Karen Miller ,  Anita Diu-Hercend ,  Thierry Hercend ,  Paul Lang ,  Peter Weber ,  Julian Golec ,  Michael Mortimore

IPC分类号： A61K038/06 ,  A61K038/05 ,  A61K038/04 ,  C07K005/06 ,  C07K005/04

CPC分类号： C07D235/24 ,  A61K38/00 ,  C07C233/64 ,  C07C233/83 ,  C07C235/52 ,  C07C237/22 ,  C07C237/42 ,  C07C255/57 ,  C07C271/22 ,  C07C271/28 ,  C07C2601/14 ,  C07D209/42 ,  C07D209/86 ,  C07D211/60 ,  C07D217/24 ,  C07D233/90 ,  C07D239/90 ,  C07D401/06 ,  C07D405/12 ,  C07D409/06 ,  C07D417/06 ,  C07D455/04 ,  C07D487/04 ,  C07F9/3264 ,  C07F9/65128 ,  C07K5/0202 ,  G01N33/6863 ,  G01N2333/525 ,  G01N2500/04 ,  Y02A50/411

摘要： The present invention relates to methods for identifying compounds useful for regulating TNF-alpha levels and/or activity. The invention also relates to methods for decreasing TNF-alpha levels and/or activity. Compounds and compositions according to this invention are useful for treating TNF-mediated diseases. The invention also relates to kits comprising the compounds and compositions herein and a tool for measuring TNF-alpha activity and/or levels.

摘要翻译： 本发明涉及用于鉴定可用于调节TNF-α水平和/或活性的化合物的方法。 本发明还涉及降低TNF-α水平和/或活性的方法。 根据本发明的化合物和组合物可用于治疗TNF介导的疾病。 本发明还涉及包含本文的化合物和组合物的试剂盒以及用于测量TNF-α活性和/或水平的工具。

公开(公告)号：US20040043987A1

公开(公告)日：2004-03-04

申请号：US10642224

申请日：2003-08-18

申请人： Neurosearch A/S.

发明人： Alex Haaht Gouliaev ,  Mogens Larsen ,  Thomas Varming ,  Claus Mathiesen ,  Tina Holm Johansen ,  Jorgen Scheel-Kruger ,  Gunnar M. Olsen ,  Elsesbet Ostergaard Nielsen

IPC分类号： A61K031/538 ,  A61K031/517 ,  A61K031/4709

CPC分类号： C07D417/04 ,  C07D239/90 ,  C07D285/24 ,  C07D285/28 ,  C07D513/04

摘要： The invention provides novel compounds represented by the general formula 5 compound represented by the formula: 1 wherein the bond represented by the broken line may be a single, a double bond or absent; and if the bond is absent, then the nitrogen is substituted with a hydrogen and R2; X represents SO2 or CnullO or CH2; Y represents nullCH(R4)null, nullN(R4)null or nullN(R4)nullCH2null, O; and the meaning of R2, R3, R4, R5, R6, R7, and R8 are as defined in the application The compounds are useful as positive modulators of the AMPA-receptor.

摘要翻译： 本发明提供由通式5表示的由下式表示的化合物的新化合物：其中由虚线表示的键可以是单键，双键或不存在; 如果不存在键，则氮被氢和R 2取代; X表示SO 2或C = O或CH 2; Y表示-CH（R 4） - ， - N（R 4） - 或-N（R 4）-CH 2 - ，O; R 2，R 3，R 4，R 5，R 6，R 7和R 8的含义如本申请中所定义。该化合物可用作 AMPA受体的阳性调节剂。

公开(公告)号：US20040038969A1

公开(公告)日：2004-02-26

申请号：US10445170

申请日：2003-05-20

发明人： Elizabeth M. Doherty ,  Jiawang Zhu ,  Markian Stec ,  Mark H. Norman ,  Vassil I. Ognyanov ,  Christopher H. Fotsch ,  Ning Chen ,  Partha P. Chakrabarti ,  Liping H. Pettus ,  Hui-Ling Wang ,  Xianghong Wang ,  Premilla Arasasingham

IPC分类号： C07D417/02 ,  C07D413/02 ,  C07D43/02 ,  A61K031/541 ,  A61K031/5377 ,  A61K031/496 ,  A61K031/506 ,  A61K031/501

CPC分类号： C07D231/40 ,  C07D209/08 ,  C07D209/12 ,  C07D209/42 ,  C07D209/48 ,  C07D213/26 ,  C07D213/643 ,  C07D213/74 ,  C07D213/75 ,  C07D215/227 ,  C07D215/38 ,  C07D217/04 ,  C07D231/56 ,  C07D233/38 ,  C07D237/20 ,  C07D239/42 ,  C07D239/90 ,  C07D241/42 ,  C07D263/56 ,  C07D265/36 ,  C07D277/62 ,  C07D277/82 ,  C07D307/79 ,  C07D319/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： Compounds having the general structure 1 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, pruritis, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

摘要翻译： 具有一般结构和含有它们的组合物的化合物，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， 咳嗽痛，交感神经痛，交感综合征，哮喘，上皮组织损伤或功能障碍，单纯疱疹，呼吸道内脏运动紊乱，泌尿生殖道，胃肠道或血管区，伤口，烧伤，过敏性皮肤反应，瘙痒症，白癜风，一般胃肠道疾病， G 腹部溃疡，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。