公开(公告)号：US07314874B2

公开(公告)日：2008-01-01

申请号：US10942733

申请日：2004-09-15

申请人： Bing-Yan Zhu ,  Penglie Zhang ,  Wenrong Huang ,  Robert M. Scarborough, deceased

发明人： Bing-Yan Zhu ,  Penglie Zhang ,  Wenrong Huang ,  Robert M. Scarborough, deceased

IPC分类号： C07D401/02 ,  A61K31/44

CPC分类号： A61K31/44 ,  A61K9/20 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/48 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/616 ,  A61K45/06 ,  A61K2201/094 ,  C07C237/42 ,  C07C255/60 ,  C07C257/18 ,  C07C259/18 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D295/125 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

摘要： Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

摘要翻译： 描述了具有抗哺乳动物因子Xa活性的新型苯甲酰胺化合物，包括其药学上可接受的异构体，盐，水合物，溶剂合物和前药衍生物。 还描述了含有这些化合物的组合物。 化合物和组合物在体外或体内可用于预防或治疗凝血障碍。

公开(公告)号：US20070275932A1

公开(公告)日：2007-11-29

申请号：US11637251

申请日：2006-12-08

申请人： Michael Kelly ,  Satyanarayana Janagani ,  Ravindra Upasani

发明人： Michael Kelly ,  Satyanarayana Janagani ,  Ravindra Upasani

IPC分类号： A61K31/5377 ,  A61K31/192 ,  A61K31/216 ,  A61P37/06 ,  C07D209/18 ,  C07D231/12 ,  C07D295/04 ,  C07D401/04 ,  C07D413/04 ,  C07D333/38 ,  C07D233/56 ,  C07D213/70 ,  C07C323/09 ,  A61P19/02 ,  A61K31/404

CPC分类号： C07C291/02 ,  C07C309/46 ,  C07C309/61 ,  C07C309/76 ,  C07C311/16 ,  C07C323/47 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/42 ,  C07D213/65 ,  C07D213/70 ,  C07D213/74 ,  C07D213/75 ,  C07D215/36 ,  C07D231/12 ,  C07D233/06 ,  C07D295/135 ,  C07D333/38 ,  C07F9/3856 ,  C07F9/4021

摘要： Disclosed are aryl, heteroaromatic and bicyclic aryl nitrone compounds and pharmaceutical compositions containing such derivatives. The disclosed compositions are useful for preventing and/or treating pain, neurodegenerative, autoimmune and inflammatory diseases or conditions in mammals.

摘要翻译： 公开了芳基，杂芳族和双环芳基硝酮化合物和含有这些衍生物的药物组合物。 所公开的组合物可用于预防和/或治疗哺乳动物中的疼痛，神经退行性，自身免疫性和炎性疾病或病症。

公开(公告)号：US20070244153A1

公开(公告)日：2007-10-18

申请号：US11658098

申请日：2005-07-19

申请人： Takeshi Kakimoto ,  Hisato Kamekawa ,  Yutaka Chiba ,  Toshiyuki Kohno ,  Yumi Kobayashi ,  Naofumi Tomura ,  Natsuko Araki ,  Masako Yoshida ,  Yoji Aoki ,  Shinichi Banba

发明人： Takeshi Kakimoto ,  Hisato Kamekawa ,  Yutaka Chiba ,  Toshiyuki Kohno ,  Yumi Kobayashi ,  Naofumi Tomura ,  Natsuko Araki ,  Masako Yoshida ,  Yoji Aoki ,  Shinichi Banba

IPC分类号： A01N37/12 ,  A01N43/06 ,  A01N43/08 ,  A01N43/32 ,  A01N43/40 ,  A01N43/42 ,  C07C233/01

CPC分类号： C07D405/12 ,  C07C209/42 ,  C07C269/04 ,  C07C269/06 ,  C07C271/22 ,  C07C271/34 ,  C07C271/54 ,  C07C311/16 ,  C07C317/44 ,  C07C323/41 ,  C07C333/04 ,  C07C2601/08 ,  C07C2601/14

摘要： It is an object of the invention to provide a novel fungicide which exhibits a wide controlling spectrum against pathogens of various crops, and solves the toleration problem. The diamine derivative represented by the formula (1) and a process for preparation of the same, fungicides comprising the same as an active ingredient are disclosed: [wherein R1 is substituents such as an alkyl group having 1 to 6 carbon atoms and the like, R2 and R5 are each independently substituents such as hydrogen atom, an alkyl group having 1 to 6 carbon atoms and the like, R3 and R4 are each independently substituents such as hydrogen atom, an alkyl group having 1 to 6 carbon atoms and the like, or R3 and R4 may be bonded to each other to form a hydrocarbon ring having 3 to 6 carbon atoms, R6, R7, R8 and R9 are each independently substituents such as hydrogen atom, an alkyl group having 1 to 6 carbon atoms and the like, R10 is a substituent such as hydrogen atom, an alkyl group having 1 to 6 carbon atoms and the like, A is an oxygen atom or a sulfur atom, and Q is an aryl group or a heterocycle].

摘要翻译： 本发明的目的是提供一种对各种作物的病原体具有广泛控制谱的新型杀真菌剂，并解决了耐受性问题。 公开了式（1）表示的二胺衍生物及其制备方法：其中R1为具有1-6个碳原子的烷基等的取代基， R 2和R 5各自独立地为氢原子，碳原子数为1〜6的烷基等取代基，R 3和R 4各自独立地为氢原子，碳原子数1〜6的烷基等取代基， 或者R 3和R 4可以彼此键合形成具有3至6个碳原子的烃环，R 6，R 7，R 8和R 9各自独立地为氢原子，具有1至6个碳原子的烷基等取代基 中，R 10为氢原子，碳原子数为1〜6的烷基等取代基，A为氧原子或硫原子，Q为芳基或杂环。

公开(公告)号：US20070105914A1

公开(公告)日：2007-05-10

申请号：US10571842

申请日：2004-09-14

申请人： Helen Armstrong ,  Linda Chang ,  Ravindra Guthikonda ,  William Hagmann ,  Linus Lin ,  Shrenik Shah

发明人： Helen Armstrong ,  Linda Chang ,  Ravindra Guthikonda ,  William Hagmann ,  Linus Lin ,  Shrenik Shah

IPC分类号： A61K31/44 ,  A61K31/277 ,  A61K31/18

CPC分类号： C07C311/06 ,  A61K31/18 ,  A61K31/277 ,  A61K31/44 ,  C07C311/03 ,  C07C311/13 ,  C07C311/16 ,  C07C311/17 ,  C07C311/19 ,  C07C311/29 ,  C07D209/08

摘要： The substituted sulfonamides of the invention are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

摘要翻译： 本发明的取代磺酰胺是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。 本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管 事故和头部创伤，焦虑症，压力，癫痫，帕金森病，运动障碍和精神分裂症。该化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘， 便秘，慢性肠假性梗阻和肝硬化。

公开(公告)号：US20070082897A1

公开(公告)日：2007-04-12

申请号：US11548501

申请日：2006-10-11

申请人： Hartmut STROBEL ,  Paulus WOHLFART ,  Alena SAFAROVA ,  Armin WALSER ,  Teri SUZUKI ,  Karl SCHONAFINGER ,  Ramalinga DHARANIPRAGADA

发明人： Hartmut STROBEL ,  Paulus WOHLFART ,  Alena SAFAROVA ,  Armin WALSER ,  Teri SUZUKI ,  Karl SCHONAFINGER ,  Ramalinga DHARANIPRAGADA

IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/517 ,  A61K31/498 ,  A61K31/497 ,  A61K31/4709 ,  A61K31/428 ,  A61K31/423 ,  C07D417/02 ,  C07D413/02

CPC分类号： C07D213/81 ,  C07C233/58 ,  C07C233/65 ,  C07C233/66 ,  C07C233/74 ,  C07C233/76 ,  C07C235/42 ,  C07C235/54 ,  C07C235/84 ,  C07C237/38 ,  C07C237/42 ,  C07C255/57 ,  C07C255/60 ,  C07C309/66 ,  C07C309/73 ,  C07C311/08 ,  C07C311/16 ,  C07C311/21 ,  C07C317/44 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2602/08 ,  C07D207/34 ,  C07D213/56 ,  C07D213/82 ,  C07D215/48 ,  C07D235/08 ,  C07D241/24 ,  C07D249/04 ,  C07D261/18 ,  C07D295/185 ,  C07D307/78 ,  C07D307/84 ,  C07D317/60 ,  C07D333/24 ,  C07D401/06

摘要： The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1—R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B is CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description. These compounds are useful in the upregulation of endothelial nitric oxide synthase (eNOS), and may therefore be useful for the manufacture of medicaments for the treatment of cardiovascular diseases, stable or unstable angina pectoris, coronary heart disease, Prinzmetal angina, acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease, endothelial dysfunction, atherosclerosis, restenosis, endothelial damage after PTCA, hypertension, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular hypertension, chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, diabetes or diabetes complications, nephropathy or retinopathy, angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, osteoporosis, restricted memory performance, a restricted ability to learn, or for the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives.

摘要翻译： 本发明涉及根据通式（I）的酰化茚满基胺，其中R 1 -R 4具有说明书中给出的含义，A是CH CH 2或CH-（C 1 -C 3 - 烷基），B是CH 2或CH-（C（C 1 -C 3） C 1 -C 3烷基），R 5是可以被描述中所列取代基取代的芳基或杂芳基。 这些化合物可用于内皮一氧化氮合酶（eNOS）的上调，因此可用于制备用于治疗心血管疾病，稳定或不稳定型心绞痛，冠心病，Prinzmetal心绞痛，急性冠状动脉综合征， 心脏衰竭，心肌梗塞，中风，血栓形成，外周动脉闭塞性疾病，内皮功能障碍，动脉粥样硬化，再狭窄，PTCA后的内皮损伤，高血压，原发性高血压，肺动脉高压，继发性高血压，肾血管性高血压，慢性肾小球肾炎，勃起功能障碍，室性心律失常， 糖尿病或糖尿病并发症，肾病或视网膜病变，血管生成，支气管哮喘，慢性肾功能衰竭，肝硬化，骨质疏松症，受限记忆能力，受限的学习能力或降低绝经后妇女的心血管危险或摄入避孕药 。

公开(公告)号：US20070021472A1

公开(公告)日：2007-01-25

申请号：US11488455

申请日：2006-07-17

申请人： Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song ,  Robert Scarborough

发明人： Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song ,  Robert Scarborough

IPC分类号： A61K31/44

CPC分类号： A61K31/44 ,  A61K9/20 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/48 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/616 ,  A61K45/06 ,  A61K2201/094 ,  C07C237/42 ,  C07C255/60 ,  C07C257/18 ,  C07C259/18 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D295/125 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

摘要： Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

摘要翻译： 描述了具有抗哺乳动物因子Xa活性的新型苯甲酰胺化合物，包括其药学上可接受的异构体，盐，水合物，溶剂合物和前药衍生物。 还描述了含有这些化合物的组合物。 化合物和组合物在体外或体内可用于预防或治疗凝血障碍。

公开(公告)号：US20060287377A1

公开(公告)日：2006-12-21

申请号：US10556229

申请日：2004-05-13

申请人： Yevgeni Besidski ,  Inger Kers ,  Martin Nylof ,  Didier Rotticci ,  Andis Slaitas ,  Mats Svensson

发明人： Yevgeni Besidski ,  Inger Kers ,  Martin Nylof ,  Didier Rotticci ,  Andis Slaitas ,  Mats Svensson

IPC分类号： A61K31/4184 ,  C07D403/02

CPC分类号： C07D209/08 ,  C07C215/16 ,  C07C229/56 ,  C07C233/15 ,  C07C233/47 ,  C07C311/16 ,  C07C317/14 ,  C07C317/36 ,  C07D235/06 ,  C07D235/08 ,  C07D401/12 ,  C07D403/04 ,  C07D405/12 ,  C07D417/12

摘要： Compounds of formula I, wherein R1, m, R2, R3, p, n, R5 and R9 are as defined as in the specification, salts, solvates or solvated salts thereof, processes for their preparation, intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and the use of said compounds in therapy.

摘要翻译： 式I的化合物，其中R 1，m，R 2，R 3，p，n，R 5， >和R 9如本说明书中所定义，其盐，溶剂合物或溶剂化盐，其制备方法，其制备中使用的中间体，含有所述化合物的药物制剂和所述化合物的用途 在治疗。

公开(公告)号：US20060128957A1

公开(公告)日：2006-06-15

申请号：US11338378

申请日：2006-01-24

申请人： Wei Zhang ,  Zhiyong Luo

发明人： Wei Zhang ,  Zhiyong Luo

IPC分类号： C40B40/04 ,  C07D207/40

CPC分类号： C07D491/10 ,  C07B51/00 ,  C07B63/02 ,  C07C17/16 ,  C07C22/08 ,  C07C43/23 ,  C07C45/71 ,  C07C47/575 ,  C07C53/50 ,  C07C211/14 ,  C07C211/15 ,  C07C213/00 ,  C07C265/04 ,  C07C273/1827 ,  C07C311/16 ,  C07C323/20 ,  C07C335/16 ,  C07D207/46 ,  C07D209/14 ,  C07D209/16 ,  C07D211/62 ,  C07D213/74 ,  C07D217/04 ,  C07D217/06 ,  C07D231/38 ,  C07D265/26 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07C217/34 ,  C07C275/28

摘要： The present invention includes methods and compositions for increasing the fluorous nature of an organic compound by reacting it with at least one fluorous compound to produce a fluorous tagged organic compound. The increased fluorous nature of the fluorous tagged organic compound can then be utilized to separate the fluorous organic compound from untagged reagents, reactants, catalysts and/or products derived therefrom. The resultant fluorous tagged organic compound can be subjected to subsequent chemical transformations, wherein the fluorous nature of the tagged compound is utilized to increase the ease of separation of the fluorous tagged organic compound from untagged reagents, reactants, catalysts and/or products derived therefrom, after each chemical transformation. The chemical transformations result in a second fluorous tagged organic compound wherein the fluorous nature of the second fluorous tagged organic compound can then be reduced by removing the fluorous group therefrom, thereby producing a second organic compound that may be employed as a pharmaceutical compound or intermediate, or a combinatorial library component.

公开(公告)号：US07060850B2

公开(公告)日：2006-06-13

申请号：US10617431

申请日：2003-07-11

申请人： Wei Zhang ,  Zhiyong Luo ,  Tadamichi Nagashima ,  Christine Hiu-Tung Chen ,  Marvin S. Yu

发明人： Wei Zhang ,  Zhiyong Luo ,  Tadamichi Nagashima ,  Christine Hiu-Tung Chen ,  Marvin S. Yu

IPC分类号： C07F7/08

CPC分类号： C07D491/10 ,  C07B51/00 ,  C07B63/02 ,  C07C17/16 ,  C07C22/08 ,  C07C43/23 ,  C07C45/71 ,  C07C47/575 ,  C07C53/50 ,  C07C211/14 ,  C07C211/15 ,  C07C213/00 ,  C07C265/04 ,  C07C273/1827 ,  C07C311/16 ,  C07C323/20 ,  C07C335/16 ,  C07D207/46 ,  C07D209/14 ,  C07D209/16 ,  C07D211/62 ,  C07D213/74 ,  C07D217/04 ,  C07D217/06 ,  C07D231/38 ,  C07D265/26 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07C217/34 ,  C07C275/28

摘要： The present invention includes methods and compositions for increasing the fluorous nature of an organic compound by reacting it with at least one fluorous compound to produce a fluorous tagged organic compound. The increased fluorous nature of the fluorous tagged organic compound can then be utilized to separate the fluorous organic compound from untagged reagents, reactants, catalysts and/or products derived therefrom. The resultant fluorous tagged organic compound can be subjected to subsequent chemical transformations, wherein the fluorous nature of the tagged compound is utilized to increase the ease of separation of the fluorous tagged organic compound from untagged reagents, reactants, catalysts and/or products derived therefrom, after each chemical transformation. The chemical transformations result in a second fluorous tagged organic compound wherein the fluorous nature of the second fluorous tagged organic compound can then be reduced by removing the fluorous group therefrom, thereby producing a second organic compound that may be employed as a pharmaceutical compound or intermediate, or a combinatorial library component.

公开(公告)号：US20050261346A1

公开(公告)日：2005-11-24

申请号：US10942733

申请日：2004-09-15

申请人： Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song ,  Robert Scarborough

发明人： Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song ,  Robert Scarborough

IPC分类号： A61K31/443 ,  A61K31/444 ,  A61P7/02 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14 ,  C07D521/00 ,  C07D41/02 ,  C07D49/02

CPC分类号： A61K31/44 ,  A61K9/20 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/48 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/616 ,  A61K45/06 ,  A61K2201/094 ,  C07C237/42 ,  C07C255/60 ,  C07C257/18 ,  C07C259/18 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D295/125 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

摘要： Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

摘要翻译： 描述了具有抗哺乳动物因子Xa活性的新型苯甲酰胺化合物，包括其药学上可接受的异构体，盐，水合物，溶剂合物和前药衍生物。 还描述了含有这些化合物的组合物。 化合物和组合物在体外或体内可用于预防或治疗凝血障碍。