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111. 发明申请

US20040138223A1 Novel amide derivatives and medicinal use thereof ugs 失效
标题翻译：新型酰胺衍生物及其药物用途
公开(公告)号：US20040138223A1
公开(公告)日：2004-07-15
申请号：US10380502
申请日：2003-05-08
发明人： Mitsuharu Nakamura , Takao Kamahori , Seigo Ishibuchi , Yoichi Naka , Hiroshi Sumichika , Katsuhiko Itoh
IPC分类号： A61K031/506 , A61K031/501 , A61K031/497 , A61K031/4709 , C07D43/02
CPC分类号： C07D213/40 , C07C233/59 , C07C233/60 , C07C233/62 , C07C235/40 , C07C255/29 , C07C255/60 , C07C317/32 , C07C317/40 , C07C323/40 , C07C327/46 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D213/64 , C07D213/65 , C07D213/69 , C07D213/74 , C07D213/75 , C07D215/50 , C07D231/12 , C07D233/56 , C07D249/08 , C07D277/28 , C07D295/13 , C07D295/135 , C07D295/185 , C07D309/12 , C07D311/04 , C07D311/66 , C07D317/58 , C07D317/66 , C07D319/18 , C07D333/20 , C07D333/36 , C07D335/06 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/06 , C07D409/14 , C07D417/12 , C07D417/14 , C07D513/04
摘要： The present invention relates to an amide derivative of the formula (1), having a C5a receptor antagonistic action 1 wherein each symbol is as defined in the specification. The above-mentioned amide derivative, an optically active form thereof and a pharmaceutically acceptable salt thereof are promising as an agent for the treatment or prophylaxis of diseases or syndromes caused by inflammation caused by C5a nulle.g., autoimmune diseases such as rheumatism, systemic lupus erythematosus and the like, sepsis, adult respiratory distress syndrome, chronic obstructive pulmonary disease, allergic diseases such as asthma and the like, atherosclerosis, cardiac infarction, brain infarction, psoriasis, Alzheimer's disease and serious organ injury (e.g., pneumonia, nephritis, hepatitis and pancreatitis and the like) due to activation of leukocytes caused by ischemia reperfusion, trauma, burn, surgical invasion and the likenull. Moreover, they are useful as a therapeutic or prophylactic agent for the infectious diseases caused by bacteria and virus that invade via a C5a receptor.
摘要翻译：本发明涉及具有C5a受体拮抗作用的式（1）的酰胺衍生物，其中每个符号如说明书中所定义。上述酰胺衍生物，其光学活性形式和其药学上可接受的盐有望用作治疗或预防由C5a引起的炎症引起的疾病或综合征的药物[例如，自身免疫疾病如风湿病，系统性红斑狼疮败血症，成人呼吸窘迫综合征，慢性阻塞性肺病，哮喘等过敏性疾病，动脉粥样硬化，心肌梗死，脑梗塞，牛皮癣，阿尔茨海默病和严重器官损伤（例如肺炎，肾炎，肝炎和胰腺炎等）由于由缺血再灌注，创伤，烧伤，手术入侵等引起的白细胞的活化]。此外，它们可用作由通过C5a受体侵入的细菌和病毒引起的感染性疾病的治疗或预防剂。

112. 发明授权

US06750255B2 Calcium receptor-active compounds 失效
标题翻译：钙受体活性化合物
公开(公告)号：US06750255B2
公开(公告)日：2004-06-15
申请号：US10053133
申请日：2002-01-17
申请人： Teruyuki Sakai , Atsuya Takami , Rika Nagao
发明人： Teruyuki Sakai , Atsuya Takami , Rika Nagao
IPC分类号： A61K31145
CPC分类号： C07D207/335 , C07B2200/07 , C07C211/30 , C07C217/20 , C07C217/58 , C07C237/06 , C07C237/08 , C07C237/10 , C07C317/18 , C07C317/28 , C07C323/25 , C07C2603/18 , C07D209/08 , C07D209/14 , C07D209/88 , C07D213/38 , C07D213/40 , C07D213/70 , C07D215/36 , C07D241/12 , C07D263/58 , C07D277/28 , C07D277/74 , C07D281/06 , C07D307/52 , C07D307/91 , C07D311/30 , C07D317/58 , C07D333/20 , C07D333/34
摘要： A novel calcium receptor active compound having the formula is provided: Ar1—[CR1R2]p—X—[CR3R4]q—[CR5R6]—NR7—[CR8R9]—Ar2 wherein: Ar1 is selected from the group consisting of aryl, heteroaryl, bis(arylmethyl)amino, bis(heteroarylmethyl)amino and arylmethyl(heteroarylmethyl)amino; X is selected from the group consisting of oxygen, sulfur, sulfinyl, sulfonyl, carbonyl and amino; R1, R2, R3, R4, R5, R6, R7, R8 and R9 are, for example, hydrogen or alkyl; Ar2 is selected from the group consisting of aryl and heteroaryl; p is an integer of from 0 to 6, inclusive; and, q is an integer of from 0 to 14, inclusive.
摘要翻译：提供了具有下式的新型钙受体活性化合物：其中：Ar 1选自芳基，杂芳基，双（芳基甲基）氨基，双（杂芳基甲基）氨基和芳基甲基（杂芳基甲基）氨基; X选自由氧，硫，亚磺酰基，磺酰基，羰基和氨基组成; R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 7， R 8和R 9是例如氢或烷基; Ar 2选自芳基和杂芳基; p是0至6的整数，包括0和6; q为0〜14的整数，包括端值。

113. 发明申请

US20040110753A1 Tyrosine derivatives 审中-公开
标题翻译：酪氨酸衍生物
公开(公告)号：US20040110753A1
公开(公告)日：2004-06-10
申请号：US10198328
申请日：2002-07-16
申请人： Genentech, Inc.
发明人： David Y. Jackson , Frederick C. Sailes , Daniel P. Sutherlin
IPC分类号： A61K031/537 , A61K031/4747 , A61K031/495 , A61K031/454 , A61K031/445 , A61K031/401 , C07D43/02 , C07D471/12
CPC分类号： C07D213/75 , C07C233/87 , C07C271/22 , C07C271/44 , C07C271/48 , C07C271/54 , C07C271/56 , C07C271/58 , C07C311/06 , C07C311/09 , C07C311/58 , C07C323/43 , C07C323/59 , C07D207/16 , C07D207/22 , C07D207/28 , C07D211/46 , C07D211/60 , C07D211/62 , C07D215/36 , C07D217/06 , C07D217/14 , C07D217/22 , C07D231/16 , C07D235/06 , C07D235/26 , C07D249/18 , C07D277/12 , C07D277/56 , C07D295/205 , C07D317/58 , C07D333/20 , C07D333/34 , C07D333/38 , C07D333/62 , C07D333/72 , C07D471/10
摘要： The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.
摘要翻译：本发明的化合物是含有整合素介导的与配体如VCAM-1和MAdCAM结合的α4的抑制剂。

114. 发明授权

US06723743B1 High affinity small molecule C5a receptor modulators 失效
标题翻译：高亲和力小分子C5a受体调节剂
公开(公告)号：US06723743B1
公开(公告)日：2004-04-20
申请号：US09672071
申请日：2000-09-28
申请人： Andrew Thurkauf , Xiao-shu He , He Zhao , John Peterson , Xiaoyan Zhang , Robbin Brodbeck , James Krause , George Maynard , Alan Hutchison
发明人： Andrew Thurkauf , Xiao-shu He , He Zhao , John Peterson , Xiaoyan Zhang , Robbin Brodbeck , James Krause , George Maynard , Alan Hutchison
IPC分类号： A61K31415
CPC分类号： C07D207/327 , C07C233/11 , C07C233/22 , C07C233/65 , C07C233/66 , C07C233/73 , C07C233/78 , C07C235/46 , C07C235/48 , C07C235/54 , C07C235/60 , C07C235/62 , C07C235/66 , C07C237/20 , C07C323/62 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2603/18 , C07D213/38 , C07D213/82 , C07D215/12 , C07D217/04 , C07D217/06 , C07D217/14 , C07D217/16 , C07D231/12 , C07D233/64 , C07D233/68 , C07D235/02 , C07D235/14 , C07D235/18 , C07D317/58 , C07D333/24 , C07D333/28 , C07D333/54 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12 , C07D471/04
摘要： This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors, preferably human C5a receptors, Preferred compounds of the invention possess one or more, and preferably two or more, three or more, four or more, or all of the following properties in that they are; 1) multi-aryl in structure (having a plurality of un-fused or fused aryl groups), 2) heteroaryl in structure, 3) orally available in vivo (such that a sub-lethal or preferably a pharmaceutically acceptable oral dose can provide a detectable in vitro effect such as a reduction of C5a-induced neutropenia), 4) comprised of fewer than four, preferably fewer than three, or fewer than two, or no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar concentrations and preferably at sub-nanomolar concentrations. Specifically exemplified representative compounds include, but are not limited to optionally substituted arylimidazoles, optionally substituted arylpyridyls, optionally substituted aryl-substituted cycloalkylimidazoles, optionally substituted arylpyrazoles, optionally substituted benzimidazoles, optionally substituted aryl-substituted tetrahydroisoquinolines, and optionally substituted biaryl carboxamides. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory and immune system disorders. Additionally, this invention relates to the use such compounds as probes for the localization of C5a receptors.
摘要翻译：本发明涉及作为哺乳动物补体C5a受体调节剂的低分子量，非肽，非拟肽，有机分子，优选用作高亲和力C5a受体配体的调节剂，还涉及作为拮抗剂或反向激动剂的这些配体的补体C5a受体，优选人C5a受体。本发明的优选化合物具有一个或多个，优选两个或更多个，三个或更多个，四个或更多个或全部以下性质： 1）结构上的多芳基（具有多个未稠合或稠合芳基），2）结构上的杂芳基，3）在体内可口服（使得亚致死或优选药学上可接受的口服剂量可提供可检测的体外效应，例如C5a诱导的中性粒细胞减少的减少），4）由少于4个，优选少于3个，或少于2个或不存在的酰胺键组成，以及5）能够以纳摩尔浓度抑制白细胞趋化性，优选亚纳摩尔浓度。具体示例的代表性化合物包括但不限于任选取代的芳基咪唑，任选取代的芳基吡啶基，任选取代的芳基取代的环烷基咪唑，任选取代的芳基吡唑，任选取代的苯并咪唑，任选取代的芳基取代的四氢异喹啉和任选取代的双芳基甲酰胺。本发明还涉及包含这些化合物的药物组合物。它还涉及这些化合物在治疗各种炎性和免疫系统疾病中的应用。此外，本发明涉及使用这些化合物作为C5a受体定位的探针。

115. 发明授权

US06710080B2 Substituted 2-dialkylaminoalkylbiphenyl derivatives 失效
标题翻译：取代的2-二烷基氨基烷基联苯衍生物
公开(公告)号：US06710080B2
公开(公告)日：2004-03-23
申请号：US10071229
申请日：2002-02-11
申请人： Bernd Sundermann , Babette-Yvonne Koegel , Helmut Buschmann
发明人： Bernd Sundermann , Babette-Yvonne Koegel , Helmut Buschmann
IPC分类号： A61K31275
CPC分类号： C07D307/79 , C07C211/29 , C07C215/46 , C07C215/50 , C07C215/52 , C07C217/54 , C07C217/58 , C07C217/60 , C07C223/02 , C07C225/16 , C07C233/43 , C07C317/32 , C07D317/58
摘要： Substituted 2-dialkylaminoalkylbiphenyl derivatives, processes for their preparation, pharmaceutical compositions comprising these compounds and methods using these compounds for the preparation of medicaments and for the treatment of diseases.
摘要翻译：取代的2-二烷基氨基烷基联苯衍生物，其制备方法，包含这些化合物的药物组合物和使用这些化合物制备药物和治疗疾病的方法。

116. 发明申请

US20040053933A1 Ligands of melanocortin receptors and compositions and methods related thereto 审中-公开
标题翻译：黑皮质素受体配体及其组合物和方法
公开(公告)号：US20040053933A1
公开(公告)日：2004-03-18
申请号：US10434803
申请日：2003-05-09
申请人： Neurocrine Biosciences, Inc.
发明人： Joseph Pontillo , Dragan Marinkovic , Marion C. Lanier , Joe Anh Tran , Melissa Arellano , Jessica Parker , Jodie Nelson , Chen Chen , Fabio C. Tucci , Caroline Chen , Wanlong Jiang , Nicole White
IPC分类号： A61K031/506 , A61K031/497 , A61K031/501 , A61K031/496 , C07D43/02
CPC分类号： C07D207/27 , C07D207/14 , C07D207/16 , C07D207/273 , C07D207/335 , C07D211/14 , C07D211/26 , C07D211/28 , C07D211/58 , C07D211/60 , C07D211/62 , C07D213/38 , C07D213/74 , C07D217/26 , C07D223/04 , C07D233/36 , C07D241/08 , C07D265/30 , C07D277/28 , C07D295/185 , C07D295/215 , C07D307/14 , C07D307/52 , C07D317/58 , C07D333/20 , C07D333/22 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14
摘要： Compounds which function as melanocortin receptor ligands and having utility in the treatment of melanocortin receptor-based disorders. The compounds have the following structure (I): 1 including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein Ar, R1, R2, R3a, R3b, R4a, R4b, R5, R7a, R7b, q, r, X, Y1, Y2, Y3 and Y4 are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.
摘要翻译：作为黑皮质素受体配体起作用并可用于治疗基于黑皮质素受体的疾病的化合物。其中Ar，R 1，R 2，R 3a，R 3b，R 4a，R 4b，R 5，R 7a，R 7b，q，r，X，Y 1， Y2，Y3和Y4如本文所定义。还公开了含有结构（I）化合物的药物组合物以及与其用途有关的方法。

117. 发明申请

US20040048913A1 Substituted biaryl amides as C5a receptor modulators 失效
标题翻译：取代的联芳酰胺作为C5a受体调节剂
公开(公告)号：US20040048913A1
公开(公告)日：2004-03-11
申请号：US10401270
申请日：2003-03-27
发明人： Yang Gao , Alan J. Hutchison , John M. Peterson , Wallace C. Pringle , Andrew Thurkauf , Taeyoung Yoon , He Zhao
IPC分类号： A61K031/4178 , A61K031/4025 , C07D45/02 , C07D233/56
CPC分类号： C07D209/08 , C07C233/65 , C07C233/66 , C07C233/73 , C07C235/62 , C07C237/30 , C07C2602/08 , C07D207/325 , C07D231/56 , C07D317/58 , C07D333/24 , C07D405/12
摘要： Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies. 1
摘要翻译：提供式I的取代的联芳酰胺。这些化合物是可用于在体内或体外调节C5a受体活性的配体，并且特别可用于治疗与人类，驯养的伴侣动物和家畜中的病理性C5a受体激活相关的病症。还提供了用于治疗这些病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

118. 发明申请

US20040044075A1 Alpha acyloxyacetamides for kallikrein and urokinase inhibition 审中-公开
标题翻译： α酰氧基乙酰胺，用于激肽释放酶和尿激酶抑制
公开(公告)号：US20040044075A1
公开(公告)日：2004-03-04
申请号：US10448447
申请日：2003-05-29
申请人： Genzyme Corporation
发明人： Mark M. Staveski , Scott F. Sneddon
IPC分类号： A61K031/24
CPC分类号： C07D405/12 , C07C235/34 , C07C235/36 , C07C235/38 , C07C237/30 , C07C255/57 , C07C323/25 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D209/18 , C07D215/12 , C07D239/38 , C07D317/58 , C07D495/04
摘要： Disclosed herein is a compound represented by Structural Formula (I): 1 R1 is a substituted or unsubstituted aryl group or alkyl group; R2 is a substituted or unsubstituted aryl group or cycloalkyl group; Ar is a substituted or unsubstituted aryl group; X is a nullCH2null, nullOnull, nullSnull or nullCOnull; m is an integer from zero to two; n is an integer from 0-2 when X is nullOnull, nullSnull and 1-2 when X is nullCH2null or nullCOnull. Also disclosed are methods of inhibiting kallikrein activity or urokinase activity in subject in need of such inhibition by administering a compound represented by Structural Formula (I).
摘要翻译：本文公开了由结构式（I）表示的化合物：R 1是取代或未取代的芳基或烷基; R2是取代或未取代的芳基或环烷基; Ar是取代或未取代的芳基; X是-CH 2 - ， - O - ， - S-或-CO-; m是从零到二的整数; 当X是-CH 2 - 或-CO-时，当X是-O - ， - S-和1-2时，n是0-2的整数。还公开了通过施用由结构式（I）表示的化合物来抑制需要这种抑制的受试者的激肽释放酶活性或尿激酶活性的方法。

119. 发明授权

US06696442B2 Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof 失效
标题翻译：碳环和杂环取代的缩氨基脲和缩氨基硫脲和其用途
公开(公告)号：US06696442B2
公开(公告)日：2004-02-24
申请号：US10178477
申请日：2002-06-25
申请人： Yan Wang , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana , Victor I. Ilyin
发明人： Yan Wang , Sui Xiong Cai , Nancy C. Lan , John F. W. Keana , Victor I. Ilyin
IPC分类号： A61K3117
CPC分类号： C07D213/643 , A61K31/17 , A61K31/175 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/505 , C07C281/12 , C07C281/14 , C07C2601/14 , C07D209/14 , C07D211/46 , C07D213/68 , C07D215/12 , C07D307/91 , C07D309/12 , C07D317/50 , C07D317/58 , C07D317/62 , C07D317/64 , C07D319/18
摘要： This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl-82-; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention also is directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.
摘要翻译：本发明涉及由式I表示的碳环和杂环取代的缩氨基脲和缩氨基硫脲或其药学上可接受的盐或前药，其中：Y是氧或硫; R1，R21，R22和R23独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基-82-。或R 22和R 23与N一起形成杂环; A1和A2独立地是芳基，杂芳基，饱和或部分不饱和的碳环或饱和或部分不饱和的杂环，其中任何一个任选被取代; X是1或O，S，NR 24，CR 25 R 26，C（O），NR 24 C（O），C（O）NR 24，SO，SO 2或共价键; 其中R 24，R 25和R 26独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基。本发明还涉及使用碳环和杂环取代的缩氨基脲和缩氨基硫脲来治疗全身和局部缺血后的神经元损伤，用于治疗或预防神经变性疾病如肌萎缩性侧索硬化（ALS），用于治疗和预防涉及谷氨酸毒性和治疗，预防或改善疼痛，作为抗惊厥药，以及作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病和尿失禁的抗疟药抑制剂。

120. 发明授权

US06686350B1 Cell adhesion inhibitors 失效
公开(公告)号：US06686350B1
公开(公告)日：2004-02-03
申请号：US09237273
申请日：1999-01-25
申请人： Zhongli Zheng , Carol L. Ensinger , Steven P. Adams
发明人： Zhongli Zheng , Carol L. Ensinger , Steven P. Adams
IPC分类号： A61K3155
CPC分类号： G01N33/5005 , A61K31/195 , A61K31/44 , C07C233/29 , C07C233/47 , C07C233/63 , C07C235/38 , C07C237/22 , C07C237/42 , C07C275/40 , C07C275/42 , C07C311/06 , C07C311/60 , C07C323/41 , C07C2601/10 , C07C2601/16 , C07C2602/10 , C07D207/09 , C07D207/16 , C07D207/26 , C07D207/27 , C07D209/08 , C07D209/42 , C07D211/26 , C07D211/34 , C07D211/60 , C07D211/70 , C07D213/75 , C07D217/26 , C07D233/68 , C07D233/88 , C07D237/04 , C07D243/12 , C07D243/14 , C07D243/24 , C07D253/06 , C07D271/107 , C07D271/113 , C07D273/00 , C07D277/06 , C07D277/46 , C07D277/56 , C07D295/135 , C07D295/15 , C07D307/68 , C07D317/58 , C07D317/60 , C07D335/10 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D471/04 , C07K5/021 , C07K5/06026 , C07K5/0808 , G01N33/5008 , G01N33/502 , G01N33/5029 , G01N33/68 , G01N2500/00
摘要： The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

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