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91. 发明申请

US20090186920A1 SULFONAMIDES AS OREXIN ANTAGONISTS 有权
标题翻译： SULFONAMIDES作为OREXIN拮抗剂
公开(公告)号：US20090186920A1
公开(公告)日：2009-07-23
申请号：US12353506
申请日：2009-01-14
申请人： HENNER KNUST , MATTHIAS NETTEKOVEN , EMMANUEL PINARD , OLIVIER ROCHE , MARK ROGERS-EVANS
发明人： HENNER KNUST , MATTHIAS NETTEKOVEN , EMMANUEL PINARD , OLIVIER ROCHE , MARK ROGERS-EVANS
IPC分类号： A61K31/451 , C07D295/192 , C07D211/30 , A61K31/40
CPC分类号： C07D207/06 , C07D207/08 , C07D211/16
摘要： The present invention is concerned with novel sulfonamides of formula wherein R1, R2, R3 and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.
摘要翻译：本发明涉及新型的具有下式的磺酰胺，其中R1，R2，R3和n如说明书和权利要求中所述。这些化合物是食欲素受体拮抗剂，可用于治疗食欲素途径参与的病症。

92. 发明授权

US07557215B2 Anthraquinone compounds as anti cancer compounds 失效
标题翻译：蒽醌化合物作为抗癌化合物
公开(公告)号：US07557215B2
公开(公告)日：2009-07-07
申请号：US10596783
申请日：2004-12-22
申请人： Laurence Hylton Patterson , Klaus Pors , Paul Henry Teesdale-Spittle
发明人： Laurence Hylton Patterson , Klaus Pors , Paul Henry Teesdale-Spittle
IPC分类号： C07D211/00 , C07D207/04
CPC分类号： C07D207/08 , C07D207/06 , C07D207/10 , C07D207/12 , C07D207/46 , C07D211/18 , C07D211/22 , C07D211/38 , C07D211/46 , C07D211/94
摘要： Anthraquinone compounds of the general formula (I) or a salt thereof (Formula I) in which R1 to R4 are each selected from the group consisting of H, C1-4 alkyl, X1, —NHR0N (R5)2 in which R0 is a C1-12 alkanediyl and each R5 is H or optionally substituted C1-4 alkyl, and a group of formula (II) in which at least one of R6, R7 and R8 is selected from X2, and X2 substituted C1-4 alkyl and any others are H or C1-4 alkyl; R9 is selected from H, C1-4 alkyl, X2 and X2 substituted C1-4 alkyl; m is 0 or 1; n is 1 or 2; X1 is a halogen atom, a hydroxyl group, a C1-6 alkoxyl group, an aryloxy group or an acyloxy group; and X2 is a halogen atom, a hydroxyl group, a C1-6 alkoxyl group, an aryloxy group or an acyloxy group; provided that at least one of R1 to R4 is a group of formula (II). The N-oxides are useful prodrugs which are selectively bioreduced in hypoxic tumours to the corresponding cyclic amine derivatives. The amine compounds are cytotoxic and may be used as alkylating agents having topoisomerase II inhibiting activities in cancer therapy.
摘要翻译：通式（I）的蒽醌化合物或其盐（式I）其中R 1至R 4各自选自H，C 1-4烷基，X 1，-NHRO N（R 5）2，其中R 0为 C 1-12烷二基，每个R 5为H或任选取代的C 1-4烷基，以及其中R 6，R 7和R 8中的至少一个选自X 2，以及X 2取代的C 1-4烷基和任何其余为H或C 1-4烷基; R 9选自H，C 1-4烷基，X 2和X 2取代的C 1-4烷基; m为0或1; n为1或2; X1是卤素原子，羟基，C1-6烷氧基，芳氧基或酰氧基; X2是卤素原子，羟基，C1-6烷氧基，芳氧基或酰氧基; 条件是R 1至R 4中的至少一个为式（II）的基团。 N-氧化物是有用的前药，其在缺氧肿瘤中选择性地生物还原成相应的环胺衍生物。胺化合物是细胞毒性的，并且可以用作在癌症治疗中具有拓扑异构酶II抑制活性的烷化剂。

93. 发明授权

US07553964B2 Cyclobutyl amine derivatives 有权
标题翻译：环丁基胺衍生物
公开(公告)号：US07553964B2
公开(公告)日：2009-06-30
申请号：US11444825
申请日：2006-06-01
申请人： Huaqing Liu , Kathryn J. Hancock, legal representative , Marlon D. Cowart
发明人： Arthur A. Hancock
IPC分类号： C07D237/08 , C07D213/02 , C07D291/04 , C07D291/06 , C07D291/08 , C07D285/06 , C07D285/08 , C07D285/10 , C07D285/12 , C07D285/22 , C07D285/20 , C07D277/22
CPC分类号： C07D207/06 , C07D401/10 , C07D403/10 , C07D417/10
摘要： Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
摘要翻译：式（I）化合物可用于治疗由组胺-3受体配体预防或改善的病症或病症。还公开了包含组胺-3受体配体的药物组合物，使用这些化合物和组合物的方法，以及制备式（I）范围内的化合物的方法。

94. 发明申请

US20090163482A1 TETRALINES ANTAGONISTS OF THE H-3 RECEPTOR 审中-公开
标题翻译： H-3受体的四分之一拮抗剂
公开(公告)号：US20090163482A1
公开(公告)日：2009-06-25
申请号：US12282545
申请日：2007-03-01
申请人： Stanton Furst McHardy , Vinod Dipak Parikh
发明人： Stanton Furst McHardy , Vinod Dipak Parikh
IPC分类号： A61K31/541 , C07D295/14 , A61K31/40 , C07D417/12 , A61P11/00
CPC分类号： C07D207/06 , C07D401/08 , C07D401/10 , C07D403/10 , C07D405/10 , C07D409/10 , C07D413/10
摘要： This invention is directed to a compound of formula (I), as defined herein, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing a compound of formula (I) a process of en preparation of a compound of formula (I), a method of treatment of a disorder or condition that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula (I) as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), psychotic disorders, cognitive disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-intestinal tract, the method comprising administering to a mammal in need of such treatment a compound of formula (I) as described above.
摘要翻译：本发明涉及如本文所定义的式（I）化合物或其药学上可接受的盐，含有式（I）化合物的药物组合物，其制备式（I）化合物的方法，治疗可以通过拮抗组胺H3受体治疗的病症或病症的方法，所述方法包括向需要这种治疗的哺乳动物施用如上所述的式（I）化合物，以及治疗病症或选自抑郁症，情绪障碍，精神分裂症，焦虑症，阿尔茨海默病，注意缺陷多动障碍（ADHD），精神障碍，认知障碍，睡眠障碍，肥胖，头晕，癫痫，运动病，呼吸系统疾病，过敏，过敏引起的气道反应，过敏性鼻炎，鼻充血，过敏性充血，充血，低血压，心血管疾病，GI trac疾病 t，超低运动性和胃肠道的酸性分泌，所述方法包括向需要这种治疗的哺乳动物施用如上所述的式（I）化合物。

95. 发明申请

US20090054630A1 Compositions and methods for detecting and treating diseases and conditions related to chemokine receptors 有权
标题翻译：用于检测和治疗与趋化因子受体相关的疾病和病症的组合物和方法
公开(公告)号：US20090054630A1
公开(公告)日：2009-02-26
申请号：US11820743
申请日：2007-06-19
申请人： Jennifer M. Burns , Bretton Summers , Maureen C. Howard , Thomas J. Schall
发明人： Jennifer M. Burns , Bretton Summers , Maureen C. Howard , Thomas J. Schall
IPC分类号： C07K16/44
CPC分类号： G01N33/6863 , C07D207/06 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/14 , C07D211/26 , C07D211/42 , C07D211/56 , C07D241/04 , C07D241/42 , C07D295/13 , C07D401/04 , C07D401/06 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , G01N2500/10
摘要： Antibodies that bind CCX-CKR2 are described.
摘要翻译：描述了结合CCX-CKR2的抗体。

96. 发明申请

US20090054448A1 Amino Acid Derivatives as Histone Deacetylase (HDAC) Inhibitors 审中-公开
标题翻译：氨基酸衍生物作为组蛋白脱乙酰酶（HDAC）抑制剂
公开(公告)号：US20090054448A1
公开(公告)日：2009-02-26
申请号：US11991579
申请日：2006-09-05
申请人： Philip Jones
发明人： Philip Jones
IPC分类号： A61K31/16 , C07D209/18 , C07D263/58 , C07D213/75 , C07D277/28 , C07D333/22 , C07D233/26 , C07D401/02 , C07D417/02 , A61K31/495 , A61K31/4709 , A61K31/47 , A61K31/427 , A61K31/426 , A61K31/381 , A61K31/423 , A61P25/18 , A61P25/28 , A61P9/10 , A61K31/27
CPC分类号： C07D263/58 , C07C323/60 , C07C2601/08 , C07D207/06 , C07D209/18 , C07D211/58 , C07D211/62 , C07D213/75 , C07D213/82 , C07D215/12 , C07D231/14 , C07D233/90 , C07D241/44 , C07D257/04 , C07D277/28 , C07D295/13 , C07D295/15 , C07D307/52 , C07D333/28 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts or stereoisomers thereof. The compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或立体异构体。本发明化合物是组蛋白脱乙酰酶（HDAC）的抑制剂，可用于治疗包括癌症在内的细胞增殖性疾病。此外，本发明的化合物可用于治疗神经变性疾病，精神分裂症和中风等疾病。

97. 发明授权

US07491724B2 Substituted cyclic hydroxamates as inhibitors of matrix metalloproteinases 有权
标题翻译：取代的环状异羟肟酸盐作为基质金属蛋白酶的抑制剂
公开(公告)号：US07491724B2
公开(公告)日：2009-02-17
申请号：US10965215
申请日：2004-10-15
申请人： Yun-Long Li , Jincong Zhuo , David Burns , Wenqing Yao , Ravi Kumar Jalluri
发明人： Yun-Long Li , Jincong Zhuo , David Burns , Wenqing Yao , Ravi Kumar Jalluri
IPC分类号： A61K31/497 , C07D403/00
CPC分类号： C07D401/14 , C07D207/06 , C07D207/08 , C07D211/16 , C07D211/32 , C07D211/60 , C07D213/50 , C07D241/04 , C07D295/185 , C07D401/06 , C07D401/08 , C07D401/10 , C07D401/12 , C07D403/08 , C07D403/12 , C07D405/08 , C07D405/12 , C07D405/14 , C07D413/08 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D495/04
摘要： The present invention provides compounds of the formula I: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula I are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.
摘要翻译：本发明提供了式I化合物：其对映异构体，非对映体，外消旋混合物，前体药物，结晶形式，非结晶形式，其无定形形式，其溶剂化物，其代谢物和药学上可接受的盐，其中环A取代基在下面的公开内容中被完全定义。式I化合物是金属蛋白酶如基质金属蛋白酶和脱落酶的抑制剂，可用于治疗诸如类风湿性关节炎，牛皮癣，肿瘤性疾病，过敏症以及所有需要MMP抑制的疾病。

98. 发明申请

US20080275046A1 Compounds Comprising an Oxazole or Thiazole Moiety, Processes for Making Them, and Their Uses 失效
标题翻译：包含恶唑或噻唑的化合物，其制备方法及其用途
公开(公告)号：US20080275046A1
公开(公告)日：2008-11-06
申请号：US11910191
申请日：2006-03-28
申请人： Sylvain Celanire , Frederic Denonne
发明人： Sylvain Celanire , Frederic Denonne
IPC分类号： A61K31/4545 , C07D401/14 , A61P25/28 , C07D413/14 , A61P25/18 , A61P29/00 , A61P3/04 , A61P9/00 , A61P25/16 , A61P25/22 , A61K31/5377 , A61P25/24 , A61K31/454
CPC分类号： C07D263/14 , C07D207/06 , C07D211/14 , C07D263/16 , C07D263/32 , C07D263/36 , C07D263/52 , C07D277/10 , C07D277/24 , C07D277/28 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to compounds comprising an oxazole or thiazole moiety of formula (I), processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as H3-receptor ligands, Formula (I), wherein, A1 is CH, C(alkyl), C-halogen or N; R1 is hydrogen, halogen, C1-6 alkyl or alkoxy; R2 is, Formula (II′), A3 is O or S; R3 is hydrogen, halogen, C1-6 alkyl or alkoxy; R4 is hydrogen, halogen, C1-6 alkyl, alkoxy or —O-L; R5 is hydrogen or —O-L, wherein L is an aminoalkyl group and at least one of R4 and R5 should be —O-L.
摘要翻译：本发明涉及包含式（I）的恶唑或噻唑部分的化合物，其制备方法，包含所述化合物的药物组合物及其作为H 3 - 受体配体的用途，式（I），其中，A 1是CH，C（烷基），C-卤素或N; R 1是氢，卤素，C 1-6烷基或烷氧基; R 2是式（II'），A 3是O或S; R 3是氢，卤素，C 1-6烷基或烷氧基; R 4是氢，卤素，C 1-6烷基，烷氧基或-O-L; R 5是氢或-O-L，其中L是氨基烷基，R 4和R 5中的至少一个应为-O-L。

99. 发明申请

US20080039634A1 NOVEL ONIUM SALT, ELECTROLYTE FOR NONAQUEOUS CELL CONTAINING THE NOVEL ONIUM SALT FOR NONAQUEOUS CELL AND METHOD FOR OPTIMIZING NEGATIVE ELECTRODE USING ELECTROLYTE CONTAINING ONIUM SALT 有权
标题翻译：新型盐酸盐，电解槽用于非水溶液中含有新型盐酸盐的非水溶液，以及使用含有电解质盐的电解液优化负极的方法
公开(公告)号：US20080039634A1
公开(公告)日：2008-02-14
申请号：US11870058
申请日：2007-10-10
申请人： Tomonori Matsunaga , Takeo Kawahara , Hajime Matsumoto
发明人： Tomonori Matsunaga , Takeo Kawahara , Hajime Matsumoto
IPC分类号： C07D233/00
CPC分类号： C07D233/56 , C07C211/63 , C07C233/05 , C07C311/51 , C07D207/06 , C07F9/5407 , C07F9/5442 , C07F9/65688 , H01M4/04 , H01M4/0438 , H01M4/0445 , H01M4/06 , H01M4/13 , H01M6/166 , H01M10/052 , H01M10/0568
摘要： There are provided a novel onium salt and a method for optimizing the interface of a negative electrode by the use of the novel onium salt and /or a conventional onium salt. Such a method is characterized in that an electrolyte comprising novel 2, 2, 2-trifluoro-N-(trifluoromethanesulfonyl) acetamide·tetraethyl ammonium salt is made to intervene between a negative electrode and a positive electrode in an electrochemical device having the constitution: a negative electrode|an electrolyte |a positive electrode, thereby constructing an electrode structure in the electrochemical device, and applying a voltage between the negative electrode and the positive electrode so as for the negative electrode to have a potential of −1 V to −5 V in terms of the potential relative to a reference electrode of I−/I3−, thereby forming a passive-state layer comprising a decomposition product of the above electrolyte or salt on the surface of the above negative electrode.
摘要翻译：提供了一种新的鎓盐和通过使用新的鎓盐和/或常规的鎓盐来优化负极界面的方法。这种方法的特征在于，在具有以下结构的电化学装置中，制备包含新型2,2,2-三氟-N-（三氟甲磺酰基）乙酰胺四乙基铵盐的电解质在负极和正极之间进行介入负极|电解质|正极，由此在电化学装置中构成电极结构，在负极和正极之间施加电压，使负极具有-1V〜-5V的电位在相对于参比电极的电位方面，由此形成包含上述电解质或盐的分解产物的被动状态层，上述负极的表面。

100. 发明申请

US20070299071A1 Substituted phenyl methanone derivatives 有权
标题翻译：取代苯甲酮衍生物
公开(公告)号：US20070299071A1
公开(公告)日：2007-12-27
申请号：US11818676
申请日：2007-06-15
申请人： Synese Jolidon , Robert Narquizian , Roger Norcross , Emmanuel Pinard
发明人： Synese Jolidon , Robert Narquizian , Roger Norcross , Emmanuel Pinard
IPC分类号： A61K31/164 , A61K31/4025 , A61K31/5355 , C07C233/64 , C07D207/04 , C07D413/08
CPC分类号： C07D207/06 , C07D207/08 , C07D211/16 , C07D403/10 , C07D407/10
摘要： The present invention relates to compounds of formula I wherein R1, R2, R3, X, n, and m are as defined herein and to pharmaceutically acceptable acid addition salts thereof, to pharmaceutical compositions containing them, and to methods for treating neurological and neuropsychiatric disorders.
摘要翻译：本发明涉及式I化合物，其中R 1，R 2，R 3，X，n和m如本文所定义及其药学上可接受的酸加成盐，含有它们的药物组合物，以及治疗神经和神经精神障碍的方法。

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