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21. 发明授权

US07816522B2 Triazolone derivatives 有权
标题翻译：三唑酮衍生物
公开(公告)号：US07816522B2
公开(公告)日：2010-10-19
申请号：US11723893
申请日：2007-03-22
申请人： Richard Clark , Fumiyoshi Matsuura , Kazunobu Kira , Shinsuke Hirota , Hiroshi Azuma , Tadashi Nagakura , Tatsuo Horizoe , Kimiyo Tabata , Kazutomi Kusano , Takao Omae , Atsushi Inoue
发明人： Richard Clark , Fumiyoshi Matsuura , Kazunobu Kira , Shinsuke Hirota , Hiroshi Azuma , Tadashi Nagakura , Tatsuo Horizoe , Kimiyo Tabata , Kazutomi Kusano , Takao Omae , Atsushi Inoue
IPC分类号： A61K31/41 , A61K31/415 , C07D233/00 , C07D249/00
CPC分类号： C07D249/12 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/04 , C07D413/14 , C07D417/04
摘要： A Compound represented by the following general formula (1), salts thereof or hydrates of the foregoing is a novel compound useful for treatment and/or prevention of diseases associated with thrombus formation, and which is safer with suitable physicochemical stability. [wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc.; R2 represents optionally substituted phenyl, etc.; R3 represents optionally substituted C6-10 aryl, etc.; and Z1 and Z2 each independently represent hydrogen]
摘要翻译：由以下通式（1）表示的化合物，其盐或其前体的水合物是可用于治疗和/或预防与血栓形成有关的疾病的新型化合物，其具有合适的理化稳定性更安全。 [其中R1a，R1b，R1c和R1d各自独立地表示氢等; R2代表任选取代的苯基等; R3代表任选取代的C6-10芳基等; 并且Z 1和Z 2各自独立地表示氢]

22. 发明授权

US07812045B2 Antifungal triazole derivatives 有权
标题翻译：抗真菌三唑衍生物
公开(公告)号：US07812045B2
公开(公告)日：2010-10-12
申请号：US11910014
申请日：2006-03-30
申请人： Joon Seok Park , Kyung A Yu , Il Yeong Jeong
发明人： Joon Seok Park , Kyung A Yu , Il Yeong Jeong
IPC分类号： A61K31/41 , C07D233/00 , C07D249/00
CPC分类号： C07D403/06 , C07D401/14 , C07D405/14 , C07D409/14
摘要： Disclosed herein are antifungal triazole derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same.
摘要翻译：本文公开了抗真菌三唑衍生物或其药学上可接受的盐，其制备方法和包含其的药物组合物。

23. 发明申请

US20100113800A1 Formation of Carbon-nitrogen bond 审中-公开
标题翻译：形成碳 - 氮键
公开(公告)号：US20100113800A1
公开(公告)日：2010-05-06
申请号：US11990012
申请日：2006-08-04
申请人： Christelle Mauger , Gerard Mignani , Roland Jacquot
发明人： Christelle Mauger , Gerard Mignani , Roland Jacquot
IPC分类号： C07D233/00
CPC分类号： C07D233/56
摘要： The present invention relates to a process to create a carbon-nitrogen bond by the reaction of an aromatic compound carrying at least one electro attractive group with one nitrogenous heterocyclic type nucleophile compound. The invention aims, in particular, at a link reaction between an aromatic compound carrying at least one electro attractive group and an imidazole heterocycle type. The invention process, consisting of the reaction of an aromatic compound carrying one leaving group and at least one electro attractive group and a nitrogenous heterocyclic type nucleophile compound comprising a N—H pattern likely to substitute the leaving group, thereby creating a carbon-nitrogen bond in the presence of a copper catalyst, of a base in an organic solvent, is characterized by the fact that the said nitrogenous heterocycle reacts with an aromatic type electrophile compound carrying one leaving group (Y) chosen from bromine, chlorine or sulfonic ester and at least one electro attractive group (Z1), in the presence of a copper catalyst, of a mineral or organic base, of an extracting agent selected from aliphatic diamines, aliphatic amino alcohols and diols in a polar aprotic organic solvent with a dielectric constant less than about 20 and a basicity such that its “donor number” is less than about 25.
摘要翻译：本发明涉及通过携带至少一个电吸引基团的芳族化合物与一种含氮杂环型亲核化合物的反应产生碳 - 氮键的方法。本发明特别涉及携带至少一个电吸引基团的芳族化合物和咪唑杂环类型之间的连接反应。本发明方法由携带一个离去基团的芳族化合物和至少一个电吸引基团和含氮杂环型亲核化合物的反应组成，该化合物包含可能代替离去基团的N-H型，从而产生碳 - 氮键在铜催化剂存在下，在有机溶剂中存在碱，其特征在于所述含氮杂环与携带选自溴，氯或磺酸酯的一个离去基团（Y）的芳香族亲电子试剂反应，并且在在铜催化剂存在下，在介电常数小于或等于的极性非质子有机溶剂中的选自脂族二胺，脂族氨基醇和二醇的萃取剂的至少一个电吸引组（Z1）大约20岁，并且其“捐赠人数”小于约25的碱度。

24. 发明授权

US07709514B2 Therapeutic molecules and methods-1 失效
标题翻译：治疗分子及方法1
公开(公告)号：US07709514B2
公开(公告)日：2010-05-04
申请号：US10517264
申请日：2003-06-06
申请人： Eric Francis Morand , Magdy Naguib Iskander , Basil Danylec
发明人： Eric Francis Morand , Magdy Naguib Iskander , Basil Danylec
IPC分类号： A61K31/415 , C07D233/00
CPC分类号： C07D403/12 , A61K31/4184 , A61K31/585 , C07C43/225 , C07C43/23 , C07C45/004 , C07C45/46 , C07C59/58 , C07C65/24 , C07C65/28 , C07C69/94 , C07C205/59 , C07C229/70 , C07C255/37 , C07C309/60 , C07C309/75 , C07C333/04 , C07D235/26 , C07D235/28 , C07D263/58 , C07D307/83 , C07D319/18 , C07H13/10 , Y02A50/401 , Y02A50/411 , C07C47/575 , C07C49/84
摘要： Methods of inhibiting the cytokine or biological activity of Macrophage Migration Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) as defined herein, is provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (I), either alone or as part of a combination therapy. Novel heterocyclic compounds are also provided for.
摘要翻译：提供了抑制巨噬细胞迁移抑制因子（MIF）的细胞因子或生物活性的方法，其包括使MIF与本文定义的式（I）化合物接触。本发明还涉及治疗涉及MIF细胞因子或生物学活性的疾病或病症的方法，包括单独施用或作为组合疗法的一部分施用式（I）化合物。还提供了新的杂环化合物。

25. 发明申请

US20100041573A1 AMINE REACTION COMPOUNDS COMPRISING ONE OR MORE ACTIVE INGREDIENT 审中-公开
标题翻译：包含一种或多种活性成分的胺反应化合物
公开(公告)号：US20100041573A1
公开(公告)日：2010-02-18
申请号：US12603730
申请日：2009-10-22
申请人： Jean-Luc Philippe Bettiol , Alfred Busch , Hugo Denutte , Christophe Laudamiel , Peter Marie Kamiel Perneel , Marie Montserrat Sanchez-Pena , Johan Smets
发明人： Jean-Luc Philippe Bettiol , Alfred Busch , Hugo Denutte , Christophe Laudamiel , Peter Marie Kamiel Perneel , Marie Montserrat Sanchez-Pena , Johan Smets
IPC分类号： C11D3/50 , C07D233/00 , C08G77/38 , C08G73/02 , C07F7/10 , C07D241/04
CPC分类号： C11D3/3742 , C07C251/24 , C11D3/0015 , C11D3/2093 , C11D3/22 , C11D3/30 , C11D3/37 , C11D3/3723 , C11D3/50 , C11D3/507 , C11D17/0039 , C11D17/06
摘要： The present invention relates to a product of reaction between a primary and/or secondary amine and one or more active ingredients. By the present invention, there is provided a release of the active component over a longer period of time than by the use of the active itself.
摘要翻译：本发明涉及伯胺和/或仲胺与一种或多种活性成分之间的反应产物。通过本发明，通过使用活性物质在更长的时间内提供活性成分的释放。

26. 发明申请

US20090274632A1 Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in composition and use thereof 有权
标题翻译：识别在组合物中引起苦味的苦味化合物作用的人类T2R受体的鉴定及其在测定中用于鉴定组合物中抑制（阻断）苦味的化合物及其用途的用途
公开(公告)号：US20090274632A1
公开(公告)日：2009-11-05
申请号：US12222918
申请日：2008-08-19
申请人： Xiaodong Li , Andrew Patron , Catherine Tachdjian , Hong Xu , Qing Li , Alexey Pronin , Guy Servant , Lan Zhang , Thomas Brady , Vincent Darmohusodo , Melissa Arellano , Victor Selchau , Brett Weylan Ching , Donald S. Karanewsky , Paul Brust , Jing Ling , Wen Zhao , Chad Priest
发明人： Xiaodong Li , Andrew Patron , Catherine Tachdjian , Hong Xu , Qing Li , Alexey Pronin , Guy Servant , Lan Zhang , Thomas Brady , Vincent Darmohusodo , Melissa Arellano , Victor Selchau , Brett Weylan Ching , Donald S. Karanewsky , Paul Brust , Jing Ling , Wen Zhao , Chad Priest
IPC分类号： A61K9/68 , G01N33/68 , C12Q1/02 , G01N33/53 , C07D261/06 , C07C65/00 , C07D307/02 , C07D413/02 , A61K31/192 , A61K31/7034 , A61K31/4439 , A61K31/55 , C07K14/435 , C07D241/36 , C07D263/54 , C07D213/62 , C07D223/18 , C07D239/72 , C07D487/02 , C07D413/14 , C07D403/14 , C07D233/00 , C07D249/12 , C07D251/02 , A61K31/4164 , A61K31/4196 , A61K31/53 , A61K31/42 , A61K8/49 , A61P27/00 , A61Q11/00
CPC分类号： C07C311/17 , A23L27/86 , A61K8/46 , A61K8/466 , A61K8/4933 , A61K8/494 , A61K8/4973 , A61K8/498 , A61K8/4986 , A61K31/135 , A61K31/4439 , A61K31/485 , A61K31/60 , A61K31/704 , A61K45/06 , A61Q11/00 , C07C233/73 , C07C311/04 , C07C311/13 , C07C311/16 , C07C311/18 , C07C311/19 , C07C311/20 , C07C311/21 , C07C311/29 , C07C311/46 , C07C323/49 , C07C335/16 , C07C335/18 , C07D213/42 , C07D213/71 , C07D217/08 , C07D223/18 , C07D307/14 , C07D307/52 , C07D317/58 , C07D333/20 , C07D333/34 , A61K2300/00
摘要： The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.
摘要翻译：本发明涉及T2R味觉受体家族中的特定人味受体对存在于例如咖啡中的特定苦味化合物的反应的发现。此外，本发明涉及含有作为苦味抑制剂的特定化合物和组合物的发现，以及其作为例如咖啡和咖啡风味食品，饮料和药物中的苦味抑制剂或风味调节剂的用途。此外，本发明涉及一种拮抗多种不同人类T2R的化合物的发现及其在测定中的用途以及用于摄取人类和动物的组合物中的苦味阻滞剂。

27. 发明授权

US07612064B2 Sulfopyrroles 有权
标题翻译：硫磺吡咯
公开(公告)号：US07612064B2
公开(公告)日：2009-11-03
申请号：US10557664
申请日：2004-05-24
申请人： Martin Eberle , Philipp Ermert , Daniel Obrecht , Frank Lach , Anatol Luther , Felix Bachmann , Allessandro Strebel
发明人： Martin Eberle , Philipp Ermert , Daniel Obrecht , Frank Lach , Anatol Luther , Felix Bachmann , Allessandro Strebel
IPC分类号： C07D233/00 , C07D249/08 , C07D413/00 , A61K31/535 , A01N43/50 , A01N43/64
CPC分类号： C07D401/04 , C07D207/48 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： The invention relates to compounds of formula (I) wherein R1 represents aryl, aralkyl or heteroaryl, R2 is aryl or heteroaryl and R3 is aryl, heteroaryl or optionally substituted aminomethyl, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to the use of a compounds of formula (I) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using compounds of formula (I) or of pharmaceutical compositions containing same.
摘要翻译：本发明涉及式（I）化合物，其中R 1表示芳基，芳烷基或杂芳基，R 2为芳基或杂芳基，R 3为芳基，杂芳基或任选取代的氨基甲基，合成这些化合物的方法为含有式（I）化合物用于制备用于治疗肿瘤和自身免疫性疾病的药物组合物的式（I）化合物的使用，以及使用式（I）或式（I）化合物治疗肿瘤和自身免疫性疾病的方法，含有该组合物的药物组合物。

28. 再颁专利

USRE40795E1 Process for producing 5-substituted oxazole compounds and 5-substituted imidazole compounds 有权
标题翻译：制备5-取代的恶唑化合物和5-取代的咪唑化合物的方法
公开(公告)号：USRE40795E1
公开(公告)日：2009-06-23
申请号：US11825114
申请日：2002-03-20
申请人： Atsushi Ogihara , Hiroshi Sakai , Nobuo Matsui , Hidekazu Miyazaki
发明人： Atsushi Ogihara , Hiroshi Sakai , Nobuo Matsui , Hidekazu Miyazaki
IPC分类号： C07D263/02 , C07D233/00 , C07D263/30
CPC分类号： C07D233/64 , C07D263/32
摘要： A process for producing heterocyclic compounds which are useful as pesticides, drugs, fungicidal materials or intermediates thereof. TosMIC is reacted with an aldehyde or an imino compound: 1) in a solvent mixture of an aprotic solvent with a protic solvent in the presence of a base, 2) in the presence of a phase-transfer catalyst and an inorganic base, or 3) in the presence of an inorganic base. Thus, a desired product can be efficiently obtained using a solution without isolating TosMIC which is irritating and unstable, has a low decomposition point and shows explosivity.
摘要翻译：可用作杀虫剂，药物，杀真菌物质或其中间体的杂环化合物的制备方法。或者在相转移催化剂和无机碱的存在下，将TosMIC与醛或亚氨基化合物反应：1）在非质子溶剂与质子溶剂的溶剂混合物中，在碱的存在下，）在无机碱的存在下进行。因此，可以使用不分离有刺激性和不稳定性的TosMIC的溶液，具有低分解点并显示爆炸性的方式，有效地获得所需产物。

29. 发明授权

US07544807B2 Ionic liquids 有权
标题翻译：离子液体
公开(公告)号：US07544807B2
公开(公告)日：2009-06-09
申请号：US11833529
申请日：2007-08-03
申请人： Peter Wasserscheid , Andreas Bösmann , Roy Van Hal
发明人： Peter Wasserscheid , Andreas Bösmann , Roy Van Hal
IPC分类号： C07D401/04 , C07D213/26 , C07D233/00 , C07F9/02 , C07D229/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： Low melting ionic compounds of the general formula (cation) (R′SO4) in which R′ is a branched or linear, saturated or unsaturated, aliphatic or alicyclic functionalized or non-functionalized hydrocarbon chain with 3-36 carbon atoms are provided. These compounds can serve as ionic liquids, e.g. as solvents or solvent additives in chemical reactions, as extraction agents or as heat carriers. The compounds comprise a cation and anionic sulfate ester.
摘要翻译：提供通式（阳离子）（R'SO 4）的低熔点离子化合物，其中R'是具有3-36个碳原子的支链或直链，饱和或不饱和的脂族或脂环族官能化或非官能化烃链。这些化合物可以作为离子液体，例如作为化学反应中的溶剂或溶剂添加剂，作为萃取剂或作为热载体。该化合物包括阳离子和阴离子硫酸酯。

30. 发明授权

US07531560B2 Anti-cytokine heterocyclic compounds 有权
标题翻译：抗细胞因子杂环化合物
公开(公告)号：US07531560B2
公开(公告)日：2009-05-12
申请号：US11270207
申请日：2005-11-09
申请人： Derek Cogan , Matthew Russell Netherton
发明人： Derek Cogan , Matthew Russell Netherton
IPC分类号： A61K31/41 , A61K31/415 , C07D233/00 , C07D249/04
CPC分类号： C07D403/14 , C07D401/04 , C07D401/14 , C07D403/04
摘要： Disclosed are compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
摘要翻译：公开了抑制参与炎症过程的细胞因子产生的式（I）化合物，因此可用于治疗涉及炎症的疾病和病理状况，例如慢性炎性疾病。还公开了制备这些化合物的方法和包含这些化合物的药物组合物。

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