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81. 发明授权

US07799805B2 Piperidine carboxylic acid amide derivatives 失效
标题翻译：哌啶羧酸酰胺衍生物
公开(公告)号：US07799805B2
公开(公告)日：2010-09-21
申请号：US11915594
申请日：2006-05-23
申请人： Olivier Bezencon , Christoph Boss , Daniel Bur , Austin Chih-Yu Chen , Olivier Corminboeuf , Daniel Dube , Walter Fischli , Corinna Grisostomi , Lubos Remen , Sylvia Richard-Bildstein , Thierry Sifferlen , Michel Therien , Thomas Weller
发明人： Olivier Bezencon , Christoph Boss , Daniel Bur , Austin Chih-Yu Chen , Olivier Corminboeuf , Daniel Dube , Walter Fischli , Corinna Grisostomi , Lubos Remen , Sylvia Richard-Bildstein , Thierry Sifferlen , Michel Therien , Thomas Weller
IPC分类号： A01N43/40 , A61K31/445 , C07D211/68 , C07D211/80 , C07D213/02
CPC分类号： C07D471/08 , C07D211/78 , C07D401/10 , C07D401/12
摘要： The invention relates to novel piperidine carboxylic acid amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of these novel compounds, pharmaceutical compositions comprising such compounds and especially the use of such compounds as inhibitors of renin.
摘要翻译：本发明涉及新型的哌啶羧酸酰胺衍生物及其在制备药物组合物中作为活性成分的用途。本发明还涉及包括制备这些新化合物的方法，包含这些化合物的药物组合物，特别是使用这些化合物作为肾素抑制剂的相关方面。

82. 发明授权

US07662966B2 Benzoimidazole compounds 有权
公开(公告)号：US07662966B2
公开(公告)日：2010-02-16
申请号：US12229892
申请日：2008-08-26
申请人： James P. Edwards , Michael D. Hack , David E. Kindrachuk , Jennifer D. Venable
发明人： James P. Edwards , Michael D. Hack , David E. Kindrachuk , Jennifer D. Venable
IPC分类号： C07D211/68 , C07D211/80 , C07D213/02
CPC分类号： C07D235/18 , C04B35/632 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07K16/00 , C07K2317/50 , C07K2317/53 , C07K2318/10
摘要： Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.

83. 发明授权

US07612103B2 Pleuromutilin derivatives as antimicrobials 有权
标题翻译： Pleuromutilin衍生物作为抗微生物剂
公开(公告)号：US07612103B2
公开(公告)日：2009-11-03
申请号：US10521926
申请日：2003-07-23
申请人： Heinz Berner , Gabriele Kerber
发明人： Heinz Berner , Gabriele Kerber
IPC分类号： A61K35/31 , A31K35/27 , C07D211/80
CPC分类号： A61K31/445 , A61K31/45 , C07D207/12 , C07D211/20 , C07D211/54 , C07D211/56 , C07D211/58 , C07D211/60 , C07D211/72 , C07D223/06 , C07D493/04
摘要： Compounds of formula wherein R1 and R1′ are hydrogen or deuterium, R2, R3 and R4 are hydrogen or deuterium, R5 is the residue of an amino acid, X is S or N-ALK, is piperidinyl or tetrahydropyridinyl, ALK is (C1-4)alkyl, and R6 is hydrogen, hydroxy or (C2-12)acyloxy, and their use as antimicrobials.
摘要翻译：式中R 1和R 1'是氢或氘，R 2，R 3和R 4是氢或氘的化合物，R 5是氨基酸的残基，X是S或N-ALK，是哌啶基或四氢吡啶基，ALK是（C1- 4）烷基，R6是氢，羟基或（C2-12）酰氧基，它们作为抗微生物剂的用途。

84. 发明申请

US20090093479A1 ANTI-CANCER AGENTS AND USES THEREOF 审中-公开
标题翻译：抗癌药剂及其用途
公开(公告)号：US20090093479A1
公开(公告)日：2009-04-09
申请号：US12336857
申请日：2008-12-17
申请人： Martha KELLY , Younghee LEE , Bin LIU , Ted FUJIMOTO , Joel FREUNDLICH , Bruce D. DORSEY , Gary A. FLYNN , Arifa HUSAIN
发明人： Martha KELLY , Younghee LEE , Bin LIU , Ted FUJIMOTO , Joel FREUNDLICH , Bruce D. DORSEY , Gary A. FLYNN , Arifa HUSAIN
IPC分类号： A61K31/5377 , C07D401/02 , C07D211/80 , C07D409/02 , C07D401/14 , C07D405/02 , A61K31/497 , A61K31/506 , A61P35/00 , A61K31/422 , A61K31/4709 , A61K31/4439 , A61K31/4436 , A61K31/443 , A61K31/44 , C07D413/02
CPC分类号： C07D209/08 , C07D213/74 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/10 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/10
摘要： The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, non-small cell lung and colon.
摘要翻译：本发明涉及新型化合物及其盐，其合成及其作为抗癌剂的用途。化合物包括式I化合物及其溶剂合物，水合物及其药学上可接受的盐，其中A1为N或CR1; A3是N或CR3; A5为N或CR5; R1，R3-R6和L在说明书中定义; n为0或1; 并且X是在环部分中具有6-10个碳的任选取代的芳基，在环部分中具有1-3个氮原子的任选取代的6元杂芳基，任选取代的5元杂芳基具有0 -4个氮原子，并且在环部分中任选具有1个硫原子或1个氧原子，或任选取代的杂芳基，其中6元环稠合到5元环或6元环其中在每种情况下，1,2,3或4个环原子是独立地选自氮，氧和硫的杂原子。它们对广泛的癌症尤其是白血病，非小细胞肺和结肠有效。

85. 发明授权

US07501418B2 Fused heterocyclic isoxazoline derivatives and their use as anti-depressants 有权
标题翻译：稠合杂环异恶唑啉衍生物及其作为抗抑郁剂的用途
公开(公告)号：US07501418B2
公开(公告)日：2009-03-10
申请号：US10524123
申请日：2003-08-13
申请人： José Ignacio Andrés-Gil , Manuel Jesús Alcázar-Vaca , José Manuel Bartolomé -Nebreda , Francisco Javier Fernández-Gadea , Margaretha Henrica Maria Bakker , Antonius Adrianus Hendrikus Megens
发明人： José Ignacio Andrés-Gil , Manuel Jesús Alcázar-Vaca , José Manuel Bartolomé -Nebreda , Francisco Javier Fernández-Gadea , Margaretha Henrica Maria Bakker , Antonius Adrianus Hendrikus Megens
IPC分类号： A01N43/54 , A01N43/40 , A61K31/445 , A61K31/497 , C07D211/32 , C07D211/68 , C07D211/80 , C07D213/02 , C07D261/20 , C07D239/00 , C07D237/26 , C07D237/36 , C07D413/00 , C07D417/00 , C07D419/00 , C07D471/00 , C07D487/00 , C07D491/00 , C07D495/00 , C07D497/00
CPC分类号： C07D498/14
摘要： The invention concerns fused heterocyclic isoxazoline derivatives of Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof, more in particular, tetrahydropyranoisoxazole, hexahydroisoxazolopyridine, tetrahydrothiopyrano isoxazole and hexahydrobenzoisoxazole derivatives fused to a heterocyclic ring system via the 6-membered ring of the bicyclic moiety as well as processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for treating depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia, wherein the variables are defined as in Claim 1. The compounds have surprisingly been shown to have selective serotonine (5-HT) reuptake inhibitor activity as well as α2-adrenoceptor antagonist activity, compounds according to the invention are also suitable for treatment and/or prophylaxis in diseases where either one of the activities alone or the combination of said activities may be of therapeutic use.
摘要翻译：本发明涉及式（I）的稠合杂环异恶唑啉衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构体形式及其N-氧化物形式，更特别是四氢吡喃异恶唑，六氢异恶唑并吡啶，四氢噻喃异恶唑和六氢苯并异恶唑衍生物通过双环部分的6元环以及其制备方法，包含它们的药物组合物及其作为药物的用途，特别是用于治疗抑郁症，焦虑症，运动障碍，精神病，帕金森病和包括神经性厌食症和贪食症的体重紊乱，其中变量如权利要求1中所定义。化合物惊奇地显示具有选择性5-羟色胺（5-HT）再摄取抑制剂活性以及α2-肾上腺素受体拮抗剂活性，根据发明也适用于f 或治疗和/或预防疾病，其中单独的一种活性或所述活性的组合可能具有治疗用途。

86. 发明授权

US07345064B2 TNF-α production inhibitors 失效
标题翻译： TNF-α产生抑制剂
公开(公告)号：US07345064B2
公开(公告)日：2008-03-18
申请号：US11472603
申请日：2006-06-22
申请人： Masakazu Ban , Hiroshi Suhara , Masato Horiuchi , Noriyoshi Yamamoto , Hiroshi Enomoto , Hiroyuki Inoue
发明人： Masakazu Ban , Hiroshi Suhara , Masato Horiuchi , Noriyoshi Yamamoto , Hiroshi Enomoto , Hiroyuki Inoue
IPC分类号： C07D211/80 , A61K31/44
CPC分类号： C07D213/56 , C07D213/30 , C07D213/32 , C07D213/38 , C07D213/40 , C07D213/68 , C07D213/75 , C07D401/06
摘要： A purpose of the present invention is to provide TNF-α production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. Novel compounds having the structure represented by the general formula [1] or salts thereof according to the present invention have excellent TNF-α production inhibitory activities, wherein A is —(NR4)—, —(CR5R6)— or —O—, B is alkylene or alkenylene, R1, R2, R4, R5 and R6 are hydrogen, alkyl, alkenyl, adamantyl or the like, R3 is aryl or an unsaturated heterocycle, and X is oxygen or sulfer respectively.
摘要翻译：本发明的目的是提供TNF-α产生抑制剂，其可用作自身免疫疾病如类风湿性关节炎的治疗剂。具有本发明通式[1]所示结构或其盐的新化合物具有优异的TNF-α产生抑制活性，其中A是 - （NR 4） - ， - （CR 或-O - ，B是亚烷基或亚烯基，R 1，R 2，R 2， R 4，R 5和R 6是氢，烷基，链烯基，金刚烷基等，R 3，是芳基或不饱和杂环，X分别是氧或硫。

87. 发明申请

US20070276143A1 Method for producing optically active compound 失效
标题翻译：光学活性化合物的制造方法
公开(公告)号：US20070276143A1
公开(公告)日：2007-11-29
申请号：US11812052
申请日：2007-06-14
申请人： Toru Yamano , Naohiro Taya , Akio Ojida
发明人： Toru Yamano , Naohiro Taya , Akio Ojida
IPC分类号： C07D233/54 , C07D211/80
CPC分类号： C07D233/64 , C07D213/55
摘要： The present invention provides a method for producing an optically active β-hydroxy ester compound represented by the general formula: wherein R1 represents an optionally substituted hydrocarbon group and the like, R2 represents a nitrogen-containing heterocyclic group different from R1, which is represented by the general formula: wherein the ring may be substituted and the like, R3 represents an optionally substituted hydrocarbon group and the like, R4 and R5 represent, the same or different, a hydrogen atom, a halogen atom and the like, the symbol “*” represents an optically active center, which comprises reacting in the presence of a cinchona alkaloid and the like a compound represented by the general formula: wherein R1 and R2are as defined above with a compound represented by the general formula: wherein R3, R4and R5 are as defined above, and X is a halogen atom.
摘要翻译：本发明提供一种制备由以下通式表示的光学活性β-羟基酯化合物的方法：其中R 1表示任选取代的烃基等，R 2 O >表示不同于R 1的含氮杂环基，其由以下通式表示：其中该环可以被取代等，R 3表示任选地取代烃基等，R 4和R 5表示相同或不同的氢原子，卤素原子等，符号“*”表示光学活性中心，其包括在cinchona生物碱等存在下反应，由通式表示的化合物：其中R 1和R 2如上定义与由下列通式表示的化合物：其中R 3，R 4和R 5如上定义，X是卤素原子。

88. 发明授权

US07138525B2 N-substituted-2-oxodihydropyridine derivatives 失效
标题翻译： N-取代-2-氧代二氢吡啶衍生物
公开(公告)号：US07138525B2
公开(公告)日：2006-11-21
申请号：US10899162
申请日：2004-07-27
申请人： Nagaaki Sato , Makoto Ando , Shiho Ishikawa , Tsuyoshi Nagase , Keita Nagai , Akio Kanatani
发明人： Nagaaki Sato , Makoto Ando , Shiho Ishikawa , Tsuyoshi Nagase , Keita Nagai , Akio Kanatani
IPC分类号： C07D211/80
CPC分类号： C07D213/80 , C07D401/04 , C07D401/14
摘要： A compound of the formula (I): (wherein Ar1 and Ar2 are independently aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of cyano, halogen, nitro, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl, lower alkenyl, lower alkylamino, di-lower alkylamino, lower alkanoylamino, lower alkylsulfonylamino, arylsulfonylamino, hydroxy, lower alkoxy, halo-lower alkoxy, aryloxy, heteroaryloxy, lower alkylthio, carboxyl, formyl, lower alkanoyl, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, di-lower alkylcarbamoyl, lower alkylsulfonyl, arylsulfonyl, aryl and heteroaryl; R1 and R2 are independently lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl or lower alkoxy, any of which is optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl; R3, R4 and R5 are independently hydrogen, cyano, halogen or hydroxy, or lower alkyl, lower alkoxy or lower alkylthio, the last three groups being optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl), or a salt or ester thereof is useful as a neuropeptide Y receptor antagonist agent and is also useful as an agent for the treatment of bulimia, obesity or diabetes.
摘要翻译：式（I）的化合物：其中Ar 1和Ar 2独立地为芳基或杂芳基，其中任何一个任选被选自以下的取代基取代：氰基，卤素，硝基，低级烷基，卤代低级烷基，羟基 - 低级烷基，环 - 低级烷基，环（低级烷基） - 低级烷基，低级烯基，低级烷基氨基，二低级烷基氨基，低级烷酰基氨基，低级烷基磺酰基氨基，芳基磺酰基氨基，羟基，低级烷氧基，卤代低级烷氧基，芳氧基，杂芳氧基，低级烷硫基，羧基，甲酰基，低级烷酰基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，二低级烷基氨基甲酰基，低级烷基磺酰基，芳基磺酰基，芳基和杂芳基; R R 1和R 2独立地是低级烷基，环 - 低级烷基，环（低级烷基） - 低级烷基或低级烷氧基，其中任何一个任选被选定的取代基取代由卤素，低级烷基氨基，二低级烷基氨基，低级烷酰氨基，低级烷基氨基，低级烷氧基，甲酰基，低级烷氧基羰基，低级烷基氨基甲酰基和二低级烷基氨基甲酰基; R 3，R 4和R 5独立地是氢，氰基，卤素或羟基，或低级烷基，低级烷氧基或低级烷硫基，最后三个基团任选被选自卤素，低级烷基氨基，二低级烷基氨基，低级烷酰基氨基，羟基，低级烷氧基，甲酰基，低级烷氧基羰基，低级烷基氨基甲酰基和二低级烷基氨基甲酰基的取代基取代）或盐或其酯可用作神经肽Y受体拮抗剂，并且也可用作治疗贪食症，肥胖症或糖尿病的药剂。

89. 发明申请

US20060241155A1 TNF-alpha production inhibitors 失效
标题翻译： TNF-α产生抑制剂
公开(公告)号：US20060241155A1
公开(公告)日：2006-10-26
申请号：US11472603
申请日：2006-06-22
申请人： Masakazu Ban , Hiroshi Suhara , Masato Horiuchi , Noriyoshi Yamamoto , Hiroshi Enomoto , Hiroyuki Inoue
发明人： Masakazu Ban , Hiroshi Suhara , Masato Horiuchi , Noriyoshi Yamamoto , Hiroshi Enomoto , Hiroyuki Inoue
IPC分类号： A61K31/44 , C07D211/80
CPC分类号： C07D213/56 , C07D213/30 , C07D213/32 , C07D213/38 , C07D213/40 , C07D213/68 , C07D213/75 , C07D401/06
摘要： A purpose of the present invention is to provide TNF-α production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. Novel compounds having the structure represented by the general formula [1] or salts thereof according to the present invention have excellent TNF-α production inhibitory activities, wherein A is —(NR4)—, —(CR5R6)— or —O—, B is alkylene or alkenylene, R1, R2, R4, R5 and R6 are hydrogen, alkyl, alkenyl, adamantyl or the like, R3 is aryl or an unsaturated heterocycle, and X is oxygen or sulfer respectively.
摘要翻译：本发明的目的是提供TNF-α产生抑制剂，其可用作自身免疫疾病如类风湿性关节炎的治疗剂。具有本发明通式[1]所示结构或其盐的新化合物具有优异的TNF-α产生抑制活性，其中A是 - （NR 4） - ， - （CR 或-O - ，B是亚烷基或亚烯基，R 1，R 2，R 2， R 4，R 5和R 6是氢，烷基，链烯基，金刚烷基等，R 3，是芳基或不饱和杂环，X分别是氧或硫。

90. 发明申请

US20050014795A1 Aralkyl-tetrahydro-pyridines, their preparation and pharmaceutical compositions containing same 失效
标题翻译：芳烷基 - 四氢 - 吡啶，其制备方法和含有它们的药物组合物
公开(公告)号：US20050014795A1
公开(公告)日：2005-01-20
申请号：US10492770
申请日：2002-10-14
申请人： Marco Baroni , Bernard Bourrie , Rosanna Cardamone , Pierre Casellas
发明人： Marco Baroni , Bernard Bourrie , Rosanna Cardamone , Pierre Casellas
IPC分类号： A61K20060101 , A61K31/4409 , A61K31/4418 , A61K31/444 , A61P20060101 , A61P1/04 , A61P1/10 , A61P9/10 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/06 , A61P19/08 , A61P25/00 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/02 , A61P31/04 , A61P31/06 , A61P31/08 , A61P35/00 , A61P37/00 , A61P37/06 , A61P37/08 , C07C57/50 , C07D20060101 , C07D211/70 , C07D211/72 , C07D211/80 , C07D401/04 , C07
CPC分类号： C07D401/04 , C07D211/70
摘要： The present invention relates to compounds of formula (I): in which X represents N or CH; R1 represents a hydrogen or halogen atom or a CF3 group; n is an integer from 1 to 5; A represents a partially saturated carbonaceous bi- or tricycle; it also relates to their salts, solvates, N-oxides, the pharmaceutical compositions containing them, a method for their preparation and synthesis intermediates in this method.
摘要翻译：本发明涉及式（I）化合物：其中X表示N或CH; R1表示氢或卤素原子或CF3基团; n为1〜5的整数; A表示部分饱和的碳质二元或三轮车; 它还涉及它们的盐，溶剂合物，N-氧化物，含有它们的药物组合物，其制备方法和该方法中的合成中间体。

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