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51. 发明授权

US09090575B2 Phenyl-piperazine derivatives as serotonin reuptake inhibitors 有权
标题翻译：苯基哌嗪衍生物作为血清素再摄取抑制剂
公开(公告)号：US09090575B2
公开(公告)日：2015-07-28
申请号：US13927678
申请日：2013-06-26
申请人： H. Lundbeck A/S
发明人： Thomas Ruhland , Garrick P. Smith , Benny Bang-Andersen , Ask Puschl , Ejner K. Moltzen , Kim Andersen
IPC分类号： C07D295/096 , C07D211/20 , C07D211/70 , C07D243/08
CPC分类号： C07D295/145 , C07D211/20 , C07D211/70 , C07D243/08 , C07D295/033 , C07D295/096
摘要： The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.
摘要翻译：本发明提供由通式I表示的化合物，其中取代基在本申请中定义。这些化合物可用于治疗情感障碍，包括抑郁症，焦虑症，包括一般焦虑症，惊恐障碍和强迫症。

52. 发明申请

US20130237709A1 INTERMEDIATES USEFUL FOR THE SYNTHESIS OF FEXOFENADINE, PROCESSES FOR THEIR PREPARATION AND FOR THE PREPARATION OF FEXOFENADINE 审中-公开
标题翻译：中间体有用于合成FEXOFENADINE，其制备方法和制备FEXOFENADINE
公开(公告)号：US20130237709A1
公开(公告)日：2013-09-12
申请号：US13772832
申请日：2013-02-21
申请人： CHEMELECTIVA S.R.L.
发明人： Graziano CASTALDI , Marco BARATELLA , Mauro GABOARDI
IPC分类号： C07D307/20 , C07D211/22 , C07C67/313
CPC分类号： C07D307/20 , C07C67/31 , C07C67/313 , C07C69/73 , C07D211/20 , C07D211/22 , C07C69/738
摘要： Intermediates useful for the synthesis of fexofenadine, processes for their preparation and processes for the synthesis of fexofenadine are described.
摘要翻译：描述了用于合成非索非那定的中间体，其制备方法和非索非那定的合成方法。

53. 发明申请

US20130190488A1 APOPTOSIS PROMOTERS 有权
标题翻译： APOPTOSIS促销者
公开(公告)号：US20130190488A1
公开(公告)日：2013-07-25
申请号：US13712715
申请日：2012-12-12
申请人： Abbott Laboratories
发明人： Milan Bruncko , Hong Ding , Steven Elmore , Aaron Kunzer , Christopher L. Lynch , William McClellan , Cheol-Min Park , Andrew Petros , Xiaohong Song , Xilu Wang , Noah Tu , Michael Wendt , Alexander Shoemaker , Michael Mitten
IPC分类号： C07D295/155 , C07D233/24 , C07D333/34 , C07D211/70 , C07D213/82 , C07D309/20 , C07D207/09 , C07D487/08 , C07D405/12 , C07D205/04 , C07D491/048 , C07D498/08 , C07D491/08 , C07D209/02 , C07D273/01 , C07D211/38 , C07D265/30 , C07D277/04 , C07D267/10 , C07D211/34 , C07C311/51 , C07D307/14 , C07D239/20
CPC分类号： C07D295/155 , C07C311/51 , C07D205/04 , C07D207/06 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/20 , C07D207/24 , C07D207/50 , C07D209/02 , C07D209/52 , C07D211/14 , C07D211/20 , C07D211/26 , C07D211/34 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/58 , C07D211/62 , C07D211/70 , C07D211/72 , C07D213/36 , C07D213/38 , C07D213/42 , C07D213/70 , C07D213/74 , C07D213/81 , C07D213/82 , C07D215/12 , C07D231/12 , C07D231/56 , C07D233/06 , C07D233/22 , C07D233/24 , C07D233/61 , C07D233/64 , C07D235/08 , C07D239/06 , C07D239/20 , C07D239/38 , C07D241/04 , C07D249/18 , C07D257/04 , C07D261/20 , C07D263/12 , C07D263/22 , C07D263/58 , C07D265/30 , C07D267/10 , C07D273/01 , C07D277/04 , C07D277/36 , C07D277/74 , C07D295/185 , C07D295/30 , C07D307/14 , C07D307/22 , C07D307/81 , C07D309/14 , C07D309/20 , C07D317/66 , C07D333/20 , C07D333/34 , C07D335/02 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/10 , C07D413/04 , C07D451/02 , C07D471/08 , C07D487/04 , C07D487/08 , C07D491/04 , C07D491/048 , C07D491/08 , C07D498/08
摘要： Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
摘要翻译：公开了抑制抗凋亡蛋白家族成员的活性的化合物，含有化合物的组合物和化合物用于制备用于治疗疾病的药物的用途，其中发生表达一种或多种抗凋亡蛋白家族成员。

54. 发明授权

US08153657B2 Dopamine-, norepinephrine- and serotonin-transporter-selective heterocyclic compounds and their therapeutic applications 失效
标题翻译：多巴胺，去甲肾上腺素和5-羟色胺转运体选择性杂环化合物及其治疗应用
公开(公告)号：US08153657B2
公开(公告)日：2012-04-10
申请号：US10576620
申请日：2004-10-22
申请人： Alan P. Kozikowski , Jia Zhou
发明人： Alan P. Kozikowski , Jia Zhou
IPC分类号： A61K31/445 , C07D211/54
CPC分类号： C07D211/20 , C07D211/22 , C07D211/24 , C07D405/12 , C07D413/12
摘要： One aspect of the invention relates to piperidine compounds that are useful as inhibitors of monoamine transporters. The invention also relates to pharmaceutical compositions, comprising a piperidine compound of the invention. Another aspect of the present invention relates to the use of the aforementioned compounds in a method of treating a disorder of the central nervous system in a mammal.
摘要翻译：本发明的一个方面涉及可用作单胺转运蛋白抑制剂的哌啶化合物。本发明还涉及包含本发明的哌啶化合物的药物组合物。本发明的另一方面涉及上述化合物在治疗哺乳动物中的中枢神经系统病症的方法中的用途。

55. 发明授权

US07816375B2 Ligands for monoamine receptors and transporters, and methods of use thereof 有权
标题翻译：单胺受体和转运蛋白的配体及其使用方法
公开(公告)号：US07816375B2
公开(公告)日：2010-10-19
申请号：US12403311
申请日：2009-03-12
申请人： Brian M. Aquila , Thomas D. Bannister , Gregory D. Cuny , James R. Hauske , Joanne M. Holland , Paul E. Persons , Heike Radeke , Fengjiang Wang , Liming Shao
发明人： Brian M. Aquila , Thomas D. Bannister , Gregory D. Cuny , James R. Hauske , Joanne M. Holland , Paul E. Persons , Heike Radeke , Fengjiang Wang , Liming Shao
IPC分类号： A61P25/00 , A61K31/445 , C07D211/00
CPC分类号： C40B40/04 , C07B2200/11 , C07C255/46 , C07C2601/04 , C07D205/02 , C07D207/06 , C07D207/08 , C07D207/09 , C07D211/12 , C07D211/16 , C07D211/18 , C07D211/20 , C07D211/26 , C07D211/32 , C07D211/40 , C07D211/42 , C07D211/60 , C07D233/04 , C07D233/10 , C07D265/30 , C07D267/10 , C07D303/08 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/06 , C40B30/04 , C40B50/14
摘要： One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
摘要翻译：本发明的一个方面涉及杂环化合物。本发明的第二方面涉及杂环化合物作为各种哺乳动物细胞受体（包括多巴胺，5-羟色胺或去甲肾上腺素转运蛋白）的配体的用途。本发明的化合物可用于治疗多种疾病，疾病，其包括但不限于成瘾，焦虑，抑郁，性功能障碍，高血压，偏头痛，阿尔茨海默病，肥胖，呕吐，精神病，精神分裂症，帕金森病，炎症性疼痛，神经性疼痛，Lesche-Nyhane病，Wilson氏病和Tourette综合征。本发明的另一方面涉及杂环化合物的组合文库的合成，以及用于生物活性的那些文库的筛选，例如在基于多巴胺转运蛋白的测定中。

56. 发明申请

US20100137605A1 PROCESS FOR PRODUCTION OF PIPERIDINE DERIVATIVES 失效
标题翻译：生产哌啶衍生物的方法
公开(公告)号：US20100137605A1
公开(公告)日：2010-06-03
申请号：US12686516
申请日：2010-01-13
申请人： Thomas E. D'Ambra , Garry M. Pilling
发明人： Thomas E. D'Ambra , Garry M. Pilling
IPC分类号： C07D211/34
CPC分类号： C07D211/22 , C07D211/14 , C07D211/20 , C07D211/46
摘要： The present invention is directed to a process for preparing the piperidine derivative compound 4-[4-[4-hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylphenylacetic acid of formula comprising the sequential steps of: (1) reacting 4-bromo-α,α-dimethyl-α-(4,4-dimethylisoxazolin-2-yl) toluene with N,N-dimethyl cyclopropylcarboxylic acid amide to provide 4-(cyclopropyl-oxo-methyl)-α,α-dimethyl-α-(4,4-dimethyloxozolin-2-yl) toluene; (2) hydrolyzing said 4-(cyclopropyl-oxo-methyl)-α,α-dimethyl-α-(4,4-dimethyloxozolin-2-yl) toluene to provide 4-(4-chloro-1-oxobutyl)-α,α-dimethylphenylacetic acid; (3) reacting said 4-(4-chloro-1-oxobutyl)-α,α-dimethylphenylacetic acid with methanol to provide methyl 4-(4-chloro-1-oxobutyl)-α,α-dimethylphenylacetate; (4) reacting said methyl 4-(4-chloro-1-oxobutyl)-α,α-dimethylphenylacetate with 4-(α,α-diphenyl)piperidinemethanol to provide methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-oxobutyl]-α,α-dimethylphenylacetate; (5) reducing said methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-oxobutyl]-α,α-dimethylphenylacetate to provide methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylphenylacetate; and (6) hydrolyzing said methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylphenylacetate to provide said 4-[4-[4-hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylphenylacetic acid.
摘要翻译：本发明涉及制备下式的哌啶衍生化合物4- [4- [4-羟基联苯甲基）-1-哌啶基] -1-羟基丁基]-α，α-二甲基苯基乙酸的方法，其包括以下顺序步骤：（ 1）使4-溴-α，α-二甲基-α-（4,4-二甲基异恶唑啉-2-基）甲苯与N，N-二甲基环丙基羧酸酰胺反应，得到4-（环丙基 - 氧代 - 甲基）-α， α-二甲基-α-（4,4-二甲基恶唑啉-2-基）甲苯; （2）水解所述4-（环丙基 - 氧代甲基）-α，α-二甲基-α-（4,4-二甲基恶唑啉-2-基）甲苯，得到4-（4-氯-1-氧代丁基）-α ，α-二甲基苯乙酸; （3）使所述4-（4-氯-1-氧代丁基）-α，α-二甲基苯基乙酸与甲醇反应，得到4-（4-氯-1-氧代丁基）-α，α-二甲基苯基乙酸甲酯; （4）使4-（4-氯-1-氧代丁基）-α，α-二甲基苯基乙酸甲酯与4-（α，α-二苯基）哌啶甲醇反应，得到4- [4- [4-（羟基二苯基甲基）-1 - 哌啶基] -1-氧代丁基]-α，α-二甲基苯基乙酸酯; （5）还原4- [4- [4-（羟基二苯基甲基）-1-哌啶基] -1-氧代丁基]-α，α-二甲基苯基乙酸甲酯，得到4- [4- [4-（羟基二苯基甲基）-1- 哌啶基] -1-羟基丁基]-α，α-二甲基苯基乙酸酯; 和（6）水解所述4- [4- [4-（羟基二苯基甲基）-1-哌啶基] -1-羟基丁基]-α，α-二甲基苯基乙酸甲酯，得到所述4- [4- [4-羟基二苯基甲基）-1- 哌啶基] -1-羟基丁基]-α，α-二甲基苯基乙酸。

57. 发明申请

US20100137366A1 4- [2- (4-METHYLPHENYLSULFANYL) PHENYL] PIPERIDINE FOR THE TREATMENT OF IRRITABLE BOWEL SYNDROME (IBS) 有权
标题翻译： 4- [2-（4-甲基苯基）苯基]哌啶用于治疗可重复的牙龈综合征（IBS）
公开(公告)号：US20100137366A1
公开(公告)日：2010-06-03
申请号：US12600884
申请日：2008-06-13
申请人： Silke Miller
发明人： Silke Miller
IPC分类号： A61K31/4465 , A61P1/00 , C07D211/20
CPC分类号： A61K31/451 , C07D211/20
摘要： The use of 4-[2-(4-methylphenylsulfanyl)phenyl]piperidine or a pharmaceutically acceptable salt thereof in the treatment of irritable bowl syndrome.
摘要翻译： 4- [2-（4-甲基苯基硫烷基）苯基]哌啶或其药学上可接受的盐在治疗肠易激综合征中的用途。

58. 发明授权

US07683053B2 Phenyl-piperazine derivatives as serotonin reuptake inhibitors 有权
标题翻译：苯基哌嗪衍生物作为血清素再摄取抑制剂
公开(公告)号：US07683053B2
公开(公告)日：2010-03-23
申请号：US11551188
申请日：2006-10-19
申请人： Thomas Ruhland , Garrick Paul Smith , Benny Bang-Andersen , Ejner Knud Moltzen , Kim Andersen
发明人： Thomas Ruhland , Garrick Paul Smith , Benny Bang-Andersen , Ejner Knud Moltzen , Kim Andersen
IPC分类号： A61P25/00 , A61K31/55 , C07D243/08
CPC分类号： C07D295/145 , C07D211/20 , C07D211/70 , C07D243/08 , C07D295/033 , C07D295/096
摘要： The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.
摘要翻译：本发明提供由通式I表示的化合物，其中取代基在本申请中定义。这些化合物可用于治疗情感障碍，包括抑郁症，焦虑症，包括一般焦虑症，惊恐障碍和强迫症。

59. 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。

60. 发明授权

US07598271B1 Crystalline paroxetine methane sulfonate 有权
标题翻译：结晶帕罗西汀磺酸甲酯
公开(公告)号：US07598271B1
公开(公告)日：2009-10-06
申请号：US09200743
申请日：1998-11-30
申请人： Franciscus Bernardus Gemma Benneker , Frans Van Dalen , Jacobus Maria Lemmens , Theodorus Hendricus Antonium Peters , Frantisek Picha
发明人： Franciscus Bernardus Gemma Benneker , Frans Van Dalen , Jacobus Maria Lemmens , Theodorus Hendricus Antonium Peters , Frantisek Picha
IPC分类号： A61K31/445 , C07D405/12
CPC分类号： C07D405/12 , C07D211/20
摘要： The invention relates to a compound, and pharmaceutically acceptable salts, having the formula I: wherein: R represents an alkyl or alkynyl group having 1-4 carbon atoms, or a phenyl group optionally substituted by C1-4 alkyl, alkylthio, alkoxy, halogen, nitro, acylamino, methylsulfonyl or methylenedioxy, or represents tetrahydronaphthyl, R1 represents hydrogen, trifluoro (C1-4) alkyl, alkyl or alkynyl, X represents hydrogen, alkyl having 1-4 carbon atoms, alkoxy, trifluoroalkyl, hydroxy, halogen, methylthio or aralkoxy, R2 represents: a C1-C10 alkyl group, a phenyl group optionally substituted by one or more of the following groups: a C1-C10 alkyl group, a halogen group, a nitro group, hydroxy group, and/or an alkoxy group.
摘要翻译：本发明涉及具有式I的化合物和药学上可接受的盐：其中：R表示具有1-4个碳原子的烷基或炔基，或任选被C 1-4烷基，烷硫基，烷氧基，卤素取代的苯基，硝基，酰氨基，甲基磺酰基或亚甲二氧基，或表示四氢萘基，R 1表示氢，三氟（C 1-4）烷基，烷基或炔基，X表示氢，具有1-4个碳原子的烷基，烷氧基，三氟烷基，羟基，或芳烷氧基，R 2表示：C 1 -C 10烷基，任选被一个或多个下列基团取代的苯基：C 1 -C 10烷基，卤素基，硝基，羟基和/或烷氧基组。

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