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71. 发明授权

US07153849B2 Antidepressant arylpiperazine derivatives of hetrocycle-fused benzodioxans 失效
标题翻译：抗坏血酸的芳基哌嗪衍生物
公开(公告)号：US07153849B2
公开(公告)日：2006-12-26
申请号：US10659537
申请日：2003-09-10
申请人： Deborah Ann Evrard , Dahui Zhou , Gary Paul Stack , Aranapakam Madumbai Venkatesan , Amedeo A. Failli , Susan Christman Croce
发明人： Deborah Ann Evrard , Dahui Zhou , Gary Paul Stack , Aranapakam Madumbai Venkatesan , Amedeo A. Failli , Susan Christman Croce
IPC分类号： A61K31/55 , A61K31/497 , C07D401/06 , C07D243/06
CPC分类号： C07D491/04 , Y02P20/582
摘要： Compounds of the formula I: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive-compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.
摘要翻译：式I化合物可用于治疗抑郁症（包括但不限于重度抑郁症，儿童抑郁症和抑郁症），焦虑症，恐慌症，创伤后应激障碍，经前期焦虑症（也称为月经前）综合征），注意缺陷障碍（伴有和不伴有多动症），强迫症，社会焦虑症，广泛性焦虑症，肥胖症，进食障碍如神经性厌食症和神经性贪食症，血管舒缩性潮红，可卡因和酒精成瘾，性功能障碍及相关疾病

72. 发明申请

US20020052498A1 (2-substituted oxyphenyl)alkanamide derivative, hair growth promoter and external composition for skin using the same 失效
标题翻译：（2-取代的氧苯基）烷酰胺衍生物，毛发生长促进剂和使用其的外用皮肤组合物
公开(公告)号：US20020052498A1
公开(公告)日：2002-05-02
申请号：US09984202
申请日：2001-10-29
申请人： Shiseido Co., Ltd.
发明人： Koji Kobayashi , Hirotada Fukunishi , Tokuro Iwabuchi
IPC分类号： C07D241/02 , C07D243/06
CPC分类号： C07D295/185 , A61K8/42 , A61K8/445 , A61K8/4926 , A61K8/494 , A61Q7/00 , C07C235/34 , C07C271/44 , C07C271/52 , C07C271/64 , C07C271/66 , C07C281/02 , C07D295/088 , C07D295/13 , C07D295/205
摘要： A (2-substituted oxyphenyl)alkanamide derivative or a salt thereof expressed by the following Formula (I): 1 wherein one of A and B is a hydrocarbon group of C3-30 expressed by R1 and the other is null(CH2)n-NR2R3; Z is nullCOnull or nullCONR6null; R2 and R3 individually represent H, lower alkyl or benzyl, or nullNR2R3 may be a heterocycle having 3-7 members; wherein nullCONR5null(CH2)nnullNR2R3 or nullCONR6null(CH2)n-NR2R3 may be the following Group (II): 2 wherein ring Y is a heterocycle of 6 or 7 members; R4 is selected from the group consisting of H, halogen, lower alkyl, lower acyl and etc; R5 and R6 are individually H, lower alkyl, lower acyl or lower alkylcarbamoyl, or may form a part of said Group(II); 1 is 0 or 1; m is 1 or 2; and n is an integer of 0-5. The (2-substituted oxyphenyl)alkanamide derivative or the salt thereof has excellent hair growth and regrowth promoting effects, which are useful for care, improvement or prevention of hair loss in mammals and, in particular, in human.
摘要翻译：由下式（I）表示的（2-取代的氧苯基）烷酰胺衍生物或其盐：其中A和B中的一个是由R 3表示的C3-30的烃基，另一个是 - （CH 2）n -NR 2 R 3 ; Z是-CO-或-CONR 6 - ; R2和R3各自表示H，低级烷基或苄基，或-NR2R3可以是具有3-7个成员的杂环; 其中-CONR 5 - （CH 2）n -NR 2 R 3或-CONR 6 - （CH 2）n -NR 2 R 3可以是下列基团（II）：其中环Y是6或7个成员的杂环; R4选自H，卤素，低级烷基，低级酰基等; R5和R6各自为H，低级烷基，低级酰基或低级烷基氨基甲酰基，或可形成所述组（II）的一部分。 1为0或1; m为1或2; n为0-5的整数。（2-取代的氧苯基）烷酰胺衍生物或其盐具有优异的毛发生长和再生长促进作用，其可用于哺乳动物，特别是人的护发，改善或预防脱发。

73. 发明授权

US6011045A Vitronectin receptor antagonists, their preparation and their use 失效
标题翻译： Vitronectin受体拮抗剂，其制备及其应用
公开(公告)号：US6011045A
公开(公告)日：2000-01-04
申请号：US995521
申请日：1997-12-22
申请人： Volkmar Wehner , Hans Ulrich Stilz , Anuschirwan Peyman , Jochen Knolle , Jean-Marie Ruxer , Denis Carniato , Jean-Michel Lefrancois , Thomas Richard Gadek , Robert McDowell
发明人： Volkmar Wehner , Hans Ulrich Stilz , Anuschirwan Peyman , Jochen Knolle , Jean-Marie Ruxer , Denis Carniato , Jean-Michel Lefrancois , Thomas Richard Gadek , Robert McDowell
IPC分类号： C07D239/00 , A61K31/155 , A61K31/16 , A61K31/18 , A61K31/33 , A61K31/395 , A61K31/415 , A61K31/4184 , A61K31/47 , A61K31/472 , A61K31/55 , A61K38/04 , A61P9/00 , A61P19/08 , A61P19/10 , A61P25/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07C279/20 , C07C279/24 , C07C311/64 , C07C313/30 , C07C327/00 , C07D217/24 , C07D233/04 , C07D235/16 , C07D243/06 , C07D253/06 , C07D253/08 , C07D263/52 , C07D267/08 , C07D277/60 , C07D471/02 , C07D471/04 , C07D487/04 , C07K5/04 , G07D217/24
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of the formula IA--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.
摘要翻译：本发明涉及式IA-B-D-E-F-G（I）的化合物，其中A，B，D，E，F和G具有专利权利要求中给出的含义，其制备和用作药物。本发明的化合物用作玻连蛋白受体拮抗剂和骨吸收抑制剂。

74. 发明授权

US5747488A 2-aryl-5,11-dihydro-6H-dipyrido�3,2-B:2',3'-E!�1, 4!diazepines and their use in the treatment of HIV infection 失效
标题翻译： 2-芳基-5,11-二氢-6H-二吡啶并[3,2-B：2'，3'-E] [1,4]二氮杂及其在治疗HIV感染中的用途
公开(公告)号：US5747488A
公开(公告)日：1998-05-05
申请号：US769081
申请日：1996-12-18
申请人： Karl D. Hargrave , John R. Proudfoot
发明人： Karl D. Hargrave , John R. Proudfoot
IPC分类号： A61K31/55 , A61P31/12 , A61P31/18 , A61P37/04 , A61P43/00 , C07D471/22 , C07D243/06 , A61K31/415 , C07D401/14
CPC分类号： C07D471/22
摘要： Disclosed are novel 2-aryl-5,11-dihydro-6H-dipyrido�3,2-b:2',3'-e!�1,4!diazepines. These are useful in the of HIV infection. Exemplary compounds are: 8-Ethyl-1-methyl-10-(4-pyrazolyl)imidazo�2',3':6,5!dipyrido�3,2-b:2',3'-e!�1,4!diazepine; 8-c-Propyl-1-methyl-10-(4-pyrazolyl)imidazo�2',3':6,5!dipyrido�3,2-b:2',3'-e!�1,4!diazepine; 8-Ethyl-12-methyl-10-(4-pyrazolyl)imidazo�2',3':6,5!dipyrido�3,2-b:2',3'-e!�1,4!diazepine; and, 8-c-Propyl-12-methyl-10-(4-pyrazolyl)imidazo�2',3':6,5!dipyrido�3,2-b:2',3 '-e!�1,4!diazepine.
摘要翻译：公开了新的2-芳基-5,11-二氢-6H-二吡啶并[3,2-b：2'，3'-e] [1,4]二氮杂。这些在艾滋病毒感染中是有用的。示例性化合物是：8-乙基-1-甲基-10-（4-吡唑基）咪唑并[2'，3'：6,5]二吡啶并[3,2-b：2'，3'-e] 4]二氮杂 8-C-丙基-1-甲基-10-（4-吡唑基）咪唑并[2'，3'：6,5]二吡啶并[3,2-b：2'，3'-e] [1,4] 二氮杂 8-乙基-12-甲基-10-（4-吡唑基）咪唑并[2'，3'：6,5]二吡啶并[3,2-b：2'，3'-e] [1,4]二氮杂和8-C-丙基-12-甲基-10-（4-吡唑基）咪唑并[2'，3'：6,5]二吡啶并[3,2-b：2'，3'-e] 4]二氮杂。

75. 发明授权

US5503830A Compounds having immunostimulating activity and methods of use thereof 失效
标题翻译：具有免疫刺激活性的化合物及其使用方法
公开(公告)号：US5503830A
公开(公告)日：1996-04-02
申请号：US120001
申请日：1993-09-10
申请人： Nekrasov A. Vasilevich , Puchkova N. Grigorjevna , Ataullakhanov R. Inojativich , Petrov R. Victorovich , Khaitov R. Musaevich , Ivanova A. Sergeevna
发明人： Nekrasov A. Vasilevich , Puchkova N. Grigorjevna , Ataullakhanov R. Inojativich , Petrov R. Victorovich , Khaitov R. Musaevich , Ivanova A. Sergeevna
IPC分类号： A61K39/00 , A61K39/385 , A61K39/39 , C07D233/00 , C07D241/02 , C07D403/00 , C12N11/08 , C07D231/04 , C07D243/02 , C07D243/04 , C07D243/06 , C07D243/08 , C07D403/06
CPC分类号： A61K39/0003 , C12N11/08 , A61K2039/6093
摘要： Polymeric compounds comprising subunits of the following formulas ##STR1## wherein R.sub.1, X, x, y, z, x', y' and z' are as defined in the application. The polymeric compounds are capable of stimulating the immune response system of animals, including humans. The polymeric compounds are useful also in the manufacture of medicaments, including vaccines, for the prophalaxis and treatment of conditions requiring an enhanced immune response.
摘要翻译：包含下列式（A）和（B）的亚基的聚合化合物，其中R1，X，x，y，z，x'，y'和z'如本申请中所定义。聚合物能够刺激包括人在内的动物的免疫应答系统。聚合物化合物也可用于制造包括疫苗在内的药物，用于发炎和治疗需要增强的免疫应答的病症。

76. 发明授权

US4096140A 5-Amino or substituted amino-7-phenyl or substituted phenyl-2,3-dihydro-1H-1,4-diazepines 失效
标题翻译： 5-氨基或取代的氨基-7-苯基或取代的苯基-2,3-二氢-1H-1,4-二氮杂
公开(公告)号：US4096140A
公开(公告)日：1978-06-20
申请号：US725440
申请日：1976-09-22
申请人： William R. Simpson
发明人： William R. Simpson
IPC分类号： C07D243/08 , C07D401/04 , C07D403/04 , C07D405/10 , C07D243/06 , A61K31/55
CPC分类号： C07D401/04 , C07D243/08 , C07D403/04 , C07D405/10 , Y10S514/866 , Y10S514/909
摘要： Compounds of the formula ##STR1## WHEREIN R.sub.1 is hydrogen, alkyl of 1 to 6 carbon atoms or amino, R.sub.2 is hydrogen or alkyl of 1 to 6 carbon atoms, with the provisos that (1) at least one of R.sub.1 and R.sub.2 is not a tertiary alkyl group and (2) R.sub.2 is hydrogen when R.sub.1 is amino, orR.sub.1 and R.sub.2 taken together and with the nitrogen atom to which they are joined are pyrrolidino, piperidino or N'-2-hydroxyethylpiperazino,Each X' is independently alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or halo, or two X's on adjacent carbon atoms together are methylenedioxy, andn is 0, 1, 2 or 3,And the pharmaceutically acceptable acid addition salts thereof,Are useful as anti-obesity and anti-diabetic agents. The compounds wherein R.sub.1 is alkyl and R.sub.2 is hydrogen are synthesized by a two-step synthesis from 2-alkyl-5-arylisoxazolium salts and ethylenediamine. The compounds wherein R.sub.1 and R.sub.2 are hydrogen are synthesized by cleaving the t-butyl group from the corresponding compounds wherein R.sub.1 is t-butyl and R.sub.2 is hydrogen. The compounds wherein R.sub.1 is amino are synthesized from the corresponding compounds wherein R.sub.1 is hydrogen or alkyl. All of the compounds are synthesized by reacting ammonia, a suitable amine or hydrazine with a compound of the formula ##STR2## WHEREIN R' is primary or secondary alkyl of 1 to 4 carbon atoms.
摘要翻译：下式的化合物，其中R 1为氢，1至6个碳原子的烷基或氨基，R 2为氢或1至6个碳原子的烷基，条件是（1）R 1和R 2中的至少一个不为叔烷基和（2）当R 1是氨基时，R 2是氢，或者R 1和R 2与它们连接的氮原子一起是吡咯烷子基，哌啶子基或N'-2-羟乙基哌嗪基，每个X'独立地是烷基 1至4个碳原子的烷氧基或1至4个碳原子的烷氧基或卤素，或相邻碳原子上的两个X一起是亚甲二氧基，N IS 0,1,2或3，并且其药学上可接受的酸加法盐，有用作为抗生素和抗糖尿病药物。其中R1是烷基，R2是氢的化合物是通过2-烷基-5-芳基异恶唑鎓盐和乙二胺的两步合成来合成的。其中R1和R2是氢的化合物是通过从相应的化合物中分离出叔丁基来合成的，其中R 1是叔丁基，R 2是氢。其中R 1为氨基的化合物由相应的化合物合成，其中R1为氢或烷基。所有这些化合物都是通过氨，合适的胺或肼与下式化合物的反应来合成的：其中R 1是具有1-4个碳原子的伯或仲烷基。

77. 发明授权

US3962255A 1,4-Diazaepine-5-ones 失效
标题翻译： 1,4-DIAZAEPINE-5-ONES
公开(公告)号：US3962255A
公开(公告)日：1976-06-08
申请号：US492087
申请日：1974-07-26
申请人： Alexander Michael Chalmers
发明人： Alexander Michael Chalmers
IPC分类号： C08K5/00 , C07D243/08 , C08K5/3442 , C08L1/00 , C08L7/00 , C08L21/00 , C08L23/00 , C08L27/00 , C08L27/06 , C08L33/00 , C08L33/02 , C08L51/00 , C08L51/02 , C08L77/00 , C08L101/00 , C09K15/30 , C07D243/06
CPC分类号： C07D243/08 , C08K5/3442
摘要： According to the present invention, there are provided compounds having the formula: ##SPC1##And salts thereof, wherein n is 1 or 2, X is O of NH, Y is O, hydrogen or a branched- or straight chain alkyl residue having from 1 to 4 carbons and R.sub.1 is a hydrocarbyl residue having from 1 to 20 carbon atoms, which are useful as stabilisers for polymers.

78. 发明授权

US08513239B2 Chiral cis-imidazolines 有权
标题翻译：手性顺式 - 咪唑啉
公开(公告)号：US08513239B2
公开(公告)日：2013-08-20
申请号：US12248095
申请日：2008-10-09
申请人： David Joseph Bartkovitz , Jianping Cai , Xin-Jie Chu , Hongju Li , Allen John Lovey , Binh Thanh Vu , Chunlin Zhao
发明人： David Joseph Bartkovitz , Jianping Cai , Xin-Jie Chu , Hongju Li , Allen John Lovey , Binh Thanh Vu , Chunlin Zhao
IPC分类号： A61K31/55 , A61K31/03 , A61K31/44 , A61K31/535 , A61K31/505 , C07D243/06 , C07D243/14 , C07D279/10 , C07D413/08 , C07D403/08 , C07D239/02 , C07D215/02
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/10
摘要： There are provided compounds of the formula or the pharmaceutically acceptable salts thereof, wherein X, Y, Z, V1, V2, R1, R2, R3, R4 and R5 are herein described. These compounds are useful as anticancer agents.
摘要翻译：提供下式的化合物或其药学上可接受的盐，其中本文描述了X，Y，Z，V1，V2，R 1，R 2，R 3，R 4和R 5。这些化合物可用作抗癌药。

79. 发明授权

US08501750B2 Heterocyclic compound and use thereof 失效
标题翻译：杂环化合物及其用途
公开(公告)号：US08501750B2
公开(公告)日：2013-08-06
申请号：US12451602
申请日：2008-05-20
申请人： Takanobu Kuroita , Hideyuki Igawa , Hiroki Sakamoto , Kouhei Asano , Minoru Sasaki
发明人： Takanobu Kuroita , Hideyuki Igawa , Hiroki Sakamoto , Kouhei Asano , Minoru Sasaki
IPC分类号： C07D495/04 , A61K31/519 , C07D239/545 , C07D513/04 , C07D471/02 , C07D243/06 , C07D235/00 , A61K31/4365 , A61K31/5513 , A61K31/4188 , A61K31/506
CPC分类号： C07D413/10 , C07D495/04 , C07D495/14 , C07D513/04
摘要： Heterocyclic compounds, pharmaceutical agent and methods thereof, having superior pharmacological action and/or physicochemical properties, which are useful for the prophylaxis or treatment of circulatory diseases such as hypertension, cardiac diseases, arteriosclerosis, renal diseases and cerebral apoplexy and/or metabolic diseases such as hyperlipidemia, obesity and diabetes and/or central nervous disorders such as cerebral infarction, and/or mental diseases such as dementia depression and depression.
摘要翻译：具有优异的药理作用和/或物理化学性质的杂环化合物，药物及其方法，其可用于预防或治疗诸如高血压，心脏病，动脉硬化，肾脏疾病和脑中风和/或代谢疾病之类的循环系统疾病如高脂血症，肥胖症和糖尿病和/或中枢神经障碍如脑梗死和/或精神疾病如痴呆抑郁症和抑郁症。

80. 发明授权

US08324200B2 Compositions and methods for inhibition of the JAK pathway 有权
标题翻译：用于抑制JAK途径的组合物和方法
公开(公告)号：US08324200B2
公开(公告)日：2012-12-04
申请号：US12692493
申请日：2010-01-22
申请人： Hui Li , Thilo J. Heckrodt , Yan Chen , Darren John McMurtrie , Vanessa Taylor , Rajinder Singh , Pingyu Ding , Sambaiah Thota , Rose Yen
发明人： Hui Li , Thilo J. Heckrodt , Yan Chen , Darren John McMurtrie , Vanessa Taylor , Rajinder Singh , Pingyu Ding , Sambaiah Thota , Rose Yen
IPC分类号： A61K31/33 , A61K31/55 , A61K31/505 , A61K31/535 , C07D243/06 , C07D413/14 , C07D401/14
CPC分类号： C07D413/12 , A61K31/155 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/54 , A61K31/541 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/635 , A61K31/675 , A61K45/06 , C07D401/14 , C07D403/12 , C07D413/04 , C07D413/14 , C07D419/14 , C07D451/02 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/08 , C07D498/04 , C07F9/65583
摘要： Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
摘要翻译：公开了式I的化合物，含有它们的组合物，以及用于化合物和组合物用于治疗JAK途径的调节或JAK激酶，特别是JAK 2和JAK 3的抑制在治疗上有用的条件的方法。

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