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11. 发明申请

US20080287489A1 Ophthalmic compositions for treating ocular hypertension 审中-公开
标题翻译：用于治疗高眼压症的眼用组合物
公开(公告)号：US20080287489A1
公开(公告)日：2008-11-20
申请号：US12220306
申请日：2008-07-23
申请人： Dong-Ming Shen , James B. Doherty
发明人： Dong-Ming Shen , James B. Doherty
IPC分类号： A61K31/472 , A61K31/352 , C07D307/81 , C07D217/18 , A61P27/00 , A61K31/381 , C07D333/60
CPC分类号： C07D307/81 , C07D307/80 , C07D333/56 , C07D333/60 , C07D405/06
摘要： This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
摘要翻译：本发明涉及式I的有效钾通道阻断剂化合物或其制剂用于治疗青光眼和导致患者眼睛眼内压升高的其它病症。本发明还涉及这些化合物对哺乳动物物种尤其是人的眼睛的神经保护作用的用途。

12. 发明授权

US07335659B2 Substituted 10-aryl-11H-benzo[b]fluorenes and 7-aryl-5, 6-dihydro-benzo[a]anthracenes for selective effects on estrogen receptors 有权
公开(公告)号：US07335659B2
公开(公告)日：2008-02-26
申请号：US10505631
申请日：2003-02-14
申请人： Hubert Jan Jozef Loozen , Markus Wagener , Gerrit Veeneman , Eduard Willem Zwart
发明人： Hubert Jan Jozef Loozen , Markus Wagener , Gerrit Veeneman , Eduard Willem Zwart
IPC分类号： A61K31/496 , A61K31/44 , A61K31/40 , A61K31/138 , A61K31/085 , C07D403/04 , C07D211/70 , C07D207/12 , C07D217/18 , C07D43/205
CPC分类号： C07D239/42 , C07C39/17 , C07C43/225 , C07C43/23 , C07C49/753 , C07C217/58 , C07C323/18 , C07C2603/40 , C07C2603/42 , C07D211/70 , C07D277/62 , C07D295/088 , C07D317/54
摘要： This invention provides a compound, or its possible salt, having the formula, wherein: Re and ′Re are OH, optionally independently etherified or esterified; Z is —CH2CH2— or —C(R4,R5)—, wherein R4 and R5 are independently H, (1C-2C)alkyl or form together a spiro(3C-5C)cycloalkyl; R1 is H, halogen, CF3, or (1C-4C)alkyl; R2 and R3 are independently H, halogen, —CF3, —OCF3, (1C-8C)alkyl, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo(1C-8C)alkyl, —O(CH2)mX, wherein X is halogen or phenyl and m=2-4; —O(CH2)mNRaRb, —S(CH2)mNRaRb or —(CH2)mNRaRb, wherein m=2-4 and wherein Ra, Rb are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, which alkyl, alkenyl and aryl can optionally be substituted with halogen, —CF3, —OCF3, —CN, —NO2, —OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl or halo(1C-8C)alkyl; or Ra and Rb form a 3-8 membered ring structure, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, hydroxy, hydroxy(1C-4C)alkyl, (1C-8C)alkoxy, aryloxy, (1C-8C)alkylthio, carboxyl, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl, halo(1C-8C)alkyl.

13. 发明授权

US06962996B2 Inhibitors of p38 有权
公开(公告)号：US06962996B2
公开(公告)日：2005-11-08
申请号：US10883305
申请日：2004-07-01
申请人： John Cochran , Roger Tung
发明人： John Cochran , Roger Tung
IPC分类号： A61K31/472 , A61K31/4725 , A61K31/496 , A61K31/551 , A61P1/00 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P7/00 , A61P7/02 , A61P7/06 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/00 , A61P19/00 , A61P19/02 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D217/18 , C07D217/22 , C07D217/24 , C07D401/04 , C07D217/00 , C07D217/16
CPC分类号： C07D217/12 , C07D217/18 , C07D217/22
摘要： The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

14. 发明授权

US06956033B2 3,4-dihydroisoquinoline derivative compound and a pharmaceutical agent comprising it as active ingredient 失效
标题翻译： 3,4-二氢异喹啉衍生物和作为有效成分的药剂
公开(公告)号：US06956033B2
公开(公告)日：2005-10-18
申请号：US10333591
申请日：2001-07-30
申请人： Mikio Ogawa , Yoshikazu Takaoka , Akira Ohhata
发明人： Mikio Ogawa , Yoshikazu Takaoka , Akira Ohhata
IPC分类号： A61K31/472 , A61K31/4725 , A61P11/06 , A61P17/00 , A61P25/04 , A61P27/16 , A61P29/00 , A61P37/04 , A61P37/06 , A61P37/08 , C07D217/16 , C07D217/18 , C07D221/20 , C07D265/14 , C07D401/04 , C07D401/06 , C07D405/04 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D471/04 , C07D491/04 , C07D491/10 , C07D491/107 , C07D495/04 , C07D401/02 , A61K31/47
CPC分类号： C07D221/20 , A61K31/472 , A61K31/4725 , C07D217/16 , C07D217/18 , C07D265/14 , C07D401/04 , C07D401/06 , C07D405/04 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D471/04 , C07D491/04 , C07D491/10 , C07D495/04
摘要： A 3,4-dihydroisoquinoline derivative compound of formula (I) or a non-toxic salt thereof and a pharmaceutical agent comprising it as active ingredient (wherein all symbols have the same meaning as described in the specification). The compound of formula (I) has agonizing activity on CB2 receptor and therefore it is useful for the prophilaxis and/or treatment of various diseases such as asthma, nasal allergy, atopic dermatitis, autoimmune diseases, rheumatoid arthritis, immune dysfunction, postoperative pain, carcinomatous pain, etc.
摘要翻译：式（I）的3,4-二氢异喹啉衍生物或其无毒盐和包含它作为有效成分的药剂（其中所有符号具有与说明书中所述相同的含义）。式（I）化合物对CB2受体具有激动作用，因此可用于各种疾病如哮喘，鼻过敏，特应性皮炎，自身免疫性疾病，类风湿性关节炎，免疫功能障碍，术后疼痛，癌性疼痛等

15. 发明授权

US06911453B2 Substituted 4-phenyltetrahydroisoquinolinium, process for their preparation, their use as a medicament, and medicament containing them 有权
标题翻译：取代的4-苯基四氢异喹啉鎓，其制备方法，它们作为药物的用途，以及含有它们的药物
公开(公告)号：US06911453B2
公开(公告)日：2005-06-28
申请号：US10309352
申请日：2002-12-04
申请人： Armin Hofmeister , Uwe Heinelt , Hans-Jochen Lang , Markus Bleich , Klaus Wirth , Michael Gekle
发明人： Armin Hofmeister , Uwe Heinelt , Hans-Jochen Lang , Markus Bleich , Klaus Wirth , Michael Gekle
IPC分类号： C07D217/18 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D217/00 , A61K31/47
CPC分类号： C07D401/12 , C07D217/18 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The invention relates to compounds of the formula I in which R1 to R9 are as defined herein. In one embodiment, these compounds may be used as antihypertensives, for reducing or preventing ischemia-induced damage, as medicaments for surgical intervention for the treatment of ischemias of the nervous system, of stroke and of cerebral edema, of shock, of impaired respiratory drive, for the treatment of snoring, as laxative, as agent against ectoparasites, to prevent the formation of gallstones, as antiatherosclerotics, agents against late complications of diabetes, cancers, fibrotic disorders, endothelial dysfunction, organ hypertrophies and hyperplasias. In one embodiment, the compounds may be inhibitors of the cellular sodium-proton antiporter and influence serum lipoproteins and thus be used for the prophylaxis and for the regression of atherosclerotic lesions.
摘要翻译：本发明涉及其中R 1至R 9如本文所定义的式I化合物。在一个实施方案中，这些化合物可以用作抗高血压药物，用于减少或预防缺血诱发的损伤，作为用于治疗神经系统缺血性卒中和脑水肿的外科手术的药物，休克，受损的呼吸驱动用于治疗打鼾，作为缓泻剂，作为对外寄生虫剂的药剂，以防止胆结石的形成，作为抗动脉粥样硬化剂，用于治疗糖尿病晚期并发症的药物，癌症，纤维化病症，内皮功能障碍，器官肥厚和增生。在一个实施方案中，化合物可以是细胞钠 - 质子逆转录酶的抑制剂并影响血清脂蛋白，因此用于预防动脉粥样硬化病变的消退。

16. 发明申请

US20050004360A1 Compounds and methods for modulation of estrogen receptors 失效
标题翻译：用于调节雌激素受体的化合物和方法
公开(公告)号：US20050004360A1
公开(公告)日：2005-01-06
申请号：US10731666
申请日：2003-12-08
申请人： Leah Gayo-Fung , Bernd Stein
发明人： Leah Gayo-Fung , Bernd Stein
IPC分类号： A61K31/4035 , A61K31/454 , A61K31/472 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P9/00 , A61P9/14 , A61P13/02 , A61P13/08 , A61P15/00 , A61P15/12 , A61P17/00 , A61P17/02 , A61P19/00 , A61P25/00 , A61P25/28 , A61P27/12 , A61P35/00 , A61P43/00 , C07D209/44 , C07D217/04 , C07D217/16 , C07D217/18 , C07D217/20 , C07D223/16 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D413/12 , C07D417/12 , C07
CPC分类号： C07D223/16 , C07D209/44 , C07D217/04 , C07D217/16 , C07D217/18 , C07D217/20 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04
摘要： Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-β over ER-α. Methods are disclosed for modulating ER-β in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-β. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.
摘要翻译：公开了调节雌激素受体（ER）的化合物以及含有它们的药物组合物。在一个具体的实施方案中，化合物是针对ER-α的ER-β的选择性调节剂。公开了用于在表达其的细胞和/或组织中调节ER-β的方法，包括优先表达ER-β的细胞和/或组织。更一般地，还公开了治疗雌激素相关病症的方法，包括诸如乳腺癌，睾丸癌，骨质疏松症，子宫内膜异位症，心血管疾病，高胆固醇血症，前列腺肥大，前列腺癌，肥胖症，潮热，皮肤效应，情绪波动，记忆丧失，尿失禁，脱发，白内障，天然荷尔蒙失衡，以及与暴露于环境化学品相关的不良生殖影响。

17. 发明授权

US6043253A Fused piperidine substituted arylsulfonamides as .beta.3-agonists 失效
标题翻译：将哌啶取代的芳基磺酰胺作为β3-激动剂
公开(公告)号：US6043253A
公开(公告)日：2000-03-28
申请号：US257707
申请日：1999-02-25
申请人： Linda Brockunier , Ann E. Weber , Emma R. Parmee
发明人： Linda Brockunier , Ann E. Weber , Emma R. Parmee
IPC分类号： C07D217/16 , C07D217/18 , C07D217/00 , A61K31/47
CPC分类号： C07D217/18 , C07D217/16
摘要： Fused piperidine substituted arylsulfonamides are .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for decreasing gut motility are also disclosed.
摘要翻译：融合的哌啶取代的芳基磺酰胺是具有非常少的β1和β2肾上腺素能受体活性的β3肾上腺素能受体激动剂，因此这些化合物能够增加细胞中的脂肪分解和能量消耗。因此，这些化合物在治疗II型糖尿病和肥胖中具有有效的活性。该化合物也可用于降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠道运动性。此外，该化合物可用于减少神经源性炎症或作为抗抑郁剂。还公开了使用该化合物治疗糖尿病和肥胖以及降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠蠕动的组合物和方法。

18. 发明授权

US5866610A Substituted benzoylguanidines, process for their preparation, their use as a pharmaceutical as inhibitors of the cellular NA+/H+ exchange or as a diagnostic, and pharmaceutical containing them 失效
标题翻译：取代的苯甲酰胍，其制备方法，它们作为药物用作细胞NA + / H +交换的抑制剂或作为诊断剂，以及含有它们的药物
公开(公告)号：US5866610A
公开(公告)日：1999-02-02
申请号：US683141
申请日：1996-07-18
申请人： Hans-Jochen Lang , Andreas Weichert , Heinz-Werner Kleemann , Jan-Robert Schwark , Wolfgang Scholz , Udo Albus
发明人： Hans-Jochen Lang , Andreas Weichert , Heinz-Werner Kleemann , Jan-Robert Schwark , Wolfgang Scholz , Udo Albus
IPC分类号： A61K31/165 , A61K31/155 , A61K31/166 , A61K31/44 , A61K31/47 , A61K31/472 , A61P1/04 , A61P1/16 , A61P3/10 , A61P7/02 , A61P9/00 , A61P9/02 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/08 , A61P13/12 , A61P35/00 , A61P43/00 , C07C233/65 , C07C277/08 , C07C279/18 , C07C279/22 , C07D213/30 , C07D213/56 , C07D215/14 , C07D215/50 , C07D217/18 , C07D217/24
CPC分类号： C07C279/22 , Y10S514/821
摘要： Substituted benzoylguanidines, process for their preparation, their use as a pharmaceutical or diagnostic, and pharmaceutical containing them.Described are benzoylguanidines of the formula I ##STR1## where R(1) to R(3) are H, Hal, (cyclo)alkyl, N.sub.3, CN or OH, alkyloxy, phenyl, phenoxy or benzoyl, and their pharmacologically acceptable salts, but with the exception of the compounds benzoylguanidine, 4-chlorobenzoylguanidine, 3,4-dichlorobenzoylguanidine and 3- or 4-methylbenzoylguanidine.They are obtained by reacting a compound II ##STR2## with guanidine, L being a leaving group.
摘要翻译：取代的苯甲酰胍，其制备方法，它们作为药物或诊断用途，以及含有它们的药物。描述了式I（I）的苯甲酰胍，其中R（1）至R（3）为H，Hal，（环）烷基，N 3，CN或OH，烷氧基，苯基，苯氧基或苯甲酰基，但是除了化合物苯甲酰胍，4-氯苯甲酰胍，3,4-二氯苯甲酰胍和3-或4-甲基苯甲酰基胍之外。它们通过使化合物II（II）与胍反应而获得，L是离去基团。

19. 发明授权

US5674878A Anellated dihydropyridines and the use thereof for the production of pharmaceutical preparations 失效
标题翻译： Anellated dihydropyridines及其用于制备药物制剂的用途
公开(公告)号：US5674878A
公开(公告)日：1997-10-07
申请号：US477214
申请日：1995-06-07
申请人： Dietrich Arndts , Walter Losel , Otto Roos
发明人： Dietrich Arndts , Walter Losel , Otto Roos
IPC分类号： C07D217/14 , C07D217/18 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D491/04 , C07D495/04 , A61K31/44 , A61K31/535 , A61K31/54
CPC分类号： C07D401/12 , C07D217/14 , C07D217/18 , C07D405/12 , C07D409/12 , C07D471/04 , C07D491/04 , C07D495/04
摘要： Compound of general formula I ##STR1## wherein A is a benzo or thieno group; R.sub.1 is (C.sub.4-6)cycloalkyl, (C.sub.4-6)cycloalkyl-(C.sub.1-5)alkyl or ##STR2## R.sup.2, m, R.sup.3, R.sup.4, R and u are defined as in the specification, and pharmaceutical preparations containing this compound and the new pharmaceutical uses thereof.
摘要翻译：通式I的化合物其中A是苯并或噻吩基; R1是（C4-6）环烷基，（C4-6）环烷基 - （C1-5）烷基或R2，m，R3，R4，R和u如说明书中所定义，含有该化合物的药物制剂及其新药用途。

20. 发明授权

US5359074A Process for the preparation of racemic and optically active 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid and its precursors 失效
公开(公告)号：US5359074A
公开(公告)日：1994-10-25
申请号：US76772
申请日：1993-06-15
申请人： Bernhard Kammermeier , Ulrich Lerch
发明人： Bernhard Kammermeier , Ulrich Lerch
IPC分类号： C07D217/26 , C07D217/20 , A61K31/47 , C07D217/18
CPC分类号： C07D217/26
摘要： A process for the preparation of racemic and optically active 1,2.3,4-tetrahydroisoquinoline-3-carboxylic acid is described, in which dihalo-o-xylylenes are cyclized to dicarboxylic acid esters in basic medium using dialkyl N-acylamidomalonates of the formula (CO.sub.2 R.sup.1).sub.2 CHNHCOR.sup.2, in which R.sup.1 is (C.sub.1 -C.sub.4)-alkyl and R.sup.2 is H, (C.sub.1 -C.sub.4)-alkyl or (C.sub.6 -C.sub.12)-aryl, decarboxylated by basic hydrolysis and subsequent acid work-up and then reacted in acid medium to give (D,L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, or dihalo-o-xylylenes are cyclized in basic medium to give the dicarboxylic acid esters and these are reacted directly without isolation in a one-pot process to give (D,L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, if desired the racemic 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid is reacted with (-)menthol and p-toluenesulfonic acid to give (-)menthyl (D)- or (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate, then the diastereomers are separated by column chromatography and subjected to basic hydrolysis to give (D)-or (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, or (D,L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid is esterified by means of benzyl alcohol and p-toluenesulfonic acid, reacted with D(-)mandelic acid to give benzyl (D)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (D)-mandelate and benzyl (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (D)-mandelate or with L(+)mandelic acid to give benzyl (D)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (L)-mandelate and benzyl (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (L)-mandelate and then the compounds obtained are separated into the optical antipodes by fractional crystallization in an inert solvent and the enantiomers (D)- or (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid are liberated by basic hydrolysis, the chiral auxiliary reagent being recovered.

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