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61. 发明授权

US09487494B2 Cyclic hydrocarbon compounds for the treatment of diseases 有权
标题翻译：用于治疗疾病的环状碳氢化合物
公开(公告)号：US09487494B2
公开(公告)日：2016-11-08
申请号：US12744137
申请日：2008-11-20
申请人： Jef Fensholdt , Sophie Elisabeth Havez , Bjarne Nørremark
发明人： Jef Fensholdt , Sophie Elisabeth Havez , Bjarne Nørremark
IPC分类号： C07D295/182 , C07C211/35 , C07C211/36 , C07C211/48 , C07C215/28 , C07C217/52 , C07C217/74 , C07C233/05 , C07C233/41 , C07C237/24 , C07C237/30 , C07C237/32 , C07C237/34 , C07C237/36 , C07C237/40 , C07C239/14 , C07C255/03 , C07C255/32 , C07C255/50 , C07C257/18 , C07C259/10 , C07C259/18 , C07C271/44 , C07C309/15 , C07C311/05 , C07C311/08 , C07C311/37 , C07C311/51 , C07C317/32 , C07D205/04 , C07D207/08 , C07D207/12 , C07D207/16 , C07D207/27 , C07D209/08 , C07D209/12 , C07D209/20 , C07D211/46 , C07D211/60 , C07D211/62 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/80 , C07D231/12 , C07D231/40 , C07D233/61 , C07D233/90 , C07D263/22 , C07D271/06 , C07D295/088 , C07D295/13 , C07D295/135 , C07D295/192 , C07D295/195 , C07D295/26 , C07D305/08 , C07D307/12 , C07D307/52 , C07D307/68 , C07D307/79 , C07D309/10 , C07D319/18 , C07D333/38 , C07D333/40 , C07D333/58 , C07D413/04 , C07D413/06 , C07D417/06
CPC分类号： C07D295/182 , C07C211/35 , C07C211/36 , C07C211/48 , C07C215/28 , C07C217/52 , C07C217/74 , C07C233/05 , C07C233/41 , C07C237/24 , C07C237/30 , C07C237/32 , C07C237/34 , C07C237/36 , C07C237/40 , C07C239/14 , C07C255/03 , C07C255/32 , C07C255/50 , C07C257/18 , C07C259/10 , C07C259/18 , C07C271/44 , C07C309/15 , C07C311/05 , C07C311/08 , C07C311/37 , C07C311/51 , C07C317/32 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D205/04 , C07D207/08 , C07D207/12 , C07D207/16 , C07D207/27 , C07D209/08 , C07D209/12 , C07D209/20 , C07D211/46 , C07D211/60 , C07D211/62 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/80 , C07D231/12 , C07D231/40 , C07D233/61 , C07D233/90 , C07D263/22 , C07D271/06 , C07D295/088 , C07D295/13 , C07D295/135 , C07D295/192 , C07D295/195 , C07D295/26 , C07D305/08 , C07D307/12 , C07D307/52 , C07D307/68 , C07D307/79 , C07D309/10 , C07D319/18 , C07D333/38 , C07D333/40 , C07D333/58 , C07D413/04 , C07D413/06 , C07D417/06
摘要： The invention relates to novel cyclic hydrocarbon compounds and derivatives thereof, processes for the preparation thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.
摘要翻译：本发明涉及新的环烃化合物及其衍生物，其制备方法，用作药物的所述化合物，用于治疗的所述化合物，包含所述化合物的药物组合物，涉及用所述化合物治疗疾病的方法，以及所述化合物在制备药物中的用途。

62. 发明授权

US09474739B2 Substituted 2-[2-(phenyl) ethylamino] alkaneamide derivatives and their use as sodium and/or calcium channel modulators 有权
公开(公告)号：US09474739B2
公开(公告)日：2016-10-25
申请号：US14615227
申请日：2015-02-05
申请人： NEWRON PHARMACEUTICALS S.P.A.
发明人： Piero Melloni , Alessandra Restivo , Emanuela Izzo , Simona Francisconi , Elena Colombo , Cibele Sabido-David
IPC分类号： A61K31/165 , A61K31/137 , A61P1/00 , A61K31/381 , C07C237/08 , C07C317/28 , C07C323/25 , C07C327/42 , C07D295/182 , A61K31/40 , A61K31/4515 , A61K31/519 , A61K31/5513 , C07C237/06 , C07D207/16 , C07D333/20 , C07C237/20 , C07C321/26 , C07C327/44
CPC分类号： A61K31/381 , A61K31/137 , A61K31/165 , A61K31/40 , A61K31/4515 , A61K31/519 , A61K31/5513 , C07C237/06 , C07C237/08 , C07C237/20 , C07C317/28 , C07C321/26 , C07C323/25 , C07C327/42 , C07C327/44 , C07D207/16 , C07D295/182 , C07D333/20
摘要： Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives of formula (I) wherein X, Y, Z, R, R1, R2, R3, R′3 R4, R5, R6, R7 have the meanings defined in the specification and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.

63. 发明授权

US09474738B2 Substituted 2-[2-(phenyl) ethylamino] alkaneamide derivatives and their use as sodium and/or calcium channel modulators 有权
公开(公告)号：US09474738B2
公开(公告)日：2016-10-25
申请号：US14615176
申请日：2015-02-05
申请人： NEWRON PHARMACEUTICALS S.P.A.
发明人： Piero Melloni , Alessandra Restivo , Emanuela Izzo , Simona Francisconi , Elena Colombo , Cibele Sabido-David
IPC分类号： A61K31/165 , A61K31/137 , A61P13/00 , A61K31/381 , C07C237/08 , C07C317/28 , C07C323/25 , C07C327/42 , C07D295/182 , A61K31/40 , A61K31/4515 , A61K31/519 , A61K31/5513 , C07C237/06 , C07D207/16 , C07D333/20 , C07C237/20 , C07C321/26 , C07C327/44
CPC分类号： A61K31/381 , A61K31/137 , A61K31/165 , A61K31/40 , A61K31/4515 , A61K31/519 , A61K31/5513 , C07C237/06 , C07C237/08 , C07C237/20 , C07C317/28 , C07C321/26 , C07C323/25 , C07C327/42 , C07C327/44 , C07D207/16 , C07D295/182 , C07D333/20
摘要： Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives of formula (I) wherein X, Y, Z, R, R1, R2, R3, R′3 R4, R5, R6, R7 have the meanings defined in the specification and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.

64. 发明授权

US09458094B2 Fatty acid acetylated salicylates and their uses 有权
公开(公告)号：US09458094B2
公开(公告)日：2016-10-04
申请号：US14251247
申请日：2014-04-11
申请人： Catabasis Pharmaceuticals, Inc.
发明人： Jill C. Milne , Michael R. Jirousek , Jean E. Bemis , Jesse J. Smith
IPC分类号： C07C235/60 , C07C69/86 , C07C69/94 , C07C233/18 , C07C233/49 , C07C233/55 , C07C237/22 , C07C271/28 , C07C275/42 , C07D295/182 , C07D295/192 , C07C235/52 , A61K31/60
CPC分类号： A61K31/609 , A61K31/60 , C07C69/86 , C07C69/94 , C07C233/18 , C07C233/49 , C07C233/55 , C07C235/52 , C07C235/60 , C07C237/22 , C07C271/28 , C07C275/42 , C07D295/182 , C07D295/192
摘要： The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative.

65. 发明授权

US08889685B2 Method for treating a sleep disorder with eszopiclone maleate 有权
标题翻译：用马来酸右佐匹克隆治疗睡眠障碍的方法
公开(公告)号：US08889685B2
公开(公告)日：2014-11-18
申请号：US13928571
申请日：2013-06-27
申请人： Sunovion Pharmaceuticals Inc.
发明人： H. Scott Wilkinson , Richard Hsia , Tushar Misra , Kostas Saranteas , Patrick Mousaw
IPC分类号： A61K31/444 , A61K31/495 , A61K31/4985 , C07D213/61 , C07D295/182 , C07D471/04 , C07D487/04
CPC分类号： C07D487/04 , C07C57/145
摘要： Maleate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided. The salts are useful for treating sleep disorders.
摘要翻译：（6-（5-氯-2-吡啶基）-5 - [（4-甲基-1-哌嗪基）羰氧基] -7-氧代-6,7-二氢-5H-吡咯并[3,4-b ]吡嗪）。这些盐可用于治疗睡眠障碍。

66. 发明申请

US20120252776A1 C4 Monomethyl Triterpenoid Derivatives and Methods of Use Thereof 有权
标题翻译： C4单甲基三萜衍生物及其使用方法
公开(公告)号：US20120252776A1
公开(公告)日：2012-10-04
申请号：US13417519
申请日：2012-03-12
申请人： Eric Anderson , Christopher F. Bender , Xiaofeng Liu , Xin Jiang , Melean Visnick
发明人： Eric Anderson , Christopher F. Bender , Xiaofeng Liu , Xin Jiang , Melean Visnick
IPC分类号： A61K31/277 , C07D233/61 , A61K31/4164 , C07D271/10 , A61K31/4245 , C07D271/06 , C07D295/182 , A61K31/5375 , C07D205/04 , A61K31/397 , A61K31/4453 , C07D305/08 , A61K31/337 , C07C311/07 , A61P29/00 , A61P39/06 , C07C275/26 , C07D491/107 , C07C255/47
CPC分类号： C07J63/008 , C07J71/0005
摘要： Disclosed herein are novel C4-monomethyl triterpenoid compounds and derivatives thereof, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example as antioxidant inflammation modulators, and compositions thereof are also provided.
摘要翻译：本文公开了新的C4-单甲基三萜化合物及其衍生物，包括下式的化合物：其中变量在本文中定义。还提供了包含这些化合物的药物组合物，试剂盒和制品。还提供了可用于制备化合物的方法和中间体，以及使用化合物的方法，例如抗氧化剂炎症调节剂及其组合物。

67. 发明申请

US20090270385A1 SUBSTITUTED ARYLCYCLOPENTENES AS THERAPEUTIC AGENTS 有权
标题翻译：作为治疗剂代替ARYLCYCLOPENTEN
公开(公告)号：US20090270385A1
公开(公告)日：2009-10-29
申请号：US12427803
申请日：2009-04-22
申请人： David W. Old , Vinh X. Ngo
发明人： David W. Old , Vinh X. Ngo
IPC分类号： A61K31/5377 , C07C69/76 , C07D295/182 , C07D333/38 , C07D413/12 , A61K31/235 , A61K31/5375 , A61K31/381 , A61P17/14
CPC分类号： C07C69/736 , C07C405/00 , C07C2601/08 , C07C2601/10 , C07D295/104 , C07D333/38
摘要： Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein G, B, Y, and A are as described.Methods, compositions, and medicaments related thereto are also disclosed.
摘要翻译：公开了包含其药学上可接受的盐或其前药的化合物，其中G，B，Y和A如上所述。还公开了与之相关的方法，组合物和药物。

68. 发明申请

US20090131452A1 BENZENESULFONANILIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 有权
标题翻译：适用于治疗依托莫司汀5-HT6受体调节的病症的苯并呋喃半导体化合物
公开(公告)号：US20090131452A1
公开(公告)日：2009-05-21
申请号：US12262455
申请日：2008-10-31
申请人： Wilfried Martin Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Wolfgang Wernet , Matthias Mayrer , Ana Jongen-Relo , Anton Bespalov , Min Zhang
发明人： Wilfried Martin Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Wolfgang Wernet , Matthias Mayrer , Ana Jongen-Relo , Anton Bespalov , Min Zhang
IPC分类号： A61K31/496 , C07D295/182 , C07D405/12 , A61P25/00 , A61K31/495
CPC分类号： C07D295/12 , C07D405/12
摘要： The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I′ and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein R1 is hydrogen or methyl R2 is hydrogen or methyl R3 hydrogen, fluorine C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R4 is hydrogen, C1-C4 alkyl or fluorinated C1-C4 alkyl; R5 is hydrogen, fluorine, C1-C2 alkyl fluorinated C1-C2 alkyl C1-C2 alkoxy or fluorinated C1-C2 alkoxy; and R6 is hydrogen, fluorine or chlorine.
摘要翻译：本发明涉及式I和I'的新型苯磺酰苯胺化合物和生理上耐受的酸加成盐及其N-氧化物。该化合物具有有价值的治疗特性，特别适用于治疗对血清素5-HT 6受体调节作出反应的疾病。其中R1是氢或甲基R2是氢或甲基R3氢，氟C1-C2烷氧基或氟化C1-C2烷氧基; R4是氢，C1-C4烷基或氟化C1-C4烷基; R5是氢，氟，C1-C2烷基氟化C1-C2烷基C1-C2烷氧基或氟化C1-C2烷氧基; R6是氢，氟或氯。

69. 发明授权

US5663174A Aromatic sulfonamide derivatives, their use as enzyme inhibitors and pharmaceutical compositions containing them 失效
标题翻译：芳族磺酰胺衍生物，它们作为酶抑制剂和含有它们的药物组合物的用途
公开(公告)号：US5663174A
公开(公告)日：1997-09-02
申请号：US785251
申请日：1997-01-17
申请人： Raymond Dumont
发明人： Raymond Dumont
IPC分类号： A61K31/18 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/47 , A61K31/495 , A61P13/12 , A61P19/02 , A61P29/00 , A61P37/00 , A61P43/00 , C07C311/14 , C07C311/15 , C07C311/16 , C07C311/18 , C07C311/19 , C07C311/21 , C07D207/02 , C07D207/16 , C07D207/48 , C07D209/20 , C07D217/22 , C07D295/18 , C07D295/182 , C07D295/185 , C07D295/20 , C07D295/205 , C07D295/26 , C07D401/12 , C07D403/12 , C12N9/99 , C07D403/06
CPC分类号： C07D295/185 , C07C311/19 , C07C311/21 , C07D207/48 , C07D209/20 , C07D295/205 , C07D401/12
摘要： Aromatic sulfonamide derivatives, particularly benzenesulfonamide, 4-fluorobenzenesulfonamide, 5-chloro-1-naphthalenesulfonamide and 5-isoquinolinesulfonamide derivatives are provided that inhibit Ca.sup.2+ -dependent enzymes and proteins such as Phospholipase A.sub.2, protein kinases such as Protein Kinase C, and inhibit membrane fusion, thereby being a valuable drug for the treatment of inflammation, arthritis, infarction, nephritis and many other types of tissue injury.
摘要翻译：提供芳族磺酰胺衍生物，特别是苯磺酰胺，4-氟苯磺酰胺，5-氯-1-萘磺酰胺和5-异喹啉磺酰胺衍生物，其抑制Ca 2+依赖性酶和蛋白质如磷脂酶A2，蛋白激酶如蛋白激酶C，并抑制膜融合从而成为用于治疗炎症，关节炎，梗死，肾炎和许多其他类型的组织损伤的有价值的药物。

70. 发明授权

US5432178A Amidinophenol derivatives 失效
标题翻译：脒基苯酚衍生物
公开(公告)号：US5432178A
公开(公告)日：1995-07-11
申请号：US121499
申请日：1993-09-16
申请人： Hisao Nakai , Masanori Kawamura , Tsumoru Miyamoto
发明人： Hisao Nakai , Masanori Kawamura , Tsumoru Miyamoto
IPC分类号： C07D295/18 , A61K31/235 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/495 , A61P29/00 , A61P37/08 , A61P43/00 , C07C257/18 , C07C323/59 , C07C323/62 , C07C323/63 , C07D205/04 , C07D207/08 , C07D207/16 , C07D209/20 , C07D223/04 , C07D295/185 , C07D295/192 , A61K31/445 , C07D241/04 , C07D295/182
CPC分类号： C07D295/185 , C07C257/18 , C07C323/59 , C07C323/62 , C07D207/16 , C07D209/20 , C07D295/192 , C07C2101/02 , C07C2101/04 , C07C2101/10 , C07C2101/14
摘要： Amidinophenol derivatives of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are (i) H, (ii) C1-4 alkyl, (iii) C1-4 alkoxy, (iv) C2-5 acyl, (v) halogen, (vi) NO.sub.2, (vii) benzoyl, (viii) COOR.sup.4 (in which R.sup.4 is C1-3 alkyl); A is bond, C1-4 alkylene, --C(R.sup.5).dbd.C(R.sup.6)-- (in which R.sup.5 and R.sup.6 are H or C1-4 alkyl; R.sup.3 is (i) CON(R.sup.7)(R.sup.8), (ii) CON(R.sup.9)--CH(R.sup.7)(R.sup.8) or (iii) ##STR2## in which ##STR3## is 4-7 membered, mono-cyclic hetero ring containing 1 or 2 N atom; R.sup.10 is H, C7-10 phenylalkyl or COOR.sup.13 (in which R.sup.13 is H, C1-4 alkyl or C7-10 phenylalkyl)); with the proviso that (i) both R.sup.7 and R.sup.8 do not represent hydrogen at the same time, and (ii) when at least one group in R.sup.7, R.sup.8 and R.sup.9 represents the group containing t-butyl ester, the other groups do not represent tile group containing carboxy; or an acid-addition salt thereof, have inhibitory activities on PLA.sub.2 and on various proteases such as trypsin, plasmin, thrombin, kallikrein, especially trypsin, and are useful for the prevention and/or the treatment of various inflammatory diseases, allergic diseases, disseminated intravascular coagulation, pancreatitis, severity in pancreatitis and multiple organ failure.
摘要翻译：式（I）的脒基苯酚衍生物：其中R 1和R 2是（ⅰ）H，（ⅱ）C 1-4烷基，（ⅲ）C 1-4烷氧基，（ⅳ）C 2-5酰基，（ v）卤素，（vi）NO 2，（vii）苯甲酰基，（viii）COOR 4（其中R 4是C 1-3烷基）; A是键，C1-4亚烷基，-C（R5）= C（R6） - （其中R5和R6是H或C1-4烷基; R3是（i）CON（R7）（R8） CON（R9）-CH（R7）（R8）或（iii）其中IMAGE是含有1或2个N原子的4-7元单环杂环; R10是H，C7-10苯基烷基或COOR13（其中R13为H，C1-4烷基或C7-10苯基烷基））; 条件是（i）R7和R8不同时代表氢，和（ii）当R7，R8和R9中的至少一个基团代表含有叔丁基的基团时，其它基团不表示含羧基的瓷砖组; 或其酸加成盐对PLA2和各种蛋白酶如胰蛋白酶，纤溶酶，凝血酶，激肽释放酶，特别是胰蛋白酶具有抑制活性，可用于预防和/或治疗各种炎性疾病，过敏性疾病，传播性疾病血管内凝血，胰腺炎，胰腺炎和多器官功能衰竭的严重程度。

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