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1. 发明授权

US06251926B1 Oxyiminoalkanoic acid derivatives with hypoglycemic and hypolipidemic activity 失效
标题翻译：具有低血糖和降血脂活性的氧亚氨基链烷酸衍生物
公开(公告)号：US06251926B1
公开(公告)日：2001-06-26
申请号：US09423854
申请日：1999-11-15
申请人： Yu Momose , Hiroyuki Odaka , Hiroshi Imoto , Hiroyuki Kimura , Junichi Sakamoto
发明人： Yu Momose , Hiroyuki Odaka , Hiroshi Imoto , Hiroyuki Kimura , Junichi Sakamoto
IPC分类号： A61K314245
CPC分类号： C07D213/74 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/426 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/47 , A61K31/4745 , A61K31/505 , C07D215/14 , C07D239/42 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/24 , C07D413/12 , C07D471/04
摘要： This invention provides a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance and impaired glucose tolerance.
摘要翻译：本发明提供一种具有优异的降血糖和降血脂作用的新型氧亚氨基链烷酸衍生物，其用于治疗糖尿病，高脂血症，胰岛素不敏感，胰岛素抵抗和葡萄糖耐量异常。

2. 发明授权

US06716861B2 3-ox(adi)azolylpropanohydroxamic acids useful as procollagen C-proteinase inhibitors 失效
标题翻译：可用作原胶原C-蛋白酶抑制剂的3-氧（adi）唑基丙酰异羟肟酸
公开(公告)号：US06716861B2
公开(公告)日：2004-04-06
申请号：US10021721
申请日：2001-12-12
申请人： Usa Datta , Paul Vincent Fish , Kim James , Gavin Alistair Whitlock
发明人： Usa Datta , Paul Vincent Fish , Kim James , Gavin Alistair Whitlock
IPC分类号： A61K314245
CPC分类号： C07D263/16 , A61K31/421 , A61K31/422 , A61K31/4245 , C07C235/74 , C07C259/14 , C07C311/06 , C07C2601/14 , C07D205/04 , C07D211/60 , C07D211/96 , C07D231/12 , C07D233/56 , C07D249/08 , C07D263/32 , C07D263/34 , C07D271/06 , C07D271/07 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/06
摘要： Compounds of formula (I): wherein the substituents are as defined herein, and their salt, solvates, and prodrugs are procollagen C-proteinase (PCP) inhibitors useful in treating conditions mediated by PCP.
摘要翻译：式（I）化合物：其中取代基如本文所定义，其盐，溶剂合物和前药是用于治疗由PCP介导的病症的前胶原C-蛋白酶（PCP）抑制剂。

3. 发明授权

US06277873B1 Oxadiazole antifungal agents 失效
标题翻译：恶二唑抗真菌剂
公开(公告)号：US06277873B1
公开(公告)日：2001-08-21
申请号：US09729901
申请日：2000-12-05
申请人： Dingwei Tim Yu , Orest Taras Macina , Ila Sircar , Jagadish Chandra Sircar , Christopher Mark Riviello
发明人： Dingwei Tim Yu , Orest Taras Macina , Ila Sircar , Jagadish Chandra Sircar , Christopher Mark Riviello
IPC分类号： A61K314245
CPC分类号： C07D277/28
摘要： Disclosed is a novel class of thiazole, thiadiazole, and oxadiazole compounds which are substituted at their nuclear carbons by aromatic moieties. These compounds exhibit antifungal activity against a variety of fungi including strains which have proven to be resistant to treatment with known antifungal agents such as Fluconazole.
摘要翻译：公开了一类新的噻唑，噻二唑和恶二唑化合物，它们在其核碳上被芳族部分取代。这些化合物对各种真菌表现出抗真菌活性，包括已被证明对已知的抗真菌剂例如氟康唑的治疗具有抗性的菌株。

4. 发明授权

US06720343B2 Oxadiazole derivatives having anticancer effects 失效
标题翻译：具有抗癌作用的恶二唑衍生物
公开(公告)号：US06720343B2
公开(公告)日：2004-04-13
申请号：US10257917
申请日：2002-10-18
申请人： Takayuki Yoshioka , Ryuji Maekawa , Fumihiko Watanabe
发明人： Takayuki Yoshioka , Ryuji Maekawa , Fumihiko Watanabe
IPC分类号： A61K314245
CPC分类号： C07D271/06 , A61K31/4245 , A61K31/4439 , C07D409/04 , C07D413/04
摘要： A pharmaceutical composition for treating or preventing cancer containing a compound of the general formula (I), a prodrug, a pharmaceutically acceptable salt, or a solvate thereof as an active ingredient: wherein R1 is hydroxy or the like; R2 is optionally substituted lower alkyl or the like; R3 is hydrogen or the like; R4 is optionally substituted arylene or the like; R5 is optionally substituted aryl or the like.
摘要翻译：一种用于治疗或预防癌症的药物组合物，其含有通式（I）化合物，其前药，药学上可接受的盐或溶剂化物作为活性成分：其中R 1是羟基等; R 2是任选取代的低级烷基等; R 3是氢等; R 4是任选取代的亚芳基等; R 5是任选取代的芳基等。

5. 发明授权

US06436974B1 Amino heterocycles useful as pharmaceutical agents 失效
标题翻译：用作药剂的氨基杂环
公开(公告)号：US06436974B1
公开(公告)日：2002-08-20
申请号：US09980187
申请日：2001-11-30
申请人： Thomas Richard Belliotti , Andrew John Thorpe , David Juergen Wustrow
发明人： Thomas Richard Belliotti , Andrew John Thorpe , David Juergen Wustrow
IPC分类号： A61K314245
CPC分类号： C07D403/04 , C07D413/04
摘要： The instant invention is a novel series of amino heterocycles useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, and sleep disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.
摘要翻译：本发明是用于治疗癫痫，微弱发作，运动功能减退，颅内障碍，神经变性障碍，抑郁，焦虑，恐慌，疼痛，神经病理学障碍和睡眠障碍的新型氨基杂环。还公开了用于制备的方法和可用于制备的中间体。

6. 发明授权

US06326388B1 Substituted 1,3,4-oxadiazoles and a method of reducing TNF-alpha level 有权
标题翻译：取代的1,3,4-恶二唑和降低TNF-α水平的方法
公开(公告)号：US06326388B1
公开(公告)日：2001-12-04
申请号：US09470203
申请日：1999-12-21
申请人： Hon-Wah Man , George W. Muller
发明人： Hon-Wah Man , George W. Muller
IPC分类号： A61K314245
CPC分类号： C07D413/06 , C07D471/04
摘要： Substituted 1,3,4-oxadiazole compounds reduce the levels of TNF&agr; in a mammal. Typical embodiments are 2-[1-(3-cyclopentyloxy-4-methoxyphenyl)-2-(1,3,4-oxadiazol-2-yl)ethyl]-5-methylisoindoline-1,3-dione and 2-[1-(3-ethoxy-4-methoxyphenyl)-2-(1,3,4-oxadiazol-2-yl)ethyl]isoindoline-1,3-dione.
摘要翻译：取代的1,3,4-恶二唑化合物降低哺乳动物TNFalpha的水平。典型的实施方案是2- [1-（3-环戊氧基-4-甲氧基苯基）-2-（1,3,4-恶二唑-2-基）乙基] -5-甲基异吲哚啉-1,3-二酮和2- [1 - （3-乙氧基-4-甲氧基苯基）-2-（1,3,4-恶二唑-2-基）乙基]异二氢吲哚-1,3-二酮。

7. 发明授权

US06297241B1 Carbamate derivatives of diaryl 1,3,4-oxadiazolone 有权
标题翻译：二芳基1,3,4-恶二唑酮的氨基甲酸酯衍生物
公开(公告)号：US06297241B1
公开(公告)日：2001-10-02
申请号：US09707207
申请日：2000-11-06
申请人： Piyasena Hewawasam , Xi Chen , John E. Starrett
发明人： Piyasena Hewawasam , Xi Chen , John E. Starrett
IPC分类号： A61K314245
CPC分类号： C07D271/113
摘要： The present invention provides novel carbamate oxadiazolone derivatives having the general formula wherein R1 and R2 are as defined herein, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of the large conductance calcium-activated potassium channels.
摘要翻译：本发明提供新的具有通式R 1和R 2如本文所定义的氨基甲酸酯恶二唑衍生物或其无毒的药学上可接受的盐或溶剂合物，并且可用于治疗对大电导钙激活的开放有反应的病症钾通道。

8. 发明授权

US06211211B1 Benzopyrans and their use as therapeutic agents 失效
标题翻译：苯并吡喃及其作为治疗剂的用途
公开(公告)号：US06211211B1
公开(公告)日：2001-04-03
申请号：US09056554
申请日：1998-04-07
申请人： Wai Ngor Chan , Mervyn Thompson , John Morris Evans
发明人： Wai Ngor Chan , Mervyn Thompson , John Morris Evans
IPC分类号： A61K314245
CPC分类号： C07D413/12 , C07C233/76 , C07D311/68
摘要： This invention relates to substituted benzopyran amides useful in treating certain medical conditions and to processes for preparing these compounds.
摘要翻译：本发明涉及可用于治疗某些医学病症的取代的苯并吡喃酰胺和制备这些化合物的方法。

9. 发明授权

US06797720B2 1,3,4-oxadiazoline derivative and an agent comprising its derivative as active ingredient 失效
标题翻译： 1,3,4-恶二唑啉衍生物和包含其衍生物作为活性成分的试剂
公开(公告)号：US06797720B2
公开(公告)日：2004-09-28
申请号：US10148613
申请日：2002-08-28
申请人： Kazuyuki Ohmoto , Iori Itagaki
发明人： Kazuyuki Ohmoto , Iori Itagaki
IPC分类号： A61K314245
CPC分类号： C07D271/113 , A61K38/00 , C07D271/12 , C07D413/12 , C07D417/12 , C07D493/08 , C07K5/06139
摘要： A 1,3,4-oxadiazoline derivative of formula (I) wherein W is oxygen, sulfer; R is hydrogen, alkyl, CycA, etc.; AA1 is a single bond, amino acid residue, etc.; AA2 is a single bond, amino acid residue, etc.; R7 and R8 are hydrogen, alkyl, etc.; R9 is hydrogen, alkyl, etc., and a non-toxic salt thereof. The compound of formula (I) has an inhibitory activity against cysteine protease and therefore it is useful as an agent for the prophylaxis and/or treatment of inflammatory diseases, diseases induced by apoptosis, diseases induced by disorders of immune responses, autoimmune diseases, diseases induced by decomposition of proteins which compose organism, shock, circulatory system disorders, blood coagulation systems disorders, malignant tumors, acquired immune deficiency syndrome (AIDS) and AIDS-related complex (ARC), parasitic diseases, nerve degeneration diseases, pulmonary disorders, bone resorption diseases, endocrinesthenia, etc.
摘要翻译：式（I）的1,3,4-恶二唑啉衍生物，其中W是氧，硫醇; R是氢，烷基，CycA等; AA <1>是单键，氨基酸残基等; AA <2>是单键，氨基酸残基等; R 7和R 8是氢，烷基等; R 9是氢，烷基等，及其无毒盐。式（I）化合物对半胱氨酸蛋白酶具有抑制活性，因此可用作预防和/或治疗炎症性疾病，由细胞凋亡引起的疾病，由免疫应答障碍引起的疾病，自身免疫性疾病，由构成生物体的蛋白质分解引起的疾病，休克，循环系统疾病，凝血系统疾病，恶性肿瘤，获得性免疫缺陷综合征（AIDS）和艾滋病相关综合征（ARC），寄生虫病，神经变性疾病，肺功能障碍，骨吸收疾病，内分泌感染等。

10. 发明授权

US06596742B1 Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones, their preparation and their use in medicaments 有权
标题翻译：取代的3-苯基-5-烷氧基-1,3,4-恶二唑-2-酮，它们的制备及其在药物中的用途
公开(公告)号：US06596742B1
公开(公告)日：2003-07-22
申请号：US09655373
申请日：2000-09-05
申请人： Stefan Petry , Karl Schoenafinger , Guenter Mueller , Karl-Heinz Baringhaus
发明人： Stefan Petry , Karl Schoenafinger , Guenter Mueller , Karl-Heinz Baringhaus
IPC分类号： A61K314245
CPC分类号： C07D271/113
摘要： Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones of the formula 1 in any optically isomeric form, and their physiologically acceptable salts, where R1 is C1-C6-alkyl, C3-C9-cycloalkyl, both of which may be unsubstituted or substituted, and R2 and R3 independently of one another are hydrogen, C6-C10-aryl, C3-C8-cycloalkyl, C6-C10-aryloxymethyl, O-benzyl, O—C6-C10-aryl, O—C3-C8-cycloalkyl, O—C1-C6-alkyl, SO2—NH—C1-C6-alkyl, SO2—NH-(2,2,6,6-tetramethylpiperidin-4-yl), SO2—NH—C3-C8-cycloalkyl, SO2—N(C1-C6-alkyl)2 or COX, where X is O—C1-C6-alkyl, NH—C1-C6-alkyl, NH—C3-C8-cycloalkyl or N(C1-C6-alkyl)2, with the proviso that the substitutents R2 and R3 may in some instances be unsubstituted or substituted and are not both simultaneously hydrogen. A process for their preparation, and their inhibitory effect on the hormone-sensitive lipase, HSL.
摘要翻译：以任何光学异构体形式的取代的3-苯基-5-烷氧基-1,3,4-恶二唑-2-酮及其生理上可接受的盐，其中R 1是C 1 -C 6 - 烷基，C 3 -C 9 - 环烷基，两者可以是未取代的或取代的，R 2和R 3彼此独立地是氢，C 6 -C 10 - 芳基，C 3 -C 8 - 环烷基，C 6 -C 10 - 芳氧基甲基，O-苄基，O-C 6 -C 10 - 芳基， O-C 3 -C 8 - 环烷基，O-C 1 -C 6烷基，SO 2 -NH-C 1 -C 6烷基，SO 2 -NH-（2,2,6,6-四甲基哌啶-4-基），SO 2 -NH- C 3 -C 8 - 环烷基，SO 2 -N（C 1 -C 6 - 烷基）2或COX，其中X是O-C 1 -C 6烷基，NH-C 1 -C 6烷基，NH-C 3 -C 8环烷基或N -C 1-6 - 烷基）2，条件是取代基R2和R3在一些情况下可以是未取代的或取代的，并且不同时是氢。其制备方法及其对激素敏感性脂肪酶HSL的抑制作用。

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