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1. 发明授权

US06632831B2 Branched chain amino acid-dependent aminotransferase inhibitors and their use in the treatment of neurodegenerative diseases 失效
标题翻译：支链氨基酸依赖性氨基转移酶抑制剂及其在治疗神经退行性疾病中的应用
公开(公告)号：US06632831B2
公开(公告)日：2003-10-14
申请号：US10305094
申请日：2002-11-26
申请人： Sheryl Jeanne Hays , Lain-Yen Hu , Huangshu Lei , Jeffrey David Scholten , David Juergen Wustrow
发明人： Sheryl Jeanne Hays , Lain-Yen Hu , Huangshu Lei , Jeffrey David Scholten , David Juergen Wustrow
IPC分类号： C07D27734
CPC分类号： C07D277/20 , C07D417/06 , C07D417/12
摘要： The invention relates to BCAT inhibitors and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, neuropathic pain, Parkinson's disease, diabetic retinopathy, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.
摘要翻译：本发明涉及BCAT抑制剂及其用于治疗或预防与中风，缺血，CNS创伤，低血糖和手术相关的神经元损失以及治疗包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病和唐氏综合征的神经变性疾病的治疗或治疗或预防兴奋性氨基酸过度刺激的不良后果，治疗焦虑症，精神病，抽搐，氨基糖苷类抗生素诱发的听力损失，偏头痛，慢性疼痛，神经性疼痛，帕金森病，糖尿病性视网膜病变，青光眼，CMV视网膜炎，尿失禁，阿片类药物耐受或戒断，诱导麻醉以及增强认知功能

2. 发明授权

US06768008B2 Materials and methods for the treatment of diabetes, hyperlipidemia, hypercholesterolemia, and atherosclerosis 失效
标题翻译：用于治疗糖尿病，高脂血症，高胆固醇血症和动脉粥样硬化的材料和方法
公开(公告)号：US06768008B2
公开(公告)日：2004-07-27
申请号：US09961542
申请日：2001-09-21
申请人： Pascal Druzgala , Peter G. Milner , Jurg R. Pfister
发明人： Pascal Druzgala , Peter G. Milner , Jurg R. Pfister
IPC分类号： C07D27734
CPC分类号： C07D277/20 , C07D261/12 , C07D277/34 , C07D311/70 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07J3/00 , Y10S514/866
摘要： The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.
摘要翻译：本发明提供了可用于治疗II型糖尿病的药物化合物。这些化合物是有利的，因为它们容易被代谢药物解毒系统代谢。特别地，提供了被设计为在化合物的结构内包含酯的噻唑烷二酮类似物。本发明还涉及治疗疾病如糖尿病的方法，其包括施用包含化合物的治疗有效组合物，所述化合物被设计为由血清或细胞内水解酶和酯酶代谢。还教导了含酯的噻唑烷二酮类似物的药物组合物。

3. 发明授权

US06437143B1 Thiazolidone-2 derivatives, 4-diketone substituted, method for obtaining them and pharmaceutical compositions containing same 有权
公开(公告)号：US06437143B1
公开(公告)日：2002-08-20
申请号：US09202076
申请日：1998-12-07
申请人： Gérard Moinet , Gérard Botton , Etienne Prugnard , Liliane Doare , Micheline Kergoat , Didier Mesangeau
发明人： Gérard Moinet , Gérard Botton , Etienne Prugnard , Liliane Doare , Micheline Kergoat , Didier Mesangeau
IPC分类号： C07D27734
摘要： The present invention relates to the field of chemistry and more particularly to that of therapeutic chemistry. The subject of the present invention is more precisely new 5-phenoxyalkyl-2,4-thiazolidinediones of general formula I: in which A represents a linear or branched alkylene group comprising from 2 to 16 carbon atoms D represents a homo- or heterocarbon mono-, di- or tricyclic aromatic structure which may include one or more heteroatoms X represents the substituent of the aromatic structure and is as defined in Claim 1 n is an integer ranging from 1 to 3 with the proviso that if A represents a butyl radical, does not represent the 4-chlorophenyl group. The invention also relates to the tautomeric forms, to the enantiomers, diastereoisomers and epimers of the compounds of general formula I, in free or salified form. The present invention also relates to the processes for producing the compounds of general formula I, their use as antidiabetic agents, and in the treatment of the metabolic syndrome of insulin resistance, as well as the pharmaceutical compositions which contain the compounds of general formula I.

4. 发明授权

US06515003B1 Heterocyclic derivatives for the treatment of diabetes and other diseases 失效
标题翻译：用于治疗糖尿病等疾病的杂环衍生物
公开(公告)号：US06515003B1
公开(公告)日：2003-02-04
申请号：US09652810
申请日：2000-08-31
申请人： Magnus Pfahl , Catherine Tachdjian , Hussien A. Al-Shamma , Andrea Fanjul , David P. M. Pleynet , Lyle W. Spruce
发明人： Magnus Pfahl , Catherine Tachdjian , Hussien A. Al-Shamma , Andrea Fanjul , David P. M. Pleynet , Lyle W. Spruce
IPC分类号： C07D27734
CPC分类号： C07D277/20 , C07D233/40 , C07D233/42 , C07D233/72 , C07D233/84 , C07D233/86 , C07D233/96 , C07D261/12 , C07D277/34 , C07D277/36 , C07D401/06 , C07D401/10 , C07D403/10 , C07D405/10 , C07D417/06 , C07D417/10
摘要： The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease.
摘要翻译：本发明涉及某些可用于治疗与脂质和碳水化合物代谢有关的疾病的取代的式（I）的杂环，例如2型糖尿病，脂肪细胞分化，不受控制的增殖，例如淋巴瘤，霍奇金病，白血病，乳腺癌一般癌症，前列腺癌或癌症; 和炎症，例如骨关节炎，类风湿性关节炎，克罗恩病或炎症性肠病。

5. 发明授权

US06358983B1 Heterocyclically substituted &agr;-hydroxycarboxylic acid derivatives, method for producing the same and their use as endothelin receptor antagonists 失效
标题翻译：杂环取代的α-羟基羧酸衍生物，其制备方法及其作为内皮素受体拮抗剂的用途
公开(公告)号：US06358983B1
公开(公告)日：2002-03-19
申请号：US09530382
申请日：2000-04-27
申请人： Wilhelm Amberg , Rolf Jansen , Heinz Hillen , Stefan Hergenröder , Manfred Raschack , Liliane Unger
发明人： Wilhelm Amberg , Rolf Jansen , Heinz Hillen , Stefan Hergenröder , Manfred Raschack , Liliane Unger
IPC分类号： C07D27734
CPC分类号： C07D275/03 , C07D261/12 , C07D263/38 , C07D277/34 , C07D277/60 , C07D277/68
摘要： The present invention relates to carboxylic acid derivatives of the formula I the substituents having the meanings explained in the description, preparation and use as endothelin receptor antagonists.
摘要翻译：本发明涉及下式的羧酸衍生物，其具有在作为内皮素受体拮抗剂的描述，制备和用途中解释的含义的取代基。

6. 发明授权

US06809101B2 Compounds having anti-hepatitis C virus effect 失效
标题翻译：具有抗丙型肝炎病毒作用的化合物
公开(公告)号：US06809101B2
公开(公告)日：2004-10-26
申请号：US10362368
申请日：2003-02-27
申请人： Toshio Fujishita , Kenji Abe
发明人： Toshio Fujishita , Kenji Abe
IPC分类号： C07D27734
CPC分类号： A61K31/381 , A61K31/365 , A61K31/4162 , A61K31/421 , A61K31/426 , C07D277/34
摘要： It is found out that compounds represented by the formula (I): wherein R1 is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; and R2 and R3 taken together with the adjacent carbon atom form an optionally substituted heterocyclic group having one or more of oxo and/or thioxo; have an HCV RNA-dependent RNA synthase inhibitory effect.

7. 发明授权

US06541493B1 Crystals of 5-[{6-(2-fluorobenzyl)oxy-2-naphthyl}methyl]-2,4-thiazolidinedione 失效
标题翻译： 5 - [{6-（2-氟苄基）氧基-2-萘基}甲基] -2,4-噻唑烷二酮的晶体
公开(公告)号：US06541493B1
公开(公告)日：2003-04-01
申请号：US09856295
申请日：2001-08-20
申请人： Takayuki Oe , Hiroaki Ueno , Akira Maruyama , Katsuhiko Masuda
发明人： Takayuki Oe , Hiroaki Ueno , Akira Maruyama , Katsuhiko Masuda
IPC分类号： C07D27734
CPC分类号： C07D277/34
摘要： The invention relates to type A crystal of 5-[{6-(2-fluorobenzyl)oxy-2-naphthyl}methyl]-2,4-thiazolidinedione characterized to have characteristic absorption peaks (2&thgr;) at 11.5°±0.3°, 14.5°±0.2°, 16.2°±0.3°, 17.0°±0.3°, 17.7°±0.2°, 18.6°±0.3°, 19.1°±0.2°, 21.3°±0.4°, 22.4°±0.5°, 25.7°±0.5° and 28.3°±0.5° in a powder X-ray diffraction pattern, and also to a method for preparation thereof, and a pharmaceutical composition comprising the same. The crystal is excellent in stability, and has advantages in handling, storage, and pharmaceutical preparation. The invention also relates to type B, C and D crystals of said compound.
摘要翻译：本发明涉及5 - [{6-（2-氟苄基）氧基-2-萘基}甲基] -2,4-噻唑烷二酮的A型晶体，其特征在于在11.5°±0.3°，14.5°具有特征吸收峰（2θ） °±0.2°，16.2°±0.3°，17.0°±0.3°，17.7°±0.2°，18.6°±0.3°，19.1°±0.2°，21.3°±0.4°，22.4°±0.5°，25.7°± 粉末X射线衍射图中为0.5°和28.3°±0.5°，以及其制备方法，以及包含该方法的药物组合物。该晶体的稳定性优异，在处理，储存和制药方面具有优势。本发明还涉及所述化合物的B，C和D型晶体。

8. 发明授权

US06288096B1 Thiazolidinedione, oxazolidinedione and oxadiazolidinedione derivatives 失效
标题翻译：噻唑烷二酮，恶唑烷二酮和恶二唑烷二酮衍生物
公开(公告)号：US06288096B1
公开(公告)日：2001-09-11
申请号：US09091875
申请日：1998-06-25
申请人： Kjell Andersson , Maria Boije , Eva-Lotte Lindstedt , Bengt Ljung , Bo Nordén
发明人： Kjell Andersson , Maria Boije , Eva-Lotte Lindstedt , Bengt Ljung , Bo Nordén
IPC分类号： C07D27734
CPC分类号： C07D263/44 , C07D271/07 , C07D277/34
摘要： Novel thiazolidinedione, oxazolidinedione and oxadiazolidinedione derivatives, process for their manufacture, pharmaceutical preparations containing them and the use of the compounds in conditions associated with insulin resistance.
摘要翻译：新的噻唑烷二酮，恶唑烷二酮和恶二唑烷二酮衍生物，其制备方法，含有它们的药物制剂以及该化合物在与胰岛素抵抗相关的条件下的用途。

9. 发明授权

US06818776B2 Alkali metal salt of thiazolidine-2,4-dione derivative 失效
标题翻译：噻唑烷-2,4-二酮衍生物的碱金属盐
公开(公告)号：US06818776B2
公开(公告)日：2004-11-16
申请号：US10181432
申请日：2002-07-25
申请人： Michiro Ohnota , Kazuo Orita , Noriyuki Yoshida
发明人： Michiro Ohnota , Kazuo Orita , Noriyuki Yoshida
IPC分类号： C07D27734
CPC分类号： C07D277/34
摘要： The invention provides alkali metal salt of 5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-methoxy-N-[[4-(trifluoromethyl)phenyl]methyl]benzamide and its hydrate. A method has been found, wherein, upon preparing KRP-297, the alkali metal salt of KRP-297 and its hydrate are formed in the reaction system and, after separation and purification, they are freed again from salt, thereby KRP-297 can be advantageously purified industrially for preparation.
摘要翻译：本发明提供5 - [（2,4-二氧代噻唑烷-5-基）甲基] -2-甲氧基-N - [[4-（三氟甲基）苯基]甲基]苯甲酰胺及其水合物的碱金属盐。已经发现了一种方法，其中在制备KRP-297时，在反应体系中形成KRP-297的碱金属盐及其水合物，分离和纯化后再次从盐中释放出来，从而KRP-297可以有利地在工业上纯化用于制备。

10. 发明授权

US06620830B2 Thyroid receptor ligands 失效
标题翻译：甲状腺受体配体
公开(公告)号：US06620830B2
公开(公告)日：2003-09-16
申请号：US09836765
申请日：2001-04-17
申请人： Yuan-Ching P. Chiang
发明人： Yuan-Ching P. Chiang
IPC分类号： C07D27734
CPC分类号： C07D271/07 , C07D249/12 , C07D277/20 , C07D277/34
摘要： The invention provides thiazolidinedione, oxadiazolidinedione, and triazolone compounds of Formula (I) which compounds are thyroid receptor ligands. The invention further provides pharmaceutical compositions and kits comprising such compounds and methods of treating obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer, diabetes, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesterolemia, depression, and osteoporosis using such compounds.
摘要翻译：本发明提供了式（I）的噻唑烷二酮，恶二唑烷二酮和三唑酮化合物，其化合物是甲状腺受体配体。本发明还提供包含这些化合物的药物组合物和试剂盒，以及治疗肥胖，超重状况，高脂血症，青光眼，心律失常，皮肤疾病，甲状腺疾病，甲状腺功能减退，甲状腺癌，糖尿病，动脉粥样硬化，高血压，冠心病，充血性心力衰竭，高胆固醇血症，抑郁症和使用这些化合物的骨质疏松症。

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