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1. 发明授权

US06673820B2 Aminoheterocyclylamides as pesticides and antiparasitic agents 失效
标题翻译：氨基杂环酰胺作为农药和抗寄生虫剂
公开(公告)号：US06673820B2
公开(公告)日：2004-01-06
申请号：US10148644
申请日：2002-05-31
申请人： Pierre Ducray , Jacques Bouvier , Maurizio Schwarzenbach
发明人： Pierre Ducray , Jacques Bouvier , Maurizio Schwarzenbach
IPC分类号： C07D41712
CPC分类号： C07D275/03 , C07D277/46 , C07D285/08 , C07D333/36 , C07D409/12 , C07D417/12
摘要： The invention relates to novel compounds of the general formula: in which R1 is hydrogen, halogen, C1-C6alkyl, C1-C6alkoxy, C1-C6haloalkyl or unsubstituted or mono- to pentasubstituted phenyl, where the substituents are selected from the group consisting of C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, aryloxy, halogen, cyano and nitro, where, if the number of substituents exceeds 1, the substituents can be identical or different; R2 is hydrogen, C1-C6alkyl, (C1-C6alkylene)phenyl, pyridyl, COOR6, CONR7R8, COR6, allyl or CH2—O—R6; R3 is unsubstituted or substituted heterocyclyl, where the substituents are in each case selected from the group consisting of unsubstituted or substituted phenyl, where the substituents are selected from the group consisting of C1-C6alkyl, C1-C6alkoxy, halogen, cyano and nitro, where, if the number of substituents exceeds 1, the substituents can be identical or different, benzyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, aryloxy, halogen, cyano, hydroxyl, amino and nitro, where, if the number of substituents exceeds 1, the substituents can be identical or different; R6 is C1-C6alkyl, phenyl or benzyl; R7 and R8 independently of one another are hydrogen or C1-C6alkyl; X1 and X2 are each N; and X3 is O or S. The novel compounds have advantageous pesticidal properties and are particularly suitable for controlling pests in domestic and useful animals.
摘要翻译：本发明涉及以下通式的新化合物：其中R 1是氢，卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6卤代烷基或未被取代的或一至五取代的苯基，其中取代基选自C1 C 1-6烷基，C 1 -C 6卤代烷基，C 1 -C 6烷氧基，芳氧基，卤素，氰基和硝基，其中如果取代数超过1，则取代基可以相同或不同; R2是氢，C1-C6烷基，（C1-C6亚烷基）苯基，吡啶基，COOR6，CONR7R8，COR6，烯丙基或CH2-O-R6; R3是未取代或取代的杂环基，其中取代基各自选自未取代或取代的苯基，其中取代基选自C 1 -C 6烷基，C 1 -C 6烷氧基，卤素，氰基和硝基，其中如果取代基数目超过1，则取代基可以相同或不同，苄基，C1-C6烷基，C1-C6卤代烷基，C1-C6烷氧基，芳氧基，卤素，氰基，羟基，氨基和硝基，其中如果取代基数目超过1，取代基可以相同或不同; R6是C1-C6烷基，苯基或苄基; R 7和R 8彼此独立地是氢或C 1 -C 6烷基; X1和X2分别为N; X3是O或S.新化合物具有有利的杀虫特性，特别适用于控制家畜和有用动物的害虫。

2. 发明授权

US06562849B1 Amine derivative compounds 失效
标题翻译：胺衍生物
公开(公告)号：US06562849B1
公开(公告)日：2003-05-13
申请号：US09971634
申请日：2001-10-05
申请人： Takashi Fujita , Kunio Wada , Minoru Oguchi , Hidehito Honma , Toshihiko Fujiwara
发明人： Takashi Fujita , Kunio Wada , Minoru Oguchi , Hidehito Honma , Toshihiko Fujiwara
IPC分类号： C07D41712
CPC分类号： C07D413/12 , A61K31/427 , C07D417/12 , C07D471/04
摘要： An amine compound of the formula (I): wherein R1 represents an optionally substituted carbamoyl group, etc., R2 represents a hydrogen atom, etc., R3 represents a C1-C10 alkyl group etc., W1, W2 and W3 are the same or different and each represent a single bond or a C1-C8 alkylene group, X, Y and Q represent a sulfur atom, etc., Z represents a ═CH— group, etc., Ar represents a benzene ring, etc. and L represents a hydrogen atom, etc., or a pharmacologically acceptable salt thereof. These compounds are useful in the treatment and/or prophylaxis of diseases such as diabetes, hyperlipemia, arteriosclerosis, cancer, etc.
摘要翻译：式（I）的胺化合物：其中R 1表示任选取代的氨基甲酰基等，R 2表示氢原子等，R 3表示C 1 -C 10烷基等，W 1，W 2和W 3相同或不同，各自表示单键或C1-C8亚烷基，X，Y和Q表示硫原子等，Z表示= CH-基等，Ar表示苯环等，L表示表示氢原子等，或其药理学上可接受的盐。这些化合物可用于治疗和/或预防疾病如糖尿病，高脂血症，动脉硬化，癌症等。

3. 发明授权

US06365748B1 Method for preparing lintitript potassium salt 失效
标题翻译：制备枸橼酸钾盐的方法
公开(公告)号：US06365748B1
公开(公告)日：2002-04-02
申请号：US09744000
申请日：2001-01-18
申请人： Joël Radisson
发明人： Joël Radisson
IPC分类号： C07D41712
CPC分类号： C07D417/12
摘要： A method for preparing the potassium dihydrate salt of 2-[[4-(2-chlorophenyl)-2-thiazolyl]carbamoyl]indole-1-acetic acid, by reacting 2-[[4-(2-chlorophenyl)-2-thiazolyl]carbamoyl]indole-1-acetic acid or its C1-C4 alkyl esters with potassium carbonate in a two phase solvent system comprising a mixture of water and an organic solvent which is only slightly miscible with water and optionally recrystallising the precipitated intermediate solvate from water and to the potassium dihydrate salt thus obtained.
摘要翻译： 2 - [[4-（2-氯苯基）-2-噻唑基]氨基甲酰基]吲哚-1-乙酸二水合盐酸盐的制备方法，噻唑基]氨基甲酰基]吲哚-1-乙酸或其C1-C4烷基酯与碳酸钾在两相溶剂体系中的混合物，其包含水和仅与水轻微混溶的有机溶剂的混合物，并任选地将沉淀的中间体溶剂化物从水和由此获得的二水合二水合盐。

4. 发明授权

US06730670B2 7-phenyl-benzo[b]thiophen amide derivatives 失效
标题翻译： 7-苯基 - 苯并[b]噻吩酰胺衍生物
公开(公告)号：US06730670B2
公开(公告)日：2004-05-04
申请号：US10315821
申请日：2002-12-10
申请人： Alexander Alanine , Alexander Flohr
发明人： Alexander Alanine , Alexander Flohr
IPC分类号： C07D41712
CPC分类号： C07D409/12 , C07D333/66
摘要： A compound of the formula Compounds of formula I have a good affinity to the A2A receptor and are useful for the treatment of diseases mediated by this receptor.
摘要翻译：式I化合物式I化合物对A2A受体具有良好的亲和力，可用于治疗由该受体介导的疾病。

5. 发明授权

US06664278B2 Hydrate of 5-[4-[2-(N-methyl-N-(2-pyridil)amino)ethoxy]benzyl]thiazolidine-2,4-dione maleic acid salt 失效
公开(公告)号：US06664278B2
公开(公告)日：2003-12-16
申请号：US10072096
申请日：2002-02-07
申请人： Michael John Sasse , Paul David James Blackler , David C. Lee
发明人： Michael John Sasse , Paul David James Blackler , David C. Lee
IPC分类号： C07D41712
CPC分类号： C07D417/12
摘要： The present invention provides a novel hydrate of 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione, maleic acid.

6. 发明授权

US06469167B1 Process for the preparation of thiazolidine-2,4-dione derivatives 有权
标题翻译：噻唑烷-2,4-二酮衍生物的制备方法
公开(公告)号：US06469167B1
公开(公告)日：2002-10-22
申请号：US09763940
申请日：2001-05-02
申请人： Prabhakar Chebiyyam , Rajender Kumar Potlapally , Chinna Bakki Reddy Gade , Balaram Mahanti Satish , Ramabhadra Sarma Mamillapalli , Om Reddy Gaddam
发明人： Prabhakar Chebiyyam , Rajender Kumar Potlapally , Chinna Bakki Reddy Gade , Balaram Mahanti Satish , Ramabhadra Sarma Mamillapalli , Om Reddy Gaddam
IPC分类号： C07D41712
CPC分类号： C07D417/12 , C07D277/24
摘要： An improved process for the preparation of 5-[4-[[3-Methyl-4-oxo-3,4-dihydroquinazolin-2-yl]methoxy]benzyl]thiazolidine-2,4-dione of formula (1) which comprises: reducing the compound of formula (2′) where R represents a (C1-C4)alkyl group using Raney Nickel or Magnesium in alcohol having 1 to 4 carbon atoms or mixtures thereof, if desired reesterifying using sufphuric acid at a temperature in the range of 0° C. to 60° C. to obtain a compound of formula (3′) wherein R is as defined above, hydrolyzing the compound of formula (3′) wherein R is as defined above, by conventional methods to obtain the acid of formula (4), condensing the acid of formula (4) with N-methyl anthranilamide directly without any preactivation of the acid to produce the compound of formula (1) and if desired, converting the compound of formula (1) to pharmaceutically acceptable salts thereof by conventional methods.
摘要翻译：制备式（1）的5- [4 - [[3-甲基-4-氧代-3,4-二氢喹唑啉-2-基]甲氧基]苄基]噻唑烷-2,4-二酮的改进方法，其包括：使用阮内镍或镁在具有1至4个碳原子的醇或其混合物中还原其中R表示（C 1 -C 4）烷基的式（2'）化合物，如果需要，使用磺菲酸在范围内的温度下再酯交换通过常规方法获得式（3'）化合物，其中R如上定义，通过常规方法水解其中R如上所定义的式（3'）化合物以获得酸直接将式（4）的酸与N-甲基邻氨基苯甲酰胺缩合而无需任何预活化的酸，以产生式（1）化合物，如果需要，将式（1）的化合物转化为药学上可接受的其盐通过常规方法。

7. 发明授权

US06353011B1 1,2-dithiolane derivatives 失效
标题翻译： 1,2-二硫戊环衍生物
公开(公告)号：US06353011B1
公开(公告)日：2002-03-05
申请号：US09520208
申请日：2000-03-07
申请人： Harrihar A. Pershadsingh , Mitchell A. Avery
发明人： Harrihar A. Pershadsingh , Mitchell A. Avery
IPC分类号： C07D41712
CPC分类号： C07D417/12 , C07C323/12 , C07C323/62 , C07D277/34
摘要： This invention provides new thiazolindinedione derivatives and new arylacetic acid derivatives. These compounds are useful for the treatment of cardiovascular diseases, certain endocrine diseases, certain inflammatory diseases, certain neoplastic (malignant) and non-malignant proliferative diseases, certain neuro-psychiatric disorders, certain viral diseases, and diseases associated with these viral infections as discussed herein.
摘要翻译：本发明提供了新的噻唑啉二酮衍生物和新的芳基乙酸衍生物。这些化合物可用于治疗心血管疾病，某些内分泌疾病，某些炎性疾病，某些肿瘤（恶性）和非恶性增殖性疾病，某些神经精神疾病，某些病毒性疾病以及与这些病毒感染有关的疾病这里。

8. 发明授权

US06184385B2 Process for the manufacture of a sulfenimide 有权
标题翻译：制备亚硫酰亚胺的方法
公开(公告)号：US06184385B2
公开(公告)日：2001-02-06
申请号：US09292682
申请日：1999-04-16
申请人： Jayant S. Lodaya , Donald L. Fields, Jr. , Raymond T. Parker , Phillip B. Balderson
发明人： Jayant S. Lodaya , Donald L. Fields, Jr. , Raymond T. Parker , Phillip B. Balderson
IPC分类号： C07D41712
CPC分类号： C07D277/80
摘要： A process for the manufacture of a sulfenimide by reacting sulfenamide in slurry with a water immiscible organic solvent with an acid to yield a solvent slurry comprising sulfenimide product. The product is recovered from the solvent slurry by a method comprising the addition of water to the solvent slurry and the isolating of the product by a single filtration step. While water is added to the solvent slurry an azeotrope of solvent and water may be distilled under vacuum until substantially all solvent is separated from product and product becomes part of an aqueous slurry. Alternatively, water may be added to the solvent slurry while the resulting mixture is being agitated, followed by filtering the mixture in the single filtration step for recovery of product from the mixture.
摘要翻译：通过使浆料中的次磺酰胺与与水不混溶的有机溶剂与酸反应制备亚磺酰亚胺的方法，以产生包含亚硫酰亚胺产物的溶剂浆料。通过包括向溶剂浆料中加入水并通过单一过滤步骤分离产物的方法从溶剂浆料中回收产物。当将水加入到溶剂浆料中时，溶剂和水的共沸物可以在真空下蒸馏，直到基本上所有溶剂与产物分离，并且产物成为含水浆料的一部分。或者，可以在搅拌所得混合物的同时将水加入到溶剂淤浆中，然后在单过滤步骤中过滤混合物以从混合物中回收产物。

9. 发明授权

US06815457B1 Thiazolidinedione derivative and its use as antidiabetic 失效
标题翻译：噻唑烷二酮衍生物及其用作抗糖尿病药
公开(公告)号：US06815457B1
公开(公告)日：2004-11-09
申请号：US10030323
申请日：2002-05-15
申请人： Paul David James Blackler , Robert Gordon Giles , Michael Sasse
发明人： Paul David James Blackler , Robert Gordon Giles , Michael Sasse
IPC分类号： C07D41712
CPC分类号： C07D417/12
摘要： A polymorphic form of 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]-benzyl]thiazolidine-2,4-dione, maleic acid salt (the “Polymorph”) characterized in that it: (i) provides an infra red spectrum containing peaks at 1360, 1326, 1241, 714 and 669 cm−1; and/or (ii) provides a Raman spectrum containing peaks at 1581, 768, 670, 271 and 226 cm−1; and/or (iii) provides a solid-state nuclear magnetic resonance spectrum containing peaks at chemical shifts substantially as set out in Table I; and/or (iv) provides an X-ray powder diffraction (XRPD) pattern containing peaks substantially as set out in Table II; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of such a compound in medicine.

10. 发明授权

US06613911B2 Process for preparing arylacetylaminothiazoles 有权
标题翻译：制备芳基乙酰氨基噻唑的方法
公开(公告)号：US06613911B2
公开(公告)日：2003-09-02
申请号：US10067723
申请日：2002-02-05
申请人： Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Joseph E. Sundeen , Rulin Zhao
发明人： Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Joseph E. Sundeen , Rulin Zhao
IPC分类号： C07D41712
CPC分类号： C07D417/12 , A61K31/427 , A61K31/454 , C07D231/12 , C07D233/56 , C07D249/08 , C07D417/14
摘要： The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-arylacetylaminothiazole compounds of formula I: or a pharmnaceutically acceptable salt thereof, wherein: R1, R2, R4, R5, R6, R8, R9, R12 and R13 are each independently hydrogen, alkyl, aryl or heteroaryl; R3, R7, R10 and R11 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; and X is CH or N, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention also concerns a new process for the preparation of formylarylacetates and formylarylacetic acids.
摘要翻译：本发明涉及制备式I的5-（2-恶唑基烷硫基）-2-芳基乙酰氨基噻唑化合物的新的，有效的方法：或其药物上可接受的盐，其中：R1，R2，R4，R5，R6，R8， R9，R12和R13各自独立地为氢，烷基，芳基或杂芳基; R3，R7，R10和R11各自独立地为氢，烷基，芳基，杂芳基，卤素，羟基或烷氧基; 而X是CH或N，它们是细胞周期蛋白依赖性激酶（cdks）的新型有效抑制剂。本发明还涉及制备甲酰芳基乙酸酯和甲酰芳基乙酸的新方法。

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