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1. 发明授权

EP1292561B1 PROCESS FOR THE PREPARATION OF CYCLOPROPYL CARBOXYLIC ACID ESTERS AND DERIVATIVES 有权
标题翻译：用于生产CYCLOPROPYLCARBONSÄUREESTERN及其衍生物
公开(公告)号：EP1292561B1
公开(公告)日：2008-02-13
申请号：EP01937110.3
申请日：2001-05-31
申请人： AstraZeneca AB
发明人： CLARK, Adrian , JONES, Elfyn , LARSSON, Ulf , MINIDIS, Anna
IPC分类号： C07C67/347 , C07C69/003 , C07C69/017 , C07C69/743 , C07C69/753 , C07C61/04 , C07C69/96 , C07C233/58
CPC分类号： C07C61/40 , C07B2200/07 , C07C51/09 , C07C51/38 , C07C51/60 , C07C57/60 , C07C57/66 , C07C67/347 , C07C69/753 , C07C211/40 , C07C247/22 , C07C2601/02 , C07C2601/14 , C07D487/04
摘要： The invention relates to a novel process for the preparation of certain cyclopropyl carboxylic acid esters and other cyclopropyl carboxylic acid derivatives; a novel process for the preparation of dimethylsulfoxonium methylide and dimethylsulfonium methylide; to the use of certain cyclopropyl carboxylic acid esters in a process for the preparation of intermediates that can be used in the synthesis of pharmaceutically active entities; and to certain intermediates provided by these processes.

2. 发明公开

EP1622602A4 METHOD FOR MONITORING BLOOD FLOW AND METABOLIC UPTAKE IN TISSUE WITH RADIOLABELED ALKANOIC ACID 有权
标题翻译：程序用于监视的血流量及代谢中夹杂物的织物放射性注明的烷酸
公开(公告)号：EP1622602A4
公开(公告)日：2006-06-21
申请号：EP04760019
申请日：2004-04-19
申请人： GEN HOSPITAL CORP
发明人： ELMALEH DAVID R , FISCHMAN ALAN J , SHOUP TIMOTHY M
IPC分类号： A61B20060101 , A61K31/19 , A61K31/20 , A61K51/00 , B65D71/00 , C07C61/04 , C07C63/33 , C07F5/00
CPC分类号： A61K51/0402

3. 发明授权

EP1343746B1 USE OF CARBOXYLIC ACID COMPOUND HAVING CYCLOPROPANE RING AS MEDICAMENT 有权
标题翻译：使用含CYCLOPROPANCYCLUS羧酸化合物AS的药物
公开(公告)号：EP1343746B1
公开(公告)日：2006-06-14
申请号：EP01271349.1
申请日：2001-12-18
申请人： Tox K.K. , Nishizaki, Tomoyuki
发明人： NISHIZAKI, Tomoyuki , TANAKA, Akito,
IPC分类号： C07C61/04 , C07C53/134 , C07C61/35 , C07C57/26 , C07C61/12 , C07C61/28 , A61K31/20 , A61K31/202 , A61K31/19 , A61P25/00
CPC分类号： C07C61/04 , C07C53/134 , C07C57/26 , C07C61/12 , C07C61/28 , C07C61/35
摘要： A carboxylic acid compound having cyclopropane ring(s) of the formula (I): wherein R is alkyl or alkenyl optionally having one or more 1,2-cyclopropylene in a carbon chain and/or optionally having cyclopropyl at the end of a chain,X is a single bond or alkylene, wherein the total number of carbon less the number of cyclopropane ring is 10-25, and a pharmaceutically acceptable salt thereof are provided. The compound (I) shows an LTP-like potentiation of synaptic transmission, allows slow metabolism in the living body, shows a stable LTP-like potentiation of synaptic transmission, and is useful as an agent for LTP-like potentiation of synaptic transmission, a cognition-enhancing drug or an agent for the prophylaxis and treatment of dementia, a learning and memory disorder and a neurotransmitter release disorder.

4. 发明公开

EP1615899A1 ALPHA-SUBSTITUTED CARBOXYLIC ACIDS AS PPAR MODULATORS 审中-公开
标题翻译： ALPHA-SUBSTITUIERTECARBONSÄURENALS PPAR MODULATOREN
公开(公告)号：EP1615899A1
公开(公告)日：2006-01-18
申请号：EP04725121.0
申请日：2004-04-01
申请人： PFIZER INC.
发明人： BAILEY, Simon, Pfizer Global R&D , HUMPHRIES, Paul Stuart, Pfizer Global R&D , SKALITZKY, Donald James, Pfizer Global R&D , SU, Wei-Guo, Pfizer Global R&D , ZEHNDER, Luke Raymond, Pfizer Global R&D
IPC分类号： C07D263/32 , C07D213/66 , C07D405/06 , C07C59/125 , C07C61/04 , C07D413/12 , C07D401/04 , C07D307/79 , C07D411/12 , C07D413/14 , C07D249/06 , C07D417/14
CPC分类号： C07D213/66 , C07C59/68 , C07C62/34 , C07C271/14 , C07C271/16 , C07C311/08 , C07C311/29 , C07C317/22 , C07C2601/04 , C07D249/06 , C07D263/32 , C07D307/79 , C07D401/04 , C07D405/06 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Alpha substituted carboxylic acids of formula (I): wherein R' and R2 are as defined in the specification and R3 is A) formula (II); B) formula (III); C) formula (IV); and D) formula (V); wherein Y, Art, Are, AP, R4, R5, R6, R7, R6, R9, R9a, R10, R', R12, R17, ring A, and p are as defined in the specification; pharmaceutical compositions containing effective amounts of said compounds or their salts are useful for treating PPAR, specifically PPAR α/y related disorders, such as diabetes, dyslipidemia, obesity and inflammatory disorders.
摘要翻译：式（I）的α取代的羧酸：其中R'和R 2如说明书中所定义，R 3是A）式（II）; B）式（III）; C）式（IV）; 和D）式（V）; 其中Y，Art，Are，AP，R4，R5，R6，R7，R6，R9，R9a，R10，R“，R12，R17，环A和p如说明书中所定义;含有有效量的所述化合物或其盐可用于治疗PPAR，特别是PPARα/ y相关疾病，例如糖尿病，血脂异常，肥胖症和炎症性疾病。

5. 发明公开

EP0933993A4 SUBSTITUTED CYCLOPENTANE COMPOUNDS USEFUL AS NEURAMINIDASE INHIBITORS 失效
标题翻译：取代的环戊烷衍生物作为神经氨酸酶抑制剂的有用的是
公开(公告)号：EP0933993A4
公开(公告)日：2004-09-08
申请号：EP97931014
申请日：1997-06-13
申请人： BIOCRYST PHARM INC
发明人： BABU YARLAGADDA S , CHAND POORAN , MONTGOMERY JOHN A
IPC分类号： C07D295/18 , A01N37/12 , A01N37/18 , A01N47/44 , A61K31/00 , A61K31/04 , A61K31/045 , A61K31/08 , A61K31/155 , A61K31/16 , A61K31/18 , A61K31/19 , A61K31/195 , A61K31/275 , A61K31/395 , A61K31/397 , A61K31/40 , A61K31/445 , A61P31/00 , A61P31/16 , C07C61/06 , C07C62/02 , C07C69/757 , C07C233/47 , C07C237/22 , C07C279/14 , C07C279/16 , C07D205/04 , C07D211/16 , C07D211/70 , C07D295/185 , A01N37/52 , C07C61/04 , C07C233/00 , C07C281/00
CPC分类号： C07D295/185 , C07C61/06 , C07C62/02 , C07C69/757 , C07C233/47 , C07C279/14 , C07C279/16 , C07C2601/08 , C07D205/04

6. 发明公开

EP0436348A2 Pyridyl cyclopropane derivatives with fungicidal activity 失效
标题翻译： Fungizide。
公开(公告)号：EP0436348A2
公开(公告)日：1991-07-10
申请号：EP90313836.0
申请日：1990-12-18
申请人： ZENECA LIMITED , ICI AMERICAS INC.
发明人： Worthington, Paul Antohony , Matthews, Ian Richard , Bartholomew, David , Crowley, Patrick Jelf , Baker, Don Robert , Fisher, Karl Joseph
IPC分类号： C07D213/75 , C07D213/74 , A01N53/00 , C07C61/04 , C07C51/245
CPC分类号： C07D213/75 , A01N53/00 , C07C51/29 , C07C61/15
摘要： Compounds of having the general formula (I):

and stereoisomers thereof, wherein R¹ is hydrogen, halogen, C₁₋₄ alkoxy, C₁₋₄ alkyl, C₂₋₄ alkenyl, C₂₋₄ alkynyl, C₁₋₄ haloalkyl, C₁₋₄ haloalkoxy, COR or cyano; R², R³ and R⁴ are independently hydrogen, halogen or methyl, provided that R², R³ and R⁴ are not all hydrogen and provided that when one of them is methyl then at least one of the other two is not hydrogen;

wherein R⁵ is hydrogen, C₁₋₄ alkyl (optionally substituted by hydrogen or cyano), optionally substituted benzyl, C₂₋₄ alkenyl, C₂₋₄ alkynyl, cyano, COR C₁₋₄ thioalkoxy C₁₋₄ thiohaloalkoxy or SNR⁷R⁸; R⁷ and R⁸ are independently C₁₋₄ alkyl or CO₂R; Y is oxygen or sulphur; R⁶ is C₁₋₄ alkoxy, C₁₋₄ thioalkoxy or -NR⁹ R¹⁰ ; and R⁹ and R¹⁰ are independently hydrogen, C₁₋₄ alkyl, aryl or aralkyl or R⁹ and R¹⁰ join to form an optionally substituted heterocyclic ring and R is C₁₋₄ alkyl or C₃₋₇ cycloalkyl. These compounds are fungicidally active.
摘要翻译：具有通式（I）：的化合物及其立体异构体，其中R 1是氢，卤素，C 1-4烷氧基，C 1-4烷基，C 2-4烯基，C 2-4炔基，C 1-4 卤代烷基，C 1-4卤代烷氧基，COR或氰基; R 2，R 3和R 4独立地为氢，卤素或甲基，条件是R 2，R 3和R 4不全部为氢，条件是当其中一个为甲基，则其他两个中的至少一个不是氢; 其中R 5为氢，C 1-4烷基（任选被氢或氰基取代），任选取代的苄基，C 2-4烯基，C 2-4炔基，氰基，COR C 1-4硫烷氧基C 1-4硫代卤代烷氧基或 SNR <7> - [R <8>; R 7和R 8独立地是C 1-4烷基或CO 2 R; Y是氧或硫; R 6是C 1-4烷氧基，C 1-4硫代烷氧基或-NR 9 R 1; 并且R 9和R 1独立地是氢，C 1-4烷基，芳基或芳烷基或R 9和R 1连接形成任选被取代的杂环，R是C1 -4-烷基或C 3-7环烷基。这些化合物是杀真菌活性的。

7. 发明授权

EP0197428B1 A method for producing cyclopropanecarboxylic acid derivatives 失效
标题翻译：一种生产环丙烷基羧酸衍生物的方法
公开(公告)号：EP0197428B1
公开(公告)日：1989-02-01
申请号：EP86104097.0
申请日：1986-03-25
申请人： SUMITOMO CHEMICAL COMPANY, LIMITED
发明人： Matsuo, Noritada , Tsushima, Kazunori
IPC分类号： C07C61/04 , C07C51/00 , C07C49/16
CPC分类号： C07C45/63 , C07C45/00 , C07C49/16 , C07C51/00 , C07C61/04

8. 发明授权

EP0093511B1 Method for producing and optically active 2,2-dimethylcyclopropanecarboxylic acid 失效
标题翻译：生产和光活性的2,2-二甲基环戊烷羧酸的方法
公开(公告)号：EP0093511B1
公开(公告)日：1986-09-24
申请号：EP83301925.0
申请日：1983-04-06
申请人： SUMITOMO CHEMICAL COMPANY, LIMITED
发明人： Minai, Masayoshi , Katsura, Tadashi , Hamada, Kazuhiko , Suzukamo, Gohfu
IPC分类号： C07C61/04 , C12P41/00
CPC分类号： C07C51/487 , C07C61/04

9. 发明授权

EP0033160B1 Substituierte 3-(1,2-Dibrom-alkyl)-2,2-dimethyl-cyclo-propan-1-carbonsäureester, Verfahren sowie Zwischenprodukte zu ihrer Herstellung und ihre Verwendung in Schädlingsbekämpfungsmitteln 失效
标题翻译：取代的3-（1,2-二溴 - 烷基）-2,2-二甲基 - 环丙烷-1-羧酸酯，其制备和中间体及其作为杀虫剂的应用
公开(公告)号：EP0033160B1
公开(公告)日：1985-05-02
申请号：EP81100615.4
申请日：1981-01-28
申请人： BAYER AG
发明人： Fuchs, Rainer, Dr. , Naumann, Klaus, Dr. , Hammann, Ingeborg, Dr. , Stendel, Wilhelm, Dr.
IPC分类号： C07C121/75 , C07C69/74 , C07C61/04 , C07C67/10 , A01N53/00
CPC分类号： C07C61/40 , A01N53/00

10. 发明授权

EP0003666B1 Oxabicyclo 3.1.0 hexanes useful in the production of cyclopropanecarboxylate insecticides and intermediate compounds 失效
标题翻译： OXABICYCLO 3.1.0 HEXANES有用的生产环丙烷氧基甲酸酯类杀虫剂和中间体化合物
公开(公告)号：EP0003666B1
公开(公告)日：1983-04-06
申请号：EP79300173.6
申请日：1979-02-02
申请人： FMC Corporation
发明人： Hatch, Charles Eldrige , Kondo, Kiyoshi , Takashima, Toshiyuki , Tunemoto, Daiei
IPC分类号： C07D307/93 , C07C61/04 , C07C67/00 , C07C69/38 , C07C69/72 , C07C69/74 , C07C113/00
CPC分类号： C07D307/93 , C07B2200/07 , C07B2200/09 , C07C29/095 , C07C29/56 , C07C29/64 , C07C61/40 , C07C69/38 , C07C69/72 , C07C33/423
摘要： The invention provides compounds of the formulae: in which R is hydrogen or CX3, each X, which is the same as or different from the other, is a chlorine or bromine atom, R is lower alkyl or lower alkoxy, R is hydrogen, lower alkoxycarbonyl or lower alkanoyl, and R is hydrogen or lower alkoxycarbonyl. The compounds of Formula III are made by intramolecular carbenoid cyclization of compounds of Formula II; the compounds of Formula II are made from compounds of Formula I, e.g. by treatment with azide followed by a base; the compounds of Formula I are prepared by reacting an alcohol of formula: with a hydrazone. Those compounds of Formula I in which R is CX3 can be converted to a compound of the formula: in which the carboxy and dihalovinyl groups are cis with respect to each other, which are insecticidal, by treatment with certain metals in selected solvents.

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