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52. 发明公开

EP0711751A1 Process for the preparation of intermediates for oxime ether- or 2-phenyl-3-methyl propenoate-fungicides 失效
标题翻译：一种制备中间体化合物的肟醚或2-苯基-3-甲氧基 - propenester杀真菌剂处理
公开(公告)号：EP0711751A1
公开(公告)日：1996-05-15
申请号：EP96102169.8
申请日：1992-09-09
申请人： ZENECA LIMITED
发明人： Matthews, Ian Richard , Clouch, John Martin , Godfrey, Christopher Richard Ayles
IPC分类号： C07C249/12 , C07C251/48 , C07D311/76 , C07D307/83 , C07C69/96
CPC分类号： C07D213/75 , A01N47/06 , A01N47/12 , A01N47/16 , A01N47/18 , A01N47/20 , A01N47/22 , C07C69/734 , C07C69/96 , C07C249/04 , C07C249/12 , C07C251/48 , C07C271/28 , C07C271/64 , C07C317/42 , C07C323/36 , C07C327/48 , C07C329/02 , C07C329/04 , C07C333/08 , C07D295/205 , C07D311/76
摘要： Fungicidal compounds having the formula (I):

wherein W is CH₃O.CH=CCO₂CH₃, CH₃ON=CCONR³R⁴ or CH₃ON=CCO₂CH₃ and stereoisomers thereof; n is O or 1; X is oxygen or sulphur; Z is oxygen, sulphur or NR¹; R¹ is hydrogen or alkyl optionally substituted with halogen, C₁₋₆ alkoxy, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₆ cycloalkyl or aryl; R² is alkyl, haloalkyl, alkenyl, alkynyl, alkoxycarbonyl(C₁₋₄)alkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aryl(C₁₋₄)alkyl, optionally substituted heteroaryl(C₁₋₄)alkyl, optionally substituted aryloxy(C₁₋₄)alkyl, optionally substituted heteroaryloxy(C₁₋₄)alkyl, optionally substituted aryloxy(C₂₋₄)alkenyl, optionally substituted heteroaryloxy(C₂₋₄)alkenyl, optionally substituted aryl(C₂₋₄)alkenyl, optionally substituted heteroaryl(C₂₋₄)alkenyl, optionally substituted arylcarbonyl(C₁₋₄)alkyl, optionally substituted heteroarylcarbonyl(C₁₋₄)alkyl, optionally substituted aryloxycarbonyl(C₁₋₄)alkyl, optionally substituted heteroaryloxycarbonyl-(C₁₋₄)alkyl or -COR⁵; or R¹ and R² together form an optionally substituted 4-, 5- or 6-membered heterocyclic ring system; R³ and R⁴ are independently hydrogen or methyl; and R⁵ is optionally substituted heteroaryl or optionally substituted aryl; and processes for preparing, compositions comprising and methods of combating fungi using compounds of formula (I). Also provided is a process for the preparation of a compound of formula (XX):

wherein p is 0 or 1.
摘要翻译：具有式（I）的杀真菌化合物： worin W是CH3O.CH = CCO2CH3，CH3ON = CCONR <3> [R <4>或= CH3ON CCO2CH3和立体异构体; n是0或1; X是氧或硫; Z是氧，硫或NR <1>; [R <1>是氢或烷基被卤素OPTIONALLY substituiertem，C 1-6烷氧基，C 2-6烯基，C 2-6炔基，C 3-6环烷基或芳基; [R <2>的烷基，卤代烷基，烯基，炔基，烷氧基羰基（C 1-4）烷基，芳基OPTIONALLY substituiertem，任选substituiertem杂芳基，任选substituiertem芳基（C 1-4）烷基，任选substituiertem杂芳基（C 1-4）烷基，任选取代的芳氧基（C 1-4）烷基，任选取代的杂芳氧基（C 1-4）烷基，任选取代的芳氧基（C 2-4）烯基，任选取代的杂芳氧基（C 2-4）烯基，任选取代的芳基（C 2-4）烯基，任选取代的杂芳基（C 2-4）烯基，任选substituiertem芳基羰基（C 1-4）烷基，任选substituiertem杂芳（C 1-4）烷基，任选substituiertem芳氧基羰基（C 1-4）烷基，任选substituiertem杂芳氧，（C 1-4）烷基或 COR <5>; 或R <1>和R <2>一起形成在OPTIONALLY substituiertem 4-，5-或6元杂环环系; [R <3>和R <4>是unabhängig氢或甲基; 且R <5>任选substituiertem杂芳基或任选substituiertem芳基; 和制备打击使用式（I）的化合物真菌的，组合物和方法，其包括处理。所以提供了一种用于制备式（XX）的化合物的制备： worin p是0或第一

53. 发明授权

EP0503630B1 Cyclohexanetriol derivatives 失效
标题翻译： Cyclohexantriolderivate
公开(公告)号：EP0503630B1
公开(公告)日：1995-12-27
申请号：EP92104293.3
申请日：1992-03-12
申请人： Kuraray Co., Ltd.
发明人： Takahashi, Takashi , Shiono, Manzo
IPC分类号： C07D317/46 , C07D311/76 , C07D261/20 , C07D498/04 , C07D493/04 , C07F7/18
CPC分类号： C07D493/04 , C07D261/20 , C07D311/76 , C07D317/46 , C07F7/1856 , Y02P20/55

54. 发明公开

EP0679642A1 Condensed heterocyclic compounds, their production and use 失效
标题翻译： Kondensierte hybridlische Verbindungen，ihre Herstellung und Anwendung。
公开(公告)号：EP0679642A1
公开(公告)日：1995-11-02
申请号：EP95106189.4
申请日：1995-04-26
申请人： TAKEDA CHEMICAL INDUSTRIES, LTD.
发明人： Kato, Kaneyoshi , Sugiura, Yoshihiro , Kato, Koichi , Nagai, Yasuo
IPC分类号： C07D217/14 , C07D311/76 , A61K31/47 , A61K31/35 , C07D405/06 , C07D401/06 , C07D409/12
CPC分类号： C07D249/08 , C07D217/14 , C07D231/12 , C07D233/56 , C07D311/76 , C07D401/06 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/04 , C07D417/12 , C07D471/10 , C07D495/10
摘要： The compound

wherein ring A represents a benzene ring; Ar represents an aromatic group; R¹ and R² independently represent hydrogen, acyl or hydrocarbon group or R¹ and R² taken together with the adjacent nitrogen atom represent a nitrogen-containing heterocyclic group; m represents an integer of 1 to 6; n represents an integer of 2 to 3; represents a single bond or a double bond; X stands for -O- or -NR³- in which R³ represents hydrogen, acyl or hydrocarbon group where is a single bond or =N- where is a double bond has excellent GnRH receptor antagonizing activity, calcium antagonizing and monoamine-uptake inhibiting activities and and value as a prophylactic/therapeutic drug for sex hormone-dependent diseases and for central diseases.
摘要翻译：化合物其中环A表示苯环; Ar表示芳基; R 1和R 2独立地表示氢，酰基或烃基或与相邻氮原子一起的R 1和R 2表示含氮杂环基; m表示1〜6的整数， n表示2〜3的整数， @表示单键或双键; X代表-O-或-NR 3 - ，其中R 3表示氢，酰基或烃基，其中@是单键或= N-，其中@是双键具有优异的GnRH受体拮抗活性，钙拮抗和单胺摄取抑制活性，并且作为性激素依赖性疾病和中枢性疾病的预防/治疗药物。

55. 发明公开

EP0481383A1 Heterocyclic amine derivatives, their production and use 失效
标题翻译： Heterozyklische Aminderivate，deren Herstellung und deren Verwendung。
公开(公告)号：EP0481383A1
公开(公告)日：1992-04-22
申请号：EP91117442.3
申请日：1991-10-12
申请人： Takeda Chemical Industries, Ltd.
发明人： Natsugari, Hideaki , Tawada, Hiroyuki , Ikeda, Hitoshi
IPC分类号： C07D311/76 , C07D335/06 , C07D217/24 , A61K31/35 , A61K31/38 , A61K31/47
CPC分类号： C07D335/06 , C07D217/24 , C07D311/76
摘要： A novel heterocyclic amine derivative of the general formula:

wherein a ring A and a ring B stand independently for an optionally substituted benzene ring, Z° stands for O or S or

stands for -CH₂-, X stands for O, S or NR¹ wherein R¹ stands for hydrogen atom or an alkyl group, Y stands for NH, O or (CH₂) n wherein n denotes 0 to 2, and R² stands for an optionally substituted hydrocarbon group, or their salts. The compound (I) is useful as a safe agent of lowering cholesterol in blood and a therapeutic drug for arteriosclerosis and the like. A process of the compound of preparation of the formula (I or a salt thereof and a pharmaceutical composition comprising the compound of the formula (I) or a pharmaceutically acceptable salt thereof as an active component are also disclosed.
摘要翻译：一种通式为：CHEM的新型杂环胺衍生物，其中环A和环B独立地代表任选取代的苯环，Z代表O或S或代表-CH 2 - ，X代表 O，S或NR 1其中R 1表示氢原子或烷基，Y表示NH，O或（CH 2）n，其中n表示0至2，R 2表示任选取代的烃基或其盐。化合物（I）可用作降低血液中的胆固醇的安全剂和用于动脉硬化的治疗药物等。还公开了式（I或其盐和包含式（I）化合物或其可药用盐作为活性成分的药物组合物）的制备方法。

56. 发明授权

EP0192713B1 XENOCOUMACINS 失效
公开(公告)号：EP0192713B1
公开(公告)日：1991-11-06
申请号：EP85904407.5
申请日：1985-09-05
申请人： BIOTECHNOLOGY AUSTRALIA PTY. LTD.
发明人： GREGSON, Richard, Peter , McINERNEY, Bernard, Vincent
IPC分类号： C07D311/76 , C07D405/12 , C07D413/12 , C07D417/12 , A61K31/36 , A61K31/40 , C12P17/06 , C12P17/10
CPC分类号： C07D405/12 , C07D311/76 , C12P17/06 , C12P17/162 , C12R1/01
摘要： The invention relates to compounds of formula (I), some of which are derived from culture of Xenorhabdus nematophilus and Xenorhabdus luminescens. The compounds possess antibacterial, antifungal, acaricidal, anti-inflammatory and antiulcerogenic properties.
摘要翻译：本发明涉及式（I）的化合物，其中一些衍生自嗜线虫致病杆菌（Xenorhabdus nematophilus）和发光致病杆菌（Xenorhabdus luminescens）的培养物。这些化合物具有抗菌，抗真菌，杀螨，抗炎和抗溃疡性质。

57. 发明公开

EP0192713A4 XENOCOUMACINS. 失效
标题翻译： XENOCOUMACINE。
公开(公告)号：EP0192713A4
公开(公告)日：1987-08-24
申请号：EP85904407
申请日：1985-09-05
申请人： BIOTECH AUSTRALIA PTY LTD
发明人： GREGSON RICHARD PETER , MCINERNEY BERNARD VINCENT
IPC分类号： C12P17/06 , A61K31/35 , A61K31/352 , A61K31/40 , A61K31/4025 , A61P1/04 , A61P31/00 , A61P31/04 , C07D207/00 , C07D311/00 , C07D311/76 , C07D405/00 , C07D405/12 , C12P17/16 , C12R1/01 , A61K31/36 , C07D413/12 , C07D417/12 , C12P17/10
CPC分类号： C07D405/12 , C07D311/76 , C12P17/06 , C12P17/162 , C12R1/01
摘要： The invention relates to compounds of formula (I), some of which are derived from culture of Xenorhabdus nematophilus and Xenorhabdus luminescens. The compounds possess antibacterial, antifungal, acaricidal, anti-inflammatory and antiulcerogenic properties.
摘要翻译：本发明涉及式（I）的化合物，其中一些衍生自嗜线虫致病杆菌（Xenorhabdus nematophilus）和发光致病杆菌（Xenorhabdus luminescens）的培养物。这些化合物具有抗菌，抗真菌，杀螨，抗炎和抗溃疡性质。

58. 发明公开

EP0134582A2 Novel peptides and process for preparing the same and pharmaceutical composition 失效
标题翻译：肽，其制备方法和药物组合物的过程。
公开(公告)号：EP0134582A2
公开(公告)日：1985-03-20
申请号：EP84110619.8
申请日：1984-09-06
申请人： Tanabe Seiyaku Co., Ltd.
发明人： Sugano, Hiroshi , Ishida, Ryuichi , Yamamura, Michio
IPC分类号： C07K5/06 , C07K1/00 , A61K37/02
CPC分类号： C07D311/76 , C07D217/26 , C07K5/06147 , Y02P20/55
摘要： A compound of the formula:
wherein A is a group of the formula:

R 1 and R' are the same or different and each hydrogen atom, nitro, amino, a protected amino, hydroxy or lower alkoxy,
Y is oxygen atom or a group of the formula: -NR 3- ,
R 3 is hydrogen atom or lower alkyl.
X is methylene or sulphur atom and
the dotted line is an optional double bond, or a pharmaceutically acceptable acid addition salt thereof is useful as a medicine for the treatment of consciousness disorders. Also processes for the preparation of these compounds are disclosed.

59. 发明公开

EP0099339A3 Condensed N-phenylsulfonyl-N'-pyrimidinyl and triazinyl urea 失效
标题翻译：浓缩的N-苯基磺酰基-N'-吡啶二酮和三乙胺
公开(公告)号：EP0099339A3
公开(公告)日：1984-12-27
申请号：EP83810314
申请日：1983-07-11
申请人： CIBA-GEIGY AG
发明人： Ehrenfreund, Josef, Dr. , Föry, Werner, Dr. , Meyer, Willy , Töpfl, Werner, Dr.
IPC分类号： A01N47/36 , C07D405/12 , C07D409/12 , C07D411/12 , C07D401/12 , C07D215/36 , C07D307/79 , C07D307/83 , C07D307/88 , C07D311/58 , C07D311/70 , C07D317/62 , C07D317/66 , C07D319/18 , C07D327/06 , C07D333/54 , C07D335/06
CPC分类号： C07D307/79 , A01N47/36 , C07D209/08 , C07D215/36 , C07D307/83 , C07D307/88 , C07D311/18 , C07D311/22 , C07D311/58 , C07D311/70 , C07D311/76 , C07D317/46 , C07D317/62 , C07D319/18 , C07D327/06 , C07D333/54 , C07D335/06 , C07D521/00

60. 发明公开

EP0061267A1 Process for the production of indanes; process for the production of isochromans and indane precursors used in this process 失效
标题翻译：一种用于二氢化茚的制备方法; 一种制备Isochromanen和使用Indanvorläufer这个过程中的过程。
公开(公告)号：EP0061267A1
公开(公告)日：1982-09-29
申请号：EP82301264.6
申请日：1982-03-12
申请人： BUSH BOAKE ALLEN Limited
发明人： Ferber, Gerald John , Goddard, Peter John
IPC分类号： C07C13/465 , C07C2/42 , C07C15/44 , C07D311/76
CPC分类号： C07D311/76 , C07C2/42 , C07C13/465 , C07C15/44 , C07C2527/173 , C07C2602/08
摘要： Process for the preparation of indanes with the formula
wherein R 3 represents a hydrogen atom or a methyl group; at least one of R, and R 2 represents a methyl group and the other represents a hydrogen atom or a methyl group and R 4 and R 5 which may be the same or different represent alkyl groups having form 1 to 3 carbon atoms in which alkenes selected from the group consisting of propylene, 2-methyl- but-1-ene, 2-methyl-but-2-ene, 2-methyl-pent-l-ene, 2-methyl-pent-2-ene, 3-methyl-but-1-ene, isobutylene and diisobutylene, are reacted with a styrene with the formula
wherein R 1 represents a hydrogen atom or a methyl group; in the presence of phosphoric acid. The indanes (or their precursors) can be reacted with an alkylen oxide and subsequently with formaldehyde to yield isochromanes.
摘要翻译：用于制备茚满与式过程... ... worin R3 darstellt氢原子或甲基; R1和R2中的至少一个darstellt甲基和其他darstellt氢原子或甲基，R4和R5可以是相同或不同，表示具有形式1烷基以选自在其中烯烃3个碳原子由丙烯的，2-甲基 - 丁-1-烯，2-甲基 - 丁-2-烯，2-甲基 - 戊-1-烯，2-甲基 - 戊-2-烯，3-甲基 - 丁 - -1-烯，异丁烯和二异丁烯，进行反应与下式的苯乙烯... ... worin R1 darstellt氢原子或甲基; 在磷酸的存在下进行。的二氢化茚（或其前体）可与在烯化氧进行反应，随后用甲醛，得到isochromanes。

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