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141. 发明公开

EP1252144A1 SUBSTITUIERTE GLUTARIMIDE UND IHRE VERWENDUNG ALS INHIBITOREN DER IL-12 PRODUKTION 有权
标题翻译：取代戊二酰亚胺及其作为IL-12产生的抑制剂
公开(公告)号：EP1252144A1
公开(公告)日：2002-10-30
申请号：EP01900400.1
申请日：2001-01-09
申请人： Grünenthal GmbH
发明人： GERMANN, Tieno , FROSCH, Stefanie , WADE, Erik , BUSCHMANN, Helmut , ZIMMER, Oswald
IPC分类号： C07D211/88 , A61K31/45 , A61P37/02
CPC分类号： C07D211/92 , C07D211/88
摘要： The invention relates to substituted glutarimides of formula (I), wherein x is a group of formula (CH2)n-(CR8R9)p-Z-(CR8R9)m, Z represents a sulphur or oxygen atom, the SO or SO2 group, the radical NR8 (optionally in the form of N oxide) or a CR8R9 group, m and p are 0 or 1, n is 0, 1, 2 or 3, m, n and p cannot simultaneously be 0. The invention also relates to the production and use thereof in medicaments, especially as immunomodulators and inhibitors of angiopathies and/or haematological//oncological diseases..

142. 发明公开

EP1242378A1 NOVEL PROCESSES 审中-公开
标题翻译：新工艺
公开(公告)号：EP1242378A1
公开(公告)日：2002-09-25
申请号：EP00986715.1
申请日：2000-12-22
申请人： SmithKline Beecham Corporation , SmithKline Beecham plc
发明人： BROOK, Christopher, S. , CURZONS, Alan, D. , GRADY, Carolyn, W. , O'CONNOR, Anthony, J.
IPC分类号： C07D211/22 , C07D211/88 , A61K31/445
CPC分类号： C07D211/22 , A61K31/445
摘要： A process for the manufacture of the (-) trans piperidine carbinol (1) by a process comprising contacting a racemic mixture of the piperidine carbinol in solution with (-)-ditoluoyltartaric acid, crystallising the (-)-ditoluoyltartaric acid salt of the piperidine carbinol, isolating the crystalline salt and neutralising the crystalline salt to regenerate the (-) trans isomer of the piperidine carbinol and the (-)-ditoluoyltartaric acid, which is characterised by one or more of the following steps: (1) combining solutions of the racemic piperidine carbinol and (-)-ditoluoyltartaric acid in acetone so that the combined solution contains 2-3 % wt/wt of water, (2) consolidating the chiral salt crystallisation at from 30 to 40 °C, (3) cooling the crystallisation mixture to from 3 to 7 °C before isolating the chiral salt, (4) regenarating the (-) trans piperidine carbinol at a pH of from 10.5 to 11.5, (5) forming a concentrated solution of the (-) trans piperidine carbinol in toluene, contacting the solution with heptane at 60-65 °C, and cooling stepwise to crystallise the (-) trans piperidine carbinol. Alternatively, a solution of the racemic piperidine carbinol in toluene, suitably from a previous stage in the manufacture of paroxetine, is combined with a solution of (-)-ditoluoyltartaric acid in acetone. The resultant (-) trans piperidine carbinol of structure (1) may be coupled with sesamol, then deprotected, to give paroxetine (2), with optional formation of a pharmaceutically acceptable salt of paroxetine.

143. 发明授权

EP0912499B1 PESTICIDES 失效
标题翻译： PESTIZIDE
公开(公告)号：EP0912499B1
公开(公告)日：2001-12-12
申请号：EP97925980.1
申请日：1997-06-04
申请人： Bayer Aktiengesellschaft
发明人： SZCZEPANSKI, Henry , ZELLER, Martin , HÜTER, Ottmar Franz
IPC分类号： C07C251/60 , C07D213/53 , C07D211/88 , C07D233/84 , C07D261/08 , C07D295/14 , A01N37/50
CPC分类号： C07D213/53 , A01N37/36 , A01N37/42 , A01N37/50 , A01N43/40 , A01N43/50 , A01N43/80 , C07C251/60 , C07C2601/16 , C07D211/76 , C07D233/86 , C07D261/08 , C07D295/155
摘要： Pesticidally active compounds of formula (I) wherein: X is CH or N; Y is O, S, S=O or NR5; Z is OR2, SR2 or N(R3)R4; n is 0, 1, 2, 3, 4 or 5; or Y and Z together form a 5- to 7-membered ring containing 2 or 3 hetero atoms O and/or N that is unsubstituted or mono- or poly-substituted by C1-C4alkyl, halo-C1-C4alkyl, halogen, =O or by cyclopropyl; W is an aldimino or ketimino group; R1 is cyclopropyl, C1-C6alkyl or halo-C1-C6alkyl; R2 and R3 are each independently of the other C1-C6alkyl or halo-C1-C6alkyl; R4 and R5 are each independently of the other hydrogen, C1-C6alkyl or C1-C6alkoxy; R8 and R9 are each independently of the other hydrogen or C1-C3alkyl; or R8 and R9 together are C2-C6alkenyl or C3-C6cycloalkyl; R21 and R22 are each independently of the other hydrogen, halogen, C1-C8alkyl, C1-C8alkoxy or C1-C8alkylthio; and R23, R24, R25 and R26 are each independently of the others hydrogen, halogen, C1-C8alkyl or C1-C8alkoxy. The compounds may be used in the control of pests, especially as fungicides, acaricides and insecticides in plant protection.
摘要翻译：要求保护作为酯，肟或酰胺的式I的农药活性环己二烯基衍生物化合物。这些化合物可用作植物保护中的杀真菌剂，杀螨剂和杀虫剂。

144. 发明授权

EP0688317B1 PROCESS FOR PREPARING ACRYL-PIPERIDINE CARBINOLS 失效
标题翻译：用于制备丙烯酸哌啶甲醇类
公开(公告)号：EP0688317B1
公开(公告)日：2001-10-31
申请号：EP94909935.2
申请日：1994-03-08
申请人： SMITHKLINE BEECHAM PLC
发明人： CALLANDER, Sidney, Edward
IPC分类号： C07D211/22 , C07D211/88 , C07D405/12
CPC分类号： C07D405/12 , C07D211/22 , C07D211/60
摘要： A process for the preparation of a compound of formula (I) in which R3 is hydrogen, C1-6 alkyl or C1-6 alkylaryl, by reduction using diborane, of a compound of formula (II), in which R3 is as defined in relation to formula (I) and R4 is C1-6 alkyl.

145. 发明授权

EP0757673B1 HETEROCYCLYLBENZONITRILE 失效
公开(公告)号：EP0757673B1
公开(公告)日：2001-10-04
申请号：EP95916668.7
申请日：1995-04-18
申请人： BAYER AG
发明人： DREWES, Mark-Wilhelm , ANDREE, Roland , FINDEISEN, Kurt , HAAS, Wilhelm , LENDER, Andreas , LINKER, Karl-Heinz , SCHALLNER, Otto , DOLLINGER, Markus , SANTEL, Hans-Joachim
IPC分类号： C07D209/48 , C07D263/38 , C07D263/44 , C07D211/88 , C07D207/448 , C07D209/46 , C07D249/20 , C07D249/16 , C07C311/08 , A01N43/38
CPC分类号： C07D207/452 , A01N41/06 , A01N43/38 , A01N43/90 , C07D209/48 , C07D211/88 , C07D471/04
摘要： The invention concerns novel heterocyclylbenzonitriles of general formula (I) in which R?1, R2, R3¿ and Het have the meanings given in the description. The invention further concerns novel processes as well as novel intermediate products for their preparation and their use as herbicides.

146. 发明公开

EP1132379A1 NOVEL THIOL DERIVATIVES, PROCESS FOR PRODUCING THE SAME AND UTILIZATION THEREOF 审中-公开
标题翻译： THIOLDERIVATE，VERFAHREN ZU IHRER HERSTELLUNG UND IHRE ANWENDUNG
公开(公告)号：EP1132379A1
公开(公告)日：2001-09-12
申请号：EP99943412.9
申请日：1999-09-20
申请人： Takeda Chemical Industries, Ltd.
发明人： YAMASHITA, Toshiro , NARA, Hiroshi , TAKIZAWA, Masayuki , YOSHIMURA, Koji
IPC分类号： C07D207/26 , C07D207/40 , C07D211/88 , C07D405/12 , C07D403/12 , C07D401/12 , C07D409/12 , A61K31/40 , A61K31/44 , A61K31/445 , A61K31/505 , A61K31/535
CPC分类号： C07D207/273 , C07D207/40 , C07D207/416 , C07D209/48 , C07D211/76 , C07D211/78 , C07D211/88 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12
摘要： The present invention provides a compound represented by Formula:
wherein ring A and ring B may be same or different and each is an optionally substituted homocyclic or heterocyclic ring and the like, each R 1 may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group, an optionally substituted heterocyclic group or SR 2 , etc., X 1 is a bond, an optionally substituted divalent C 1-3 aliphatic hydrocarbon group or -NR 3 -, etc, X 2 is a bond, an optionally substituted divalent C 1-3 aliphatic hydrocarbon group, -NR 4 -, -O- or -S(O) p -(wherein p is 0, 1 or 2), each Y may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, a halogen atom, a carboxyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, SR 5 , an oxo group, a thioxo group, an optionally substituted imino group, a nitro group, a cyano group, etc., each m may be same or different and is 0 or 1, n is an integer of 1 to 3, q 1 is an integer of 1 to 2n+4, q 2 is an integer of 0 to 2n+3, and the sum of q 1 and q 2 is 2n+4 or a salt thereof.
摘要翻译：本发明提供由式：CHEM表示的化合物，其中环A和环B可以相同或不同，并且各自为任选取代的杂环或杂环等，每个R 1可以相同或不同，并且为氢原子，任选取代的烃基，酰基，任选取代的杂环基或SR 2等，X 1是键，任选取代的二价C 1-3脂族烃基或-NR 3→等，X 2是键，任选取代的二价C 1-3脂族烃基，-NR 4 - ， - O-或-S（O）p - （其中p是0,1）或2）中，每个Y可以相同或不同，为氢原子，任选取代的烃基，卤素原子，羧基，酰基，任选取代的羟基，任选取代的氨基，SR 5 氧代基，硫代基，任选取代的亚氨基，硝基，氰基等，各m可以相同或不同，为0或1，n为1至3的整数，q1为1至2n + 4的整数，q2为0至2n + 3的整数，q1和q2之和为2n + 4或盐它们。

147. 发明公开

EP1058684A1 GLYCINE TRANSPORT INHIBITORS 审中-公开
标题翻译：甘氨酸转运抑制剂
公开(公告)号：EP1058684A1
公开(公告)日：2000-12-13
申请号：EP99937930.8
申请日：1999-02-26
申请人： JANSSEN PHARMACEUTICA N.V.
发明人： LUYTEN, Walter Herman Maria Louis , JANSSENS, Frans Eduard , KENNIS, Ludo Edmond Josephine
IPC分类号： C07D487/04 , A61K31/445 , C07D471/04 , C07D405/06 , C07D401/04 , C07D513/04 , C07D405/14 , C07D401/06 , C07D211/14 , C07D211/18 , C07D211/30 , C07D211/58 , C07D211/88 , C07D401/12 , C07D211/34
CPC分类号： C07D401/04 , A61K31/451 , A61K31/4523 , A61K31/519 , A61K31/55 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/30 , C07D211/34 , C07D211/58 , C07D211/88 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention is concerned with the use of glycine transport inhibiting α,α-diphenyl-1-piperidinebutanamides for the preparation of medicaments for treating disorders of the central and peripheral nervous system, in particular psychoses, pain, epilepsy, neurodegenerative diseases (Alzheimer's disease), stroke, head trauma, multiple sclerosis and the like. The invention further comprises novel compounds, their preparation and their pharmaceutical forms.
摘要翻译：本发明涉及甘氨酸转运抑制α，α-二苯基-1-哌啶丁酰胺在制备用于治疗中枢和外周神经系统疾病，特别是精神病，疼痛，癫痫，神经退行性疾病（阿尔茨海默病），中风，头部创伤，多发性硬化症等。本发明还包括新化合物，它们的制备和它们的药物形式。

148. 发明公开

EP0791592A3 Azetidines 失效
标题翻译：氮杂环丁烷
公开(公告)号：EP0791592A3
公开(公告)日：2000-05-17
申请号：EP97200200.0
申请日：1997-01-24
申请人： Pfizer Limited , Pfizer Research and Development Company, N.V./S.A.
发明人： Mackenzie, Alexander Roderick , Marchington, Allan Patrick , Meadows, Sandra Dora , Middleton, Donald Stuart
IPC分类号： C07D401/06 , C07D401/12 , A61K31/44 , C07D211/88
CPC分类号： C07D401/06 , C07D211/88
摘要： The present invention provides compounds of the formula (I):- and the pharmaceutically acceptable salts thereof, wherein R is C 3 -C 7 cycloalkyl, aryl or C 1 -C 6 alkyl, said C 1 -C 6 alkyl being optionally substituted by fluoro, -COOH, -COO(C 1 -C 4 ) alkyl, C 3 -C 7 cycloalkyl, adamantyl, aryl or het 1 , and said C 3 -C 7 cycloalkyl being optionally substituted by 1 or 2 substituents each independently selected from C 1 -C 4 alkyl, C 3 -C 7 cycloalkyl, C 1 -C 4 alkoxy, hydroxy, fluoro, fluoro(C 1 -C 4 ) alkyl and fluoro(C 1 -C 4 )alkoxy; R1 is phenyl, benzyl, naphthyl, thienyl, benzothienyl or indolyl, each optionally substituted by 1 or 2 substituents each independently selected from C1-C4 alkyl, C1-C4 alkoxy, halo and trifluoromethyl; R2 represents various groups; X is C1-C4 alkylene; and X1 is a direct link or C1-C6 alkylene. Such compounds and salts are useful as tachykinin antagonists.

149. 发明公开

EP0654025A4 METHOD OF PREPARING OPTICALLY PURE PRECURSORS OF PAROXETINE. 失效
标题翻译： VERFAHREN ZUR HERSTELLUNG VON OPTISCH REINEN PRECURSORN VON PAROXETIN。
公开(公告)号：EP0654025A4
公开(公告)日：1995-10-11
申请号：EP93918661
申请日：1993-08-05
申请人： SEPRACOR INC
发明人： ZEPP CHARLES M , GAO YUN , HEEFNER DONALD L
IPC分类号： C07D211/22 , C07D211/88 , C12P41/00
CPC分类号： C07D211/88 , C07D211/22 , C12P41/005
摘要： A biocatalytic method of preparing optically pure precursors of paroxetine and a method of preparing paroxetine therefrom are disclosed. A racemic trans ester precursor compound of paroxetine is first prepared. The racemic trans ester precursor compound comprises a mixture of (3S, 4R) and (3R, 4S) enantiomers. The (3R, 4S) enantiomer is hydrolyzed biocatalytically to the corresponding (3R, 4S)-trans carboxylic acid or alternatively, the (3S, 4R) enantiomer is biocatalytically hydrolyzed to the (3S, 4R)-trans carboxylic acid in a reaction catalyzed by an isolated enzyme or a microorganism. In the first instance, the unhydrolyzed (3S, 4R) enantiomer is separated from the (3R, 4S)-trans carboxylic acid, whereas in the second instance the (3S, 4R)-trans carboxylic acid is separated from the unhydrolyzed (3R, 4S) enantiomer. The (3S, 4R) enantiomer obtained following the selective hydrolysis is reduced to form a (-)-trans-(3S, 4R) primary alcohol precursor of paroxetine. Paroxetine is then formed from the (-)-trans-(3S, 4R) primary alcohol precursor.
摘要翻译：公开了制备光学纯的帕罗西汀前体的生物催化方法和由其制备帕罗西汀的方法。首先制备帕罗西汀的外消旋转酯前体化合物。外消旋的转酯前体化合物包含（3S，4R）和（3R，4S）对映体的混合物。（3R，4S）对映异构体被生物催化水解为相应的（3R，4S） - 反式羧酸，或者在催化的反应中将（3S，4R）对映异构体生物催化水解成（3S，4R） - 反式羧酸通过分离的酶或微生物。首先，将未水解的（3S，4R）对映体从（3R，4S） - 反式羧酸中分离出来，而在第二种情况下将（3S，4R） - 反式羧酸从未水解的（3R， 4S）对映体。选择性水解后得到的（3S，4R）对映体被还原形成帕罗西汀的（ - ） - 反式 - （3S，4R）伯醇前体。然后由（ - ） - 反式 - （3S，4R）伯醇前体形成帕罗西汀。

150. 发明公开

EP0574758A1 Hydroxamic acid derivatives as collagenase inhibitors 失效
标题翻译： Hydroxamsäure衍生物胶原酶抑制剂。
公开(公告)号：EP0574758A1
公开(公告)日：1993-12-22
申请号：EP93108628.4
申请日：1993-05-28
申请人： F. HOFFMANN-LA ROCHE AG
发明人： Broadhurst, Michael John , Brown, Paul Anthony , Johnson, William Henry , Lawton, Geoffrey
IPC分类号： C07D209/48 , A61K31/395 , C07D401/06 , C07D491/10 , C07D249/12 , C07D211/88 , C07D233/72 , C07D207/40 , C07D207/26 , C07D417/06 , C07D403/12 , C07D271/06 , C07D233/96 , C07D403/06
CPC分类号： C07D207/27 , C07D207/404 , C07D209/48 , C07D211/88 , C07D233/74 , C07D249/12 , C07D271/07 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D417/06 , C07D491/10
摘要： The invention provides hydroxamic acid derivatives of the formula

wherein R¹ represents a 5- or 6-membered N-heterocyclic ring, R² and R³ each represent lower alkyl or NR²R³ represents a saturated 5-, 6- or 7-membered heterocyclic ring, R⁴, R⁵, R⁶ and R⁷ each represent hydrogen or methyl, provided that at least two of these symbols represent hydrogen and n stands for 1-4, and their pharmaceutically acceptable salts, which are collagenase inhibitors useful for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis or for the treatment of invasive tumours, atherosclerosis or multiple sclerosis.
摘要翻译：本发明提供式的异羟肟酸衍生物，其中R 1表示5-或6-元N-杂环，R 2和R 3各自代表低级烷基或NR 2 R 3>表示饱和的5-，6-或7-元杂环，R 4，R 5，R 6和R 7各自表示氢或甲基，条件是这些符号中的至少两个代表氢，n代表1-4，以及它们的药学上可接受的盐，它们是用于控制或预防变性关节疾病如类风湿性关节炎和骨关节炎或用于治疗侵袭性肿瘤，动脉粥样硬化或多发性硬化的胶原酶抑制剂。

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