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1. 发明授权

EP2509966B1 AMINO OXAZINE DERIVATIVES 有权
标题翻译：氨基 - 恶嗪衍生物
公开(公告)号：EP2509966B1
公开(公告)日：2014-10-22
申请号：EP10790920.2
申请日：2010-12-07
申请人： F.Hoffmann-La Roche AG
发明人： BANNER, David , HILPERT, Hans , MAUSER, Harald , MAYWEG, Alexander V. , ROGERS-EVANS, Mark
IPC分类号： C07D265/08 , C07D413/12 , C07D417/12 , C07D495/04 , C07D498/04 , A61K31/5355 , A61P3/10
CPC分类号： C07D413/12 , C07D265/08 , C07D417/12 , C07D495/04 , C07D498/04

2. 发明公开

EP2151435A1 PHARMACEUTICAL COMPOSITION FOR TREATMENT OF ALZHEIMER'S DISEASE 审中-公开
标题翻译：药剂师ZUSAMMENSETZUNG ZUR BEHANDLUNG VON MORBUS ALZHEIMER
公开(公告)号：EP2151435A1
公开(公告)日：2010-02-10
申请号：EP08751980.7
申请日：2008-04-23
申请人： Shionogi&Co., Ltd.
发明人： KOBAYASHI, Naotake , UEDA, Kazuo , ITOH, Masahiro , SUZUKI, Shinji , SAKAGUCHI, Gaku , KATO, Akira , YUKIMASA, Akira , HORI, Akihiro , KOORIYAMA, Yuuji , HARAGUCHI, Hidekazu , YASUI, Ken , KANDA, Yasuhiko
IPC分类号： C07D239/14 , A61K31/426 , A61K31/505 , A61K31/535 , A61K31/54 , A61K31/541 , A61K31/554 , A61P25/28 , C07D265/08 , C07D277/18 , C07D279/06 , C07D281/02 , C07D405/04 , C07D417/04 , C07D417/10 , C07D417/12 , C07D471/04
CPC分类号： C07D471/04 , A61K9/0019 , A61K9/1623 , A61K9/2018 , A61K31/426 , A61K31/506 , A61K31/535 , A61K31/54 , A61K31/541 , A61K31/554 , C07D239/14 , C07D265/08 , C07D277/18 , C07D279/06 , C07D281/02 , C07D285/36 , C07D295/155 , C07D295/192 , C07D405/04 , C07D417/04 , C07D417/10 , C07D417/12 , A61K2300/00
摘要： A pharmaceutical composition for treating Alzheimer's disease containing a compound represented by the general formula (I):

wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group;
E is lower alkylene, etc.;
X is S, O, or NR 1 ;
R 1 is a hydrogen atom or lower alkyl;
R 2a , R 2b , R 3a , R 3b , R 4a and R 4b are each independently a hydrogen atom, halogen, hydroxy, etc.;
n and m are each independently an integer of 0 to 3;
n+m is an integer of 1 to 3; and
R 5 is a hydrogen atom, optionally substituted lower alkyl, etc.;
its pharmaceutically acceptable salt, or a solvate thereof as an active ingredient.
摘要翻译：一种用于治疗含有由通式（I）表示的化合物的阿尔茨海默病的药物组合物：其中环A是任选取代的碳环基团或任选取代的杂环基团; E是低级亚烷基等; X是S，O或NR 1; R 1是氢原子或低级烷基; R 2a，R 2b，R 3a，R 3b，R 4a和R 4b各自独立地为氢原子，卤素，羟基等; n和m各自独立地为0〜3的整数; n + m为1〜3的整数。 R 5为氢原子，任意取代的低级烷基等; 其药学上可接受的盐或其溶剂合物作为活性成分。

3. 发明公开

EP2085392A1 HALOALKYLSULFONANILIDE DERIVATIVE OR SALT THEREOF, HERBICIDE COMPRISING THE DERIVATIVE AS ACTIVE INGREDIENT, AND USE OF THE HERBICIDE 审中-公开
标题翻译： HALOGENALKYLSULFONANILIDDERIVAT或其盐，衍生AS含有活性除草剂施用除草剂
公开(公告)号：EP2085392A1
公开(公告)日：2009-08-05
申请号：EP07831986.0
申请日：2007-11-16
申请人： Nihon Nohyaku CO., LTD.
发明人： HINO, Tomokazu , YAMADA, Yasuko , SHIGENARI, Toshihiko , MAMETSUKA, Koki
IPC分类号： C07D265/08 , A01N47/04 , A01P13/00 , C07D265/10 , C07D267/06 , A01N33/18 , A01N43/72 , A01N43/86
CPC分类号： C07D265/08 , A01N43/72 , A01N43/76 , C07D265/10 , C07D267/06
摘要： A haloalkylsulfonanilide derivative represented by general formula (I) or a salt thereof wherein R 1 represents a halo(C 1 -C 8 )alkyl group, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 represent hydrogen atoms, etc., n represents 1 or 2, A represents an oxygen atom, W represents an oxygen atom, X represents a halogen atom and m represents an integer of 0 to 4, are compounds useful as herbicides having both of remarkable herbicidal effect and characteristics such as excellent crop-weed selectivity. General formula (I):
摘要翻译：由通式（I）化合物或其worin，R 1盐表示的卤代烷基磺酰苯胺衍生物表示卤代（C 1 -C 8）烷基，R 2，R 3，R 4，R 5，R 6，R 7，R 8 中，R 9和R 10表示氢原子等，n表示1或2，氧原子的darstellt，W darstellt氧原子，X为卤素原子，m darstellt到darstellt 0〜4的整数，分别为有用的化合物如优异的作物 - 杂草的选择性：具有两个显着的除草效果和特性的除草剂。通式（I）：

4. 发明公开

EP1720844A2 PYRROLIDIN-1,2-DICARBONSÄURE-1-(PHENYLAMID)-2-(4-(3-OXO-MORPHOLIN-4-YL)-PHENYLAMID) DERIVATE UND VERWANDTE VERBINDUNGEN ALS INHIBITOREN DES KOAGULATIONSFAKTORS XA ZUR BEHANDLUNG VON THROMBOEMBOLISCHEN ERKRANKUNGEN 有权
标题翻译：吡咯烷-1,2-二羧酸1-（苯基氨基）-2-（4-（3-氧代 - 吗啉-4-基）-PHENYLAMID）作为凝血因子的抑制剂衍生物和相关化合物XA治疗血栓栓塞性病症的
公开(公告)号：EP1720844A2
公开(公告)日：2006-11-15
申请号：EP04718299.3
申请日：2004-03-08
申请人： Merck Patent GmbH
发明人： TSAKLAKIDIS, Christos , DORSCH, Dieter , MEDERSKI, Werner , CEZANNE, Bertram , GLEITZ, Johannes
IPC分类号： C07D265/32
CPC分类号： C07D413/12 , C07D207/16 , C07D207/27 , C07D211/60 , C07D211/76 , C07D213/64 , C07D213/68 , C07D223/10 , C07D241/18 , C07D265/08 , C07D265/32 , C07D267/10 , C07D401/04 , C07D401/12 , C07D401/14 , C07D413/02 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/08
摘要： The invention relates to the compounds of formula (I), wherein W represents N, CR3, or a sp2 hybridized C atom, E, together with W, represents a 3- to 7-membered saturated carbocylic or heterocyclic ring having 0 to 3 N atoms, 0 to 2 O atoms and/or 0 to 2 S atoms, which ring may contain a double bond, D represents a mononuclear or binuclear unsubstituted aromatic carbocycle or heterocycle having 0 to 4 N atoms, O atoms and/or S atoms or being monosubstituted or polysubstituted by Hal, A, OR3, N(R3)2, NO2, CN, COOR3 or CON(R3)2, G represents -[C(R4)2]n-, -[C(R4)2]nNR3-, -[C(R4)2]nO-, -[C(R4)2]nS- or -[C(R4)=C(R4)]n-, X represents -[C(R4)2]nCONR3[C(R4)2]n-, -[C(R4)2]nNR3CO[C(R4)2]n-, -[C(R4)2]nNR3[C(R4)2]n-, -[C(R4)2]nO[C(R4)2]n-, -[C(R4)2]nCO[C(R4)2]n- or -[C(R4)2]nCOO[C(R4)2]n-, Y represents alkylene, cycloalkylene, Het-diyl or Ar-diyl, T represents a mononuclear or binuclear saturated or unsaturated carbocycle or heterocycle having 0 to 4 N atoms, O atoms and/or S atoms, which is monosubstituted or polysubstituted by =O, =S, =NR3, =N-CN, =N-NO2, =NOR3, =NCOR3, =NCOOR3, =NOCOR3 and which may further be monosubstituted, disubstituted or trisubstituted by R3, Hal, A,-[C(R4)2]n, -Ar, -[C(R4)2]n-het, -[C(R4)2]n-cycloalkyl, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2NR3 and/or S(O)nA, and R1 and R2 are defined as in claim 1. The inventive compounds inhibit coagulation factor Xa and can be used in the prophylaxis and/or therapy of thrombo-embolic diseases and for treating tumors.

5. 发明公开

EP1635909A2 TREATMENT OF AMYLOID- AND EPILEPTOGENESIS-ASSOCIATED DISEASES 审中-公开
标题翻译： BEHANDLUNG AMYLOID-UND EPILEPTOGENESIS-ASSOZIIERTER KRANKHEITEN
公开(公告)号：EP1635909A2
公开(公告)日：2006-03-22
申请号：EP04776863.5
申请日：2004-06-21
申请人： Neurochem (International) Limited
发明人： KONG, Xianqi , LU, Wenshuo , WU, Xinfu
IPC分类号： A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P27/00 , A61P29/00 , A61K31/185
CPC分类号： C07D239/06 , A61K31/185 , C07C309/14 , C07C309/26 , C07C2601/14 , C07C2602/10 , C07D209/14 , C07D213/38 , C07D233/24 , C07D233/28 , C07D263/10 , C07D263/16 , C07D265/08 , C07D277/10 , C07D277/12 , C07D279/06 , C07D317/58 , C07D333/20 , C07D333/58
摘要： Methods of treating or preventing an amyloid-related disease in a subject by administering to a subject a therapeutic amount of a compound of the invention are described. Also included are methods for inhibiting epileptogenesis in a subject, by administering to a subject an effective amount of an anti-epileptogenic agent. Methods for treating a subject suffering from an epileptogenesis-associated condition, by administering to the subject an effective amount of an anti-epileptogenic agent are also included. Methods for treating convulsions in a subject by administering to the subject an effective amount of a therapeutic amount of a compound of the invention are also described.
摘要翻译：描述了通过向受试者施用治疗量的本发明化合物来治疗或预防受试者的淀粉样蛋白相关疾病的方法。还包括通过向受试者施用有效量的抗癫痫发生剂来抑制受试者中癫痫发生的方法。还包括通过向受试者施用有效量的抗癫痫发生剂来治疗患有癫痫发生相关病症的受试者的方法。还描述了通过向受试者施用有效量的治疗量的本发明化合物来治疗受试者惊厥的方法。

6. 发明公开

EP1608619A1 MUSCARINIC AGONISTS 审中-公开
标题翻译：毒蕈碱受体激动剂
公开(公告)号：EP1608619A1
公开(公告)日：2005-12-28
申请号：EP04720318.7
申请日：2004-03-12
申请人： ELI LILLY AND COMPANY
发明人： ALLEN, Jennifer, Rebecca , HITCHCOCK, Stephen Andrew , TURNER, William, Wilson, Jr. , LIU, Bin
IPC分类号： C07D211/72 , C07D207/22 , C07D263/28 , C07D265/08 , C07D277/18 , C07D279/06 , C07D409/12 , A61P25/28 , A61P25/18 , A61K31/4025 , A61K31/421 , A61K31/426 , A61K31/4402 , A61K31/40
CPC分类号： C07D409/12 , C07D207/22 , C07D211/72 , C07D239/14 , C07D263/28 , C07D265/08 , C07D277/18 , C07D279/06
摘要： The present invention relates to compounds of Formula (I): which are agonists of the M-1 muscarinic receptor.

7. 发明授权

EP0472560B1 CYCLISCHE POLYIMINOETHER 失效
公开(公告)号：EP0472560B1
公开(公告)日：1996-07-10
申请号：EP90907005.4
申请日：1990-05-07
申请人： Henkel Kommanditgesellschaft auf Aktien
发明人： HASE, Brigitte , KRAUSE, Horst-Jürgen , FRISTAD, William
IPC分类号： C07D263/14 , C07D265/08 , C08K5/35
CPC分类号： C07D265/08 , C07D263/14 , C08G69/44
摘要： Polyiminoethers of general formula (I) in which A is an aliphatic, aromatic or araliphatic group with 4 to 40 C atoms and n free valencies on various C atoms, X can assum values betwen 0 and 40, n is equal to 2, 3, or 4, Z is either a direct bond or the CR5R6 group, the residues R1 to R6 independently of each other denote H, alkyl or aryl with up to 8 C atoms, the R7 residue is hydrogen, methyl or ethyl and Q is either a phenyl group, which may be substituted by 1 or 2 methyl groups, or the -CHR-M- group, R being chosen from the group alkylene, alkenylene, arylene and alkarylene, and the molecular moieties of R and M independently of each other have 0 to 12 C atoms and can additionally be substituted by an alkoxy group with 1 to 3 C atoms. These compounds are made from polyisocyanates of formula A(NCO)¿n? and cyclic monoiminoethers containing hydroxyl groups and are suitable for subsequent processing to polymers.
摘要翻译：通式（I）的聚亚氨基醚其中A是具有4至40个C原子且在各种C原子上具有n个游离价的脂肪族，芳香族或芳香脂肪族基团，X可具有0至40之间的值，n等于2,3或3。或4，Z为直接键或CR 5 R 6基团，残基R 1至R 6彼此独立地表示H，具有至多8个C原子的烷基或芳基，R 7残基为氢，甲基或乙基且Q为苯基，其可以被1或2个甲基取代，或者-CHR-M-基团，R选自亚烷基，亚烯基，亚芳基和亚烷芳基，并且R和M的分子部分彼此独立地具有 0至12个C原子并且可以另外被具有1至3个C原子的烷氧基取代。这些化合物由式A（NCO）n的多异氰酸酯制成。和含有羟基的环状单亚氨基醚，并适用于随后的聚合物加工。

8. 发明公开

EP0695299A1 METHOD FOR THE PREPARATION OF OXAZOLINES OR OXAZINES USING A BATCH PROCESS 失效
标题翻译：在批处理过程及其制造方法嗪恶唑啉
公开(公告)号：EP0695299A1
公开(公告)日：1996-02-07
申请号：EP94914379.0
申请日：1994-04-15
申请人： Henkel Kommanditgesellschaft auf Aktien
发明人： BARLAGE, Wilhelm , BECK, Michael , RITTER, Wolfgang , FISCHER, Herbert
IPC分类号： C07D263 , C07D265 , C08G73
CPC分类号： B01J31/0212 , C07D263/12 , C07D265/08 , C08G73/0233
摘要： The invention concerns a method of preparing oxazines or oxazolines in which 3-propanolamides or ethanolamides of carboxylic acids are condensed, optionally in the presence of a catalyst, at elevated temperatures and reduced pressure. The method is characterized in that, during the reaction, a slow stream of nitrogen is passed through the reaction vessel to drive out the water of reaction formed, and the oxazolines or oxazines formed are distilled off directly by a thin-film evaporator.

9. 发明公开

EP0098356A3 Process for the preparation of pure anhydrous imido-acid esters by the reaction between nitriles and amino-alcohols 失效
标题翻译：通过硝酸和氨基醇反应制备纯无机酸对硝酸酯的方法
公开(公告)号：EP0098356A3
公开(公告)日：1985-01-23
申请号：EP83104262
申请日：1983-04-30
申请人： CHEMISCHE WERKE HÜLS AG
发明人： Kleine Homann, Walter, Dr.
IPC分类号： C07D263/12 , C07D265/08
CPC分类号： C07D265/08 , C07D263/12

10. 发明公开

EP0083683A1 Method of preparing 1,4-bis(substituted-amino)-5,8-dihydroxyanthraquinones and pharmaceutical compositions containing them 失效
标题翻译：一种1,4-双（取代的氨基）-5,8- dihydroxyanthraquinonen和含有它们的药物组合物的制备方法。
公开(公告)号：EP0083683A1
公开(公告)日：1983-07-20
申请号：EP82106213.0
申请日：1982-07-12
申请人： AMERICAN CYANAMID COMPANY
发明人： Murdock, Keith Chadwick
IPC分类号： C07D263/04 , C07D265/06 , A61K31/42 , A61K31/535
CPC分类号： C07D263/04 , C07D265/08
摘要： This disclosure describes compositions of matter useful as inhibitors of transplanted mouse tumor growth and the method of inducing the regression and/or palliation of leukemia and related cancers in mammals therewith, the active ingredients of said compositions of matter being certain 1,4-bis(substituted-amino)-5,8-dihydroxy- anthraquinones.
摘要翻译：本发明描述作为物质移植小鼠肿瘤的生长和诱导消退和/或白血病的减轻的方法的抑制剂的组合物和在哺乳动物那里，所说的组合物的物质的所述活性成分被某些1,4-双相关的癌症（ substituiertem氨基）-5,8- dihydroxyanthraquinones。

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