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91. 发明公开

EP1114024A1 UROKINASE-INHIBITOREN 有权
标题翻译：尿激酶抑制剂
公开(公告)号：EP1114024A1
公开(公告)日：2001-07-11
申请号：EP98942443.7
申请日：1998-09-18
申请人： Pentapharm A.G.
发明人： WIKSTRÖM, Peter , VIEWEG, Helmut , STÜRZEBECHER,Jörg
IPC分类号： C07C311/19 , C07D295/20 , C07D211/60 , C07D211/62 , C07D211/16 , C07D409/12 , C07D295/18 , A61K31/445 , A61K31/50
CPC分类号： C07D295/185 , C07C311/19 , C07D211/16 , C07D211/60 , C07D211/62 , C07D295/205 , C07D409/12
摘要： The N-α-triisopropylphenylsulfonyl-protected 3-amidinophenylalanine derivatives of formula (I) represent a group of novel urokinase inhibitors which have a high affinity and which can be used for combating tumors and in diagnosis.

92. 发明公开

EP1070049A1 BENZAMIDE AND SULFONAMIDE SUBSTITUTED AMINOGUANIDINES AND ALKOXYGUANIDINES AS PROTEASE INHIBITORS 有权
标题翻译： BOENZOESÄUREAMID和取代的磺酰胺氨基胍和alkoxyguanidines作为蛋白酶抑制剂
公开(公告)号：EP1070049A1
公开(公告)日：2001-01-24
申请号：EP99914339.9
申请日：1999-04-05
申请人： 3-DIMENSIONAL PHARMACEUTICALS, INC.
发明人： SOLL, Richard, M. , LU, Tianbao , TOMCZUK, Bruce, E. , MARKOTAN, Thomas, P. , SIEDEM, Colleen
IPC分类号： C07C279/00 , C07D211/16 , C07D213/40 , C07D223/04 , C07D295/192 , A61K31/445 , A61K31/495 , A61K31/395
CPC分类号： C07D213/40 , C07C279/00 , C07D211/16 , C07D211/62 , C07D213/74 , C07D217/06 , C07D295/192
摘要： The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula (I), wherein X is O or NH, L is -O- or -SO2-, and R?1-R4, R9-R19, Ra, Rb, Rc¿, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing the compounds of Formula (I). Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage.

93. 发明公开

EP1036062A1 HYDROXAMIC ACID DERIVATIVES AS MATRIX METALLOPROTEASE (MMP) INHIBITORS 有权
标题翻译：异羟肟酸衍生物作为金属蛋白酶MATRIX
公开(公告)号：EP1036062A1
公开(公告)日：2000-09-20
申请号：EP98955494.4
申请日：1998-10-09
申请人： Pfizer Limited , PFIZER INC.
发明人： Dack, Kevin Neil , Whitlock, Gavin Alistair
IPC分类号： C07D211/16 , C07D211/22 , A61K31/44 , C07D211/70 , C07D405/12 , C07D401/10 , C07D405/10
CPC分类号： C07D401/10 , C07D211/16 , C07D211/22 , C07D211/70 , C07D405/10 , C07D405/12 , Y02P20/55
摘要： Compounds of formula (I) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R ?1 and R2¿ are each independently selected from hydrogen, C¿1? to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR?6¿ or which is optionally benzo-fused; R3 is hydrogen, halo, R?7 or OR7; R4¿ is hydrogen, C¿1? to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R?6¿ is hydrogen or C¿1? to C4 alkyl; R?7¿ is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diseases.

94. 发明公开

EP0839134A1 BENZOYL PIPERIDINES/PYRROLIDINES FOR ENHANCING SYNAPTIC RESPONSE 失效
标题翻译： BENZOLPIPERIDINE /吡咯烷，以提高响应突触
公开(公告)号：EP0839134A1
公开(公告)日：1998-05-06
申请号：EP96916599.0
申请日：1996-05-23
申请人： CORTEX PHARMACEUTICALS, INC.
发明人： ROGERS, Gary, A. , NILSSON, Lena
IPC分类号： C07D295 , A61K31 , A61P25 , A61P43 , C07D211 , C07D317 , C07D498
CPC分类号： C07D211/16 , C07D211/14
摘要： Benzoyl piperidines and pyrrolidines and compounds of related structure (Formula I) are disclosed for use in enhancing synaptic responses mediated by AMPA receptors. The compounds are effective in the treatment of subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number or strength of excitatory synapses or in the number of AMPA receptors. The compounds can also be used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors, for improving the performance of subjects with memory deficiencies, for treating depression, alcoholism and schizophrenia, and for improving memory encoding.

95. 发明授权

EP0288563B1 CYCLIC AMINE DERIVATIVES 失效
标题翻译：环胺衍生物
公开(公告)号：EP0288563B1
公开(公告)日：1994-05-11
申请号：EP86905925.3
申请日：1986-09-30
申请人： Eisai Co., Ltd.
发明人： SUGIMOTO, Hachiro , NAKAMURA, Takaharu , KARIBE, Norio , SAITO, Isao , HIGURASHI, Kunizo , YONAGA, Masahiro , KANEKO, Takeru , NAKAZAWA, Takahiro , UENO, Masataka , YAMATSU, Kiyomi
IPC分类号： C07D211/14 , C07D211/18 , C07D211/22 , C07D211/32 , C07D211/70 , C07D295/18 , C07D401/06 , C07D405/04 , C07D409/04 , A61K31/445 , A61K31/47
CPC分类号： C07D295/192 , C07D211/16 , C07D211/18 , C07D211/32 , C07D295/03 , C07D401/06 , C07D405/06
摘要： Compounds represented by general formula (I), (wherein A represents substituted or unsubstituted phenyl, pyridyl, thienyl, substituted or unsubstituted naphthyl, tetralyl, quinolyl, benzofuranyl, quinazolyl, benzothienyl, a compound of formula (II) or (III); X represents -CH2-, -C(=O)-, -CH(OH)-, -CH(CH3)- or -CH(CH2N(C2H5)2)-; n represents an integer of 0 to 4; m represents an integer of 1 to 3; Y represents a carbon or nitrogen atom; Z represents -CH2-, -C(=O)-, -CH(OR1)-, (wherein R1 represents H, lower alkyl, acyl, arylalkyl or heteroarylalkyl), -CH(Hal)-, =CH-, a compound of formula (IV), (V) or (VI); Hal represents a halogen atom; a symbol ------ between Y and Z represents a single or double bond, and a group ------ Z$(1,5)$B is bound to the ring at the 3- or 4-position of the above structural formula; B represents a phenyl or naphthyl group optionally substituted by one or two of the same or different substituents selected from among halogen, lower alkyl, and lower alkoxy) and salts. They are effective for retrieval, therapy and prophylaxis of mental troubles accompanying brain blood vessel troubles.
摘要翻译：（I）表示的化合物，其中A表示取代或未取代的苯基，吡啶基，噻吩基，取代或未取代的萘基，四联苯基，喹啉基，苯并呋喃基，喹唑啉基，苯并噻吩基，式（= O） - ， - CH（OH） - ， - CH（CH 3） - 或-CH（CH 2 N（C 2 H 5）2） - ; n表示0至4的整数; m表示（其中R 1表示H，低级烷基，酰基，芳基烷基或杂芳基烷基），-CH（Hal） - ，= CH-，式（IV），（V）或（VI）的化合物; Hal代表卤素原子; Y和Z之间的符号代表单个或双键，并且基团Z 1（1,5）$ B与上述结构式的3-或4-位上的环结合; B表示苯基或萘基，其任选地被一个或两个选自卤素，低级烷基和低级烷氧基的相同或不同的取代基）和s 低价竞标。它们对于伴随脑血管疾病的精神疾病的检索，治疗和预防是有效的。

96. 发明公开

EP0547090A1 PHENOLIC THIOETHERAMIDES AS 5-LIPOXYGENASE INHIBITORS 失效
标题翻译：酚醛THIOETHERAMIDE THAN 5-脂氧合酶抑制剂。
公开(公告)号：EP0547090A1
公开(公告)日：1993-06-23
申请号：EP91915352.0
申请日：1991-09-05
申请人： G.D. SEARLE & CO.
发明人： MUELLER, Richard, August , PARTIS, Richard, Allen
IPC分类号： C07D , A61K31 , A61P29 , A61P37 , C07D211 , C07D213 , C07D279 , C07D295
CPC分类号： C07D213/40 , C07D211/16 , C07D295/185
摘要： L'invention se rapporte à des thioétheramides de la formule (I) dans laquelle R1 et R2 représentent tert-alkyle ou phényle, Alk1 et Alk2 représentent alkylène; X représente soufre ou oxygène, m est 0, 1 ou 2 et R représente a) où R3 et R4 représentent hydrogène ou alkyle et Alk3 représente alkylène; ou b) où Y représente CH, N, O ou S; R6 représente hydrogène, alkyle, phényle, phényle substitué, benzyle, benzyle substitué ou une amine hétérocyclique; et R7 représente hydrogène ou alkyle. Les composés inhibent la 5-lipoxygénase et sont efficaces pour le traitement des états inflammatoires ou allergiques.

97. 发明公开

EP0428434A2 Composés aromatiques aminés et leurs énantiomères, procédé pour leur préparation et compositions pharmaceutiques les contenant 失效
标题翻译：芳族胺和其对映体，制备方法和含有它们的药物组合物的化合物。
公开(公告)号：EP0428434A2
公开(公告)日：1991-05-22
申请号：EP90403125.9
申请日：1990-11-06
申请人： SANOFI
发明人： Emonds-Alt, Xavier , Goulaouic, Pierre , Proietto, Vincenzo , Van Broeck, Didier
IPC分类号： C07D211/14 , C07D409/06 , C07D401/06 , C07D401/12 , C07D409/12 , C07D413/12 , C07D405/12 , C07D211/32 , C07D211/22 , C07D211/70 , C07D295/13
CPC分类号： C07D295/192 , C07D211/14 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/28 , C07D211/32 , C07D211/70 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/13 , C07D317/58 , C07D317/60 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/12 , C07D417/12
摘要： L'invention concerne des composés de formule
dans laquelle :

- m est un nombre entier de 1 à 3 ;
- Ar et Ar représentent, indépendamment, un groupe thiényle, un groupe phényle substitué ou non substitué; un groupe imidazolyle; Ar pouvant également être un groupe benzothiényle non substitué ou substitué par un halogène; un groupe naphtyle non substitué ou substitué par un halogène; un groupe biphényle; un indolyle non substitué ou substitué;
- X représente l'hydrogène;
- X représente l'hydrogène, un groupe hydroxyle, ou est réuni à X ci-dessous pour former une liaison carbone-carbone;
. ou bien X et X, ensemble, forment un groupe oxo ou dialkylaminoalkyloxyimino de formule = N-O-(CH 2 )p-Am, où p est 2 ou 3 et Am est un groupe dialkylamino;
- Y représente un atome d'azote ou un groupe C(X") où X" est l'hydrogène ou, avec X', forme une liaison carbone-carbone;
- Q représente l'hydrogène, un groupe alkyle en C 1 -C 4 ou un groupe aminoalkyle de formule -(CH 2 ) q -Am', où q est 2 ou 3 et Am est un groupe pipéridino, benzyl-4 pipéridino ou dialkylamino;
- R représente l'hydrogène, un groupe méthyle ou un groupe (CH 2 ) n -L, où n est un nombre entier de 2 à 6 et L est l'hydrogène ou un groupe amino,
- T représente un groupe choisi parmi
W étant un atome d'oxygène ou de soufre, et
- Z représente soit l'hydrogène, soit M ou OM lorsque T représente le groupe
soit M lorsque T représente le groupe

M représente l'hydrogène ou un alkyle droit ou ramifié; un phénylalkyle non substitué ou substitué; un pyridylalkyle; un naphtylalkyle; un pyridylthioalkyle; un styryle; un (méthyl-1) imidazolyl-2 thioalkyle ; un oxo-1 phénylindan-3 yle-2; un groupe aromatique ou hétéroaromatique non substitué ou substitué; ou un de leurs sels avec des acides minéraux ou organiques.

Application : antagonistes des récepteurs des neurokinines.
摘要翻译：本发明涉及式... 的化合物...其中：...... - m是从1到3的整数; ... - Ar和Ar“独立地代表噻吩基，一个substituiertem奥德unsubstituiertem苯基; 在咪唑基; 所以其中可以在Ar“是苯并噻吩基，或用卤素unsubstituiertem substituiertem; 萘基，或用卤素unsubstituiertem substituiertem; 联苯基; 在unsubstituiertem substituiertem或吲哚基; ... - X darstellt氢; ... - X“darstellt氢或羟基基团，或连接到X”“之下，形成一个碳 - 碳键; .... 或可替代地，X和X“一起形成氧代基团或给dialkylaminoalkyloxyimino式的基团= N-O-（CH 2）p-Am的，其中p是2或3和AM为二烷基氨基; 氢，Y表示氮原子或基团C（X'），其中X'是或，其中X”，形成碳 - 碳键 - ...; ... - 氢，Q darstellt一个C 1 -C 4烷基或在式氨基烷基 - （CH 2）Q-AM '其中q是2或3和AM' 是哌啶子，4-苄基哌或二烷基氨基; ... - R的darstellt氢，甲基或基团（CH 2）N-L，其中n是从2至6的整数，L是氢或氨基; ... - T的darstellt从... 。W是氧或硫原子，和...中选择的基团 - z darstellt是氢，或M或OM当T darstellt组... ...或M当T darstellt的组 ... ...，M darstellt氢或直链或支链烷基; 在unsubstituiertem或取代的苯基烷基; 一个吡啶基烷基; 一个萘基烷基; 一个pyridylthioalkyl; 苯乙烯; 一个（1-甲基）-2- imidazolylthioalkyl; 1-氧代-3-苯基-2-基; 在unsubstituiertem或取代的芳族或杂芳族基团; ...或它们与无机酸或有机酸的盐之一。 ... 应用：神经激肽受体拮抗剂。

98. 发明公开

EP0288563A4 CYCLIC AMINE DERIVATIVES 失效
标题翻译：循环胺衍生物
公开(公告)号：EP0288563A4
公开(公告)日：1990-09-26
申请号：EP86905925
申请日：1986-09-30
申请人： EISAI CO., LTD.
发明人： SUGIMOTO, HACHIRO , NAKAMURA, TAKAHARU , KARIBE, NORIO , SAITO, ISAO , HIGURASHI, KUNIZO , YONAGA, MASAHIRO , KANEKO, TAKERU , NAKAZAWA, TAKAHIRO , UENO, MASATAKA , YAMATSU, KIYOMI
IPC分类号： A61K31/445 , A61K31/47 , C07D211/14 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/32 , C07D211/70 , C07D295/02 , C07D295/03 , C07D295/18 , C07D295/192 , C07D401/06 , C07D405/04 , C07D405/06 , C07D409/04
CPC分类号： C07D295/192 , C07D211/16 , C07D211/18 , C07D211/32 , C07D295/03 , C07D401/06 , C07D405/06
摘要： Compounds represented by general formula (I), (wherein A represents substituted or unsubstituted phenyl, pyridyl, thienyl, substituted or unsubstituted naphthyl, tetralyl, quinolyl, benzofuranyl, quinazolyl, benzothienyl, a compound of formula (II) or (III); X represents -CH2-, -C(=O)-, -CH(OH)-, -CH(CH3)- or -CH(CH2N(C2H5)2)-; n represents an integer of 0 to 4; m represents an integer of 1 to 3; Y represents a carbon or nitrogen atom; Z represents -CH2-, -C(=O)-, -CH(OR1)-, (wherein R1 represents H, lower alkyl, acyl, arylalkyl or heteroarylalkyl), -CH(Hal)-, =CH-, a compound of formula (IV), (V) or (VI); Hal represents a halogen atom; a symbol ------ between Y and Z represents a single or double bond, and a group ------ Z$(1,5)$B is bound to the ring at the 3- or 4-position of the above structural formula; B represents a phenyl or naphthyl group optionally substituted by one or two of the same or different substituents selected from among halogen, lower alkyl, and lower alkoxy) and salts. They are effective for retrieval, therapy and prophylaxis of mental troubles accompanying brain blood vessel troubles.

99. 发明公开

EP0183271A3 Lysin derivative and proteinase inhibitor 失效
标题翻译： LYSIN衍生物和蛋白酶抑制剂
公开(公告)号：EP0183271A3
公开(公告)日：1987-05-20
申请号：EP85115142
申请日：1985-11-29
申请人： Okamoto, Shosuke , SHOWA DENKO KABUSHIKI KAISHA
发明人： Okamoto, Shosuke , Okada, Yoshio , Okunomiya, Akiko , Naito, Taketoshi SHOWA DENKO K.K. , Yamada, Morihiko SHOWA DENKO K.K. , Kimura, Yoshio SHOWA DENKO K.K. , Katsuura, Yasuhiro SHOWA DENKO K.K. , Suzuki, Hiroshi SHOWA DENKO K.K. , Ohno, Norio SHOWA DENKO K.K. , Seki, Yumi SHOWA DENKO K.K.
IPC分类号： C07C143/78 , C07C143/80 , C07K05/06 , C07K05/08 , C07D211/16 , C07D211/42 , C07D213/34 , C07D213/40 , C07D215/06 , C07D215/36 , C07D215/08
CPC分类号： C07D213/40 , A61K38/00 , C07C279/18 , C07C2601/14 , C07D211/16 , C07D211/22 , C07D211/42 , C07D211/60 , C07D211/62 , C07D213/34 , C07D215/08 , C07D215/36 , C07D215/42 , C07D295/185 , C07D295/192 , C07D307/91 , C07D311/16 , C07D405/12 , C07K5/06086
摘要： A lysine derivative having the general formula: A-Y-Lys- B (L-form) (A) wherein A represents
or
wherein X and X' independently represent hydrogen, halogen, alkyl, cycloalkyl, alkoxy, aryloxy, dialkylamino, alkylcarbonyl amino, arylcarbonyl amino, and n, is an integer of 3 to 6, n 2 is an integer of 1 to 3, and n 3 is an integer of 0 to 3; Y represents S0 2 or CO; -Lys- represents
B represents NR 1 R 2 , NZW, or tetrahydroquinolyl, wherein R' and R 2 independently represents hydrogen provided that both R' and R 2 cannot be hydrogen at the same time; alkyl substituted with carboxyl, alkoxycarbonyl, phenyl, hydroxyphenyl, or benzoyl; cycloalkyl which may be substituted with arylcarbonyl; cycloalkyl-alkyl which may be substituted with carboxyl, arylcarbonyl, or aralkyloxycar- bonyi; phenyl which may be substituted with halogen, nitro, cyano, trifluoromethyl, alkyl, alkoxy, alkoxycarbonyl, alkoxycarbonylalkyl, phenylalkyl which may be further substituted with dialkylamino, alkylcarbonyl, phenylalkenyl which may be further substituted with dialkylamino, phenoxy, pheny-Icarbonyl which may be further substituted with an amino, dialkylamino, alkoxycarbonyl, or nitro group, pyridylmethyl, phenyl hydroxyalkyl, alkylsulfonyl, or alkoxycarbonyl alkylcarbonyl, coumaryl which may be substituted with alkyl; quinolyl; adamantyl; norbornyl; or tetrahydronaphthyl; and
W is hydrogen; hydroxyl; carboxyl; aminocarbonyl; alkyl; alkoxy carbonyl; phenyl; phenylalkyl which may be substituted with dialkylamino; or phenylcarbonyl which may be substituted with alkoxycarbonyl; or tetrahydroquinolyl; and or the pharmaceutically acceptable salt thereof. This lysine derivative is effective as a proteinase inhibitor.

100. 发明公开

EP0192431A2 Agent for cerebral protection 失效
标题翻译：用于保护大脑。
公开(公告)号：EP0192431A2
公开(公告)日：1986-08-27
申请号：EP86301021.1
申请日：1986-02-14
申请人： KYOWA HAKKO KOGYO KABUSHIKI KAISHA , IHARA CHEMICAL KOGYO KABUSHIKI KAISHA
发明人： Nakamura, Joji , Kubo, Kazuhiro , Ichikawa, Shunji , Takahashi, Hajime , Isozumi, Keisuke , Yamada, Toyofumi
IPC分类号： C07D211/14 , C07D295/10 , C07D211/22 , A61K31/33 , C07D265/30
CPC分类号： C07D265/30 , C07D211/16 , C07D211/22 , C07D279/12 , C07D295/185
摘要： Compounds of the general formula
wherein:

X is halogen or trifluoromethyl;
R, is hydrogen, halogen or trifluoromethyi;
R 2 is hydrogen, methyl or hydroxymethyl;
R 3 is hydrogen or lower alkyl; and
Y is methylene, methylene substituted with a lower alkyl or hydroxyl group, sulfinyl, sulfonyl, oxygen or sulfur, exhibit a cerebral protective effect and are applicable to the treatment of cerebral ischaemia and cerebral hypoxia.

The compounds may be made by acylating a suitable piperidine or morpholine with the appropriate cinnamoyl chloride, and if necessary oxidizing the reaction product.

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