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81. 发明授权

EP1066316B1 CINNAMIC ACID DERIVATIVES HAVING CELL ADHESION MODULATING ACTIVITY 有权
标题翻译：与细胞粘附调节活性ZIMTZSÄURE衍生物
公开(公告)号：EP1066316B1
公开(公告)日：2004-05-12
申请号：EP99909093.9
申请日：1999-03-16
申请人： CELLTECH THERAPEUTICS LIMITED
发明人： ARCHIBALD, Sarah Catherine , HEAD, John Clifford , WARRELLOW, Graham John , PORTER, John Robert
IPC分类号： C07K5/078 , C07D213/82 , C07C233/81 , A61K38/05 , A61K31/44 , A61K31/195
CPC分类号： C07D213/82 , A61K38/00 , C07C233/81 , C07K5/06139 , C07K5/06191 , Y10S514/826 , Y10S514/858 , Y10S514/863 , Y10S514/866 , Y10S514/885 , Y10S514/886 , Y10S514/887
摘要： Compounds of formula (1) are described, wherein L1 is a covalent bond or a linker atom or group; R is a carboxylic acid (-CO¿2?H) or a derivative thereof; R?6 and R7¿ which may be the same or different is each an atom or group -L2(Alk2)tL3R12 in which L?2, L3, Alk2¿ and t are as previously defined and R12 is a hydrogen or halogen atom or an -OR?9, -NR9R10, -NO¿2, -CN, -CO2R?9, -CONR9R10, -COR9, -N(R9)COR10, -N(R9)CSR10, -SO¿2N(R?9)(R10), -N(R9)SO¿2R?9, -N(R9)CON(R10)(R11), -N(R9)CSN(R10)(R11), -N(R9)SO¿2N(R10)(R11), or an optionally substituted aliphatic, heteroaliphatic, cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group provided that R?6 and R7¿ are not both hydrogen atoms and when R7 is a hydrogen atom then R?4 and R5¿ is each a hydrogen or halogen atom or an alkyl, alkoxy or nitro group; and the salts, solvates, hydrates and N-oxides thereof, for use in modulating cell adhesion. The compounds are able to inhibit the binding of alpha 4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.

82. 发明公开

EP1370519A1 SYNTHETIC EXCITATORY AMINO ACIDS 审中-公开
标题翻译： SYNTHETISCHE EXCITATORISCHEAMINOSÄUREN
公开(公告)号：EP1370519A1
公开(公告)日：2003-12-17
申请号：EP02705812.2
申请日：2002-02-12
申请人： ELI LILLY AND COMPANY
发明人： MASSEY, Steven, Marc , MONN, James, Allen , PRIETO, Lourdes , VALLI, Matthew, John
IPC分类号： C07C275/18 , C07C275/34 , C07C335/16 , C07D333/38 , C07C233/52 , C07C233/81 , C07C237/38 , C07C235/54 , C07C233/63 , C07C235/62 , C07D209/42 , C07D217/26 , C07D213/81 , C07D213/82 , C07D241/44 , C07C235/84 , C07D233/90 , C07C229/48 , C07C271/38 , C07C237/14 , C07D263/56
CPC分类号： C07D213/81 , C07C229/48 , C07C233/52 , C07C233/63 , C07C233/81 , C07C235/54 , C07C235/62 , C07C235/84 , C07C237/14 , C07C237/38 , C07C271/38 , C07C275/18 , C07C275/34 , C07C335/16 , C07C2602/18 , C07D209/42 , C07D213/82 , C07D217/26 , C07D233/90 , C07D241/44 , C07D263/56 , C07D277/64 , C07D333/38
摘要： The present invention provides novel compounds that affect certain excitatory amino acid receptors, and are useful in the treatment of neurological disorders and psychiatric disorders.
摘要翻译：本发明提供影响某些兴奋性氨基酸受体的新型化合物，并且可用于治疗神经障碍和精神障碍。

83. 发明公开

EP1289936A1 SUBSTITUTED STILBENES AS GLUCOSE UPTAKE ENHANCERS 有权
标题翻译：取代芪葡萄糖录音抑制剂
公开(公告)号：EP1289936A1
公开(公告)日：2003-03-12
申请号：EP01941753.4
申请日：2001-06-01
申请人： TELIK, INC.
发明人： PATTERSON, John , PARK, Jeong, Weong , LUM, Robert, T. , SPEVAK, Wayne, R.
IPC分类号： C07C237/42 , C07C237/40 , C07C233/81 , C07C235/56 , C07C309/61 , A61K31/196 , A61K31/24 , C07C231/02
CPC分类号： C07C233/81 , C07C233/88 , C07C235/56 , C07C235/64 , C07C235/84 , C07C237/40 , C07C237/42 , C07C309/51 , C07C309/61 , C07D317/60
摘要： The present invention relates to chemical compounds, pharmaceutical compositions comprising said compounds, methods of treatment administering these compounds to mammalian hosts, and processes for their preparation. Specifically, the invention relates to a means to enhance insulin-dependent glucose uptake. More specifically, the invention concerns compounds and pharmaceutical compositions that activate the insulin receptor kinase, which leads to increased sensitivity to insulin and an increase in glucose uptake, as well as processes for the preparation of the compounds. The invention also specifically concerns methods for treating humans with hyperglycemia, especially for the treatment of Type II diabetes.

84. 发明公开

EP0661261A1 Phenyl or phenylalkyl substituted naphtalene derivatives having retinoid-like activity as well as anti-tumor activities 失效
标题翻译：苯基苯基烷基取代基Naphthalenderivate mitRetinoidähnlicherAktivitätund Antitumor Wirkungen。
公开(公告)号：EP0661261A1
公开(公告)日：1995-07-05
申请号：EP95100032.2
申请日：1995-01-02
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： Starrett Jr., John E. , Mansuri, Muzammil N. , Tortolani, David R.
IPC分类号： C07C235/84 , C07C233/81 , C07C69/76 , C07C63/66 , C07C63/33 , C07C327/48 , A61K31/165 , A61K31/19
CPC分类号： C07C63/72 , C07C63/331 , C07C69/76 , C07C233/81 , C07C235/66 , C07C327/48
摘要： This invention relates to a retinoid compound of formula I

in which

Y is -CO-NH-, -CR²=CR³-, -CO-O-, -O-CO-, -C(=S)-NH-, -C≡C-, -O-CH₂-, -CH₂-O-, or -CH₂-CH₂-;
A is -(CH₂) t - or a bond;
Q is phenyl optionally substituted with one to three same or different C₁₋₆alkyl, C₁₋₆alkoxy, halogen, or -CO₂R⁴;
R¹ is -CO₂Z, -CONHR⁵, C₁₋₆alkyl, -CH₂OH, or -CHO;
R², R³, R⁴, R⁵, and Z are independently hydrogen or C₁₋₆alkyl;
t is one to six.
摘要翻译：本发明涉及其中Y是-CO-NH-，-CR 2 = CR 3 - ， - CO-O-，-O-CO-，-C（ = S）-NH-，-C元素C，-O-CH 2 - ， - CH 2 -O-或-CH 2 -CH 2 - ; A是 - （CH 2）t - 或键; Q是任选被一至三个相同或不同的C 1-6烷基，C 1-6烷氧基，卤素或-CO 2 R 4取代的苯基; R 1是-CO 2 Z，-CONHR 5，C 1-6烷基，-CH 2 OH或-CHO; R 2，R 3，R 4，R 5和Z独立地是氢或C 1-6烷基; t是一到六。

85. 发明授权

EP0279633B1 Anticonvulsant agents 失效
标题翻译：有毒物质
公开(公告)号：EP0279633B1
公开(公告)日：1993-04-07
申请号：EP88301285.8
申请日：1988-02-17
申请人： ELI LILLY AND COMPANY
发明人： Beedle, Edward Earl , Robertson, David Wayne
IPC分类号： C07C233/65 , C07C233/67 , C07C323/00 , C07D233/61 , A61K31/165 , A61K31/415 , C07C233/81
CPC分类号： C07D231/12 , C07C233/65 , C07C255/00 , C07D233/56 , C07D249/08

86. 发明授权

EP0322255B1 N-acyl-N-naphthoylglycines as aldose reductase inhibitors 有权转让
标题翻译： N-酰基-N-萘甲酰甘氨酸作为醛糖还原酶抑制剂
公开(公告)号：EP0322255B1
公开(公告)日：1993-03-24
申请号：EP88312313.5
申请日：1988-12-23
申请人： AMERICAN HOME PRODUCTS CORPORATION
发明人： Wrobel, Jay E. , Bauman, John G. , Sestanj, Kazimir
IPC分类号： C07C233/77 , C07C233/81 , C07C233/65 , C07C327/38 , A61K31/195
CPC分类号： C07C237/22 , C07C43/225 , C07C43/23 , C07C65/24 , C07C235/66 , C07C271/64 , C07C327/48

87. 发明公开

EP0360417A2 Derivatives of 4-fluoroanthranilic acid and their use as fungicides 失效
标题翻译：推出von 4-Fluoroanthranilsäureund deren Verwendung als Fungizide。
公开(公告)号：EP0360417A2
公开(公告)日：1990-03-28
申请号：EP89308459.0
申请日：1989-08-21
申请人： SCHERING AGROCHEMICALS LIMITED
发明人： Richards, Ian Christopher , Wright, Brian John , Parsons, John Henry , Baillie, Alister Cameron
IPC分类号： C07C233/81 , A01N37/46 , C07D265/22 , A01N43/86 , C07C229/56 , A01N37/44 , C07C237/30 , C07C275/42 , A01N47/30 , C07D239/96 , A01N43/48
CPC分类号： C07D265/22 , A01N37/44 , A01N37/46 , A01N41/08 , A01N43/16 , A01N43/38 , A01N43/54 , A01N43/86 , A01N47/20 , A01N47/30 , A01N55/00 , C07C229/56 , C07C233/54 , C07C233/87 , C07C237/08 , C07C237/40 , C07C251/08 , C07C251/24 , C07C271/28 , C07C275/42 , C07C317/48 , C07D209/38 , C07D239/96 , C07D265/26 , C07F7/0818
摘要： Compounds of formula I
where A, B and R¹⁻⁶ are as defined in the description have pesticidal and especially fungicidal activity. Many of the compounds are novel and these compounds per se , form part of the invention.
摘要翻译：式I的化合物其中A，B和R 1〜6如描述中所定义，具有杀虫活性，特别是杀真菌活性。许多化合物是新颖的，这些化合物本身是本发明的一部分。

88. 发明公开

EP0333282A1 Preparation of optically active N-substituted alanine herbicides 失效
标题翻译： Herstellung von optisch aktiven N-substitutionierten Alaninherbiciden。
公开(公告)号：EP0333282A1
公开(公告)日：1989-09-20
申请号：EP89200631.3
申请日：1989-03-10
申请人： SHELL INTERNATIONALE RESEARCH MAATSCHAPPIJ B.V.
发明人： Miedema, Alle
IPC分类号： C07C233/81 , C07C231/00
CPC分类号： C07C233/83 , C07C231/18
摘要： Optically active compounds of formula I
wherein
Y and Z each independently is hydrogen, chlorine or fluorine;
W is hydrogen, alkyl, haloalkyl, alkenyl, cycloalkyl, aryl, alkaryl, aralkyl or a group -N=CR¹R² in which R¹ and R² each independently is hydrogen, alkyl, aryl, aralkyl, alkaryl or alkenyl, or R¹ and R² together form an alkylene group optionally interupted by one or more hetero atoms; and
R is benzoyl,
may be prepared by benzoylating a starting compound of formula I, where R is hydrogen and possessing the R -configuration at C² , with a benzoylating agent in the presence of a solvent and a tertiary amine.
摘要翻译：式I的光学活性化合物其中Y和Z各自独立地是氢，氯或氟; W是氢，烷基，卤代烷基，烯基，环烷基，芳基，烷芳基，芳烷基或基团-N = CR 1 R 2，其中R 1和R 2各自独立地是氢，烷基，芳基芳烷基，烷芳基或链烯基，或R 1和R 2一起形成任选地被一个或多个杂原子中间的亚烷基; 并且R是苯甲酰基，可以通过在溶剂和叔胺的存在下，用苯甲酰化剂苯甲酰化式Ⅰ的起始化合物，其中R是氢并且在C 2上具有R-构型。

89. 发明公开

EP0298135A1 Phenylalanine derivative and proteinase inhibitor 失效
标题翻译：苯丙氨酸蛋白酶抑制剂冯蛋白酶。
公开(公告)号：EP0298135A1
公开(公告)日：1989-01-11
申请号：EP87104691.8
申请日：1987-03-30
申请人： Okamoto, Shosuke , SHOWA DENKO KABUSHIKI KAISHA
发明人： Okamoto, Shosuke , Okada, Yoshio , Okunomiya, Akiko , Naito, Taketoshi , Kimura, Yoshio , Yamada, Morihiko , Ohno, Norio , Katsuura, Yasuhiro , Nojima, Hiroshi , Shishikura, Takashi
IPC分类号： C07C273/04 , C07C233/76 , C07C233/81 , C07C257/00 , C07D213/32 , C07D213/40 , C07D213/75 , C07D295/182
CPC分类号： C07D213/40 , A61K38/00 , C07C279/14 , C07C279/18 , C07D211/32 , C07D213/75 , C07K5/06078
摘要： A phenylalanine derivative having the formula (I):
X represents hydrogen, (b) hydroxy, (c) nitro, or (d) C₁-C₄ alkyloxy which may be substituted with phenyl;
Y represents
wherein R¹ and R² are, independently, (a) hydrogen, provided that both R¹ and R² are not hydrogen at the same time; (b) phenyl, which may be substituted with (i) phenylcarbonyl, (ii) C₁-C₄ alkylcarbonyl, (iii) C₁-C₄ alkyl, which may be further substituted with C₁-C₄ alkoxycarbonyl or hydroxycarbonyl, (iv) C₂-C₅ alkenyl, which may further be substituted with C₁-C₄ alkoxycarbonyl, (v) trifluoromethyl; (c) pyridyl, which may be substituted with C₁-C₄ alkoxy; (d) C₁-C₄ alkyl, which may be substituted with (i) hydroxy, (ii) C₁-C₄ alkoxycarbonyl, (iii) pyridyl, or (iv) phenyl, which may be further substituted with C₁-C₄ alkylaminocarbonyl; (e) C₅-C₇ cycloalkyl, which may be substituted with C₁-C₄ alkyl; or (f) R¹ and R² may form, with the nitrogen atom attached thereto, (i) piperidino, which may be substituted with phenylcarbonyl or (ii) pyrrolidyl, which may be substituted with C₁-C₄ alkoxycarbonyl; or a pharmaceutically acceptable salt thereof.
This phenylalanine derivative is effective as a proteinase inhibitor.
摘要翻译：具有式（I）的苯丙氨酸衍生物： X表示氢，（b）羟基，（c）硝基或（d）可被苯基取代的C 1 -C 4烷氧基; Y表示，其中R 1和R 2独立地为（a）氢，条件是R 1和R 2不同时为氢; （b）苯基，其可被（i）苯基羰基取代，（ii）C 1 -C 4烷基羰基，（iii）可以被C 1 -C 4烷氧基羰基或羟基羰基进一步取代的C 1 -C 4烷基，（iv）C 2 -C 5 烯基，其可以进一步被C 1 -C 4烷氧基羰基取代，（v）三氟甲基; （c）可被C 1 -C 4烷氧基取代的吡啶基; （d）可被（i）羟基，（ⅱ）C 1 -C 4烷氧基羰基，（ⅲ）吡啶基或（ⅳ）苯基取代的C 1 -C 4烷基，其可进一步被C 1 -C 4烷基氨基羰基取代; （e）可被C 1 -C 4烷基取代的C 5 -C 7环烷基; 或（f）R 1和R 2可以与其连接的氮原子形成，（i）可被苯基羰基取代的哌啶子基或可以被C 1 -C 4烷氧基羰基取代的（ⅱ）吡咯烷基; 或其药学上可接受的盐。该苯丙氨酸衍生物作为蛋白酶抑制剂是有效的。

90. 发明公开

EP0284632A1 Phenylalanine derivative and proteinase inhibitor 失效
标题翻译：苯丙氨酸蛋白酶抑制剂冯蛋白酶。
公开(公告)号：EP0284632A1
公开(公告)日：1988-10-05
申请号：EP87104690.0
申请日：1987-03-30
申请人： Okamoto, Shosuke , SHOWA DENKO KABUSHIKI KAISHA
发明人： Okamoto, Shosuke , Okada, Yoshio , Okunomiya, Akiko , Naito, Taketoshi SHOWA DENKO KABUSHIKI KAISHA , Kimura, Yoshio SHOWA DENKO KABUSHIKI KAISHA , Yamada, Morihiko SHOWA DENKO KABUSHIKI KAISHA , Ohno, Norio SHOWA DENKO KABUSHIKI KAISHA , Katsuura, Yasuhiro SHOWA DENKO KABUSHIKI KAISHA , Nojima, Hiroshi SHOWA DENKO KABUSHIKI KAISHA , Shishikura, Takashi SHOWA DENKO KABUSHIKI KAISHA
IPC分类号： C07C233/65 , C07C233/67 , C07C233/76 , C07C233/77 , C07C233/81 , C07C233/57 , C07D213/75 , C07D213/80 , C07D213/643 , C07D213/30
CPC分类号： C07D213/643 , C07D211/60 , C07D211/62 , C07D213/75 , C07D213/80 , C07D233/88 , C07D239/42 , C07D257/06 , C07D277/46 , C07D295/185
摘要： A phenylalanine derivative having the formula (I):
wherein A represents (a) H 2 N-, (b)
or
B represents (a)
(b)
or
wherein m is 0, 1, or 2 and n is 3, 4, or 5;

X represents (a) hydroxy, (b) nitro, (c) amino, (d) phenoxy which may be substituted with (i) halogen or (ii) nitro, (e) C 1 -C 4 alkyloxy which may be substituted with (i) phenyl or (ii) benzoyl, (f) benzoyl, (g) pyridyloxy which may be substituted with (i) halogen or (ii) nitro, or (h) C 1 -C 4 alkyl which may be substituted with halogen;
Y represents
or -OR 3 wherein
R 1 and R 2 are independently (a) hydrogen, (b) phenyl which may be substituted with (i) benzoyl, (ii) C 1 -C 4 alkylcarbonyl, (iii) C 1 -C 4 alkyl which may be further substituted with C 1 -C 4 alkoxycarbonyl or hydroxycarbonyl, (iv) C 2 -Cs alkenyl which may be further substituted with hydroxycarbonyl or C 1 -C 4 alkoxycarbonyl, (v) C 1 -C 4 alkoxycarbonyl, or (vi) amidino, (c) pyridyl which may be substituted with halogen or carboxyl (d) imidazolyl, (e) pyrimidyl, (f) tetrazolyl, (g) thiazolyl which may be substituted with C,-C 4 alkyl which may be further substituted with C 1 -C 4 alkoxycarbonyl, (h) C 1 -C 6 alkyl which may be substituted with C 1 -C 4 alkoxy, C 1 -C 4 alkoxycarbonyl, phenyl, or benzoyl, (i) C S -C 7 cycloalkyl which may be substituted with C 1 -C 4 alkoxycarbonyl or (j) R' and R 2 may form, with the nitrogen atom attached thereto, (i) pyperazyl which may be substituted on the nitrogen atom with C 1 -C 4 alkyl which may be further substituted with phenyl, (ii) piperidino which may be substituted with carboxyl or C 1 -C 4 alkoxycarbonyl, (iii) pyrrolidyl which may be substituted with C 1 -C 4 alkoxycarbonyl, or (iv) morpholyl; and
R 3 represents (a) hydrogen, (b) C 1 -C 6 alkyl which may be substituted with (i) C 1 -C 4 alkoxy, (ii) phenyl, or (iii) pyridyl, or (c) pyridyl; or a pharmaceutically acceptable acid salt thereof.

This phenylalanine derivative is effective as a proteinase.
摘要翻译：具有式（I）的苯丙氨酸衍生物：其中m为0,1或2，n为3,4或5; X表示（a）羟基，（b）硝基，（c）氨基，（d）可被（i）卤素或（ii）硝基取代的苯氧基，（e）可被（i ）苯基或（ii）苯甲酰基，（f）苯甲酰基，（g）可被（i）卤素或（ii）硝基取代的吡啶氧基，或（h）可被卤素取代的C 1 -C 4烷基; Y表示或-OR 3，其中R 1和R 2独立地为（a）氢，（b）可被（i）苯甲酰基取代的苯基，（ii）C 1 -C 4烷基羰基，（iii）可以被C1-C4烷氧基羰基或羟基羰基进一步取代的C1-C4烷基，（iv）可以被羟基羰基或C1-C4烷氧基羰基进一步取代的C2-C5烯基，（v）C1-C4烷氧基羰基或（ vi）脒基，（c）可以被卤素或羧基取代的吡啶基（d）咪唑基，（e）嘧啶基，（f）四唑基，（g）可被可以被C 1 -C 4烷基取代的噻唑基， C 1 -C 4烷氧基羰基，（h）可被C 1 -C 4烷氧基取代的C 1 -C 6烷基，C 1 -C 4烷氧基羰基，苯基或苯甲酰基，（i）可被C 1 -C 4烷氧基羰基取代的C 5 -C 7环烷基或（ j）R 1和R 2可以与其连接的氮原子形成，（i）可以被氮原子取代的可以被苯基进一步取代的C 1 -C 4烷基的哒嗪基，（ii）可被羧基或C 1 -C 4烷氧基羰基取代的哌啶子基，（iii）可被C 1 -C 4烷氧基羰基取代的吡咯烷基，或（iv）吗啉基; （ⅰ）C 1 -C 4烷氧基，（ⅱ）苯基或（ⅲ）吡啶基或（c）吡啶基）取代的C 1 -C 6烷基，或其药学上可接受的酸盐。该苯丙氨酸衍生物作为蛋白酶有效。

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