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1. 发明公开

EP3400213A1 INHIBITORS OF THE PD-1/PD-L1 PROTEIN/PROTEIN INTERACTION 审中-公开
公开(公告)号：EP3400213A1
公开(公告)日：2018-11-14
申请号：EP17700176.5
申请日：2017-01-09
申请人： Rijksuniversiteit Groningen
发明人： DÖMLING, Alexander
IPC分类号： C07D211/34 , C07C233/77 , C07D213/64 , A61K31/44 , A61P35/00
CPC分类号： C07D211/34 , C07C217/58 , C07D211/60 , C07D213/69 , C07D233/36 , C07D417/12
摘要： The present invention provides novel compounds of formula (I) that are useful as inhibitors of the PD-1/PD-L1 protein/ protein interaction.

2. 发明公开

EP2419431A1 DERIVES DE N-[(7-AZA-BICYCLO[2.2.1]HEPT-1-YL)-ARYL-METHYL]-BENZAMIDE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE 审中-公开
标题翻译： [（7-氮杂双环[2.2.1]庚-1-基）芳基甲基]苯甲酰胺，其制备及其治疗用途 - N中的衍生物
公开(公告)号：EP2419431A1
公开(公告)日：2012-02-22
申请号：EP10723665.5
申请日：2010-04-13
申请人： SANOFI
发明人： DARGAZANLI, Gihad , ESTENNE-BOUHTOU, Geneviève
IPC分类号： C07D487/08 , C07D207/14 , C07C233/77 , A61K31/407 , A61P25/00
CPC分类号： C07D487/08 , C07D207/14
摘要： The inventions relates to the compounds of formula (I) where: R is a hydrogen atom or a group selected from the (C
1 d- C
6 )alkyl and (C
3 -C
7 )-cycloalkyl groups, optionally substituted by one or more groups independently selected from a fluorine atom, the (C
3 -C
7 )-cycloalkyl, (C
2 -C
4 )alkenyl, phenyl, (C
1 -C
6 )alkoxy, and hydroxy groups; the phenyl group being optionally substituted by one or more (C
1 -C
6 )alkoxy groups; R
1 is a phenyl group optionally substituted by one or more substituants independently selected from halogen atoms, the (C
1 -C
6 )alkyl, (C
1 -C
6 )alkoxy, halo-(C
1 C
6 )alkyl, hydroxy, halo-(C
1 -C
6 )alkoxy, (C
1 -C
6 )alkyl-thio, and (C
1 -C
6 )alkyl-SO
2 groups; R
2 is one or more substituants selected from hydrogen atoms, halogen atoms, the halo-(C
1 -C
6 )alkyl, (C
1 -C
6 )alkyl, (C
3 -C
7 )cycloalkyl, (C
3 -C
7 )-cycloalkyl-(C
1 -C
3 )alkyl, (C
1 C
6 )alkoxy, (C
1 C
6 )alkyl-thio, and (C
1 -C
6 )alkyl-SO
2 groups; in the form of a base or an addition salt to an acid. The invention further relates to the use thereof in therapy and to a method for synthesizing same.

3. 发明公开

EP1745011A2 MODULATORS OF CANNABINOID RECEPTORS 有权
标题翻译：大麻素受体调节剂
公开(公告)号：EP1745011A2
公开(公告)日：2007-01-24
申请号：EP05708399.0
申请日：2005-02-21
申请人： UCL Biomedica plc
发明人： OKUYAMA, Masahiro,Mitsubishi Pharma Corporation , SELWOOD, David, Wolfson Inst. for Biomed. Research , VISINTIN, Cristina, Wolfson Inst. for Biomed. Res. , BAKER, David,Department of Neuroinflammation , PRYCE, Gareth, Department of Neuroinflammation
IPC分类号： C07C233/68 , C07C233/77 , C07C63/04 , C07C69/78 , A61K31/167 , A61K31/192 , A61K31/216 , A61K31/235
CPC分类号： C07C235/42 , A61K31/165 , C07C69/76 , C07C69/78 , C07C233/11 , C07C233/65 , C07C233/66 , C07C233/69 , C07C235/34 , C07C235/78 , C07C235/84 , C07C237/32 , C07C237/38 , C07C237/42 , C07C255/41 , C07C255/44
摘要： The present invention relates to a compound of formula I, or a pharmaceutically acceptable salt thereof, wherein Z is OR 1 or NR 1 R 2 wherein each of R 1 and R 2 is independently H, or a hydrocarbyl group;X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO 2 -alkyl, alkenyl, CN, NH 2 , hydroxy, halo, alkoxy, CF 3 and nitro; Y is a polar functional group selected from OH, NO 2 CN, COR 3 , COOR 3 , NR 3 R 4 , CONR 3 R 4 , SO 3 H, SO 2 -R 3 , SO 2 NR 3 R 4 and CF 3 , where each of R 3 and R 4 is independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH 2 ) n where n is 0, 1, 2, 3, 4 or 5; with the proviso that: (i) when A is phenyl, n is 0, and Z is OH, X-Y is other than meta -C‰¡C-(CH 2 ) 2 CO 2 H, meta -C‰¡C-(CH 2 ) 2 OH, meta -C‰¡C-(CH 2 ) 2 CO 2 Me, meta- (CH 2 ) 4 CO 2 H, ortho -CH 2 CO 2 H, ortho -(CH 2 ) 2 CO 2 H and ortho -(CH 2 ) 4 CO 2 H; and (ii) when A is phenyl, n is 0, and Z is OMe, X-Y is other than meta -C‰¡C-(CH 2 ) 4 OH. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors.

4. 发明公开

EP1501786A1 BIPHENYLCARBOXAMIDE 审中-公开
标题翻译：联苯甲酰
公开(公告)号：EP1501786A1
公开(公告)日：2005-02-02
申请号：EP03725044.6
申请日：2003-04-16
申请人： Bayer CropScience AG
发明人： DUNKEL, Ralf , ELBE, Hans-Ludwig , RIECK, Heiko , MARKERT, Robert , WACHENDORFF-NEUMANN, Ulrike , MAULER-MACHNIK, Astrid , KUCK, Karl-Heinz , KUGLER, Martin , JAETSCH, Thomas
IPC分类号： C07C233/77 , C07D319/16 , C07D317/46 , A01N43/30
CPC分类号： A01N43/30 , A01N43/32 , A01N43/56 , A01N43/78 , C07D317/58 , C07D319/20 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12
摘要： Disclosed are novel biphenyl carboxamides of formula (I), in which R1, R2, m, n, R3, Y, and A have the meanings indicated in the description, several methods for producing said substances, the use thereof for controlling undesired microorganisms, and novel intermediate products and the production thereof.
摘要翻译：公开了式（I）的新颖联苯甲酰胺，其中R 1，R 2，m，n，R 3，Y和A具有说明书中指出的含义，几种生产所述物质的方法，其用于防治不需要的微生物，和新颖的中间产品及其生产。

5. 发明授权

EP0322255B1 N-acyl-N-naphthoylglycines as aldose reductase inhibitors 失效
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

6. 发明授权

EP0260555B1 Benzo-fused cycloalkane and oxa- and thia-, cycloalkane trans-1,2-diamine derivatives 失效
标题翻译：苯并呋喃环和烷氧基 - 和环 - 环己烷衍生的1,2-二胺衍生物
公开(公告)号：EP0260555B1
公开(公告)日：1992-04-22
申请号：EP87113010.0
申请日：1987-09-05
申请人： THE DU PONT MERCK PHARMACEUTICAL COMPANY
发明人： Pennev, Penio , Rajagopalan, Parthasarathi , Scribner, Richard Merrill
IPC分类号： C07C233/77 , C07D295/125 , C07D311/94 , C07D335/06 , A61K31/16 , A61K31/33
CPC分类号： C07D295/135 , C07C233/41 , C07C323/41 , C07C2602/10

7. 发明授权

EP0306827B1 Amide compounds, process for preparing the same, and composition for activating gastric motor function containing the same 失效
标题翻译：酰胺化合物，其制备方法以及用于活化含有该组合物的气体电动机功能的组合物
公开(公告)号：EP0306827B1
公开(公告)日：1991-09-04
申请号：EP88114257.4
申请日：1988-09-01
申请人： Hokuriku Pharmaceutical Co.,Ltd
发明人： Itoh, Yasuo , Kato, Hideo , Koshinaka, Eiichi , Ogawa, Nobuo , Nishino, Hiroyuki , Sakaguchi, Jun
IPC分类号： C07C233/77 , C07C255/50 , C07C311/15 , C07D295/08 , C07D317/68 , C07C231/00 , A61K31/165 , A61K31/18 , A61K31/33
CPC分类号： C07D295/088 , C07C255/00 , C07D317/68

8. 发明公开

EP0166571A3 Peracid and bleach activator compounds and use thereof in cleaning compositions 失效
标题翻译： PERACID和漂白活化剂化合物及其在清洁组合物中的应用
公开(公告)号：EP0166571A3
公开(公告)日：1989-07-19
申请号：EP85304373.5
申请日：1985-06-19
申请人： THE PROCTER & GAMBLE COMPANY , Procter & Gamble Limited
发明人： Hardy, Frederick Edward , Ingram, Barry Thomas
IPC分类号： C07C409/24 , C07C409/40 , C11D3/39 , C07C69/60 , C07C69/76 , C07C233/77 , C07C233/90 , C07C291/04 , C07C305/00 , C07C309/24 , C07C317/00
CPC分类号： C07C409/42 , C07C409/24 , C11D3/3917 , C11D3/392 , C11D3/3945 , F16B15/0038
摘要： Per-acids and per-acid precursor compounds of the general type RXAOOH and RXAL, wherein R is a hydrocarbyl group, X is a hetero-atom, A is a carbonyl bridging group and L is a leaving group, especially oxybenzenesulfonate, are useful bleaching compounds for fabrics. Laundry products containing same are disclosed.

9. 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。

10. 发明公开

EP2177503A1 MODULATORS OF CANNABINOID RECEPTORS 失效转让
标题翻译：大麻素受体的调节因子
公开(公告)号：EP2177503A1
公开(公告)日：2010-04-21
申请号：EP09012361.3
申请日：2005-02-21
申请人： UCL Business PLC
发明人： Okuyama, Masahiro , Baker, David , Pryce, Gareth , Selwood, David , Visintin, Cristina
IPC分类号： C07C233/68 , C07C233/77 , C07C63/04 , C07C69/78 , A61K31/167 , A61K31/192 , A61K31/216 , A61K31/235
CPC分类号： C07C235/42 , A61K31/165 , C07C69/76 , C07C69/78 , C07C233/11 , C07C233/65 , C07C233/66 , C07C233/69 , C07C235/34 , C07C235/78 , C07C235/84 , C07C237/32 , C07C237/38 , C07C237/42 , C07C255/41 , C07C255/44
摘要： The present invention relates to a compound of formula I, or a pharmaceutically acceptable salt thereof,

wherein Z is OR 1 or NR 1 R 2 wherein each of R 1 and R 2 is independently H, or a hydrocarbyl group;X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO 2 -alkyl, alkenyl, CN, NH 2 , hydroxy, halo, alkoxy, CF 3 and nitro;
Y is a polar functional group selected from OH, NO 2 CN, COR 3 , COOR 3 , NR 3 R 4 , CONR 3 R 4 , SO 3 H, SO 2 -R 3 , SO 2 NR 3 R 4 and CF 3 , where each of R 3 and R 4 is independently H or a hydrocarbyl group;
A is an aryl or heteroaryl group, each of which may be optionally substituted; and
B is (CH 2 ) n where n is 0, 1, 2, 3, 4 or 5;

with the proviso that:
(i) when A is phenyl, n is 0, and Z is OH, X-Y is other than meta -C≡C-(CH 2 ) 2 CO 2 H, meta -C≡C-(CH 2 ) 2 OH, meta -C≡C-(CH 2 ) 2 CO 2 Me, meta- (CH 2 ) 4 CO 2 H, ortho -CH 2 CO 2 H, ortho -(CH 2 ) 2 CO 2 H and ortho -(CH 2 ) 4 CO 2 H; and
(ii) when A is phenyl, n is 0, and Z is OMe, X-Y is other than meta -C≡C-(CH 2 ) 4 OH.
Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐，其中Z为OR1或NR1R2，其中R1和R2各自独立地为H或烃基; X为亚烷基，亚烯基或亚炔基，其各自可任选被一个或多个选自烷基，COOH，CO 2 - 烷基，烯基，CN，NH 2，羟基，卤素，烷氧基，CF 3和硝基的取代基取代; Y是选自OH，NO 2 CN，COR 3，COOR 3，NR 3 R 4，CONR 3 R 4，SO 3 H，SO 2 -R 3，SO 2 NR 3 R 4和CF 3的极性官能团，其中R 3和R 4各自独立地为H或烃基; A是芳基或杂芳基，它们中的每一个可以任选被取代; 并且B是（CH 2）n，其中n是0,1,2,3,4或5; 条件是：（i）当A为苯基，n为0且Z为OH时，XY不是间位C≡C-（CH 2）2 CO 2 H，间位C≡C-（CH 2）2 OH， C≡C-（CH2）2CO2Me，间 - （CH2）4CO2H，邻CH2CO2H，邻 - （CH2）2CO2H和邻 - （CH2）4CO2H; 和（ii）当A是苯基时，n是0，并且Z是OMe，X-Y不同于间位C≡C-（CH 2）4 OH。本发明的其他方面涉及这些化合物在制备用于治疗肌肉疾病，胃肠疾病或用于控制痉挛状态或震颤的药物中的用途。

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