公开(公告)号：EP3408253A1

公开(公告)日：2018-12-05

申请号：EP17707704.7

申请日：2017-01-27

Applicant: Acatechol, Inc.

Inventor： AHN, Byung Jun ,  LIPSHUTZ, Bruce, H. ,  NGUYEN, Sam, L. ,  LINSTADT, Roscoe

IPC: C07C205/43 ,  A61K6/00 ,  C09D5/00 ,  C09D7/12

CPC classification number: C07F9/12 ,  A61K6/0017 ,  A61K6/0052 ,  A61K6/0058 ,  A61K6/0094 ,  B05D3/002 ,  B05D3/10 ,  B05D3/107 ,  C07C69/01 ,  C07C205/42 ,  C07C205/43 ,  C07C235/06 ,  C07C235/20 ,  C07C271/16 ,  C07D217/16 ,  C07F7/0896 ,  C07F9/62 ,  C08K5/107 ,  C08K5/13 ,  C09D5/002 ,  C09D7/63 ,  A61K6/0023 ,  C08L33/10 ,  A61K6/0029

Abstract: wherein the variables EG, EG1, SP1, SP2, SP3, Ar and BG are as defined herein. In another embodiment, the application discloses a method for forming a coating on a surface of a substrate using the surface binding compound of the Formula I or Formula II.

公开(公告)号：EP2408750A1

公开(公告)日：2012-01-25

申请号：EP10710749.2

申请日：2010-03-19

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： DEMATTEI, John ,  LOOKER, Adam, R. ,  NEUBERT-LANGILLE, Bobbianna ,  TRUDEAU, Martin ,  ROEPER, Stefanie ,  RYAN, Michael, P. ,  YAP, Dahrika, Milfred Lao ,  KRUEGER, Brian, R. ,  GROOTENHUIS, Peter, D.J. ,  VAN GOOR, Frederick, F. ,  BOTFIELD, Martyn, C. ,  ZLOKARNIK, Gregor

IPC: C07D215/233

CPC classification number: C07C205/43 ,  C07C68/02 ,  C07C69/96 ,  C07C201/08 ,  C07C213/02 ,  C07C229/66 ,  C07D215/233 ,  C07D215/56 ,  G01N33/5041 ,  G01N33/6872 ,  Y02P20/55

Abstract: The invention provides a process for the preparation of a compound of Formula 1; comprising coupling a carboxylic acid of Formula 2; with an aniline of Formula 3; in the presence of a coupling agent.

公开(公告)号：EP1404324B1

公开(公告)日：2007-12-05

申请号：EP02744314.2

申请日：2002-06-11

Applicant: Xenoport, Inc.

Inventor： GALLOP, Mark, A. ,  CUNDY, Kenneth, C. ,  ZHOU, Cindy, X. ,  QIU, Fayang, G. ,  YAO, Fenmei ,  XIANG, Jia-Ning ,  OLLMAN, Ian, R.

IPC: A61K31/44 ,  A61K31/335 ,  A61K31/27 ,  A61K31/225 ,  A61K31/195 ,  A61P25/00 ,  C07D213/02 ,  C07D317/00 ,  C07C205/00 ,  C07C229/00 ,  C07C261/00 ,  C07C269/00 ,  C07C271/00

CPC classification number: C07C201/12 ,  A61K31/19 ,  A61K31/197 ,  A61K31/22 ,  A61K31/27 ,  A61K31/341 ,  A61K47/54 ,  A61K47/555 ,  C07C271/22 ,  C07C323/58 ,  C07C2601/14 ,  C07D213/79 ,  C07D213/80 ,  C07D267/06 ,  C07D307/33 ,  C07D307/58 ,  C07D307/60 ,  C07D317/32 ,  C07D317/40 ,  C07C205/43

Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using phannaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.

公开(公告)号：EP1390343A4

公开(公告)日：2005-06-22

申请号：EP02728253

申请日：2002-05-29

Applicant: CHEBIGEN CO LTD

Inventor： UM SOO-JONG ,  SIN HONG-SIG ,  RHO YOUNG-SOY ,  PARK SI-HO ,  KWON YOUN-JA ,  PARK MYOUNG-SOON ,  HAN HYE-SOOK ,  KIM SO-MI ,  KIM DONG-MYONG ,  OH DEOK-KUN ,  PARK JONG-SUP ,  BAE TAE-SUNG

IPC: C07C235/78 ,  A61K31/165 ,  A61K31/167 ,  A61K31/195 ,  A61K31/222 ,  A61K31/223 ,  A61K31/225 ,  A61K31/232 ,  A61K31/27 ,  A61K31/66 ,  A61K31/661 ,  A61P35/00 ,  C07C205/43 ,  C07C233/10 ,  C07C233/28 ,  C07C233/33 ,  C07C233/44 ,  C07C233/55 ,  C07C403/20 ,  C07F9/12

CPC classification number: C07C403/20 ,  C07B2200/09 ,  C07C205/43 ,  C07C233/10 ,  C07C233/28 ,  C07C233/33 ,  C07C233/44 ,  C07C233/55 ,  C07C2601/16 ,  C07F9/12

公开(公告)号：EP1404324A4

公开(公告)日：2004-12-22

申请号：EP02744314

申请日：2002-06-11

Applicant: XENOPORT INC

Inventor： GALLOP MARK A ,  CUNDY KENNETH C ,  ZHOU CINDY X ,  QIU FAYANG G ,  YAO FENMEI ,  XIANG JIA-NING ,  OLLMAN IAN R

IPC: A61K9/22 ,  A61K9/26 ,  A61K31/19 ,  A61K31/197 ,  A61K31/22 ,  A61K31/27 ,  A61K31/341 ,  A61K45/00 ,  A61K47/48 ,  A61P1/00 ,  A61P1/06 ,  A61P19/02 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/32 ,  A61P39/02 ,  A61P43/00 ,  C07C205/43 ,  C07C271/22 ,  C07C323/58 ,  C07D213/80 ,  C07D267/06 ,  C07D307/58 ,  C07D317/22 ,  C07D317/32 ,  C07D317/40 ,  A61K31/44 ,  A61K31/195 ,  A61K31/225 ,  A61K31/335 ,  C07C205/00 ,  C07C229/00 ,  C07C261/00 ,  C07C269/00 ,  C07C271/00 ,  C07D213/02 ,  C07D317/00

CPC classification number: C07C201/12 ,  A61K31/19 ,  A61K31/197 ,  A61K31/22 ,  A61K31/27 ,  A61K31/341 ,  A61K47/54 ,  A61K47/555 ,  C07C271/22 ,  C07C323/58 ,  C07C2601/14 ,  C07D213/79 ,  C07D213/80 ,  C07D267/06 ,  C07D307/33 ,  C07D307/58 ,  C07D307/60 ,  C07D317/32 ,  C07D317/40 ,  C07C205/43

公开(公告)号：EP1404324A2

公开(公告)日：2004-04-07

申请号：EP02744314.2

申请日：2002-06-11

Applicant: Xenoport, Inc.

Inventor： GALLOP, Mark, A. ,  CUNDY, Kenneth, C. ,  ZHOU, Cindy, X. ,  QIU, Fayang, G. ,  YAO, Fenmei ,  XIANG, Jia-Ning ,  OLLMAN, Ian, R.

IPC: A61K31/44 ,  A61K31/335 ,  A61K31/27 ,  A61K31/225 ,  A61K31/195 ,  A61P25/00 ,  C07D213/02 ,  C07D317/00 ,  C07C205/00 ,  C07C229/00 ,  C07C261/00 ,  C07C269/00 ,  C07C271/00

CPC classification number: C07C201/12 ,  A61K31/19 ,  A61K31/197 ,  A61K31/22 ,  A61K31/27 ,  A61K31/341 ,  A61K47/54 ,  A61K47/555 ,  C07C271/22 ,  C07C323/58 ,  C07C2601/14 ,  C07D213/79 ,  C07D213/80 ,  C07D267/06 ,  C07D307/33 ,  C07D307/58 ,  C07D307/60 ,  C07D317/32 ,  C07D317/40 ,  C07C205/43

Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using phannaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.

Abstract translation: 本发明提供了GABA类似物的前药，GABA类似物前药的药物组合物和制备GABA类似物的前药的方法。 本发明还提供使用GABA类似物前药的方法和使用GABA类似物前药的药物组合物治疗或预防常见疾病和/或病症的方法。

公开(公告)号：EP1317411A1

公开(公告)日：2003-06-11

申请号：EP01967383.9

申请日：2001-09-14

Applicant: ORION CORPORATION

Inventor： BÄCKSTRÖM, Reijo ,  PYSTYNEN, Jarmo ,  LOTTA, Timo ,  OVASKA, Martti ,  TASKINEN, Jyrki

IPC: C07C215/86 ,  A61K31/495 ,  A61K31/135 ,  C07D241/40 ,  C07D455/04 ,  A61P25/16

CPC classification number: C07D207/452 ,  C07C45/00 ,  C07C45/30 ,  C07C45/46 ,  C07C45/565 ,  C07C45/673 ,  C07C47/57 ,  C07C47/575 ,  C07C49/83 ,  C07C49/84 ,  C07C65/11 ,  C07C205/25 ,  C07C205/37 ,  C07C205/43 ,  C07C205/45 ,  C07C205/59 ,  C07C245/10 ,  C07C255/53 ,  C07C311/29 ,  C07D215/20 ,  C07D217/10 ,  C07D295/192

Abstract: Compounds of formula (I') wherein A, R1 to R3 and t are as defined in claims, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.

公开(公告)号：EP1010688B1

公开(公告)日：2003-04-09

申请号：EP99310223.5

申请日：1999-12-17

Applicant: Portela & Ca., S.A.

Inventor： Benes, Jan ,  Soares da Silva, Patricio Manuel Vieira Araujo ,  Learmonth, David Alexander

IPC: C07C205/45 ,  C07C205/43 ,  C07C205/59 ,  A61K31/12 ,  A61P25/00 ,  A61P25/16

CPC classification number: C07D317/54 ,  C07C45/292 ,  C07C45/46 ,  C07C45/673 ,  C07C205/43 ,  C07C205/45 ,  C07C205/59 ,  C07C255/56 ,  C07C309/73 ,  C07C49/84

公开(公告)号：EP0891962B1

公开(公告)日：2002-09-18

申请号：EP97907369.9

申请日：1997-03-18

Applicant: F-TECH, INC.

Inventor： NUKUI, Kazunori; Central Research Laboratory,Chic ,  FUKAMI, Shinji; Central Research Laboratory,Chich ,  KAWADA, Kosuke; Central Research Laboratory,Chich

IPC: C07C45/63 ,  C07C47/14 ,  C07C49/16 ,  C07C49/227 ,  C07C49/457 ,  C07C49/687 ,  C07C49/80 ,  C07C67/307 ,  C07C69/716 ,  C07C69/738 ,  C07C69/757

CPC classification number: C07J1/0011 ,  C07B39/00 ,  C07C45/63 ,  C07C67/307 ,  C07C205/43 ,  C07C205/45 ,  C07C69/716 ,  C07C47/14 ,  C07C49/16 ,  C07C49/227 ,  C07C49/457 ,  C07C49/687 ,  C07C49/80 ,  C07C69/738 ,  C07C69/757

Abstract: A process for the preparation of fluorinated dicarbonyl compounds of general formula (2), comprising reacting dicarbonyl compounds of general formula (1) with fluorine gas without any solvent in the presence of one or more acids selected from among trifluoromethanesulfonic acid, methanesulfonic acid, hydrofluoric acid, sulfuric acid, trifluoroacetic acid, boron trifluoride and sulfonated polymers wherein R?1, R2 and R3¿ are each hydrogen, alkyl or the like; and R?1a, R2a and R3a¿ are each the same as defined for R?1, R2 and R3¿, or alternatively when R?1, R2 and R3¿ are each hydrogen, the hydrogen may be replaced by fluorine, while when R?1, R2 and R3¿ are each optionally substituted alkyl, one or more hydrogen atoms on the α-position carbon atom to the CO-group may be replaced by fluorine. This process can give fluorinated dicarbonyl compounds in high yields and at high selectivity.

公开(公告)号：EP1118324A1

公开(公告)日：2001-07-25

申请号：EP01101213.5

申请日：2001-01-19

Applicant: Seiwa Pharmaceutical, Limited

Inventor： Nakamura, Motoyuki ,  Yoshizawa, Toyokichi ,  Chi, Yu-Ming ,  Nohara, Toshihiro ,  Sakurada, Shinobu

IPC: A61K31/19 ,  A61P29/00

CPC classification number: C07C205/43 ,  A61K31/194 ,  A61K31/225 ,  C07C51/353 ,  C07C61/39 ,  C07C61/40 ,  C07C62/32 ,  C07C67/347 ,  C07C69/753 ,  C07C69/757

Abstract: An analgesic agent is provided which has analgesic action and anti-inflammatory action without significant side effects found in conventional analgesics. The analgesic agent comprises as an active ingredient a cyclobutanedicarboxylic acid derivative, containing substituted diphenyl, represented by formula (I):
wherein X 1 , X 2 , Y 1 , Y 2 , Z 1 , and Z 2 , which may be the same or different, each independently represent a hydrogen atom, hydroxyl, a halogen atom, alkyl, alkoxy, or a nitrogen-containing group; and R 1 and R 2 , which may be the same or different, each independently represent hydroxyl, a halogen atom, alkoxy, aryloxy, terpeneoxy, saccharide, or a nitrogen-containing group.

Abstract translation: 提供具有止痛作用和抗炎作用而没有常规镇痛药中发现的显着副作用的止痛剂。 该止痛剂包含作为活性成分的由式（I）表示的含有取代的二苯基的环丁烷二羧酸衍生物：其中X 1，X 2，Y 1，Y 2，Z 1和Z 2可以相同或不同，各自独立地表示 氢原子，羟基，卤原子，烷基，烷氧基或含氮基团; 并且R 1和R 2可以相同或不同，各自独立地表示羟基，卤素原子，烷氧基，芳氧基，萜烯氧基，糖或含氮基团。