公开(公告)号：EP1948600A4

公开(公告)日：2011-09-07

申请号：EP06786336

申请日：2006-07-05

Applicant: HARVARD COLLEGE

Inventor： VERDINE GREGORY L ,  NORIMINE YOSHIHIKO ,  GUDE-RODRIGUEZ LOURDES

IPC: C07D209/12 ,  A61K31/22 ,  A61K31/405 ,  A61K47/48 ,  C07D209/28 ,  C07D309/30 ,  C07D405/12

CPC classification number: A61K47/48061 ,  A61K31/22 ,  A61K31/405 ,  A61K47/549 ,  A61K47/55 ,  C07D209/28 ,  C07D309/30 ,  C07D405/12 ,  C07D405/14

公开(公告)号：EP2323976A1

公开(公告)日：2011-05-25

申请号：EP09846749.1

申请日：2009-08-14

Applicant: Shasun Chemicals And Drugs Limited

Inventor： CHODANKAR, Nandkumar ,  BIYANI, Milind ,  MUTHUNARAYANAN, Mohan ,  RADHAKRISHNAN, Selvaraju ,  SANTHANAMPILLAI, Sathish Kumar ,  NADAR, Rajendran Paul ,  SUNDARAMURTHY, Vivekanandan ,  PRABU, Sakthivel Lakshmana

IPC: C07D207/00

CPC classification number: A61K9/2018 ,  A61K9/2054 ,  A61K9/2059 ,  C07C51/412 ,  C07C57/30 ,  C07C59/56 ,  C07C59/64 ,  C07C227/16 ,  C07D209/28 ,  C07C229/42

Abstract: The invention particularly discloses a process for preparing aryl alkyl carboxylic acid salts by preparing aqueous alkali solution, adding aryl alkyl carboxylic acid to said alkali solution at a temperature ranging from 4° to 121° C for obtaining a clear solution, preferably by heating and/or stirring and concentrating and cooling to obtain aryl alkyl carboxylic acid salt The invention therefore discloses solid oral dosage forms and compositions of aryl alkyl carboxylic acid salts which are free of organic solvent/so. The solid oral dose compositions of aryl alkyl carboxylic acid salts of the invention arc prepared in situ from aryl alkyl carboxylic acids and bases to obtain aryl acid alkyl carboxylic acid sails in crystalline/powder form with or without the use of pharmaceutical excipients.

Abstract translation: 本发明特别公开了通过制备碱水溶液制备芳基烷基羧酸盐的方法，在4°至121℃的温度范围内向所述碱溶液中加入芳基烷基羧酸，以获得澄清溶液，优选通过加热和 /或搅拌和浓缩并冷却以获得芳基烷基羧酸盐因此，本发明公开了不含有机溶剂的固体口服剂型和芳基烷基羧酸盐的组合物。 本发明的芳基烷基羧酸盐的固体口服剂量组合物由芳基烷基羧酸和碱原位制备得到具有或不使用药物赋形剂的结晶/粉末形式的芳基烷基羧酸帆。

公开(公告)号：EP1948600A2

公开(公告)日：2008-07-30

申请号：EP06786336.5

申请日：2006-07-05

Applicant: THE PRESIDENT & FELLOWS OF HARVARD COLLEGE

Inventor： VERDINE, Gregory L. ,  NORIMINE, Yoshihiko

IPC: C07D209/12

CPC classification number: A61K47/48061 ,  A61K31/22 ,  A61K31/405 ,  A61K47/549 ,  A61K47/55 ,  C07D209/28 ,  C07D309/30 ,  C07D405/12 ,  C07D405/14

Abstract: Therapeutic conjugates containing a statin or a modified statin (collectively 'statin') linked to a therapeutic agent (also referred to as a drug herein) are targeted to the liver by the statin or modified statin and thereby deliver the therapeutic agent to liver cells.

公开(公告)号：EP1473288B1

公开(公告)日：2008-07-16

申请号：EP04102724.4

申请日：1997-09-02

Applicant: NicOx S.A.

Inventor： Del Soldato, Piero ,  Sannicolo', Francesco

IPC: C07C311/21 ,  C07D311/54 ,  C07D231/12 ,  C07D307/87 ,  A61K31/18 ,  A61K31/352 ,  A61K31/415 ,  A61K31/427 ,  A61P29/00 ,  A61P7/02 ,  A61P9/00

CPC classification number: A61K31/00 ,  A61K31/21 ,  A61K31/216 ,  A61K31/245 ,  A61K31/405 ,  C07C229/58 ,  C07C311/08 ,  C07C311/51 ,  C07D209/28

公开(公告)号：EP1679301A1

公开(公告)日：2006-07-12

申请号：EP05460024.2

申请日：2005-08-30

Applicant: Centrum Chemii Polimerow Pan

Inventor： Jedlinsky, Zbigniew ,  Luczyk-Juzwa, Maria ,  Zawidlak-Wegrzynska ,  Kaczmarczyk, Bozena ,  Bosek, Izabele ,  Wanic, Andrzej

IPC: C07C69/675 ,  C07C69/738 ,  C07C69/734 ,  C07C69/736 ,  C07C69/88 ,  C07C229/42 ,  C07D209/28 ,  C07C317/44 ,  C07D207/32 ,  A61K31/216 ,  A61K31/235 ,  A61K31/405 ,  A61K31/40 ,  A61P29/00 ,  C08G63/08

CPC classification number: C07D207/337 ,  C07C69/675 ,  C07C69/734 ,  C07C69/736 ,  C07C69/738 ,  C07C69/88 ,  C07C229/42 ,  C07C317/44 ,  C07D209/28 ,  C08G63/08

Abstract: Novel esters of nonsteroidal anti-inflammatory drugs with oligomers of 3-hydroxybutyric acid of the invention possess the general formula 1, where n from 2 to 35, and R is a radical of a non-steroidal anti-inflammatory drug selected from the group consisting of ibuprofen, ketoprofen, fenoprofen, naproxen, diclofenac, indomethacine, sulindac, tolmetin or salicylic acid.
The method of preparation of compounds of the formula 1 consists in converting nonsteroidal anti-inflammatory drugs into a monosodium or monopotassium salts in the presence of a strongly polar solvent, preferably dimethyl sulfoxide (DMSO) or dimethylformamide (DMF), and in subjecting the obtained salts to the reaction with β-butyrolactone to open the lactone ring and to polymerize the lactone.
The esters of the invention contain a nonsteroidal anti-inflammatory drugs bonded by means of an ester bond with oligomers of 3-hydroxybutyric acid including 2-35 mers as constituting biocompatible polymer carriers.

Abstract translation: 本发明的具有3-羟基丁酸的低聚物的非甾族抗炎药的新型酯具有通式1，其中n为2至35，R为非甾体抗炎药的基团，其选自 布洛芬，酮洛芬，非诺洛芬，萘普生，双氯芬酸，吲哚美辛，舒林酸，托美丁或水杨酸。 制备式1化合物的方法在于将非甾体抗炎药物在强极性溶剂（DMSO）或二甲基甲酰胺（DMF）的存在下转化为单钠盐或单钾盐​​，并将所得的 与β-丁内酯反应的盐以打开内酯环并使内酯聚合。 本发明的酯含有通过酯键与包含2-35个聚合物的3-羟基丁酸的低聚物键合的非甾族抗炎药物，构成生物相容性聚合物载体。

公开(公告)号：EP1643961A2

公开(公告)日：2006-04-12

申请号：EP04756634.4

申请日：2004-07-01

Applicant: Microbia, INC.

Inventor： BARTOLINI, Wilmin ,  CALI, Brian, M. ,  CHEN, Barbara ,  CHIEN, Yueh-tyng ,  CURRIE, Mark, G. ,  MILNE, Todd, G. ,  PEARSON, James, Philip ,  TALLEY, John, Jeffrey ,  ZIMMERMAN, Craig

IPC: A61K6/00

CPC classification number: C07D209/26 ,  C07D209/28

Abstract: The invention features compounds that inhibit COX-2 and/or FAAH. The COX-2 inhibitors are selective COX-2 inhibitors in that they are selective for COX-2 compared to COX-1. Certain of the FAAH inhibitors are selective for FAAH relative to COX-2. Certain of the COX-2 inhibitors, in addition for being selective for COX-2 relative to COX-1, are selective for COX-2 relative to FAAH.

公开(公告)号：EP1610776A2

公开(公告)日：2006-01-04

申请号：EP04758273.9

申请日：2004-03-24

Applicant: Merck & Co. Inc. ,  Evotec OAI

Inventor： FISHER, Michael, H. ,  GARCIA, Maria, L. ,  KACZOROWSKI, Gregory, J. ,  MEINKE, Peter, T. ,  PARSONS, William, H. ,  BOYD, Edward Andrew ,  PRICE, Stephen ,  STIBBARD, John

IPC: A61K31/404 ,  C07D209/04

CPC classification number: C07D405/12 ,  C07D209/28 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.

公开(公告)号：EP0759899B1

公开(公告)日：1999-09-15

申请号：EP95915185.3

申请日：1995-04-04

Applicant: NICOX S.A.

Inventor： DEL SOLDATO, Piero ,  SANNICOLO', Francesco

IPC: C07C203/04 ,  C07D487/04 ,  A61K31/40 ,  A61K31/405 ,  A61K31/21 ,  C07D333/22

CPC classification number: C07D487/04 ,  C07C203/04 ,  C07D209/28 ,  C07D333/24

公开(公告)号：EP0882721A1

公开(公告)日：1998-12-09

申请号：EP97940327.6

申请日：1997-09-10

Applicant: DAIKIN INDUSTRIES, LIMITED

Inventor： OHIRA, Yutaka

IPC: C07D309/28 ,  C07D498/04 ,  C07D335/02 ,  C07C229/48 ,  C07C247/18 ,  C07C255/46 ,  C07C255/61 ,  C07C279/18 ,  C07C309/25 ,  C07C323/66

CPC classification number: C07D209/28 ,  C07D309/28

Abstract: Compounds represented by general formula (I) and salts thereof useful as non-tolerance-inducing antiviral agents, wherein A is O, CH 2 or S; R 1 is lower alkoxycarbonyl, COOH or the like; R 2 is H, OR 6 , F, Cl, Br, CN, NHR 6 or SR 6 (wherein R 6 is H, C 1 -C 6 lower alkyl or the like); one of R 3 and R 3' is H and the other thereof is H, CN, a nitrogenous group such as amino, or the like; R 4 is -NHR 6 or -N=CHR 6 ; and R 5 is CH 2 CH 2 XR 6 or CH(XR 6 )CH 2 XR 6 (wherein X is O, S or NH).

Abstract translation: 由通式（I）表示的化合物及其盐可用作非耐受性抗病毒剂，其中A为O，CH 2或S; R 1是低级烷氧基羰基，COOH等; R 2是H，OR 6，F，Cl，Br，CN，NHR 6或SR 6（其中R 6是H，C 1 -C 6低级烷基等）; R 3和R 3'之一是H，另一个是H，CN，含氮基团如氨基等; R 4是-NHR 6或-N = CHR 6; 和R 5是CH 2 CH 2 XR 6或CH（XR 6）CH 2 XR 6（其中X是O，S或NH）。

公开(公告)号：EP0722434B1

公开(公告)日：1998-07-29

申请号：EP94928801.3

申请日：1994-09-23

Applicant: NICOX S.A.

Inventor： DEL SOLDATO, Piero

IPC: C07C203/04 ,  C07D487/04 ,  C07D209/28 ,  A61K31/40 ,  A61K31/405 ,  A61K31/21

CPC classification number: C07D487/04 ,  C07C203/04 ,  C07D209/28

Abstract: The present invention refers to nitric esters of derivatives of propionic acid, 1-(p-chlorobenzoyl)-5-methoxy-2-methyl-3-indolylacetic acid, 5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid, 6-methoxy-2-naphthylacetic acid, having general formula (IA), their pharmaceutical use and the process for their preparation.