公开(公告)号：EP3300499B1

公开(公告)日：2023-10-04

申请号：EP16728721.8

申请日：2016-06-02

Inventor： HEGGIE, William ,  NABER, John ,  BAZINET, Patrick R ,  TOMAS, Filipe

IPC: C07C227/04 ,  C07C227/16 ,  C07C227/18 ,  C07C231/02 ,  C07C231/12 ,  C07C237/46 ,  C07C237/32 ,  C07C233/69 ,  C07C229/62 ,  C07C235/16

公开(公告)号：EP3990429B1

公开(公告)日：2023-07-26

申请号：EP20734217.1

申请日：2020-06-25

Inventor： MELDRUM, Eric ,  MACHIN, Peter ,  DE CHASSEY, Benoît ,  COUSIN, David

IPC: C07D207/09 ,  C07C233/65 ,  C07D211/26 ,  C07D231/56 ,  A61K31/44 ,  A61P31/12 ,  C07C237/30 ,  C07C237/32 ,  C07C237/42

公开(公告)号：EP2681209A1

公开(公告)日：2014-01-08

申请号：EP11860054.3

申请日：2011-03-02

Applicant: Aquilus Pharmaceuticals, Inc

Inventor： SUCHOLEIKI, Irving

IPC: C07D409/12 ,  C07C237/32 ,  C07C43/263 ,  A61K31/404 ,  A61K31/12 ,  A61P25/04

CPC classification number: C07D207/337 ,  A61K31/12 ,  A61K31/404 ,  A61K45/06 ,  C07B2200/05 ,  C07C231/12 ,  C07C237/26 ,  C07C311/19 ,  C07C317/44 ,  C07D209/16 ,  C07D209/48 ,  C07D211/60 ,  C07D233/72 ,  C07D307/85 ,  C07D309/04 ,  C07D309/06 ,  C07D331/02 ,  C07D333/34 ,  C07D409/12 ,  Y02A50/465 ,  A61K2300/00

Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.

Abstract translation: 本发明涉及基因的反弹到药剂，并且特别地，涉及金属蛋白酶抑制剂的化合物。 更具体地，本发明提供了一类新的双重作用的MMP-2和MMP-9抑制性化合物也表现出相对于增加的效力，代谢稳定性和/或降低的毒性，以目前已知MMP-2和MMP-9抑制剂，用于治疗 的疼痛和其它疾病。 另外，本发明涉及用于治疗疼痛，成瘾和/或戒断症状在患者中包括给予所述患者的疼痛减轻有效量的本发明化合物的方法。

公开(公告)号：EP2483236A1

公开(公告)日：2012-08-08

申请号：EP10761108.9

申请日：2010-09-28

Applicant: Mallinckrodt LLC

Inventor： CAVIGGIOLA III, Tino, J. ,  JONES, Michelle, M.

IPC: C07C231/12 ,  C07C235/16 ,  C07C237/32

CPC classification number: C07C231/12 ,  C07D265/36 ,  C07C237/46

Abstract: The present disclosure generally relates to an improved process for alkylating a triiodo-substituted arylamide to form a compound suitable for use as an X-ray contrast agent. More particularly, the present disclosure is directed to such a process that limits the formation of fused bicyclic impurities, such as Impurity G, in the alkylation reaction mixture.

公开(公告)号：EP2234961A2

公开(公告)日：2010-10-06

申请号：EP08851324.7

申请日：2008-11-20

Applicant: LEO PHARMA A/S

Inventor： FENSHOLDT, Jef ,  HAVEZ, Sophie Elisabeth ,  NØRREMARK, Bjarne

IPC: C07C211/35 ,  C07C211/36 ,  C07C211/48 ,  C07C215/28 ,  C07C217/52 ,  C07C217/74 ,  C07C233/05 ,  C07C233/41 ,  C07C237/24 ,  C07C237/30 ,  C07C237/32 ,  C07C237/34 ,  C07C237/36 ,  C07C237/40 ,  C07C239/14

CPC classification number: C07D295/182 ,  C07C211/35 ,  C07C211/36 ,  C07C211/48 ,  C07C215/28 ,  C07C217/52 ,  C07C217/74 ,  C07C233/05 ,  C07C233/41 ,  C07C237/24 ,  C07C237/30 ,  C07C237/32 ,  C07C237/34 ,  C07C237/36 ,  C07C237/40 ,  C07C239/14 ,  C07C255/03 ,  C07C255/32 ,  C07C255/50 ,  C07C257/18 ,  C07C259/10 ,  C07C259/18 ,  C07C271/44 ,  C07C309/15 ,  C07C311/05 ,  C07C311/08 ,  C07C311/37 ,  C07C311/51 ,  C07C317/32 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07D205/04 ,  C07D207/08 ,  C07D207/12 ,  C07D207/16 ,  C07D207/27 ,  C07D209/08 ,  C07D209/12 ,  C07D209/20 ,  C07D211/46 ,  C07D211/60 ,  C07D211/62 ,  C07D213/30 ,  C07D213/38 ,  C07D213/40 ,  C07D213/80 ,  C07D231/12 ,  C07D231/40 ,  C07D233/61 ,  C07D233/90 ,  C07D263/22 ,  C07D271/06 ,  C07D295/088 ,  C07D295/13 ,  C07D295/135 ,  C07D295/192 ,  C07D295/195 ,  C07D295/26 ,  C07D305/08 ,  C07D307/12 ,  C07D307/52 ,  C07D307/68 ,  C07D307/79 ,  C07D309/10 ,  C07D319/18 ,  C07D333/38 ,  C07D333/40 ,  C07D333/58 ,  C07D413/04 ,  C07D413/06 ,  C07D417/06

Abstract: The invention relates to novel cyclic hydrocarbon compounds and derivatives thereof, processes for the preparation thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.

Abstract translation: 本发明涉及新型环状烃化合物及其衍生物，其制备方法，用作药物的所述化合物，用于治疗的所述化合物，包含所述化合物的药物组合物，涉及用所述化合物治疗疾病的方法 ，以及所述化合物在制备药物中的用途。

公开(公告)号：EP1870396A4

公开(公告)日：2009-07-22

申请号：EP06730399

申请日：2006-03-29

Applicant: NIPPON ZOKI PHARMACEUTICAL CO

Inventor： HIGASHIURA KUNIHIKO ,  OGINO TAKASHI ,  FURUKAWA KAZUHITO

IPC: C07C233/18 ,  C07C233/73 ,  C07C235/48 ,  C07C237/08 ,  C07C237/24 ,  C07C237/32 ,  C07C271/16 ,  C07C271/22 ,  C07C271/24 ,  C07C271/48 ,  C07D207/06 ,  C07D211/14 ,  C07D213/20 ,  C07D213/56 ,  C07D215/50 ,  C07D241/24 ,  C07D317/22

CPC classification number: C07D317/22 ,  C07C233/18 ,  C07C233/73 ,  C07C235/48 ,  C07C237/08 ,  C07C237/24 ,  C07C237/32 ,  C07C271/16 ,  C07C271/22 ,  C07C271/24 ,  C07C271/28 ,  C07C271/48 ,  C07C2601/14 ,  C07D207/06 ,  C07D211/14 ,  C07D211/62 ,  C07D213/20 ,  C07D213/56 ,  C07D213/89 ,  C07D215/50 ,  C07D241/24

Abstract: Disclosed is a novel benzyloxypropylamine derivative having an excellent tachykinin receptor antagonistic effect. This compound shows a good transfer into the blood and a long blood half-life in the blood kinetic test using a guinea pig orally administered with the compound and is stable in an animal plasma. The compound also shows a high transfer to the central nervous system when it is orally administered to a guinea pig at a certain dose. Accordingly, the benzyloxypropylamine derivative is quite useful as a novel anti-tachykinin agent.

Abstract translation: 公开了具有优异的速激肽受体拮抗作用的新型苄氧基丙胺衍生物。 该化合物在使用化合物口服给药的豚鼠的血液动力学试验中显示出良好的血液转移和血中半衰期，并且在动物血浆中稳定。 当以特定剂量口服给予豚鼠时，该化合物也显示出高度转移至中枢神经系统。 因此，苄氧基丙胺衍生物作为新型抗速激肽药物是非常有用的。

公开(公告)号：EP1140787B1

公开(公告)日：2004-07-28

申请号：EP99966181.2

申请日：1999-12-14

Applicant: Eastman Chemical Company

Inventor： HEIDT, Philip, C. ,  ELLIOTT, Matthew, L.

IPC: C07C211/18 ,  C07C211/27 ,  C07C237/32 ,  C07C237/24 ,  C07C31/27 ,  C09D201/02

CPC classification number: C07C237/32 ,  C07C31/27 ,  C07C211/18 ,  C07C211/27 ,  C07C237/24 ,  C07C2601/14 ,  C09D201/02

Abstract: The present invention relates to the composition, process of preparation, and use of novel derivatives prepared from 1,5-bis-(4'-carbomethoxyphenyl)-1,4-pentadien-3-one. These novel compositions can act as crosslinkers with polyfunctional monomeric, oligomeric, and/or polymeric anhydrides, esters, carboxylic acids, isocyantes, epoxies, carbonates, acetoacetates, and alkoxylated melamines.

公开(公告)号：EP1368325A1

公开(公告)日：2003-12-10

申请号：EP02701852.2

申请日：2002-03-05

Applicant: AstraZeneca AB

Inventor： BROWN, William,AstraZeneca R & D Montreal ,  PLOBECK, Niklas,AstraZeneca R & D Montreal

IPC: C07D241/04 ,  C07D401/06 ,  C07D215/12 ,  C07D307/79 ,  C07D401/14 ,  C07D403/14 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07C237/32 ,  A61K31/496 ,  A61P25/04

CPC classification number: C07D405/12 ,  C07D215/12 ,  C07D409/12

Abstract: An asymmetric synthesis of diarylmethylpiperazines is described. The synthetic route enables preparation of a variety of enatiomerically pure amines with different N-alkyl groups. The invention includes an asymmetric addition of organometallic compounds to chiral sulfinimine to give adducts in predominantly one diastereomer can subsequently be transferred into pure enantiomers of by cleavage of the chiral auxilliary which is followed by synthesis of the piperazine ring by alkylation procedures.

公开(公告)号：EP0816331B1

公开(公告)日：2000-05-24

申请号：EP97304191.6

申请日：1997-06-16

Applicant: ROHM AND HAAS COMPANY

Inventor： Michelotti, Enrique Luis ,  Young, David Hamilton

IPC: C07C237/32 ,  C07C309/65 ,  C07C331/04 ,  C07C331/20 ,  C07D213/81 ,  A01N37/20 ,  A01N41/04 ,  A01N47/46 ,  A01N47/48 ,  C07C225/06 ,  A01N35/02

CPC classification number: C07D213/82 ,  A01N37/44 ,  A01N37/48 ,  A01N43/40 ,  C07C225/06 ,  C07C237/32 ,  C07C251/48

公开(公告)号：EP0905167A1

公开(公告)日：1999-03-31

申请号：EP97902655.6

申请日：1997-02-12

Applicant: NISSAN CHEMICAL INDUSTRIES, LIMITED

Inventor： NIHIRA, Takayasu, Nissan Chemical Industries, Ltd ,  NAWATA, Hideyuki, Nissan Chemical Industries, Ltd ,  FUKURO, Hiroyoshi, Nissan Chemical Industries Ltd

IPC: C08G73/10 ,  C07C217/76 ,  C07C217/84 ,  C07C219/32 ,  C07C219/34 ,  C07C237/32 ,  C07C237/34 ,  C07C237/36 ,  C09K19/56 ,  G02F1/1337

CPC classification number: C08G73/10 ,  C07C217/90 ,  C07C229/60 ,  C07C2601/14 ,  G02F1/133723 ,  Y10T428/1023 ,  Y10T428/31721

Abstract: A diaminobenezene derivative represented by the general formula (1), and a polyimide obtained by reacting a diamine containing at least 1 mol% of said diaminobenzene derivative, with a tetracarboxylic acid and its derivative to obtain a polyimide precursor having a reduced viscosity of from 0.05 to 5.0 dl/g (in N-methylpirrolidone at a temperature of 30°C, concentration: 0.5 g/dl) and ring-closing it, and having a repeating unit represented by the general formula (2), as well as a liquid crystal alignment film containing said polyimide.
(in the formula (1), P is a single bond or a bivalent organic group selected from -O-, -COO-, and -CONH-, Q is a cyclic substituent selected from an aromatic ring, an aliphatic ring, a hetero ring and their substitution products, R 1 is an aliphatic ring, and R 2 is a C 1-22 straight chain alkyl group, and in the formula (2), A is a tetravalent organic group constituting a tetracarboxylic acid, B is a bivalent organic group constituting a diamine, and P, Q, R 1 and R 2 are the same as in the above formula (1)).