公开(公告)号：EP2291349A2

公开(公告)日：2011-03-09

申请号：EP09733451.0

申请日：2009-04-14

申请人： The Board of Regents of The University of Texas System ,  The Arizona Board of Regents on behalf of the University of Arizona

发明人： MAHADEVAN, Daruka ,  MEUILLET, Emmanuelle, J. ,  MASH, Eugene, A. ,  GOHKALE, Vijay, M. ,  POWIS, Garth ,  ZHANG, Shuxing

IPC分类号： C07C233/80 ,  C07D213/75 ,  C07D237/18 ,  C07D239/42 ,  C07D239/69 ,  C07D263/40

CPC分类号： A61K31/433 ,  C07C59/90 ,  C07C65/40 ,  C07C233/75 ,  C07C235/64 ,  C07C237/42 ,  C07C271/22 ,  C07C311/21 ,  C07C317/14 ,  C07C317/18 ,  C07C317/28 ,  C07C317/44 ,  C07C323/65 ,  C07D213/50 ,  C07D213/643 ,  C07D213/74 ,  C07D213/76 ,  C07D231/06 ,  C07D231/12 ,  C07D231/20 ,  C07D231/38 ,  C07D231/42 ,  C07D233/20 ,  C07D233/26 ,  C07D233/64 ,  C07D237/08 ,  C07D237/18 ,  C07D239/26 ,  C07D239/34 ,  C07D239/38 ,  C07D239/42 ,  C07D239/52 ,  C07D261/08 ,  C07D261/20 ,  C07D263/32 ,  C07D263/42 ,  C07D263/56 ,  C07D271/10 ,  C07D271/113 ,  C07D277/52 ,  C07D277/64 ,  C07D285/12 ,  C07D285/125 ,  C07D285/135 ,  C07D295/135 ,  C07D295/192 ,  C07D295/26 ,  C07D333/38 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/06 ,  C07D417/06 ,  C07D417/10 ,  C07D417/12 ,  C07F9/65583

摘要： Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.

公开(公告)号：EP1620434B1

公开(公告)日：2011-03-09

申请号：EP04751135.7

申请日：2004-05-03

申请人： ABBOTT LABORATORIES

发明人： COWART, Marlon, D. ,  KU, Yin-Yin ,  CHANG, Sou-Jen ,  FERNANDO, Dilinie, P. ,  GRIEME, Timothy, A. ,  ALTENBACH, Robert, A.

IPC分类号： C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D403/06 ,  C07D413/06 ,  A61P25/00 ,  A61K31/425 ,  A61K31/404 ,  A61K31/423

CPC分类号： C07D263/56 ,  C07D209/14 ,  C07D235/14 ,  C07D277/64 ,  C07D279/16 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D413/06 ,  C07D417/04

摘要： Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions. X is O, S, NH, or N(alkyl); Y, and Y’ are each independently selected from the group consisting of CH, CF, and N; Z is C or N, provided that when X is O or S, Z is N; one of R1 and R2 is selected from the group consisting of aryl, heteroaryl, and heterocycle; the other of R1 and R2 is selected from the group consisting of hydrogen, alkyl, alkoxy, aryl, cycloalkyl, halo, cyano, and thioalkoxy; R3 is absent when Z is N and, when present, R3 is selected from the group consisting of hydrogen, methyl, alkoxy, halo and cyano; R4 and R5 are each independently selected from the group consisting of alkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, cycloalkyl, and cycloalkylalkyl, or R4 and R5 taken together with the nitrogen atom to which each is attached form a non-aromatic ring L is -[C(R15)(R16)]n-; m is an integer from 0-3; and n is an integer from 2-3.

公开(公告)号：EP1542692B1

公开(公告)日：2011-01-05

申请号：EP03755509.1

申请日：2003-05-20

申请人： AMGEN INC.

发明人： DOHERTY, Elizabeth, M. ,  ZHU, Jiawang ,  STEC, Markian ,  NORMAN, Mark, H. ,  FOTSCH, Christopher, H. ,  CHEN, Ning ,  CHAKRABARTI, Partha, P. ,  OGNYANOV, Vassil I. ,  WANG, Hui-Ling ,  WANG, Xianghong ,  ARASASINGHAM, Premilla ,  PETTUS, Liping.H

IPC分类号： A61K31/501 ,  A61K31/506 ,  A61P25/00 ,  C07D417/12 ,  C07D405/12 ,  C07D403/12 ,  C07D401/12 ,  C07D239/42 ,  C07D471/04 ,  C07D417/14

CPC分类号： C07D231/40 ,  C07D209/08 ,  C07D209/12 ,  C07D209/42 ,  C07D209/48 ,  C07D213/26 ,  C07D213/643 ,  C07D213/74 ,  C07D213/75 ,  C07D215/227 ,  C07D215/38 ,  C07D217/04 ,  C07D231/56 ,  C07D233/38 ,  C07D237/20 ,  C07D239/42 ,  C07D239/90 ,  C07D241/42 ,  C07D263/56 ,  C07D265/36 ,  C07D277/62 ,  C07D277/82 ,  C07D307/79 ,  C07D319/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritis, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

公开(公告)号：EP2196454A3

公开(公告)日：2010-09-22

申请号：EP10001845.6

申请日：2006-01-12

申请人： Schering Corporation

发明人： Wu, George G. ,  Sudhakar, Anantha ,  Wang, Tao ,  Xie, Ji ,  Chen, Frank Xing ,  Poirier, Marc ,  Huang, Mingsheng ,  Sabesen, Vijay ,  Kwok, Daw-long ,  Cui, Jian ,  Yang, Xiaojing ,  Thiruvengadam, Tiruvettipuram K. ,  Liao, Jing

IPC分类号： C07C235/28 ,  C07C69/732 ,  C07D333/56 ,  C07C231/12

CPC分类号： C07D263/56 ,  C07C69/606 ,  C07C69/732 ,  C07C201/10 ,  C07C201/12 ,  C07C205/44 ,  C07C205/55 ,  C07C231/10 ,  C07C231/12 ,  C07C235/28 ,  C07C303/32 ,  C07C309/08 ,  C07C2601/16 ,  C07D277/64 ,  C07D307/92 ,  C07D333/56 ,  C07D405/06 ,  C07D413/06 ,  C07D417/06 ,  C07F7/1852 ,  C07F9/582 ,  Y02P20/55 ,  C07C233/28

摘要： This application discloses compounds which are useful in the preparation of himbacine analogs as well as processes for their preparation:

wherein Rs and R 6 are each independently selected from the group consisting of H, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, aryl, alkylaryl, arylalkyl, heterocyclic and heteroaryl groups, or R 5 and R 6 , together with the nitrogen to which they are attached, form a 3- to 6-membered heterocyclic compound containing 1-4 heteroatoms, P is a protecting group and is selected from the group consisting of THP or SiR 1 R 2 R 3 , wherein R 1 , R 2 and R 3 are independently selected from the group consisting of H, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, alkylaryl, heterocyclic, and heteroaryl.

摘要翻译： 本申请公开了可用于制备伊巴菌素类似物的化合物及其制备方法：其中R 5和R 6各自独立地选自H，烷基，烯基，炔基，烷氧基，环烷基，芳基，烷芳基， 芳基烷基，杂环基和杂芳基，或者R 5和R 6与它们所连接的氮一起形成含有1-4个杂原子的3-至6-元杂环化合物，P是保护基并且选自 的THP或SiR 1 R 2 R 3，其中R 1，R 2和R 3独立地选自H，烷基，烯基，环烷基，芳基，芳基烷基，烷基芳基，杂环和杂芳基。

公开(公告)号：EP1853565B1

公开(公告)日：2010-09-22

申请号：EP06705356.1

申请日：2006-02-23

申请人： Givaudan SA

发明人： COLE, Lucienne ,  FURRER, Stefan, Michael ,  GALOPIN, Christophe ,  KRAWEC, Pablo, Victor ,  MASUR, Adam ,  SLACK, Jay, Patrick

IPC分类号： C07D231/12 ,  C07D249/08 ,  C07D263/32 ,  C07D295/135 ,  A61K8/49

CPC分类号： C07D231/12 ,  A61K8/42 ,  A61K8/49 ,  A61K2800/244 ,  A61Q11/00 ,  A61Q19/00 ,  C07D249/08 ,  C07D263/32 ,  C07D263/56 ,  C07D277/62 ,  C07D295/135

摘要： A compound of the formula (I) in which X and Y are selected as defined in the description. The compounds have cooling properties and are useful in, for example, foodstuffs , dentifrices and cosmetics .

公开(公告)号：EP2225216A1

公开(公告)日：2010-09-08

申请号：EP08853012.6

申请日：2008-11-20

申请人： Decode Genetics EHF

发明人： SINGH, Jasbir ,  GURNEY, Mark ,  BURGIN, Alex ,  KISELYOV, Alexander ,  RAO, Munagala

IPC分类号： C07D263/56 ,  C07D263/58 ,  C07D277/62 ,  C07D277/82 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D513/04 ,  A61K31/428 ,  A61K31/423 ,  A61K31/519 ,  A61K31/4439 ,  A61P29/00

CPC分类号： C07D417/14 ,  A61K31/423 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/519 ,  C07D263/56 ,  C07D263/58 ,  C07D277/64 ,  C07D277/82 ,  C07D417/04 ,  C07D417/06 ,  C07D498/04 ,  C07D513/04

摘要： The invention relates to substituted benzothiazoles, benzoxazoles - and their counterparts having pyridine and pyrimidine rings replacing the benzene ring - that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula (I), in which A and B are carbocycles or heterocycles. A particular embodiment is Formula (II).

公开(公告)号：EP2225215A1

公开(公告)日：2010-09-08

申请号：EP08853006.8

申请日：2008-11-20

申请人： Decode Genetics EHF

发明人： SINGH, Jasbir ,  GURNEY, Mark ,  BURGIN, Alex ,  SANDANAYAKA, Vincent ,  KISELYOV, Alexander ,  RAO, Munagala

IPC分类号： C07D263/56 ,  C07D263/58 ,  C07D277/62 ,  C07D277/82 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D513/04 ,  A61K31/428 ,  A61K31/423 ,  A61K31/519 ,  A61K31/4439 ,  A61P29/00

CPC分类号： C07D417/14 ,  A61K31/423 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/519 ,  C07D263/56 ,  C07D263/58 ,  C07D277/64 ,  C07D277/82 ,  C07D417/04 ,  C07D417/06 ,  C07D498/04 ,  C07D513/04

摘要： The invention relates to substituted benzothiazoles, benzoxazoles - and their counterparts having pyridine and pyrimidine rings replacing the benzene ring - that are are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula (I) in which A and B are carbocycles or heterocycles. A particular embodiment is formula (AB).

公开(公告)号：EP2217650A2

公开(公告)日：2010-08-18

申请号：EP08859554.1

申请日：2008-12-02

申请人： Henkel AG & Co. KGaA ,  Henkel Corporation

发明人： KREILING, Stefan ,  SCHONFELD, Rainer ,  TADEN, Andreas ,  LEHMANN, Stanley, L.

IPC分类号： C08K5/35 ,  C08K3/00 ,  C08K5/00 ,  C07D498/06 ,  C08L101/00

CPC分类号： C08K5/357 ,  C07D263/56 ,  C07D263/62 ,  C08G18/12 ,  C08G18/6677 ,  C08G73/0233 ,  C08L79/02 ,  C08G18/3237

摘要： The invention relates to a curable composition comprising: at least one benzoxazine and at least one toughening additive which can be bound to the at least one benzoxazine in the curing process, characterized in that the toughening additive is distributed in the cured composition in form of discrete domains, and that at least 50% of the discrete domains related to the total amount of discrete domains having a maximum length in any direction of space in the range of 10 nm to 500 nm as determined by transmission electron microscopy (TEM).

公开(公告)号：EP1910360B1

公开(公告)日：2010-03-03

申请号：EP06787590.6

申请日：2006-07-17

申请人： Merck & Co., Inc.

发明人： SAGGAR, Sandeep, A. ,  SISKO, John, T. ,  TUCKER, Thomas, J. ,  TYNEBOR, Robert, M. ,  SU, Dai-Shi ,  ANTHONY, Neville, J.

IPC分类号： C07D471/04 ,  A61P31/12 ,  A61K31/437

CPC分类号： C07C311/46 ,  C07C255/54 ,  C07C255/60 ,  C07C307/06 ,  C07C317/40 ,  C07C2601/14 ,  C07D209/08 ,  C07D213/65 ,  C07D213/75 ,  C07D231/56 ,  C07D235/06 ,  C07D249/04 ,  C07D249/06 ,  C07D263/56 ,  C07D271/06 ,  C07D271/10 ,  C07D271/107 ,  C07D277/64 ,  C07D333/48 ,  C07D471/04

摘要： Compounds having the structure: are HIV reverse transcriptase inhibitors, wherein A, X, Y, Z, R1 and R2 are defined herein. The compounds and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

公开(公告)号：EP1848705B1

公开(公告)日：2010-02-24

申请号：EP06718069.5

申请日：2006-01-12

申请人： Schering Corporation

发明人： Wu, George ,  Sudhakar, Anantha ,  Wang, Tao ,  Xie, Ji ,  Chen, Frank, Xing ,  Poirier, Marc ,  Huang, Mingsheng ,  Sabesan, Vijay ,  Kwok, Daw-long ,  Cui, Jian ,  Yang, Xiaojing ,  Thiruvengadam, Tiruvettipuram, K. ,  Liao, Jing ,  Zavialov, Ilia ,  Nguyen, Hoa, N. ,  Lim, Ngiap Kie

IPC分类号： C07D307/92 ,  C07C235/28 ,  C07D405/06 ,  C07C205/55 ,  C07D413/06 ,  C07D417/06 ,  C07C205/44 ,  C07C309/08 ,  C07D235/12 ,  C07D263/56 ,  C07D277/64

CPC分类号： C07D263/56 ,  C07C69/606 ,  C07C69/732 ,  C07C201/10 ,  C07C201/12 ,  C07C205/44 ,  C07C205/55 ,  C07C231/10 ,  C07C231/12 ,  C07C235/28 ,  C07C303/32 ,  C07C309/08 ,  C07C2601/16 ,  C07D277/64 ,  C07D307/92 ,  C07D333/56 ,  C07D405/06 ,  C07D413/06 ,  C07D417/06 ,  C07F7/1852 ,  C07F9/582 ,  Y02P20/55 ,  C07C233/28

摘要： The application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following. (I)

摘要翻译： 该申请公开了一种制备可用作凝血酶受体拮抗剂的喜巴辛类似物的新方法。 该方法部分基于使用碱促进的手性硝基中心的动态差向异构化。 在此教导的化学可以通过以下例示。 （一世）