公开(公告)号：EP1812412A1

公开(公告)日：2007-08-01

申请号：EP05806565.7

申请日：2005-10-29

申请人： Sanofi-Aventis Deutschland GmbH

发明人： KLEEMAN, Heinz-Werner

IPC分类号： C07D277/20 ,  C07D279/02 ,  C07D285/00 ,  C07D285/16 ,  A61K31/00 ,  A61P9/00

CPC分类号： C07D277/20 ,  C07D277/22 ,  C07D279/02 ,  C07D285/01 ,  C07D285/16

摘要： The invention relates to substituted benzoylguanidines of formula (I), where R1 to R8, X and Y have the meanings given in the claims and the pharmaceutically-acceptable salts thereof which are substituted acylguanidines and inhibit cellular Sodium/Proton antiporter (Na+/H+-Exchanger, NHE). Compounds of formula (I) and the pharmaceutically-acceptable salts thereof are suitable for the prevention and treatment of disease caused by activation of or by an activated NHE as a result of the NHE-inhibitory properties thereof and also of secondary diseases caused by damage brought about by the NHE.

公开(公告)号：EP1644346A1

公开(公告)日：2006-04-12

申请号：EP04731671.6

申请日：2004-05-07

申请人： MERCK SHARP & DOHME LTD.

发明人： DINNELL, Kevin ,  HARRISON, Timothy ,  NADIN, Alan, John ,  OWENS, Andrew, Pate ,  SHAW, Duncan, Edward ,  WILLIAMS, Brian, John

IPC分类号： C07D285/16 ,  C07D513/04 ,  C07D279/02 ,  A61K31/5415

CPC分类号： C07D279/02

摘要： Compounds of formula (I) inhibit the processing of APP by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.

公开(公告)号：EP1311490A4

公开(公告)日：2005-07-13

申请号：EP01962348

申请日：2001-08-06

申请人： UNIV KANSAS

发明人： HANSON PAUL R ,  DOUGHERTY JOSEPH M ,  PROBST DONALD A

IPC分类号： C07C307/06 ,  C07D285/36 ,  C07D285/16 ,  C07D417/06

CPC分类号： C07C307/06 ,  C07D285/36

摘要： New sulfamide compounds and methods of forming those compounds are provided. The inventive methods comprise subjecting a template opened-ring sulfamide compound to a ring-closing metathesis reaction in the presence of a Grubbs catalyst to yield a heterocyclic sulfamide. Advantageously, the template structures can be provided with a wide array of functional groups (e.g., substituted and unsubstituted amino acid side chains, peptides) chosen to provide particular properties to the compound. The preferred heterocyclic sulfamides are represented by a formula selected from the group consisting of formulae (I), (II), (III), and (IV).

公开(公告)号：EP1477482A1

公开(公告)日：2004-11-17

申请号：EP03705344.4

申请日：2003-02-20

申请人： Ajinomoto Co., Inc.

发明人： SAGI, Kazuyuki, c/o AJINOMOTO CO., INC. ,  IZAWA, Hiroyuki, c/o AJINOMOTO CO., INC. ,  CHIBA, Akira, c/o AJINOMOTO CO., INC. ,  OKUZUMI, Tatsuya, c/o AJINOMOTO CO., INC. ,  YOSHIMURA, Toshihiko, c/o AJINOMOTO CO., INC. ,  TANAKA, Yuji, c/o AJINOMOTO CO., INC. ,  ONO, Miho, c/o AJINOMOTO CO., INC. ,  MURATA, Masahiro, c/o AJINOMOTO CO., INC.

IPC分类号： C07D239/96 ,  C07D239/52 ,  C07D239/78 ,  C07D239/80 ,  C07D285/16 ,  C07D285/32 ,  C07D487/04 ,  C07D405/12 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5415

CPC分类号： C07D265/26 ,  C07D239/54 ,  C07D239/80 ,  C07D239/96 ,  C07D253/04 ,  C07D285/16 ,  C07D285/24 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04 ,  C07D487/04

摘要： The present invention relates to the following phenylalanine derivatives or analogues thereof having an antagonistic activity to α4 integrin and therapeutic agents for various diseases concerning α4 integrin.

摘要翻译： 本发明涉及对α4整联蛋白具有拮抗作用的以下苯丙氨酸衍生物或其类似物以及涉及α4整联蛋白的各种疾病的治疗剂。

公开(公告)号：EP0971908B1

公开(公告)日：2004-06-30

申请号：EP98909998.1

申请日：1998-02-12

申请人： SmithKline Beecham Corporation

发明人： NIE, Hong ,  WIDDOWSON, Katherine, L.

IPC分类号： C07D291/08 ,  C07D285/16 ,  C07D279/02 ,  A61K31/54

CPC分类号： C07D279/02

摘要： The invention relates to certain 8-ureido and 8-thioureido 1,2-benzothiazines, 1,2,4-benzothioxazines and 1,2,4-benzothiodiazines useful in the treatment of disease states mediated by the chemokine, Interleukin-8.

公开(公告)号：EP0796251B1

公开(公告)日：2001-10-17

申请号：EP95941683.5

申请日：1995-12-07

申请人： Byk Gulden Lomberg Chemische Fabrik GmbH

发明人： BOER, Rainer ,  BOSS, Hildegard ,  ELTZE, Manfrid ,  BELLER, Klaus-Dieter ,  SANDERS, Karl ,  BRAND, Ursula ,  PRÜSSE, Wolfgang ,  ULRICH, Wolf-Rüdiger

IPC分类号： C07D239/54 ,  C07D239/60 ,  C07D285/16 ,  A61K31/505

CPC分类号： C07D239/545 ,  C07D239/557 ,  C07D239/60 ,  C07D285/16

摘要： Disclosed are compounds of formula I, in which the substituents and symbols have the meanings indicated in the description. These compounds are novel 5-HT1A-agonists and α1-adrenoceptor blockers.

公开(公告)号：EP0866710A4

公开(公告)日：2001-07-11

申请号：EP96936906

申请日：1996-10-23

申请人： ZYMOGENETICS INC ,  OSTEOSCREEN INC ,  UNIV TEXAS AT AUSTIN

发明人： PETRIE CHARLES ,  ORME MARK W ,  BAINDUR NAND ,  ROBBINS KIRK G ,  HARRIS SCOTT M ,  KONTOYIANNI MARIA ,  HURLEY LAURENCE H ,  KERWIN SEAN M ,  MUNDY GREGORY R

IPC分类号： C07D285/16 ,  A61K31/12 ,  A61K31/47 ,  A61K31/549 ,  A61K31/54 ,  A61K31/35 ,  A61K45/06 ,  A61P19/00

CPC分类号： A61K31/549 ,  A61K31/47

摘要： Compounds containing two aromatic systems covalently linked through a linker containing one or more atoms, or "linker" defined as including a covalent bond per se so as to space the aromatic systems at a distance 1.5-15 ANGSTROM , are effective in treating conditions associated with bone deficits. The compounds can be administered to vertebrate subjects alone or in combination with additional agents that promote bone growth or that inhibit bone resorption. They can be screened for activity prior to administration by assessing their ability to effect the transcription of a reporter gene coupled to a promoter associated with a bone morphogenetic protein and/or their ability to stimulate calvarial growth in model animal systems.

公开(公告)号：EP1005462A1

公开(公告)日：2000-06-07

申请号：EP98942624.2

申请日：1998-07-25

申请人： BASF AKTIENGESELLSCHAFT

发明人： MERKLE, Hans, Rupert ,  WÖRZ, Otto ,  FRETSCHNER, Erich ,  HANSEN, Hanspeter ,  MÜLLER, Albrecht ,  BENZ, Kurt

IPC分类号： C07D285/16

CPC分类号： C07D285/16

摘要： The invention relates to a method for the production of 3-isopropyl-1H-2,1,3-benzothiazine-4(3H)-one-2,2-dioxide (I) or its salt. The method is characterized in that anthranilic acid isopropylamide (II) is reacted simultaneously with sulphur trioxide or chlorosulphonic acid in the presence of an organic base, or with sulphur trioxide adducts on organic bases, and phosphoroxychloride at 50 °C until reflux temperature, and then optionally transformed into their salts.

公开(公告)号：EP0877024A4

公开(公告)日：1999-03-31

申请号：EP95944775

申请日：1995-12-28

申请人： PROCTER & GAMBLE ,  LIGAND NTP TOO

发明人： CHUPAKHIN OLEG NIKOLAEVICH ,  SIDOROVA LARISA PETROVNA ,  TARAKHTY EMMA AFANASIEVNA ,  NOVIKOVA ANTONINA PETROVNA ,  PEROVA NATALYA MIKHAILOVNA ,  VINOGRADOV VALENTIN ANTONOVICH ,  VAN GINKEL MICHIEL FRANCISCUS

IPC分类号： A61K31/54 ,  C07D285/16 ,  C07D417/04

CPC分类号： C07D285/16

摘要： The disclosure relates to substituted 6H-1,3,4-thiadiazine-2-amines of general formula (I), in which Ar stands for phenyl which can be substituted with one or more atoms of chlorine, bromine, C1-C4 alkoxy or C1-C4 alkyl groups; and (a) represents a morpholine, thiomorpholine, piperidine, pyrrolidine or hexamethylene imine fragment; to the pharmacologically acceptable salts of said compounds; to their use as anaesthetising, cardiovascular and hypometabolic agents; and to pharmaceutical compositions containing them.

摘要翻译： 取代的6H-1,3,4-噻二嗪-2- cardamines以下通式： worin Ar是苯基，其任选被一个或多个氯，溴原子，C1-C4烷氧基或C1-C4烷基substituiertem; 和 darstellt一个吗啉代，硫代吗啉代，哌啶子基，吡咯烷基，六亚甲基亚或部分，其药学上可接受的盐和它们的用途如麻醉剂，心血管和代谢减退剂以及含有它们的药物组合物。

公开(公告)号：EP0897921A1

公开(公告)日：1999-02-24

申请号：EP98306559.0

申请日：1998-08-18

申请人： ELI LILLY AND COMPANY LIMITED

发明人： Fairhurst, John

IPC分类号： C07D417/14 ,  C07D513/04 ,  A61K31/54 ,  C07D285/16

CPC分类号： C07D285/16 ,  A61K9/2059 ,  A61K9/4866 ,  C07D417/14 ,  C07D513/04

摘要： Compounds having the formula:
in which n is 1 or 2, m is 1 or 2,

p is 1 to 6, q is 0 or 1 to 3,
R 1 and R 2 are each hydrogen or C 1-4 alkyl,
R 3 , R 4 and R 5 are each hydrogen, C 1-4 alkyl, optionally substituted phenyl or optionally substituted phenyl-C 1-4 alkyl, or R 3 and R 4 together form an alkylene link of formula -(CH 2 ) 3 - or -(CH 2 ) 4 -, or R 4 and R 5 together with the carbon atom to which they are attached form a C 3-6 cycloalkyl group,
R 6 is C 1-4 alkyl, C 1-4 alkoxy, carboxy, hydroxy, cyano, halo, trifluoromethyl, nitro or amino,
the dotted line represents an optional double bond, and
the fluorine atom is attached at the 6 or 7-position;
and salts and esters thereof, are binding to the 5-HT serotonin receptor and are useful in the treatment of CNS disorders.

摘要翻译： 具有下式的化合物：其中n为1或2，m为1或2，p为1至6，q为0或1至3，R 1和R 2各自为氢或C1 -4-烷基，R 3，R 4和R 5各自为氢，C 1-4烷基，任选取代的苯基或任选取代的苯基-C 1-4烷基，或R 3和R 4为氢， 一起形成式 - （CH 2）3 - 或 - （CH 2）4 - 或R 4和R 5与它们所连接的碳原子一起形成C 3-6环烷基的亚烷基连接，R C 6烷基，C 1-4烷氧基，羧基，羟基，氰基，卤素，三氟甲基，硝基或氨基，虚线表示任选的双键，氟原子连接在6位或7位 ; 其盐和酯与5-HT血清素受体结合，可用于治疗CNS疾病。