公开(公告)号：EP2035371A2

公开(公告)日：2009-03-18

申请号：EP07730150.5

申请日：2007-06-14

申请人： F.HOFFMANN-LA ROCHE AG

发明人： JOLIDON, Synese ,  NARQUIZIAN, Robert ,  NORCROSS, Roger ,  PINARD, Emmanuel

IPC分类号： C07D205/04 ,  C07D207/06 ,  C07D211/16 ,  C07D407/10 ,  A61K31/445 ,  A61P25/18

CPC分类号： C07D207/06 ,  C07D207/08 ,  C07D211/16 ,  C07D403/10 ,  C07D407/10

摘要： The present invention relates to compounds of the general formula (i), wherein R1 is -OR1', heterocycloalkyl, aryl or heteroaryl, which are unsubstituted or substituted by lower alkyl or halogen; R1' is lower alkyl, lower alkyl substituted by halogen, or is -(CH2)o-cycloalkyl; R2 is -S(O)2-lower alkyl, -S(O)2NH-lower alkyl, NO2 or CN; R3 is aryl or heteroaryl, which are unsubstituted or substituted by one to three substituents, selected from the group consisting of lower alkyl, lower alkoxy, CN, NO2, halogen, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, aryl or sulfonamide; X is a bond, -CH2-, -NH-, -CH2O- or -OCH2-; n is 1 or 2; m is 1 or 2; o is 0 or 1; to pharmaceutically acceptable acid addition salts thereof, to pharmaceutical compositions containing them and their use in the treatment of neurological and neuropsychiatric disorders. It has been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GlyT-1).

公开(公告)号：EP1958945A1

公开(公告)日：2008-08-20

申请号：EP06834301.1

申请日：2006-12-08

申请人： Chisso Corporation ,  Chisso Petrochemical Corporation

发明人： GOTO, Mayumi ,  SUGIURA, Teruyo ,  HATTORI, Norikatsu ,  SAGOU, Kouki

IPC分类号： C07D311/20 ,  C07D311/76 ,  C07D405/04 ,  C07D407/04 ,  C07D407/06 ,  C07D407/08 ,  C07D407/10 ,  C09K19/12 ,  C09K19/14 ,  C09K19/16 ,  C09K19/18 ,  C09K19/20 ,  C09K19/30 ,  C09K19/32 ,  C09K19/34 ,  C09K19/42 ,  G02F1/133

CPC分类号： C09K19/3402 ,  C07D311/20 ,  C07D311/58 ,  C07D311/76 ,  C07D405/04 ,  C07D407/04 ,  C07D407/06 ,  C07D407/08 ,  C07D407/10 ,  C09K2019/3425 ,  Y10T428/10 ,  Y10T428/1036

摘要： A liquid crystal compound is to be obtained that has stability to heat, light and so forth, a high clearing point, a suitable optical anisotropy, a large negative dielectric anisotropy, and excellent compatibility with other liquid crystal compounds. A liquid crystal composition containing the compound is also to be obtained that has a low viscosity, a suitable optical anisotropy, a suitable negative dielectric anisotropy, a low threshold voltage, a high maximum temperature of a nematic phase (phase transition temperature from a nematic phase to an isotropic phase), and a low minimum temperature of a nematic phase. A compound having a hydrocoumarin skeleton is synthesized, and a liquid crystal composition containing the compound is produced.

摘要翻译： 可以得到对热，光等具有稳定性，高透明度，适当的光学各向异性，大的负介电各向异性，与其它液晶化合物的相容性优异的液晶性化合物。 还可以获得含有该化合物的液晶组合物，其具有低粘度，适当的光学各向异性，适当的负介电各向异性，低阈值电压，向列相的高最高温度（从向列相的相变温度 到各向同性相）和向列相的低最低温度。 合成具有氢香豆素骨架的化合物，制备含有该化合物的液晶组合物。

公开(公告)号：EP1517895B1

公开(公告)日：2007-03-14

申请号：EP03760540.9

申请日：2003-06-23

申请人： Merck Frosst Canada Ltd.

发明人： DESCHENES, Denis ,  DUBE, Daniel ,  DUBE, Laurence ,  GALLANT, Michel ,  GIRARD, Yves ,  LACOMBE, Patrick ,  MACDONALD, Dwight

IPC分类号： C07D215/04 ,  C07D215/12 ,  C07D409/10 ,  C07D407/10 ,  C07D401/10 ,  C07D413/10 ,  C07D413/14 ,  C07D471/04 ,  C07D401/04 ,  C07D403/10 ,  C07D417/10 ,  A61K31/4709 ,  A61K31/47 ,  A61K31/497 ,  A61P29/00

CPC分类号： C07D215/04 ,  C07D215/06 ,  C07D215/12 ,  C07D215/14 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D405/10 ,  C07D407/10 ,  C07D409/10 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/12 ,  C07D471/04 ,  C07F7/0812 ,  C07F9/60

摘要： 8-(biaryl) quinolines wherein the bi-aryl group at the 8-position is in a meta relationship to the quinoline group, are PDE4 inhibitors useful in the treatment of asthma, chronic bronchitis, chronic obstructive pulmonary disease, eosinophilic granuloma, psoriasis and other benign or malignant proliferative skin diseases, endotoxic shock, laminitis in horses, colic in horses, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and brain, inflammatory arthritis, chronic glomerulonephritis, atopic dermatitis, urticaria, adult respiratory distress syndrome, chronic obstructive pulmonary disease in animals, diabetes insipidus, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, arterial restenosis, ortherosclerosis, atherosclerosis, neurogenic inflammation, pain, cough, rheumatoid arthritis, ankylosing spondylitis, transplant rejection, graft versus host disease, hypersecretion of gastric acid, bacterial, fungal induced sepsis, viral induced sepsis, fungal induced septic shock, viral induced septic shock, inflammation-mediated chronic tissue degeneration, cytokine-mediated chronic tissue degeneration, osteoarthritis, cancer, cachexia, muscle wasting, depression, memory impairment, tumour growth, or cancerous invasion of normal tissues.In another aspect, the present invention is directed to a method of enhancing cognition in a healthy subject comprising administering a safe cognition enhancing amount of phosphodiesterase-4 inhibitor. In particular, this invention is directed to a method of enhancing memory, learning, retention, recall, awareness and judgement in health subjects comprising administering a safe and cognition enhancing amount of a phosphodiesterase-4 inhibitor.

公开(公告)号：EP0889889B1

公开(公告)日：2006-09-20

申请号：EP97908288.0

申请日：1997-03-20

申请人： DUPHAR INTERNATIONAL RESEARCH B.V

发明人： FEENSTRA, Roelof, Willem ,  KRUSE, Cornelis, Gerrit ,  TULP, Martinus, Theodorus, Maria ,  KUIPERS, Wilma ,  LONG, Stephen, Kenneth

IPC分类号： C07D405/04 ,  C07D411/04

CPC分类号： C07D263/58 ,  C07D209/08 ,  C07D215/12 ,  C07D265/36 ,  C07D307/79 ,  C07D311/18 ,  C07D317/66 ,  C07D319/08 ,  C07D319/18 ,  C07D321/10 ,  C07D327/06 ,  C07D333/54 ,  C07D405/04 ,  C07D407/10 ,  C07D409/10 ,  C07D413/10

摘要： The invention relates to a group of new piperazine and piperidine compounds having interesting pharmacological properties. It has been found that compounds of formula (a) wherein A represents a heterocyclic group of 5-7 ring atoms wherein 1-3 heteroatoms from the group O, N and S are present; R1 is hydrogen or fluoro; R2 is C1-4-alkyl, C1-4-alkoxy or an oxo group, and p is 0, 1 or 2; Z represents carbon or nitrogen, and the dotted line is a single bond when Z is nitrogen, and a single or double bond when Z is carbon; R3 and R4 independently are hydrogen or C1-4-alkyl; n has the value 1 or 2; R5 is halogen, hydroxy, C1-4-alkoxy or C1-4-alkyl, and q is 0, 1, 2 or 3; Y is phenyl, furanyl or thienyl, which groups may be substituted with 1-3 substituents of the group hydroxy, halogen, C1-4-alkoxy, C1-4-alkyl, cyano, aminocarbonyl, mono- or di-C1-4-alkylaminocarbonyl; and salts thereof show high affinity for both the dopamine D2 and serotonin 5-HT1A receptors.

公开(公告)号：EP1545513A2

公开(公告)日：2005-06-29

申请号：EP03785208.4

申请日：2003-08-11

申请人： Viropharma Incorporated

发明人： NITZ, Theodore, J. ,  GABOURY, Janet, A. ,  BURNS, Christopher, J. ,  LAQUERRE, Sylvie ,  PEVEAR, Daniel, C. ,  LESSEN, Thomas, A. ,  RYS, David, J.

IPC分类号： A61K31/41 ,  A61K31/335 ,  A61P25/00 ,  C07D317/44 ,  C07D257/04

CPC分类号： C07D275/02 ,  A61K31/11 ,  A61K31/136 ,  A61K31/18 ,  A61K31/196 ,  A61K31/222 ,  A61K31/357 ,  A61K31/41 ,  A61K31/425 ,  A61K31/427 ,  A61K31/4453 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07C47/565 ,  C07C69/18 ,  C07C223/06 ,  C07C235/16 ,  C07C235/68 ,  C07C311/29 ,  C07D211/32 ,  C07D257/04 ,  C07D401/14 ,  C07D407/10 ,  C07D417/14

摘要： Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infection.

公开(公告)号：EP1534689A1

公开(公告)日：2005-06-01

申请号：EP03794886.6

申请日：2003-08-16

申请人： BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG

发明人： LEHMANN-LINTZ, Thorsten ,  STENKAMP, Dirk ,  LENTER, Martin ,  WIELAND, Heike-Andrea ,  RUDOLF, Klaus ,  MÜLLER, Stephan, Georg ,  LOTZ, Ralf, R., H. ,  ARNDT, Kirsten ,  LUSTENBERGER, Philipp ,  LEHMANN-LINTZ, Thorsten

IPC分类号： C07D239/80 ,  C07D211/58 ,  C07D211/16

CPC分类号： C07D209/48 ,  C07C233/78 ,  C07C2601/02 ,  C07D205/04 ,  C07D207/09 ,  C07D207/16 ,  C07D207/20 ,  C07D209/14 ,  C07D209/44 ,  C07D209/46 ,  C07D211/34 ,  C07D211/52 ,  C07D211/64 ,  C07D213/40 ,  C07D213/56 ,  C07D213/74 ,  C07D217/04 ,  C07D221/24 ,  C07D221/26 ,  C07D223/16 ,  C07D239/91 ,  C07D239/96 ,  C07D249/18 ,  C07D295/073 ,  C07D295/096 ,  C07D295/135 ,  C07D295/185 ,  C07D295/192 ,  C07D295/215 ,  C07D401/04 ,  C07D401/10 ,  C07D403/10 ,  C07D407/10 ,  C07D451/02 ,  C07D471/10 ,  C07D487/10

摘要： The invention relates to carboxamide compounds of general formula (I), in which the groups and radicals A, B, W, X, Y, Z, R1, R2, R3, and k have the meanings indicated in claim 1. The invention also relates to methods for producing said carboxamide compounds and medicaments containing at least one inventive carboxamide. The inventive medicaments are suitable for treating metabolic disorders and/or eating disorders, especially obesity, bulimia, anorexia, hyperphagia, and diabetes due to the MCH receptor-antagonistic activity thereof.

摘要翻译： 甲酰胺（I）互变异构体，对映异构体，对映异构体的混合物和盐是新的。 式（I）及其互变异构体，非对映体，对映异构体，混合物和盐的羧酰胺是新的，包括在上羧基或氮氢原子被一个基团代替也可以在体内裂解的化合物。 R 1和R 2 =氢，1-8C烷基或3-7C-环烷基，由R 11，或苯基两者任选substituiertem，任选被一个或多个R 12和/或硝基，R1 + R2 = 2-8C亚烷基（特别是具有一个或取代 两个CH2换成CH = N或CH = CH;或具有一个或两个CH 2被氧代替，硫，CO，C（= CH 2）或NR 13，设置有两个杂原子是不相邻的;具有一个或多个氢由R14取代; 或由1或2赛扬取代的，通过单键或双键结合，单C，形成螺环系统中，两个相邻的C和/或N，形成稠合的双环体系，或3个或多个C和/或N原子， 形成一个桥连的双环系统; R 3 =氢，1-6C烷基，3-7C环烷基，由1-6C烷氧基或氨基环烷基3-7C（1-4C）烷基或2-6C烷基substituiertem，任选被1或2个 1-3C烷基; X =单键或1-8C亚烷基（特别是具有1或2个CH 2由CH = CH，乙炔基，氧，S（O）X，CO或NR 4取代，所提供的杂原子不连接;和/或 具有由水合1个或2个C substituiertem 乐声，ω-（羟基或烷氧基1-3C）烷基和/或烷氧基1-3C和/或1-6C的烷基; X + Z + R 1或R 3 =杂环; Z = 1-4C亚烷基（特别是两个相邻的C可通过另一1-4C亚烷基连接; 2一个CH 2可被氧或NR 5，或C 1，或者可以被羟基取代，ω-（羟基或1-3C来代替 烷氧基）烷基，1-3C-烷氧基或氨基（1-3C）烷基（任选N-被1个或2 1-3C烷基取代）和/或1或2个C 1-6烷基）; A + Y“=碳环或杂环基团（CY），且R 1与Y可形成稠合的Y上的杂环基团和/或R 3可以与Y上的饱和或部分不饱和的杂环稠合Y上形成; A + R3（即-N（R 3）CO-A）=式（i）的部分; Q = CR6R7，CR 6 = CR 7，N = CR 8，N = N，CONR9，CR8 = N或CO; L1-L3 = R20; B“= CY，通过碳环部分的碳原子键合的或稠合的苯基或吡啶基，或通过杂环部分的N或C原子; W“=单键，氧，1-4C-亚烷基（氧），2-4C烯基，氧代（1-4C）亚烷基，亚烷氧基1-3C（1-3C）亚烷基，（1-3C烷基）亚氨基，（1 -3C烷基）亚氨基（1-4C）亚烷基或1-4C-亚烷基（1-3C烷基）亚氨基; W'-B '= W'= B“（即（氧）亚烷基或亚烷氧基亚）; CY =饱和的3-7元碳氮化周期; 不饱和的5-7元碳氮化周期; 苯基; 的4-7元饱和或不饱和的5-7元含氮杂环，氧或硫作为杂原子; （不）饱和5-7元杂环具有两个或多个N或用一个N和一个O或S; 芳族5或6元杂环与一个或多个的N，O和/或S; 所述5-7元环可以被稠合到苯基或吡啶基环和/或具有一个CH 2被CO，C（= CH 2）代替，SO或SO 2; 和6-7元环可以作为桥连的系统，含亚氨基或亚甲基，被1个或2 1-3C烷基任选取代的（任选被1-3C烷基substituiertem）; 和全部任选在一个或多个C由R20（由硝基即对于苯基）和/或由一个或多个R 21在N个substituiertem; R4，R5和R16 =氢，3-7C环烷基（CYL）CYL（1-3C）烷基，4-7C环烯基（氰）氰（1-3C）烷基，ω-（羟基或1-3C烷氧基） 2-3C烷基，氨基或（1-6C）烷基，任选被1个或2 1-3C烷基N-取代; R6-R9 =氢，1-6C烷基或（羟基或1-3C烷氧基）烷基的ω; 因此（除R 9）卤素; R11 = R15O，R15OCO，R16R17N，或R18R19NCO赛扬; R12和R20 =卤素，羟基，氰基，1-4C-烷基，柱面，（1-3C）烷基羟基，R22-（1-3C）烷基或R 22; R13和R17 R16 =，所以苯基，苯基（1-3C）烷基，二氧戊环-2-基，1-3C-烷基羰基，羧基（1-3C）烷基，烷基羰基氨基1-3C（2-3C）烷基，1-3C 烷基磺酰基或烷基磺酰1-3C（2-3C）烷基; R14 =卤素，1-6C烷基，R15O，R15OCO，R16R17N，R18R19NCO，R15O-或R15-OCO - （1-3C）烷基，R16R17N（1-3C）烷基，R18R19NCO（1-3C）烷基或成分Cy（ 1-3C）烷基; R15 =氢，1-4C-烷基，

公开(公告)号：EP0912561B1

公开(公告)日：2002-12-04

申请号：EP97917340.8

申请日：1997-04-17

申请人： AstraZeneca AB

发明人： GRAVESTOCK, Michael, Barry

IPC分类号： C07D405/10 ,  A61K31/365 ,  C07D407/10 ,  C07D405/12 ,  C07D409/10 ,  A61K31/505 ,  A61K31/445

CPC分类号： C07D405/10 ,  C07D405/12 ,  C07D407/10 ,  C07D409/10

公开(公告)号：EP1140859A2

公开(公告)日：2001-10-10

申请号：EP99968917.7

申请日：1999-12-17

申请人： AXYS PHARMACEUTICALS, INC.

发明人： ALLEN, Darin, Arthur ,  HATAYE, Jason, M. ,  HRUZEWICZ, Witold, N. ,  KOLESNIKOV, Aleksandr ,  MACKMAN, Richard, Laurence ,  RAI, Roopa ,  SPENCER, Jeffrey, R. ,  VERNER, Erik, J. ,  YOUNG, Wendy, B. ,  SHRADER, William, Dvorak

IPC分类号： C07D235/18 ,  A61K31/415 ,  A61P7/02

CPC分类号： C07D401/10 ,  C07D209/12 ,  C07D209/18 ,  C07D235/18 ,  C07D235/20 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12 ,  C07D407/10 ,  C07D407/12 ,  C07D409/10 ,  C07D409/12 ,  C07D413/10 ,  C07D417/10 ,  C07D417/12 ,  C07D471/04

摘要： The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a partially unsaturated bicyclic heterocyclic ring structure, and B represents an aryl or a heteroaryl group. Preferred compounds of the present invention comprise a benzimidazole or indole nucleus. The compounds of this invention are inhibitors of serine proteases, Urokinase (uPA), Factor Xa (FXa), and/or Factor VIIa (FVIIa), and have utility as anti cancer agents and/or as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals.

公开(公告)号：EP1037886A1

公开(公告)日：2000-09-27

申请号：EP98963082.7

申请日：1998-12-11

申请人： Abbott Laboratories

发明人： HENKIN, Jack ,  DAVIDSON, Donald, J. ,  SHEPPARD, George, S. ,  WOODS, Keith, W. ,  MCCROSKEY, Richard, W.

IPC分类号： C07D403/04 ,  A61K31/53 ,  C07D401/04 ,  C07D251/18 ,  C07D417/04 ,  C07D413/10 ,  C07D401/12 ,  C07D409/10 ,  C07D407/10 ,  C07D407/04 ,  C07D409/04 ,  C07D409/06 ,  C07D405/04 ,  C07D453/02 ,  C07D401/10

CPC分类号： C07D401/04 ,  C07D251/18 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D407/04 ,  C07D407/10 ,  C07D409/04 ,  C07D409/06 ,  C07D409/10 ,  C07D413/10 ,  C07D417/04 ,  C07D453/02

摘要： Compounds having Formula (I) or pharmaceutically acceptable salts or prodrugs thereof, are useful for treating pathological states which arise from or are exacerbated by angiogenesis. The invention also relates to pharmaceutical compositions comprising these compounds and to methods of inhibiting angiogenesis in a mammal.

公开(公告)号：EP0379716B1

公开(公告)日：1996-03-13

申请号：EP89123690.3

申请日：1989-12-21

申请人： TROPIX, INC.

发明人： Schaap, Arthur Paul ,  Akhaven-Tafti, Hashem

IPC分类号： C07D321/00 ,  C07D405/12 ,  C07D417/12 ,  C07D277/64 ,  C07D311/86

CPC分类号： C07D405/12 ,  C07C43/1788 ,  C07C51/15 ,  C07C2603/18 ,  C07C2603/74 ,  C07D207/46 ,  C07D311/82 ,  C07D321/00 ,  C07D407/10 ,  C07D407/12 ,  C07D417/12 ,  C07D493/10 ,  C07D495/04 ,  C07F7/1852 ,  C07F7/1856 ,  C07F9/6541 ,  C07F9/65512 ,  C07F9/65522 ,  C07F9/65586 ,  C07F9/6561 ,  C07H15/203 ,  C07C65/11