公开(公告)号：US20090281141A1

公开(公告)日：2009-11-12

申请号：US11995714

申请日：2006-07-28

申请人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Bernard Raboisson ,  Sandrine Marie Helene Vendeville ,  Lili Hu ,  Abdellah Tahri ,  Dominique Louis nestor Ghislain Surleraux ,  Wim Van De Vreken ,  Ismet Dorange ,  Yvan Simonnet ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Åsa Annica Kristina Rosenquist ,  Hans Kristian Wallberg

发明人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Bernard Raboisson ,  Sandrine Marie Helene Vendeville ,  Lili Hu ,  Abdellah Tahri ,  Dominique Louis nestor Ghislain Surleraux ,  Wim Van De Vreken ,  Ismet Dorange ,  Yvan Simonnet ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Åsa Annica Kristina Rosenquist ,  Hans Kristian Wallberg

IPC分类号： A61K31/4709 ,  C07D245/00 ,  A61P31/12

CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D417/14 ,  C07D487/04 ,  C07K5/06191

摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers thereof, wherein X is N, CH and where X bears a double bond it is C; R1 is —OR1, —NH—SO2R6; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; R4 is isoquinolinyl optionally substituted with one, two or three substituents each independently selected from C1-6alkyl, C1-6alkoxy, hydroxy, halo, polyhaloC1-6alkyl, polyhaloC1-6alkoxy, amino, mono- or diC1-6alkylamino, mono- or diC1-6alkylaminocarbonyl, C1-6alkylcarbonyl-amino, aryl, and Het; n is 3, 4, 5, or 6; each dashed line (represented by - - - - - ) represents an optional double bond; R5 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R6 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; each aryl is phenyl optionally substituted with one, two or three substituents; and each Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.

摘要翻译： 式（I）的HCV复制抑制剂及其N-氧化物，盐和立体异构体，其中X为N，CH，X为双键时为C; R1为-OR1，-NH-SO2R6; R2是氢，并且其中X是C或CH，R2也可以是C1-6烷基; R 3是氢，C 1-6烷基，C 1-6烷氧基C 1-6烷基或C 3-7环烷基; R 4是任选被一个，两个或三个独立地选自C 1-6烷基，C 1-6烷氧基，羟基，卤素，多卤代C 1-6烷基，多卤代C 1-6烷氧基，氨基，单或二C 1-6烷基氨基，单或二-C 1-6烷基， C 1-6烷基氨基羰基，C 1-6烷基羰基 - 氨基，芳基和Het; n为3,4,5或6; 每个虚线（由 - - - - 表示）表示可选的双键; R5是氢; 芳基; Het; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; R6是芳基; Het; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; 每个芳基是任选被一个，两个或三个取代基取代的苯基; 并且每个Het是含有1至4个各自独立地选自氮，氧和硫的杂原子的5或6元饱和，部分不饱和或完全不饱和的杂环，并且任选地被一个，两个或三个取代基取代; 含有化合物（I）的药物组合物和制备化合物（I）的方法。 还提供了式（I）的HCV抑制剂与利托那韦的生物可利用组合。

公开(公告)号：US20090281139A1

公开(公告)日：2009-11-12

申请号：US12507907

申请日：2009-07-23

申请人： Eldon Scott Priestley ,  Daniel L. Cheney ,  Nicolas Ronald Wurtz ,  Peter W. Glunz

发明人： Eldon Scott Priestley ,  Daniel L. Cheney ,  Nicolas Ronald Wurtz ,  Peter W. Glunz

IPC分类号： A61K31/4725 ,  C07D245/00 ,  A61P7/02

CPC分类号： C07D401/12 ,  C07D217/22 ,  C07D245/04 ,  C07D255/04 ,  C07D273/02 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates generally to novel macrocycles of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, B, L, M, W, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of the serine protease coagulation factor VIIa which can be used as medicaments.

摘要翻译： 本发明一般涉及式（I）的新型大环或其立体异构体，互变异构体，药学上可接受的盐，溶剂合物或前药，其中变量A，B，L，M，W，Z，R 1，R 2，R 3， R4，R5，R6，R7，R8，R9和R10如本文所定义。 这些化合物是可用作药物的丝氨酸蛋白酶凝血因子VIIa的选择性抑制剂。

公开(公告)号：US20080293932A1

公开(公告)日：2008-11-27

申请号：US11829726

申请日：2007-07-27

申请人： Fu-Shing Wang ,  Kuang-Mei Hsu

发明人： Fu-Shing Wang ,  Kuang-Mei Hsu

IPC分类号： C07D245/00 ,  G01N21/00

CPC分类号： C07D487/22

摘要： A phthalocyanine compound of formula (I) is provided for use in a recording layer of an optical recording media. In formula (I), M1 is a divalent transition metal, or two hydrogen atoms; X is halogen; Y is —OR1; R1 is alkyl which is unsubstituted or substituted by halogen, halogen, hydroxyl, alkoxy, alkylamino; R2 is R3 and R4 independently denote H, halogen, alkyl and alkoxyl; R5 is unsubstituted or substituted phenyl, benzyl, nathalenyl, or heterocycle; E denotes a single bond, C1-C4 alkyl, R6—C—O—C(═O), R6—O—C(═O)— or R6—S—C(═O)—; R6 is unsubstituted or substituted phenyl, benzyl, nathalenyl, heterocycle or C1-C4 alkyl; x is a number from 0 to 8; y is a number from 0 to 8; z is a number from 0 to 4; and M2 is a divalent transition metal.

摘要翻译： 提供式（I）的酞菁化合物用于光学记录介质的记录层。 在式（I）中，M1是二价过渡金属或两个氢原子; X是卤素; Y为-OR1; R1是未取代的或被卤素，卤素，羟基，烷氧基，烷基氨基取代的烷基; R2是R3和R4独立地表示H，卤素，烷基和烷氧基; R5是未取代或取代的苯基，苄基，萘烷基或杂环; E表示单键，C1-C4烷基，R6-C-O-C（-O），R6-O-C（-O） - 或R6-S-C（-O） - ; R6是未取代或取代的苯基，苄基，萘烷基，杂环或C1-C4烷基; x是从0到8的数字; y是从0到8的数字; z是从0到4的数字; M2是二价过渡金属。

公开(公告)号：US07122664B2

公开(公告)日：2006-10-17

申请号：US10667221

申请日：2003-09-17

申请人： Kurt E. Geckeler ,  Friederike Constabel

发明人： Kurt E. Geckeler ,  Friederike Constabel

IPC分类号： C07D245/00

CPC分类号： C07D487/08

摘要： The present invention relates to a complex composed of cucurbituril and fullerene and a method for manufacturing the complex on a solid-phase.A complex in accordance with the present invention can be usefully used as a medicine delivery means in the field of pharmaceutics.

摘要翻译： 本发明涉及由葫芦巴和富勒烯组成的复合物及其制备方法。 根据本发明的复合物可以有用地用作药物领域中的药物递送装置。

公开(公告)号：US06984734B2

公开(公告)日：2006-01-10

申请号：US10373949

申请日：2003-02-26

申请人： Jonathan L. Sessler ,  Daniel Seidel ,  Frederic R. Bolze ,  Thomas Koehler

发明人： Jonathan L. Sessler ,  Daniel Seidel ,  Frederic R. Bolze ,  Thomas Koehler

IPC分类号： C07D245/00 ,  G02F1/035 ,  G11B7/24 ,  B32B3/26

CPC分类号： C07D487/22 ,  Y10T428/249953

摘要： The present invention provides an oxidative coupling procedure that allows efficient synthesis of novel cyclo[n]pyrrole macrocycles. Therefore, the present invention provides cyclo[n]pyrroles where n is 6, 7, 8, 9, 10, 11, or 12, and derivatives, multimers, isomers, and ion and neutral molecule complexes thereof as new compositions of matter. A protonated form of cyclo[n]pyrrole displays a gap of up to 700 nm between strong Soret and Q-like absorption bands in the electronic spectrum, demonstrating no significant ground state absorption in the visible portion of the electronic spectrum. Uses of cyclo[n]pyrroles as separation media, nonlinear optical materials, information storage media and infrared filters are provided.

公开(公告)号：US20030195228A1

公开(公告)日：2003-10-16

申请号：US10357919

申请日：2003-02-04

申请人： Boehringer Ingelheim Pharmaceuticals, Inc.

发明人： Shirlynn Chen ,  Xiaohui Mei

IPC分类号： A61K038/12 ,  A61K031/4709 ,  C07D245/00

CPC分类号： A61K31/4709 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/1075 ,  A61K9/145 ,  A61K9/146 ,  A61K9/4866 ,  A61K47/18 ,  A61K2300/00

摘要： Disclosed are pharmaceutical compositions of hepatitis C viral protease inhibitors having improved bioavailability, and methods of using these compositions for inhibiting the replication of the hepatitis C virus (HCV) and for the treatment of an HCV infection. These compositions include co-solvent systems, lipid based systems, solid dispersions and granulations, and all comprise the hepatitis C viral protease inhibitor, at least one pharmaceutically acceptable amine and optionally one or more additional ingredients.

摘要翻译： 公开了具有改善的生物利用度的丙型肝炎病毒蛋白酶抑制剂的药物组合物，以及使用这些组合物抑制丙型肝炎病毒（HCV）的复制和用于治疗HCV感染的方法。 这些组合物包括共溶剂体系，基于脂质的体系，固体分散体和颗粒，并且全部包含丙型肝炎病毒蛋白酶抑制剂，至少一种药学上可接受的胺和任选的一种或多种另外的成分。

公开(公告)号：US20030191053A1

公开(公告)日：2003-10-09

申请号：US10362574

申请日：2003-02-24

发明人： Hiroharu Matsuoka ,  Tsutomu Sato

IPC分类号： A61K038/12 ,  C07K005/12 ,  C07D245/00

CPC分类号： C07K5/0202 ,  A61K38/00 ,  C07K5/0205 ,  C07K5/0215

摘要： The present invention aims to provide cyclic peptide derivatives having motilin receptor antagonist activity or the like and useful as pharmaceuticals. The present invention provides a compound of general formula (1): 1 wherein R1 represents an optionally substituted phenyl group or the like; R2 represents an amino group or the like; R3 to R6 represent a hydrogen atom, a methyl group or the like; R7 represents a hydrogen atom or the like; V to Z represent a carbonyl group or a methylene group; m represents an integer of 0-2; and n represents an integer of 0-3; or a hydrate or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明旨在提供具有胃动素受体拮抗剂活性等的环状肽衍生物，可用作药物。 本发明提供通式（1）的化合物：其中R 1表示任选取代的苯基等; R2表示氨基等; R3〜R6表示氢原子，甲基等; R7表示氢原子等; V至Z表示羰基或亚甲基; m表示0-2的整数; n表示0〜3的整数。 或其水合物或其药学上可接受的盐。

公开(公告)号：US6153608A

公开(公告)日：2000-11-28

申请号：US117433

申请日：1998-07-29

申请人： Hiroyoshi Hidaka ,  Akira Matsuura ,  Takushi Matsuzaki

发明人： Hiroyoshi Hidaka ,  Akira Matsuura ,  Takushi Matsuzaki

IPC分类号： A61K31/495 ,  C07D217/02 ,  C07D217/04 ,  C07D217/22 ,  C07D401/12 ,  C07D471/08 ,  A61K31/55 ,  C07D239/00 ,  C07D239/02 ,  C07D239/70 ,  C07D245/00 ,  C07D401/00 ,  C07D487/00 ,  C07D491/00

CPC分类号： C07D401/12 ,  A61K31/495 ,  C07D217/02 ,  C07D217/04 ,  C07D217/22 ,  C07D471/08

摘要： The invention relates to a compound of the following general formula [I] or a medicinally acceptable salt thereof, or a solvate thereof, ##STR1## wherein R.sup.1 represents alkyl, alkenyl, alkynyl, alkoxy, hydroxy, cyano, or halogen; R.sup.2 represents hydrogen, hydroxy, or halogen; R.sup.3 represents hydrogen, alkyl, or amidino; Ring A represents a 5 to 11-membered cyclic amino group which may be substituted, which cyclic amino group may be bridged between two carbon atoms in optional positions. The compound of this invention is useful for the prevention or treatment of cerebral tissue impairment due to the vasospasm following cerebral hemorrhage.

摘要翻译： PCT No.PCT / JP97 / 00240 Sec。 371日期1998年7月29日第 102（e）日期1998年7月29日PCT 1997年1月31日PCT PCT。 公开号WO97 / 28130 日期：1997年8月7日本发明涉及以下通式[I]的化合物或其药学上可接受的盐或其溶剂合物，其中R1表示烷基，烯基，炔基，烷氧基，羟基，氰基或卤素; R2代表氢，羟基或卤素; R3表示氢，烷基或脒基; 环A表示可被取代的5至11元环状氨基，该环状氨基可以在任选位置的两个碳原子之间桥连。 本发明的化合物可用于预防或治疗由脑出血引起的血管痉挛引起的脑组织损伤。

公开(公告)号：US5417959A

公开(公告)日：1995-05-23

申请号：US130618

申请日：1993-10-04

申请人： Rebecca A. Wallace

发明人： Rebecca A. Wallace

IPC分类号： A61K49/00 ,  A61K49/06 ,  C07D487/08 ,  C07K14/00 ,  A61B5/055 ,  C07D225/00 ,  C07D245/00

CPC分类号： C07D487/08 ,  A61K49/0002 ,  A61K49/06 ,  C07K14/001 ,  Y10T436/24

摘要： The present invention provides new and structurally diverse compositions comprising compounds of the general formula: ##STR1## Wherein V is CR.sub.1 or N; W is CR.sub.2 or N; R.sub.1 and R.sub.2 may be the same or different and are hydrogen, C.sub.1 -C.sub.8 alkyl, or C.sub.6 -C.sub.10 aryl, optionally R.sub.1 and R.sub.2 may be substituted by one or more hydroxy, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 hydroxyalkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.6 -C.sub.10 aryl, C.sub.6 -C.sub.10 hydroxyaryl, C.sub.6 -C.sub.10 aryloxy, --CO.sub.2 R.sub.3, CONR.sub.4 R.sub.5, or --NR.sub.4 R.sub.5 ; X and Y may be the same or different and the O, NR.sub.6, S, or CR.sub.7 R.sub.8 ; R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 may be the same or different and are hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 hydroxyalkyl, or C.sub.1 -C.sub.8 alkoxyalkyl; R.sub.4 and R.sub.5 may form a 5 or 6 membered carbocyclic ring optionally containing singularly or in combination nitrogen, oxygen or sulfur; a, b, c, d and e may be same or different and are zero to about 10; and Z is --CO.sub.2 H, --PO.sub.3 H.sub.2, --SO.sub.3 H, or --CONHOH.Methods for imaging using compositions of the invention as diagnostic imaging agents are also provided.

摘要翻译： 本发明提供新的和结构不同的组合物，其包含以下通式的化合物：其中V是CR 1或N; W为CR2或N; R 1和R 2可以相同或不同，为氢，C 1 -C 8烷基或C 6 -C 10芳基，任选地R 1和R 2可以被一个或多个羟基，C 1 -C 8烷基，C 1 -C 8羟烷基，C 1 -C 8 烷氧基，C 6 -C 10芳基，C 6 -C 10羟基芳基，C 6 -C 10芳氧基，-CO 2 R 3，CONR 4 R 5或-NR 4 R 5; X和Y可以相同或不同，O，NR6，S或CR7R8; R 3，R 4，R 5，R 6，R 7和R 8可以相同或不同，为氢，C 1 -C 8烷基，C 1 -C 8羟烷基或C 1 -C 8烷氧基烷基; R4和R5可以形成任选地单独或组合地含有氮，氧或硫的5或6元碳环; a，b，c，d和e可以相同或不同，为零至约10; Z是-CO 2 H，-PO 3 H 2，-SO 3 H或-CONHOH。 还提供了使用本发明的组合物作为诊断成像剂成像的方法。

公开(公告)号：US4762924A

公开(公告)日：1988-08-09

申请号：US62033

申请日：1987-06-15

申请人： Cedric H. Hassall ,  Geoffrey Lawton ,  Sally Redshaw

发明人： Cedric H. Hassall ,  Geoffrey Lawton ,  Sally Redshaw

IPC分类号： C07D237/04 ,  C07D487/04 ,  C07D245/00 ,  A61K31/50 ,  C07D487/06

CPC分类号： C07D487/04 ,  C07D237/04

摘要： Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkanoyl or aroyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or aryl; R.sup.4 and R.sup.5 each are hydrogen or R.sup.4 and R.sup.5 taken together are oxo; and Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --N(R.sup.6)-- in which R.sup.6 is hydrogen, alkyl or aralkyl,as well as pharmaceutically acceptable salts thereof with bases when R.sup.2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is --N(R.sup.6)--, which have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations, are described.The compounds of formula I contain at least one asymmetric carbon atom. Therefore, the invention comprises not only the optically uniform forms of these compounds, but also the various diastereoisomeric racemates and mixtures of different diastereoisomeric racemates.

摘要翻译： 式Ⅰ的化合物，其中R1是氢，烷酰基或芳酰基; R2是氢或烷基; R3是氢或芳基; R4和R5各自为氢或R4和R5一起为氧代; 其中当R 2为氢时，其中R 6为氢，烷基或芳烷基，以及其与碱的药学上可接受的盐及其与Y的药学上可接受的盐，Y为-CH 2 - ， - CH 2 CH 2 - 或-N（R 6） 描述了具有抗高血压活性并且可以用作药物制剂形式的药物的-N（R 6） - 。 式I化合物含有至少一个不对称碳原子。 因此，本发明不仅包括这些化合物的光学均匀形式，还包括各种非对映异构体外消旋体和不同非对映异构体外消旋体的混合物。