公开(公告)号：US20050288513A1

公开(公告)日：2005-12-29

申请号：US11205426

申请日：2005-08-17

Applicant: Ian Lynch ,  Michael Sasse ,  Bernadette Choudary

Inventor： Ian Lynch ,  Michael Sasse ,  Bernadette Choudary

IPC: A61K31/425 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4439 ,  A61P3/10 ,  C07D20060101 ,  C07D417/02 ,  C07D417/12

CPC classification number: C07D417/12

Abstract: A hydrate of 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl)thiazolidine-2,4-dione, maleic acid salt, characterized in that it: (i) comprises water in the range of from 0.3 to 0.6 molar equivalents; and (ii) provides an infra red spectrum containing peaks at 1757, 1331, 1290, 1211 and 767 cm−1; and/or (iii) provides a Raman spectrum containing peaks at 1758, 1610, 1394, 1316 and 1289 cm−1; and/or (iv) provides a solid state nuclear magnetic resonance spectrum containing chemical shifts substantially as set out in Table I herein; and/or (v) provides an X-ray powder diffraction (XRPD) pattern substantially as set out in Figure IV herein; a process for the preparation of such a compound, a pharmaceutical composition containing such a compound and the use of such a compound or composition in medicine.

Abstract translation: 5- [4- [2-（N-甲基-N-（2-吡啶基）氨基）乙氧基]苄基）噻唑烷-2,4-二酮的马来酸盐的水合物，其特征在于：（i）包含 在0.3至0.6摩尔当量的范围内的水; 和（ii）提供在1757,1331,1290,1211和767cm -1处含有峰的红外光谱; 和/或（iii）提供在1758,1610,1394,1316和1289cm -1处含有峰的拉曼光谱; 和/或（iv）提供包含基本如本文表I所示的化学位移的固态核磁共振光谱; 和/或（v）提供基本上如图IV中所示的X射线粉末衍射（XRPD）图案; 制备这种化合物的方法，含有这种化合物的药物组合物和这种化合物或组合物在医药中的用途。

公开(公告)号：US20050261320A1

公开(公告)日：2005-11-24

申请号：US10646980

申请日：2003-08-22

Applicant: Chung Chu ,  Yung-Chi Cheng

Inventor： Chung Chu ,  Yung-Chi Cheng

IPC: A61K31/506 ,  A61K20060101 ,  A61K31/505 ,  A61K31/513 ,  A61P35/00 ,  C07D20060101 ,  C07D405/04 ,  C07F20060101 ,  C07H17/00 ,  C07D45/04

CPC classification number: C07D405/04 ,  C07H17/00

Abstract: (−)-(2S,4S)-1-(2-Hydroxymethyl-1,3-dioxolan-4-yl)cytosine (also referred to as (−)-OddC) or its derivative and its use to treat cancer in animals, including humans.

Abstract translation: （ - ） - （2S，4S）-1-（2-羟甲基-1,3-二氧戊环-4-基）胞嘧啶（也称为（ - ） - OddC）或其衍生物及其用于治疗动物癌症的用途 ，包括人类。

公开(公告)号：US20050261279A1

公开(公告)日：2005-11-24

申请号：US10515998

申请日：2003-05-28

Applicant: Ian Forbes ,  Vincenzo Garzya ,  Andrew Gribble ,  Andrew Lightfoot ,  Andrew Payne ,  Graham Walker

Inventor： Ian Forbes ,  Vincenzo Garzya ,  Andrew Gribble ,  Andrew Lightfoot ,  Andrew Payne ,  Graham Walker

IPC: C07D217/22 ,  A61K20060101 ,  A61K31/4035 ,  A61K31/47 ,  A61K31/4704 ,  A61K31/472 ,  A61K31/55 ,  A61P20060101 ,  A61P1/00 ,  A61P1/08 ,  A61P3/04 ,  A61P15/00 ,  A61P25/00 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/36 ,  A61P43/00 ,  C07D20060101 ,  C07D209/44 ,  C07D217/02 ,  C07D223/16 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

CPC classification number: C07D223/16 ,  C07D209/44 ,  C07D217/02

Abstract: The invention provides compounds of formula (I): wherein A and B represent the groups —(CH2)m— and —(CH2)n— respectively; R1 represents hydrogen or C1-6alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxy C1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR5R6, —SO2NR5R6, —(CH2)pNR5R6, —(CF)pNR5COR6, optionally substituted aryl ring, optionally substituted heteroaryl ring or optionally substituted heterocyclyl ring; R3 represents optionally substituted aryl ring or optionally substituted heteroaryl ring; R4 represents hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, trifluoromethyl, trifluoromethoxy, halogen, —OSO2CF3, —(CH2)pC3-6cycloalkyl, —(CH2)qOC1-6alkyl or —(CH2)pOC3-6cycloalkyl; R5 and R6 each independently represent hydrogen, C1-6alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalkyl ring or an oxo-substituted azacycloalkyl ring; Z represents —(CH2)rX— wherein the —(CH2)r— group is attached to R3, or —X(CH2)r— wherein X is attached to R3, and wherein any of the —CH2— groups may be optionally substituted by one or more C1-6alkyl groups; X represents oxygen, —NR7 or —CH2— wherein the —CH2— group may be optionally substituted by one or more C1-6alkyl groups; R7 represents hydrogen or C1-6alkyl; m and n independently represent an integer selected from 1 and 2; p independently represents an integer selected from 0, 1, 2 and 3; q independently represents an integer selected from 1, 2 and 3; r independently represents an integer selected from 0, 1, and 2; or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful in therapy, in particular as antipsychotic agents.

公开(公告)号：US20050250776A1

公开(公告)日：2005-11-10

申请号：US11179507

申请日：2005-07-13

Applicant: Tjeerd Barf ,  Rikard Emond ,  Guido Kurz ,  Marianne Nilsson ,  Jerk Vallgarda ,  Lian Zhang

Inventor： Tjeerd Barf ,  Rikard Emond ,  Guido Kurz ,  Marianne Nilsson ,  Jerk Vallgarda ,  Lian Zhang

IPC: C07D20060101 ,  C07D277/38 ,  C07D277/52 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D521/00 ,  C07D417/02 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/5377

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D277/52 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

Abstract translation: 本发明涉及具有式（I）的化合物以及包含该化合物的药物组合物，以及该化合物在医药中的用途以及制备作用于人类11-β-羟基类固醇脱氢酶 1型酶。

公开(公告)号：US20050245592A1

公开(公告)日：2005-11-03

申请号：US11158941

申请日：2005-06-22

Applicant: Shuichi Suzuki ,  Makoto Kotake ,  Mitsuaki Miyamoto ,  Tetsuya Kawahara ,  Akiharu Kajiwara ,  Ieharu Hishinuma ,  Kazuo Okano ,  Syuhei Miyazawa ,  Richard Clark ,  Fumihiro Ozaki ,  Nobuaki Sato ,  Masanobu Shinoda ,  Atsushi Kamada ,  Itaru Tsukada ,  Fumiyoshi Matsuura ,  Yoshimitsu Naoe ,  Taro Terauchi ,  Yoshiaki Oohashi ,  Osamu Ito ,  Hiroshi Tanaka ,  Takashi Musha ,  Motoji Kogushi ,  Tsutomu Kawata ,  Toshiyuki Matsuoka ,  Hiroko Kobayashi ,  Ken-ichi Chiba ,  Akifumi Kimura ,  Naoto Ono

Inventor： Shuichi Suzuki ,  Makoto Kotake ,  Mitsuaki Miyamoto ,  Tetsuya Kawahara ,  Akiharu Kajiwara ,  Ieharu Hishinuma ,  Kazuo Okano ,  Syuhei Miyazawa ,  Richard Clark ,  Fumihiro Ozaki ,  Nobuaki Sato ,  Masanobu Shinoda ,  Atsushi Kamada ,  Itaru Tsukada ,  Fumiyoshi Matsuura ,  Yoshimitsu Naoe ,  Taro Terauchi ,  Yoshiaki Oohashi ,  Osamu Ito ,  Hiroshi Tanaka ,  Takashi Musha ,  Motoji Kogushi ,  Tsutomu Kawata ,  Toshiyuki Matsuoka ,  Hiroko Kobayashi ,  Ken-ichi Chiba ,  Akifumi Kimura ,  Naoto Ono

IPC: A61K20060101 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/437 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/538 ,  A61P20060101 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P19/10 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D20060101 ,  C07D207/22 ,  C07D207/24 ,  C07D207/26 ,  C07D207/263 ,  C07D207/267 ,  C07D207/34 ,  C07D209/44 ,  C07D209/52 ,  C07D209/54 ,  C07D209/62 ,  C07D209/96 ,  C07D213/73 ,  C07D213/74 ,  C07D233/46 ,  C07D233/66 ,  C07D233/88 ,  C07D233/90 ,  C07D235/30 ,  C07D249/14 ,  C07D261/14 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07D409/10 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  C07D491/10 ,  C07D498/04 ,  C07D521/00 ,  C07D209/48 ,  C07D471/02

CPC classification number: C07D209/44

Abstract: A 2-iminopyrrolidine derivative represented by the formula: {wherein ring B represents a benzene ring, pyridine ring, etc.; R101-R103 represent hydrogen, halogen, C1-6 alkyl, etc.; R5 represents hydrogen, C1-6 alkyl, C1-6 alkoxy-C1-6 alkyl, etc.; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R10-R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc.; and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocyclic ring], etc.}, or a salt thereof.

Abstract translation: 由下式表示的2-亚氨基吡咯烷衍生物：其中环B表示苯环，吡啶环等; R 101为-O-，卤素，C 1-6烷基等; R 5表示氢，C 1-6烷基，C 1-6烷氧基-C 1-6烷基 等等 R 6表示氢，C 1-6烷基，C 1-6烷氧基羰基等; Y 1表示单键，-CH 2 - 等; Y 2表示单键，-CO-等; 和Ar表示氢，由下式表示的基团：其中R 10 -R 14表示氢，C 1-6烷基，羟基 C 1-6烷氧基等; 并且R 11和R 12或R 12和R 13可以键合在一起形成5-8个 - 杂环]等，或其盐。

公开(公告)号：US20050234052A1

公开(公告)日：2005-10-20

申请号：US11159897

申请日：2005-06-23

Applicant: J. Slatter

Inventor： J. Slatter

IPC: C07D263/22 ,  A61K9/20 ,  A61K9/48 ,  A61K31/5377 ,  A61K31/541 ,  A61P27/02 ,  A61P31/04 ,  C07D20060101

CPC classification number: A61K31/5377 ,  A61K31/541

Abstract: The invention provides a method for treating ocular infections such as endophthalmitis.

Abstract translation: 本发明提供了治疗眼内感染如眼内炎的方法。

公开(公告)号：US20050232871A1

公开(公告)日：2005-10-20

申请号：US11152741

申请日：2005-06-13

Applicant: Michael Humphrey ,  Paul Miller ,  Michael Shepherd

Inventor： Michael Humphrey ,  Paul Miller ,  Michael Shepherd

IPC: C07D471/14 ,  A61K20060101 ,  A61K9/00 ,  A61K9/14 ,  A61K9/72 ,  A61K31/437 ,  A61K31/46 ,  A61K47/26 ,  A61M13/00 ,  A61M15/00 ,  A61P20060101 ,  A61P11/00 ,  A61P11/06 ,  A61P43/00 ,  C07D20060101 ,  A61K31/4745 ,  A61L9/04

CPC classification number: A61K9/0075 ,  A61K9/14 ,  A61K31/437 ,  A61K31/439 ,  A61K31/46 ,  A61K47/26 ,  A61M13/00 ,  A61M15/00 ,  C07D471/14 ,  A61K2300/00

Abstract: The present invention relates to an inhaled formulation comprising a compound selected from a particular class of 5,6-dihydro-9H-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-a]pyridines which is capable of delivering the compound as fine, solid particles to the lung and the use of such a formulation in the treatment of certain diseases such as respiratory diseases. By the use of such formulations, it is possible to eliminate the unwanted cough response associated with the use of these compounds in solution metered dose inhalers, which response can prevent the administration of a therapeutically effective dose and, in the long term, undermine patient compliance.

Abstract translation: 本发明涉及包含选自特定类别的5,6-二氢-9H-吡唑并[3,4-c] -1,2,4-三唑并[4,3-a]吡啶的化合物的吸入制剂，其中 能够将化合物作为细小的固体颗粒递送至肺，以及使用这种制剂来治疗某些疾病如呼吸道疾病。 通过使用这种制剂，可以消除与在溶液计量吸入器中使用这些化合物相关的不希望的咳嗽反应，该反应可以防止施用治疗有效剂量，并且从长期来看，会破坏患者依从性 。

公开(公告)号：US06956123B2

公开(公告)日：2005-10-18

申请号：US10664539

申请日：2003-09-18

Applicant: James H. Johnson ,  T. G. Sambandan ,  Barry J. Haad ,  Christopher D. Howe ,  Roland R. Franke ,  Brian A. Bucher ,  John S. Juchum ,  Rex T. Gallagher ,  Marc A. Plant ,  Edward M. De Simone, III ,  Dong S. Yang

Inventor： James H. Johnson ,  T. G. Sambandan ,  Barry J. Haad ,  Christopher D. Howe ,  Roland R. Franke ,  Brian A. Bucher ,  John S. Juchum ,  Rex T. Gallagher ,  Marc A. Plant ,  Edward M. De Simone, III ,  Dong S. Yang

IPC: C07D20060101 ,  C07D305/14

CPC classification number: C07D305/14 ,  B01D15/3804 ,  B01D15/424

Abstract: This invention is directed to a method for isolating and/or purifying one or more taxanes from materials comprising taxanes. In one embodiment, the method comprises the steps of: (a) treating a taxane containing material with an amino containing material attached to a solid matrix, such as a polyethyleneimine-bonded silica chromatographic resin; (b) eluting the desired taxane compound from the resin; and (c) recovering the eluted taxane compound.

Abstract translation: 本发明涉及一种用于从包含紫杉烷类的材料中分离和/或纯化一种或多种紫杉烷的方法。 在一个实施方案中，该方法包括以下步骤：（a）用附着在固体基质上的含氨基物质如聚乙烯亚胺键合的二氧化硅色谱树脂处理含紫杉烷的材料; （b）从树脂中洗脱所需的紫杉烷化合物; 和（c）回收洗脱的紫杉烷化合物。

公开(公告)号：US20050209235A1

公开(公告)日：2005-09-22

申请号：US11125021

申请日：2005-05-09

Applicant: Harold Mastalerz ,  Guifen Zhang ,  James Tarrant ,  Gregory Vite

Inventor： Harold Mastalerz ,  Guifen Zhang ,  James Tarrant ,  Gregory Vite

IPC: A61K31/53 ,  A61K31/5377 ,  A61K45/00 ,  A61P35/00 ,  A61P43/00 ,  C07D20060101 ,  C07D487/04

CPC classification number: C07D487/04 ,  C04B41/009 ,  C04B41/4584 ,  C04B2111/00793 ,  C04B41/4515 ,  C04B41/4535 ,  C04B41/457 ,  C04B41/4582 ,  C04B14/46

Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.

Abstract translation: 本发明提供式I化合物及其药学上可接受的盐。 式I化合物抑制生长因子受体如HER1，HER2和HER4的酪氨酸激酶活性，从而使其成为抗增殖剂。 式I化合物还可用于治疗与通过生长因子受体操作的信号转导途径相关的其它疾病。

公开(公告)号：US06946555B2

公开(公告)日：2005-09-20

申请号：US10368928

申请日：2003-02-19

Applicant: Michael Butters ,  Alan John Pettman

Inventor： Michael Butters ,  Alan John Pettman

IPC: C07D239/26 ,  A61K31/4196 ,  A61K31/505 ,  A61P31/04 ,  C07D20060101 ,  C07D239/30 ,  C07D239/34 ,  C07D239/36 ,  C07D249/08 ,  C07D403/06

CPC classification number: C07D239/30 ,  C07D239/34 ,  C07D239/36 ,  C07D403/06

Abstract: The invention provides a process for the preparation of a compound of the formula: or an acid addition or base salt thereof, wherein R is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and trifluoromethyl; R1 is C1-C6 alkyl; and “Het” is pyrimidinyl optionally substituted by 1 to 3 substituents each independently selected from C1-C4 alkyl, C1-C4 alkoxy, halo, oxo, benzyl and benzyloxy, comprising reaction of a compound of the formula:  wherein R is as previously defined for a compound of the formula (I), with a compound of the formula:  wherein R1 and “Het” are as previously defined for a compound of the formula (I) and X is chloro, bromo or iodo, in the presence of zinc, iodine and/or a Lewis acid and an aprotic organic solvent: said process being optionally followed by conversion of the compound of the formula (I) to an acid addition or base salt thereof.

Abstract translation: 本发明提供了一种制备下式化合物或其酸加成盐或碱盐的方法，其中R是任选被1-3个各自独立地选自卤素和三氟甲基的取代基取代的苯基; R 1是C 1 -C 6烷基; R 1是C 1 -C 6烷基; “Het”是任选被1至3个独立地选自C 1 -C 4烷基，C 1 -C 3烷基的取代基取代的嘧啶基， 包括下式化合物与式（I）化合物反应：其中R如前面定义的式（I）化合物与下式化合物反应：其中 R 1和/或Het如先前对于式（I）化合物所定义，X是氯，溴或碘，在锌，碘和/或路易斯酸和 非质子有机溶剂：所述方法任选地随后将式（I）化合物转化为其酸加成盐或碱盐。