公开(公告)号：US08088726B2

公开(公告)日：2012-01-03

申请号：US10518914

申请日：2003-06-24

Applicant: Kazumichi Yamamoto ,  Kazuhiro Saito ,  Tetsuo Hoshino

Inventor： Kazumichi Yamamoto ,  Kazuhiro Saito ,  Tetsuo Hoshino

IPC: A61K38/00 ,  A61K51/00

CPC classification number: A61K38/09 ,  A61K9/1647 ,  A61K9/1694

Abstract: A process for producing a sustained-release composition which comprises mixing an aqueous solution containing a physiologically active substance and an acid or base in a molar amount of 1.5 or more times that of the physiologically active substance with a solution of a biodegradable polymer and then drying the mixture is provided.

Abstract translation: 一种缓释组合物的制造方法，其特征在于，将含有生理活性物质的水溶液与生理活性物质的摩尔量为1.5以上的酸或碱的水溶液与生物降解性聚合物的溶液混合，然后干燥 提供混合物。

公开(公告)号：US08071766B2

公开(公告)日：2011-12-06

申请号：US12363640

申请日：2009-01-30

Applicant: Young K. Chen ,  Erick Co ,  Prasuna Guntupalli ,  John D. Lawson ,  Wolfgang Reinhard Ludwig Notz ,  Jeffrey A. Stafford ,  Huong-Thu Ton-Nu

Inventor： Young K. Chen ,  Erick Co ,  Prasuna Guntupalli ,  John D. Lawson ,  Wolfgang Reinhard Ludwig Notz ,  Jeffrey A. Stafford ,  Huong-Thu Ton-Nu

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/4375

CPC classification number: C07D401/10 ,  C07D239/84 ,  C07D401/14 ,  C07D487/04

Abstract: The invention relates to HSP90 inhibiting compounds consisting of the formula: wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

Abstract translation: 本发明涉及由下式组成的HSP90抑制化合物：其中变量如本文所定义。 本发明还涉及包含这些化合物的药物组合物，试剂盒和制品; 用于制备化合物的方法和中间体; 以及使用所述化合物的方法。

公开(公告)号：US20110288040A1

公开(公告)日：2011-11-24

申请号：US13204093

申请日：2011-08-05

Applicant: Atsushi Hasuoka ,  Terufumi Takagi ,  Masahiro Kajino ,  Haruyuki Nishida

Inventor： Atsushi Hasuoka ,  Terufumi Takagi ,  Masahiro Kajino ,  Haruyuki Nishida

IPC: A61K31/7048 ,  A61K31/417 ,  A61K31/4439 ,  A61K31/4178 ,  A61P31/04 ,  A61K31/426 ,  A61K31/43 ,  A61P1/04 ,  A61P35/00 ,  A61P7/04 ,  A61K31/40 ,  A61K31/415

CPC classification number: C07D207/36 ,  A61K31/40 ,  A61K31/415 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/426 ,  A61K31/4439 ,  C07D231/12 ,  C07D233/64 ,  C07D233/84 ,  C07D277/36 ,  C07D401/12 ,  C07D409/12

Abstract: The present invention provides a compound having a superior acid secretion inhibitory action, an antiulcer activity and the like.A proton pump inhibitor containing a compound represented by the formula (I) wherein ring A is a saturated or unsaturated 5- or 6-membered ring group optionally having, as a ring-constituting atom besides carbon atom, 1 to 4 hetero atoms selected from a nitrogen atom, an oxygen atom and a sulfur atom, ring-constituting atoms X1 and X2 are each a carbon atom or a nitrogen atom, a ring-constituting atom X3 is a carbon atom, a nitrogen atom, an oxygen atom or a sulfur atom, R1 is an optionally substituted aryl group or an optionally substituted heteroaryl group, R2 is an optionally substituted alkyl group, an optionally substituted aryl group or an optionally substituted heteroaryl group, R3 is an aminomethyl group optionally substituted by 1 or 2 lower alkyl groups, which is a substituent on a ring-constituting atom other than X1, X2 and X3, and ring A optionally further has substituent(s) selected from a lower alkyl group, a halogen atom, a cyano group and an oxo group, or a salt thereof or a prodrug thereof.

Abstract translation: 本发明提供具有优异的酸分泌抑制作用，抗溃疡活性等的化合物。 含有式（I）表示的化合物的质子泵抑制剂，其中环A是饱和或不饱和的5-或6-元环基，任选具有除碳原子之外的环构成原子，含有1-4个选自 氮原子，氧原子和硫原子，构成环的原子X1和X2各自为碳原子或氮原子，构成环的原子X3为碳原子，氮原子，氧原子或硫原子 原子，R 1是任选取代的芳基或任选取代的杂芳基，R 2是任选取代的烷基，任选取代的芳基或任选取代的杂芳基，R 3是任选被1或2个低级烷基取代的氨基甲基 其是除X1，X2和X3以外的环构成原子上的取代基，环A任选地还具有选自低级烷基，卤素原子，氰基和氧代基的取代基，或 盐在那里 f或其前药。

公开(公告)号：US08034812B2

公开(公告)日：2011-10-11

申请号：US12263884

申请日：2008-11-03

Applicant: Nozomu Sakai ,  Shinichi Imamura ,  Naoki Miyamoto ,  Takaharu Hirayama

Inventor： Nozomu Sakai ,  Shinichi Imamura ,  Naoki Miyamoto ,  Takaharu Hirayama

IPC: C07D487/04 ,  A61K31/4985 ,  A61P35/00

CPC classification number: C07D487/04

Abstract: The present invention provides an imidazopyridazine derivative compound having a potent kinase inhibitory activity and a pharmaceutical agent thereof useful for treatment or prevention of cancer and the like. One such compound is represented by the formula: or a salt thereof or a prodrug thereof. The pharmaceutical agent contains the imidazopyridazine derivative compound or a prodrug thereof, which is a kinase (VEGFR, VEGFR2, PDGFR, Raf) inhibitor, an angiogenesis inhibitor, an agent for the prophylaxis or treatment of cancer, a cancer growth inhibitor, or a cancer metastasis suppressor.

Abstract translation: 本发明提供了可用于治疗或预防癌症等的具有强激酶抑制活性的咪唑并哒嗪衍生化合物及其药剂。 一种这样的化合物由下式表示：或其盐或其前药。 药剂含有作为激酶（VEGFR，VEGFR2，PDGFR，Raf）抑制剂，血管发生抑制剂，癌症预防或治疗剂，癌症生长抑制剂或癌症的咪唑并哒嗪衍生物化合物或其前药 转移抑制因子

公开(公告)号：US08030333B2

公开(公告)日：2011-10-04

申请号：US12771486

申请日：2010-04-30

Applicant: Akira Fujishima ,  Isao Aoki ,  Keiji Kamiyama

Inventor： Akira Fujishima ,  Isao Aoki ,  Keiji Kamiyama

IPC: A61K31/04 ,  C07D215/38

CPC classification number: C07D401/12 ,  A61K31/4439 ,  C07B2200/13

Abstract: A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.

Abstract translation: （R）-2 - [[3-甲基-4-（2,2,2-三氟乙氧基）-2-吡啶基]甲基]亚磺酰基] -1H-苯并咪唑或其盐的新结晶为 适用于优秀的抗溃疡剂。

公开(公告)号：US08026234B2

公开(公告)日：2011-09-27

申请号：US12237306

申请日：2008-09-24

Applicant: Takashi Ichikawa ,  Stephen W. Kaldor

Inventor： Takashi Ichikawa ,  Stephen W. Kaldor

IPC: C07D487/04 ,  A61K31/55

CPC classification number: C07D487/04 ,  C07D487/14 ,  C07D519/00

Abstract: Compounds of the following formula are provided for use with kinases: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

Abstract translation: 提供下式的化合物用于激酶：其中变量如本文所定义。 还提供了包含这些化合物的药物组合物，试剂盒和制品; 用于制备化合物的方法和中间体; 以及使用所述化合物的方法。

公开(公告)号：US08022057B2

公开(公告)日：2011-09-20

申请号：US12267353

申请日：2008-11-07

Applicant: Qing Dong ,  Toufike Kanouni ,  Michael B. Wallace

Inventor： Qing Dong ,  Toufike Kanouni ,  Michael B. Wallace

IPC: C07D471/04 ,  C07D513/04 ,  C07D498/04 ,  A61K31/437 ,  A61K31/4375 ,  A61P35/04 ,  C12N9/99

CPC classification number: C07D471/04 ,  C07D498/04 ,  C07D513/04

Abstract: Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

Abstract translation: 提供下式的化合物用于MEK：其中变量如本文所定义。 还提供了包含这些化合物的药物组合物，试剂盒和制品; 用于制备化合物的方法和中间体; 以及使用所述化合物的方法。

公开(公告)号：US07989445B2

公开(公告)日：2011-08-02

申请号：US11919301

申请日：2006-04-27

Applicant: Toshiki Murata ,  Shingo Makino

Inventor： Toshiki Murata ,  Shingo Makino

IPC: A61K31/55 ,  A61K31/519 ,  A61P3/04 ,  C07D495/04

CPC classification number: C07D495/04

Abstract: The present invention relates to a compound represented by the formula: wherein Ar is an optionally substituted ring; A is a spacer having a main chain of 1 to 4 atoms; B is a bond, a C1-10 alkylene group or an oxygen atom; R3 and R5 are each independently a hydrogen atom or a substituent; R4 is an optionally substituted cyclic group or an optionally substituted C1-10 alkyl group; and R1 and R2 are each independently a hydrogen atom or a substituent, or R1 and R2 or R1 and B are bonded to form an optionally substituted nitrogen-containing heterocycle, or R1 and Ar are bonded to form an optionally substituted nitrogen-containing fused heterocycle, or a salt thereof. The thienopyrimidone compound of the present invention has a superior melanin-concentrating hormone receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of obesity and the like.

Abstract translation: 本发明涉及由下式表示的化合物：其中Ar是任选取代的环; A是具有1至4个原子的主链的间隔基; B是键，C1-10亚烷基或氧原子; R3和R5各自独立地为氢原子或取代基; R4是任选取代的环状基团或任选取代的C 1-10烷基; 并且R 1和R 2各自独立地为氢原子或取代基，或R 1和R 2或R 1和B键合以形成任选取代的含氮杂环，或R 1和Ar键合以形成任选取代的含氮稠合杂环 ，或其盐。 本发明的噻吩并嘧啶酮化合物具有优异的黑色素浓缩激素受体拮抗作用，可用作预防或治疗肥胖症等的药剂。

公开(公告)号：US20110178060A1

公开(公告)日：2011-07-21

申请号：US13119743

申请日：2009-09-18

Applicant: Junya Shirai ,  Hideyuki Sugiyama ,  Taku Kamei ,  Hironobu Maezaki

Inventor： Junya Shirai ,  Hideyuki Sugiyama ,  Taku Kamei ,  Hironobu Maezaki

IPC: A61K31/397 ,  C07D211/58 ,  A61K31/451 ,  C07D401/06 ,  A61K31/4545 ,  C07D207/50 ,  A61K31/40 ,  C07D403/02 ,  A61K31/4178 ,  C07D401/02 ,  A61K31/4439 ,  C07D413/02 ,  A61K31/5355 ,  A61P13/00 ,  A61P1/00 ,  A61P25/00

CPC classification number: C07D401/04 ,  C07D207/14 ,  C07D211/58 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D413/04 ,  C07D413/06 ,  C07D413/08 ,  C07D413/14 ,  C07D417/08

Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle; ring B is an aromatic ring optionally having substituent(s); ring D is an aromatic ring optionally having substituent(s); L is a group represented by the formula R2, R3, R4a and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain; R1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like. The compound has a superior tachykinin receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of various diseases such as lower urinary tract diseases, digestive tract diseases, central neurological disease and the like.

Abstract translation: 本发明涉及由下式表示的化合物：其中环A是含氮杂环; 环B是任选具有取代基的芳香环; 环D是任选具有取代基的芳香环; L是由式R2表示的基团，R3，R4a和R4b各自独立地为氢原子，任选卤代的C 1-6烷基或任选卤代的C 3-6环烷基，或者R 2和R 3经由亚烷基 链或亚链烯基，或者R4a和R4b任选地通过亚烷基链或亚烯基链键合; R1是氢原子或取代基; m和n各自独立地为0〜5的整数; m + n为2〜5的整数。 并且是单键或双键，或其盐; 等等。 该化合物具有优异的速激肽受体拮抗作用，可用作预防或治疗诸如下尿路疾病，消化道疾病，中枢神经疾病等各种疾病的药剂。

公开(公告)号：US07982044B2

公开(公告)日：2011-07-19

申请号：US13022563

申请日：2011-02-07

Applicant: Masato Yoshida ,  Nobuki Sakauchi

Inventor： Masato Yoshida ,  Nobuki Sakauchi

IPC: C07D213/82

CPC classification number: C07D213/82 ,  C07D401/10 ,  C07D413/10

Abstract: The present invention aims to provide an iminopyridine derivative compound having an α1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.

Abstract translation: 本发明旨在提供具有α1D肾上腺素能受体拮抗作用的亚氨基吡啶衍生物化合物，其可用作预防或治疗下尿路疾病等。 本发明提供由下式表示的化合物，其中每个符号如说明书中所定义，或其盐。