公开(公告)号：US20120172293A1

公开(公告)日：2012-07-05

申请号：US13381737

申请日：2010-07-01

Applicant: Taiji Asami ,  Naoki Nishizawa ,  Ayumu Niida ,  Yusuke Adachi

Inventor： Taiji Asami ,  Naoki Nishizawa ,  Ayumu Niida ,  Yusuke Adachi

IPC: A61K38/10 ,  A61P3/04 ,  C07K7/08

CPC classification number: C07K14/575 ,  A61K38/00

Abstract: The present invention aims to provide a peptide having a superior Y2 receptor agonist action and useful as an agent for the prophylaxis or treatment of obesity and the like.A peptide represented by the formula: P1-X1-A25-A26-A27-A28-A29-A30-A31-A32-A33-A34-A35-A36-NH2 wherein each symbol is as described in the specification, or a salt thereof.

Abstract translation: 本发明的目的在于提供具有优异的Y2受体激动剂作用的肽，可用作预防或治疗肥胖症等的药剂。 由式：P1-X1-A25-A26-A27-A28-A29-A30-A31-A32-A33-A34-A35-A36-NH2表示的肽，其中每个符号如说明书中所述，或其盐 。

公开(公告)号：US08212046B2

公开(公告)日：2012-07-03

申请号：US13168121

申请日：2011-06-24

Applicant: Hideo Hashimoto ,  Hideaki Maruyama

Inventor： Hideo Hashimoto ,  Hideaki Maruyama

IPC: C07D401/00

CPC classification number: C07D401/12 ,  A61K31/4439 ,  C30B7/00

Abstract: The present invention relates to a production method of a crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]benzimidazole.n′H2O (wherein n′ is about 0 to about 0.1) or a salt thereof, which characteristically includes crystallization from an organic solvent solution or suspension in which (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]benzimidazole.nH2O (wherein n is about 0.1 to about 1.0) or a salt thereof has been dissolved or suspended, and the like, and provides a convenient method for efficiently producing an optically active sulfoxide derivative having an extremely high enantiomer excess in high yield at an industrial large scale.

Abstract translation: 本发明涉及（R）-2 - [[[3-甲基-4-（2,2,2-三氟乙氧基）-2-吡啶基]甲基]亚磺酰基]苯并咪唑的溶液的制备方法。 （其中n'为约0至约0.1）或其盐，其特征在于包括从有机溶剂溶液或悬浮液中结晶，其中（R）-2 - [[[3-甲基-4-（2,2,2' - 三氟乙氧基）-2-吡啶基]甲基]亚磺酰基]苯并咪唑nH 2 O（其中n为约0.1至约1.0）或其盐已经溶解或悬浮等，并且提供了有效制备光学活性的方便的方法 在工业上大规模地高收率地具有极高对映体过量的亚砜衍生物。

公开(公告)号：US20120142005A1

公开(公告)日：2012-06-07

申请号：US13322176

申请日：2010-05-25

Applicant: Masaki Hosoya ,  Yuya Kunisada ,  Masanobu Shoji

Inventor： Masaki Hosoya ,  Yuya Kunisada ,  Masanobu Shoji

IPC: C12Q1/68

CPC classification number: G01N33/5073 ,  G01N33/5023

Abstract: A method for screening for a substance capable of regulating the regeneration, proliferation or differentiation of a cell or an organ, which comprises the steps of: (1) allowing a cell having a regenerative, proliferative or differentiative capability to form an embryoid body; (2) treating the embryoid body produced in step (1) with a digestive enzyme to prepare single cells from the embryoid body; (3) seeding the cells prepared in step (2) onto an adhesive plate, and adding a candidate substance to the plate to perform adhesion culturing of the cells on the plate; (4) conducting quantitative and simultaneous analysis of the levels of expression of at least two types of genes involved in the regeneration, proliferation or differentiation of cells after the adhesion culturing of step (3); and (5) evaluating the influence of the candidate substance on the regeneration, proliferation or differentiation of cells based on the results of the quantitative analysis obtained in step (4).

Abstract translation: 一种筛选能够调节细胞或器官的再生，增殖或分化的物质的方法，其包括以下步骤：（1）使具有再生，增殖或分化能力的细胞形成胚状体; （2）用消化酶处理步骤（1）产生的胚状体，从胚状体中制备单细胞; （3）将步骤（2）中制备的细胞接种到粘合板上，并将候选物质加入板中以进行细胞在板上的粘附培养; （4）对步骤（3）的粘附培养后细胞的再生，增殖或分化中至少两种类型的基因的表达水平进行定量和同时分析; （5）基于步骤（4）中得到的定量分析结果，评估候选物质对细胞再生，增殖或分化的影响。

公开(公告)号：US08163755B2

公开(公告)日：2012-04-24

申请号：US12869452

申请日：2010-08-26

Applicant: Bohan Jin ,  Nicholas Scorah ,  Qing Dong

Inventor： Bohan Jin ,  Nicholas Scorah ,  Qing Dong

IPC: A61K31/497 ,  C07D237/36

CPC classification number: C07D498/14

Abstract: The present invention provides mTOR inhibitors of the formula wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods of making the compounds and intermediates thereof; and methods of using the compounds.

Abstract translation: 本发明提供下式的mTOR抑制剂，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; 制备化合物及其中间体的方法; 和使用该化合物的方法。

公开(公告)号：US20120095057A1

公开(公告)日：2012-04-19

申请号：US13260507

申请日：2010-03-25

Applicant: Haruyuki Nishida ,  Ikuo Fujimori

Inventor： Haruyuki Nishida ,  Ikuo Fujimori

IPC: A61K31/4439 ,  A61P1/04 ,  A61P35/00 ,  C07D401/04

CPC classification number: C07D401/04

Abstract: Provided is a compound having a superior acid secretion suppressive action, antiulcer activity and the like.A compound represented by the formula wherein R1 is a substituent, R2 is (i) a hydrogen atom, (ii) a C1-6 alkyl group optionally having a halogen atom or (iii) a cyano group, R3 is (i) a hydrogen atom, (ii) a halogen atom, (iii) a cyano group, (iv) a C1-6 alkyl group optionally having a halogen atom or (v) a C1-6 alkoxy group optionally having a halogen atom, one of R2 and R3 is a hydrogen atom, and the other is a substituent other than a hydrogen atom, or a salt thereof.

Abstract translation: 提供具有优异的酸分泌抑制作用，抗溃疡活性等的化合物。 由下式表示的化合物其中R1是取代基，R2是（i）氢原子，（ii）任选具有卤素原子的C1-6烷基或（iii）氰基，R3是（i）氢 原子，（ii）卤素原子，（iii）氰基，（iv）任选具有卤素原子的C 1-6烷基或（v）任选具有卤素原子的C 1-6烷氧基，R 2和 R3是氢原子，另一个是氢原子以外的取代基或其盐。

公开(公告)号：US20120088826A1

公开(公告)日：2012-04-12

申请号：US13325946

申请日：2011-12-14

Applicant: Shinichi Urayama ,  Eigo Mutou ,  Atsushi Inagaki ,  Takashi Okada ,  Shigeharu Sugisaki

Inventor： Shinichi Urayama ,  Eigo Mutou ,  Atsushi Inagaki ,  Takashi Okada ,  Shigeharu Sugisaki

IPC: A61K31/343 ,  A61P25/20 ,  C07D307/77

CPC classification number: C07D307/77 ,  A61K31/343 ,  C07D307/80 ,  C07D307/81

Abstract: An industrial process for production of high-purity optically active amine derivatives in high yield while inhibiting the formation of by-products, which comprises subjecting (E)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-ylidene)ethylamine to asymmetric reduction, catalytically reducing the obtained product at a reaction temperature of 40 to 100° C. and a pH of 3 to 9, subjecting the obtained (S)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethylamine to propionylation, and then crystallizing the reaction mixture.

Abstract translation: 一种以高产率生产高纯度光学活性胺衍生物同时抑制副产物形成的工业方法，其包括使（E）-2-（1,6,7,8-四氢-2H-茚并[5 ，4-b]呋喃-8-亚基）乙胺进行不对称还原，在40〜100℃的反应温度和3〜9的pH下催化还原得到的（S）-2-（ 1,6,7,8-四氢-2H-茚并[5,4-b]呋喃-8-基）乙胺进行丙酰化，然后使反应混合物结晶。

公开(公告)号：US08148383B2

公开(公告)日：2012-04-03

申请号：US12696147

申请日：2010-01-29

Applicant: Tsuyoshi Maekawa ,  Hideyuki Igawa

Inventor： Tsuyoshi Maekawa ,  Hideyuki Igawa

IPC: A01N43/90 ,  A61K31/519 ,  C07D487/00

Abstract: Provided is a novel compound represented by the following formula Wherein each symbol is as defined in the specification, or a salt thereof, which has an angiotensin II receptor antagonistic activity and a peroxisome proliferator-activated receptor γ agonistic activity, and is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and/or metabolic diseases such as diabetes and the like, and the like.

公开(公告)号：US08097737B2

公开(公告)日：2012-01-17

申请号：US11662684

申请日：2005-09-12

Applicant: Shinichi Urayama ,  Eigo Mutou ,  Atsushi Inagaki ,  Takashi Okada ,  Shigeharu Sugisaki

Inventor： Shinichi Urayama ,  Eigo Mutou ,  Atsushi Inagaki ,  Takashi Okada ,  Shigeharu Sugisaki

IPC: C07D307/93

CPC classification number: C07D307/77 ,  A61K31/343 ,  C07D307/80 ,  C07D307/81

Abstract: An industrial process for production of high-purity optically active amine derivatives in high yield while inhibiting the formation of by-products, which comprises subjecting (E)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-ylidene)ethylamine to asymmetric reduction, catalytically reducing the obtained product at a reaction temperature of 40 to 100° C. and a pH of 3 to 9, subjecting the obtained (S)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethylamine to propionylation, and then crystallizing the reaction mixture.

Abstract translation: 一种以高产率生产高纯度光学活性胺衍生物同时抑制副产物形成的工业方法，其包括使（E）-2-（1,6,7,8-四氢-2H-茚并[5 ，4-b]呋喃-8-亚基）乙胺进行不对称还原，在40〜100℃的反应温度和3〜9的pH下催化还原得到的（S）-2-（ 1,6,7,8-四氢-2H-茚并[5,4-b]呋喃-8-基）乙胺进行丙酰化，然后使反应混合物结晶。

公开(公告)号：US08093382B2

公开(公告)日：2012-01-10

申请号：US12964410

申请日：2010-12-09

Applicant: Jun Feng ,  Stephen L. Gwaltney ,  Michael B. Wallace ,  Jeffrey A. Stafford ,  Zhiyuan Zhang

Inventor： Jun Feng ,  Stephen L. Gwaltney ,  Michael B. Wallace ,  Jeffrey A. Stafford ,  Zhiyuan Zhang

IPC: C07D513/04

CPC classification number: C07D471/04 ,  C07D487/04 ,  C07D513/04

Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a member selected from the group consisting of: wherein E is CH or N, Q is selected from the group consisting of CO, CS, SO, SO2, or C═NR4, and L, X, Z, R2 and R3 are as defined herein.

Abstract translation: 提供化合物，药物，试剂盒和方法用于DPP-IV和其它S9蛋白酶，其包含选自以下的成员：其中E是CH或N，Q选自CO，CS，SO ，SO 2或C≡NR4，并且L，X，Z，R 2和R 3如本文所定义。

公开(公告)号：US08088821B2

公开(公告)日：2012-01-03

申请号：US12659695

申请日：2010-03-17

Applicant: Tsuneo Yasuma ,  Nobuyuki Negoro ,  Masahiro Itou

Inventor： Tsuneo Yasuma ,  Nobuyuki Negoro ,  Masahiro Itou

IPC: A61K31/343 ,  C07D307/80

CPC classification number: C07D409/12 ,  C07D307/80

Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof. The compound or a salt thereof or a prodrug thereof has a GPR40 receptor function modulating action and is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.

Abstract translation: 本发明提供由式（I）表示的化合物：其中每个符号如说明书中所定义，或其盐。 化合物或其盐或其前药具有GPR40受体功能调节作用，并且可用作胰岛素促分泌素或用于预防或治疗糖尿病等的药剂。