公开(公告)号：US09896467B1

公开(公告)日：2018-02-20

申请号：US15467940

申请日：2017-03-23

申请人： National Tsing Hua University

发明人： Yun Chi ,  Yang Wang ,  Han-Yan Tsai

IPC分类号： C07D487/04 ,  C07D491/20 ,  C07D495/20 ,  C07D487/20 ,  C07F9/6561

CPC分类号： C07F9/6561 ,  C07D487/04 ,  C07D487/20 ,  C07D491/20 ,  C07D495/20

摘要： An organic compound with a tetrahedral-like geometry is disclosed. The organic compound has a structure represented by formula (I): wherein A1 to A4 each independently represent a 5-membered or 6-membered unsaturated ring; B1 represents direct bonding, —C—, —O—, —N—, —S— or —C═C—; m is 0 or 1; each of Ra's is independently hydrogen, fluorine, oxygen, substituted or unsubstituted C1-C12 alkyl or substituted or unsubstituted C6-C12 aryl; and n is an integer of 0 to 2.

公开(公告)号：US09717735B2

公开(公告)日：2017-08-01

申请号：US14690180

申请日：2015-04-17

申请人： G1 Therapeutics, Inc.

发明人： Jay Copeland Strum ,  John Emerson Bisi ,  Patrick Joseph Roberts ,  Ricky D. Gaston ,  Robert C. Gadwood

IPC分类号： C07D487/20 ,  C07D487/14 ,  C07D471/20 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/527 ,  A61K31/519

CPC分类号： A61K31/5377 ,  A61K31/519 ,  A61K31/527 ,  A61K45/06 ,  C07D471/20 ,  C07D487/14 ,  C07D487/20

摘要： This invention is in the area of tricyclic lactam compounds for and methods of treating selected Rb-positive cancers and other Rb-positive abnormal cellular proliferative disorders while minimizing the deleterious effects on healthy cells, for example healthy Hematopoietic Stem Cells and Progenitor Cells (HSPCs), associated with current treatment modalities. In one aspect, treatment of select Rb-positive cancers is disclosed using specific compounds disclosed herein. In certain embodiments, the compounds described herein act as selective cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects.

公开(公告)号：US20170130124A1

公开(公告)日：2017-05-11

申请号：US15129812

申请日：2015-03-26

申请人： Kanto Kagaku Kabushiki Kaisha

发明人： Jiro ABE ,  Hiroaki TAMASHITA ,  Kazuhiko TSUTIYA ,  Takayoshi SUGA

IPC分类号： C09K9/02 ,  C08K5/3447 ,  G02B5/22 ,  C07D233/58 ,  C07D233/64 ,  G02B5/23 ,  C08K5/3445 ,  C07D487/20

CPC分类号： C09K9/02 ,  C07D233/58 ,  C07D233/64 ,  C07D487/10 ,  C07D487/20 ,  C08K5/3445 ,  C08K5/3447 ,  C08L101/00 ,  C09D11/50 ,  C09K2211/1007 ,  C09K2211/1029 ,  C09K2211/1044 ,  G02B5/223 ,  G02B5/23

摘要： In order to address the problems of conventional photochromic compounds, which are the insufficient coloring/discoloring speed and durability exhibited thereby and the large number of production steps, the present invention provides a photochromic compound that exhibits a high speed coloring/discoloring reaction and high durability while it is able to be synthesized in low cost, and that has industrial applicability. The compound of the present invention is characterized by the insertion of a diarylimidazolyl radical into the ortho position of an aryl group. The compound exhibits photochromic properties, and achieves a photochromic compound having both a high speed color switching reaction and high durability. Furthermore low cost synthesis is possible, and the photochromic compound has industrial applicability.

公开(公告)号：US20170129903A1

公开(公告)日：2017-05-11

申请号：US15318224

申请日：2015-06-11

申请人： ADAMED SP. Z O.O.

发明人： Marcin FEDER ,  Iwona KALINOWSKA ,  Joanna Adriana JASZCZEWSKA ,  Ewa BURCHARD ,  Wojciech LEWANDOWSKI ,  Urszula BULKOWSKA ,  Maria MAZUR ,  Katarzyna WOS-LATOSI

IPC分类号： C07D487/20 ,  C07D487/10

CPC分类号： C07D487/20 ,  C07D487/10

摘要： A spirooxoindole compound represented by the formula selected from the group consisting of formula (IA) and (IB), wherein all symbols are as defined in the description. The compound can find use in a method of prevention and/or treatment of diseases selected from the group consisting of cancer, immune diseases, inflammatory conditions, allergic skin diseases associated with excessive proliferation, and viral infections.

公开(公告)号：US09556188B2

公开(公告)日：2017-01-31

申请号：US14951494

申请日：2015-11-25

申请人： BeiGene, Ltd.

发明人： Zhiwei Wang ,  Yunhang Guo

IPC分类号： A61K31/4162 ,  C07D487/04 ,  C07D487/20 ,  A61K31/5517 ,  C07D487/14 ,  C07D471/14 ,  C07D471/20 ,  C07D519/00 ,  A61K31/4188 ,  A61K31/435 ,  A61K31/437 ,  A61K31/519 ,  A61K31/527 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06

CPC分类号： C07D487/04 ,  A61K31/4188 ,  A61K31/435 ,  A61K31/437 ,  A61K31/438 ,  A61K31/519 ,  A61K31/527 ,  A61K31/55 ,  A61K31/551 ,  A61K31/5517 ,  A61K45/06 ,  C07D471/14 ,  C07D471/20 ,  C07D487/14 ,  C07D487/20 ,  C07D519/00

摘要： The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.

摘要翻译： 本发明是式（I）的稠合杂环化合物及其盐，其组合物及其用途。 特别地，本文所公开的是可用于抑制蛋白激酶（包括Bruton's酪氨酸激酶（Btk））以及由此介导的病症的某些稠合杂环化合物。

公开(公告)号：US20160311824A1

公开(公告)日：2016-10-27

申请号：US15034217

申请日：2014-11-14

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Upender Velaparthi ,  Chetan Padmakar Dame ,  Peiying Liu ,  Mark D Wittman ,  Bradley C. Pearce ,  Erika M.V. Araujo ,  Bireshwar Dasgupta ,  Jalathi Surendran Nair ,  Sakthi Kumaran Janakiraman ,  Chandrasekhar Reddy Rachamreddy ,  Mallikarjuna Rao Mettu ,  Arul Mozhi Selvan Subbiah Karuppiah ,  Bandreddy Subba Reddy ,  Pulicharla Nagalakshmi ,  Rajesh Onkardas Bora ,  Shilpa Holehatti Maheshwarappa ,  Selvakumar Kumaravel ,  Dibakar Mullick ,  Ramesh Sistla

IPC分类号： C07D487/04 ,  C07D487/20 ,  C07D491/147 ,  C07D491/20 ,  C07D519/00 ,  C07D487/10

CPC分类号： C07D487/04 ,  C07D487/10 ,  C07D487/20 ,  C07D491/147 ,  C07D491/20 ,  C07D519/00

摘要： The invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.

摘要翻译： 及其药学上可接受的盐。 式（I）的化合物抑制蛋白激酶活性，从而使它们用作抗癌剂。

公开(公告)号：US09434737B2

公开(公告)日：2016-09-06

申请号：US14104597

申请日：2013-12-12

申请人： Dainippon Sumitomo Pharma Co., Ltd. ,  Kyowa Hakko Bio Co., Ltd.

发明人： Masaji Kasai ,  Shinji Kita ,  Tadashi Ogawa ,  Hideaki Tokai

IPC分类号： C07D487/20 ,  C07C271/22 ,  C07D207/416 ,  C12P7/62 ,  C12P17/10 ,  C12P41/00 ,  C12P17/18

CPC分类号： C07D487/20 ,  C07B2200/07 ,  C07C271/22 ,  C07D207/416 ,  C12P7/62 ,  C12P17/10 ,  C12P17/182 ,  C12P41/005

摘要： Provided is a process for producing (3R)-2′-(4-bromo-2-fluorobenzyl)spiro{pyrrolidine-3,4′(1′H)-pyrrolo[1,2-a]pyrazine}-1′,2,3′,5(2′H)-tetraone (compound A). The method includes converting an optically active succinimide derivative of formula (I) to compound A, in which the compound of formula (I) has been prepared by reacting a base with an optically active amide derivative of formula (VI).

摘要翻译： 提供（3R）-2' - （4-溴-2-氟苄基）螺（吡咯烷-3,4'（1'H） - 吡咯并[1,2-a]吡嗪} -1'的方法， 2,3'，5（2'H） - 四酮（化合物A）。 该方法包括将式（I）的光学活性琥珀酰亚胺衍生物转化为化合物A，其中式（I）化合物是通过使碱与式（Ⅵ）的光学活性酰胺衍生物反应来制备的。

公开(公告)号：US20160122358A1

公开(公告)日：2016-05-05

申请号：US14994346

申请日：2016-01-13

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Upender Velaparthi ,  Chetan Padmakar Darne ,  Peiying Liu ,  Mark D. Wittman ,  Bradley C. Pearce ,  Erika M. V. Araujo ,  Bireshwar Dasgupta ,  Jalathi Surendran Nair ,  Sakthi Kumaran Janakiraman ,  Chandrasekhar Reddy Rachamreddy ,  Mallikarjuna Rao Mettu ,  Arul Mozhi Subbiah Karuppiah ,  Subba Reddy Bandreddy ,  Nagalakshmi Pulicharla ,  Rajesh Onkardas Bora ,  Shilpa Maheshwarappa Holehatti ,  Selvakumar Kumaravel ,  Dibakar Mullick ,  Ramesh Kumar Sistla

IPC分类号： C07D487/04 ,  C07D487/20 ,  C07D491/20 ,  C07D487/10 ,  C07D491/147

CPC分类号： C07D487/04 ,  C07D487/10 ,  C07D487/20 ,  C07D491/147 ,  C07D491/20 ,  C07D519/00

摘要： The invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.

公开(公告)号：US20160083400A1

公开(公告)日：2016-03-24

申请号：US14857682

申请日：2015-09-17

申请人： Sunovion Pharmaceuticals Inc. ,  Sumitomo Dainippon Pharma Co., Ltd.

发明人： Douglas F. Burdi ,  Daisuke Tanaka ,  Hiroaki Fujiwara

IPC分类号： C07D498/14 ,  C07D487/20 ,  C07D487/14

CPC分类号： C07D498/14 ,  C07D487/14 ,  C07D487/20

摘要： Disclosed are compounds useful as inhibitors of Phosphodiesterase 1 (PDE1), compositions thereof, and methods of using the same.

摘要翻译： 公开了可用作磷酸二酯酶1（PDE1）的抑制剂的化合物，其组合物及其使用方法。

公开(公告)号：US09273058B2

公开(公告)日：2016-03-01

申请号：US14541343

申请日：2014-11-14

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Upender Velaparthi ,  Chetan Padmakar Darne ,  Peiying Liu ,  Mark D. Wittman ,  Bradley C. Pearce ,  Erika M. V. Araujo ,  Bireshwar Dasgupta ,  Jalathi Surendran Nair ,  Sakthi Kumaran Janakiraman ,  Chandrasekhar Reddy Rachamreddy ,  Mettu Mallikarjuna Rao ,  Arul Mozhi Selvan Subbiah Karuppiah ,  Bandreddy Subba Reddy ,  Pulicharla Nagalakshmi ,  Rajesh Onkardas Bora ,  Shilpa Holehatti Maheshwarappa ,  Selvakumar Kumaravel ,  Dibakar Mullick ,  Ramesh Sistla

IPC分类号： C07D487/04 ,  C07D487/10 ,  C07D487/20 ,  C07D491/147 ,  C07D491/20 ,  A61K31/4985 ,  A61K31/499 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61P19/02

CPC分类号： C07D487/04 ,  C07D487/10 ,  C07D487/20 ,  C07D491/147 ,  C07D491/20 ,  C07D519/00

摘要： The invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.

摘要翻译： 本发明提供式（I）化合物及其药学上可接受的盐。 式（I）的化合物抑制蛋白激酶活性，从而使它们用作抗癌剂。