公开(公告)号：US11001575B1

公开(公告)日：2021-05-11

申请号：US16541863

申请日：2019-08-15

申请人： OTSUKA PHARMACEUTICAL CO., LTD.

发明人： Valerio Berdini ,  Ildiko Maria Buck ,  James Edward Harvey Day ,  Charlotte Mary Griffiths-Jones ,  Thomas Daniel Heightman ,  Steven Howard ,  Christopher William Murray ,  David Norton ,  Marc O'Reilly ,  Alison Jo-Anne Woolford ,  Michael Liam Cooke ,  David Cousin ,  Stuart Thomas Onions ,  Jonathan Martin Shannon ,  John Paul Watts

IPC分类号： C07D405/14 ,  A61K31/55 ,  C07D487/04 ,  A61P35/00 ,  A61K31/553 ,  C07D403/14 ,  C07D471/08 ,  C07D403/04 ,  C07D413/14 ,  A61K31/506 ,  C07D498/22 ,  A61K31/5377 ,  C07D417/14 ,  C07D409/14 ,  C07D513/04 ,  A61K31/444 ,  C07D401/14 ,  C07D471/04 ,  C07D497/08 ,  A61K31/541

摘要： The invention provides a compound of formula (0): or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and C—F; Z is selected from C—Rz and N; R1 is selected from: -(Alk1)t-Cyc1; wherein t is 0 or 1; Optionally substituted C1-6 acyclic hydrocarbon groups R2 is selected from hydrogen; halogen; and C1-3 hydrocarbon groups optionally substituted with one or more fluorine atoms; R3 is hydrogen or a group L-R7; R4 is selected from hydrogen; methoxy; and optionally substituted C1-3 alkyl; and R4a is selected from hydrogen and a C1-3 alkyl group; wherein Rz, Alk1, Cyc1, L1 and R7 are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof. The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.

公开(公告)号：US10457669B2

公开(公告)日：2019-10-29

申请号：US15767775

申请日：2016-10-20

申请人： OTSUKA PHARMACEUTICAL CO., LTD.

发明人： Valerio Berdini ,  Ildiko Maria Buck ,  James Edward Harvey Day ,  Charlotte Mary Griffiths-Jones ,  Thomas Daniel Heightman ,  Steven Howard ,  Christopher William Murray ,  David Norton ,  Marc O'Reilly ,  Alison Jo-Anne Woolford ,  Michael Liam Cooke ,  David Cousin ,  Stuart Thomas Onions ,  Jonathan Martin Shannon ,  John Paul Watts

IPC分类号： C07D405/14 ,  C07D401/14 ,  C07D413/14 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D403/04 ,  C07D487/04 ,  C07D497/08 ,  C07D498/22 ,  C07D513/04 ,  A61P35/00 ,  A61K31/444 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553

摘要： The invention provides a compound of formula (0): or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and C—F; Z is selected from C—Rz and N; R1 is selected from: -(Alk1)t-Cyc1; wherein t is 0 or 1; Optionally substituted C1-6 acyclic hydrocarbon groups R2 is selected from hydrogen; halogen; and C1-3 hydrocarbon groups optionally substituted with one or more fluorine atoms; R3 is hydrogen or a group L1-R7; R4 is selected from hydrogen; methoxy; and optionally substituted C1-3 alkyl; and R4a is selected from hydrogen and a C1-3 alkyl group; wherein Rz, Alk1, Cyc1, L1 and R7 are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof. The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.

公开(公告)号：US20190047990A1

公开(公告)日：2019-02-14

申请号：US15767775

申请日：2016-10-20

申请人： OTSUKA PHARMACEUTICAL CO., LTD.

发明人： Valerio BERDINI ,  Ildiko Maria BUCK ,  James Edward Harvey DAY ,  Charlotte Mary GRIFFITHS-JONES ,  Thomas Daniel HEIGHTMAN ,  Steven HOWARD ,  Christopher William MURRAY ,  David NORTON ,  Marc O'REILLY ,  Alison Jo-Anne WOOLFORD ,  Michael Liam COOKE ,  David COUSIN ,  Stuart Thomas ONIONS ,  Jonathan Martin SHANNON ,  John Paul WATTS

IPC分类号： C07D405/14 ,  A61P35/00 ,  A61K31/506 ,  C07D471/04 ,  C07D487/04 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/553 ,  C07D498/22 ,  C07D497/08 ,  C07D513/04 ,  C07D403/04 ,  C07D403/14 ,  A61K31/444 ,  C07D409/14 ,  A61K31/541

CPC分类号： C07D405/14 ,  A61K31/444 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  A61P35/00 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D497/08 ,  C07D498/22 ,  C07D513/04

摘要： The invention provides a compound of formula (0): or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and C—F; Z is selected from C—Rz and N; R1 is selected from: -(Alk1)t-Cyc1; wherein t is 0 or 1; Optionally substituted C1-6 acyclic hydrocarbon groups R2 is selected from hydrogen; halogen; and C1-3 hydrocarbon groups optionally substituted with one or more fluorine atoms; R3 is hydrogen or a group L1-R7; R4 is selected from hydrogen; methoxy; and optionally substituted C1-3 alkyl; and R4a is selected from hydrogen and a C1-3 alkyl group; wherein Rz, Alk1, Cyc1, L1 and R7 are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof. The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.

公开(公告)号：US08362236B2

公开(公告)日：2013-01-29

申请号：US12529222

申请日：2008-02-29

申请人： Nobuo Shimma ,  Takuo Tsukuda ,  Hiroshi Koyano ,  Atsushi Suda ,  Tadakatsu Hayase ,  Kihito Hada ,  Ken-Ichi Kawasaki ,  Susumu Komiyama ,  Naomi Ono ,  Toshikazu Yamazaki ,  Ryoichi Saitoh ,  Masami Kohchi ,  Kiyoshi Hasegawa

发明人： Nobuo Shimma ,  Takuo Tsukuda ,  Hiroshi Koyano ,  Atsushi Suda ,  Tadakatsu Hayase ,  Kihito Hada ,  Ken-Ichi Kawasaki ,  Susumu Komiyama ,  Naomi Ono ,  Toshikazu Yamazaki ,  Ryoichi Saitoh ,  Masami Kohchi ,  Kiyoshi Hasegawa

IPC分类号： C07D497/08 ,  C07D513/08 ,  C07D513/20 ,  A61K31/529 ,  A61K31/53 ,  A61K31/5377 ,  A61P35/00

CPC分类号： C07D497/08 ,  C07D513/08 ,  C07D513/18 ,  C07D513/20

摘要： The present invention provides a novel class of compounds that have the activity of inhibiting HSP90 enzyme and are useful as anti-cancer agents or such, and compounds that are useful as synthetic intermediates thereof. Specifically, the present invention provides compounds represented by the following formula (1), and pharmaceutically acceptable salts thereof: wherein X, R1, R2, R3, R4, R5, R6, R7, L1, L2, and L3 are as defined in the specification.

摘要翻译： 本发明提供具有抑制HSP90酶的活性的新型化合物，可用作抗癌剂等，以及可用作其合成中间体的化合物。 具体而言，本发明提供下述式（1）表示的化合物及其药学上可接受的盐：其中X，R1，R2，R3，R4，R5，R6，R7，L1，L2和L3如 规范。

公开(公告)号：US5116862A

公开(公告)日：1992-05-26

申请号：US222405

申请日：1988-07-21

申请人： John B. Weston ,  John P. Larkin ,  Ian H. Smith

发明人： John B. Weston ,  John P. Larkin ,  Ian H. Smith

IPC分类号： A01N43/90 ,  A01N47/06 ,  A01N47/48 ,  A01N55/00 ,  A01N55/04 ,  C07D493/08 ,  C07D495/08 ,  C07D497/08 ,  C07F7/08

CPC分类号： C07D493/08 ,  A01N43/90 ,  A01N47/06 ,  A01N47/48 ,  A01N55/00 ,  A01N55/04 ,  C07D495/08 ,  C07D497/08 ,  C07F7/0812

摘要： The present invention provides a class of novel substituted bicyclooctanes which have pesticidal activity, particularly against arthropod pests. Pesticidal formulations containing the compounds of the formula (I), their use in the control of pests and methods for their preparation are also disclosed.

摘要翻译： 本发明提供一类具有杀虫活性的新型取代的双环辛烷，特别是针对节肢动物害虫。 还公开了含有式（I）化合物的杀虫剂，它们在防治害虫中的用途及其制备方法。

公开(公告)号：US4965257A

公开(公告)日：1990-10-23

申请号：US384067

申请日：1989-07-24

申请人： John E. Casida ,  Christopher J. Palmer ,  John P. Larkin ,  Ian H. Smith

发明人： John E. Casida ,  Christopher J. Palmer ,  John P. Larkin ,  Ian H. Smith

IPC分类号： A01N43/90 ,  A01N55/00 ,  C07D493/08 ,  C07D497/08 ,  C07F7/08

CPC分类号： C07D493/08 ,  A01N43/90 ,  A01N55/00 ,  C07D497/08 ,  C07F7/0812

摘要： Bicyclo-[2,2,1]-heptanes, bicyclo-[2,2,2]-octanes and bicyclo-[2,2,3]-nonanes, having 2 or 3 ring hetero atoms selected from O, S and N, substituted at the 1-position by a 4-alkynylphenyl group and at the 4-position and optionally at the 3 and/or 5-position are valuable pesticides, particularly insecticides and acaracides. The compounds may be prepared by reacting an alkyne with the corresponding 4-iodophenyl substituted compounds or by debromination of the corresponding 4-dibromomethylphenyl substituted compound.

摘要翻译： 具有2或3个选自O，S和N的环杂原子的双环 - [2,2,1]庚烷，双环 - [2,2,2] - 辛烷和双环 - [2,2,3] - 壬烷 在4-位被4-炔基苯基取代，在4位和任选在3位和/或5位被取代是有价值的农药，特别是杀虫剂和吖啶。 化合物可以通过使炔与相应的4-碘苯基取代的化合物反应或通过相应的4-二溴甲基苯基取代的化合物的脱溴来制备。

公开(公告)号：US09920032B2

公开(公告)日：2018-03-20

申请号：US15281679

申请日：2016-09-30

申请人： Incyte Corporation

发明人： Oleg Vechorkin ,  Yun-Long Li ,  Alexander Sokolsky ,  Anlai Wang ,  Wenyu Zhu ,  Jincong Zhuo

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D497/08 ,  C07D498/08 ,  C07D471/08

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D491/048 ,  C07D498/08

摘要： The present application is concerned with heterocyclic compounds that inhibit the activity of Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancers and other diseases.

公开(公告)号：US09403830B2

公开(公告)日：2016-08-02

申请号：US13942988

申请日：2013-07-16

申请人： Asitha Abeywardane ,  Steven Richard Brunette ,  Michael Jason Burke ,  Thomas Martin Kirrane, Jr. ,  Chuk Chui Man ,  Daniel Richard Marshall ,  Anil Kumar Padyana ,  Hossein Razavi ,  Robert Sibley ,  Lana Louise Smith Keenan ,  Roger John Snow ,  Ronald John Sorcek ,  Hidenori Takahashi ,  Steven John Taylor ,  Michael Robert Turner ,  Erick Richard Roush Young ,  Qiang Zhang ,  Yunlong Zhang ,  Renee M. Zindell

发明人： Asitha Abeywardane ,  Steven Richard Brunette ,  Michael Jason Burke ,  Thomas Martin Kirrane, Jr. ,  Chuk Chui Man ,  Daniel Richard Marshall ,  Anil Kumar Padyana ,  Hossein Razavi ,  Robert Sibley ,  Lana Louise Smith Keenan ,  Roger John Snow ,  Ronald John Sorcek ,  Hidenori Takahashi ,  Steven John Taylor ,  Michael Robert Turner ,  Erick Richard Roush Young ,  Qiang Zhang ,  Yunlong Zhang ,  Renee M. Zindell

IPC分类号： C07D487/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/04 ,  C07D401/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/20 ,  C07D491/20 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/549 ,  A61K31/55 ,  A61K31/551 ,  C07D405/12 ,  C07D497/08 ,  C07D498/04

CPC分类号： C07D487/04 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/549 ,  A61K31/55 ,  A61K31/551 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/20 ,  C07D491/20 ,  C07D497/08 ,  C07D498/04

摘要： The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein A1, A2, L1 and B are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.

摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，其中A1，A2，L1和B如本文所定义。 式（I）化合物可用作白三烯A4水解酶（LTA4H）的抑制剂和治疗LTA4H相关病症。 本发明还涉及包含式（I）化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，以及制备这些化合物的方法。

公开(公告)号：US5925643A

公开(公告)日：1999-07-20

申请号：US935515

申请日：1992-08-25

申请人： Chung K. Chu

发明人： Chung K. Chu

IPC分类号： C07D473/18 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/52 ,  A61K31/522 ,  A61K31/53 ,  A61K31/675 ,  A61K31/7076 ,  A61K38/21 ,  A61P31/12 ,  A61P31/18 ,  A61P37/04 ,  C07D327/04 ,  C07D405/04 ,  C07D411/04 ,  C07D473/00 ,  C07D473/16 ,  C07D473/30 ,  C07D473/34 ,  C07D473/40 ,  C07D497/08 ,  C07F9/6561

CPC分类号： C07D473/00 ,  A61K31/675 ,  A61K31/70 ,  A61K31/704 ,  A61K31/7076 ,  A61K38/21 ,  C07D327/04 ,  C07D411/04 ,  C07D497/08 ,  C07B2200/07

摘要： A method and composition for the treatment of humans infected with HIV that includes the administration of an HIV treatment amount of an enantiomerically pure .beta.-D-dioxolanyl purine nucleoside of the formula: ##STR1## wherein R is OH, Cl, NH.sub.2, or H, or a pharmaceutically acceptable salt or derivative of the compound, optionally in a pharmaceutically acceptable carrier or diluent.

摘要翻译： 用于治疗感染HIV的人的方法和组合物，其包括施用HIV治疗量的下式的其中R为OH，Cl，NH 2或H的对映异构体纯的β-D-二氧戊环嘌呤核苷，或 化合物的药学上可接受的盐或衍生物，任选地在药学上可接受的载体或稀释剂中。

公开(公告)号：US5834474A

公开(公告)日：1998-11-10

申请号：US839713

申请日：1997-04-15

申请人： Raymond F. Schinazi

发明人： Raymond F. Schinazi

IPC分类号： C07D473/18 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/52 ,  A61K31/522 ,  A61K31/53 ,  A61K31/675 ,  A61K31/70 ,  A61K31/7076 ,  A61K31/708 ,  A61K38/21 ,  A61P31/12 ,  A61P31/18 ,  A61P31/20 ,  A61P37/04 ,  C07D327/04 ,  C07D405/04 ,  C07D411/04 ,  C07D473/00 ,  C07D473/02 ,  C07D473/16 ,  C07D473/30 ,  C07D473/32 ,  C07D473/34 ,  C07D473/40 ,  C07D497/08

CPC分类号： A61K31/70 ,  A61K31/52 ,  A61K31/675 ,  A61K31/704 ,  A61K31/7076 ,  A61K31/708 ,  A61K38/21 ,  C07D327/04 ,  C07D411/04 ,  C07D473/00 ,  C07D497/08

摘要： A method and composition for the treatment of humans infected with HBV that includes the administration of an HBV treatment amount of a .beta.-dioxolanyl purine nucleoside of the formula: ##STR1## wherein R is OH, Cl, NH.sub.2, or H, or a pharmaceutically acceptable salt or derivative of the compound, optionally in a pharmaceutically acceptable carrier or diluent.

摘要翻译： 用于治疗感染HBV的人的方法和组合物，其包括给予HBV治疗量的下式的β-二氧杂环戊基嘌呤核苷：其中R是OH，Cl，NH 2或H，或药学上 化合物的可接受的盐或衍生物，任选地在药学上可接受的载体或稀释剂中。