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：US20230019032A1

公开(公告)日：2023-01-19

申请号：US17224733

申请日：2021-04-07

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 ,  C07D403/14 ,  C07D409/14 ,  C07D471/04 ,  C07D413/14 ,  C07D471/08 ,  C07D401/14 ,  C07D417/14 ,  A61P35/00 ,  A61K31/444 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  C07D403/04 ,  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：US09546181B2

公开(公告)日：2017-01-17

申请号：US14951104

申请日：2015-11-24

申请人： JNC CORPORATION ,  JNC PETROCHEMICAL CORPORATION

发明人： Sayaka Fujimori ,  Hiroyuki Tanaka

IPC分类号： C07D309/06 ,  C07D319/06 ,  C07D237/06 ,  C07D213/30 ,  C09K19/20 ,  C09K19/30 ,  C09K19/34 ,  C09K19/54 ,  C07D497/08 ,  C07D239/26 ,  C09K19/32 ,  C09K19/04 ,  C09K19/12

CPC分类号： C07D497/08 ,  C07D213/30 ,  C07D239/26 ,  C07D309/06 ,  C07D319/06 ,  C09K19/20 ,  C09K19/3059 ,  C09K19/3066 ,  C09K19/3068 ,  C09K19/32 ,  C09K19/322 ,  C09K19/3402 ,  C09K19/3458 ,  C09K2019/044 ,  C09K2019/0466 ,  C09K2019/122 ,  C09K2019/123 ,  C09K2019/3004 ,  C09K2019/3009 ,  C09K2019/301 ,  C09K2019/3071 ,  C09K2019/3077 ,  C09K2019/3078 ,  C09K2019/308 ,  C09K2019/3083 ,  C09K2019/3422 ,  C09K2019/3425

摘要： The subject is to provide a liquid crystal compound satisfying at least one of physical properties such as a high stability to heat or light, a high clearing point (or a high maximum temperature), a low minimum temperature of a liquid crystal phase, a small viscosity, a suitable optical anisotropy, a large dielectic anisotropy, a suitable elastic constant and an excellent compatibility with any other liquid crystal compound, a liquid crystal composition including this compound and a liquid crystal display device including this composition. The compound is represented by the following formula (1a): wherein R1 is alkyl having 1 to 15 carbons or the like; ring A1, ring A2, ring A3 and ring A4 are independently 1,4-phenylene, naphthalene-2,6-diyl or the like; Z1 and Z2 are independently a single bond or the like; o and p are independently 0, 1 or 2; and n is an integer from 2 to 10.

摘要翻译： 题目主题是提供一种液晶化合物，其满足物理性能如热或光的高稳定性，高清亮点（或高最高温度），液晶相的最低最低温度， 适合的光学各向异性，大的介电各向异性，合适的弹性常数和与任何其它液晶化合物的优异的相容性，包含该化合物的液晶组合物和包含该组合物的液晶显示装置。 解决方法该方法涉及由式（1a）表示的化合物。 式（1a）中，R 1为碳原子数1〜15的烷基等; 环A1，环A2，环A3和环A4独立地为1,4-亚苯基，萘-2,6-二基等; Z1和Z2独立地为单键等; o和p独立地为0,1或2; n为2〜10的整数。

公开(公告)号：US5817692A

公开(公告)日：1998-10-06

申请号：US701423

申请日：1996-08-22

申请人： Gary H. Posner

发明人： Gary H. Posner

IPC分类号： A61K31/357 ,  C07D493/08 ,  C07D493/10 ,  C07D497/08 ,  A61K31/335 ,  C07D321/10 ,  C07D323/04

CPC分类号： A61K31/357 ,  C07D493/08 ,  C07D493/10 ,  C07D497/08

摘要： The present invention relates to novel biologically-active organic peroxides and to novel uses of both known and new organic peroxides. More specifically, this invention details organic endoperoxides having antiparasitic activity, methods for their preparation and methods for treating malaria and cerebral toxoplasmic encephalitis with the organic endoperoxides.

摘要翻译： 本发明涉及新颖的生物活性有机过氧化物和新型有机过氧化物的新用途。 更具体地，本发明详述了具有抗寄生虫活性的有机内过氧化物，其制备方法和用有机内过氧化物治疗疟疾和脑弓形虫脑炎的方法。

公开(公告)号：US5767122A

公开(公告)日：1998-06-16

申请号：US469465

申请日：1995-06-06

申请人： Chung K. Chu ,  Raymond F. Schinazi

发明人： Chung K. Chu ,  Raymond F. Schinazi

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治疗量的下式的对映体纯的β-D-二氧戊环嘌呤核苷：其中R是OH，Cl，NH 2或H ，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。