公开(公告)号：US20210340139A1

公开(公告)日：2021-11-04

申请号：US17243358

申请日：2021-04-28

申请人： Plexxikon Inc.

发明人： Jack Lin ,  Jason Walters

IPC分类号： C07D471/04 ,  C07D213/76

摘要： Provided herein are intermediates and processes useful for facile synthesis of compounds of Formula 2: wherein R1 is C(O)R2; R2 is alkyl optionally substituted with 1-5 halogens; G is phenyl or a 5-6 membered heteroaryl optionally substituted with 1-2 R3; and each R3 is independently C1-C6 alkyl, CN, C1-C6 alkyl-CN, 3-6 membered cycloalkyl, or 4-6 membered heterocycloalkyl.

公开(公告)号：US10577366B2

公开(公告)日：2020-03-03

申请号：US15925270

申请日：2018-03-19

申请人： Plexxikon Inc.

发明人： Jack Lin ,  Marika Nespi ,  Jason Walters

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K45/06

摘要： Forms of 4-(1-(1,1-di(pyridin-2-yl)ethyl)-6-(3,5-dimethylisoxazol-4-yl)-1H-pyrrolo[3,2-b]pyridin-3-yl)benzoic acid were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the forms of Compound I.

公开(公告)号：US09994567B2

公开(公告)日：2018-06-12

申请号：US15705097

申请日：2017-09-14

申请人： Plexxikon Inc.

发明人： Prabha N. Ibrahim ,  Jack Lin ,  Wayne Spevak ,  Jiazhong Zhang

IPC分类号： C07D471/04 ,  C07D403/04

CPC分类号： C07D471/04 ,  C07D403/04

摘要： Provided herein are intermediates and processes useful for facile synthesis of compounds of formula (I): or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Q, P1 and P2 are as defined in this disclosure.

公开(公告)号：US09718847B2

公开(公告)日：2017-08-01

申请号：US14486986

申请日：2014-09-15

申请人： Plexxikon Inc.

发明人： Jiazhong Zhang ,  John Buell ,  Katrina Chan ,  Prabha N. Ibrahim ,  Jack Lin ,  Phuongly Pham ,  Songyuan Shi ,  Wayne Spevak ,  Guoxian Wu ,  Jeffrey Wu

IPC分类号： C07D471/04 ,  C07F9/6561 ,  A61K31/422 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/675 ,  A61K31/695 ,  C07D413/04 ,  C07D413/14 ,  C07F7/10

CPC分类号： C07F9/6561 ,  A61K31/422 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/675 ,  A61K31/695 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07F7/10 ,  Y02A50/411

摘要： Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.

公开(公告)号：US20170157120A1

公开(公告)日：2017-06-08

申请号：US15435569

申请日：2017-02-17

申请人： Plexxikon Inc.

发明人： Prabha N. Ibrahim ,  Chao Zhang ,  Wayne Spevak ,  Jiazhong Zhang ,  Guoxian Wu ,  Jack Lin ,  Hanna Cho ,  Marika Nespi ,  Songyuan Shi ,  Todd Ewing ,  Ying Zhang

IPC分类号： A61K31/506

CPC分类号： A61K31/506 ,  A61K31/437 ,  A61K31/5377 ,  C07D471/04

摘要： Compounds active on protein kinases are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.

公开(公告)号：US20160339025A1

公开(公告)日：2016-11-24

申请号：US15160729

申请日：2016-05-20

申请人： Plexxikon Inc.

发明人： Prabha N. Ibrahim ,  Chao Zhang ,  Wayne Spevak ,  Jiazhong Zhang ,  Guoxian Wu ,  Jack Lin ,  Hanna Cho ,  Marika Nespi ,  Songyuan Shi ,  Todd Ewing ,  Ying Zhang ,  Gideon Bollag

IPC分类号： A61K31/506 ,  A61K45/06

CPC分类号： A61K31/506 ,  A61K31/519 ,  A61K45/06

摘要： The present disclosure provides methods of treating a subject suffering from or at risk of a BRAF V600 mutation or BRAF fusion mutation related disease or condition, without activating the MAPK pathway or inducing expression of MAPK pathway genes in cells harboring wild-type BRAF.

摘要翻译： 本公开提供了治疗患有或处于BRAF V600突变或BRAF融合突变相关疾病或病症风险的受试者的方法，而不激活MAPK途径或诱导携带野生型BRAF的细胞中MAPK途径基因的表达。

公开(公告)号：US20240217965A1

公开(公告)日：2024-07-04

申请号：US18221546

申请日：2023-07-13

申请人： PLEXXIKON INC.

发明人： Jack Lin ,  Jason Walters

IPC分类号： C07D471/04 ,  C07D213/76

CPC分类号： C07D471/04 ,  C07D213/76

摘要： Provided herein are intermediates and processes useful for facile synthesis of compounds of Formula 2:




wherein R1 is C(O)R2; R2 is alkyl optionally substituted with 1-5 halogens; G is phenyl or a 5-6 membered heteroaryl optionally substituted with 1-2 R3; and each R3 is independently C1-C6 alkyl, CN, C1-C6 alkyl-CN, 3-6 membered cycloalkyl, or 4-6 membered heterocycloalkyl.

公开(公告)号：US10301280B2

公开(公告)日：2019-05-28

申请号：US15620396

申请日：2017-06-12

申请人： Plexxikon Inc.

发明人： Guoxian Wu ,  Katrina Chan ,  Todd Ewing ,  Prabha N. Ibrahim ,  Jack Lin ,  Marika Nespi ,  Wayne Spevak ,  Ying Zhang

IPC分类号： C07D403/12 ,  C07D401/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04 ,  A61K31/519 ,  A61K31/506 ,  A61K31/437 ,  A61K31/675 ,  C07F5/02 ,  A61K31/5377 ,  C07F9/6561

摘要： Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and/or mutant c-kit protein kinases.

公开(公告)号：US10227357B2

公开(公告)日：2019-03-12

申请号：US14019442

申请日：2013-09-05

申请人： Plexxikon Inc.

发明人： Jack Lin ,  John Buell ,  Katrina Chan ,  Todd Ewing ,  Prabha Ibrahim ,  Marika Nespi ,  Phuongly Pham ,  Songyuan Shi ,  Wayne Spevak ,  Guoxian Wu ,  Jiazhong Zhang ,  Ying Zhang

IPC分类号： C07D495/04 ,  A61K31/519 ,  C07D401/12 ,  A61K31/52 ,  C07D239/74 ,  A61K31/5377 ,  C07D491/056 ,  C07D473/00 ,  C07D487/04 ,  A61K31/517 ,  C07D519/00

摘要： Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and mutant c-kit protein kinases.

公开(公告)号：US20180002332A1

公开(公告)日：2018-01-04

申请号：US15705097

申请日：2017-09-14

申请人： Plexxikon Inc.

发明人： Prabha N. Ibrahim ,  Jack Lin ,  Wayne Spevak ,  Jiazhong Zhang

IPC分类号： C07D471/04 ,  C07D403/04

CPC分类号： C07D471/04 ,  C07D403/04

摘要： Provided herein are intermediates and processes useful for facile synthesis of compounds of formula (I): or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Q, P1 and P2 are as defined in this disclosure.