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：US20220054507A1

公开(公告)日：2022-02-24

申请号：US17407811

申请日：2021-08-20

申请人： Plexxikon Inc.

发明人： Ben Powell ,  Athanasios Tsiatis ,  Jackie Walling

IPC分类号： A61K31/58 ,  A61K31/444 ,  A61K31/573 ,  A61K31/502 ,  A61K31/4166 ,  A61P35/00

摘要： Disclosed is a method of treating a subject suffering from a cancer, comprising administering to the subject a combination of agents comprising: (a) Compound I: or a pharmaceutically acceptable salt thereof; and (b) one or more inhibitors of the androgen receptor signaling pathway; or (c) one or more PARP inhibitors; wherein the amount of the combination of agents is therapeutically effective in the treatment.

公开(公告)号：US10584122B2

公开(公告)日：2020-03-10

申请号：US16219730

申请日：2018-12-13

申请人： Plexxikon Inc.

发明人： Prabha N. Ibrahim ,  Gary Conard Visor

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/337 ,  A61K31/352 ,  A61K31/4188 ,  A61K31/436 ,  A61K31/444 ,  A61K45/06

摘要： Solid forms of the compound, [5-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-pyridin-2-yl]-(6-trifluoromethyl-pyridin-3-ylmethyl)-amine HCl salt (Compound I) and its free base, active on the receptor protein kinases c-Kit and/or c-Fms and/or Flt3, were prepared and characterized: Also provided are methods of using the solid forms.

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：US10189833B2

公开(公告)日：2019-01-29

申请号：US15725197

申请日：2017-10-04

申请人： Plexxikon Inc.

发明人： Prabha N. Ibrahim ,  Gary Conard Visor

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/337 ,  A61K31/352 ,  A61K31/4188 ,  A61K31/436 ,  A61K31/444 ,  A61K45/06

摘要： Solid forms of the compound, [5-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-pyridin-2-yl]-(6-trifluoromethyl-pyridin-3-ylmethyl)-amine HCl salt (Compound I) and its free base, active on the receptor protein kinases c-Kit and/or c-Fms and/or Flt3, were prepared and characterized: Also provided are methods of using the solid forms.

公开(公告)号：US10040792B2

公开(公告)日：2018-08-07

申请号：US15665804

申请日：2017-08-01

申请人： Plexxikon Inc. ,  Daiichi Sankyo Company, Limited

发明人： Prabha N. Ibrahim ,  Masayoshi Jin ,  Shinji Matsuura

IPC分类号： C07D471/04

摘要： The present disclosure provides processes for the preparation of a compound of formula I: or a salt thereof, active on the receptor protein kinases c-Kit and/or c-Fms and/or Flt3. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.

公开(公告)号：US20170349572A1

公开(公告)日：2017-12-07

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

CPC分类号： C07D401/12 ,  A61K31/437 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/675 ,  C07D403/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04 ,  C07F5/025 ,  C07F9/65616

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：US09776998B2

公开(公告)日：2017-10-03

申请号：US15161103

申请日：2016-05-20

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：US09447089B2

公开(公告)日：2016-09-20

申请号：US12752035

申请日：2010-03-31

申请人： Dipen Desai ,  Ralph Diodone ,  Zenaida Go ,  Prabha N. Ibrahim ,  Raman Iyer ,  Hans-Juergen Mair ,  Harpreet K. Sandhu ,  Navnit H. Shah ,  Gary Visor ,  Nicole Wyttenbach ,  Stephan Lauper ,  Johannes Pudewell ,  Frank Wierschem

发明人： Dipen Desai ,  Ralph Diodone ,  Zenaida Go ,  Prabha N. Ibrahim ,  Raman Iyer ,  Hans-Juergen Mair ,  Harpreet K. Sandhu ,  Navnit H. Shah ,  Gary Visor ,  Nicole Wyttenbach ,  Stephan Lauper ,  Johannes Pudewell ,  Frank Wierschem

IPC分类号： A61K9/14 ,  C07D471/04 ,  A61K31/437 ,  A61K9/10 ,  A61K9/16 ,  A61K9/00

CPC分类号： C07D471/04 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/10 ,  A61K9/1635 ,  A61K9/1652 ,  A61K31/437 ,  C07B2200/13

摘要： Provided are solid dispersions, solid molecular complexes, salts and crystalline polymorphs involving propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide.

摘要翻译： 提供的是固体分散体，固体分子复合物，盐和结晶多晶型物，其涉及丙烷-1-磺酸{3- [5-（4-氯 - 苯基）-1H-吡咯并[2,3-b]吡啶-3-羰基] -2,4-二氟 - 苯基} - 酰胺。