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1. CN111635406 - Improved forms of PI3K[delta] selective inhibitor for use in pharmaceutical formulations

Office
China
Application Number 202010471226.5
Application Date 26.05.2015
Publication Number 111635406
Publication Date 08.09.2020
Publication Kind A
IPC
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07C 309/30
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
309Sulfonic acids; Halides, esters, or anhydrides thereof
01Sulfonic acids
28having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
29of non-condensed six-membered aromatic rings
30of six-membered aromatic rings substituted by alkyl groups
C07C 303/32
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
303Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
32of salts of sulfonic acids
A61K 31/519
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 35/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
02specific for leukemia
CPC
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07B 2200/13
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
13Crystalline forms, e.g. polymorphs
A61P 29/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61K 31/519
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Applicants RHIZEN PHARMACEUTICALS SA
理森制药股份公司
Inventors VAKKALANKA SWAROOP KUMAR VENKATA SATYA
斯瓦鲁普·库马尔·文卡塔·萨蒂亚·瓦卡拉恩卡
Agents 北京集佳知识产权代理有限公司 11227
北京集佳知识产权代理有限公司 11227
Priority Data 2596/CHE/2014 27.05.2014 IN
2597/CHE/2014 27.05.2014 IN
Title
(EN) Improved forms of PI3K[delta] selective inhibitor for use in pharmaceutical formulations
(ZH) 用于药物制剂中的PI3Kδ选择性抑制剂的改良形式
Abstract
(EN) The present invention relates to solid state forms of a p-toluene sulfonic acid salt (PTSA) of a selective PI3K[delta] inhibitor (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-3-(3-fluorophenyl)-4H-chromen-4-one (TGR-1202). The present invention also relates to methods of preparing the salt, pharmaceutical compositions containing the salt, and methods oftreating a PI3K kinase mediated diseases or disorders, such as cancer, by administering the salt.
(ZH) 本发明涉及选择性PI3Kδ抑制剂(S)‑2‑(1‑(4‑氨基‑3‑(3‑氟‑4‑异丙氧基苯基)‑1H‑吡唑并[3,4‑d]嘧啶‑1‑基)乙基)‑3‑(3‑氟苯基)‑4H‑色烯‑4‑酮(TGR‑1202)的对甲苯磺酸盐(PTSA)的固态形式。本发明还涉及制备所述盐的方法,含有所述盐的药物组合物,及通过施用所述盐治疗PI3K激酶介导的疾病或病症,如癌症的方法。