AU2016289454B2 - Diaryl macrocycle polymorph - Google Patents

Diaryl macrocycle polymorph Download PDF

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Publication number
AU2016289454B2
AU2016289454B2 AU2016289454A AU2016289454A AU2016289454B2 AU 2016289454 B2 AU2016289454 B2 AU 2016289454B2 AU 2016289454 A AU2016289454 A AU 2016289454A AU 2016289454 A AU2016289454 A AU 2016289454A AU 2016289454 B2 AU2016289454 B2 AU 2016289454B2
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Australia
Prior art keywords
compound
formula
alkyl
boc
trifluoroacetyl
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AU2016289454A1 (en
Inventor
Jingrong J. Cui
Evan W. ROGERS
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Turning Point Therapeutics Inc
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Turning Point Therapeutics Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C269/06—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/16—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Indole Compounds (AREA)
AU2016289454A 2015-07-06 2016-07-05 Diaryl macrocycle polymorph Active AU2016289454B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562188846P 2015-07-06 2015-07-06
US62/188,846 2015-07-06
US201562218672P 2015-09-15 2015-09-15
US62/218,672 2015-09-15
PCT/US2016/040972 WO2017007759A1 (en) 2015-07-06 2016-07-05 Diaryl macrocycle polymorph

Publications (2)

Publication Number Publication Date
AU2016289454A1 AU2016289454A1 (en) 2018-01-04
AU2016289454B2 true AU2016289454B2 (en) 2020-07-09

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AU2016289454A Active AU2016289454B2 (en) 2015-07-06 2016-07-05 Diaryl macrocycle polymorph

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US (5) US10294242B2 (enExample)
EP (2) EP4397665A3 (enExample)
JP (2) JP6917974B2 (enExample)
KR (1) KR102623734B1 (enExample)
CN (2) CN113354653B (enExample)
AU (1) AU2016289454B2 (enExample)
BR (1) BR112018000297A2 (enExample)
CA (1) CA2990020C (enExample)
DK (1) DK3319969T3 (enExample)
ES (1) ES2979111T3 (enExample)
FI (1) FI3319969T3 (enExample)
HR (1) HRP20240780T1 (enExample)
HU (1) HUE067352T2 (enExample)
IL (2) IL256443B (enExample)
LT (1) LT3319969T (enExample)
MX (2) MX386680B (enExample)
PL (1) PL3319969T3 (enExample)
PT (1) PT3319969T (enExample)
RS (1) RS65593B1 (enExample)
RU (1) RU2765181C2 (enExample)
SI (1) SI3319969T1 (enExample)
SM (1) SMT202400213T1 (enExample)
WO (1) WO2017007759A1 (enExample)
ZA (1) ZA201708436B (enExample)

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HRP20191283T1 (hr) 2014-01-24 2019-10-18 Turning Point Therapeutics, Inc. Diaril makrocikli kao modulatori protein kinaze
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EP4397665A3 (en) * 2015-07-06 2024-08-21 Turning Point Therapeutics, Inc. Diaryl macrocycle polymorph
DK3325488T3 (da) * 2015-07-21 2020-09-14 Turning Point Therapeutics Inc Chiral diaryl-makrocyklus og anvendelse deraf til behandling af cancer
TW201815799A (zh) 2016-07-28 2018-05-01 美商Ｔｐ生物醫藥公司 巨環激酶抑制劑
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CN107586796B (zh) * 2017-07-20 2021-08-06 暨明医药科技（苏州）有限公司 (r)-2-(1-氨基乙基)-4-氟苯酚的合成方法
BR112020001695A2 (pt) 2017-07-28 2020-07-21 Turning Point Therapeutics, Inc. compostos macrocíclicos e usos dos mesmos
CN111511746B (zh) 2017-12-19 2024-01-09 特普医药公司 用于治疗疾病的巨环化合物
CN113956269A (zh) * 2018-04-16 2022-01-21 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白激酶活性的二(杂)芳基大环化合物
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WO2020233645A1 (zh) 2019-05-21 2020-11-26 浙江海正药业股份有限公司 大环类衍生物、及其制备方法和用途
KR20220046549A (ko) * 2019-06-19 2022-04-14 터닝 포인트 테라퓨틱스, 인크. 거대고리 카이네이스 억제제의 다형체
AU2020391220A1 (en) 2019-11-27 2022-06-30 Turning Point Therapeutics, Inc. Combination therapy involving diaryl macrocyclic compounds
US11654145B2 (en) * 2019-11-27 2023-05-23 Turning Point Therapeutics, Inc. Combination therapy involving diaryl macrocyclic compounds
EP4114530A4 (en) * 2020-03-02 2024-04-17 Turning Point Therapeutics, Inc. THERAPEUTIC USES OF MACROCYCLIC COMPOUNDS
WO2021223748A1 (zh) * 2020-05-08 2021-11-11 山东轩竹医药科技有限公司 大环类酪氨酸激酶抑制剂的晶型及其制备方法
CN112174982A (zh) * 2020-09-10 2021-01-05 上海希迈医药科技有限公司 一种洛普替尼晶型及其制备方法
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MX386680B (es) 2025-03-19
RU2018104269A3 (enExample) 2019-12-17
US12187739B2 (en) 2025-01-07
IL283184A (en) 2021-06-30
EP4397665A3 (en) 2024-08-21
CN108026108A (zh) 2018-05-11
IL256443B (en) 2021-05-31
KR102623734B1 (ko) 2024-01-10
EP3319969A1 (en) 2018-05-16
RU2018104269A (ru) 2019-08-06
IL256443A (en) 2018-02-28
CA2990020A1 (en) 2017-01-12
AU2016289454A1 (en) 2018-01-04
CA2990020C (en) 2024-02-27
NZ738180A (en) 2024-04-26
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