US20180325901A1 - Chiral diaryl macrocycles and uses thereof - Google Patents

Chiral diaryl macrocycles and uses thereof Download PDF

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Publication number
US20180325901A1
US20180325901A1 US15/745,915 US201615745915A US2018325901A1 US 20180325901 A1 US20180325901 A1 US 20180325901A1 US 201615745915 A US201615745915 A US 201615745915A US 2018325901 A1 US2018325901 A1 US 2018325901A1
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Prior art keywords
alkyl
alk
fusion protein
cancer
ros1
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Abandoned
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US15/745,915
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Inventor
Jingrong J. CUI
Yishan LI
Evan W. ROGERS
Dayong Zhai
Wei Deng
Zhongdong HUANG
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Turning Point Therapeutics Inc
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Individual
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Priority to US15/745,915 priority Critical patent/US20180325901A1/en
Publication of US20180325901A1 publication Critical patent/US20180325901A1/en
Assigned to Turning Point Therapeutics, Inc. reassignment Turning Point Therapeutics, Inc. CHANGE OF NAME (SEE DOCUMENT FOR DETAILS). Assignors: TP THERAPEUTICS, INC.
Abandoned legal-status Critical Current

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    • 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
    • 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
    • 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
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C07D491/16—Peri-condensed systems
    • 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
    • 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
US15/745,915 2015-07-21 2016-07-20 Chiral diaryl macrocycles and uses thereof Abandoned US20180325901A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
US15/745,915 US20180325901A1 (en) 2015-07-21 2016-07-20 Chiral diaryl macrocycles and uses thereof

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201562195081P 2015-07-21 2015-07-21
US201662302231P 2016-03-02 2016-03-02
US15/745,915 US20180325901A1 (en) 2015-07-21 2016-07-20 Chiral diaryl macrocycles and uses thereof
PCT/US2016/043132 WO2017015367A1 (en) 2015-07-21 2016-07-20 Chiral diaryl macrocycles and uses thereof

Related Parent Applications (1)

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PCT/US2016/043132 A-371-Of-International WO2017015367A1 (en) 2015-07-21 2016-07-20 Chiral diaryl macrocycles and uses thereof

Related Child Applications (1)

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US16/998,763 Continuation US11452725B2 (en) 2015-07-21 2020-08-20 Chiral diaryl macrocycles and uses thereof

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US20180325901A1 true US20180325901A1 (en) 2018-11-15

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US15/745,915 Abandoned US20180325901A1 (en) 2015-07-21 2016-07-20 Chiral diaryl macrocycles and uses thereof
US16/998,763 Active 2036-07-24 US11452725B2 (en) 2015-07-21 2020-08-20 Chiral diaryl macrocycles and uses thereof
US17/819,858 Pending US20230346786A1 (en) 2015-07-21 2022-08-15 Chiral diaryl macrocycles and uses thereof

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US16/998,763 Active 2036-07-24 US11452725B2 (en) 2015-07-21 2020-08-20 Chiral diaryl macrocycles and uses thereof
US17/819,858 Pending US20230346786A1 (en) 2015-07-21 2022-08-15 Chiral diaryl macrocycles and uses thereof

Country Status (16)

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US (3) US20180325901A1 (de)
EP (2) EP3325488B1 (de)
JP (1) JP6817287B2 (de)
KR (1) KR20180033194A (de)
CN (1) CN108026109B (de)
AU (1) AU2016296878B2 (de)
BR (1) BR112018001065A2 (de)
CA (1) CA2992324A1 (de)
DK (1) DK3325488T3 (de)
ES (1) ES2818528T3 (de)
HK (1) HK1254606A1 (de)
IL (1) IL256868B (de)
MX (1) MX2018000718A (de)
RU (2) RU2728579C2 (de)
WO (1) WO2017015367A1 (de)
ZA (1) ZA201800416B (de)

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10618912B2 (en) 2014-01-24 2020-04-14 Turning Point Therapeutics, Inc. Diaryl macrocycles as modulators of protein kinases
US10689400B2 (en) 2016-07-28 2020-06-23 Turning Point Therapeutics, Inc. Macrocycle kinase inhibitors
US10745416B2 (en) 2017-12-19 2020-08-18 Turning Point Therapeutics, Inc. Macrocyclic compounds for treating disease
US11008337B2 (en) 2015-07-02 2021-05-18 Turning Point Therapeutics, Inc. Chiral diaryl macrocycles as modulators of protein kinases
WO2021108672A1 (en) * 2019-11-27 2021-06-03 Turning Point Therapeutics, Inc. Combination therapy involving diaryl macrocyclic compounds
US11155563B2 (en) 2017-07-28 2021-10-26 Turning Point Therapeutics, Inc. Macrocyclic compounds and uses thereof
US11291667B2 (en) 2017-01-25 2022-04-05 Turning Point Therapeutics, Inc. Combination therapy involving diaryl macrocyclic compounds
US11452725B2 (en) 2015-07-21 2022-09-27 Turning Point Therapeutics, Inc. Chiral diaryl macrocycles and uses thereof
US11731956B2 (en) 2018-10-22 2023-08-22 Alumis Inc. Substituted 1,2,4-triazoles as intermediates in the synthesis of TYK2 inhibitors
US11981684B2 (en) 2022-02-22 2024-05-14 Turning Point Therapeutics, Inc. Macrocyclic compounds and uses thereof

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CN113354653A (zh) * 2015-07-06 2021-09-07 特普医药公司 二芳基大环多晶型物及其制备方法
CN107267458B (zh) * 2017-07-06 2019-10-29 中南大学湘雅二医院 一种耐克唑替尼人的非小细胞肺癌细胞株h3122-cr23及其应用
CN109516999B (zh) * 2017-11-01 2021-08-17 郑州泰基鸿诺医药股份有限公司 用作蛋白质激酶调节剂的化合物及其应用
TW201927790A (zh) 2017-11-10 2019-07-16 美商安捷克斯製藥公司 作為trk激酶抑制劑之巨環化合物及其用途
JP2021519297A (ja) * 2018-03-28 2021-08-10 フォチョン・ファーマシューティカルズ・リミテッドＦｏｃｈｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｌｔｄ． Ｔｒｋキナーゼ阻害剤としての大環状化合物
JP7092405B2 (ja) * 2018-04-16 2022-06-28 深▲チェン▼市塔吉瑞生物医薬有限公司 キナーゼ活性を阻害するためのジ（ヘテロ）アリール大環状化合物
WO2019210835A1 (zh) * 2018-05-04 2019-11-07 正大天晴药业集团股份有限公司 作为蛋白激酶调节剂的二芳基大环化合物
CN111171049B (zh) * 2018-11-09 2021-06-04 山东轩竹医药科技有限公司 酪氨酸激酶抑制剂及其用途
JP2022537385A (ja) * 2019-06-19 2022-08-25 ターニング・ポイント・セラピューティクス・インコーポレイテッド 大環状キナーゼ阻害剤の多形
CN111689883B (zh) * 2020-05-22 2022-02-11 上海应用技术大学 一种二芳基砜类化合物的合成方法
EP4163283A1 (de) * 2020-06-04 2023-04-12 Scinnohub Pharmaceutical Co., Ltd Verbindung mit makrocyclischer struktur und verwendung davon

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CN1050844C (zh) * 1993-12-07 2000-03-29 伊莱利利公司 蛋白激酶ｃ抑制剂
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CN113354653A (zh) * 2015-07-06 2021-09-07 特普医药公司 二芳基大环多晶型物及其制备方法
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KR102645316B1 (ko) 2017-07-28 2024-03-07 터닝 포인트 테라퓨틱스, 인크. 거대환형 화합물 및 이의 용도

Cited By (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10618912B2 (en) 2014-01-24 2020-04-14 Turning Point Therapeutics, Inc. Diaryl macrocycles as modulators of protein kinases
US11008337B2 (en) 2015-07-02 2021-05-18 Turning Point Therapeutics, Inc. Chiral diaryl macrocycles as modulators of protein kinases
US11452725B2 (en) 2015-07-21 2022-09-27 Turning Point Therapeutics, Inc. Chiral diaryl macrocycles and uses thereof
US10689400B2 (en) 2016-07-28 2020-06-23 Turning Point Therapeutics, Inc. Macrocycle kinase inhibitors
US11291667B2 (en) 2017-01-25 2022-04-05 Turning Point Therapeutics, Inc. Combination therapy involving diaryl macrocyclic compounds
US11155563B2 (en) 2017-07-28 2021-10-26 Turning Point Therapeutics, Inc. Macrocyclic compounds and uses thereof
US11286264B2 (en) 2017-07-28 2022-03-29 Turning Point Therapeutics, Inc. Macrocyclic compounds and uses thereof
US10745416B2 (en) 2017-12-19 2020-08-18 Turning Point Therapeutics, Inc. Macrocyclic compounds for treating disease
US11286265B2 (en) 2017-12-19 2022-03-29 Turning Point Therapeutics, Inc. Macrocyclic compounds for treating disease
US11731956B2 (en) 2018-10-22 2023-08-22 Alumis Inc. Substituted 1,2,4-triazoles as intermediates in the synthesis of TYK2 inhibitors
WO2021108672A1 (en) * 2019-11-27 2021-06-03 Turning Point Therapeutics, Inc. Combination therapy involving diaryl macrocyclic compounds
US11666574B2 (en) 2019-11-27 2023-06-06 Turning Point Therapeutics, Inc. Combination therapy involving diaryl macrocyclic compounds
US11981684B2 (en) 2022-02-22 2024-05-14 Turning Point Therapeutics, Inc. Macrocyclic compounds and uses thereof

Also Published As

Publication number Publication date
KR20180033194A (ko) 2018-04-02
DK3325488T3 (da) 2020-09-14
RU2018106245A3 (de) 2019-12-26
IL256868A (en) 2018-03-29
US20230346786A1 (en) 2023-11-02
JP6817287B2 (ja) 2021-01-20
BR112018001065A2 (pt) 2018-09-11
US11452725B2 (en) 2022-09-27
ES2818528T3 (es) 2021-04-13
CA2992324A1 (en) 2017-01-26
EP3325488B1 (de) 2020-06-24
CN108026109A (zh) 2018-05-11
HK1254606A1 (zh) 2019-07-26
EP3733187A1 (de) 2020-11-04
CN108026109B (zh) 2021-03-02
MX2018000718A (es) 2020-01-20
RU2020123800A (ru) 2020-10-02
IL256868B (en) 2021-03-25
JP2018524382A (ja) 2018-08-30
AU2016296878B2 (en) 2020-12-17
EP3325488A1 (de) 2018-05-30
RU2728579C2 (ru) 2020-07-30
ZA201800416B (en) 2021-07-28
WO2017015367A1 (en) 2017-01-26
RU2018106245A (ru) 2019-08-21
AU2016296878A1 (en) 2018-01-25
EP3325488A4 (de) 2019-04-24
US20210030756A1 (en) 2021-02-04

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