KR102698366B1 - 피라졸 피리미딘 유도체 및 이의 용도 - Google Patents

피라졸 피리미딘 유도체 및 이의 용도 Download PDF

Info

Publication number
KR102698366B1
KR102698366B1 KR1020187006128A KR20187006128A KR102698366B1 KR 102698366 B1 KR102698366 B1 KR 102698366B1 KR 1020187006128 A KR1020187006128 A KR 1020187006128A KR 20187006128 A KR20187006128 A KR 20187006128A KR 102698366 B1 KR102698366 B1 KR 102698366B1
Authority
KR
South Korea
Prior art keywords
compound
stereoisomer
pharmaceutically acceptable
branched
alkyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
KR1020187006128A
Other languages
English (en)
Korean (ko)
Other versions
KR20180043794A (ko
Inventor
이논 벤 네리아
가이 브라치야
이도 버스테인
웰리드 민젤
이리트 스니어-알카레이
조셉 보카
단수 리
Original Assignee
이섬 리서치 디벨러프먼트 컴파니 오브 더 히브루 유니버시티 오브 예루살렘 엘티디.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 이섬 리서치 디벨러프먼트 컴파니 오브 더 히브루 유니버시티 오브 예루살렘 엘티디. filed Critical 이섬 리서치 디벨러프먼트 컴파니 오브 더 히브루 유니버시티 오브 예루살렘 엘티디.
Publication of KR20180043794A publication Critical patent/KR20180043794A/ko
Application granted granted Critical
Publication of KR102698366B1 publication Critical patent/KR102698366B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/08—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020187006128A 2015-08-04 2016-08-04 피라졸 피리미딘 유도체 및 이의 용도 Active KR102698366B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562200846P 2015-08-04 2015-08-04
US62/200,846 2015-08-04
US201562268750P 2015-12-17 2015-12-17
US62/268,750 2015-12-17
PCT/IL2016/050852 WO2017021969A1 (en) 2015-08-04 2016-08-04 Pyrazole pyrimidine derivative and uses thereof

Publications (2)

Publication Number Publication Date
KR20180043794A KR20180043794A (ko) 2018-04-30
KR102698366B1 true KR102698366B1 (ko) 2024-08-26

Family

ID=56738143

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020187006128A Active KR102698366B1 (ko) 2015-08-04 2016-08-04 피라졸 피리미딘 유도체 및 이의 용도

Country Status (23)

Country Link
US (4) US10376511B2 (enExample)
EP (1) EP3331877B1 (enExample)
JP (1) JP7083309B2 (enExample)
KR (1) KR102698366B1 (enExample)
CN (1) CN108137562B (enExample)
AU (2) AU2016304464B2 (enExample)
CA (1) CA2994644A1 (enExample)
CY (1) CY1124898T1 (enExample)
DK (1) DK3331877T3 (enExample)
ES (1) ES2901349T3 (enExample)
HR (1) HRP20211949T1 (enExample)
HU (1) HUE057607T2 (enExample)
IL (1) IL257282B (enExample)
LT (1) LT3331877T (enExample)
MX (1) MX384172B (enExample)
PL (1) PL3331877T3 (enExample)
PT (1) PT3331877T (enExample)
RS (1) RS62728B1 (enExample)
RU (1) RU2735522C2 (enExample)
SI (1) SI3331877T1 (enExample)
SM (1) SMT202100720T1 (enExample)
WO (1) WO2017021969A1 (enExample)
ZA (1) ZA201800671B (enExample)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7083309B2 (ja) * 2015-08-04 2022-06-10 イッサム リサーチ ディベロップメント カンパニー オブ ザ ヘブリュー ユニバーシティ オブ エルサレム エルティーディー． ピラゾールピリミジン誘導体及びその使用
US11072599B2 (en) * 2017-02-01 2021-07-27 Biotheryx, Inc. Pyrazole compounds and uses thereof
JOP20180011A1 (ar) 2017-02-16 2019-01-30 Gilead Sciences Inc مشتقات بيرولو [1، 2-b]بيريدازين
AU2019219678A1 (en) * 2018-02-08 2020-08-27 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use
TWI842978B (zh) 2018-07-13 2024-05-21 美商基利科學股份有限公司 衍生物
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
WO2020168197A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors
WO2020180959A1 (en) 2019-03-05 2020-09-10 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
IL288547B2 (en) * 2019-06-03 2025-10-01 Biotheryx Inc Non-hygroscopic crystalline pyrazole compound salts, pharmaceutical preparations thereof and use thereof
WO2021000957A1 (zh) * 2019-07-04 2021-01-07 北京国鸿生物医药科技有限公司 一种杂环化合物、其药物组合物及用途
PH12022550361A1 (en) 2019-08-14 2023-02-27 Incyte Corp Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
PE20221905A1 (es) 2019-10-11 2022-12-23 Incyte Corp Aminas biciclicas como inhibidoras de la cdk2
WO2021146220A1 (en) * 2020-01-13 2021-07-22 Biotheryx, Inc. Pyrazolylpyrimidines and use thereof
WO2021155050A1 (en) * 2020-01-29 2021-08-05 Biotheryx, Inc. Kinase modulators, pharmaceutical compositions, and therapeutic applications
WO2021191384A1 (en) * 2020-03-26 2021-09-30 Janssen Pharmaceutica Nv Aryl piperidines as monoacylglycerol lipase modulators
AU2022242818A1 (en) * 2021-03-24 2023-10-05 Yissum Research Development Company Of The Hebrew University Of Jerusalem, Ltd. Pyrazolylpyrimidines for treating malignant solid tumor
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
US11752151B2 (en) * 2021-07-12 2023-09-12 Buddhist Tzu Chi Medical Foundation Method for enhancing hair growth
US20230053307A1 (en) * 2021-07-19 2023-02-16 Buddhist Tzu Chi Medical Foundation Method for preventing or treating skin disorders and conditions
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
WO2025199440A1 (en) * 2024-03-21 2025-09-25 Edgewood Oncology Methods of treating liposarcoma using a pyrazole compound

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20150094305A1 (en) 2013-09-27 2015-04-02 Nimbus Iris, Inc. Irak inhibitors and uses thereof
WO2015058140A1 (en) 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
US20150202205A1 (en) 2011-11-04 2015-07-23 Jasco Pharmaceuticals, LLC Aminopyrimidine kinase inhibitors

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2307667T3 (es) * 2000-12-05 2008-12-01 Vertex Pharmaceuticals Incorporated Inhibidires de quinasas terminales c-jun(jnk) y otras proteinas quinasas.
AU2002308748A1 (en) 2001-05-16 2002-11-25 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
GB0215844D0 (en) * 2002-07-09 2002-08-14 Novartis Ag Organic compounds
AU2005227997A1 (en) 2004-03-30 2005-10-13 Arena Pharmaceuticals, Inc. Pyrimidine derivatives and methods of treatment related to the use thereof
JP2007145819A (ja) * 2005-10-28 2007-06-14 Tanabe Seiyaku Co Ltd 医薬組成物
WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
JP2009538352A (ja) * 2006-05-26 2009-11-05 アストラゼネカ アクチボラグ 細胞増殖を阻害するための薬剤としての２−カルボシクロアミノ−４−イミダゾリルピリミジン類
KR20100098521A (ko) * 2007-12-07 2010-09-07 노파르티스 아게 피라졸 유도체 및 그의 사이클린 의존성 키나제 억제제로서의 용도
JP7083309B2 (ja) 2015-08-04 2022-06-10 イッサム リサーチ ディベロップメント カンパニー オブ ザ ヘブリュー ユニバーシティ オブ エルサレム エルティーディー． ピラゾールピリミジン誘導体及びその使用
US11072599B2 (en) * 2017-02-01 2021-07-27 Biotheryx, Inc. Pyrazole compounds and uses thereof
AU2019219678A1 (en) 2018-02-08 2020-08-27 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20150202205A1 (en) 2011-11-04 2015-07-23 Jasco Pharmaceuticals, LLC Aminopyrimidine kinase inhibitors
US20150094305A1 (en) 2013-09-27 2015-04-02 Nimbus Iris, Inc. Irak inhibitors and uses thereof
WO2015058140A1 (en) 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)

Also Published As

Publication number Publication date
US10960003B2 (en) 2021-03-30
MX2018001395A (es) 2018-04-13
US10376511B2 (en) 2019-08-13
DK3331877T3 (da) 2022-01-03
HK1256535A1 (en) 2019-09-27
PT3331877T (pt) 2021-12-27
US20210251992A1 (en) 2021-08-19
RU2018107668A3 (enExample) 2020-01-13
CN108137562B (zh) 2021-11-30
AU2021200839A1 (en) 2021-03-04
CA2994644A1 (en) 2017-02-09
US20180214447A1 (en) 2018-08-02
SMT202100720T1 (it) 2022-01-10
WO2017021969A1 (en) 2017-02-09
RS62728B1 (sr) 2022-01-31
MX384172B (es) 2025-03-14
NZ739511A (en) 2023-08-25
US20190365759A1 (en) 2019-12-05
HRP20211949T1 (hr) 2022-03-18
HUE057607T2 (hu) 2022-06-28
SI3331877T1 (sl) 2022-02-28
JP7083309B2 (ja) 2022-06-10
AU2016304464A1 (en) 2018-02-22
RU2735522C2 (ru) 2020-11-03
EP3331877A1 (en) 2018-06-13
RU2018107668A (ru) 2019-09-05
AU2016304464B2 (en) 2020-11-19
IL257282A (en) 2018-03-29
ZA201800671B (en) 2020-05-27
US20250049793A1 (en) 2025-02-13
ES2901349T3 (es) 2022-03-22
KR20180043794A (ko) 2018-04-30
US11925641B2 (en) 2024-03-12
CN108137562A (zh) 2018-06-08
LT3331877T (lt) 2022-01-10
IL257282B (en) 2021-06-30
CY1124898T1 (el) 2023-01-05
EP3331877B1 (en) 2021-09-22
PL3331877T3 (pl) 2022-01-31
JP2018525441A (ja) 2018-09-06

Similar Documents

Publication Publication Date Title
KR102698366B1 (ko) 피라졸 피리미딘 유도체 및 이의 용도
CN112778276A (zh) 作为shp2抑制剂的化合物及其应用
WO2020094104A1 (zh) 一类含氮稠杂环类shp2抑制剂化合物、制备方法和用途
CN115776891A (zh) Stat降解剂和其用途
JP2010514690A (ja) Ｊａｎｕｓキナーゼ阻害剤としての置換複素環
CN105579452A (zh) 作为NIK抑制剂的新型3-(1H-吡唑-4-基)-1H-吡咯并[2,3-c]吡啶衍生物
CN107074881A (zh) 作为nik抑制剂的新的噻吩并嘧啶衍生物
TW201625629A (zh) 新穎吡咯并嘧啶化合物或其鹽，及含有其之醫藥組成物，特別是基於ｎａｅ抑制作用的腫瘤等之預防劑及／或治療劑
CN110475771B (zh) Ck1和/或irak1抑制剂、药物组合物和用于癌症治疗的治疗应用
CN117561058A (zh) Cdk2抑制剂及其使用方法
HK1256535B (en) Pyrazole pyrimidine derivative and uses thereof
NZ739511B2 (en) Pyrazole pyrimidine derivative and uses thereof
CN121085992A (zh) 信号转导及转录激活蛋白6选择性降解剂化合物
HK40057478B (zh) Hpk1抑制剂及其使用方法
HK40019133B (en) N1-(4-(5-(cyclopropylmethyl)-1-methyl-1h-pyrazol-4-yl)pyridin-2-yl)cyclohexane-1,4-diamine derivatives and related compounds as ck1 and/or iraki inhibitors for treating cancer

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

R18-X000 Changes to party contact information recorded

St.27 status event code: A-3-3-R10-R18-oth-X000

A201 Request for examination
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000