KR101965025B1 - 피라졸로[1,5-a]피리미딘계 화합물, 그를 포함하는 조성물 및 그의 사용 방법 - Google Patents

피라졸로[1,5-a]피리미딘계 화합물, 그를 포함하는 조성물 및 그의 사용 방법 Download PDF

Info

Publication number
KR101965025B1
KR101965025B1 KR1020147028071A KR20147028071A KR101965025B1 KR 101965025 B1 KR101965025 B1 KR 101965025B1 KR 1020147028071 A KR1020147028071 A KR 1020147028071A KR 20147028071 A KR20147028071 A KR 20147028071A KR 101965025 B1 KR101965025 B1 KR 101965025B1
Authority
KR
South Korea
Prior art keywords
mmol
delete delete
pyrimidin
pyrazolo
hydrocarbyl
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
KR1020147028071A
Other languages
English (en)
Korean (ko)
Other versions
KR20140138864A (ko
Inventor
잉지 비
케네스 고든 카슨
지오바니 시안체타
마이클 앨런 그린
고드윈 쿠미
앨런 메인
율리안 장
글렌 그레고리 지프
Original Assignee
렉시컨 파마슈티컬스 인코퍼레이티드
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 렉시컨 파마슈티컬스 인코퍼레이티드 filed Critical 렉시컨 파마슈티컬스 인코퍼레이티드
Publication of KR20140138864A publication Critical patent/KR20140138864A/ko
Application granted granted Critical
Publication of KR101965025B1 publication Critical patent/KR101965025B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020147028071A 2012-03-09 2013-03-05 피라졸로[1,5-a]피리미딘계 화합물, 그를 포함하는 조성물 및 그의 사용 방법 Active KR101965025B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261608765P 2012-03-09 2012-03-09
US61/608,765 2012-03-09
PCT/US2013/029056 WO2013134228A1 (en) 2012-03-09 2013-03-05 PYRAZOLO[1,5-a]PYRIMIDINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE

Publications (2)

Publication Number Publication Date
KR20140138864A KR20140138864A (ko) 2014-12-04
KR101965025B1 true KR101965025B1 (ko) 2019-04-02

Family

ID=47892052

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020147028071A Active KR101965025B1 (ko) 2012-03-09 2013-03-05 피라졸로[1,5-a]피리미딘계 화합물, 그를 포함하는 조성물 및 그의 사용 방법

Country Status (25)

Country Link
US (3) US8946415B2 (enExample)
EP (1) EP2834243B1 (enExample)
JP (1) JP6418950B2 (enExample)
KR (1) KR101965025B1 (enExample)
CN (1) CN104302649B (enExample)
AR (1) AR090292A1 (enExample)
AU (1) AU2013230128B2 (enExample)
BR (1) BR112014022000A8 (enExample)
CA (1) CA2866143C (enExample)
DK (1) DK2834243T3 (enExample)
ES (1) ES2676224T3 (enExample)
HU (1) HUE038786T2 (enExample)
IL (1) IL234486A (enExample)
IN (1) IN2014DN07384A (enExample)
MX (2) MX345830B (enExample)
NZ (1) NZ630721A (enExample)
PL (1) PL2834243T3 (enExample)
PT (1) PT2834243T (enExample)
RU (1) RU2014140735A (enExample)
SG (1) SG11201405561RA (enExample)
TR (1) TR201808280T4 (enExample)
TW (1) TW201341386A (enExample)
UY (1) UY34668A (enExample)
WO (1) WO2013134228A1 (enExample)
ZA (1) ZA201406149B (enExample)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8969565B2 (en) 2012-03-09 2015-03-03 Lexicon Pharmaceuticals, Inc. Imidazo[1,2-b]pyridazine-based compounds, compositions comprising them, and methods of their use
CN104302649B (zh) 2012-03-09 2017-06-23 莱西肯医药有限公司 基于吡唑并[1,5‑a]嘧啶的化合物、包含它们的组合物及其使用方法
US8901305B2 (en) 2012-07-31 2014-12-02 Bristol-Myers Squibb Company Aryl lactam kinase inhibitors
WO2014130258A1 (en) 2013-02-22 2014-08-28 Bristol-Myers Squibb Company 5h-chromeno[3,4-c]pyridines as inhibitors of adaptor associated kinase 1 (aak1)
TW201542550A (zh) * 2013-09-06 2015-11-16 Lexicon Pharmaceuticals Inc 吡唑并[1,5-a]嘧啶基化合物、包含彼之組合物以及使用彼之方法
JP6473146B2 (ja) 2013-10-11 2019-02-20 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company ピロロトリアジンキナーゼ阻害剤
HRP20191283T1 (hr) 2014-01-24 2019-10-18 Turning Point Therapeutics, Inc. Diaril makrocikli kao modulatori protein kinaze
EA201691397A1 (ru) * 2014-01-31 2016-11-30 Бристол-Майерс Сквибб Компани Хинолиновые ингибиторы киназы
TW201620911A (zh) * 2014-03-17 2016-06-16 雷西肯製藥股份有限公司 銜接子關聯激酶1之抑制劑、包含其之組成物、及其使用方法
US20170239249A1 (en) * 2014-09-30 2017-08-24 Bristol-Myers Squibb Company Quinazoline-based kinase inhibitors
CN107207514B (zh) * 2014-12-15 2020-01-24 康联制药有限公司 稠环杂芳基化合物及其作为trk抑制剂的用途
US10174044B2 (en) 2015-04-10 2019-01-08 Bristol-Myers Squibb Company Fused pyridines as kinase inhibitors
AU2016287568B2 (en) 2015-07-02 2020-08-20 Turning Point Therapeutics, Inc. Chiral diaryl macrocycles as modulators of protein kinases
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
ES2765738T3 (es) * 2015-11-02 2020-06-10 Janssen Pharmaceutica Nv Compuesto de [1,2,4]triazolo[1,5-a]pirimidin-7-ilo
TW201815799A (zh) 2016-07-28 2018-05-01 美商Tp生物醫藥公司 巨環激酶抑制劑
EP3535269B1 (en) 2016-11-02 2020-12-09 Janssen Pharmaceutica NV [1,2,4]triazolo[1,5-a]pyrimidine compounds as pde2 inhibitors
KR20190067788A (ko) 2016-11-02 2019-06-17 얀센 파마슈티카 엔.브이. Pde2 억제제로서의 [1,2,4]트리아졸로[1,5-a]피리미딘 화합물
UA125302C2 (uk) 2016-11-02 2022-02-16 Янссен Фармацевтика Нв Похідні [1,2,4]триазоло[1,5-a]піримідину як інгібітори pde2
TWI808958B (zh) 2017-01-25 2023-07-21 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
BR112020001695A2 (pt) 2017-07-28 2020-07-21 Turning Point Therapeutics, Inc. compostos macrocíclicos e usos dos mesmos
JP7216705B2 (ja) 2017-07-28 2023-02-02 ニンバス ラクシュミ, インコーポレイテッド Tyk2阻害剤およびその使用方法
PL3724191T3 (pl) * 2017-12-15 2022-04-25 Pyramid Biosciences, Inc. Pochodne 5-(2-(2,5-difluorofenylo)pirolidyn-1-ylo)-3-(1h-pirazol-1-ilo)pirazolo[1,5-a]pirymidyny i pokrewne związki jako inhibitory kinaz trk do leczenia nowotworu
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
WO2019120194A1 (zh) 2017-12-22 2019-06-27 深圳市塔吉瑞生物医药有限公司 一种取代的吡唑并[1,5-a]嘧啶化合物及其药物组合物及用途
EP3744723B1 (en) 2018-01-23 2023-10-18 Shenzhen TargetRx, Inc. Substituted pyrazolo[1,5-a]pyrimidine macrocyclic compound
CN112771047A (zh) * 2018-09-27 2021-05-07 重庆复创医药研究有限公司 作为RET激酶抑制剂的取代的咪唑[1,2-a]吡啶和[1,2,4]三唑[1,5-a]吡啶化合物
US11414431B2 (en) * 2018-10-15 2022-08-16 Nimbus Lakshmi, Inc. Substituted pyrazolo[1,5-a]pyrimidines as TYK2 inhibitors
US11730723B2 (en) 2020-04-21 2023-08-22 Lexicon Pharmaceuticals, Inc. Compounds and methods for treating viral infections
CN115427045A (zh) * 2020-04-21 2022-12-02 莱西肯医药有限公司 用于治疗cov-229e或cov-oc43冠状病毒感染的4-(3-(吡啶-3-基)吡唑并[1,5-a]嘧啶-5-基)哌嗪
US11478733B2 (en) 2020-11-24 2022-10-25 Caterpillar Inc. Filter interlock with tabs mating with a pedestal or a housing
US20250122207A1 (en) * 2023-09-08 2025-04-17 Satellos Bioscience Inc. Ap2 associated kinase 1 inhibitors and uses thereof
WO2025230262A1 (ko) * 2024-04-29 2025-11-06 심플렉스 주식회사 신규한 헤테로아릴 유도체 및 이의 aak1 억제 용도

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5464764A (en) 1989-08-22 1995-11-07 University Of Utah Research Foundation Positive-negative selection methods and vectors
WO1993004169A1 (en) 1991-08-20 1993-03-04 Genpharm International, Inc. Gene targeting in animal cells using isogenic dna constructs
US6194410B1 (en) * 1998-03-11 2001-02-27 Hoffman-La Roche Inc. Pyrazolopyrimidine and pyrazolines and process for preparation thereof
JP4847275B2 (ja) * 2005-10-21 2011-12-28 田辺三菱製薬株式会社 ピラゾロ[1,5−a]ピリミジン化合物
RU2009115954A (ru) 2006-09-29 2010-11-10 Новартис АГ (CH) Пиразолопиримидины в качестве ингибиторов липидной киназы р13к
US20120058997A1 (en) * 2006-11-06 2012-03-08 Supergen, Inc. Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
EA019507B1 (ru) * 2008-05-13 2014-04-30 Айрм Ллк Конденсированные азотсодержащие гетероциклы и содержащие их композиции в качестве ингибиторов киназы
PT3106463T (pt) * 2008-10-22 2018-05-18 Array Biopharma Inc Compostos de pirazolo[1,5-]pirimidina substituídos como inibidores de cinase trk
AR077468A1 (es) * 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
WO2011029027A1 (en) 2009-09-03 2011-03-10 Array Biopharma Inc. SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS
WO2011087999A1 (en) * 2010-01-14 2011-07-21 Merck Sharp & Dohme Corp. Pyrazolo[1,5-a]pyrimidines as mark inhibitors
PL3409278T3 (pl) * 2011-07-21 2021-02-22 Sumitomo Pharma Oncology, Inc. Heterocykliczne inhibitory kinazy białkowej
HUE036040T2 (hu) * 2012-03-09 2018-06-28 Lexicon Pharmaceuticals Inc Adaptor-asszociált kináz 1 gátlása fájdalom kezelésére
CN104302649B (zh) 2012-03-09 2017-06-23 莱西肯医药有限公司 基于吡唑并[1,5‑a]嘧啶的化合物、包含它们的组合物及其使用方法
US8969565B2 (en) 2012-03-09 2015-03-03 Lexicon Pharmaceuticals, Inc. Imidazo[1,2-b]pyridazine-based compounds, compositions comprising them, and methods of their use
TW201620911A (zh) * 2014-03-17 2016-06-16 雷西肯製藥股份有限公司 銜接子關聯激酶1之抑制劑、包含其之組成物、及其使用方法

Also Published As

Publication number Publication date
RU2014140735A (ru) 2016-04-27
BR112014022000A8 (pt) 2021-06-15
IL234486A (en) 2016-10-31
MX2014010589A (es) 2014-09-18
JP2015509535A (ja) 2015-03-30
AU2013230128A1 (en) 2014-09-25
EP2834243A1 (en) 2015-02-11
JP6418950B2 (ja) 2018-11-07
SG11201405561RA (en) 2014-10-30
CA2866143A1 (en) 2013-09-12
PT2834243T (pt) 2018-08-01
US20150183792A1 (en) 2015-07-02
US20170129896A1 (en) 2017-05-11
DK2834243T3 (en) 2018-07-23
MX381849B (es) 2025-03-13
TW201341386A (zh) 2013-10-16
NZ630721A (en) 2016-12-23
EP2834243B1 (en) 2018-04-25
IN2014DN07384A (enExample) 2015-04-24
WO2013134228A1 (en) 2013-09-12
CN104302649B (zh) 2017-06-23
UY34668A (es) 2013-10-31
CA2866143C (en) 2020-08-04
HUE038786T2 (hu) 2018-11-28
BR112014022000A2 (pt) 2017-06-20
US20130253194A1 (en) 2013-09-26
KR20140138864A (ko) 2014-12-04
AU2013230128B2 (en) 2017-08-17
PL2834243T3 (pl) 2018-09-28
US9403832B2 (en) 2016-08-02
ES2676224T3 (es) 2018-07-17
US8946415B2 (en) 2015-02-03
TR201808280T4 (tr) 2018-07-23
CN104302649A (zh) 2015-01-21
HK1201257A1 (en) 2015-08-28
AR090292A1 (es) 2014-11-05
MX345830B (es) 2017-02-17
ZA201406149B (en) 2016-06-29

Similar Documents

Publication Publication Date Title
KR101965025B1 (ko) 피라졸로[1,5-a]피리미딘계 화합물, 그를 포함하는 조성물 및 그의 사용 방법
US8969565B2 (en) Imidazo[1,2-b]pyridazine-based compounds, compositions comprising them, and methods of their use
JP6472450B2 (ja) ピラゾロ[1,5−a]ピリミジン系化合物、それを含む組成物、及びそれらの使用方法
US20150183791A1 (en) IMIDAZO[1,2-b]PYRIDAZINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE
JP2017507980A (ja) アダプター関連キナーゼ1の阻害剤、それを含む組成物、及びその使用方法
HK1201257B (en) Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use
HK1217658B (zh) 基於吡唑并[1,5-a]嘧啶的化合物、包含其的组合物和其使用方法

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20141006

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
A201 Request for examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20180219

Comment text: Request for Examination of Application

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

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20190320

GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20190327

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20190327

End annual number: 3

Start annual number: 1

PG1601 Publication of registration
PR1001 Payment of annual fee

Payment date: 20220216

Start annual number: 4

End annual number: 4

PR1001 Payment of annual fee

Payment date: 20250106

Start annual number: 7

End annual number: 7