AU2013230128B2 - Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use - Google Patents

Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use Download PDF

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Publication number
AU2013230128B2
AU2013230128B2 AU2013230128A AU2013230128A AU2013230128B2 AU 2013230128 B2 AU2013230128 B2 AU 2013230128B2 AU 2013230128 A AU2013230128 A AU 2013230128A AU 2013230128 A AU2013230128 A AU 2013230128A AU 2013230128 B2 AU2013230128 B2 AU 2013230128B2
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mmol
pyrimidin
pyrazolo
ric
hydrocarbyl
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AU2013230128A1 (en
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Yingzhi Bi
Kenneth Gordon Carson
Giovanni Cianchetta
Michael Alan Green
Godwin KUMI
Alan Main
Yulian Zhang
Glenn Gregory ZIPP
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Lexicon Pharmaceuticals Inc
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Lexicon Pharmaceuticals Inc
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    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds

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  • 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)
AU2013230128A 2012-03-09 2013-03-05 Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use Active AU2013230128B2 (en)

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

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AU2013230128A1 AU2013230128A1 (en) 2014-09-25
AU2013230128B2 true AU2013230128B2 (en) 2017-08-17

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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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6194410B1 (en) * 1998-03-11 2001-02-27 Hoffman-La Roche Inc. Pyrazolopyrimidine and pyrazolines and process for preparation thereof

Family Cites Families (15)

* 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
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6194410B1 (en) * 1998-03-11 2001-02-27 Hoffman-La Roche Inc. Pyrazolopyrimidine and pyrazolines and process for preparation thereof

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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
KR101965025B1 (ko) 2019-04-02
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
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

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