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 PDFInfo
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- 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
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- pyrimidin
- pyrazolo
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- 0 *c1c2nc(*)cc[n]2nc1 Chemical compound *c1c2nc(*)cc[n]2nc1 0.000 description 5
- WSZHSTRLEOLQEE-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CCN1c(cc[n]1nc2)nc1c2Br)=O Chemical compound CC(C)(C)OC(N(CC1)CCN1c(cc[n]1nc2)nc1c2Br)=O WSZHSTRLEOLQEE-UHFFFAOYSA-N 0.000 description 1
- DYEMAGIQCRKEGO-UHFFFAOYSA-N CC(C)OC(N(C)CCNc(cc[n]1nc2)nc1c2-c1ccncc1OC)=O Chemical compound CC(C)OC(N(C)CCNc(cc[n]1nc2)nc1c2-c1ccncc1OC)=O DYEMAGIQCRKEGO-UHFFFAOYSA-N 0.000 description 1
- XGVKICRLMGGHBY-UHFFFAOYSA-N CCC(C)CCCNc1nc2c(C)cn[n]2cc1 Chemical compound CCC(C)CCCNc1nc2c(C)cn[n]2cc1 XGVKICRLMGGHBY-UHFFFAOYSA-N 0.000 description 1
- CTLHUJXIVFTLIJ-UHFFFAOYSA-N CCCCNc1nc2ccn[n]2cc1 Chemical compound CCCCNc1nc2ccn[n]2cc1 CTLHUJXIVFTLIJ-UHFFFAOYSA-N 0.000 description 1
- ZNMDIOWCFMTWTC-UHFFFAOYSA-N CNCCNc(cc[n]1nc2)nc1c2Br Chemical compound CNCCNc(cc[n]1nc2)nc1c2Br ZNMDIOWCFMTWTC-UHFFFAOYSA-N 0.000 description 1
- JDIMQUKJAVZZGD-UHFFFAOYSA-N COCCNc(cc[n]1nc2)nc1c2-c(cc1)ccc1-c1nnn[nH]1 Chemical compound COCCNc(cc[n]1nc2)nc1c2-c(cc1)ccc1-c1nnn[nH]1 JDIMQUKJAVZZGD-UHFFFAOYSA-N 0.000 description 1
- AYROYQBHFFRDPV-UHFFFAOYSA-N Nc([nH]nc1)c1-c1ccc[s]1 Chemical compound Nc([nH]nc1)c1-c1ccc[s]1 AYROYQBHFFRDPV-UHFFFAOYSA-N 0.000 description 1
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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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- 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
- 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
- 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
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- 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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- 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)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
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
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020147028071A KR101965025B1 (ko) | 2012-03-09 | 2013-03-05 | 피라졸로[1,5-a]피리미딘계 화합물, 그를 포함하는 조성물 및 그의 사용 방법 |
Country Status (26)
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| MX347917B (es) | 2012-03-09 | 2017-05-17 | Lexicon Pharmaceuticals Inc | Compuestos a base de imidazo[1,2-b]piridazina, composiciones que los comprenden, y metodos para su uso. |
| 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 |
| EP2958924B1 (en) | 2013-02-22 | 2016-12-28 | 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 |
| US9737542B2 (en) | 2013-10-11 | 2017-08-22 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| HUE045208T2 (hu) | 2014-01-24 | 2019-12-30 | Turning Point Therapeutics Inc | Diaril makrociklusok mint protein kinázok modulátorai |
| ES2701903T3 (es) * | 2014-01-31 | 2019-02-26 | Bristol Myers Squibb Co | Inhibidores de cinasa a base de quinolina |
| 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 |
| WO2016053794A1 (en) * | 2014-09-30 | 2016-04-07 | Bristol-Myers Squibb Company | Quinazoline-based kinase inhibitors |
| US9701681B2 (en) * | 2014-12-15 | 2017-07-11 | Cmg Pharmaceutical Co., Ltd. | Fused ring heteroaryl compounds and their use as Trk inhibitors |
| ES2740224T3 (es) | 2015-04-10 | 2020-02-05 | Bristol Myers Squibb Co | 6H-isocromeno[3,4-c]piridinas y benzo[c][1,7]naftiridin-6-(5H)-onas como inhibidores de la cinasa asociada a adaptador 1 (AAK1) |
| WO2017004342A1 (en) | 2015-07-02 | 2017-01-05 | Tp Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| 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 |
| DK3325488T3 (da) | 2015-07-21 | 2020-09-14 | Turning Point Therapeutics Inc | Chiral diaryl-makrocyklus og anvendelse deraf til behandling af cancer |
| JP6872541B2 (ja) * | 2015-11-02 | 2021-05-19 | ヤンセン ファーマシューティカ エヌ．ベー． | ［１，２，４］トリアゾロ［１，５−ａ］ピリミジン−７−イル化合物 |
| CN109715165A (zh) | 2016-07-28 | 2019-05-03 | Tp生物医药公司 | 巨环激酶抑制剂 |
| SG11201903892UA (en) * | 2016-11-02 | 2019-05-30 | Janssen Pharmaceutica Nv | [1,2,4]triazolo[1,5-a]pyrimidine derivatives as pde2 inhibitors |
| ES2912264T3 (es) | 2016-11-02 | 2022-05-25 | Janssen Pharmaceutica Nv | Compuestos de [1,2,4]triazolo[1,5-a]pirimidina como inhibidores de PDE2 |
| ES2855032T3 (es) | 2016-11-02 | 2021-09-23 | Janssen Pharmaceutica Nv | Compuestos de [1,2,4]triazolo[1,5-a]pirimidina como inhibidores de 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 |
| 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 |
| WO2019023417A1 (en) | 2017-07-28 | 2019-01-31 | Tp Therapeutics, Inc. | MACROCYCLIC COMPOUNDS AND USES THEREOF |
| PL3728271T3 (pl) | 2017-12-19 | 2023-01-23 | Turning Point Therapeutics, Inc. | Związki makrocykliczne do leczenia chorób |
| US11453672B2 (en) | 2017-12-22 | 2022-09-27 | Shenzhen Targetrx, Inc. | Substituted pyrazolo[1,5-a]pyrimidines as tropomyosin receptor kinase inhibitors |
| WO2019144885A1 (zh) | 2018-01-23 | 2019-08-01 | 深圳市塔吉瑞生物医药有限公司 | 取代的吡唑并[1,5-a]嘧啶类的大环化合物 |
| JP2022503932A (ja) * | 2018-09-27 | 2022-01-12 | フォチョン・ファーマシューティカルズ・リミテッド | Ｒｅｔキナーゼ阻害剤としての置換イミダゾ［１，２－ａ］ピリジン及び［１，２，４］トリアゾロ［１，５－ａ］ピリジン化合物 |
| AU2019360941A1 (en) * | 2018-10-15 | 2021-04-29 | Takeda Pharmaceutical Company Limited | TYK2 inhibitors and uses thereof |
| CA3175970A1 (en) | 2020-04-21 | 2021-10-28 | Suma GOPINATHAN | Aak1 inhibitors for use in treating viral infections |
| WO2021216454A1 (en) * | 2020-04-21 | 2021-10-28 | Lexicon Pharmaceuticals, Inc. | 4-(3-(pyridin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)piperazine for use in the the treatment of cov-229e or cov-oc43 coronaviruses infections |
| US11478733B2 (en) | 2020-11-24 | 2022-10-25 | Caterpillar Inc. | Filter interlock with tabs mating with a pedestal or a housing |
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| 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 |
| CA2664378A1 (en) | 2006-09-29 | 2008-04-03 | Novartis Ag | Pyrazolopyrimidines as pi3k lipid kinase inhibitors |
| 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 |
| US8507488B2 (en) * | 2008-05-13 | 2013-08-13 | Irm Llc | Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors |
| PL3372605T3 (pl) * | 2008-10-22 | 2022-03-07 | Array Biopharma Inc. | Podstawione związki pirazolo[1,5-a]pirymidynowe jako inhibitory kinaz 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 |
| JP6105578B2 (ja) * | 2011-07-21 | 2017-03-29 | トレロ ファーマシューティカルズ， インコーポレイテッド | 複素環式プロテインキナーゼ阻害剤 |
| 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 |
| MX347917B (es) | 2012-03-09 | 2017-05-17 | Lexicon Pharmaceuticals Inc | Compuestos a base de imidazo[1,2-b]piridazina, composiciones que los comprenden, y metodos para su uso. |
| JP2015513557A (ja) * | 2012-03-09 | 2015-05-14 | レクシコン ファーマシューティカルズ インコーポレイテッド | 疼痛の治療に対するアダプター関連キナーゼ１の阻害 |
| 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 |
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2013
- 2013-03-05 CN CN201380012483.0A patent/CN104302649B/zh active Active
- 2013-03-05 CA CA2866143A patent/CA2866143C/en active Active
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- 2013-03-05 HU HUE13710250A patent/HUE038786T2/hu unknown
- 2013-03-05 DK DK13710250.5T patent/DK2834243T3/en active
- 2013-03-05 BR BR112014022000A patent/BR112014022000A8/pt not_active Application Discontinuation
- 2013-03-05 US US13/785,355 patent/US8946415B2/en active Active
- 2013-03-05 PT PT137102505T patent/PT2834243T/pt unknown
- 2013-03-05 RU RU2014140735A patent/RU2014140735A/ru not_active Application Discontinuation
- 2013-03-05 PL PL13710250T patent/PL2834243T3/pl unknown
- 2013-03-05 JP JP2014561024A patent/JP6418950B2/ja active Active
- 2013-03-05 ES ES13710250.5T patent/ES2676224T3/es active Active
- 2013-03-05 KR KR1020147028071A patent/KR101965025B1/ko active IP Right Grant
- 2013-03-05 WO PCT/US2013/029056 patent/WO2013134228A1/en active Application Filing
- 2013-03-05 MX MX2014010589A patent/MX345830B/es active IP Right Grant
- 2013-03-05 AU AU2013230128A patent/AU2013230128B2/en active Active
- 2013-03-05 IN IN7384DEN2014 patent/IN2014DN07384A/en unknown
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- 2013-03-05 NZ NZ630721A patent/NZ630721A/en unknown
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- 2013-03-08 TW TW102108283A patent/TW201341386A/zh unknown
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- 2013-03-11 UY UY0001034668A patent/UY34668A/es not_active Application Discontinuation
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2014
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- 2014-09-07 IL IL234486A patent/IL234486A/en active IP Right Grant
- 2014-09-11 US US14/483,898 patent/US9403832B2/en active Active
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2015
- 2015-02-13 HK HK15101651.1A patent/HK1201257A1/xx unknown
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