CN104302649B - 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 - Google Patents
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 Download PDFInfo
- Publication number
- CN104302649B CN104302649B CN201380012483.0A CN201380012483A CN104302649B CN 104302649 B CN104302649 B CN 104302649B CN 201380012483 A CN201380012483 A CN 201380012483A CN 104302649 B CN104302649 B CN 104302649B
- Authority
- CN
- China
- Prior art keywords
- pyrimidin
- mmol
- pyrazolo
- compound
- piperazine
- 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.)
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- 0 *N(*)C(C=C[n]1nccc1N)=C Chemical compound *N(*)C(C=C[n]1nccc1N)=C 0.000 description 5
- AFVKKRXDGYHAQP-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CCN1c(cc[n]1nc2)nc1c2-c(cccn1)c1OC)=O Chemical compound CC(C)(C)OC(N(CC1)CCN1c(cc[n]1nc2)nc1c2-c(cccn1)c1OC)=O AFVKKRXDGYHAQP-UHFFFAOYSA-N 0.000 description 2
- MFINLMYILJJJND-UHFFFAOYSA-N Brc(cn[n]1cc2)c1nc2N1CCNCC1 Chemical compound Brc(cn[n]1cc2)c1nc2N1CCNCC1 MFINLMYILJJJND-UHFFFAOYSA-N 0.000 description 1
- NZVGDAUQGIPJKS-INIZCTEOSA-N CC(C)(C)OC(N1[C@H](CNc(cc[n]2nc3)nc2c3-c(cccc2)c2OC)CCC1)=O Chemical compound CC(C)(C)OC(N1[C@H](CNc(cc[n]2nc3)nc2c3-c(cccc2)c2OC)CCC1)=O NZVGDAUQGIPJKS-INIZCTEOSA-N 0.000 description 1
- DIMLBYMJHJEEOJ-NSHDSACASA-N CC(C)(C)OC(N1[C@H](CNc2nc3c(C(F)(F)F)cn[n]3cc2)CCC1)=O Chemical compound CC(C)(C)OC(N1[C@H](CNc2nc3c(C(F)(F)F)cn[n]3cc2)CCC1)=O DIMLBYMJHJEEOJ-NSHDSACASA-N 0.000 description 1
- GIOFAIKYNCSSTB-LBPRGKRZSA-N CC(C)(C)OC(N1[C@H](CNc2nc3ccn[n]3cc2)CCC1)=O Chemical compound CC(C)(C)OC(N1[C@H](CNc2nc3ccn[n]3cc2)CCC1)=O GIOFAIKYNCSSTB-LBPRGKRZSA-N 0.000 description 1
- QDNRGSZLDNADBY-NSHDSACASA-N CC(C)(C)OC(N[C@@H](CC1)CN1c(cc[n]1nc2)nc1c2[Br]=C)=O Chemical compound CC(C)(C)OC(N[C@@H](CC1)CN1c(cc[n]1nc2)nc1c2[Br]=C)=O QDNRGSZLDNADBY-NSHDSACASA-N 0.000 description 1
- MQHVRERVQJNPBQ-GOSISDBHSA-N CC(C)(C)[C@@H](C(N(CC1)CCN1c(cc[n]1nc2)nc1c2-c1cccnc1OC)=O)N Chemical compound CC(C)(C)[C@@H](C(N(CC1)CCN1c(cc[n]1nc2)nc1c2-c1cccnc1OC)=O)N MQHVRERVQJNPBQ-GOSISDBHSA-N 0.000 description 1
- HRIFHNOAWYENEC-KRWDZBQOSA-N CC(C)C[C@H](C)C(N(CC1)CCN1c(cc[n]1nc2)nc1c2-c1cccnc1OC)=O Chemical compound CC(C)C[C@H](C)C(N(CC1)CCN1c(cc[n]1nc2)nc1c2-c1cccnc1OC)=O HRIFHNOAWYENEC-KRWDZBQOSA-N 0.000 description 1
- DYEMAGIQCRKEGO-UHFFFAOYSA-N CC(C)OC(N(C)CCNc(cc[n]1nc2)nc1c2-c(ccnc1)c1OC)=O Chemical compound CC(C)OC(N(C)CCNc(cc[n]1nc2)nc1c2-c(ccnc1)c1OC)=O DYEMAGIQCRKEGO-UHFFFAOYSA-N 0.000 description 1
- BLIQHWVRJJIHLP-UHFFFAOYSA-N CC(C)OC(N(CC1)CCN1c(cc[n]1nc2)nc1c2-c(cccc1)c1OC)=O Chemical compound CC(C)OC(N(CC1)CCN1c(cc[n]1nc2)nc1c2-c(cccc1)c1OC)=O BLIQHWVRJJIHLP-UHFFFAOYSA-N 0.000 description 1
- JUSUMSXFHDTEMR-UHFFFAOYSA-N CC(C)OC(N(CC1)CCN1c(cc[n]1nc2)nc1c2Br)=O Chemical compound CC(C)OC(N(CC1)CCN1c(cc[n]1nc2)nc1c2Br)=O JUSUMSXFHDTEMR-UHFFFAOYSA-N 0.000 description 1
- VFCUOYBRMOCPFC-UHFFFAOYSA-N CC(C)OC(N(CC1)CCN1c(cc[n]1nc2)nc1c2C1=CC=CN(C)C1=C)=O Chemical compound CC(C)OC(N(CC1)CCN1c(cc[n]1nc2)nc1c2C1=CC=CN(C)C1=C)=O VFCUOYBRMOCPFC-UHFFFAOYSA-N 0.000 description 1
- KPLRELRHNCQSFD-UHFFFAOYSA-N COCC(C(N(CC1)CCN1c(cc[n]1nc2)nc1c2-c1cccnc1OC)=O)=N Chemical compound COCC(C(N(CC1)CCN1c(cc[n]1nc2)nc1c2-c1cccnc1OC)=O)=N KPLRELRHNCQSFD-UHFFFAOYSA-N 0.000 description 1
- IYNBELLOHXMHJN-UHFFFAOYSA-N COCCOC(N(CC1)CCN1c(cc[n]1nc2)nc1c2-c(cccn1)c1OC)=O Chemical compound COCCOC(N(CC1)CCN1c(cc[n]1nc2)nc1c2-c(cccn1)c1OC)=O IYNBELLOHXMHJN-UHFFFAOYSA-N 0.000 description 1
- IYSBSUPWYUVHKG-UHFFFAOYSA-N Clc(cc[n]1nc2)nc1c2Br Chemical compound Clc(cc[n]1nc2)nc1c2Br IYSBSUPWYUVHKG-UHFFFAOYSA-N 0.000 description 1
- WEPRLWNMBTYGGD-UHFFFAOYSA-N Clc1nc2ccn[n]2cc1 Chemical compound Clc1nc2ccn[n]2cc1 WEPRLWNMBTYGGD-UHFFFAOYSA-N 0.000 description 1
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
- A61K31/519—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
- 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
-
- 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)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (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 |
|---|---|
| CN104302649A CN104302649A (zh) | 2015-01-21 |
| CN104302649B true CN104302649B (zh) | 2017-06-23 |
Family
ID=47892052
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380012483.0A Active CN104302649B (zh) | 2012-03-09 | 2013-03-05 | 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 |
Country Status (25)
| Country | Link |
|---|---|
| US (3) | US8946415B2 (https=) |
| EP (1) | EP2834243B1 (https=) |
| JP (1) | JP6418950B2 (https=) |
| KR (1) | KR101965025B1 (https=) |
| CN (1) | CN104302649B (https=) |
| AR (1) | AR090292A1 (https=) |
| AU (1) | AU2013230128B2 (https=) |
| BR (1) | BR112014022000A8 (https=) |
| CA (1) | CA2866143C (https=) |
| DK (1) | DK2834243T3 (https=) |
| ES (1) | ES2676224T3 (https=) |
| HU (1) | HUE038786T2 (https=) |
| IL (1) | IL234486A (https=) |
| IN (1) | IN2014DN07384A (https=) |
| MX (2) | MX381849B (https=) |
| NZ (1) | NZ630721A (https=) |
| PL (1) | PL2834243T3 (https=) |
| PT (1) | PT2834243T (https=) |
| RU (1) | RU2014140735A (https=) |
| SG (1) | SG11201405561RA (https=) |
| TR (1) | TR201808280T4 (https=) |
| TW (1) | TW201341386A (https=) |
| UY (1) | UY34668A (https=) |
| WO (1) | WO2013134228A1 (https=) |
| ZA (1) | ZA201406149B (https=) |
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| 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 |
| WO2013134219A1 (en) | 2012-03-09 | 2013-09-12 | Lexicon Pharmaceuticals, Inc. | Imidazo [1, 2 - b] pyridazine - based compounds, compositions comprising them, and uses thereof |
| US8901305B2 (en) | 2012-07-31 | 2014-12-02 | Bristol-Myers Squibb Company | Aryl lactam kinase inhibitors |
| JP2016509066A (ja) | 2013-02-22 | 2016-03-24 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | アダプター関連キナーゼ１（ａａｋ１）の阻害剤としての５ｈ−クロメノ［３，４−ｃ］ピリジン |
| 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 |
| EP3054955B1 (en) | 2013-10-11 | 2018-05-30 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| ES2933350T3 (es) | 2014-01-24 | 2023-02-06 | Turning Point Therapeutics Inc | Macrociclos de diarilo como moduladores de proteína quinasas |
| MX2016009352A (es) * | 2014-01-31 | 2016-10-13 | Bristol Myers Squibb Co | Inhibidores de quinasa 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 |
| CA2971024C (en) * | 2014-12-15 | 2023-09-26 | Handok Inc. | 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) |
| AU2016287568B2 (en) | 2015-07-02 | 2020-08-20 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| RU2765181C2 (ru) | 2015-07-06 | 2022-01-26 | Тёрнинг Поинт Терапьютикс, Инк. | Полиморфная форма диарильного макроцикла |
| PT3733187T (pt) | 2015-07-21 | 2024-11-08 | Turning Point Therapeutics Inc | Macrociclo de diarilo quiral e utilização do mesmo no tratamento do cancro |
| ES2765738T3 (es) * | 2015-11-02 | 2020-06-10 | Janssen Pharmaceutica Nv | Compuesto de [1,2,4]triazolo[1,5-a]pirimidin-7-ilo |
| US10689400B2 (en) | 2016-07-28 | 2020-06-23 | Turning Point Therapeutics, Inc. | Macrocycle kinase inhibitors |
| MX385576B (es) * | 2016-11-02 | 2025-03-18 | Janssen Pharmaceutica Nv | Derivados de [1,2,4]triazol[1,5-a]pirimidina como inhibidores de pde2 |
| CA3038916A1 (en) | 2016-11-02 | 2018-05-11 | Janssen Pharmaceutica Nv | [1,2,4]triazolo[1,5-a]pyrimidine compounds as pde2 inhibitors |
| AU2017353313C1 (en) | 2016-11-02 | 2022-06-09 | Janssen Pharmaceutica Nv | (1,2,4)triazolo(1,5-a)pyrimidine compounds as PDE2 inhibitors |
| 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 |
| CN111182903A (zh) | 2017-07-28 | 2020-05-19 | 特普医药公司 | 巨环化合物及其用途 |
| SI3658557T1 (sl) | 2017-07-28 | 2024-10-30 | Takeda Pharmaceutical Company Limited | Zaviralci TYK2 in njihova uporaba |
| SG11202005237SA (en) * | 2017-12-15 | 2020-07-29 | Pyramid Biosciences Inc | 5-(2-(2,5-difluorophenyl)pyrrolidin-1 -yl)-3-(1h-pyrazol-1-yl)pyrazolo[1,5-a]pyrimidine derivatives and related compounds as trk kinase inhibitors for treating cancer |
| LT3728271T (lt) | 2017-12-19 | 2022-12-12 | Turning Point Therapeutics, Inc. | Makrocikliniai junginiai, skirti ligų gydymui |
| EP3730492A4 (en) * | 2017-12-22 | 2021-08-11 | Shenzhen TargetRx, Inc. | SUBSTITUTED PYRAZOLO [1,5-A] PYRIMIDINE COMPOUND AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
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| 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 |
| CN113271940A (zh) * | 2018-10-15 | 2021-08-17 | 林伯士拉克许米公司 | Tyk2抑制剂和其用途 |
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| AU2021258128A1 (en) | 2020-04-21 | 2022-11-03 | 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 |
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| DK2822555T3 (en) * | 2012-03-09 | 2018-02-05 | Lexicon Pharmaceuticals Inc | Inhibition of adapter-associated kinase 1 for the treatment of pain |
| 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 |
| 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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| CN1236780A (zh) * | 1998-03-11 | 1999-12-01 | 弗·哈夫曼-拉罗切有限公司 | 吡唑并嘧啶和吡唑并三嗪 |
| WO2011087999A1 (en) * | 2010-01-14 | 2011-07-21 | Merck Sharp & Dohme Corp. | Pyrazolo[1,5-a]pyrimidines as mark inhibitors |
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