AR090292A1 - Compuestos basados en pirazolo[1,5-a]pirimidina, composiciones que los comprenden y metodos que los utilizan - Google Patents
Compuestos basados en pirazolo[1,5-a]pirimidina, composiciones que los comprenden y metodos que los utilizanInfo
- Publication number
- AR090292A1 AR090292A1 ARP130100765A ARP130100765A AR090292A1 AR 090292 A1 AR090292 A1 AR 090292A1 AR P130100765 A ARP130100765 A AR P130100765A AR P130100765 A ARP130100765 A AR P130100765A AR 090292 A1 AR090292 A1 AR 090292A1
- Authority
- AR
- Argentina
- Prior art keywords
- halo
- cyano
- or1c
- optionally substituted
- hydrocarbyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 238000000034 method Methods 0.000 title abstract 3
- 239000000203 mixture Substances 0.000 title abstract 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 13
- 125000001475 halogen functional group Chemical group 0.000 abstract 13
- 125000001183 hydrocarbyl group Chemical group 0.000 abstract 10
- 238000006467 substitution reaction Methods 0.000 abstract 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 108091000080 Phosphotransferase Proteins 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 2
- 102000020233 phosphotransferase Human genes 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 208000037765 diseases and disorders Diseases 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 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
-
- 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
- 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
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)
- 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 (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261608765P | 2012-03-09 | 2012-03-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR090292A1 true AR090292A1 (es) | 2014-11-05 |
Family
ID=47892052
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130100765A AR090292A1 (es) | 2012-03-09 | 2013-03-11 | Compuestos basados en pirazolo[1,5-a]pirimidina, composiciones que los comprenden y metodos que los utilizan |
Country Status (25)
| Country | Link |
|---|---|
| US (3) | US8946415B2 (OSRAM) |
| EP (1) | EP2834243B1 (OSRAM) |
| JP (1) | JP6418950B2 (OSRAM) |
| KR (1) | KR101965025B1 (OSRAM) |
| CN (1) | CN104302649B (OSRAM) |
| AR (1) | AR090292A1 (OSRAM) |
| AU (1) | AU2013230128B2 (OSRAM) |
| BR (1) | BR112014022000A8 (OSRAM) |
| CA (1) | CA2866143C (OSRAM) |
| DK (1) | DK2834243T3 (OSRAM) |
| ES (1) | ES2676224T3 (OSRAM) |
| HU (1) | HUE038786T2 (OSRAM) |
| IL (1) | IL234486A (OSRAM) |
| IN (1) | IN2014DN07384A (OSRAM) |
| MX (2) | MX345830B (OSRAM) |
| NZ (1) | NZ630721A (OSRAM) |
| PL (1) | PL2834243T3 (OSRAM) |
| PT (1) | PT2834243T (OSRAM) |
| RU (1) | RU2014140735A (OSRAM) |
| SG (1) | SG11201405561RA (OSRAM) |
| TR (1) | TR201808280T4 (OSRAM) |
| TW (1) | TW201341386A (OSRAM) |
| UY (1) | UY34668A (OSRAM) |
| WO (1) | WO2013134228A1 (OSRAM) |
| ZA (1) | ZA201406149B (OSRAM) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8946415B2 (en) | 2012-03-09 | 2015-02-03 | Lexicon Pharmaceuticals, Inc. | Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use |
| BR112014022271B1 (pt) | 2012-03-09 | 2021-09-21 | Lexicon Pharmaceuticals, Inc | Compostos com base em imidazo[1,2-b]piridazina, composições compreendendo-os, e usos dos mesmos |
| US8901305B2 (en) | 2012-07-31 | 2014-12-02 | Bristol-Myers Squibb Company | Aryl lactam kinase inhibitors |
| CN105121445A (zh) | 2013-02-22 | 2015-12-02 | 百时美施贵宝公司 | 作为连接蛋白相关激酶1(AAK1)抑制剂的5H-色烯并[3,4-c]吡啶 |
| 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 |
| CN105979950A (zh) | 2013-10-11 | 2016-09-28 | 百时美施贵宝公司 | 吡咯并三嗪激酶抑制剂 |
| DK3636649T3 (da) | 2014-01-24 | 2024-05-21 | Turning Point Therapeutics Inc | Diarylmakrocykler som modulatorer af proteinkinaser |
| US9932320B2 (en) * | 2014-01-31 | 2018-04-03 | Bristol-Myers Squibb Company | Quinoline-based kinase inhibitors |
| 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 |
| AU2015365587B2 (en) * | 2014-12-15 | 2020-07-23 | 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) |
| EP3317285B1 (en) | 2015-07-02 | 2021-01-27 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| WO2017007759A1 (en) | 2015-07-06 | 2017-01-12 | Tp Therapeutics, Inc. | Diaryl macrocycle polymorph |
| DK3733187T3 (da) | 2015-07-21 | 2025-01-02 | Turning Point Therapeutics Inc | Chiral diarylmakrocyklus og anvendelse deraf i behandling af cancer |
| AU2016348549B2 (en) * | 2015-11-02 | 2020-07-23 | Janssen Pharmaceutica Nv | [1,2,4]triazolo[1,5-a]pyrimidin-7-yl compound |
| US10689400B2 (en) | 2016-07-28 | 2020-06-23 | Turning Point Therapeutics, Inc. | Macrocycle kinase inhibitors |
| MX390505B (es) | 2016-11-02 | 2025-03-20 | Janssen Pharmaceutica Nv | Compuestos de [1,2,4]triazolo[1,5-a]pirimidina como inhibidores de pde2 |
| AU2017353315B2 (en) | 2016-11-02 | 2021-09-16 | Janssen Pharmaceutica Nv | (1,2,4)triazolo(1,5-a)pyrimidine compounds as PDE2 inhibitors |
| MY193511A (en) | 2016-11-02 | 2022-10-17 | Janssen Pharmaceutica Nv | [1,2,4]triazolo[1,5-a]pyrimidine derivatives 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 |
| JP7224334B2 (ja) | 2017-07-28 | 2023-02-17 | ターニング・ポイント・セラピューティクス・インコーポレイテッド | 大環式化合物およびその使用 |
| ES2994013T3 (en) | 2017-07-28 | 2025-01-15 | Takeda Pharmaceuticals Co | Tyk2 inhibitors and uses thereof |
| 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 |
| PT3728271T (pt) | 2017-12-19 | 2022-10-06 | Turning Point Therapeutics Inc | Compostos macrocíclicos para tratar doenças |
| 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 |
| EP3856743A4 (en) * | 2018-09-27 | 2022-06-15 | Fochon Pharmaceuticals, Ltd. | SUBSTITUTED IMIDAZO[1,2-A]PYRIDINE AND [1,2,4]TRIAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS |
| US11414431B2 (en) * | 2018-10-15 | 2022-08-16 | Nimbus Lakshmi, Inc. | Substituted pyrazolo[1,5-a]pyrimidines as TYK2 inhibitors |
| CA3175973A1 (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 |
| AU2021259419A1 (en) | 2020-04-21 | 2022-11-10 | Lexicon Pharmaceuticals, Inc. | AAK1 inhibitors for use in treating viral infections |
| US11478733B2 (en) | 2020-11-24 | 2022-10-25 | Caterpillar Inc. | Filter interlock with tabs mating with a pedestal or a housing |
| TW202525819A (zh) * | 2023-09-08 | 2025-07-01 | 加拿大商薩泰洛斯生物科學公司 | Ａｐ２相關激酶１抑制劑及其用途 |
Family Cites Families (16)
| 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 |
| WO2008037477A1 (en) | 2006-09-29 | 2008-04-03 | Novartis Ag | Pyrazolopyrimidines as p13k 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 |
| CN102056927B (zh) * | 2008-05-13 | 2014-06-25 | Irm责任有限公司 | 作为激酶抑制剂的稠合含氮杂环及其组合物 |
| ME03010B (me) * | 2008-10-22 | 2018-10-20 | Array Biopharma Inc | Jedinjenja supstituisanog pirazol0[1,5-]pirimidina као inhibitori trk kinaze |
| 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 |
| US8946237B2 (en) | 2010-01-14 | 2015-02-03 | Merck Sharp & Dohme Corp. | Pyrazolo[1,5-A]pyrimidines as mark inhibitors |
| EP3409278B8 (en) * | 2011-07-21 | 2020-11-04 | Sumitomo Dainippon Pharma Oncology, Inc. | Heterocyclic protein kinase inhibitors |
| BR112014022271B1 (pt) | 2012-03-09 | 2021-09-21 | Lexicon Pharmaceuticals, Inc | Compostos com base em imidazo[1,2-b]piridazina, composições compreendendo-os, e usos dos mesmos |
| DK2822555T3 (en) * | 2012-03-09 | 2018-02-05 | Lexicon Pharmaceuticals Inc | Inhibition of adapter-associated kinase 1 for the treatment of pain |
| US8946415B2 (en) | 2012-03-09 | 2015-02-03 | Lexicon Pharmaceuticals, Inc. | Pyrazolo[1,5-a]pyrimidine-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 |
-
2013
- 2013-03-05 US US13/785,355 patent/US8946415B2/en active Active
- 2013-03-05 EP EP13710250.5A patent/EP2834243B1/en active Active
- 2013-03-05 AU AU2013230128A patent/AU2013230128B2/en active Active
- 2013-03-05 MX MX2014010589A patent/MX345830B/es active IP Right Grant
- 2013-03-05 NZ NZ630721A patent/NZ630721A/en unknown
- 2013-03-05 TR TR2018/08280T patent/TR201808280T4/tr unknown
- 2013-03-05 PL PL13710250T patent/PL2834243T3/pl unknown
- 2013-03-05 WO PCT/US2013/029056 patent/WO2013134228A1/en not_active Ceased
- 2013-03-05 JP JP2014561024A patent/JP6418950B2/ja active Active
- 2013-03-05 MX MX2017002117A patent/MX381849B/es unknown
- 2013-03-05 RU RU2014140735A patent/RU2014140735A/ru not_active Application Discontinuation
- 2013-03-05 HU HUE13710250A patent/HUE038786T2/hu unknown
- 2013-03-05 ES ES13710250.5T patent/ES2676224T3/es active Active
- 2013-03-05 CA CA2866143A patent/CA2866143C/en active Active
- 2013-03-05 BR BR112014022000A patent/BR112014022000A8/pt not_active Application Discontinuation
- 2013-03-05 CN CN201380012483.0A patent/CN104302649B/zh active Active
- 2013-03-05 PT PT137102505T patent/PT2834243T/pt unknown
- 2013-03-05 DK DK13710250.5T patent/DK2834243T3/en active
- 2013-03-05 KR KR1020147028071A patent/KR101965025B1/ko active Active
- 2013-03-05 SG SG11201405561RA patent/SG11201405561RA/en unknown
- 2013-03-05 IN IN7384DEN2014 patent/IN2014DN07384A/en unknown
- 2013-03-08 TW TW102108283A patent/TW201341386A/zh unknown
- 2013-03-11 UY UY0001034668A patent/UY34668A/es not_active Application Discontinuation
- 2013-03-11 AR ARP130100765A patent/AR090292A1/es unknown
-
2014
- 2014-08-21 ZA ZA2014/06149A patent/ZA201406149B/en unknown
- 2014-09-07 IL IL234486A patent/IL234486A/en active IP Right Grant
- 2014-09-11 US US14/483,898 patent/US9403832B2/en active Active
-
2016
- 2016-07-12 US US15/207,677 patent/US20170129896A1/en not_active Abandoned
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