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)
- Hospice & Palliative Care (AREA)
- Rheumatology (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 (forum.php) |
| EP (1) | EP2834243B1 (forum.php) |
| JP (1) | JP6418950B2 (forum.php) |
| KR (1) | KR101965025B1 (forum.php) |
| CN (1) | CN104302649B (forum.php) |
| AR (1) | AR090292A1 (forum.php) |
| AU (1) | AU2013230128B2 (forum.php) |
| BR (1) | BR112014022000A8 (forum.php) |
| CA (1) | CA2866143C (forum.php) |
| DK (1) | DK2834243T3 (forum.php) |
| ES (1) | ES2676224T3 (forum.php) |
| HU (1) | HUE038786T2 (forum.php) |
| IL (1) | IL234486A (forum.php) |
| IN (1) | IN2014DN07384A (forum.php) |
| MX (2) | MX381849B (forum.php) |
| NZ (1) | NZ630721A (forum.php) |
| PL (1) | PL2834243T3 (forum.php) |
| PT (1) | PT2834243T (forum.php) |
| RU (1) | RU2014140735A (forum.php) |
| SG (1) | SG11201405561RA (forum.php) |
| TR (1) | TR201808280T4 (forum.php) |
| TW (1) | TW201341386A (forum.php) |
| UY (1) | UY34668A (forum.php) |
| WO (1) | WO2013134228A1 (forum.php) |
| ZA (1) | ZA201406149B (forum.php) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| EP2834243B1 (en) | 2012-03-09 | 2018-04-25 | Lexicon Pharmaceuticals, Inc. | PYRAZOLO[1,5-a]PYRIMIDINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE |
| US8901305B2 (en) | 2012-07-31 | 2014-12-02 | Bristol-Myers Squibb Company | Aryl lactam kinase inhibitors |
| US9708337B2 (en) | 2013-02-22 | 2017-07-18 | Bristol-Myers Squibb Company | Aryl amide-based kinase inhibitors |
| 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 |
| WO2015054358A1 (en) | 2013-10-11 | 2015-04-16 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| RS65417B1 (sr) | 2014-01-24 | 2024-05-31 | Turning Point Therapeutics Inc | Diaril makrocikli kao modulatori protein kinaza |
| JP6441947B2 (ja) * | 2014-01-31 | 2018-12-19 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | キノリンを基にしたキナーゼ阻害剤 |
| 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 |
| EP3200797A1 (en) * | 2014-09-30 | 2017-08-09 | Bristol-Myers Squibb Company | Quinazoline-based kinase inhibitors |
| JP6609631B2 (ja) * | 2014-12-15 | 2019-11-20 | シーエムジー ファーマシューティカル カンパニー,リミテッド | 縮合環ヘテロアリール化合物及びtrk抑制剤としての用途 |
| WO2016164295A2 (en) | 2015-04-10 | 2016-10-13 | Bristol-Myers Squibb Company | Fused pyridines as kinase inhibitors |
| ES2864839T3 (es) | 2015-07-02 | 2021-10-14 | Turning Point Therapeutics Inc | Macrociclos de diarilo quirales como moduladores de proteína quinasas |
| MX386680B (es) | 2015-07-06 | 2025-03-19 | Turning Point Therapeutics Inc | Polimorfo de macrociclo de diarilo. |
| HUE070316T2 (hu) | 2015-07-21 | 2025-05-28 | Turning Point Therapeutics Inc | Királis diaril makrociklus és annak felhasználása rák kezelésében |
| 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 |
| WO2018022911A1 (en) | 2016-07-28 | 2018-02-01 | Tp Therapeutics, Inc. | Macrocycle kinase inhibitors |
| JP7018944B2 (ja) | 2016-11-02 | 2022-02-14 | ヤンセン ファーマシューティカ エヌ.ベー. | PDE2阻害剤としての[1,2,4]トリアゾロ[1,5-a]ピリミジン化合物 |
| SG11201903892UA (en) * | 2016-11-02 | 2019-05-30 | Janssen Pharmaceutica Nv | [1,2,4]triazolo[1,5-a]pyrimidine derivatives as pde2 inhibitors |
| EA039102B1 (ru) | 2016-11-02 | 2021-12-03 | Янссен Фармацевтика Нв | Соединения [1,2,4]триазоло[1,5-a]пиримидина в качестве ингибиторов 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 |
| SI3658148T1 (sl) | 2017-07-28 | 2024-10-30 | Turning Point Therapeutics, Inc. | Makrociklične spojine in njihova uporaba |
| EP4438117A3 (en) | 2017-07-28 | 2024-12-18 | Takeda Pharmaceutical Company Limited | Tyk2 inhibitors and uses thereof |
| AU2018383571B2 (en) * | 2017-12-15 | 2023-09-21 | 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 |
| PE20200937A1 (es) | 2017-12-19 | 2020-09-17 | Turning Point Therapeutics Inc | Compuestos macrociclicos para tratar enfermedades |
| JP7150356B2 (ja) * | 2017-12-22 | 2022-10-11 | 深▲チェン▼市塔吉瑞生物医薬有限公司 | 置換ピラゾロ[1,5-a]ピリミジン化合物並びにその医薬組成物および使用 |
| US11345703B2 (en) | 2018-01-23 | 2022-05-31 | Shenzhen Targetrx, Inc. | Substituted pyrazolo[1,5-a]pyrimidine macrocyclic compound |
| WO2020063751A1 (en) * | 2018-09-27 | 2020-04-02 | Fochon Pharmaceuticals, Ltd. | Substituted imidazo [1, 2-a] pyridine and [1, 2, 4] triazolo [1, 5-a] pyridine compounds as ret kinase inhibitors |
| CA3115088A1 (en) * | 2018-10-15 | 2020-04-23 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
| 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 |
| CN115484951A (zh) | 2020-04-21 | 2022-12-16 | 莱西肯医药有限公司 | 用于治疗病毒感染的aak1抑制剂 |
| 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 |
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 |
| AU2515992A (en) | 1991-08-20 | 1993-03-16 | 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 |
| JP2010504933A (ja) | 2006-09-29 | 2010-02-18 | ノバルティス アーゲー | Pi3k脂質キナーゼ阻害剤としてのピラゾロピリミジン |
| 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 |
| CN102264736B (zh) * | 2008-10-22 | 2013-08-14 | 阵列生物制药公司 | 作为TRK激酶抑制剂的取代的吡唑并[1,5-a]嘧啶化合物 |
| AR077468A1 (es) * | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| TW201113286A (en) | 2009-09-03 | 2011-04-16 | 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 |
| US9416132B2 (en) * | 2011-07-21 | 2016-08-16 | Tolero Pharmaceuticals, Inc. | Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors |
| 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 |
| EP2834243B1 (en) | 2012-03-09 | 2018-04-25 | 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 |
| 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 EP EP13710250.5A patent/EP2834243B1/en active Active
- 2013-03-05 JP JP2014561024A patent/JP6418950B2/ja active Active
- 2013-03-05 IN IN7384DEN2014 patent/IN2014DN07384A/en unknown
- 2013-03-05 AU AU2013230128A patent/AU2013230128B2/en active Active
- 2013-03-05 PT PT137102505T patent/PT2834243T/pt unknown
- 2013-03-05 US US13/785,355 patent/US8946415B2/en active Active
- 2013-03-05 SG SG11201405561RA patent/SG11201405561RA/en unknown
- 2013-03-05 HU HUE13710250A patent/HUE038786T2/hu unknown
- 2013-03-05 CN CN201380012483.0A patent/CN104302649B/zh active Active
- 2013-03-05 BR BR112014022000A patent/BR112014022000A8/pt not_active Application Discontinuation
- 2013-03-05 MX MX2017002117A patent/MX381849B/es unknown
- 2013-03-05 ES ES13710250.5T patent/ES2676224T3/es active Active
- 2013-03-05 TR TR2018/08280T patent/TR201808280T4/tr unknown
- 2013-03-05 WO PCT/US2013/029056 patent/WO2013134228A1/en not_active Ceased
- 2013-03-05 MX MX2014010589A patent/MX345830B/es active IP Right Grant
- 2013-03-05 RU RU2014140735A patent/RU2014140735A/ru not_active Application Discontinuation
- 2013-03-05 CA CA2866143A patent/CA2866143C/en active Active
- 2013-03-05 NZ NZ630721A patent/NZ630721A/en unknown
- 2013-03-05 KR KR1020147028071A patent/KR101965025B1/ko active Active
- 2013-03-05 DK DK13710250.5T patent/DK2834243T3/en active
- 2013-03-05 PL PL13710250T patent/PL2834243T3/pl 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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