AR097543A1 - COMPUESTOS BASADOS EN IMIDAZO[1,2-b]PIRIDAZINA, COMPOSICIONES QUE LOS COMPRENDEN Y SUS MÉTODOS DE USO - Google Patents
COMPUESTOS BASADOS EN IMIDAZO[1,2-b]PIRIDAZINA, COMPOSICIONES QUE LOS COMPRENDEN Y SUS MÉTODOS DE USOInfo
- Publication number
- AR097543A1 AR097543A1 ARP140103295A ARP140103295A AR097543A1 AR 097543 A1 AR097543 A1 AR 097543A1 AR P140103295 A ARP140103295 A AR P140103295A AR P140103295 A ARP140103295 A AR P140103295A AR 097543 A1 AR097543 A1 AR 097543A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- halo
- cyano
- or1c
- hydrocarbyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 2
- 239000000203 mixture Substances 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 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 4
- 102100038079 AP2-associated protein kinase 1 Human genes 0.000 abstract 2
- 101000742699 Homo sapiens AP2-associated protein kinase 1 Proteins 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
Classifications
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Reivindicación 1: Un método para inhibir la actividad de la quinasa asociada al adaptador 1 (AAK1), caracterizado porque comprende poner en contacto AAK1 con un compuesto de la fórmula (1) o una de sus sales farmacéuticamente aceptables, donde: R¹ es R¹A, hidrocarbilo C₁₋₁₂ opcionalmente sustituido o heterocarbilo de 2 - 12 miembros opcionalmente sustituido, en donde dicha sustitución opcional es con uno o más R¹A; cada R¹A es, de manera independiente, -OR¹C, -N(R¹C)₂, -C(O)R¹C, -C(O)OR¹C, -C(O)N(R¹C)₂, -N(R¹C)C(O)OR¹C, ciano, halo, hidrocarbilo C₁₋₁₂ opcionalmente sustituido o heterocarbilo de 2 - 12 miembros opcionalmente sustituido, en donde dicha sustitución opcional es con uno o más R¹B; cada R¹B es, de manera independiente, -OR¹C, -N(R¹C)₂, -C(O)R¹C, -C(O)OR¹C, -C(O)N(R¹C)₂, -N(R¹C)C(O)OR¹C, ciano o halo; cada R¹C es, de manera independiente, hidrógeno, hidrocarbilo C₁₋₁₂ opcionalmente sustituido o heterocarbilo de 2 - 12, miembros opcionalmente sustituido, en donde dicha sustitución opcional es con uno o más de ciano, halo o hidroxilo; R² es hidrocarbilo C₁₋₁₂ opcionalmente sustituido o heterocarbilo de 2 - 12 miembros opcionalmente sustituido, unido a C₅ en uno de sus átomos de carbono, en donde dicha sustitución opcional es con uno o más R²C; cada R²C es, de manera independiente, -OR²D, -N(R²D)₂, -C(O)R²D, -C(O)OR²D, -C(O)N(R²D)₂, -N(R²D)C(O)OR²D, ciano, halo o hidrocarbilo C₁₋₁₂ opcionalmente sustituido o heterocarbilo de 2 - 12 miembros opcionalmente sustituido, en donde dicha sustitución opcional es con uno o más amino, ciano, halo, hidroxilo o R²D; cada R²D es, de manera independiente, hidrógeno, hidrocarbilo C₁₋₁₂ opcionalmente sustituido heterocarbilo de 2 - 12 miembros opcionalmente sustituido, en donde dicha sustitución opcional es con uno o más amino, ciano, halo o hidroxilo; y R³ es hidrógeno o alquilo C₁₋₆; opcionalmente sustituido con uno o más ciano, halo o hidroxilo. Reivindicación 27: Un compuesto de la fórmula (2) o una de sus sales farmacéuticamente aceptables, donde: A es hidrocarbilo C₁₋₁₂ cíclico o heterociclo de 4 - 7 miembros; D es hidrocarbilo C₁₋₁₂ cíclico o heterociclo de 4 - 7 miembros unido al C₅ en uno de sus átomos de carbono; cada R¹A es, de manera independiente, -OR¹C-, -N(R¹C)₂, -C(O)R¹C, -C(O)OR¹C, -C(O)N(R¹C)₂, -N(R¹C)C(O)OR¹C, ciano, halo, hidrocarbilo C₁₋₁₂ opcionalmente sustituido o heterocarbilo de 2 - 12 miembros opcionalmente sustituido, en donde dicha sustitución opcional es con uno o más R¹B; cada R¹B es, de manera independiente, -OR¹C, -N(R¹C)₂, -C(O)R¹C, -C(O)OR¹C, -C(O)N(R¹C)₂, -N(R¹C)C(O)OR¹C, ciano o halo; cada R¹C es, de manera independiente, hidrógeno, hidrocarbilo C₁₋₁₂ opcionalmente sustituido o heterocarbilo de 2 - 12 miembros opcionalmente sustituido, en donde dicha sustitución opcional es con uno o más de ciano, halo o hidroxilo; cada R²C es, de manera independiente, -OR²D, -N(R²D)₂, -C(O)R²D, -C(O)OR²D, - C(O)N(R²D)₂, -N(R²D)C(O)OR²D, ciano, halo, hidrocarbilo C₁₋₁₂ opcionalmente sustituido o heterocarbilo de 2 - 12 miembros opcionalmente sustituido, en donde dicha sustitución opcional es con uno o más de amino, ciano, halo, hidroxilo o R²D; cada R²D es, de manera independiente, hidrógeno, hidrocarbilo C₁₋₁₂ opcionalmente sustituido o heterocarbilo de 2 - 12 miembros opcionalmente sustituido, en donde dicha sustitución opcional es con uno o más de amino, ciano, halo o hidroxilo; n es 1 - 3; y m es 0 - 3.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361874398P | 2013-09-06 | 2013-09-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR097543A1 true AR097543A1 (es) | 2016-03-23 |
Family
ID=52628957
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP140103295A AR097543A1 (es) | 2013-09-06 | 2014-09-03 | COMPUESTOS BASADOS EN IMIDAZO[1,2-b]PIRIDAZINA, COMPOSICIONES QUE LOS COMPRENDEN Y SUS MÉTODOS DE USO |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20150183791A1 (es) |
| EP (1) | EP3041473A1 (es) |
| JP (1) | JP2016529319A (es) |
| CN (1) | CN105517552A (es) |
| AR (1) | AR097543A1 (es) |
| AU (1) | AU2014315075A1 (es) |
| CA (1) | CA2923420A1 (es) |
| HK (1) | HK1217659A1 (es) |
| TW (1) | TW201542552A (es) |
| WO (1) | WO2015035167A1 (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| AU2015342883B2 (en) | 2014-11-06 | 2020-07-02 | Bial - R&D Investments, S.A. | Substituted pyrrolo(1,2-a)pyrimidines and their use in the treatment of medical disorders |
| WO2016073889A1 (en) | 2014-11-06 | 2016-05-12 | Lysosomal Therapeutics Inc. | Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders |
| IL252053B2 (en) | 2014-11-06 | 2024-04-01 | Lysosomal Therapeutics Inc | SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINES AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS |
| US11124516B2 (en) | 2016-04-06 | 2021-09-21 | BIAL-BioTech Investments, Inc. | Pyrrolo[1,2-A]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| KR20180133461A (ko) | 2016-04-06 | 2018-12-14 | 리소소말 테라퓨틱스 인크. | 피라졸로[1,5-a]피리미디닐 카르복스아미드 화합물 및 의학적 장애의 치료에서의 그의 용도 |
| CA3020305A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics Inc. | Imidazo [1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| MX389579B (es) | 2016-05-05 | 2025-03-20 | Bial R&D Invest S A | IMIDAZO[1,2-b]PIRIDAZINAS SUSTITUIDAS, IMIDAZO[1,5-b]PIRIDAZINAS SUSTITUIDAS, COMPUESTOS RELACIONADOS Y SU USO EN EL TRATAMIENTO DE TRASTORNOS MÉDICOS |
| US11345698B2 (en) | 2016-05-05 | 2022-05-31 | Bial—R&D Investments, S.A. | Substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-a]pyrazines, related compounds, and their use in the treatment of medical disorders |
| WO2018013430A2 (en) | 2016-07-12 | 2018-01-18 | Arisan Therapeutics Inc. | Heterocyclic compounds for the treatment of arenavirus infection |
| ES2966825T3 (es) * | 2017-08-15 | 2024-04-24 | Agios Pharmaceuticals Inc | Activadores de piruvato quinasa para su uso en el tratamiento de trastornos sanguíneos |
| CA3118093A1 (en) * | 2018-09-28 | 2020-04-02 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Small molecule inhibitors of dyrk1/clk and uses thereof |
| US12419865B2 (en) | 2018-12-06 | 2025-09-23 | Arisan Therapeutics Inc. | Compounds for the treatment of arenavirus infection |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100973609B1 (ko) * | 2005-03-23 | 2010-08-03 | 에프. 호프만-라 로슈 아게 | ｍＧｌｕＲ2 길항제로서 아세틸렌일-피라졸로-피리미딘유도체 |
| US20070078136A1 (en) * | 2005-09-22 | 2007-04-05 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as kinase modulators |
| US20110021513A1 (en) * | 2006-09-07 | 2011-01-27 | Biogen Idec Ma Inc. | Modulators of interleukin-1 receptor-associated kinase |
| MX2009004700A (es) * | 2006-11-06 | 2009-05-15 | Supergen Inc | Derivados de imidazo[1,2-b]piridazin y pirazolo[1,5-a] pirimidina y su uso como inhibidores de proteina cinasa. |
| 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 |
| AR067326A1 (es) * | 2007-05-11 | 2009-10-07 | Novartis Ag | Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido |
| AU2009218459A1 (en) * | 2008-02-28 | 2009-09-03 | Novartis Ag | Imidazo [1,2-B] pyridazine derivatives for the treatment of C-Met tyrosine kinase mediated disease |
| AU2009246687B2 (en) * | 2008-05-13 | 2012-08-09 | Irm Llc | Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors |
| TWI491610B (zh) * | 2008-10-09 | 2015-07-11 | 必治妥美雅史谷比公司 | 作為激酶抑制劑之咪唑并嗒腈 |
| BR112012010041A2 (pt) * | 2009-10-30 | 2016-05-24 | Janssen Pharmaceutica Nv | derivados de imidazo [1,2-b] piridazina e seu uso como inibidores de pde10 |
| AU2012257513B2 (en) * | 2011-05-19 | 2017-05-11 | Fundación Del Sector Público Estatal Centro Nacional De Investigaciones Oncológicas Carlos III (F.S.P. CNIO) | Macrocyclic compounds as protein kinase inhibitors |
| SI2766359T1 (sl) * | 2011-10-14 | 2016-09-30 | Ambit Biosciences Corporation | Heterociklične spojine in njihova uporaba kot modulatorjev receptorja tirozin kinaze tipa III |
| CA2852937A1 (en) * | 2011-10-20 | 2013-04-25 | Glaxosmithkline Llc | Substituted bicyclic aza-heterocycles and analogues as sirtuin modulators |
| DK2822555T3 (en) * | 2012-03-09 | 2018-02-05 | Lexicon Pharmaceuticals Inc | Inhibition of adapter-associated kinase 1 for the treatment of pain |
| NZ630719A (en) * | 2012-03-09 | 2017-01-27 | Lexicon Pharmaceuticals Inc | Imidazo [1, 2 - b] pyridazine - based compounds, compositions comprising them, and uses thereof |
| GB201205669D0 (en) * | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
| WO2014138692A1 (en) * | 2013-03-07 | 2014-09-12 | Califia Bio, Inc. | Mixed lineage kinase inhibitors and method of treatments |
| WO2014160183A1 (en) * | 2013-03-13 | 2014-10-02 | The United States Of America,As Represented By The Secretary,Department Of Health And Human Services | Methods for modulating chemotherapeutic cytotoxicity |
-
2014
- 2014-09-03 AR ARP140103295A patent/AR097543A1/es unknown
- 2014-09-05 TW TW103130825A patent/TW201542552A/zh unknown
- 2014-09-05 CA CA2923420A patent/CA2923420A1/en not_active Abandoned
- 2014-09-05 EP EP14766638.2A patent/EP3041473A1/en not_active Withdrawn
- 2014-09-05 JP JP2016540422A patent/JP2016529319A/ja active Pending
- 2014-09-05 AU AU2014315075A patent/AU2014315075A1/en not_active Abandoned
- 2014-09-05 CN CN201480049295.XA patent/CN105517552A/zh active Pending
- 2014-09-05 WO PCT/US2014/054298 patent/WO2015035167A1/en not_active Ceased
- 2014-09-05 US US14/478,479 patent/US20150183791A1/en not_active Abandoned
- 2014-09-05 HK HK16105789.6A patent/HK1217659A1/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2014315075A1 (en) | 2016-03-10 |
| CN105517552A (zh) | 2016-04-20 |
| EP3041473A1 (en) | 2016-07-13 |
| US20150183791A1 (en) | 2015-07-02 |
| JP2016529319A (ja) | 2016-09-23 |
| TW201542552A (zh) | 2015-11-16 |
| HK1217659A1 (zh) | 2017-01-20 |
| CA2923420A1 (en) | 2015-03-12 |
| WO2015035167A1 (en) | 2015-03-12 |
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