AR110026A1 - Inhibidores de pde2 - Google Patents
Inhibidores de pde2Info
- Publication number
- AR110026A1 AR110026A1 ARP170103037A ARP170103037A AR110026A1 AR 110026 A1 AR110026 A1 AR 110026A1 AR P170103037 A ARP170103037 A AR P170103037A AR P170103037 A ARP170103037 A AR P170103037A AR 110026 A1 AR110026 A1 AR 110026A1
- Authority
- AR
- Argentina
- Prior art keywords
- independently selected
- optionally substituted
- group
- alkyl
- halo
- Prior art date
Links
- 229940121828 Phosphodiesterase 2 inhibitor Drugs 0.000 title 1
- -1 pyrimidin-yl Chemical group 0.000 abstract 18
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 9
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 6
- 125000001475 halogen functional group Chemical group 0.000 abstract 4
- 125000004076 pyridyl group Chemical group 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 101001098814 Dictyostelium discoideum 3',5'-cyclic-nucleotide phosphodiesterase regA Proteins 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 125000005871 1,3-benzodioxolyl group Chemical group 0.000 abstract 1
- 125000000355 1,3-benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 abstract 1
- KEQTWHPMSVAFDA-UHFFFAOYSA-N 2,3-dihydro-1h-pyrazole Chemical compound C1NNC=C1 KEQTWHPMSVAFDA-UHFFFAOYSA-N 0.000 abstract 1
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 abstract 1
- 125000000850 2H-chromenyl group Chemical group O1C(C=CC2=CC=CC=C12)* 0.000 abstract 1
- NSPMIYGKQJPBQR-UHFFFAOYSA-N 4H-1,2,4-triazole Chemical compound C=1N=CNN=1 NSPMIYGKQJPBQR-UHFFFAOYSA-N 0.000 abstract 1
- 125000004608 5,6,7,8-tetrahydroquinolinyl group Chemical group N1=C(C=CC=2CCCCC12)* 0.000 abstract 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 abstract 1
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical compound F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 abstract 1
- 108010081348 HRT1 protein Hairy Proteins 0.000 abstract 1
- 102100021881 Hairy/enhancer-of-split related with YRPW motif protein 1 Human genes 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 1
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 125000002541 furyl group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 abstract 1
- 125000001041 indolyl group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 abstract 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 abstract 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 230000000926 neurological effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 1
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 1
- 125000002098 pyridazinyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 abstract 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 abstract 1
- 150000003254 radicals Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
- 125000001544 thienyl group Chemical group 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
- A61K31/505—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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/34—Tobacco-abuse
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
-
- 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
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Derivados [1,2,4]triazol[1,5-a]pirimidin-ilo como inhibidores de la fosfodiesterasa 2 (PDE2). También está dirigida a composiciones farmacéuticas que comprenden los compuestos, a procesos para preparar dichas composiciones, y al uso de dichos compuestos y composiciones en la prevención y el tratamiento de trastornos en los cuales está involucrada la PDE2, tales como trastornos neurológicos y psiquiátricos. Reivindicación 1: Un compuesto de la fórmula (1), o una forma estereoisomérica del mismo, en la que RA se selecciona del grupo que consiste en H, CH₃, CN y CHF₂; RB es un radical seleccionado del grupo que consiste en los compuestos de fórmula (2), (3) y (4), donde R¹ es H, F o CH₃; R² es H o C₁₋₄ alquilo, en particular metilo o n-butilo; siempre que cuando R² es H, entonces R¹ es F o CH₃; R³ es Ar, Het o Ar-C₂₋₄ alquenilo; en donde Ar representa fenilo o naftilo, cada uno sustituido opcionalmente con 1, 2 ó 3 sustituyentes, cada uno seleccionado de manera independiente del grupo que consiste en halo; CN; NR²AR²B en donde R²A y R²B se seleccionan cada uno de manera independiente entre H y CH₃; OH; C₁₋₆ alquilo sustituido opcionalmente con 1, 2 ó 3 sustituyentes halo seleccionados de manera independiente; C₁₋₆ alquilo sustituido con CN; C₃₋₆ cicloalquilo; C₁₋₆ alquiloxi sustituido opcionalmente con 1, 2 ó 3 sustituyentes halo seleccionados de manera independiente; y pirazolilo; Het representa (i) un heteroarilo de 5 miembros seleccionado del grupo que consiste en 1H-pirrolilo; tienilo; furanilo; 1H-pirazolilo; 1H-imidazolilo; 1,2-oxazolilo; 1,3-oxazolilo; y tiazolilo; cada uno de los cuales se puede sustituir opcionalmente con 1, 2 ó 3 sustituyentes cada uno seleccionado de manera independiente del grupo que consiste en halo; C₁₋₄ alquilo sustituido opcionalmente con 1, 2 ó 3 sustituyentes halo seleccionados de manera independiente; NR³AR³B en donde R³A y R³B se seleccionan cada uno de manera independiente entre H y CH₃; y furan-2-ilo; o (ii) un heteroarilo de 6 miembros seleccionado del grupo que consiste en piridilo, pirimidinilo, pirazinilo y piridazinilo; cada uno de los cuales se puede sustituir opcionalmente con 1, 2 ó 3 sustituyentes cada uno seleccionado de manera independiente del grupo que consiste en halo; OH; CN; NR⁴AR⁴B en donde R⁴A y R⁴B se seleccionan cada uno de manera independiente entre H y CH₃; C₁₋₄ alquilo sustituido opcionalmente con 1, 2 ó 3 sustituyentes halo seleccionados de manera independiente; C₁₋₄ alquilo sustituido con OH; C₃₋₆ cicloalquilo; C₃₋₆ cicloalquiloxi; C₁₋₄ alquiloxi sustituido opcionalmente con 1, 2 ó 3 sustituyentes halo seleccionados de manera independiente; y C₁₋₄ alquiloxi-C₁₋₄ alquilo; o (iii) un heterociclilo parcialmente insaturado bicíclico de 8 a 10 miembros seleccionado del grupo que consiste en 2,3-dihidro-1-benzofuranilo; 2H-cromenilo; 3,4-dihidro-2H-cromenilo; 2,3-dihidro-1H-indolilo opcionalmente sustituido en la posición 1 con C₁₋₄ alquilo, metilsulfonilo, 1-acetilo o fluoroacetilo; 2,2-difluoro-1,3-benzodioxolilo; 1,3-benzodioxolilo opcionalmente sustituido con un sustituyente metilo; 3,4-dihidro-2H-1,4-benzoxazinilo opcionalmente sustituido con C₁₋₄ alquilo; 5,6,7,8-tetrahidroimidazol[1,2-a]piridinilo; 5,6,7,8-tetrahidroquinolinilo opcionalmente sustituido con un sustituyente halo; y 2,3-dihidropirazol[5,1-b][1,3]oxazolilo; o (iv) un heteroarilo bicíclico de 9 a 10 miembros seleccionado del grupo que consiste en 1-benzofuranilo; 1-benzotiofenilo; 1H-indolilo; 1,3-benzoxazolilo; 1,3-benzotiazolilo; indolizinilo; 1H-bencimidazolilo; imidazo[1,2-a]piridinilo; pirazol[1,5-a]piridinilo; 1H-tieno[2,3-c]pirazolilo; imidazo[2,1-b]tiazolilo; pirrol[2,3-c]piridinilo; tieno[3,2-b]piridinilo; quinolinilo; isoquinolinilo; quinoxalinilo; 1,8-naftiridinilo; y 1,6-naftiridinilo; cada uno de los cuales se puede sustituir opcionalmente con 1 ó 2 sustituyentes cada uno seleccionado de manera independiente del grupo que consiste en halo; OH; NR⁵AR⁵B en donde R⁵A y R⁵B se seleccionan cada uno de manera independiente entre H y CH₃; C₁₋₄ alquilo sustituido opcionalmente cono 1, 2 ó 3 sustituyentes halo seleccionados de manera independiente; y C₁₋₄ alquiloxi sustituido opcionalmente con 1, 2 ó 3 sustituyentes halo seleccionados de manera independiente; siempre que el compuesto no sea un compuesto de la fórmula (5); o un N-óxido, o una sal farmacéuticamente aceptable o un solvato del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16196924 | 2016-11-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR110026A1 true AR110026A1 (es) | 2019-02-13 |
Family
ID=57240919
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP170103037A AR110026A1 (es) | 2016-11-02 | 2017-11-02 | Inhibidores de pde2 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US10947242B2 (es) |
| EP (1) | EP3535267B1 (es) |
| JP (1) | JP7076441B2 (es) |
| KR (1) | KR20190070972A (es) |
| CN (1) | CN109923116B (es) |
| AR (1) | AR110026A1 (es) |
| AU (1) | AU2017353310B2 (es) |
| BR (1) | BR112019008404A2 (es) |
| CA (1) | CA3041412A1 (es) |
| EA (1) | EA039788B1 (es) |
| ES (1) | ES2864131T3 (es) |
| IL (1) | IL266305B (es) |
| MX (1) | MX385576B (es) |
| MY (1) | MY193511A (es) |
| SG (1) | SG11201903892UA (es) |
| TW (1) | TWI764950B (es) |
| UA (1) | UA125302C2 (es) |
| WO (1) | WO2018083098A1 (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20180075630A (ko) | 2015-11-02 | 2018-07-04 | 얀센 파마슈티카 엔.브이. | [1,2,4]트리아졸로[1,5-a]피리미딘-7-일 화합물 |
| 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 |
| CN109890824B (zh) | 2016-11-02 | 2022-05-24 | 詹森药业有限公司 | 作为pde2抑制剂的[1,2,4]三唑并[1,5-a]嘧啶化合物 |
| US10947242B2 (en) | 2016-11-02 | 2021-03-16 | Janssen Pharmaceutica, Nv | [1,2,4]triazolo[1,5and#8208;A]pyrimidine compounds as PDE2 inhibitors |
| CN112839648B (zh) | 2018-06-07 | 2025-04-04 | 达萨玛治疗公司 | Sarm1抑制剂 |
| US11098056B2 (en) * | 2018-10-01 | 2021-08-24 | Genzyme Corporation | UDP glycosyltransferase inhibitors and methods of use |
| EP3897670A4 (en) | 2018-12-19 | 2022-09-07 | Disarm Therapeutics, Inc. | MRSA1 INHIBITORS IN COMBINATION WITH NEUROPROTECTIVE AGENTS |
| WO2021257857A1 (en) | 2020-06-19 | 2021-12-23 | Incyte Corporation | Naphthyridinone compounds as jak2 v617f inhibitors |
| US11753413B2 (en) | 2020-06-19 | 2023-09-12 | Incyte Corporation | Substituted pyrrolo[2,1-f][1,2,4]triazine compounds as JAK2 V617F inhibitors |
| AU2021300429A1 (en) | 2020-07-02 | 2023-02-16 | Incyte Corporation | Tricyclic urea compounds as JAK2 V617F inhibitors |
| WO2022006456A1 (en) | 2020-07-02 | 2022-01-06 | Incyte Corporation | Tricyclic pyridone compounds as jak2 v617f inhibitors |
| WO2022046989A1 (en) | 2020-08-27 | 2022-03-03 | Incyte Corporation | Tricyclic urea compounds as jak2 v617f inhibitors |
| WO2022140231A1 (en) | 2020-12-21 | 2022-06-30 | Incyte Corporation | Deazaguaine compounds as jak2 v617f inhibitors |
| WO2022182839A1 (en) | 2021-02-25 | 2022-09-01 | Incyte Corporation | Spirocyclic lactams as jak2 v617f inhibitors |
| CN119173514A (zh) | 2022-03-17 | 2024-12-20 | 因赛特公司 | 作为jak2 v617f抑制剂的三环脲化合物 |
Family Cites Families (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1993000313A2 (en) | 1991-06-27 | 1993-01-07 | Virginia Commonwealth University | Sigma receptor ligands and the use thereof |
| BR9907300A (pt) | 1998-01-27 | 2000-10-24 | Aventis Pharm Prod Inc | Inibidores do fator xa oxoaza-heterociclila substituìdos |
| US6194410B1 (en) | 1998-03-11 | 2001-02-27 | Hoffman-La Roche Inc. | Pyrazolopyrimidine and pyrazolines and process for preparation thereof |
| US20040014744A1 (en) | 2002-04-05 | 2004-01-22 | Fortuna Haviv | Substituted pyridines having antiangiogenic activity |
| ES2324293T3 (es) | 2002-10-03 | 2009-08-04 | Vertex Pharmaceuticals Incorporated | Derivados de piperacina y piperidina para el tratamiento de enfermedades neurologicas. |
| US20070275961A1 (en) | 2003-06-04 | 2007-11-29 | Vernalis (Cambridge) Limited. | Triazolo ' 1, 5-A ! Pyrimidines and Their Use in Medicine |
| ATE413404T1 (de) | 2003-07-16 | 2008-11-15 | Janssen Pharmaceutica Nv | Triazolopyrimidin derivate als inhibitoren von glycogen synthase kinase-3 |
| NZ548128A (en) | 2003-12-29 | 2010-05-28 | Banyu Pharma Co Ltd | Novel 2-heteroaryl-substituted benzimidazole derivative |
| CA2580845A1 (en) | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Pyridazine derivatives for inhibiting human stearoyl-coa-desaturase |
| CA2580855A1 (en) | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
| ATE479687T1 (de) | 2004-10-15 | 2010-09-15 | Takeda Pharmaceutical | Kinaseinhibitoren |
| US7507842B2 (en) | 2005-08-12 | 2009-03-24 | Radiorx, Inc. | Cyclic nitro compounds, pharmaceutical compositions thereof and uses thereof |
| WO2007113136A1 (de) | 2006-03-30 | 2007-10-11 | Basf Aktiengesellschaft | Verwendung von substituierten riazolopyrimidinen zur bekämpfung von phyto pathogenen schadpilzen |
| JP2007332061A (ja) | 2006-06-14 | 2007-12-27 | Nippon Kayaku Co Ltd | 新規ピラゾロ［１，５−ａ］ピリミジン誘導体及びその用途 |
| US8153803B2 (en) | 2006-07-18 | 2012-04-10 | The General Hospital Corporation | Compositions and methods for modulating sirtuin activity |
| US7928103B2 (en) | 2006-10-17 | 2011-04-19 | Boehringer Ingelheim International Gmbh | Compounds which modulate the CB2 receptor |
| US8138168B1 (en) | 2007-09-26 | 2012-03-20 | Takeda Pharmaceutical Company Limited | Renin inhibitors |
| GB0719803D0 (en) | 2007-10-10 | 2007-11-21 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| TWI481607B (zh) * | 2009-12-17 | 2015-04-21 | Lundbeck & Co As H | 作為ｐｄｅ１０ａ酵素抑制劑的２－芳基咪唑衍生物 |
| CA2818903C (en) * | 2010-12-14 | 2021-03-23 | Electrophoretics Limited | 5-(1,3-benzoxazol-2-yl)-4-(pyridin-4-yl)pyrimidin-2-amine and its use as a casein kinase 1delta inhibitor |
| UA106692C2 (uk) | 2011-02-23 | 2014-09-25 | Пфайзер Інк. | ІМІДАЗО[5,1-f][1,2,4]ТРИАЗИНИ ДЛЯ ЛІКУВАННЯ НЕВРОЛОГІЧНИХ РОЗЛАДІВ |
| US10604523B2 (en) | 2011-06-27 | 2020-03-31 | Janssen Pharmaceutica Nv | 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline derivatives |
| EP2758375A1 (en) | 2011-09-23 | 2014-07-30 | Advinus Therapeutics Limited | Amide compounds, compositions and applications thereof |
| US9034882B2 (en) | 2012-03-05 | 2015-05-19 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
| 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 |
| AU2015223049B2 (en) | 2014-02-27 | 2019-03-21 | Merck Patent Gmbh | Heterocyclic compounds as NaV channel inhibitors and uses thereof |
| JP6416275B2 (ja) | 2014-03-19 | 2018-10-31 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ヘテロアリールｓｙｋ阻害剤 |
| CN106459062A (zh) * | 2014-04-23 | 2017-02-22 | 达特神经科学(开曼)有限公司 | 作为PDE2抑制剂的取代的[1,2,4]三唑并[1,5‑a]嘧啶‑7‑基化合物 |
| CN106232118A (zh) * | 2014-04-25 | 2016-12-14 | 辉瑞大药厂 | 杂芳族化合物及其作为多巴胺d1配体的用途 |
| CN105566321B (zh) | 2014-10-29 | 2020-04-21 | 广东东阳光药业有限公司 | 杂芳化合物及其在药物中的应用 |
| TWI568737B (zh) | 2014-11-05 | 2017-02-01 | 達特神經科學（開曼）有限責任公司 | 作為ｐｄｅ２抑制劑之經取代的５－甲基－［１，２，４］三唑并［１，５－ａ］嘧啶－２－胺化合物 |
| TWI530688B (zh) * | 2014-11-18 | 2016-04-21 | 彭顯智 | 製備微奈米探針設備及方法 |
| WO2016107602A1 (zh) | 2015-01-01 | 2016-07-07 | 成都贝斯凯瑞生物科技有限公司 | 一类取代氮杂环衍生物及其应用 |
| WO2016145614A1 (en) | 2015-03-17 | 2016-09-22 | Merck Sharp & Dohme Corp. | Triazolyl pyrimidinone compounds as pde2 inhibitors |
| WO2017000277A1 (en) | 2015-07-01 | 2017-01-05 | Merck Sharp & Dohme Corp. | Substituted triazolo bicycliccompounds as pde2 inhibitors |
| WO2017000276A1 (en) | 2015-07-01 | 2017-01-05 | Merck Sharp & Dohme Corp. | Bicyclic heterocyclic compounds as pde2 inhibitors |
| US20180305334A1 (en) | 2015-10-14 | 2018-10-25 | Aquinnah Pharmaceuticals, Inc. | Compounds, compositions and methods of use against stress granules |
| KR20180075630A (ko) | 2015-11-02 | 2018-07-04 | 얀센 파마슈티카 엔.브이. | [1,2,4]트리아졸로[1,5-a]피리미딘-7-일 화합물 |
| CN105898377A (zh) | 2015-12-11 | 2016-08-24 | 乐视网信息技术（北京）股份有限公司 | 用户终端、服务器及弹幕加载方法、系统 |
| WO2017157882A1 (en) | 2016-03-14 | 2017-09-21 | Université Catholique de Louvain | Serine biosynthetic pathway inhibitors |
| CN109890824B (zh) | 2016-11-02 | 2022-05-24 | 詹森药业有限公司 | 作为pde2抑制剂的[1,2,4]三唑并[1,5-a]嘧啶化合物 |
| 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 |
| US10947242B2 (en) | 2016-11-02 | 2021-03-16 | Janssen Pharmaceutica, Nv | [1,2,4]triazolo[1,5and#8208;A]pyrimidine compounds as PDE2 inhibitors |
| CA3044762A1 (en) | 2016-12-16 | 2018-06-21 | Janssen Pharmaceutica Nv | Bicyclic oga inhibitor compounds |
-
2017
- 2017-10-31 US US16/346,730 patent/US10947242B2/en not_active Expired - Fee Related
- 2017-10-31 EA EA201991109A patent/EA039788B1/ru unknown
- 2017-10-31 TW TW106137541A patent/TWI764950B/zh not_active IP Right Cessation
- 2017-10-31 MX MX2019005154A patent/MX385576B/es unknown
- 2017-10-31 EP EP17792066.7A patent/EP3535267B1/en active Active
- 2017-10-31 SG SG11201903892UA patent/SG11201903892UA/en unknown
- 2017-10-31 BR BR112019008404A patent/BR112019008404A2/pt not_active IP Right Cessation
- 2017-10-31 WO PCT/EP2017/077910 patent/WO2018083098A1/en not_active Ceased
- 2017-10-31 CN CN201780067759.3A patent/CN109923116B/zh not_active Expired - Fee Related
- 2017-10-31 AU AU2017353310A patent/AU2017353310B2/en not_active Ceased
- 2017-10-31 CA CA3041412A patent/CA3041412A1/en active Pending
- 2017-10-31 MY MYPI2019002499A patent/MY193511A/en unknown
- 2017-10-31 ES ES17792066T patent/ES2864131T3/es active Active
- 2017-10-31 UA UAA201906027A patent/UA125302C2/uk unknown
- 2017-10-31 JP JP2019522892A patent/JP7076441B2/ja active Active
- 2017-10-31 KR KR1020197015232A patent/KR20190070972A/ko not_active Abandoned
- 2017-11-02 AR ARP170103037A patent/AR110026A1/es unknown
-
2019
- 2019-04-29 IL IL266305A patent/IL266305B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| BR112019008404A2 (pt) | 2019-09-17 |
| IL266305B (en) | 2021-10-31 |
| AU2017353310B2 (en) | 2021-08-12 |
| UA125302C2 (uk) | 2022-02-16 |
| EP3535267B1 (en) | 2020-12-30 |
| CA3041412A1 (en) | 2018-05-11 |
| WO2018083098A1 (en) | 2018-05-11 |
| IL266305A (en) | 2019-06-30 |
| TWI764950B (zh) | 2022-05-21 |
| JP2019532985A (ja) | 2019-11-14 |
| JP7076441B2 (ja) | 2022-05-27 |
| EA201991109A1 (ru) | 2019-09-30 |
| KR20190070972A (ko) | 2019-06-21 |
| US10947242B2 (en) | 2021-03-16 |
| MY193511A (en) | 2022-10-17 |
| CN109923116B (zh) | 2022-12-06 |
| TW201831486A (zh) | 2018-09-01 |
| US20190276462A1 (en) | 2019-09-12 |
| MX385576B (es) | 2025-03-18 |
| AU2017353310A1 (en) | 2019-05-16 |
| MX2019005154A (es) | 2019-06-20 |
| ES2864131T3 (es) | 2021-10-13 |
| EA039788B1 (ru) | 2022-03-14 |
| SG11201903892UA (en) | 2019-05-30 |
| EP3535267A1 (en) | 2019-09-11 |
| CN109923116A (zh) | 2019-06-21 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR110026A1 (es) | Inhibidores de pde2 | |
| ES2778700T3 (es) | Nuevos derivados de piperidinilo sustituidos con (hetero)arilo, un proceso para su preparación y composiciones farmacéuticas que los contienen | |
| ES2292130T3 (es) | Pirido(2,3-d)pirimidin-7-onas pirrolil-sustituidas y derivados de las mismas como agentes terapeuticos. | |
| UY37926A (es) | Formulaciones de 6-(2-hidroxi-2-metilpropoxi)-4-(6-(6-((6-metoxipiridin-3-il)metil)-3,6-diazabiciclo[3.1.1]heptan-3-il)piridin-3-il)pirazolo[1,5-a]piridina-3-carbonitrilo | |
| HRP20211864T1 (hr) | Inhibitori hetero-halo histonske deacetilaze | |
| PH12016501164A1 (en) | Heteroaryl substituted nicotinamide compounds | |
| CL2019001633A1 (es) | Imidazol pirrol piridina como inhibidores de la familia jak de quinasas. | |
| AR080754A1 (es) | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 | |
| PE20191613A1 (es) | Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret | |
| PE20090506A1 (es) | DERIVADOS DE IMIDAZO-[1,2-b]-PIRIDAZIN COMO INHIBIDORES DE ALK5 Y/O ALK4 | |
| ZA202205900B (en) | 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 | |
| RU2018123779A (ru) | Новые соединения | |
| AR101265A1 (es) | Ácidos carboxílicos heterocíclicos como activadores de guanilato ciclasa soluble | |
| EA201000615A1 (ru) | Производные имидазо[1,2-а]пиридина, применимые в качестве ингибиторов апк (активиноподобной киназы) | |
| HRP20110428T1 (hr) | Derivati piperidin-amino-benzimidazola kao inhibitori respiratorne sincitijalne virusne replikacije | |
| AR089424A1 (es) | Derivados de dihidro-benzo-oxazina y dihidro-pirido-oxazina | |
| MY195669A (en) | 8-[6-[3-(Amino)Propoxy]-3-Pyridyl]-1 -Isopropyl-Imidazo[4,5-C]Quinolin-2-One Derivatives As Selective Modulators Of Ataxia Telangiectasia Mutated (Atm) Kinase For The Treatment Of Cancer | |
| AU2011367809A1 (en) | Piperidine derivatives and compositions for the inhibition of nicotinamide phosphoribosyltransferase (NAMPT) | |
| CN102131808A (zh) | 吡唑并吡啶激酶抑制剂 | |
| WO2015193263A1 (en) | Indolizine derivatives as phoshoinositide 3-kinases inhibitors | |
| EA201691934A1 (ru) | Замещенные 4,5,6,7-тетрагидро-пиразоло[1,5-альфа]пиримидиновые производные и 2,3-дигидро-1h-имидазо[1,2-бета]пиразольные производные в качестве ингибиторов ros1 | |
| PE20211246A1 (es) | Compuestos biciclicos para su uso como inhibidores de rip1 quinasa | |
| PH12017501121A1 (en) | Pharmaceutical formulations of tropomyosin related kinase (trk) inhibitors | |
| PE20211247A1 (es) | Sulfonas y sulfoxidos biciclicos y metodos de usos de los mismos | |
| MX382128B (es) | Derivados de piridin-2-ona fusionados triciclicos, y su uso como inhibidores de brd4. |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |