AR075894A1 - Derivados oxidados de triazolilpurinas utiles como ligandos de receptor de adenosina a2a y su uso como medicamentos. - Google Patents
Derivados oxidados de triazolilpurinas utiles como ligandos de receptor de adenosina a2a y su uso como medicamentos.Info
- Publication number
- AR075894A1 AR075894A1 ARP100100883A ARP100100883A AR075894A1 AR 075894 A1 AR075894 A1 AR 075894A1 AR P100100883 A ARP100100883 A AR P100100883A AR P100100883 A ARP100100883 A AR P100100883A AR 075894 A1 AR075894 A1 AR 075894A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- branched
- linear
- group
- independently
- Prior art date
Links
- OIRDTQYFTABQOQ-KQYNXXCUSA-N adenosine Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O OIRDTQYFTABQOQ-KQYNXXCUSA-N 0.000 title 2
- 239000002126 C01EB10 - Adenosine Substances 0.000 title 1
- 229960005305 adenosine Drugs 0.000 title 1
- 229940079593 drug Drugs 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 101150051188 Adora2a gene Proteins 0.000 abstract 1
- 101100439664 Arabidopsis thaliana CHR8 gene Proteins 0.000 abstract 1
- 201000006474 Brain Ischemia Diseases 0.000 abstract 1
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 1
- 125000005915 C6-C14 aryl group Chemical group 0.000 abstract 1
- 101100240516 Caenorhabditis elegans nhr-10 gene Chemical group 0.000 abstract 1
- 206010008120 Cerebral ischaemia Diseases 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 206010008118 cerebral infarction Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 230000003862 health status Effects 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
-
- 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
- A61K31/52—Purines, e.g. adenine
-
- 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
- A61P25/28—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
- A61P3/00—Drugs for disorders of the metabolism
-
- 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)
- 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)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
También se refiere a procesos para su preparacion y a composiciones farmacéuticas que los contienen, para el tratamiento de trastornos neurologicos o isquemia cerebral, para los cuales la inhibicion de receptor de adenosina A2A dará como resultado la mejoría del estado de salud de un paciente. Reivindicacion 1: Un compuesto que tiene la formula general 1: R1 = es alquilo C1-6 lineal o ramificado; R2 es un grupo de la formula R9-(CHR8)p-(CR6R7)m-(CR4R5)n-; R4, R6 y R8 son, independientemente H, hidroxilo o =O, con el significado de carbonilo; R5, R7 y R9 son, independientemente, H o están ausentes; m, n y p son, independientemente un numero entero comprendido entre 0 y 2; m + n + p >=4; R3 es NH2, NHR10; R10 es alquilo C1-6 o hidroxialquilo C1-6, alcoxialquilo C1-3, amino(C1-6)alquilo, donde el grupo amino está sustituido, opcionalmente por uno o dos grupos alquilo C1-3, siendo los citados grupos alquilo lineales o ramificados; arilo C6-14 o arilo C6-14-alquilo C1-6, con el grupo arilo sustituido opcionalmente por uno o más sustituyentes, ya sea iguales o diferentes, seleccionados por el grupo constituido por halogeno, hidroxi, alcoxi C1-6 lineal o ramificado, saturado o insaturado, amino, mono- o di-sustituidos con alquilo C1-6 lineal o ramificado; sus formas opticamente activas, tales como enantiomeros, diastereomeros y sus formas de racemato y sales farmacéuticamente aceptables de los mismos; con la condicion de que R4, R6 y R8 no sean todos H al mismo tiempo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09155690 | 2009-03-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR075894A1 true AR075894A1 (es) | 2011-05-04 |
Family
ID=40941572
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100100883A AR075894A1 (es) | 2009-03-20 | 2010-03-19 | Derivados oxidados de triazolilpurinas utiles como ligandos de receptor de adenosina a2a y su uso como medicamentos. |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US9133197B2 (es) |
| EP (1) | EP2408775B1 (es) |
| JP (1) | JP5648044B2 (es) |
| AR (1) | AR075894A1 (es) |
| DK (1) | DK2408775T3 (es) |
| ES (1) | ES2542555T3 (es) |
| HR (1) | HRP20150766T1 (es) |
| HU (1) | HUE025704T2 (es) |
| PL (1) | PL2408775T3 (es) |
| PT (1) | PT2408775E (es) |
| SI (1) | SI2408775T1 (es) |
| SM (1) | SMT201500174B (es) |
| TW (1) | TWI473809B (es) |
| WO (1) | WO2010106145A1 (es) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20200172628A1 (en) | 2017-06-22 | 2020-06-04 | Novartis Ag | Antibody molecules to cd73 and uses thereof |
| WO2018237157A1 (en) | 2017-06-22 | 2018-12-27 | Novartis Ag | CD73 BINDING ANTIBODY MOLECULES AND USES THEREOF |
| SG11202002886PA (en) * | 2017-09-28 | 2020-04-29 | Cstone Pharmaceuticals Suzhou Co Ltd | Fused ring derivative as a2a receptor inhibitor |
| WO2019099838A1 (en) | 2017-11-16 | 2019-05-23 | Novartis Ag | Combination therapies |
| TW201925782A (zh) | 2017-11-30 | 2019-07-01 | 瑞士商諾華公司 | 靶向bcma之嵌合抗原受體及其用途 |
| CA3092635A1 (en) | 2018-03-14 | 2019-09-19 | Surface Oncology, Inc. | Antibodies that bind cd39 and uses thereof |
| UY38247A (es) | 2018-05-30 | 2019-12-31 | Novartis Ag | Anticuerpos frente a entpd2, terapias de combinación y métodos de uso de los anticuerpos y las terapias de combinación |
| WO2019232244A2 (en) | 2018-05-31 | 2019-12-05 | Novartis Ag | Antibody molecules to cd73 and uses thereof |
| IL317554A (en) | 2018-06-01 | 2025-02-01 | Novartis Ag | Anti-BCMA binding molecules and their uses |
| AR116109A1 (es) | 2018-07-10 | 2021-03-31 | Novartis Ag | Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos |
| CN113271945A (zh) | 2018-12-20 | 2021-08-17 | 诺华股份有限公司 | 包含3-(1-氧代异吲哚啉-2-基)哌啶-2,6-二酮衍生物的给药方案和药物组合 |
| MX2021009763A (es) | 2019-02-15 | 2021-09-08 | Novartis Ag | Derivados de 3-(1-oxo-5-(piperidin-4-il)isoindolin-2-il)piperidina -2,6-diona y usos de los mismos. |
| MX2021009764A (es) | 2019-02-15 | 2021-09-08 | Novartis Ag | Derivados de 3-(1-oxoisoindolin-2-il)piperidina-2,6-diona sustituidos y usos de los mismos. |
| US20220372160A1 (en) | 2019-09-16 | 2022-11-24 | Surface Oncology, Inc. | Anti-CD39 Antibody Compositions and Methods |
| TW202124446A (zh) | 2019-09-18 | 2021-07-01 | 瑞士商諾華公司 | 與ｅｎｔｐｄ２抗體之組合療法 |
| WO2021053559A1 (en) | 2019-09-18 | 2021-03-25 | Novartis Ag | Entpd2 antibodies, combination therapies, and methods of using the antibodies and combination therapies |
| CN115087671A (zh) | 2019-09-25 | 2022-09-20 | 表面肿瘤学公司 | 抗il-27抗体及其用途 |
| JP2023507190A (ja) | 2019-12-20 | 2023-02-21 | ノバルティス アーゲー | 増殖性疾患を治療するための抗ＴＧＦβ抗体及びチェックポイント阻害薬の使用 |
| EP4168007A1 (en) | 2020-06-23 | 2023-04-26 | Novartis AG | Dosing regimen comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives |
| EP4188549A1 (en) | 2020-08-03 | 2023-06-07 | Novartis AG | Heteroaryl substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
| AU2021373366A1 (en) | 2020-11-06 | 2023-06-01 | Novartis Ag | Cd19 binding molecules and uses thereof |
| JP2024505049A (ja) | 2021-01-29 | 2024-02-02 | ノバルティス アーゲー | 抗ｃｄ７３及び抗ｅｎｔｐｄ２抗体のための投与方式並びにその使用 |
| TW202304979A (zh) | 2021-04-07 | 2023-02-01 | 瑞士商諾華公司 | 抗ＴＧＦβ抗體及其他治療劑用於治療增殖性疾病之用途 |
| AR125874A1 (es) | 2021-05-18 | 2023-08-23 | Novartis Ag | Terapias de combinación |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3990061B2 (ja) * | 1998-01-05 | 2007-10-10 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | プリン誘導体および糖尿病の予防・治療剤としてのアデノシンａ２受容体拮抗剤 |
| USRE39112E1 (en) | 1998-01-05 | 2006-05-30 | Eisai Co., Ltd. | Purine derivatives and adenosine A2 receptor antagonists serving as preventives/remedies for diabetes |
| NZ516260A (en) * | 1999-07-02 | 2004-08-27 | Eisai Co Ltd | Fused imidazole compounds and remedies for diabetes mellitus |
| PT1272897E (pt) * | 2000-02-10 | 2008-08-18 | Univ New York | Antagonistas de receptores a2a para a adenosina para o tratamento e prevenção da fibrose hepática, cirrose e fígado gordo |
| WO2003002566A1 (en) * | 2001-06-29 | 2003-01-09 | Cv Therapeutics, Inc. | Purine derivatives as a2b adenosine receptor antagonists |
| ITRM20010465A1 (it) * | 2001-07-31 | 2003-01-31 | Sigma Tau Ind Farmaceuti | Derivati della triazolil-imidazopiridina e delle triazolilpurine utili come ligandi del recettore a2a dell'adenosina e loro uso come medicam |
| JPWO2003020723A1 (ja) * | 2001-08-30 | 2004-12-16 | 協和醗酵工業株式会社 | ［１，２，４］トリアゾロ［１，５−ａ］ピリミジン誘導体 |
| GB0500785D0 (en) * | 2005-01-14 | 2005-02-23 | Novartis Ag | Organic compounds |
| JPWO2006129626A1 (ja) * | 2005-05-30 | 2009-01-08 | 協和醗酵工業株式会社 | ［１，２，４］トリアゾロ［１，５−ｃ］ピリミジン誘導体の製造法 |
-
2010
- 2010-03-18 DK DK10709526.7T patent/DK2408775T3/en active
- 2010-03-18 WO PCT/EP2010/053554 patent/WO2010106145A1/en not_active Ceased
- 2010-03-18 HU HUE10709526A patent/HUE025704T2/en unknown
- 2010-03-18 HR HRP20150766TT patent/HRP20150766T1/hr unknown
- 2010-03-18 ES ES10709526.7T patent/ES2542555T3/es active Active
- 2010-03-18 EP EP10709526.7A patent/EP2408775B1/en active Active
- 2010-03-18 US US13/257,750 patent/US9133197B2/en not_active Expired - Fee Related
- 2010-03-18 PT PT107095267T patent/PT2408775E/pt unknown
- 2010-03-18 PL PL10709526T patent/PL2408775T3/pl unknown
- 2010-03-18 SI SI201030983T patent/SI2408775T1/sl unknown
- 2010-03-18 JP JP2012500259A patent/JP5648044B2/ja not_active Expired - Fee Related
- 2010-03-19 AR ARP100100883A patent/AR075894A1/es unknown
- 2010-03-19 TW TW99108187A patent/TWI473809B/zh not_active IP Right Cessation
-
2015
- 2015-07-20 SM SM201500174T patent/SMT201500174B/xx unknown
- 2015-08-10 US US14/822,252 patent/US20160002244A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| JP5648044B2 (ja) | 2015-01-07 |
| ES2542555T3 (es) | 2015-08-06 |
| HUE025704T2 (en) | 2016-04-28 |
| JP2012520854A (ja) | 2012-09-10 |
| US20160002244A1 (en) | 2016-01-07 |
| TWI473809B (zh) | 2015-02-21 |
| TW201100425A (en) | 2011-01-01 |
| EP2408775B1 (en) | 2015-06-17 |
| HRP20150766T1 (hr) | 2015-08-14 |
| WO2010106145A1 (en) | 2010-09-23 |
| US9133197B2 (en) | 2015-09-15 |
| PT2408775E (pt) | 2015-08-05 |
| EP2408775A1 (en) | 2012-01-25 |
| US20120053191A1 (en) | 2012-03-01 |
| SI2408775T1 (sl) | 2015-08-31 |
| PL2408775T3 (pl) | 2015-10-30 |
| DK2408775T3 (en) | 2015-07-27 |
| SMT201500174B (it) | 2015-10-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |