AR037135A1 - Derivados de adenosina con un grupo acetileno en posicion 4', con actividad agonista del receptor a1 de adenosina - Google Patents
Derivados de adenosina con un grupo acetileno en posicion 4', con actividad agonista del receptor a1 de adenosinaInfo
- Publication number
- AR037135A1 AR037135A1 ARP020100976A ARP020100976A AR037135A1 AR 037135 A1 AR037135 A1 AR 037135A1 AR P020100976 A ARP020100976 A AR P020100976A AR P020100976 A ARP020100976 A AR P020100976A AR 037135 A1 AR037135 A1 AR 037135A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- cycloalkyl
- phenyl
- optionally substituted
- 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
- HSFWRNGVRCDJHI-UHFFFAOYSA-N Acetylene Chemical group C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 title 1
- 239000002126 C01EB10 - Adenosine Substances 0.000 title 1
- 229960005305 adenosine Drugs 0.000 title 1
- 150000003835 adenosine derivatives Chemical class 0.000 title 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000002619 bicyclic group Chemical group 0.000 abstract 2
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 125000003320 C2-C6 alkenyloxy group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000005133 alkynyloxy group Chemical group 0.000 abstract 1
- 150000005018 aminopurines Chemical class 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 235000021588 free fatty acids Nutrition 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000006413 ring segment Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/16—Purine radicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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]
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Rheumatology (AREA)
- Anesthesiology (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Otolaryngology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Compuestos de 6 amino purinas sustituidas de fórmula (1), donde: X representa O ó CH2; R1 representa: (i) cicloalquilo (C3-9)-(alq)n- o cicloalquenilo (C3-9)-(alq)n-, el grupo cicloalquilo o cicloalquenilo estando substituido opcionalmente por uno o más substituyeres seleccionados de OH, halógeno, alquilo C1-6, -alcoxi C1-6, alqueniloxi, C2-6 alquiniloxi C2-6 y fenilo, en donde (alq) representa alquilo C1-3 y n representa 0 ó 1, y el grupo (alq) puede opcionalmente substituirse por el grupo cicloalquilo C3-6; (ii) un grupo fenilo opcionalmente substituido por uno o más sustituyentes seleccionados de: halógeno, CF3, ciano, -alquilo C1-6, -alquilo C2-6, -alquinilo C2-6-, alcoxi C1-6-, -alquil OH C1-6, -CO2H y -CO2 alquil C1-6; iii) un grupo heterocíclico C4-7 que contiene al menos un heteroátomo seleccionado de O, N ó S, y substituido opcionalmente por uno o más sustituyentes seleccionados de OH, -alquilo C1-6-, -alcoxi C1-6, -CO2alquil C1-4, -COalquil C1-4, -CO2arilo o cicloalquil (C3-6)-CO2(alq)n, en donde (alq) representa alquilo C1-3 y n representa 0 ó 1; (iv) un grupo alquilo C1-12 de cadena recta o ramificada substituido opcionalmente por uno o más grupos seleccionados de fenilo, halógeno, hidroxi, y cicloalquilo C3-7, donde uno o más átomos de carbono del grupo alquilo C1-12 puede reemplazarse opcionalmente por un grupo independientemente seleccionado de S(=O)n (donde n es 0, 1 ó 2) y N; (v) un anillo bicíclico fundido de fórmula (2) en donde A representa cicloalquilo C4-6 o fenilo y B representa fenilo substituido opcionalmente por alquilo C1-3 y el anillo bicíclico se enlaza a la porción purina-6-amino por medio de un átomo de anillo del anillo A; R2 representa un grupo -alquilo C1-3, halógeno, hidrógeno o -alcoxi C1-3; R3 y R4 independientemente representan H o un grupo -alquilo C1-6; o una sal farmacéuticamente aceptable y/o solvato del mismo. También se dan a conocer: composiciones farmacéuticas que los contienen, su uso en la manufactura de un medicamento para el tratamiento de un paciente que sufre de una condición donde es ventajoso reducir la concentración de ácidos grasos libres en plasma o reducir el ritmo cardíaco y método para el tratamiento en un paciente con dicha condición.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0106875A GB0106875D0 (en) | 2001-03-20 | 2001-03-20 | Medicaments |
| GB0106871A GB0106871D0 (en) | 2001-03-20 | 2001-03-20 | Chemical compounds |
| GB0106877A GB0106877D0 (en) | 2001-03-20 | 2001-03-20 | Chemical compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR037135A1 true AR037135A1 (es) | 2004-10-27 |
Family
ID=27256108
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020100976A AR037135A1 (es) | 2001-03-20 | 2002-03-19 | Derivados de adenosina con un grupo acetileno en posicion 4', con actividad agonista del receptor a1 de adenosina |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US20040162422A1 (es) |
| EP (1) | EP1370568B1 (es) |
| JP (1) | JP2004534002A (es) |
| KR (1) | KR20030085014A (es) |
| CN (1) | CN1501941A (es) |
| AR (1) | AR037135A1 (es) |
| AT (1) | ATE306492T1 (es) |
| BR (1) | BR0208169A (es) |
| CA (1) | CA2441202A1 (es) |
| CZ (1) | CZ20032543A3 (es) |
| DE (1) | DE60206605D1 (es) |
| HU (1) | HUP0303533A3 (es) |
| IL (1) | IL157649A0 (es) |
| MX (1) | MXPA03008493A (es) |
| NO (1) | NO20034182L (es) |
| NZ (1) | NZ527854A (es) |
| PL (1) | PL364712A1 (es) |
| WO (1) | WO2002074780A1 (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA05001844A (es) * | 2002-08-15 | 2005-04-19 | Cv Therapeutics Inc | Combatientes completos y parciales de receptores de adenosina a1. |
| GB0221694D0 (en) * | 2002-09-18 | 2002-10-30 | Glaxo Group Ltd | Compounds |
| GT200500281A (es) * | 2004-10-22 | 2006-04-24 | Novartis Ag | Compuestos organicos. |
| GB0500785D0 (en) | 2005-01-14 | 2005-02-23 | Novartis Ag | Organic compounds |
| RU2457209C2 (ru) * | 2006-04-21 | 2012-07-27 | Новартис Аг | Производные пурина, предназначенные для применения в качестве агонистов аденозинового рецептора а2а |
| GB0607953D0 (en) * | 2006-04-21 | 2006-05-31 | Novartis Ag | Organic compounds |
| GB0607948D0 (en) * | 2006-04-21 | 2006-05-31 | Novartis Ag | Organic compounds |
| GB0607944D0 (en) * | 2006-04-21 | 2006-05-31 | Novartis Ag | Organic compounds |
| GB0607950D0 (en) * | 2006-04-21 | 2006-05-31 | Novartis Ag | Organic compounds |
| GB0607945D0 (en) * | 2006-04-21 | 2006-05-31 | Novartis Ag | Organic compounds |
| EP1889846A1 (en) | 2006-07-13 | 2008-02-20 | Novartis AG | Purine derivatives as A2a agonists |
| EP1903044A1 (en) * | 2006-09-14 | 2008-03-26 | Novartis AG | Adenosine Derivatives as A2A Receptor Agonists |
| KR20090087054A (ko) * | 2006-11-10 | 2009-08-14 | 노파르티스 아게 | 시클로펜텐 디올 모노아세테이트 유도체 |
| JP2011500631A (ja) * | 2007-10-17 | 2011-01-06 | ノバルティス アーゲー | アデノシンa1受容体リガンドとしてのプリン誘導体 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4996308A (en) * | 1988-03-25 | 1991-02-26 | Merrell Dow Pharmaceuticals Inc. | Derivatives with unsaturated substitutions for the 5'-hydroxymethyl group |
| GB9723589D0 (en) * | 1997-11-08 | 1998-01-07 | Glaxo Group Ltd | Chemical compounds |
| YU44900A (sh) * | 1998-01-31 | 2003-01-31 | Glaxo Group Limited | Derivati 2-(purin-9-il)tetrahidrofuran-3,4-diola |
| GB9813554D0 (en) * | 1998-06-23 | 1998-08-19 | Glaxo Group Ltd | Chemical compounds |
-
2002
- 2002-03-12 US US10/471,681 patent/US20040162422A1/en not_active Abandoned
- 2002-03-19 DE DE60206605T patent/DE60206605D1/de not_active Expired - Lifetime
- 2002-03-19 HU HU0303533A patent/HUP0303533A3/hu unknown
- 2002-03-19 EP EP02714332A patent/EP1370568B1/en not_active Expired - Lifetime
- 2002-03-19 JP JP2002573789A patent/JP2004534002A/ja not_active Withdrawn
- 2002-03-19 AR ARP020100976A patent/AR037135A1/es not_active Application Discontinuation
- 2002-03-19 WO PCT/GB2002/001317 patent/WO2002074780A1/en not_active Ceased
- 2002-03-19 IL IL15764902A patent/IL157649A0/xx unknown
- 2002-03-19 CA CA002441202A patent/CA2441202A1/en not_active Abandoned
- 2002-03-19 CN CNA028067754A patent/CN1501941A/zh active Pending
- 2002-03-19 KR KR10-2003-7012208A patent/KR20030085014A/ko not_active Withdrawn
- 2002-03-19 PL PL02364712A patent/PL364712A1/xx not_active Application Discontinuation
- 2002-03-19 AT AT02714332T patent/ATE306492T1/de not_active IP Right Cessation
- 2002-03-19 NZ NZ527854A patent/NZ527854A/en unknown
- 2002-03-19 BR BR0208169-5A patent/BR0208169A/pt not_active Application Discontinuation
- 2002-03-19 CZ CZ20032543A patent/CZ20032543A3/cs unknown
- 2002-03-19 MX MXPA03008493A patent/MXPA03008493A/es unknown
-
2003
- 2003-09-19 NO NO20034182A patent/NO20034182L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| HUP0303533A2 (hu) | 2004-03-01 |
| BR0208169A (pt) | 2004-03-02 |
| CA2441202A1 (en) | 2002-09-26 |
| NO20034182D0 (no) | 2003-09-19 |
| NO20034182L (no) | 2003-09-19 |
| KR20030085014A (ko) | 2003-11-01 |
| HUP0303533A3 (en) | 2005-02-28 |
| CN1501941A (zh) | 2004-06-02 |
| US20040162422A1 (en) | 2004-08-19 |
| WO2002074780A1 (en) | 2002-09-26 |
| NZ527854A (en) | 2004-09-24 |
| EP1370568A1 (en) | 2003-12-17 |
| CZ20032543A3 (en) | 2004-05-12 |
| ATE306492T1 (de) | 2005-10-15 |
| DE60206605D1 (de) | 2006-02-23 |
| PL364712A1 (en) | 2004-12-13 |
| JP2004534002A (ja) | 2004-11-11 |
| EP1370568B1 (en) | 2005-10-12 |
| MXPA03008493A (es) | 2003-12-08 |
| IL157649A0 (en) | 2004-05-12 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |