AR045117A1 - Imidazo-pirimidinas y triazolo-pirimidinas:ligandos del receptor de benzodiazepina - Google Patents
Imidazo-pirimidinas y triazolo-pirimidinas:ligandos del receptor de benzodiazepinaInfo
- Publication number
- AR045117A1 AR045117A1 ARP040102649A ARP040102649A AR045117A1 AR 045117 A1 AR045117 A1 AR 045117A1 AR P040102649 A ARP040102649 A AR P040102649A AR P040102649 A ARP040102649 A AR P040102649A AR 045117 A1 AR045117 A1 AR 045117A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- amino
- halogen
- cyano
- nitro
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 229910052736 halogen Inorganic materials 0.000 abstract 7
- 150000002367 halogens Chemical class 0.000 abstract 7
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- -1 nitro, cyano, amino Chemical group 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 3
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 3
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000002861 (C1-C4) alkanoyl group Chemical group 0.000 abstract 1
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 abstract 1
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000006648 (C1-C8) haloalkyl group Chemical group 0.000 abstract 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 125000004650 C1-C8 alkynyl group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 abstract 1
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 abstract 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 1
- 102000027484 GABAA receptors Human genes 0.000 abstract 1
- 108091008681 GABAA receptors Proteins 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 208000015114 central nervous system disease Diseases 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 239000003446 ligand Substances 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000002071 phenylalkoxy group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 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
- 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
- A61P25/08—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
- A61P25/14—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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Anesthesiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Compuesto y composición farmacéutica útiles para modular la unión de ligando a receptor GABAa, para trastornos del SNC, memoria o demencia de Alzheimer. Reivindicación 1: Un compuesto de formula (1) o una de sus sales aceptables desde el punto de vista farmacéutico, en la que: Z1 es N o CR1; Z2 es N o CR2, y Z3 es N o CR3, tal que por lo menos uno, aunque no más de dos, de Z1, Z2, y Z3 son N; R1, R2, R3 y R4 se seleccionan, cada uno de forma independiente, de: (a) H, halógeno, nitro y ciano; y (b) grupos de la fórmula (2) en la que: L es un enlace o alquileno C1-8; G es un enlace, N(RB), O, C(=O), C(=O)O, C(=O)N(RB), N(RB)C(=O), S(O)m, CH2C(=O), S(=O)mN(RB) o N(RB)S(O)m; en los que m es 0, 1 o 2; y RA y cada RB se seleccionan en forma independiente de: (i) H; y (ii) alquilo C1-8, alquenilo C2-8, alquinilo C2-8, (cicloalquil C3-8)alquilo C0-4, (heterocicloalquilo de 3 a 7 miembros)alquilo C0-4, (aril C6-10)alquilo C0-2 o (heteroarilo de 5 a 10 miembros)alquilo C0-2, cada uno de los cuales está sustituido con desde 0 hasta 4 sustituyentes seleccionados en forma independiente de halógeno, hidroxi, nitro, ciano, amino, alquilo C1-4, alcoxi C1-4, alcanoilo C1-4, mono- y di(alquil C1-4)amino, haloalquilo C1-4 y haloalcoxi c1-4; R5 es (a) H, halógeno o ciano; o (b) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-4 o mono- o di(alquil C1-4)amino, cada uno de los cuales está sustituido con desde 0 hasta 5 sustituyentes elegidos en forma independiente de halógeno, hidroxi, nitro, ciano, amino, alcoxi C1-4, haloalquilo C1-2, haloalcoxi C1-2, mono- y di(alquil C1-4)amino, cicloalquilo C3-8, fenilo, fenilalcoxi c1-4 y heteroarilo de 5 o 6 miembros; R6 y R7 son, en forma independiente, H, metilo, etilo o halógeno; R8 representa 0, 1 o 2 sustituyentes elegidos en forma independiente de halógeno, hidroxi, nitro, ciano, amino, alquilo C1-4, alcoxi C1-4, mono- y di(alquil C1-4)amino, cicloalquilo C3-7, haloalquilo C1-2 y haloalcoxi C1-2; y Ar representa fenilo, naftilo o heteroarilo de 5 a 10 miembros, cada uno de los cuales está sustituido con desde 0 hasta 4 sustituyentes elegidos en forma independiente de halógeno, hidroxi, nitro, ciano, amino, alquilo C1-8, alquenilo C1-8, alquinilo C1-8, alcoxi C1-8, (cicloalquil C3-7)alquilo C0-4, (cicloalquil C3-7)alcoxi C1-4, alquilo C1-8, éter, alcanona c1-8, alcanoilo C1-8, (heterocicloalquilo de 3 a 7 miembros)alquilo C0-4, haloalquilo C1-8, haloalcoxi C1-8, oxo, hidroxialquilo C1-8, aminoalquilo C1-8, y mono- y di(alquil C1-8)amino alquilo C0-8.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US49000603P | 2003-07-25 | 2003-07-25 | |
| US54308304P | 2004-02-09 | 2004-02-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR045117A1 true AR045117A1 (es) | 2005-10-19 |
Family
ID=34118813
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040102649A AR045117A1 (es) | 2003-07-25 | 2004-07-26 | Imidazo-pirimidinas y triazolo-pirimidinas:ligandos del receptor de benzodiazepina |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US7271170B2 (es) |
| EP (1) | EP1648899B1 (es) |
| JP (1) | JP2007500130A (es) |
| KR (1) | KR20060098425A (es) |
| AR (1) | AR045117A1 (es) |
| AT (1) | ATE350382T1 (es) |
| AU (1) | AU2004261591A1 (es) |
| BR (1) | BRPI0412908A (es) |
| CA (1) | CA2537331A1 (es) |
| CY (1) | CY1107565T1 (es) |
| DE (1) | DE602004004143T2 (es) |
| DK (1) | DK1648899T3 (es) |
| ES (1) | ES2278345T3 (es) |
| IL (1) | IL173265A0 (es) |
| MX (1) | MXPA06000887A (es) |
| NZ (1) | NZ544262A (es) |
| PL (1) | PL1648899T3 (es) |
| PT (1) | PT1648899E (es) |
| TW (1) | TW200524937A (es) |
| WO (1) | WO2005012306A2 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7482366B2 (en) * | 2001-12-21 | 2009-01-27 | X-Ceptor Therapeutics, Inc. | Modulators of LXR |
| EP1619948A4 (en) * | 2003-05-05 | 2007-02-14 | Neurogen Corp | SUBSTITUTED IMIDAZOLOPYRAZINE AND TRIAZOLOPYRAZINE DERIVATIVES: GABAA RECEPTOR LIGANDS |
| WO2006093911A2 (en) * | 2005-03-02 | 2006-09-08 | Neurogen Corporation | Thiazolylmethyl and oxazolylmethyl heteroaryl derivatives |
| US7709468B2 (en) | 2005-09-02 | 2010-05-04 | Abbott Laboratories | Imidazo based heterocycles |
| JP2010523716A (ja) * | 2007-04-11 | 2010-07-15 | サイプレス バイオサイエンシズ，インク． | ベンゾジアゼピン受容体拮抗薬を用いるダウン症候群の治療 |
| CN101687873A (zh) * | 2007-04-17 | 2010-03-31 | 百时美施贵宝公司 | 具有稠合杂环的11β-羟基类固醇Ⅰ型脱氢酶抑制剂 |
| GB0719803D0 (en) | 2007-10-10 | 2007-11-21 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| US20090270373A1 (en) * | 2008-04-11 | 2009-10-29 | Cypress Biosciences, Inc. | Treatment of down syndrom with benzodiazepine receptor antagonists |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US544057A (en) * | 1895-08-06 | Bill and letter file | ||
| BR0009539A (pt) * | 1999-04-02 | 2006-06-06 | Neurogen Corp | composto, composição farmacêutica, método para tratamento ou prevenção de uma doença ou distúrbio associado com agonismo patogênico, agonismo inverso ou antagonismo do receptor gaba a, uso de um composto, método para localizar receptores gaba a em uma amostra de tecido, método para alterar a atividade transdutora de sinal de receptores gaba a, método para o tratamento ou prevenção de distúrbios psicológicos associados com modulação do complexo receptor gaba a, e, processo para a preparação de um composto |
| US6737242B1 (en) | 1999-05-07 | 2004-05-18 | Neurogen Corporation | Methods for screening GABA-modulatory compounds for specified pharmacological activities |
| GB9929687D0 (en) | 1999-12-15 | 2000-02-09 | Merck Sharp & Dohme | Therapeutic agents |
| US6552037B2 (en) * | 2000-06-30 | 2003-04-22 | Neurogen Corporation | 2-Substituted imidazo[1,2-A]pyridine derivatives |
| GB0027561D0 (en) * | 2000-11-10 | 2000-12-27 | Merck Sharp & Dohme | Therapeutic agents |
| US6900215B2 (en) * | 2000-12-15 | 2005-05-31 | Merck Sharp & Dohme Ltd. | Imidazo-pyrimidine derivatives as ligands for gaba receptors |
| PA8535601A1 (es) * | 2000-12-21 | 2002-11-28 | Pfizer | Derivados benzimidazol y piridilimidazol como ligandos para gabaa |
| TWI248936B (en) * | 2001-03-21 | 2006-02-11 | Merck Sharp & Dohme | Imidazo-pyrimidine derivatives as ligands for GABA receptors |
| WO2002076983A1 (en) * | 2001-03-23 | 2002-10-03 | Merck Sharp & Dohme Limited | Imidazo-pyrimidine derivatives as ligands for gaba receptors |
| IL159811A0 (en) * | 2001-07-13 | 2004-06-20 | Neurogen Corp | Heteroaryl substituted fused bicyclic heteroaryl compounds as gabaa receptor ligands |
| GB0128499D0 (en) * | 2001-11-28 | 2002-01-23 | Merck Sharp & Dohme | Therapeutic agents |
| AU2003245259A1 (en) | 2002-05-02 | 2003-11-17 | Neurogen Corporation | Substituted imidazole derivatives: gabaa receptor ligands |
| US6982268B2 (en) | 2002-05-08 | 2006-01-03 | Neurogen Corporation | Substituted imidazolylmethyl pyridine and pyrazine derivatives GABAA receptor ligands |
| US6916827B2 (en) | 2002-05-17 | 2005-07-12 | Neurogen Corporation | Substituted ring-fused imidazole derivative: GABAA receptors ligands |
| CN100579579C (zh) | 2002-10-01 | 2010-01-13 | 诺华疫苗和诊断公司 | 抗癌及抗感染性疾病组合物及其使用方法 |
| DE60307499T2 (de) | 2002-11-08 | 2007-02-01 | Neurogen Corp., Branford | 4-imidazol-1-ylmethylpyrimidinderivate als liganden für gabaa-rezeptoren |
| EP1619948A4 (en) | 2003-05-05 | 2007-02-14 | Neurogen Corp | SUBSTITUTED IMIDAZOLOPYRAZINE AND TRIAZOLOPYRAZINE DERIVATIVES: GABAA RECEPTOR LIGANDS |
-
2004
- 2004-07-23 PT PT04779031T patent/PT1648899E/pt unknown
- 2004-07-23 MX MXPA06000887A patent/MXPA06000887A/es active IP Right Grant
- 2004-07-23 PL PL04779031T patent/PL1648899T3/pl unknown
- 2004-07-23 KR KR1020067001782A patent/KR20060098425A/ko not_active Ceased
- 2004-07-23 AT AT04779031T patent/ATE350382T1/de not_active IP Right Cessation
- 2004-07-23 DE DE602004004143T patent/DE602004004143T2/de not_active Expired - Lifetime
- 2004-07-23 JP JP2006521278A patent/JP2007500130A/ja active Pending
- 2004-07-23 US US10/898,690 patent/US7271170B2/en not_active Expired - Lifetime
- 2004-07-23 CA CA002537331A patent/CA2537331A1/en not_active Abandoned
- 2004-07-23 NZ NZ544262A patent/NZ544262A/xx unknown
- 2004-07-23 AU AU2004261591A patent/AU2004261591A1/en not_active Abandoned
- 2004-07-23 BR BRPI0412908-3A patent/BRPI0412908A/pt not_active IP Right Cessation
- 2004-07-23 EP EP04779031A patent/EP1648899B1/en not_active Expired - Lifetime
- 2004-07-23 WO PCT/US2004/023794 patent/WO2005012306A2/en not_active Ceased
- 2004-07-23 ES ES04779031T patent/ES2278345T3/es not_active Expired - Lifetime
- 2004-07-23 DK DK04779031T patent/DK1648899T3/da active
- 2004-07-26 AR ARP040102649A patent/AR045117A1/es unknown
- 2004-07-26 TW TW093122247A patent/TW200524937A/zh unknown
-
2006
- 2006-01-19 IL IL173265A patent/IL173265A0/en unknown
-
2007
- 2007-02-26 CY CY20071100262T patent/CY1107565T1/el unknown
- 2007-09-14 US US11/855,386 patent/US20080139580A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU2004261591A1 (en) | 2005-02-10 |
| DK1648899T3 (da) | 2007-04-02 |
| ES2278345T3 (es) | 2007-08-01 |
| BRPI0412908A (pt) | 2006-09-26 |
| CA2537331A1 (en) | 2005-02-10 |
| US20050038043A1 (en) | 2005-02-17 |
| JP2007500130A (ja) | 2007-01-11 |
| EP1648899B1 (en) | 2007-01-03 |
| ATE350382T1 (de) | 2007-01-15 |
| PL1648899T3 (pl) | 2007-06-29 |
| WO2005012306A3 (en) | 2005-04-14 |
| IL173265A0 (en) | 2006-06-11 |
| WO2005012306A2 (en) | 2005-02-10 |
| MXPA06000887A (es) | 2006-04-19 |
| DE602004004143D1 (de) | 2007-02-15 |
| TW200524937A (en) | 2005-08-01 |
| EP1648899A2 (en) | 2006-04-26 |
| US7271170B2 (en) | 2007-09-18 |
| KR20060098425A (ko) | 2006-09-18 |
| HK1089446A1 (en) | 2006-12-01 |
| DE602004004143T2 (de) | 2007-10-11 |
| US20080139580A1 (en) | 2008-06-12 |
| CY1107565T1 (el) | 2013-03-13 |
| NZ544262A (en) | 2009-06-26 |
| PT1648899E (pt) | 2007-03-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |