AR045843A1 - Derivados de bencimidazolonas y quinazolinonas sustituidas con hidronopol como agonistas en receptores orl 1 humanos - Google Patents
Derivados de bencimidazolonas y quinazolinonas sustituidas con hidronopol como agonistas en receptores orl 1 humanosInfo
- Publication number
- AR045843A1 AR045843A1 ARP040103510A ARP040103510A AR045843A1 AR 045843 A1 AR045843 A1 AR 045843A1 AR P040103510 A ARP040103510 A AR P040103510A AR P040103510 A ARP040103510 A AR P040103510A AR 045843 A1 AR045843 A1 AR 045843A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- amino
- proviso
- compounds
- hydrogen
- Prior art date
Links
- RCRVMCSPZAMFKV-UHFFFAOYSA-N 2-(6,6-dimethyl-4-bicyclo[3.1.1]heptanyl)ethanol Chemical group C1C2C(C)(C)C1CCC2CCO RCRVMCSPZAMFKV-UHFFFAOYSA-N 0.000 title 1
- 239000000556 agonist Substances 0.000 title 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- -1 amino, amino Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000002252 acyl group Chemical group 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 229940002612 prodrug Drugs 0.000 abstract 2
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 abstract 1
- 150000001408 amides Chemical class 0.000 abstract 1
- 150000001409 amidines Chemical class 0.000 abstract 1
- 150000004657 carbamic acid derivatives Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000004966 cyanoalkyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 150000002081 enamines Chemical class 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 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
- 125000002924 primary amino group Chemical group [H]N([H])* 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
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
- 125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 abstract 1
Classifications
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- 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
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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- A—HUMAN NECESSITIES
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- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
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- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
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- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Neurosurgery (AREA)
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- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
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- Diabetes (AREA)
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- Dermatology (AREA)
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- Addiction (AREA)
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Abstract
Preparación de compuestos, composiciones farmacéuticas que los comprenden y usos. Reivindicación 1: Compuestos de la fórmula general (1), en donde: R1 representa H, alquilo C1-6, alquil(C1-3)-cicloalquilo(C3-6), carbalcoxi (C2-7) o acilo (C2-7); [ ]m simboliza -(CH2)m- en donde m es 0 ó 1; R2 representa halógeno, CF3, alquilo (C1-6), alquil(C1-3)-cicloalquilo(C3-6), fenilo, amino, aminoalquilo(C1-3), alquil(C1-3)-amino dialquil(C1-3)-amino, ciano, cianoalquilo(C1-3), hidroxi, hidroxialquilo (C1-3), alcoxi (C1-3), OCF3, acilo (C2-7), trifluoroacetilo, aminocarboxilo, alquil (C1-3)-sulfonilo o trifluorometilosulfonilo, y n es un entero de 0-4, con la condición de que cuando n es 2, 3 ó 4, los sustituyentes R2 pueden ser iguales o diferentes; A es un anillo saturado o parcialmente insaturado, [ ]o y [ ]p representan -(CH2)o- y -(CH2)p- respectivamente, con la condición de que también el significado -CH- es posible cuando A es un anillo parcialmente insaturado, y o y p independientemente son 0, 1 ó 2; R3, R4, R5 y R6 representan independientemente hidrógeno, alquilo (C1-3), alquilo(C1-3)-cicloalquilo (C3-6); CH2OH o (R3 y R5) o (R3 y R6) o (R4 y R5) o (R4 y R6) juntos pueden formar un puente alquileno C1-3, con la condición de que cuando o es 2, R3 es hidrógeno, y cuando p es 2, R5 es hidrógeno; [ ]q simboliza -(CH2)q- en donde q es un entero de 0 a 2 todos los estereoisómeros, así como las sales farmacológicamente aceptables y prodrogas de los mismos, siendo las prodrogas derivados de los compuestos que tienen la fórmula (1) en donde está presente un grupo que es fácilmente removido después de la administración, tales como amidina, enamina, una base de Mannich, un derivado hidroxi-metileno, un derivado O-(aciloximetilen carbamato), carbamato, éster, amida o enaminona.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP03103671 | 2003-10-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR045843A1 true AR045843A1 (es) | 2005-11-16 |
Family
ID=34924113
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040103510A AR045843A1 (es) | 2003-10-03 | 2004-09-28 | Derivados de bencimidazolonas y quinazolinonas sustituidas con hidronopol como agonistas en receptores orl 1 humanos |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US7851630B2 (es) |
| EP (1) | EP1670457A1 (es) |
| JP (1) | JP2007507470A (es) |
| CN (1) | CN1838951A (es) |
| AR (1) | AR045843A1 (es) |
| AU (1) | AU2004277346B2 (es) |
| BR (1) | BRPI0414494A (es) |
| CA (1) | CA2534833A1 (es) |
| MX (1) | MXPA06002065A (es) |
| RU (1) | RU2357964C2 (es) |
| SA (1) | SA04250319B1 (es) |
| TW (1) | TW200519102A (es) |
| UA (1) | UA83870C2 (es) |
| WO (1) | WO2005032547A1 (es) |
| ZA (1) | ZA200603472B (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2006298852A1 (en) * | 2005-09-30 | 2007-04-12 | F. Hoffmann-La Roche Ag | Indane derivatives as MCH receptor antagonists |
| DE102007009235A1 (de) * | 2007-02-22 | 2008-09-18 | Grünenthal GmbH | Spirocyclische Cyclohexan-Derivate |
| EP3564240B1 (en) | 2007-08-31 | 2022-04-06 | Purdue Pharma L.P. | Piperidine intermediates |
| CN102675226B (zh) * | 2012-05-24 | 2014-04-23 | 西南大学 | 3-取代-1-甲基-2，4-喹唑啉二酮类化合物及其制备方法和应用 |
| CN104755465A (zh) * | 2012-08-24 | 2015-07-01 | 武田药品工业株式会社 | 杂环化合物 |
| US9951038B2 (en) | 2012-12-27 | 2018-04-24 | Purdue Pharma L.P. | Quinazolin-4(3H)-one-type piperidine compounds and uses thereof |
| CN103420944A (zh) * | 2013-07-26 | 2013-12-04 | 江西农业大学 | 一种合成顺式氢化诺卜基甲酰胺类化合物的方法 |
| GB201820165D0 (en) * | 2018-12-11 | 2019-01-23 | Ucb Biopharma Sprl | Therapeutic agents |
| CN115611856B (zh) * | 2021-07-14 | 2024-07-05 | 宜昌人福药业有限责任公司 | 一种哌啶衍生物及其药物组合物、制备方法和用途 |
| CN115124441B (zh) * | 2022-06-30 | 2024-04-02 | 南京林业大学 | 一类诺卜酸酰肼类化合物的制备方法和产品及其应用 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2097031A1 (en) | 1970-07-29 | 1972-03-03 | Berri Balzac | 2-aminoethoxyethyl-6,6-dimethyl nor pinane derivs - local anaesthetics spasmolytics and anticholinergics |
| IT1251144B (it) * | 1991-07-30 | 1995-05-04 | Boehringer Ingelheim Italia | Derivati del benzimidazolone |
| JP4366532B2 (ja) | 1997-05-30 | 2009-11-18 | 萬有製薬株式会社 | ２−オキソイミダゾール誘導体 |
| ATE219772T1 (de) | 1998-01-19 | 2002-07-15 | Pfizer | 4-(2-keto-1-benzimidazolinyl)piperidin derivate als orl1-rezeptor agoniste |
| US6340681B1 (en) * | 1999-07-16 | 2002-01-22 | Pfizer Inc | 2-benzimidazolylamine compounds as ORL-1-receptor agonists |
| WO2001039775A1 (en) | 1999-12-06 | 2001-06-07 | Euro-Celtique, S.A. | Benzimidazole compounds having nociceptin receptor affinity |
| KR100809569B1 (ko) * | 2001-10-02 | 2008-03-04 | 아카디아 파마슈티칼스 인코포레이티드 | 무스카린 제제로서 벤즈이미다졸리디논 유도체 |
| SA04250305B1 (ar) * | 2003-09-25 | 2008-06-02 | سولفاي فارماسوتيكالز بي . في | مشتقات بنزيميدازولون cenzimidazolone وكينازولينون quinazolinone كمساعادات على مستقبلات ORL1 البشرية |
| AR046756A1 (es) * | 2003-12-12 | 2005-12-21 | Solvay Pharm Gmbh | Derivados de hidronopol como agonistas de receptores orl-1 humanos. |
-
2004
- 2004-09-28 AR ARP040103510A patent/AR045843A1/es not_active Application Discontinuation
- 2004-09-29 US US10/952,180 patent/US7851630B2/en not_active Expired - Fee Related
- 2004-09-29 TW TW093129412A patent/TW200519102A/zh unknown
- 2004-10-01 CN CNA2004800240298A patent/CN1838951A/zh active Pending
- 2004-10-01 CA CA002534833A patent/CA2534833A1/en not_active Abandoned
- 2004-10-01 WO PCT/EP2004/052392 patent/WO2005032547A1/en not_active Ceased
- 2004-10-01 RU RU2006110519/04A patent/RU2357964C2/ru active
- 2004-10-01 BR BRPI0414494-5A patent/BRPI0414494A/pt not_active IP Right Cessation
- 2004-10-01 AU AU2004277346A patent/AU2004277346B2/en not_active Ceased
- 2004-10-01 JP JP2006530268A patent/JP2007507470A/ja not_active Withdrawn
- 2004-10-01 MX MXPA06002065A patent/MXPA06002065A/es unknown
- 2004-10-01 EP EP04791109A patent/EP1670457A1/en not_active Withdrawn
- 2004-10-01 UA UAA200604720A patent/UA83870C2/ru unknown
- 2004-10-02 SA SA4250319A patent/SA04250319B1/ar unknown
-
2006
- 2006-05-02 ZA ZA200603472A patent/ZA200603472B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| UA83870C2 (ru) | 2008-08-26 |
| ZA200603472B (en) | 2007-09-26 |
| JP2007507470A (ja) | 2007-03-29 |
| US20050075355A1 (en) | 2005-04-07 |
| SA04250319B1 (ar) | 2008-07-19 |
| BRPI0414494A (pt) | 2006-11-14 |
| AU2004277346A1 (en) | 2005-04-14 |
| US7851630B2 (en) | 2010-12-14 |
| MXPA06002065A (es) | 2006-05-19 |
| AU2004277346B2 (en) | 2009-02-19 |
| RU2006110519A (ru) | 2006-07-27 |
| WO2005032547A1 (en) | 2005-04-14 |
| CN1838951A (zh) | 2006-09-27 |
| EP1670457A1 (en) | 2006-06-21 |
| RU2357964C2 (ru) | 2009-06-10 |
| TW200519102A (en) | 2005-06-16 |
| CA2534833A1 (en) | 2005-04-14 |
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| FA | Abandonment or withdrawal |