AR030946A1 - Derivados de imidazoles sustituidos un metodo para su preparacion, composiciones farmaceuticas y el uso de dichos derivados para la manufactura de medicamentos como agonistas o antagonistas duales de h1 y h3 de histamina - Google Patents
Derivados de imidazoles sustituidos un metodo para su preparacion, composiciones farmaceuticas y el uso de dichos derivados para la manufactura de medicamentos como agonistas o antagonistas duales de h1 y h3 de histaminaInfo
- Publication number
- AR030946A1 AR030946A1 ARP010104399A ARP010104399A AR030946A1 AR 030946 A1 AR030946 A1 AR 030946A1 AR P010104399 A ARP010104399 A AR P010104399A AR P010104399 A ARP010104399 A AR P010104399A AR 030946 A1 AR030946 A1 AR 030946A1
- Authority
- AR
- Argentina
- Prior art keywords
- derivatives
- group
- alkyl
- manufacture
- pharmaceutical compositions
- Prior art date
Links
- 239000003814 drug Substances 0.000 title abstract 2
- 230000009977 dual effect Effects 0.000 title abstract 2
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 title 2
- 239000000556 agonist Substances 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 229960001340 histamine Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- -1 enantiomers Chemical class 0.000 abstract 2
- 150000002431 hydrogen Chemical class 0.000 abstract 2
- 150000002460 imidazoles Chemical class 0.000 abstract 2
- 125000006684 polyhaloalkyl group Polymers 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000004209 (C1-C8) alkyl 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
- 206010020751 Hypersensitivity Diseases 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 208000026935 allergic disease Diseases 0.000 abstract 1
- 230000007815 allergy Effects 0.000 abstract 1
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 239000000938 histamine H1 antagonist Substances 0.000 abstract 1
- 239000003395 histamine H3 receptor antagonist Substances 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 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
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
Classifications
-
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- 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
-
- 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
-
- 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
- C07D401/14—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 three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Derivados de imidazoles sustituidos incluyendo enantiomeros, esteroisomeros y tautomeros del mismo, o sales o solvatos farmacéuticamente aceptables de dicho compuesto; porque dichos compuestos tienen a estructura general que se muestra en la formula 1, en la cual: f = 0, 1 o 2; X e Y están independientemente seleccionadas del grupo que consiste en N, CH o N-oxidos; G es una porcion seleccionada del grupo que consiste en las porciones 2, 3 y 4 con el extremo superior de dichas 2, 3 y 4 ligado a la porcion tricíclica y en el extremo inferior de 2, 3 y 4 ligados a M, donde s = t = 1 o 2; y p = q = 0, 1 o 2; M es una porcion seleccionada del grupo que consiste en alquilo C1-8; -C(O)-(CH2)y-; -(CH2)x-A-(CH2)y-; -C(O)-O-(CH2)d-; y -C(O)-NR3-(CH2)d-; donde A es O, S(O)r-, y -NR4-; n = 0, 1, 2 o 3; x es un numero entero en el rango de 2-5; y es un numero entero en el rango de 0-5; d es un numero en el rango de 0-5; r = 0, 1 o 2; R1 y R2 pueden ser cada uno en el numero 1-3 y están independientemente seleccionados del grupo que consiste en hidrogeno, alquilo inferior, alcoxi inferior, halogeno, OCF3, OCHF2, -OH, y -N(R4)2; R3 está seleccionado del grupo que consiste en hidrogeno alquilo inferior, y polihaloalquilo inferior; R4 está seleccionado de hidrogeno, alquilo inferior, polihaloalquilo inferior; y R5 es H, alquilo C1-6 o OH, que tienen actividad antagonista dual del receptor H1 y H3de histamina así como también métodos para preparar dichos compuestos. En otra realizacion se describen composiciones farmacéuticas que comprenden dichos imidazoles así como también el uso de los mismos para la manufactura de medicamentos para tratar alergia, enfermedades inflamatorias y relacionadas con el SNC y otros.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US23405300P | 2000-09-20 | 2000-09-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR030946A1 true AR030946A1 (es) | 2003-09-03 |
Family
ID=22879692
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010104399A AR030946A1 (es) | 2000-09-20 | 2001-09-18 | Derivados de imidazoles sustituidos un metodo para su preparacion, composiciones farmaceuticas y el uso de dichos derivados para la manufactura de medicamentos como agonistas o antagonistas duales de h1 y h3 de histamina |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US6506756B2 (es) |
| EP (1) | EP1318994B1 (es) |
| JP (1) | JP2004509871A (es) |
| CN (1) | CN1461303A (es) |
| AR (1) | AR030946A1 (es) |
| AT (1) | ATE387439T1 (es) |
| AU (1) | AU2001292730A1 (es) |
| CA (1) | CA2421826C (es) |
| DE (1) | DE60133014T2 (es) |
| ES (1) | ES2300364T3 (es) |
| HK (1) | HK1052179A1 (es) |
| MX (1) | MXPA03002448A (es) |
| MY (1) | MY117975A (es) |
| TW (1) | TW589303B (es) |
| WO (1) | WO2002024659A2 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6607862B2 (en) | 2001-08-24 | 2003-08-19 | Intel Corporation | Damascene extreme ultraviolet lithography alternative phase shift photomask and method of making |
| JP4384918B2 (ja) * | 2002-04-18 | 2009-12-16 | シェーリング コーポレイション | ヒスタミンｈ３アンタゴニストとして有用な（１−４−ピペリジニル）ベンズイミダゾール誘導体 |
| NZ535764A (en) | 2002-04-18 | 2007-10-26 | Schering Corp | 1-(4-piperidinyl) benzimidazolones as histamine H3 antagonists |
| US7105505B2 (en) | 2002-04-18 | 2006-09-12 | Schering Corporation | Benzimidazole derivatives useful as histamine H3 antagonists |
| NL1026634C2 (nl) * | 2004-07-12 | 2006-01-16 | Willem Jacob Van Der Burg | Psychofarmaceutisch preparaat en werkzame stof daarin. |
| WO2013151982A1 (en) | 2012-04-03 | 2013-10-10 | Arena Pharmaceuticals, Inc. | Methods and compounds useful in treating pruritus, and methods for identifying such compounds |
| US9224955B1 (en) * | 2014-10-31 | 2015-12-29 | Feng-wen Yen | Purifying method for organic optoelectronic material |
| CN113880808B (zh) * | 2020-07-03 | 2024-12-31 | 合肥医工医药股份有限公司 | 一类三唑类化合物、制备方法及其医药用途 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2586562B1 (fr) | 1985-09-02 | 1989-03-10 | Inst Nat Sante Rech Med | Composition pharmaceutique contenant de l'a-methylhistamine |
| ATE108453T1 (de) | 1988-04-28 | 1994-07-15 | Schering Corp | Benzopyridopiperidin, -piperidyliden und - piperazin-verbindungen, zusammensetzungen, methoden zur herstellung und verwendung. |
| GB8916947D0 (en) | 1989-07-25 | 1989-09-13 | Smith Kline French Lab | Medicaments |
| EP0448765B1 (de) | 1990-03-30 | 1994-08-17 | HEUMANN PHARMA GMBH & CO | Verwendung von Guanidinderivaten zur Herstellung eines Arzneimittels mit NPY-antagonistischer Wirkung |
| GB9115740D0 (en) | 1991-07-20 | 1991-09-04 | Smithkline Beecham Plc | Medicaments |
| DE69205287T2 (de) | 1991-12-18 | 1996-03-14 | Schering Corp., Kenilworth, N.J. | Imidazolylalkyl- piperazin und -diazepin derivate als histamin h3 agonisten/antagonisten. |
| US5352707A (en) | 1992-03-26 | 1994-10-04 | Harbor Branch Oceanographic Institution, Inc. | Method for treating airway congestion |
| HUT74386A (en) | 1993-11-15 | 1996-12-30 | Schering Corp | Phenyl-alkyl imidazoles as h3-receptor antagonists and pharmaceutical compositions containing them |
| FR2732017B1 (fr) | 1995-03-21 | 2000-09-22 | Inst Nat Sante Rech Med | Nouveaux derives de l'imidazole antagonistes et/ou agonistes du recepteur h3 de l'histamine, leur preparation et leurs applications therapeutiques |
| AU7907198A (en) | 1997-06-24 | 1999-01-04 | Novo Nordisk A/S | Use of somatostatin agonists and antagonists for treating diseases related to the eye |
| US5869479A (en) | 1997-08-14 | 1999-02-09 | Schering Corporation | Treatment of upper airway allergic responses |
| WO2000005215A1 (en) * | 1998-07-24 | 2000-02-03 | Russinsky Limited | A process for preparing benzocycloheptapyridin-11-ones |
-
2001
- 2001-09-18 US US09/954,867 patent/US6506756B2/en not_active Expired - Fee Related
- 2001-09-18 AU AU2001292730A patent/AU2001292730A1/en not_active Abandoned
- 2001-09-18 WO PCT/US2001/029095 patent/WO2002024659A2/en not_active Ceased
- 2001-09-18 CA CA002421826A patent/CA2421826C/en not_active Expired - Fee Related
- 2001-09-18 AT AT01973119T patent/ATE387439T1/de not_active IP Right Cessation
- 2001-09-18 EP EP01973119A patent/EP1318994B1/en not_active Expired - Lifetime
- 2001-09-18 AR ARP010104399A patent/AR030946A1/es unknown
- 2001-09-18 HK HK03104436.1A patent/HK1052179A1/zh unknown
- 2001-09-18 MY MYPI20014365A patent/MY117975A/en unknown
- 2001-09-18 CN CN01815978A patent/CN1461303A/zh active Pending
- 2001-09-18 DE DE60133014T patent/DE60133014T2/de not_active Expired - Lifetime
- 2001-09-18 JP JP2002529071A patent/JP2004509871A/ja not_active Withdrawn
- 2001-09-18 ES ES01973119T patent/ES2300364T3/es not_active Expired - Lifetime
- 2001-09-18 MX MXPA03002448A patent/MXPA03002448A/es active IP Right Grant
- 2001-09-19 TW TW090123001A patent/TW589303B/zh not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| MY117975A (en) | 2004-08-30 |
| EP1318994A2 (en) | 2003-06-18 |
| EP1318994B1 (en) | 2008-02-27 |
| CA2421826A1 (en) | 2002-03-28 |
| TW589303B (en) | 2004-06-01 |
| WO2002024659A3 (en) | 2002-10-24 |
| JP2004509871A (ja) | 2004-04-02 |
| WO2002024659A2 (en) | 2002-03-28 |
| MXPA03002448A (es) | 2003-06-19 |
| CN1461303A (zh) | 2003-12-10 |
| DE60133014T2 (de) | 2009-02-26 |
| CA2421826C (en) | 2009-10-27 |
| HK1052179A1 (zh) | 2003-09-05 |
| ES2300364T3 (es) | 2008-06-16 |
| US20020086859A1 (en) | 2002-07-04 |
| DE60133014D1 (de) | 2008-04-10 |
| US6506756B2 (en) | 2003-01-14 |
| ATE387439T1 (de) | 2008-03-15 |
| AU2001292730A1 (en) | 2002-04-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |