CO5640041A2 - Un inhibidor de pde4 y un agente anticolinergico en combinacion para tratar enfermedades obstructivas de vias respiratorias - Google Patents
Un inhibidor de pde4 y un agente anticolinergico en combinacion para tratar enfermedades obstructivas de vias respiratoriasInfo
- Publication number
- CO5640041A2 CO5640041A2 CO03102140A CO03102140A CO5640041A2 CO 5640041 A2 CO5640041 A2 CO 5640041A2 CO 03102140 A CO03102140 A CO 03102140A CO 03102140 A CO03102140 A CO 03102140A CO 5640041 A2 CO5640041 A2 CO 5640041A2
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- cycloalkyl
- alkenyl
- group
- groups
- Prior art date
Links
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 title abstract 2
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 title abstract 2
- 239000003795 chemical substances by application Substances 0.000 title 1
- 201000010099 disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 230000000414 obstructive effect Effects 0.000 title 1
- 230000000241 respiratory effect Effects 0.000 title 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 11
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 125000003342 alkenyl group Chemical group 0.000 abstract 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 239000000812 cholinergic antagonist Substances 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000006526 (C1-C2) alkyl group Chemical group 0.000 abstract 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 101100296720 Dictyostelium discoideum Pde4 gene Proteins 0.000 abstract 1
- 101100082610 Plasmodium falciparum (isolate 3D7) PDEdelta gene Proteins 0.000 abstract 1
- 229940124639 Selective inhibitor Drugs 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000004450 alkenylene group Chemical group 0.000 abstract 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- QGZKDVFQNNGYKY-UHFFFAOYSA-O ammonium group Chemical group [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 239000011593 sulfur Substances 0.000 abstract 1
- LERNTVKEWCAPOY-DZZGSBJMSA-N tiotropium Chemical class O([C@H]1C[C@@H]2[N+]([C@H](C1)[C@@H]1[C@H]2O1)(C)C)C(=O)C(O)(C=1SC=CC=1)C1=CC=CS1 LERNTVKEWCAPOY-DZZGSBJMSA-N 0.000 abstract 1
Classifications
-
- 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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61K31/435—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
- A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pulmonology (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
1.- Una combinación inhalada de un inhibidor selectivo de PDE4 y un agente anticolinérgico, con la condición de que el agente anticolinérgico no sea una sal de tiotropio.2.- Una combinación de acuerdo con la reivindicación 1, caracterizada porque el inhibidor selectivo de PDE4 es un compuesto de la fórmula (I) o una sal o solvato farmacéuticamente aceptable de él, endonde:R1 es H, alquilo (de C1-C6), alcoxi (de C1-C6), alquenilo (deC1-C6), fenilo, -N(CH3)2, cicloalquilo (de C3-C6), cicloalquilo(de C3-C6) alquilo (de C1-C3) o acilo (de C1-C6), en donde los grupos alquilo, fenilo o alquenilo pueden ser sustituidos con hasta dos grupos -OH, alquilo (de C1-C3) o CF3 o hasta tres halógenos; R2 y R3 se seleccionan independientemente del grupo formado por H, alquilo (de C1-C14), alcoxi (de C1-C7)alquilo (de C1-C7), alquenilo (de C2-C14), cicloalquilo (de C3-C7), cicloalquilo (de C3-C7) cicloalquilo (de C3-C7) alquilo (de C1-C2), un grupo (CH2)n heterocíclico (de C4-C7) saturado o insaturado en donde n es 0, 1 o 2 que contiene como el heteroátomo uno o dos del grupo formado por oxígeno, azufre, sulfonilo, nitrógeno y NR4 en donde R4 es H o alquilo (de C1-C4); o un grupo de la fórmula (II) : en donde a es un número entero de 1 a 5; b y c son 0 o 1; R5 es H, -OH, alquilo (de C1-C5), alquenilo (de C2-C5), alcoxi (de C1-C5), cicloalcoxi (de C3-C6), halógeno, -CF3, -CO2R6, -CONR6R7, -NR6R7, -NO2, o -SO2NR6R7 en donde R6 y R7 son cada uno independientemente H, o alquilo (de C1-C6); Z es -O-, -S-, -SO2-, -CO-, o -N(R8)- en donde R8 es H o alquilo (de C1-C4); e Y es alquileno (de C1-C5) o alquenileno (de C2-C8) optativamente sustituido con hasta dos grupos alquilo (de C1-C7) o cicloalquilo (de C3-C7); en donde cada uno de los grupos alquilo, alquenilo, cicloalquilo, alcoxialquilo o hetercíclico pueden ser sustituidos con 1 a 14, preferentemente 1 a 5 grupos alquilo (de C1-C2), CF3 o halo; y R9 y R10 se seleccionan cada uno independientemente del grupo formado por H, alquilo (de C1-C6), alcoxi (de C1-C8), arilo (de C8-C10) y ariloxi (de C8-C10).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29360601P | 2001-05-25 | 2001-05-25 | |
| GB0129396A GB0129396D0 (en) | 2001-12-07 | 2001-12-07 | Pharmaceutical combination |
| GB0210240A GB0210240D0 (en) | 2002-05-03 | 2002-05-03 | Pharmaceutical combination |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO5640041A2 true CO5640041A2 (es) | 2006-05-31 |
Family
ID=27256347
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO03102140A CO5640041A2 (es) | 2001-05-25 | 2003-11-19 | Un inhibidor de pde4 y un agente anticolinergico en combinacion para tratar enfermedades obstructivas de vias respiratorias |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US20040147544A1 (es) |
| EP (1) | EP1395288A1 (es) |
| JP (1) | JP2005508861A (es) |
| KR (1) | KR20040007605A (es) |
| CN (1) | CN1511042A (es) |
| AP (1) | AP2003002909A0 (es) |
| BG (1) | BG108382A (es) |
| BR (1) | BR0209992A (es) |
| CA (1) | CA2446613A1 (es) |
| CO (1) | CO5640041A2 (es) |
| CR (1) | CR7152A (es) |
| CZ (1) | CZ20033150A3 (es) |
| EE (1) | EE200300585A (es) |
| HU (1) | HUP0400037A2 (es) |
| IL (1) | IL158776A0 (es) |
| MA (1) | MA27027A1 (es) |
| MX (1) | MXPA03010162A (es) |
| NO (1) | NO20035204D0 (es) |
| NZ (1) | NZ529335A (es) |
| OA (1) | OA12610A (es) |
| PA (1) | PA8546001A1 (es) |
| PL (1) | PL367085A1 (es) |
| SK (1) | SK14312003A3 (es) |
| TN (1) | TNSN03123A1 (es) |
| WO (1) | WO2002096463A1 (es) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2165768B1 (es) | 1999-07-14 | 2003-04-01 | Almirall Prodesfarma Sa | Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen. |
| DE10230769A1 (de) * | 2002-07-09 | 2004-01-22 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Arzneimittelkompositionen auf der Basis neuer Anticholinergika und PDE-IV-Inhibitoren |
| US20040058950A1 (en) * | 2002-07-09 | 2004-03-25 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pharmaceutical compositions based on anticholinergics and PDE-IV inhibitors |
| MXPA05010160A (es) * | 2003-03-28 | 2005-11-16 | Altana Pharma Ag | Combinacion sinergistica que comprende roflumilast y un agente anticolinergico seleccionado a partir de sales de ipratropio, oxitropio y tiotropio para el tratamiento de enfermedades respiratorias. |
| WO2004084897A1 (en) * | 2003-03-28 | 2004-10-07 | Altana Pharma Ag | Synergistic combination comprising roflumilast and an anticholinergic agent selected from ipratropium, oxitropium and tiotropium salts for the treatment of respiratory diseases |
| WO2005074918A1 (en) | 2004-02-06 | 2005-08-18 | Benzstrasse 1 D-61352 Bad Homburd | The combination of anticholinergics and glucocorticoids for the long-term treatment of asthma and copd |
| WO2005074983A2 (en) * | 2004-02-06 | 2005-08-18 | Meda Pharma Gmbh & Co. Kg | Treatment of rhinitis with anticholinergics alone in combination with antihistamines phosphodiesterase 4 inhibitors, or corticosteroids |
| RU2437658C2 (ru) * | 2004-02-06 | 2011-12-27 | Меда Фарма Гмбх Унд Ко.Кг | Комбинация (варианты) и фармацевтический препарат для лечения заболеваний дыхательных путей |
| WO2005102344A1 (ja) * | 2004-04-27 | 2005-11-03 | Kyowa Hakko Kogyo Co., Ltd. | 医薬組成物 |
| DE602004015788D1 (de) * | 2004-08-19 | 2008-09-25 | Rottapharm Spa | Verwendung von Phenylbenzamide-derivaten zur Behandlung von chronisch-obstruktiver Lungenerkrankung (COPD) |
| MX2007011273A (es) | 2005-03-16 | 2007-11-08 | Meda Pharma Gmbh & Co Kg | La combinacion de anticolinergicos y antagonistas del receptor de leucotrieno para el tratamiento de enfermedades respiratorias. |
| GB0511066D0 (en) * | 2005-05-31 | 2005-07-06 | Novartis Ag | Organic compounds |
| EP2258357A3 (en) | 2005-08-26 | 2011-04-06 | Braincells, Inc. | Neurogenesis with acetylcholinesterase inhibitor |
| AU2006282896A1 (en) | 2005-08-26 | 2007-03-01 | Braincells, Inc. | Neurogenesis by muscarinic receptor modulation |
| KR100696432B1 (ko) * | 2005-08-31 | 2007-03-19 | 김용환 | 건강진단용 팬티 |
| AU2006305620A1 (en) * | 2005-10-19 | 2007-04-26 | Ranbaxy Laboratories Limited | Compositions of phosphodiesterase type IV inhibitors |
| WO2007047978A2 (en) | 2005-10-21 | 2007-04-26 | Braincells, Inc. | Modulation of neurogenesis by pde inhibition |
| JP2009513672A (ja) | 2005-10-31 | 2009-04-02 | ブレインセルス，インコーポレイティド | 神経発生のｇａｂａ受容体媒介調節 |
| ES2389231T3 (es) | 2005-12-21 | 2012-10-24 | Meda Pharma Gmbh & Co. Kg | Combinación de anticolinérgicos, glucocorticoides y agonistas de beta2 para el tratamiento de enfermedades inflamatorias |
| US20100216734A1 (en) | 2006-03-08 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis by nootropic agents |
| EP2377531A2 (en) | 2006-05-09 | 2011-10-19 | Braincells, Inc. | Neurogenesis by modulating angiotensin |
| US20100184806A1 (en) | 2006-09-19 | 2010-07-22 | Braincells, Inc. | Modulation of neurogenesis by ppar agents |
| EP2100599A1 (en) | 2008-03-13 | 2009-09-16 | Laboratorios Almirall, S.A. | Inhalation composition containing aclidinium for treatment of asthma and chronic obstructive pulmonary disease |
| EP2100598A1 (en) | 2008-03-13 | 2009-09-16 | Laboratorios Almirall, S.A. | Inhalation composition containing aclidinium for treatment of asthma and chronic obstructive pulmonary disease |
| WO2010099217A1 (en) | 2009-02-25 | 2010-09-02 | Braincells, Inc. | Modulation of neurogenesis using d-cycloserine combinations |
| EP2510928A1 (en) | 2011-04-15 | 2012-10-17 | Almirall, S.A. | Aclidinium for use in improving the quality of sleep in respiratory patients |
| WO2013106547A1 (en) | 2012-01-10 | 2013-07-18 | President And Fellows Of Harvard College | Beta-cell replication promoting compounds and methods of their use |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5552407A (en) * | 1993-06-11 | 1996-09-03 | New York University Medical Center | Anhydroecgonine compounds and their use as anticholinergic agents |
| CA2223624C (en) * | 1995-06-06 | 2001-02-20 | Pfizer Inc. | Tricyclic 5,6-dihydro-9h-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-.alpha.]pyridines |
| US20020193393A1 (en) * | 2001-03-07 | 2002-12-19 | Michel Pairet | Pharmaceutical compositions based on anticholinergics and PDE-IV inhibitors |
-
2002
- 2002-05-24 WO PCT/EP2002/005726 patent/WO2002096463A1/en not_active Ceased
- 2002-05-24 SK SK1431-2003A patent/SK14312003A3/sk not_active Application Discontinuation
- 2002-05-24 PL PL02367085A patent/PL367085A1/xx not_active Application Discontinuation
- 2002-05-24 BR BR0209992-6A patent/BR0209992A/pt not_active IP Right Cessation
- 2002-05-24 OA OA1200300304A patent/OA12610A/en unknown
- 2002-05-24 AP APAP/P/2003/002909A patent/AP2003002909A0/en unknown
- 2002-05-24 PA PA20028546001A patent/PA8546001A1/es unknown
- 2002-05-24 CA CA002446613A patent/CA2446613A1/en not_active Abandoned
- 2002-05-24 EP EP02750977A patent/EP1395288A1/en not_active Withdrawn
- 2002-05-24 CZ CZ20033150A patent/CZ20033150A3/cs unknown
- 2002-05-24 EE EEP200300585A patent/EE200300585A/xx unknown
- 2002-05-24 NZ NZ529335A patent/NZ529335A/en unknown
- 2002-05-24 MX MXPA03010162A patent/MXPA03010162A/es unknown
- 2002-05-24 US US10/478,755 patent/US20040147544A1/en not_active Abandoned
- 2002-05-24 CN CNA028104986A patent/CN1511042A/zh active Pending
- 2002-05-24 KR KR10-2003-7015352A patent/KR20040007605A/ko not_active Ceased
- 2002-05-24 JP JP2002592972A patent/JP2005508861A/ja not_active Withdrawn
- 2002-05-24 IL IL15877602A patent/IL158776A0/xx unknown
- 2002-05-24 HU HU0400037A patent/HUP0400037A2/hu unknown
-
2003
- 2003-07-08 TN TNPCT/EP2002/005726A patent/TNSN03123A1/en unknown
- 2003-11-19 CO CO03102140A patent/CO5640041A2/es not_active Application Discontinuation
- 2003-11-19 CR CR7152A patent/CR7152A/es not_active Application Discontinuation
- 2003-11-20 MA MA27408A patent/MA27027A1/fr unknown
- 2003-11-24 BG BG108382A patent/BG108382A/bg unknown
- 2003-11-24 NO NO20035204A patent/NO20035204D0/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| WO2002096463A1 (en) | 2002-12-05 |
| JP2005508861A (ja) | 2005-04-07 |
| CN1511042A (zh) | 2004-07-07 |
| EE200300585A (et) | 2004-04-15 |
| BG108382A (bg) | 2004-12-30 |
| OA12610A (en) | 2006-06-09 |
| MXPA03010162A (es) | 2004-03-10 |
| PL367085A1 (en) | 2005-02-21 |
| NZ529335A (en) | 2005-09-30 |
| CR7152A (es) | 2004-02-23 |
| IL158776A0 (en) | 2004-05-12 |
| KR20040007605A (ko) | 2004-01-24 |
| CZ20033150A3 (cs) | 2004-06-16 |
| NO20035204D0 (no) | 2003-11-24 |
| TNSN03123A1 (en) | 2005-12-23 |
| EP1395288A1 (en) | 2004-03-10 |
| AP2003002909A0 (en) | 2003-12-31 |
| PA8546001A1 (es) | 2003-12-30 |
| CA2446613A1 (en) | 2002-12-05 |
| MA27027A1 (fr) | 2004-12-20 |
| US20040147544A1 (en) | 2004-07-29 |
| SK14312003A3 (sk) | 2004-08-03 |
| HUP0400037A2 (hu) | 2004-04-28 |
| BR0209992A (pt) | 2004-04-06 |
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