AR089505A1 - Esteres de quinuclidina de acido 1-azaheterociclilacetico que pueden usarse como agentes antimuscarinicos, proceso para elaborarlos y composiciones medicinales que los comprenden - Google Patents
Esteres de quinuclidina de acido 1-azaheterociclilacetico que pueden usarse como agentes antimuscarinicos, proceso para elaborarlos y composiciones medicinales que los comprendenInfo
- Publication number
- AR089505A1 AR089505A1 ARP120105029A ARP120105029A AR089505A1 AR 089505 A1 AR089505 A1 AR 089505A1 AR P120105029 A ARP120105029 A AR P120105029A AR P120105029 A ARP120105029 A AR P120105029A AR 089505 A1 AR089505 A1 AR 089505A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- heteroaryl
- aryl
- cycloalkyl
- Prior art date
Links
- 239000002253 acid Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title abstract 2
- 239000003149 muscarinic antagonist Substances 0.000 title 1
- SBYHFKPVCBCYGV-UHFFFAOYSA-N quinuclidine Chemical compound C1CC2CCN1CC2 SBYHFKPVCBCYGV-UHFFFAOYSA-N 0.000 title 1
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 6
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 3
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 3
- 125000004414 alkyl thio group Chemical group 0.000 abstract 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 3
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- -1 CO2R3 Chemical group 0.000 abstract 2
- 125000004644 alkyl sulfinyl group Chemical group 0.000 abstract 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 2
- 125000001589 carboacyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000006272 (C3-C7) cycloalkyl 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
- 102000017925 CHRM3 Human genes 0.000 abstract 1
- 101150060249 CHRM3 gene Proteins 0.000 abstract 1
- 150000001450 anions Chemical class 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 208000023504 respiratory system disease Diseases 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
-
- 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
- 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
- A61K31/495—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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Compuestos de fórmula (1), que pueden actuar como antagonistas selectivos de los receptores M3, proceso para elaborarlos, composición que los comprende y su uso en la terapia. Estos compuestos pueden usarse para tratar enfermedades respiratorias como el asma o la COPD, entre otras. Reivindicación 1: Un quinuclidinéster de ácido 1-azaheterociclilacético caracterizado porque es de fórmula general (1) donde: A puede ser una unión simple, unión doble, O, S, SO, SO₂, NR³, C(R³)R⁴, CO, C(O)N(R³), N(R³)C(O)O, SO₂N(R³), N(R³)C(O), OC(O)N(R³), N(R³)SO₂, C(R³)=C(R⁴) y C(R³)-(CH₂)-C(R⁴); m es un entero entre 1 y 4; n es 0 o un entero entre 1 y 4; R¹ se selecciona entre el grupo que consiste en alquilo C₁₋₁₀, arilo, cicloalquilo C₃₋₈, heteroarilo, aril-alquilo C₁₋₆ y heteroaril-alquilo C₁₋₆, opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en átomos de halógeno, OH, oxo (=O), SH, NO₂, CN, CON(R³)₂, COOH, CO₂R³, CF₃, alcoxicarbonilo C₁₋₁₀, alquilsulfanilo C₁₋₁₀, alquilsulfinilo C₁₋₁₀, alquilsulfonilo C₁₋₁₀, alquilo C₁₋₁₀, alcoxilo C₁₋₁₀, ariloxi y heteroarilo; X⁻ es un anión fisiológicamente aceptable; R² es un grupo de fórmula: ---(CH₂)ₚ---P---(CH₂)q---W donde p es 0 o un entero entre 1 y 4; q es 0 o un entero entre 1 y 4; P se encuentra ausente o se selecciona entre el grupo que consiste en O, S, SO, SO₂, CO, NR³, CH=CH, N(R³)SO₂, N(R³)COO, N(R³)C(O), SO₂N(R³), CO(O)N(R³) y C(O)N(R³); W se selecciona entre el grupo que consiste en H, alquilo C₁₋₁₀, alcoxilo C₁₋₁₀, cicloalquilo C₃₋₈, arilo, heteroarilo, heterocicloalquilo C₅₋₁₀, opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en átomos de halógeno, OH, oxo (=O), SH, NO₂, CN, CON(R³)₂, COOH, NH₂, NHCOR³, CO₂R³, alcoxicarbonilo C₁₋₁₀, alquilsulfanilo C₁₋₁₀, alquilsulfinilo C₁₋₁₀, alquilsulfonilo C₁₋₁₀, alquilo C₁₋₁₀, alcoxilo C₁₋₁₀, alcanoilo C₁₋₁₀ y arilo; R³ y R⁴ se seleccionan en forma independiente entre el grupo que consiste en H, átomos de halógeno, CONH₂, alquilo C₁₋₁₀, alquinilo C₂₋₆, alquenilo C₂₋₆, alcanoilo C₁₋₁₀, cicloalquilo C₃₋₈, heteroarilo, y arilo opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en átomos de halógeno, OH, oxo (=O), SH, NO₂, CN, CONH₂, COOH, alcoxicarbonilo C₁₋₁₀, alquilsulfanilo C₁₋₁₀, alquilsulfinilo C₁₋₁₀, alquilsulfonilo C₁₋₁₀, alquilo C₁₋₁₀, alcoxilo C₁₋₁₀ y cicloalquilo C₃₋₇.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11196173 | 2011-12-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR089505A1 true AR089505A1 (es) | 2014-08-27 |
Family
ID=47603538
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120105029A AR089505A1 (es) | 2011-12-30 | 2012-12-27 | Esteres de quinuclidina de acido 1-azaheterociclilacetico que pueden usarse como agentes antimuscarinicos, proceso para elaborarlos y composiciones medicinales que los comprenden |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US8748613B2 (es) |
| EP (1) | EP2797910B1 (es) |
| KR (1) | KR20140105746A (es) |
| CN (1) | CN104011043B (es) |
| AR (1) | AR089505A1 (es) |
| BR (1) | BR112014013179A2 (es) |
| CA (1) | CA2862008A1 (es) |
| HK (1) | HK1200165A1 (es) |
| RU (1) | RU2628082C2 (es) |
| WO (1) | WO2013098145A1 (es) |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE569710A (es) | 1957-07-25 | |||
| DK1345937T3 (da) | 2000-12-22 | 2006-01-16 | Almirall Prodesfarma Ag | Quinuclidincarbamatderivater og deres anvendelse som M3-antagonister |
| JP4505227B2 (ja) | 2001-12-20 | 2010-07-21 | キエシ・フアルマチエウテイチ・ソチエタ・ペル・アチオニ | １−アルキル−１−アゾニアビシクロ［２．２．２］オクタンカルバメート誘導体およびムスカリンレセプターアンタゴニストとしてのそれらの使用 |
| AR044134A1 (es) * | 2003-05-02 | 2005-08-24 | Novartis Ag | Derivados de quinuclidina, metodo de preparacion y composiciones farmaceuticas. |
| EP1882691A1 (en) | 2006-07-26 | 2008-01-30 | CHIESI FARMACEUTICI S.p.A. | Quinuclidine derivatives as M3 antagonists |
| CA2672446A1 (en) * | 2006-12-19 | 2008-06-26 | Astrazeneca Ab | Quinuclidinol derivatives as muscarinic receptor antagonists |
| WO2009153536A1 (en) | 2008-06-17 | 2009-12-23 | Argenta Discovery Limited | 1-aza-bicyclo [2.2.2] octane derivatives useful as muscarinic receptor antagonists |
| EP2154136A1 (en) | 2008-08-08 | 2010-02-17 | CHIESI FARMACEUTICI S.p.A. | Quinuclidine carbonate derivatives and medicinal compositions thereof |
| EP2206712A1 (en) | 2008-12-23 | 2010-07-14 | CHIESI FARMACEUTICI S.p.A. | "Alkaloid aminoester derivatives and medicinal composition thereof" |
| BR112012032333A2 (pt) | 2010-06-22 | 2016-11-08 | Chiesi Farma Spa | composto, uso de um composto, composição farmacêutica, combinação de um composto e dispositivo |
| EP2585458B1 (en) | 2010-06-22 | 2015-01-07 | Chiesi Farmaceutici S.p.A. | Alkaloid aminoester derivatives and medicinal compositions thereof |
| SG186427A1 (en) | 2010-06-22 | 2013-01-30 | Chiesi Farma Spa | Dry powder formulation comprising an antimuscarinic drug |
| KR20130087405A (ko) * | 2010-06-22 | 2013-08-06 | 키에시 파르마슈티시 엣스. 피. 에이. | 알칼로이드 아미노에스테르 유도체 및 이의 의약 조성물 |
| EP2630145A1 (en) | 2010-10-20 | 2013-08-28 | Chiesi Farmaceutici S.p.A. | Carbonate derivatives for the treatment of cough |
| WO2012069275A1 (en) | 2010-11-26 | 2012-05-31 | Chiesi Farmaceutici S.P.A. | Glycine derivatives and their use as muscarinic receptor antagonists |
| EP2702041A1 (en) | 2011-04-29 | 2014-03-05 | Chiesi Farmaceutici S.p.A. | Alkaloid ester and carbamate derivatives and medicinal compositions thereof |
-
2012
- 2012-12-19 WO PCT/EP2012/076071 patent/WO2013098145A1/en active Application Filing
- 2012-12-19 CN CN201280064205.5A patent/CN104011043B/zh not_active Expired - Fee Related
- 2012-12-19 BR BR112014013179A patent/BR112014013179A2/pt not_active Application Discontinuation
- 2012-12-19 EP EP12818780.4A patent/EP2797910B1/en active Active
- 2012-12-19 RU RU2014126064A patent/RU2628082C2/ru active
- 2012-12-19 KR KR1020147015688A patent/KR20140105746A/ko not_active Application Discontinuation
- 2012-12-19 CA CA2862008A patent/CA2862008A1/en not_active Abandoned
- 2012-12-27 AR ARP120105029A patent/AR089505A1/es unknown
- 2012-12-28 US US13/729,388 patent/US8748613B2/en active Active
-
2015
- 2015-01-16 HK HK15100541.7A patent/HK1200165A1/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| EP2797910B1 (en) | 2015-09-16 |
| RU2014126064A (ru) | 2016-02-20 |
| CA2862008A1 (en) | 2013-07-04 |
| EP2797910A1 (en) | 2014-11-05 |
| US8748613B2 (en) | 2014-06-10 |
| RU2628082C2 (ru) | 2017-08-14 |
| BR112014013179A2 (pt) | 2017-06-13 |
| KR20140105746A (ko) | 2014-09-02 |
| HK1200165A1 (en) | 2015-07-31 |
| US20130172302A1 (en) | 2013-07-04 |
| CN104011043A (zh) | 2014-08-27 |
| CN104011043B (zh) | 2016-11-16 |
| WO2013098145A1 (en) | 2013-07-04 |
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| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |