PE20151602A1 - SALES DE DERIVADOS DE 2-AMINO-1-HIDROXIETIL-8-HIDROXIQUINOLIN-2(1H)-ONA QUE TIENEN ACTIVIDAD AGONISTA DEL RECEPTOR B(beta)2 ADRENERGICO ASI COMO ACTIVIDAD ANTAGONISTA DEL RECEPTOR MUSCARINICO M3 - Google Patents
SALES DE DERIVADOS DE 2-AMINO-1-HIDROXIETIL-8-HIDROXIQUINOLIN-2(1H)-ONA QUE TIENEN ACTIVIDAD AGONISTA DEL RECEPTOR B(beta)2 ADRENERGICO ASI COMO ACTIVIDAD ANTAGONISTA DEL RECEPTOR MUSCARINICO M3Info
- Publication number
- PE20151602A1 PE20151602A1 PE2015001752A PE2015001752A PE20151602A1 PE 20151602 A1 PE20151602 A1 PE 20151602A1 PE 2015001752 A PE2015001752 A PE 2015001752A PE 2015001752 A PE2015001752 A PE 2015001752A PE 20151602 A1 PE20151602 A1 PE 20151602A1
- Authority
- PE
- Peru
- Prior art keywords
- hydroxy
- amino
- methyl
- hydroxyquinolin
- derivatives
- Prior art date
Links
- 108060003345 Adrenergic Receptor Proteins 0.000 title 1
- 102000017910 Adrenergic receptor Human genes 0.000 title 1
- 102000007202 Muscarinic M3 Receptor Human genes 0.000 title 1
- 108010008405 Muscarinic M3 Receptor Proteins 0.000 title 1
- JKMZVSFWKKXBGL-UHFFFAOYSA-N NCC(O)N1C(C=CC2=CC=CC(=C12)O)=O Chemical class NCC(O)N1C(C=CC2=CC=CC(=C12)O)=O JKMZVSFWKKXBGL-UHFFFAOYSA-N 0.000 title 1
- 230000001270 agonistic effect Effects 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 230000000694 effects Effects 0.000 title 1
- -1 2-amino-1-hydroxyethyl Chemical class 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 abstract 1
- XJFCXBNWXYOKEI-LREBCSMRSA-N C(=O)(O)[C@H](O)[C@@H](O)C(=O)O.C(C)(=O)OC=1SC=CC1 Chemical compound C(=O)(O)[C@H](O)[C@@H](O)C(=O)O.C(C)(=O)OC=1SC=CC1 XJFCXBNWXYOKEI-LREBCSMRSA-N 0.000 abstract 1
- DNFICWUITCBMTO-UHFFFAOYSA-N C(CS(=O)(=O)O)S(=O)(=O)O.C(C)(=O)O Chemical compound C(CS(=O)(=O)O)S(=O)(=O)O.C(C)(=O)O DNFICWUITCBMTO-UHFFFAOYSA-N 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-N carbonic acid Chemical compound OC(O)=O BVKZGUZCCUSVTD-UHFFFAOYSA-N 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- GUTQMBQKTSGBPQ-UHFFFAOYSA-N dithiophen-2-ylmethanone Chemical group C=1C=CSC=1C(=O)C1=CC=CS1 GUTQMBQKTSGBPQ-UHFFFAOYSA-N 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- FFVJAVUSCJCRPT-UHFFFAOYSA-N thiophen-2-yl acetate Chemical compound CC(=O)OC1=CC=CS1 FFVJAVUSCJCRPT-UHFFFAOYSA-N 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero 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
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
- C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C309/05—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing at least two sulfo groups bound to the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C59/235—Saturated compounds containing more than one carboxyl group
- C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
- C07C59/255—Tartaric acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
- C07D275/04—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
- C07D275/06—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Otolaryngology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
La presente invencion se refiere a sales de adicion cristalinas y farmaceuticamente aceptables de (i) derivados de un acido sulfonico o hidroxicarboxilico o un derivado sulfimida, o un solvato farmaceuticamente aceptable del mismo y (ii) un derivado de 2-amino-1-hidroxietil-8-hidroxiquinolin-2(1H)-ona de formula (I); donde: R1 representa un atomo de hidrogeno o un grupo alquilo C1-C4; R2 y R3 independientemente representan un atomo de hidrogeno, un atomo de halogeno, etc; A representa un grupo alquileno C1-C4 opcionalmente sustituido con uno o mas grupos alquilo C1-C2; L representa un enlace directo, un grupo -NH(CO)-, etc. Las sales preferidas son: etanodisulfonato de hidroxi(di-2-tienil)acetato de trans-4-((3-(2-cloro-4-(((2R)-2-hidroxi-2-(8-hidroxi-2-oxo-1,2-dihidroquinolin-5-il)etilamino)metil)-5-metoxifenilamino)-3-oxopropil)(metil)amino)-ciclohexilo; disacarinato de 2-hidroxi-2,2-di(tiofen-2-il)acetato de trans-4-((2-(2-cloro-4-(((R)-2-hidroxi-2-(8-hidroxi-2-oxo-1,2-dihidroquinolin-5-il)etilamino)-metil)-5-metoxifenilcarbamoiloxi)etil)-(metil)amino)-ciclohexilo, y ; Sal L-tartrato de 2-hidroxi-2,2-di(tiofen-2-il)acetato de trans-4-((2-(2-cloro-4-(((R)-2-hidroxi-2-(8-hidroxi-2-oxo-1,2-dihidroquinolin-5-il)etilamino)-metil)-5-metoxifenilcarbamoiloxi)etil)-(metil)amino)ciclohexilo
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13382060 | 2013-02-27 | ||
| US201361804558P | 2013-03-22 | 2013-03-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20151602A1 true PE20151602A1 (es) | 2015-11-04 |
Family
ID=47827112
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2015001752A PE20151602A1 (es) | 2013-02-27 | 2014-02-27 | SALES DE DERIVADOS DE 2-AMINO-1-HIDROXIETIL-8-HIDROXIQUINOLIN-2(1H)-ONA QUE TIENEN ACTIVIDAD AGONISTA DEL RECEPTOR B(beta)2 ADRENERGICO ASI COMO ACTIVIDAD ANTAGONISTA DEL RECEPTOR MUSCARINICO M3 |
Country Status (33)
| Country | Link |
|---|---|
| US (1) | US9562039B2 (es) |
| EP (1) | EP2961407B1 (es) |
| JP (1) | JP6364429B2 (es) |
| KR (1) | KR102002668B1 (es) |
| CN (1) | CN105025897B (es) |
| AR (2) | AR094910A1 (es) |
| AU (1) | AU2014222645B2 (es) |
| BR (1) | BR112015020152B1 (es) |
| CA (1) | CA2901865C (es) |
| CL (1) | CL2015002402A1 (es) |
| CR (1) | CR20150427A (es) |
| DK (1) | DK2961407T3 (es) |
| DO (1) | DOP2015000197A (es) |
| EA (1) | EA028566B1 (es) |
| ES (1) | ES2674085T3 (es) |
| HR (1) | HRP20181097T1 (es) |
| HU (1) | HUE039303T2 (es) |
| IL (1) | IL240278B (es) |
| LT (1) | LT2961407T (es) |
| MX (2) | MX2015010680A (es) |
| MY (1) | MY180350A (es) |
| PE (1) | PE20151602A1 (es) |
| PH (1) | PH12015501754A1 (es) |
| PL (1) | PL2961407T3 (es) |
| PT (1) | PT2961407T (es) |
| RS (1) | RS57297B1 (es) |
| SG (1) | SG11201505868QA (es) |
| SI (1) | SI2961407T1 (es) |
| SM (1) | SMT201800254T1 (es) |
| TW (1) | TWI643853B (es) |
| UY (1) | UY35355A (es) |
| WO (1) | WO2014131851A1 (es) |
| ZA (1) | ZA201505374B (es) |
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| EP2386555A1 (en) | 2010-05-13 | 2011-11-16 | Almirall, S.A. | New cyclohexylamine derivatives having beta2 adrenergic agonist and m3 muscarinic antagonist activities |
| ITRM20110083U1 (it) | 2010-05-13 | 2011-11-14 | De La Cruz Jose Antonio Freire | Piastra per la costruzione di carrelli per aeroplani |
| EP2592078A1 (en) | 2011-11-11 | 2013-05-15 | Almirall, S.A. | New cyclohexylamine derivatives having beta2 adrenergic agonist and M3 muscarinic antagonist activities |
| MA38260B1 (fr) | 2012-12-18 | 2018-04-30 | Almirall Sa | Nouveaux dérivés de cyclohexyl et quinuclidinyl carbamate ayant une activité d'agoniste adrénergique beta2 et une activité d'antagoniste muscarinique m3 |
| US9757395B2 (en) | 2012-12-20 | 2017-09-12 | Otitopic Inc. | Dry powder inhaler and methods of use |
| US9757529B2 (en) | 2012-12-20 | 2017-09-12 | Otitopic Inc. | Dry powder inhaler and methods of use |
| CN117045653A (zh) | 2013-01-23 | 2023-11-14 | 奥尔德拉医疗公司 | 与毒性醛相关的疾病和治疗 |
| TWI643853B (zh) | 2013-02-27 | 2018-12-11 | 阿爾米雷爾有限公司 | 同時具有β2腎上腺素受體促效劑和M3毒蕈鹼受體拮抗劑活性之2-氨基-1-羥乙基-8-羥基喹啉-2(1H)-酮衍生物之鹽類 |
| AU2013388034B2 (en) | 2013-04-30 | 2019-08-15 | Aspeya US Inc. | Dry powder formulations and methods of use |
| TWI641373B (zh) | 2013-07-25 | 2018-11-21 | 阿爾米雷爾有限公司 | 具有蕈毒鹼受體拮抗劑和β２腎上腺素受體促效劑二者之活性的２－胺基－１－羥乙基－８－羥基喹啉－２（１Ｈ）－酮衍生物之鹽 |
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| TW201617343A (zh) | 2014-09-26 | 2016-05-16 | 阿爾米雷爾有限公司 | 具有β２腎上腺素促效劑及Ｍ３蕈毒拮抗劑活性之新穎雙環衍生物 |
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| KR102398639B1 (ko) * | 2017-06-20 | 2022-05-17 | (주) 성운파마코피아 | 아미드 유도체의 염 및 그 제조방법 |
| JP7493449B2 (ja) | 2017-09-22 | 2024-05-31 | ヴェクチュラ インコーポレイテッド | ステアリン酸マグネシウムを含む乾燥粉末組成物 |
| US10786456B2 (en) | 2017-09-22 | 2020-09-29 | Otitopic Inc. | Inhaled aspirin and magnesium to treat inflammation |
| WO2019075136A1 (en) | 2017-10-10 | 2019-04-18 | Aldeyra Therapeutics, Inc. | TREATMENT OF INFLAMMATORY DISORDERS |
| AU2019319740A1 (en) * | 2018-08-06 | 2021-03-25 | Aldeyra Therapeutics, Inc. | Polymorphic compounds and uses thereof |
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