AR128147A1 - Procedimiento para la preparación del ácido (5s)-[2-(4-carboxifenil)etil][2-(2-[3-cloro-4-(trifluorometil)bifenil-4-il]metoxifenil)etil]amino-5,6,7,8-tetrahidroquinolina-2-carboxílico y sus formas cristalinas para su uso como compuesto farmacéuticamente activo - Google Patents
Procedimiento para la preparación del ácido (5s)-[2-(4-carboxifenil)etil][2-(2-[3-cloro-4-(trifluorometil)bifenil-4-il]metoxifenil)etil]amino-5,6,7,8-tetrahidroquinolina-2-carboxílico y sus formas cristalinas para su uso como compuesto farmacéuticamente activoInfo
- Publication number
- AR128147A1 AR128147A1 ARP220103632A ARP220103632A AR128147A1 AR 128147 A1 AR128147 A1 AR 128147A1 AR P220103632 A ARP220103632 A AR P220103632A AR P220103632 A ARP220103632 A AR P220103632A AR 128147 A1 AR128147 A1 AR 128147A1
- Authority
- AR
- Argentina
- Prior art keywords
- ethyl
- acid
- monohydrate
- tetrahydroquinoline
- carboxyphenyl
- Prior art date
Links
- 239000002253 acid Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 238000002360 preparation method Methods 0.000 title abstract 2
- QUPDWYMUPZLYJZ-UHFFFAOYSA-N ethyl Chemical compound C[CH2] QUPDWYMUPZLYJZ-UHFFFAOYSA-N 0.000 title 2
- 150000001875 compounds Chemical class 0.000 title 1
- 150000004682 monohydrates Chemical group 0.000 abstract 6
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 2
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 201000006306 Cor pulmonale Diseases 0.000 abstract 1
- 208000011191 Pulmonary vascular disease Diseases 0.000 abstract 1
- 230000002612 cardiopulmonary effect Effects 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 230000002685 pulmonary effect Effects 0.000 abstract 1
- 238000010956 selective crystallization Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- 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
-
- 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
- A61P11/08—Bronchodilators
-
- 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
- A61P9/12—Antihypertensives
-
- 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
-
- 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)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
La presente invención se refiere a un proceso nuevo y mejorado para preparar ácido (5S)-{[2-(4-carboxifenil)etil][2-(2-{[3-cloro-4-(trifluorometil)bifenil-4-il]metoxi}fenil)etil]amino}-5,6,7,8-tetrahidroquinolin-2-carboxílico de fórmula (1) y a nuevas forma cristalinas de este, que es la forma pseudopolimórfica monohidrato I (1-M-I) o la forma pseudopolimórfica monohidrato II (1-M-II); además, la presente invención se refiere a un proceso de cristalización nuevo y selectivo para la preparación de la forma pseudopolimórfica monohidrato I (1-M-I) o la forma pseudopolimórfica monohidrato II (1-M-II), preferiblemente monohidrato I de fórmula (1-M-I) y a composiciones farmacéuticas que comprenden monohidrato I de fórmula (1-M-I) y a su uso para el tratamiento y/o la prevención de enfermedades, en particular para el tratamiento y/o la prevención de enfermedades pulmonares, cardiopulmonares y cardiovasculares.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP21218163 | 2021-12-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR128147A1 true AR128147A1 (es) | 2024-03-27 |
Family
ID=79185525
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP220103632A AR128147A1 (es) | 2021-12-29 | 2022-12-28 | Procedimiento para la preparación del ácido (5s)-[2-(4-carboxifenil)etil][2-(2-[3-cloro-4-(trifluorometil)bifenil-4-il]metoxifenil)etil]amino-5,6,7,8-tetrahidroquinolina-2-carboxílico y sus formas cristalinas para su uso como compuesto farmacéuticamente activo |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US12202805B2 (es) |
| EP (1) | EP4457215A1 (es) |
| JP (1) | JP2025502842A (es) |
| KR (1) | KR20240144177A (es) |
| CN (1) | CN118765272A (es) |
| AR (1) | AR128147A1 (es) |
| AU (1) | AU2022429647A1 (es) |
| CA (1) | CA3244893A1 (es) |
| IL (1) | IL313922A (es) |
| MX (1) | MX2024008172A (es) |
| TW (1) | TW202342012A (es) |
| WO (1) | WO2023126436A1 (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2023126436A1 (en) | 2021-12-29 | 2023-07-06 | Bayer Aktiengesellschaft | Process for preparing (5s)-{[2-(4-carboxyphenyl)ethyl] |2-(2-{|3-chloro-4'-(trifluoromethyl)biphenyl-4- yl]methoxy}phenyl)ethyl]aminol-5,6,7,8-tetrahydroquinoline-2-carboxylic acid and its crystalline forms for use as pharmaceutically active compound |
| AU2022424376A1 (en) | 2021-12-29 | 2024-07-04 | Bayer Aktiengesellschaft | Treatment of cardiopulmonary disorders |
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| SE8004002L (sv) | 1980-05-29 | 1981-11-30 | Arvidsson Folke Lars Erik | Terapeutiskt anvendbara tetralinderivat |
| IL65501A (en) | 1981-05-08 | 1986-04-29 | Astra Laekemedel Ab | 1-alkyl-2-aminotetralin derivatives,process for their preparation and pharmaceutical compositions containing them |
| DE3718317A1 (de) | 1986-12-10 | 1988-06-16 | Bayer Ag | Substituierte basische 2-aminotetraline |
| DE3719924A1 (de) | 1986-12-22 | 1988-06-30 | Bayer Ag | 8-substituierte 2-aminotetraline |
| JP2785879B2 (ja) | 1989-05-31 | 1998-08-13 | ジ・アップジョン・カンパニー | 治療学的に有用な2―アミノテトラリン誘導体 |
| FR2659853A1 (fr) | 1990-03-22 | 1991-09-27 | Midy Spa | Utilisation de derives 2-aminotetraliniques pour la preparation de medicaments destines a combattre les troubles de la motricite intestinale. |
| AU1867095A (en) | 1994-01-10 | 1995-08-01 | Technion Research & Development Foundation Ltd. | 1-aminoindan derivatives and compositions thereof |
| ATE255888T1 (de) | 1998-06-01 | 2003-12-15 | Ortho Mcneil Pharm Inc | Tetrahydronaphtalene verbindungen und deren verwendung zur behandlung von neurodegenerativen krankheiten |
| DE19834044A1 (de) | 1998-07-29 | 2000-02-03 | Bayer Ag | Neue substituierte Pyrazolderivate |
| DE19834047A1 (de) | 1998-07-29 | 2000-02-03 | Bayer Ag | Substituierte Pyrazolderivate |
| GB9827467D0 (en) | 1998-12-15 | 1999-02-10 | Zeneca Ltd | Chemical compounds |
| DE19943635A1 (de) | 1999-09-13 | 2001-03-15 | Bayer Ag | Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften |
| AR031176A1 (es) | 2000-11-22 | 2003-09-10 | Bayer Ag | Nuevos derivados de pirazolpiridina sustituidos con piridina |
| DE10109858A1 (de) | 2001-03-01 | 2002-09-05 | Bayer Ag | Neuartige halogensubstituierte Aminodicarbonsäurederivate |
| DE10109861A1 (de) | 2001-03-01 | 2002-09-05 | Bayer Ag | Neuartige seitenkettenhalogenierte Aminodicarbonsäurederivate |
| DE10109859A1 (de) | 2001-03-01 | 2002-09-05 | Bayer Ag | Neuartige Aminodicarbonsäurederivate |
| DE10110749A1 (de) | 2001-03-07 | 2002-09-12 | Bayer Ag | Substituierte Aminodicarbonsäurederivate |
| DE10110750A1 (de) | 2001-03-07 | 2002-09-12 | Bayer Ag | Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften |
| DE10220570A1 (de) | 2002-05-08 | 2003-11-20 | Bayer Ag | Carbamat-substituierte Pyrazolopyridine |
| AU2004231342A1 (en) | 2003-04-14 | 2004-11-04 | Vectura Ltd | Dry power inhaler devices and dry power formulations for enhancing dosing efficiency |
| US20050032873A1 (en) | 2003-07-30 | 2005-02-10 | Wyeth | 3-Amino chroman and 2-amino tetralin derivatives |
| WO2006104826A2 (en) | 2005-03-30 | 2006-10-05 | Merck & Co., Inc. | Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use |
| DE102005050377A1 (de) | 2005-10-21 | 2007-04-26 | Bayer Healthcare Ag | Heterocyclische Verbindungen und ihre Verwendung |
| WO2009023669A1 (en) | 2007-08-13 | 2009-02-19 | Janssen Pharmaceutica N.V. | Substituted 5,6,7,8-tetrahydroquinoline derivatives, compositions, and methods of use thereof |
| US8455638B2 (en) | 2007-09-06 | 2013-06-04 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| JP2011185957A (ja) | 2008-07-04 | 2011-09-22 | Sharp Corp | 偏光板、表示装置及びその製造方法 |
| EP2331498B1 (en) | 2008-08-19 | 2016-11-09 | Janssen Pharmaceutica NV | Cold menthol receptor antagonists |
| DE102010020553A1 (de) | 2010-05-14 | 2011-11-17 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 8-Alkoxy-2-aminotetralin-Derivate und ihre Verwendung |
| DE102010021637A1 (de) | 2010-05-26 | 2011-12-01 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung |
| EP2585055A1 (de) | 2010-06-25 | 2013-05-01 | Bayer Intellectual Property GmbH | Verwendung von stimulatoren und aktivatoren der löslichen guanylatzyklase zur behandlung von sichelzellanämie und konservierung von blutersatzstoffen |
| PH12013500055A1 (en) | 2010-07-09 | 2017-08-23 | Bayer Ip Gmbh | Ring-fused pyrimidines and triazines and use thereof for the treatment and/or prophylaxis of cardiovascular diseases |
| DE102010040233A1 (de) | 2010-09-03 | 2012-03-08 | Bayer Schering Pharma Aktiengesellschaft | Bicyclische Aza-Heterocyclen und ihre Verwendung |
| DE102010043379A1 (de) | 2010-11-04 | 2012-05-10 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 6-Fluor-1H-Pyrazolo[4,3-b]pyridine und ihre Verwendung |
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| CN104703964B (zh) | 2012-07-20 | 2017-04-12 | 拜耳制药股份公司 | 取代氨基茚满‑和氨基萘满甲酸及其用途 |
| LT2875003T (lt) | 2012-07-20 | 2017-02-27 | Bayer Pharma Aktiengesellschaft | Naujos 5-aminotetrahidrochinolin-2-karboksirūgštys ir jų panaudojimas |
| US9624214B2 (en) | 2012-11-05 | 2017-04-18 | Bayer Pharma Aktiengesellschaft | Amino-substituted imidazo[1,2-a]pyridinecarboxamides and their use |
| GB201305825D0 (en) | 2013-03-28 | 2013-05-15 | Vectura Ltd | New use |
| WO2019081456A1 (en) | 2017-10-24 | 2019-05-02 | Bayer Aktiengesellschaft | USE OF SGC ACTIVATORS AND STIMULATORS COMPRISING A BETA2 SUBUNIT |
| CA3183771A1 (en) | 2020-05-20 | 2021-11-25 | Bayer Aktiengesellschaft | Process of preparing butyl-(5s)-5-({2-[4-(butoxycarbonyl)phenyl]ethyl}[2-(2-{[3-chloro-4'-(trifluoromethyl)[biphenyl]-4-yl]methoxy}phenyl)ethyl]amino)-5,6,7,8-tetrahydroquinoline-2-carboxylate |
| CN118804741A (zh) | 2021-12-29 | 2024-10-18 | 拜耳股份公司 | 药物干粉吸入制剂 |
| AU2022424376A1 (en) | 2021-12-29 | 2024-07-04 | Bayer Aktiengesellschaft | Treatment of cardiopulmonary disorders |
| WO2023126436A1 (en) | 2021-12-29 | 2023-07-06 | Bayer Aktiengesellschaft | Process for preparing (5s)-{[2-(4-carboxyphenyl)ethyl] |2-(2-{|3-chloro-4'-(trifluoromethyl)biphenyl-4- yl]methoxy}phenyl)ethyl]aminol-5,6,7,8-tetrahydroquinoline-2-carboxylic acid and its crystalline forms for use as pharmaceutically active compound |
-
2022
- 2022-12-28 WO PCT/EP2022/087952 patent/WO2023126436A1/en not_active Ceased
- 2022-12-28 CA CA3244893A patent/CA3244893A1/en active Pending
- 2022-12-28 AU AU2022429647A patent/AU2022429647A1/en active Pending
- 2022-12-28 TW TW111150499A patent/TW202342012A/zh unknown
- 2022-12-28 CN CN202280092729.9A patent/CN118765272A/zh active Pending
- 2022-12-28 IL IL313922A patent/IL313922A/en unknown
- 2022-12-28 AR ARP220103632A patent/AR128147A1/es unknown
- 2022-12-28 JP JP2024539928A patent/JP2025502842A/ja active Pending
- 2022-12-28 KR KR1020247025651A patent/KR20240144177A/ko active Pending
- 2022-12-28 EP EP22844516.9A patent/EP4457215A1/en active Pending
-
2023
- 2023-11-10 US US18/506,737 patent/US12202805B2/en active Active
-
2024
- 2024-06-27 MX MX2024008172A patent/MX2024008172A/es unknown
- 2024-12-02 US US18/964,918 patent/US20250263381A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| US12202805B2 (en) | 2025-01-21 |
| AU2022429647A1 (en) | 2024-07-04 |
| EP4457215A1 (en) | 2024-11-06 |
| CA3244893A1 (en) | 2023-07-06 |
| CN118765272A (zh) | 2024-10-11 |
| US20240116874A1 (en) | 2024-04-11 |
| TW202342012A (zh) | 2023-11-01 |
| WO2023126436A1 (en) | 2023-07-06 |
| KR20240144177A (ko) | 2024-10-02 |
| MX2024008172A (es) | 2025-04-02 |
| US20250263381A1 (en) | 2025-08-21 |
| JP2025502842A (ja) | 2025-01-28 |
| IL313922A (en) | 2024-08-01 |
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