[go: up one dir, main page]

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 activo

Info

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
Application number
ARP220103632A
Other languages
English (en)
Inventor
Britta Olenik
Birgit Keil
Bernd Rsler
Peter Fey
Heiko Schirmer
Guido Becker
Julian Egger
Clemens Bothe
Helene Faber
Original Assignee
Bayer Ag
Bayer Pharma AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bayer Ag, Bayer Pharma AG filed Critical Bayer Ag
Publication of AR128147A1 publication Critical patent/AR128147A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075Sprays 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline 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.
ARP220103632A 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 AR128147A1 (es)

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)

* Cited by examiner, † Cited by third party
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

Family Cites Families (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US8569339B2 (en) 2011-03-10 2013-10-29 Boehringer Ingelheim International Gmbh Soluble guanylate cyclase activators
IN2014MN00228A (es) 2011-08-12 2015-09-25 Nissan Chemical Ind Ltd
JP6118965B2 (ja) 2012-04-16 2017-04-26 トーアエイヨー株式会社 2環性化合物
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

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

Similar Documents

Publication Publication Date Title
AR128147A1 (es) 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
AR099134A1 (es) Procedimiento para la preparación de n-[(3-aminooxetán-3-il)metil]-2-(1,1-dioxo-3,5-dihidro-1,4-benzotiazepín-4-il)-6-metil-quinazolín-4-amina
AR087995A1 (es) Derivados de n-(4-{[6,7-bis(metiloxi)quinolin-4-il]oxi}fenil)-n-(4-fluorofenil)ciclopropan-1,1-dicarboxamida
ECSP14013173A (es) 3,5-diamino-6-cloro-n-(n-(4-(4-(2-(hexil(2,3,4,5,6-pentahidroxihexil)amino)etoxi)fenil)butil) carbamimidoil)pirazina-2-carboxamida
AR121483A1 (es) Hidrato cristalino de un compuesto inhibidor de jak
MX2022003984A (es) Compuestos heterociclicos antivirales.
CO6680645A2 (es) Inhibidores de oxadiazol de la producción de leucotrieno
MX2024014558A (es) Proceso para preparar acido 2-[[5-(3-clorofenil)-3-hidroxipiridina-2-carbonil]amino]acetico
PE20141322A1 (es) Ciclopropilaminas como inhibidores de desmetilasa 1 especifica de lisina
AR084011A1 (es) Compuestos nitrogenados heterociclicos utiles para el tratamiento de infecciones por el virus sincitial respiratorio (rsv), proceso para prepararlos y composiciones farmaceuticas que los contienen
UY30809A1 (es) Derivados de n-[3-[4-fenil)piperidin-1-carbonil]fenil]sulfonamidas sustituidas, procesos de preparacion y aplicaciones
BR112013011580A2 (pt) derivados de ácido bisfenil pentanoico substituído por amino como inibidores de nep
AR087668A1 (es) Derivados de oxazina y su uso en el tratamiento de enfermedades
UY39032A (es) Compuestos heterocíclicos como agentes antivirales
CO6251286A2 (es) Sales amino del acido [4, 6-bis(dimetilamino)-2-(4-(4-trifluorometil)benzamido)bencil)pirimidin-5-il]acetico, composiciones farmaceuticas de las mismas y sus usos para el tratamiento de enfermedades mediadas por crth-2
BR112021023770A2 (pt) Compostos de derivado de 1,3,4-oxadiazol como inibidor de histona desacetilase 6 e a composição farmacêutica que compreende os mesmos
AR128145A1 (es) Formulación farmacéutica de polvo seco para inhalación y proceso de preparación
CY1119452T1 (el) Μια μεθοδος παρασκευης 2-αιθοξυ-1-(2'-((υδροξυamino) ιμινομεθυλο) διφαινυλ-4-υλο) μεθυλο)-1η- βενζο (d) ιμιδαζολο-7-καρβοξυλικο οξυ και τους εστερες αυτου
MX383762B (es) Derivados de glutarimida, uso de los mismos, composición farmacéutica basada en los mismos y métodos para producir derivados de glutarimida.
AR083019A1 (es) Uso de un compuesto de [3-(1-(1h-imidazol-4-il)etil)-2-metilfenil]metanol para preparar un medicamento util para tratar enfermedades de la retina, articulo de fabricacion y composicion farmaceutica que lo comprenden
UY39642A (es) Compuestos heterocíclicos antivirales
CO2020006789A2 (es) Procedimiento para la preparación de (3s)-3-(4-cloro-3-{[(2s,3r)-2-(4-clorofenil)-4,4,4-trifluor-3-metilbutanoil]amino}fenil)-3-ácido ciclopropilpropanoico y su forma cristalina para uso como principio activo farmacéutico
MX2024008170A (es) Tratamiento de trastornos cardiopulmonares
EP4635494A3 (en) AMIDO HETERO-ROMATIC COMPOUNDS
CO6710902A2 (es) Inhibidores de oxadiazol de la producción de leucotrienos