AU2010310612A1 - Process for preparing modulators of cystic fibrosis transmembrane conductance regulator - Google Patents

Process for preparing modulators of cystic fibrosis transmembrane conductance regulator Download PDF

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Publication number
AU2010310612A1
AU2010310612A1 AU2010310612A AU2010310612A AU2010310612A1 AU 2010310612 A1 AU2010310612 A1 AU 2010310612A1 AU 2010310612 A AU2010310612 A AU 2010310612A AU 2010310612 A AU2010310612 A AU 2010310612A AU 2010310612 A1 AU2010310612 A1 AU 2010310612A1
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Australia
Prior art keywords
compound
hci
coupling
pct
hcl
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Abandoned
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AU2010310612A
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AU2010310612A2 (en
Inventor
Narendra Bhalchandra Ambhaikar
Robert Hughes
Dennis James Hurley
Elaine Chungmin Lee
Benjamin Littler
Mehdi Numa
Stefanie Roeper
Urvi Sheth
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Publication date
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of AU2010310612A1 publication Critical patent/AU2010310612A1/en
Publication of AU2010310612A2 publication Critical patent/AU2010310612A2/en
Abandoned legal-status Critical Current

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    • 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
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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    • 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
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    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A—HUMAN NECESSITIES
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    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Emergency Medicine (AREA)
  • Otolaryngology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Psychiatry (AREA)
  • Gastroenterology & Hepatology (AREA)
AU2010310612A 2009-10-23 2010-10-21 Process for preparing modulators of cystic fibrosis transmembrane conductance regulator Abandoned AU2010310612A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US25463409P 2009-10-23 2009-10-23
US61/254,634 2009-10-23
PCT/US2010/053628 WO2011050215A1 (en) 2009-10-23 2010-10-21 Process for preparing modulators of cystic fibrosis transmembrane conductance regulator

Publications (2)

Publication Number Publication Date
AU2010310612A1 true AU2010310612A1 (en) 2012-06-14
AU2010310612A2 AU2010310612A2 (en) 2012-08-16

Family

ID=43530872

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2010310612A Abandoned AU2010310612A1 (en) 2009-10-23 2010-10-21 Process for preparing modulators of cystic fibrosis transmembrane conductance regulator

Country Status (16)

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US (4) US8344147B2 (enExample)
EP (1) EP2491018A1 (enExample)
JP (1) JP5789611B2 (enExample)
KR (1) KR20120104554A (enExample)
CN (1) CN102648182A (enExample)
AR (1) AR080065A1 (enExample)
AU (1) AU2010310612A1 (enExample)
BR (1) BR112012009583A2 (enExample)
CA (1) CA2778492A1 (enExample)
IL (1) IL219326A0 (enExample)
MX (1) MX2012004790A (enExample)
NZ (1) NZ600172A (enExample)
RU (1) RU2553989C2 (enExample)
TW (1) TWI475023B (enExample)
WO (1) WO2011050215A1 (enExample)
ZA (1) ZA201202915B (enExample)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1898221A (zh) 2003-09-06 2007-01-17 沃泰克斯药物股份有限公司 Atp－结合弹夹转运蛋白的调控剂
US7977322B2 (en) 2004-08-20 2011-07-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
HUE032540T2 (en) 2004-06-24 2017-09-28 Vertex Pharma Modulators of ATP-binding cassette transporters
ATE512145T1 (de) 2005-08-11 2011-06-15 Vertex Pharma Modulatoren des cystic fibrosis transmembrane conductance regulators
EP2395002B1 (en) 2005-11-08 2014-06-18 Vertex Pharmaceuticals Inc. Pharmaceutical composition containing a heterocyclic modulator of atp-binding cassette transporters.
CA2635581C (en) 2005-12-28 2017-02-28 Vertex Pharmaceuticals Incorporated Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
CN101395147B (zh) 2005-12-28 2013-05-29 弗特克斯药品有限公司 作为atp-结合盒转运蛋白调节剂用于治疗囊性纤维化的1-(苯并[d][1,3]间二氧杂环戊烯-5-基)-n-(苯基)环丙烷-甲酰胺衍生物及相关化合物
PT2674428T (pt) 2006-04-07 2016-07-14 Vertex Pharma Modeladores de transportadores de cassetes de ligação de atp
US7645789B2 (en) 2006-04-07 2010-01-12 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
USRE50453E1 (en) 2006-04-07 2025-06-10 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
NZ581259A (en) 2007-05-09 2012-07-27 Vertex Pharma Modulators of cystic fibrosis transmembrane conductance regulator
HUE028426T2 (en) 2007-08-24 2016-12-28 Vertex Pharma Isothiazolopyridinones for (inter alia) treating cystic fibrosis
ES2556080T3 (es) 2007-11-16 2016-01-12 Vertex Pharmaceuticals Incorporated Moduladores de isoquinolina de transportadores de casete de unión a ATP
UA102534C2 (xx) 2007-12-07 2013-07-25 Вертекс Фармасьютикалз Инкорпорейтед ТВЕРДА ФОРМА 3-(6-(1-(2,2-ДИФТОРБЕНЗО$d]$1,3]-ДІОКСОЛ-5-ІЛ)-ЦИКЛОПРОПАНКАРБОКСАМІДО)-3-МЕТИЛПІРИДИН-2-ІЛ)БЕНЗОЙНОЇ КИСЛОТИ (ВАРІАНТИ)$ТВЕРДАЯ ФОРМА 3-(6-(1-(2,2-ДИФТОРБЕНЗО$d]$1,3]-ДИОКСОЛ-5-ИЛ)-ЦИКЛОПРОПАНКАРБОКСАМИДО)-3-МЕТИЛПИРИДИН-2-ИЛ)БЕНЗОЙНОЙ КИСЛОТЫ (ВАРИАНТЫ)
UA95199C2 (en) * 2007-12-07 2011-07-11 Вертекс Фармасьютикалз Инкорпорейтед Aqueous formulation of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
LT2639223T (lt) 2007-12-07 2017-06-26 Vertex Pharmaceuticals Incorporated Cikloalkilkarboksiamido-piridino benzenkarboksirūgščių gamybos būdas
US20100036130A1 (en) 2007-12-07 2010-02-11 Vertex Pharmaceuticals Incorporated Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
NZ602030A (en) 2008-02-28 2014-02-28 Vertex Pharma Heteroaryl derivatives as cftr modulators
NZ616097A (en) 2008-03-31 2015-04-24 Vertex Pharma Pyridyl derivatives as cftr modulators
US20100074949A1 (en) 2008-08-13 2010-03-25 William Rowe Pharmaceutical composition and administration thereof
US12458635B2 (en) 2008-08-13 2025-11-04 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administrations thereof
MX2011003249A (es) * 2008-09-29 2011-05-19 Vertex Pharma Unidades de dosificacion del acido 3-(6-(1-(2,2-difluorobenzo[d][1 ,3]dioxol-5-il)ciclopropancarboxamido)-3-metilpiridin-2-il)benzoi co.
AR074060A1 (es) 2008-10-23 2010-12-22 Vertex Pharma Moduladores del regulador de conductancia transmembrana de la fibrosis quistica
NZ592504A (en) * 2008-10-23 2013-04-26 Vertex Pharma Solid forms of n-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide
EP2821400B1 (en) 2009-03-20 2017-09-27 Vertex Pharmaceuticals Incorporated Process for making modulators of cystic fibrosis transmembrane conductance regulator
KR20120083416A (ko) * 2009-09-17 2012-07-25 버텍스 파마슈티칼스 인코포레이티드 아자비시클릭 화합물의 제조 방법
US8389727B2 (en) * 2009-10-23 2013-03-05 Vertex Pharmaceuticals Incorporated Solid forms of N-(4-(7-Azabicyclo[2.2.1]Heptan-7-yl)-2-Trifluoromethyl)Phenyl)-4-Oxo-5-(Trifluoromethyl)-1,4-Dihydroquinoline-3-Carboxamide
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
CN102917692A (zh) 2010-04-07 2013-02-06 弗特克斯药品有限公司 3-(6-(1-(2,2-二氟苯并[d][1,3]二氧杂环戊烯-5-基)环丙甲酰胺基)-3-甲基吡啶-2-基)苯甲酸的药物组合物和其给药方法
NZ602795A (en) 2010-04-07 2015-01-30 Vertex Pharma Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
CA2797118C (en) 2010-04-22 2021-03-30 Vertex Pharmaceuticals Incorporated Process of producing cycloalkylcarboxamido-indole compounds
US8404849B2 (en) * 2010-05-20 2013-03-26 Vertex Pharmaceuticals Processes for producing modulators of cystic fibrosis transmembrane conductance regulator
US8563593B2 (en) 2010-06-08 2013-10-22 Vertex Pharmaceuticals Incorporated Formulations of (R)-1-(2,2-difluorobenzo[D] [1,3] dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide
AU2012335714B2 (en) 2011-11-08 2017-04-13 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
RU2692779C2 (ru) 2012-02-27 2019-06-27 Вертекс Фармасьютикалз Инкорпорейтед Фармацевтическая композиция и ее введения
US8674108B2 (en) 2012-04-20 2014-03-18 Vertex Pharmaceuticals Incorporated Solid forms of N-[2,4-bis(1,1-dimethylethy)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
AU2013290444B2 (en) 2012-07-16 2018-04-26 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of (R)-1-(2,2-diflurorbenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl) cyclopropanecarboxamide and administration thereof
BR112016010403A2 (pt) 2013-11-12 2017-08-08 Vertex Pharma Processo de preparação de composições farmacêuticas para o tratamento de doenças mediadas por cftr
CA2944140C (en) 2014-04-15 2022-10-04 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
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