JP5699090B2 - 嚢胞性線維症膜コンダクタンス調節因子のモジュレーター - Google Patents

嚢胞性線維症膜コンダクタンス調節因子のモジュレーター Download PDF

Info

Publication number
JP5699090B2
JP5699090B2 JP2011544487A JP2011544487A JP5699090B2 JP 5699090 B2 JP5699090 B2 JP 5699090B2 JP 2011544487 A JP2011544487 A JP 2011544487A JP 2011544487 A JP2011544487 A JP 2011544487A JP 5699090 B2 JP5699090 B2 JP 5699090B2
Authority
JP
Japan
Prior art keywords
optionally substituted
halo
independently
membered
hydrogen
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
JP2011544487A
Other languages
English (en)
Japanese (ja)
Other versions
JP2012514038A5 (https=
JP2012514038A (ja
Inventor
ヘイリー ビンチ，
ヘイリー ビンチ，
デニス ハーレー，
デニス ハーレー，
レブ ティー．ディー． ファニング，
レブ ティー．ディー． ファニング，
ピーター ディー．ジェイ． グルーテンヒュイス，
ピーター ディー．ジェイ． グルーテンヒュイス，
マーティン ボトフィールド，
マーティン ボトフィールド，
ゴアー， フレデリック バン
ゴアー， フレデリック バン
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals Inc
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 Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of JP2012514038A publication Critical patent/JP2012514038A/ja
Publication of JP2012514038A5 publication Critical patent/JP2012514038A5/ja
Application granted granted Critical
Publication of JP5699090B2 publication Critical patent/JP5699090B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/5415—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 ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
    • 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
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10—Laxatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
    • C07D279/16—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Otolaryngology (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2011544487A 2008-12-30 2009-12-21 嚢胞性線維症膜コンダクタンス調節因子のモジュレーター Expired - Fee Related JP5699090B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US14163108P 2008-12-30 2008-12-30
US61/141,631 2008-12-30
PCT/US2009/068939 WO2010078103A1 (en) 2008-12-30 2009-12-21 Modulators of cystic fibrosis transmembrane conductance regulator

Publications (3)

Publication Number Publication Date
JP2012514038A JP2012514038A (ja) 2012-06-21
JP2012514038A5 JP2012514038A5 (https=) 2013-02-07
JP5699090B2 true JP5699090B2 (ja) 2015-04-08

Family

ID=41667198

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2011544487A Expired - Fee Related JP5699090B2 (ja) 2008-12-30 2009-12-21 嚢胞性線維症膜コンダクタンス調節因子のモジュレーター

Country Status (4)

Country Link
US (3) US8367660B2 (https=)
EP (1) EP2382197B1 (https=)
JP (1) JP5699090B2 (https=)
WO (1) WO2010078103A1 (https=)

Families Citing this family (90)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2006111093A (ru) 2003-09-06 2007-10-27 Вертекс Фармасьютикалз Инкорпорейтед (Us) Модуляторы атр-связывающих кассетных транспортеров
CN101675928A (zh) * 2003-11-14 2010-03-24 沃泰克斯药物股份有限公司 可用作atp-结合弹夹转运蛋白调控剂的噻唑和噁唑
US7977322B2 (en) 2004-08-20 2011-07-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
RS56037B1 (sr) 2004-06-24 2017-09-29 Vertex Pharma Modulatori atp-vezujućih kasetnih transportera
US7999113B2 (en) 2005-08-11 2011-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
CN102775396B (zh) 2005-11-08 2014-10-08 沃泰克斯药物股份有限公司 Atp-结合弹夹转运蛋白的杂环调控剂
CA2856037C (en) 2005-12-28 2017-03-07 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
EP3219705B1 (en) 2005-12-28 2020-03-11 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of the amorphous form of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
US7671221B2 (en) * 2005-12-28 2010-03-02 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
EP2674428B1 (en) 2006-04-07 2016-04-06 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
USRE50453E1 (en) 2006-04-07 2025-06-10 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
US7645789B2 (en) 2006-04-07 2010-01-12 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
CN104447716A (zh) 2007-05-09 2015-03-25 沃泰克斯药物股份有限公司 Cftr调节剂
JP5389030B2 (ja) 2007-08-24 2014-01-15 バーテックス ファーマシューティカルズ インコーポレイテッド （特に）嚢胞性線維症の処置に有用なイソチアゾロピリジノン
CA2702094C (en) 2007-10-10 2018-05-01 Parion Sciences, Inc. Delivering osmolytes by nasal cannula
SI2578571T1 (sl) 2007-11-16 2016-01-29 Vertex Pharmaceuticals Incorporated Izokinolinski modulatorji prenašalcev z atp-vezavno kaseto
CN101998854A (zh) * 2007-12-07 2011-03-30 沃泰克斯药物股份有限公司 3-(6-(1-(2,2-二氟苯并[d][1,3]间二氧杂环戊烯-5-基)环丙烷甲酰氨基)-3-甲基吡啶-2-基)苯甲酸的制剂
EP3683218B1 (en) 2007-12-07 2024-09-18 Vertex Pharmaceuticals Incorporated Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid
MX365732B (es) * 2007-12-07 2019-06-12 Vertex Pharma Procesos para producir acidos cicloalquilcarboxamido-piridin benzoicos.
US20100036130A1 (en) 2007-12-07 2010-02-11 Vertex Pharmaceuticals Incorporated Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
NZ720282A (en) 2008-02-28 2017-12-22 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
AR073709A1 (es) 2008-09-29 2010-11-24 Vertex Pharma Unidades de dosis de acido 3-(6-(1-(2,2-difluorobenzeno (d) (1,3) dioxol-5-il) ciclopropancarboxamido)-3-metilpiridin-2-il) benzoico
EP2349263B1 (en) * 2008-10-23 2014-04-23 Vertex Pharmaceuticals Inc. Modulators of cystic fibrosis transmembrane conductance regulator
EP2382197B1 (en) 2008-12-30 2016-10-05 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
PL2408750T3 (pl) 2009-03-20 2016-02-29 Vertex Pharma Sposób otrzymywania modulatorów błonowego regulatora przewodnictwa swoistego dla mukowiscydozy
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
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
JP2013523833A (ja) 2010-04-07 2013-06-17 バーテックス ファーマシューティカルズ インコーポレイテッド ３−（６−（１−（２，２−ジフルオロベンゾ［ｄ］［１，３］ジオキソール−５−イル）シクロプロパンカルボキサミド）−３−メチルピリジン−２−イル）安息香酸の医薬組成物およびその投与
MX2012011655A (es) 2010-04-07 2012-11-23 Vertex Pharma Formas solidas de acido 3-(6-(1-(2,2-difluorobenzo [d][1-3]dioxol-5-il]ciclopropanocarboxamido)-3-metilpiridin-2-il) benzoico.
MX353408B (es) 2010-04-22 2018-01-11 Vertex Pharma Proceso para producir compuestos de cicloalquilcarboxamido-indol.
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
CN102675280B (zh) * 2011-03-09 2015-01-14 中国科学院上海有机化学研究所 含三氟甲基的吲哚酮类化合物及其制备方法和应用
BR112013023128A2 (pt) * 2011-03-14 2019-09-24 3M Innovative Properties Co artigos nanoestruturados
US8945605B2 (en) 2011-06-07 2015-02-03 Parion Sciences, Inc. Aerosol delivery systems, compositions and methods
EP2717855A4 (en) 2011-06-07 2014-11-12 Parion Sciences Inc Methods of Treatment
AR086745A1 (es) 2011-06-27 2014-01-22 Parion Sciences Inc 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
WO2013070961A1 (en) 2011-11-08 2013-05-16 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
NZ727015A (en) 2012-01-25 2017-12-22 Vertex Pharma Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
JP2015511583A (ja) 2012-02-27 2015-04-20 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ 薬学的組成物およびその投与
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
HUE039734T2 (hu) 2012-05-29 2019-01-28 Parion Sciences Inc Nátriumcsatorna-blokkoló aktivitású, dendrimerszerû amino-amid-származékok száraz szem és más nyálkahártya-megbetegedések kezelésére
AR092857A1 (es) 2012-07-16 2015-05-06 Vertex Pharma Composiciones farmaceuticas de (r)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-il)-n-(1-(2,3-dihidroxipropil)-6-fluoro-2-(1-hidroxi-2-metilpropan-2-il)-1h-indol-5-il)ciclopropancarboxamida y administracion de las mismas
CN108658876A (zh) 2012-12-17 2018-10-16 帕里昂科学公司 3,5-二氨基-6-氯-n-(n-(4-苯基丁基)甲脒基)吡嗪-2-甲酰胺化合物
ES2674665T3 (es) 2012-12-17 2018-07-03 Parion Sciences, Inc. Compuestos de 3,5-diamino-6-cloro-N-(N-(4-fenilbutilo)carbamimidoilo)-pirazina-2-carboxamida
CA2895512C (en) 2012-12-17 2021-10-19 Parion Sciences, Inc. Chloro-pyrazine carboxamide derivatives useful for the treatment of diseases favoured by insufficient mucosal hydration
AU2014349010C1 (en) 2013-11-12 2020-08-06 Vertex Pharmaceuticals Incorporated Process of preparing pharmaceutical compositions for the treatment of CFTR mediated diseases
RU2744460C2 (ru) 2014-04-15 2021-03-09 Вертекс Фармасьютикалз Инкорпорейтед Фармацевтические композиции для лечения заболеваний, опосредованных муковисцидозным трансмембранным регулятором проводимости
JP2016017049A (ja) * 2014-07-08 2016-02-01 国立研究開発法人国立長寿医療研究センター 新規ベンズオキサジン誘導体及びこれを含有する医薬
MA41051B1 (fr) 2014-10-06 2020-11-30 Vertex Pharma Modulateurs du régulateur de conductance transmembranaire de la mucoviscidose
CN107250113B (zh) 2014-10-07 2019-03-29 弗特克斯药品有限公司 囊性纤维化跨膜传导调节蛋白的调节剂的共晶
MX2017005663A (es) 2014-10-31 2018-03-01 Abbvie Sarl Tetrahidropiranos sustituidos y metodo de uso.
RU2691136C2 (ru) 2014-11-18 2019-06-11 Вертекс Фармасьютикалз Инкорпорейтед Способ проведения высокопроизводительной тестовой высокоэффективной жидкостной хроматографии
US10047051B2 (en) 2015-06-02 2018-08-14 Abbvie S.Á.R.L. Substituted pyridines and method of use
US9840513B2 (en) 2015-07-16 2017-12-12 Abbvie S.Á.R.L. Substituted tricyclics and method of use
TW201735769A (zh) 2015-10-09 2017-10-16 盧森堡商艾伯維公司 經取代之吡唑并［３，４－ｂ］吡啶－６－羧酸及使用方法
BR112018007161B1 (pt) 2015-10-09 2024-01-16 Galapagos Nv COMPOSTOS PIRAZOLO[3,4-b]PIRIDIN-6-CARBOXAMIDA N-SULFONILADA, COMPOSIÇÃO FARMACÊUTICA CONTENDO OS DITOS COMPOSTOS E USOS DOS MESMOS PARA TRATAR FIBROSE CÍSTICA
AU2017256172A1 (en) 2016-04-26 2018-09-06 AbbVie S.à.r.l. Modulators of cystic fibrosis transmembrane conductance regulator protein
EP3455203B1 (en) * 2016-05-12 2021-09-22 Research Triangle Institute Vinylogous phenethylamines as neurotransmitter releasers
US10138227B2 (en) 2016-06-03 2018-11-27 Abbvie S.Á.R.L. Heteroaryl substituted pyridines and methods of use
US9981910B2 (en) * 2016-10-07 2018-05-29 Abbvie S.Á.R.L. Substituted pyrrolidines and methods of use
US10399940B2 (en) 2016-10-07 2019-09-03 Abbvie S.Á.R.L. Substituted pyrrolidines and methods of use
MD3551622T2 (ro) 2016-12-09 2021-03-31 Vertex Pharma Modulator al regulatorului conductanței transmembranare în fibroză chistică, compoziții farmaceutice, metode de tratament și procedeu pentru fabricarea modulatorului
EP3558982A1 (en) 2016-12-20 2019-10-30 AbbVie S.À.R.L. Deuterated cftr modulators and methods of use
TW201831471A (zh) 2017-02-24 2018-09-01 盧森堡商艾伯維公司 囊腫纖化症跨膜傳導調節蛋白的調節劑及其使用方法
US11253509B2 (en) 2017-06-08 2022-02-22 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
MA49631A (fr) 2017-07-17 2020-05-27 Vertex Pharma Méthodes de traitement de la fibrose kystique
US10988454B2 (en) 2017-09-14 2021-04-27 Abbvie Overseas S.À.R.L. Modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use
EP3720849A2 (en) 2017-12-08 2020-10-14 Vertex Pharmaceuticals Incorporated Processes for making modulators of cystic fibrosis transmembrane conductance regulator
WO2019193062A1 (en) 2018-04-03 2019-10-10 Abbvie S.Á.R.L Substituted pyrrolidines and their use
WO2020048826A1 (en) 2018-09-03 2020-03-12 Bayer Aktiengesellschaft 5-substituted 1-oxa-3,9-diazaspiro[5.5]undecan-2-one compounds
US11345691B2 (en) 2019-06-03 2022-05-31 AbbVie Global Enterprises Ltd. Prodrug modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use
WO2021011327A1 (en) 2019-07-12 2021-01-21 Orphomed, Inc. Compound for treating cystic fibrosis
EP4058434A1 (en) 2019-11-12 2022-09-21 Genzyme Corporation 6-membered heteroarylaminosulfonamides for treating diseases and conditions mediated by deficient cftr activity
WO2021113809A1 (en) 2019-12-05 2021-06-10 Genzyme Corporation Arylamides and methods of use thereof
WO2021113806A1 (en) 2019-12-05 2021-06-10 Genzyme Corporation Arylamides and methods of use thereof
CR20230120A (es) 2020-08-07 2023-09-01 Vertex Pharma Moduladores del regulador de la conductancia transmembrana de la fibrosis quística
US12324802B2 (en) 2020-11-18 2025-06-10 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US20220213041A1 (en) 2021-01-06 2022-07-07 AbbVie Global Enterprises Ltd. Modulators of the Cystic Fibrosis Transmembrane Conductance Regulator Protein and Methods of Use
EP4274828A1 (en) 2021-01-06 2023-11-15 AbbVie Global Enterprises Ltd. Modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use
MX2024002519A (es) 2021-09-03 2024-05-27 Genzyme Corp Compuestos de indol y metodos de uso.
EP4396176A1 (en) 2021-09-03 2024-07-10 Genzyme Corporation Indole compounds and uses thereof in the treatement of cystic fibrosis
WO2024054851A1 (en) 2022-09-07 2024-03-14 Sionna Therapeutics Macrocyclic compounds, compositions and methods of using thereof
WO2024054845A1 (en) 2022-09-07 2024-03-14 Sionna Therapeutics Macrocycic compounds, compositions, and methods of using thereof
JP2025530153A (ja) 2022-09-07 2025-09-11 シオナ セラピューティクス インコーポレイテッド 大環状化合物、組成物、及びそれらの使用方法
WO2025132358A1 (en) 2023-12-21 2025-06-26 Galapagos Nv Novel compounds and pharmaceutical compositions thereof for the treatment of infectious diseases

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUP0301493A2 (hu) * 2000-03-09 2003-08-28 Ono Pharmaceutical Co., Ltd. Indolszármazékok, eljárás előállításukra és alkalmazásuk
DE102004028862A1 (de) * 2004-06-15 2005-12-29 Merck Patent Gmbh 3-Aminoindazole
RS56037B1 (sr) * 2004-06-24 2017-09-29 Vertex Pharma Modulatori atp-vezujućih kasetnih transportera
EP2147914B1 (en) * 2007-04-24 2014-06-04 Shionogi&Co., Ltd. Aminodihydrothiazine derivatives substituted with cyclic groups
JP5686596B2 (ja) * 2007-05-25 2015-03-18 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ 嚢胞性線維症膜貫通コンダクタンス制御因子の調節因子
WO2009079008A1 (en) 2007-12-19 2009-06-25 Yangbo Feng Benzopyrans and analogs as rho kinase inhibitors
CA2707441A1 (en) 2008-01-09 2009-07-16 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
CN102186841A (zh) * 2008-10-22 2011-09-14 盐野义制药株式会社 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物
US20100152160A1 (en) 2008-12-12 2010-06-17 Khamrai Uttam Novel benzodioxane and benzoxazine derivatives useful as cc chemokine receptor ligands
EP2382197B1 (en) 2008-12-30 2016-10-05 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator

Also Published As

Publication number Publication date
US8367660B2 (en) 2013-02-05
US8633189B2 (en) 2014-01-21
US20100168094A1 (en) 2010-07-01
US8999976B2 (en) 2015-04-07
US20140235625A1 (en) 2014-08-21
EP2382197B1 (en) 2016-10-05
WO2010078103A1 (en) 2010-07-08
EP2382197A1 (en) 2011-11-02
US20130196983A1 (en) 2013-08-01
JP2012514038A (ja) 2012-06-21

Similar Documents

Publication Publication Date Title
JP5699090B2 (ja) 嚢胞性線維症膜コンダクタンス調節因子のモジュレーター
US9051324B2 (en) Modulators of cystic fibrosis transmembrane conductance regulator
JP5686596B2 (ja) 嚢胞性線維症膜貫通コンダクタンス制御因子の調節因子
KR101955863B1 (ko) 낭성 섬유증 막횡단 전도도 조절자의 조정자의 제조 방법
JP5645833B2 (ja) 嚢胞性線維症膜コンダクタンス制御因子の修飾因子
JP5389030B2 (ja) （特に）嚢胞性線維症の処置に有用なイソチアゾロピリジノン
JP2013513617A (ja) Ａｔｐ結合カセット輸送体のモジュレーターとしての４−オキソ−１ｈ−キノリン−３−カルボキサミド
US20190210973A1 (en) Compounds and methods for treatment of cystic fibrosis
HK1146934B (en) Modulators of cystic fibrosis transmembrane conductance regulator
HK1139666B (en) Modulators of cystic fibrosis transmembrane conductance regulator
HK1173727A (en) 4-oxo-1h-quinoline-3-carboxamides as modulators of atp-binding cassette transporters

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20121212

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20121212

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20140514

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20140807

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20150121

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20150216

R150 Certificate of patent or registration of utility model

Ref document number: 5699090

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees