AU2017248253B2 - Silicone atoms containing ivacaftor analogues - Google Patents

Silicone atoms containing ivacaftor analogues Download PDF

Info

Publication number
AU2017248253B2
AU2017248253B2 AU2017248253A AU2017248253A AU2017248253B2 AU 2017248253 B2 AU2017248253 B2 AU 2017248253B2 AU 2017248253 A AU2017248253 A AU 2017248253A AU 2017248253 A AU2017248253 A AU 2017248253A AU 2017248253 B2 AU2017248253 B2 AU 2017248253B2
Authority
AU
Australia
Prior art keywords
compound
disease
tert
cftr
mmol
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.)
Active
Application number
AU2017248253A
Other languages
English (en)
Other versions
AU2017248253A1 (en
Inventor
Cecilia M. Bastos
Benito Munoz
Daniel Parks
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.)
Kineta Inc
Original Assignee
Proteostasis Therapeutics 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 Proteostasis Therapeutics Inc filed Critical Proteostasis Therapeutics Inc
Publication of AU2017248253A1 publication Critical patent/AU2017248253A1/en
Application granted granted Critical
Publication of AU2017248253B2 publication Critical patent/AU2017248253B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • C07D215/54Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56Carbon 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/695Silicon compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10Laxatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/0803Compounds with Si-C or Si-Si linkages
    • C07F7/081Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Psychiatry (AREA)
  • Otolaryngology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
AU2017248253A 2016-04-07 2017-04-07 Silicone atoms containing ivacaftor analogues Active AU2017248253B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662319439P 2016-04-07 2016-04-07
US62/319,439 2016-04-07
PCT/US2017/026579 WO2017177124A1 (en) 2016-04-07 2017-04-07 Silicone atoms containing ivacaftor analogues

Publications (2)

Publication Number Publication Date
AU2017248253A1 AU2017248253A1 (en) 2018-10-18
AU2017248253B2 true AU2017248253B2 (en) 2021-07-29

Family

ID=58549338

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2017248253A Active AU2017248253B2 (en) 2016-04-07 2017-04-07 Silicone atoms containing ivacaftor analogues

Country Status (16)

Country Link
US (5) US10662207B2 (enExample)
EP (1) EP3440057B1 (enExample)
JP (1) JP7061076B2 (enExample)
KR (1) KR102448404B1 (enExample)
CN (1) CN109563047A (enExample)
AR (1) AR108203A1 (enExample)
AU (1) AU2017248253B2 (enExample)
BR (1) BR112018070747B1 (enExample)
CA (1) CA3019663C (enExample)
IL (1) IL262030B (enExample)
MA (1) MA43775A (enExample)
MX (1) MX386698B (enExample)
NZ (1) NZ746793A (enExample)
SA (1) SA518400164B1 (enExample)
SG (1) SG11201808682XA (enExample)
WO (1) WO2017177124A1 (enExample)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3798214B1 (en) 2014-10-06 2022-09-14 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US10548878B2 (en) 2015-07-24 2020-02-04 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods of increasing CFTR activity
NZ741093A (en) 2015-10-06 2022-12-23 Proteostasis Therapeutics Inc Compounds, compositions, and methods for modulating cftr
BR112018070747B1 (pt) 2016-04-07 2024-01-09 Proteostasis Therapeutics, Inc Átomos de silicone contendo análogos de ivacaftor, composições farmacêuticas e usos terapêuticos
EP3472156B1 (en) 2016-06-21 2023-06-07 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing cftr activity
SG10201913595YA (en) 2016-09-30 2020-02-27 Vertex Pharma Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
MA49235B1 (fr) * 2016-12-09 2021-02-26 Vertex Pharma Modulateur de régulateur de conductance transmembranaire de fibrose kystique, compositions pharmaceutiques, procédés de traitement et procédé de fabrication du modulateur
EP3634402B1 (en) 2017-06-08 2026-01-21 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
JP2020525446A (ja) * 2017-06-21 2020-08-27 ザ・ジョンズ・ホプキンス・ユニバーシティ 常染色体優性多発性嚢胞腎疾患を治療するための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
BR112020000941A2 (pt) 2017-07-17 2020-07-21 Vertex Pharmaceuticals Incorporated métodos de tratamento para fibrose cística
TWI799435B (zh) 2017-08-02 2023-04-21 美商維泰克斯製藥公司 製備化合物之製程
US20210369749A1 (en) * 2017-10-06 2021-12-02 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing cftr activity
IL273831B2 (en) 2017-10-19 2024-10-01 Vertex Pharma Crystalline forms and compositions of cftr modulators
CN111757874B (zh) 2017-12-08 2024-03-08 弗特克斯药品有限公司 用于制备囊性纤维化跨膜传导调节因子的调节剂的方法
TWI810243B (zh) 2018-02-05 2023-08-01 美商維泰克斯製藥公司 用於治療囊腫纖化症之醫藥組合物
EP3752510B1 (en) 2018-02-15 2022-12-07 Vertex Pharmaceuticals Incorporated Macrocycles as modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions thereof, their use in the treatment of cycstic fibrosis, and process for making them
WO2019195739A1 (en) 2018-04-05 2019-10-10 Alexander Russell Abela Modulators of cystic fibrosis transmembrane conductance regulator
US11414439B2 (en) 2018-04-13 2022-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
WO2020006269A1 (en) 2018-06-27 2020-01-02 Proteostasis Therapeutics, Inc. Proteasome activity enhancing compounds
CN109663129B (zh) * 2019-02-27 2021-05-11 四川大学华西第二医院 扩张型心肌病治疗药物及其应用
TWI848092B (zh) 2019-04-03 2024-07-11 美商維泰克斯製藥公司 囊腫纖維化跨膜傳導調節蛋白調節劑
TWI867024B (zh) 2019-08-14 2024-12-21 美商維泰克斯製藥公司 囊腫纖維化跨膜傳導調節蛋白之調節劑
TWI899097B (zh) 2019-08-14 2025-10-01 美商維泰克斯製藥公司 製備cftr調節劑之方法
KR20220064366A (ko) 2019-08-14 2022-05-18 버텍스 파마슈티칼스 인코포레이티드 Cftr 조절제의 결정질 형태
CA3188787A1 (en) 2020-08-13 2022-02-17 Vertex Pharmaceuticals Incorporated Crystalline forms of cftr modulators
CA3204725A1 (en) 2020-12-10 2022-06-16 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
CN116425642B (zh) * 2023-04-06 2025-06-10 浙江科聚生物医药有限公司 2-甲氧基-4-氟-5-胺基苯酚的制备方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012158885A1 (en) * 2011-05-18 2012-11-22 Concert Pharmaceuticals Inc. Deuterated derivatives of ivacaftor
US20140073667A1 (en) * 2011-05-18 2014-03-13 Adam J. Morgan Deuterated cftr potentiators

Family Cites Families (82)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3812225A1 (de) 1988-04-13 1989-10-26 Basf Ag Isoxazol(isothiazol)-5-carbonsaeureamide
CA2201478A1 (en) 1995-08-02 1997-02-13 J. Uriach & Cia S.A. New carboxamides with antifungal activity
ATE243204T1 (de) 1995-08-24 2003-07-15 Basf Ag Isoxazole- und isothiazole-5-carboxamid derivate, deren herstellung und deren verwendung als herbizide
PT957099E (pt) 1998-04-15 2003-02-28 Pfizer Prod Inc Carboxamidas heterociclicas
AU2001273040A1 (en) 2000-06-27 2002-01-08 Du Pont Pharmaceuticals Company Factor xa inhibitors
JP4901102B2 (ja) 2002-05-03 2012-03-21 エクセリクシス, インク. プロテインキナーゼモジュレーターおよびその使用方法
AU2004279855A1 (en) 2003-10-08 2005-04-21 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters containing cycloalkyl or pyranyl groups
EP1682127B1 (en) 2003-11-14 2009-07-29 Vertex Pharmaceuticals Incorporated Thiazoles and oxazoles useful as modulators of atp-binding cassette transporters
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
CA2565965A1 (en) 2004-05-06 2006-07-27 Plexxikon, Inc. Pde4b inhibitors and uses therefor
SE0401969D0 (sv) 2004-08-02 2004-08-02 Astrazeneca Ab Piperidine derivatives
US20060100226A1 (en) 2004-09-10 2006-05-11 Sikorski James A 2-Thiopyrimidinones as therapeutic agents
DE102004051277A1 (de) 2004-10-21 2006-04-27 Merck Patent Gmbh Heterocyclische Carbonylverbindungen
JP2006176443A (ja) 2004-12-22 2006-07-06 Shionogi & Co Ltd メラニン凝集ホルモン受容体アンタゴニスト
DE602006018301D1 (de) 2005-06-22 2010-12-30 Pfizer Prod Inc Histamin-3-rezeptorantagonisten
JP4822406B2 (ja) 2005-09-26 2011-11-24 ルネサスエレクトロニクス株式会社 表示制御駆動装置および表示システム
WO2007075896A2 (en) 2005-12-22 2007-07-05 Kemia, Inc. Heterocyclic cytokine inhibitors
KR101394245B1 (ko) 2005-12-30 2014-05-14 에스케이바이오팜 주식회사 아이속사졸 유도체 및 이의 용도
WO2007086584A1 (ja) 2006-01-30 2007-08-02 Meiji Seika Kaisha, Ltd. 新規FabKおよびFabI/K阻害剤
TW200815351A (en) 2006-05-02 2008-04-01 Astrazeneca Ab Novel compounds
WO2008046072A2 (en) 2006-10-13 2008-04-17 The Board Of Regents Of The University Of Texas System Chemical inducers of neurogenesis
US8193225B2 (en) 2006-10-13 2012-06-05 The Board Of Regents Of The University Of Texas System Isoxazole amides, derivatives and methods of chemical induction of neurogenesis
US7678792B2 (en) 2006-10-20 2010-03-16 Irm Llc Compositions and methods for modulating c-kit and PDGFR receptors
WO2008070739A1 (en) 2006-12-06 2008-06-12 Cytokinetics, Inc. Ksp activators
JP5311075B2 (ja) 2007-06-29 2013-10-09 エスケー バイオファーマスティカルズ カンパニー リミテッド イソキサゾール誘導体を含む、再狭窄の予防及び治療のための医薬組成物
WO2009011850A2 (en) 2007-07-16 2009-01-22 Abbott Laboratories Novel therapeutic compounds
US8211927B2 (en) 2007-08-02 2012-07-03 MSD, Oss B.V. 5-phenyl-isoxazole-3-carboxamide derivatives as TRPV1 modulators
US8642660B2 (en) 2007-12-21 2014-02-04 The University Of Rochester Method for altering the lifespan of eukaryotic organisms
US8236838B2 (en) 2008-04-21 2012-08-07 Institute For Oneworld Health Compounds, compositions and methods comprising isoxazole derivatives
US20090318429A1 (en) 2008-04-28 2009-12-24 Institute For Oneworld Health Compounds, Compositions and Methods Comprising Heteroaromatic Derivatives
US20120095002A1 (en) 2009-02-04 2012-04-19 N.V. Organon Isoxazole-5-carboxamide derivatives
BRPI1008974A2 (pt) 2009-03-11 2017-06-06 Kyorin Seiyaku Kk composto, composição farmacêutica, e, método para tratar, prevenir ou melhorar uma doença mediada com gsk-3
MX384179B (es) * 2009-03-20 2025-03-14 Vertex Pharma Proceso para producir moduladores del regulador de conductancia transmembrana de fibrosis quística.
GB0910003D0 (en) 2009-06-11 2009-07-22 Univ Leuven Kath Novel compounds for the treatment of neurodegenerative diseases
IN2012DN00352A (enExample) 2009-06-16 2015-08-21 Bikam Pharmaceuticals Inc
WO2011008931A2 (en) 2009-07-15 2011-01-20 Cystic Fibrosis Foundation Therapeutics, Inc. Arylpyrimidine compounds and combination therapy comprising same for treating cystic fibrosis & related disorders
US9212177B2 (en) 2009-08-05 2015-12-15 Versitech Limited Antiviral compounds and methods of making and using thereof
GB2474120B (en) 2009-10-01 2011-12-21 Amira Pharmaceuticals Inc Compounds as Lysophosphatidic acid receptor antagonists
US8569899B2 (en) 2009-12-30 2013-10-29 Stmicroelectronics, Inc. Device and method for alignment of vertically stacked wafers and die
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
WO2011133953A1 (en) 2010-04-22 2011-10-27 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions and administrations thereof
ES2603032T3 (es) 2010-07-15 2017-02-23 Bayer Intellectual Property Gmbh Compuestos de 3-piridil-heteroarilcarboxamida como pesticidas
DK2684880T3 (en) 2011-03-10 2018-05-22 Daiichi Sankyo Co Ltd DISPIROPYRROLIDINE DERIVATIVES
CA2736441A1 (en) 2011-04-06 2012-10-06 The Regents Of The University Of California Pyrazolylthiazole compounds as .delta.f508-cystic fibrosis transmembrane conductance regulator correctors
CA2842364A1 (en) 2011-07-29 2013-02-07 Karyopharm Therapeutics, Inc. Nuclear transport modulators and uses thereof
ES2558457T3 (es) 2011-09-16 2016-02-04 Novartis Ag Compuestos heterocíclicos para el tratamiento de fibrosis quística
US9056867B2 (en) 2011-09-16 2015-06-16 Novartis Ag N-substituted heterocyclyl carboxamides
US8623860B2 (en) 2011-12-30 2014-01-07 Boehringer Ingelheim International Gmbh Azetidine derivatives, pharmaceutical compositions and uses thereof
JP6138834B2 (ja) 2012-02-16 2017-05-31 ダウ アグロサイエンシィズ エルエルシー スルフィルイミン化合物の製造方法
UA110436C2 (en) 2012-03-06 2015-12-25 Zoetis Llc Antibacterial phenol compounds
WO2013146970A1 (ja) 2012-03-29 2013-10-03 第一三共株式会社 新規キノリン誘導体
ES2713988T3 (es) 2012-08-01 2019-05-24 United Therapeutics Corp Tratamiento de hipertensión arterial pulmonar con células progenitoras endoteliales tratadas con prostaciclina
WO2014045283A1 (en) 2012-09-24 2014-03-27 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Restoration of the cftr function by splicing modulation
WO2014081821A2 (en) 2012-11-20 2014-05-30 Discoverybiomed, Inc. Small Molecule Bicyclic and Tricyclic CFTR Correctors
AU2013348018A1 (en) 2012-11-20 2015-06-04 Discoverybiomed, Inc. Small molecule CFTR correctors
CN103833630B (zh) * 2012-11-21 2018-11-13 顶点制药(欧洲)有限公司 氘化cftr增效剂
WO2014160478A1 (en) 2013-03-13 2014-10-02 Flatley Discovery Lab Compounds and methods for the treatment of cystic fibrosis
US9783529B2 (en) 2013-03-13 2017-10-10 Flatley Discovery Lab, Llc Pyridazinone compounds and methods for the treatment of cystic fibrosis
CA2903103C (en) 2013-03-15 2020-06-09 Discoverybiomed, Inc. Coumarin derivatives and methods of use in treating cystic fibrosis, chronic obstructive pulmonary disease, and misfolded protein disorders
CA2907260A1 (en) 2013-03-15 2014-09-18 The University Of North Carolina Chapel Hill Correctors acting through msd1 of cftr protein
WO2014176553A1 (en) 2013-04-26 2014-10-30 Vertex Pharmaceuticals Incorporated Correctors acting through msd1 of cftr protein
MX368263B (es) 2013-05-07 2019-09-26 Galapagos Nv Compuestos novedosos y composiciones farmaceuticas de los mismos para el tratamiento de fibrosis quistica.
WO2014181287A1 (en) 2013-05-09 2014-11-13 Piramal Enterprises Limited Heterocyclyl compounds and uses thereof
US20160151335A1 (en) 2013-06-26 2016-06-02 Proteostasis Therapeutics, Inc. Methods of modulating cftr activity
WO2015051230A1 (en) 2013-10-04 2015-04-09 Drexel University Novel compositions useful for inhibiting hiv-1 infection and methods using same
EP3116501A1 (en) 2014-03-13 2017-01-18 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing cftr activity
EP3116870A1 (en) 2014-03-13 2017-01-18 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing cftr activity
CA2952862A1 (en) 2014-06-19 2015-12-23 Proteostasis Therapeutics, Inc. Compounds, compositions and methods of increasing cftr activity
US9855249B2 (en) 2014-10-02 2018-01-02 Flatley Discovery Lab, Llc Isoxazole compounds and methods for the treatment of cystic fibrosis
US10344023B2 (en) 2014-12-23 2019-07-09 Proteostasis Therapeutics, Inc. Derivatives of 3-heteroarylisoxazol-5-carboxylic amide useful for the treatment of inter alia cystic fibrosis
US10738011B2 (en) 2014-12-23 2020-08-11 Proteostasis Therapeutics, Inc. Derivatives of 5-(hetero)arylpyrazol-3-carboxylic amide or 1-(hetero)aryltriazol-4-carboxylic amide useful for the treatment of inter alia cystic fibrosis
US10392378B2 (en) 2014-12-23 2019-08-27 Proteostasis Therapeutics, Inc. Derivatives of 5-phenyl- or 5-heteroarylathiazol-2-carboxylic amide useful for the treatment of inter alia cystic fibrosis
MA41253A (fr) 2014-12-23 2017-10-31 Proteostasis Therapeutics Inc Composés, compositions et procédés pour augmenter l'activité du cftr
US20180147187A1 (en) 2015-01-12 2018-05-31 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing cftr activity
US10548878B2 (en) 2015-07-24 2020-02-04 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods of increasing CFTR activity
WO2017040606A1 (en) 2015-08-31 2017-03-09 Proteostasis Therapeutics, Inc. Isoxazole derivatives for use in the treatment of pulmonary diseases and disorders
NZ741093A (en) 2015-10-06 2022-12-23 Proteostasis Therapeutics Inc Compounds, compositions, and methods for modulating cftr
EP3393465A1 (en) 2015-12-22 2018-10-31 Proteostasis Therapeutics, Inc. Methods of treating pulmonary diseases and disorders
BR112018070747B1 (pt) 2016-04-07 2024-01-09 Proteostasis Therapeutics, Inc Átomos de silicone contendo análogos de ivacaftor, composições farmacêuticas e usos terapêuticos
EP3455624A1 (en) 2016-05-09 2019-03-20 Proteostasis Therapeutics, Inc. Methods of identifying cftr modulators
EP3472156B1 (en) 2016-06-21 2023-06-07 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing cftr activity

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012158885A1 (en) * 2011-05-18 2012-11-22 Concert Pharmaceuticals Inc. Deuterated derivatives of ivacaftor
US20140073667A1 (en) * 2011-05-18 2014-03-13 Adam J. Morgan Deuterated cftr potentiators

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Showell and Mills, DDT, 2003, Vol 8, No 12, 551-556 *

Also Published As

Publication number Publication date
WO2017177124A1 (en) 2017-10-12
US10662207B2 (en) 2020-05-26
AR108203A1 (es) 2018-07-25
EP3440057B1 (en) 2021-09-22
NZ746793A (en) 2022-10-28
US20240109922A1 (en) 2024-04-04
MX386698B (es) 2025-03-19
CN109563047A (zh) 2019-04-02
JP7061076B2 (ja) 2022-04-27
AU2017248253A1 (en) 2018-10-18
MA43775A (fr) 2021-05-05
US20260078136A1 (en) 2026-03-19
IL262030B (en) 2021-10-31
CA3019663C (en) 2024-09-24
RU2018137683A (ru) 2020-05-12
BR112018070747B1 (pt) 2024-01-09
US20190153000A1 (en) 2019-05-23
SG11201808682XA (en) 2018-11-29
IL262030A (en) 2018-11-29
KR102448404B1 (ko) 2022-09-27
SA518400164B1 (ar) 2022-05-08
US20240368198A1 (en) 2024-11-07
US11248010B2 (en) 2022-02-15
BR112018070747A2 (pt) 2019-06-18
MX2018012331A (es) 2019-05-23
JP2019513741A (ja) 2019-05-30
CA3019663A1 (en) 2017-10-12
US20210061823A1 (en) 2021-03-04
KR20180132803A (ko) 2018-12-12
EP3440057A1 (en) 2019-02-13
RU2018137683A3 (enExample) 2020-05-18

Similar Documents

Publication Publication Date Title
AU2017248253B2 (en) Silicone atoms containing ivacaftor analogues
EP3691638B1 (en) Compounds, compositions and methods for increasing cftr activity
US11136313B2 (en) Compounds, compositions, and methods for modulating CFTR
EP3472156B1 (en) Compounds, compositions, and methods for increasing cftr activity
US20190248779A1 (en) Compounds, compositions, and methods for increasing cftr activity
WO2018081381A1 (en) Pyridazine derivatives, compositions and methods for modulating cftr
WO2016105484A1 (en) Derivatives of 5-(hetero)arylpyrazol-3-carboxylic amide or 1-(hetero)aryltriazol-4-carboxylic amide useful for the treatment of inter alia cystic fibrosis
RU2796112C2 (ru) Кремнийсодержащие аналоги ивакафтора
HK40004165B (en) Silicone atoms containing ivacaftor analogues
HK1258811B (en) Compounds, compositions, and methods for modulating cftr

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)