CY1123794T1 - ΣΤΕΡΕΑ ΔΙΑΣΠΟΡΑ ΑΜΟΡΦΗΣ ΜΟΡΦΗΣ (R)-l-(2,2-ΔΙΦΘΟΡΟΒΕΝΖΟ[D][1,3]ΔΙΟΞΟΛ-5-ΥΛΟ)-Ν-(1-(2,3-ΔΙΥΔΡΟΞΥΠΡΟΠΥΛΟ)-6-ΦΘΟΡΟ-2-(1-ΥΔΡΟΞΥ-2-ΜΕΘΥΛΟΠΡΟΠΑΝ-2-ΥΛΟ)-1Η-ΙΝΔΟΛ-5-ΥΛΟ)-ΚΥΚΛΟΠΡΟΠΑΝΟΚΑΡΒΟΞΑΜΙΔΙΟΥ - Google Patents

ΣΤΕΡΕΑ ΔΙΑΣΠΟΡΑ ΑΜΟΡΦΗΣ ΜΟΡΦΗΣ (R)-l-(2,2-ΔΙΦΘΟΡΟΒΕΝΖΟ[D][1,3]ΔΙΟΞΟΛ-5-ΥΛΟ)-Ν-(1-(2,3-ΔΙΥΔΡΟΞΥΠΡΟΠΥΛΟ)-6-ΦΘΟΡΟ-2-(1-ΥΔΡΟΞΥ-2-ΜΕΘΥΛΟΠΡΟΠΑΝ-2-ΥΛΟ)-1Η-ΙΝΔΟΛ-5-ΥΛΟ)-ΚΥΚΛΟΠΡΟΠΑΝΟΚΑΡΒΟΞΑΜΙΔΙΟΥ

Info

Publication number
CY1123794T1
CY1123794T1 CY20211100108T CY211100108T CY1123794T1 CY 1123794 T1 CY1123794 T1 CY 1123794T1 CY 20211100108 T CY20211100108 T CY 20211100108T CY 211100108 T CY211100108 T CY 211100108T CY 1123794 T1 CY1123794 T1 CY 1123794T1
Authority
CY
Cyprus
Prior art keywords
ylo
difluorobenzo
dioxol
dihydroxypropyl
indol
Prior art date
Application number
CY20211100108T
Other languages
English (en)
Inventor
Ali Keshavarz-Shokri
Beili Zhang
Tim Edward Alcacio
Elaine Chungmin Lee
Yuegang Zhang
Mariusz Krawiec
Original Assignee
Vertex Pharmaceuticals Incorporated
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 Incorporated filed Critical Vertex Pharmaceuticals Incorporated
Publication of CY1123794T1 publication Critical patent/CY1123794T1/el

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/04—Artificial tears; Irrigation solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P37/08—Antiallergic agents
    • 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
    • A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • 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
    • A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • 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
    • 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
    • A61P5/16—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
    • 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
    • A61P5/18—Drugs for disorders of the endocrine system of the parathyroid hormones
    • 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
    • A61P5/18—Drugs for disorders of the endocrine system of the parathyroid hormones
    • A61P5/20—Drugs for disorders of the endocrine system of the parathyroid hormones for decreasing, blocking or antagonising the activity of PTH
    • 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
    • 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
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/40—Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Psychology (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Otolaryngology (AREA)
  • Psychiatry (AREA)

Abstract

Η παρούσα εφεύρεση σχετίζεται με στερεά άμορφη μορφή (R)-1 -(2,2-διφθοροβενζο[d[1,3]διοξολ-5-υλο)-Ν-(1-(2,3-διυδροξυπροπυλο)-6-φθορο-2-(1-υδροξυ-2-μεθυλοπροπαν-2-υλο)-1Η-ινδολ-5-υλο)-κυκλοπροπανοκαρβοξαμιδίου (ένωση 1), φαρμακευτικές συνθέσεις αυτού, στερεές διασπορές αυτού και την ένωση 1 για χρήση στην αγωγή μίας νόσου που διαμεσολαβείται από CFTR όπως η κυστική ίνωση.
CY20211100108T 2010-03-25 2021-02-08 ΣΤΕΡΕΑ ΔΙΑΣΠΟΡΑ ΑΜΟΡΦΗΣ ΜΟΡΦΗΣ (R)-l-(2,2-ΔΙΦΘΟΡΟΒΕΝΖΟ[D][1,3]ΔΙΟΞΟΛ-5-ΥΛΟ)-Ν-(1-(2,3-ΔΙΥΔΡΟΞΥΠΡΟΠΥΛΟ)-6-ΦΘΟΡΟ-2-(1-ΥΔΡΟΞΥ-2-ΜΕΘΥΛΟΠΡΟΠΑΝ-2-ΥΛΟ)-1Η-ΙΝΔΟΛ-5-ΥΛΟ)-ΚΥΚΛΟΠΡΟΠΑΝΟΚΑΡΒΟΞΑΜΙΔΙΟΥ CY1123794T1 (el)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US31737610P 2010-03-25 2010-03-25
US31995310P 2010-04-01 2010-04-01
US32163610P 2010-04-07 2010-04-07
US32156110P 2010-04-07 2010-04-07
EP11713134.2A EP2563778B1 (en) 2010-03-25 2011-03-25 Crystalline form of (r)-1(2,2 -difluorobenzo[d][1,3]dioxol-5yl)-n-(1-(2,3-dihyderoxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2yl)-1h-indol-5yl)cyclopropanecarboxamide
PCT/US2011/030032 WO2011119984A1 (en) 2010-03-25 2011-03-25 Solid forms of (r)-1(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-n-(1-(2,3-dihyderoxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl) cyclopropanecarboxamide

Publications (1)

Publication Number Publication Date
CY1123794T1 true CY1123794T1 (el) 2021-09-14

Family

ID=43903962

Family Applications (3)

Application Number Title Priority Date Filing Date
CY20211100108T CY1123794T1 (el) 2010-03-25 2021-02-08 ΣΤΕΡΕΑ ΔΙΑΣΠΟΡΑ ΑΜΟΡΦΗΣ ΜΟΡΦΗΣ (R)-l-(2,2-ΔΙΦΘΟΡΟΒΕΝΖΟ[D][1,3]ΔΙΟΞΟΛ-5-ΥΛΟ)-Ν-(1-(2,3-ΔΙΥΔΡΟΞΥΠΡΟΠΥΛΟ)-6-ΦΘΟΡΟ-2-(1-ΥΔΡΟΞΥ-2-ΜΕΘΥΛΟΠΡΟΠΑΝ-2-ΥΛΟ)-1Η-ΙΝΔΟΛ-5-ΥΛΟ)-ΚΥΚΛΟΠΡΟΠΑΝΟΚΑΡΒΟΞΑΜΙΔΙΟΥ
CY2021014C CY2021014I2 (el) 2010-03-25 2021-05-19 ΣΤΕΡΕΑ ΔΙΑΣΠΟΡΑ ΑΜΟΡΦΗΣ ΜΟΡΦΗΣ (R)-l-(2,2-ΔΙΦΘΟΡΟΒΕΝΖΟ[D][1,3]ΔΙΟΞΟΛ-5-ΥΛΟ)-Ν-(1-(2,3-ΔΙΥΔΡΟΞΥΠΡΟΠΥΛΟ)-6-ΦΘΟΡΟ-2-(1-ΥΔΡΟΞΥ-2-ΜΕΘΥΛΟΠΡΟΠΑΝ-2-ΥΛΟ)-1Η-ΙΝΔΟΛ-5-ΥΛΟ)-ΚΥΚΛΟΠΡΟΠΑΝΟΚΑΡΒΟΞΑΜΙΔΙΟΥ
CY20231100390T CY1126143T1 (el) 2010-03-25 2023-08-03 Συνθεση και ενδιαμεσα του (r)-1-(2,2-διφθοροβενζο[d][1,3]διοξολ-5-υλο)-ν-(1-(2,3-διυδροξυπροπυλο)-6-φθορο-2-(1-υδροξυ-2-μεθυλοπροπαν-2-υλο)-1η-ινδολ-5-υλο)-κυκλοπροπανοκαρβοξαμιδιου

Family Applications After (2)

Application Number Title Priority Date Filing Date
CY2021014C CY2021014I2 (el) 2010-03-25 2021-05-19 ΣΤΕΡΕΑ ΔΙΑΣΠΟΡΑ ΑΜΟΡΦΗΣ ΜΟΡΦΗΣ (R)-l-(2,2-ΔΙΦΘΟΡΟΒΕΝΖΟ[D][1,3]ΔΙΟΞΟΛ-5-ΥΛΟ)-Ν-(1-(2,3-ΔΙΥΔΡΟΞΥΠΡΟΠΥΛΟ)-6-ΦΘΟΡΟ-2-(1-ΥΔΡΟΞΥ-2-ΜΕΘΥΛΟΠΡΟΠΑΝ-2-ΥΛΟ)-1Η-ΙΝΔΟΛ-5-ΥΛΟ)-ΚΥΚΛΟΠΡΟΠΑΝΟΚΑΡΒΟΞΑΜΙΔΙΟΥ
CY20231100390T CY1126143T1 (el) 2010-03-25 2023-08-03 Συνθεση και ενδιαμεσα του (r)-1-(2,2-διφθοροβενζο[d][1,3]διοξολ-5-υλο)-ν-(1-(2,3-διυδροξυπροπυλο)-6-φθορο-2-(1-υδροξυ-2-μεθυλοπροπαν-2-υλο)-1η-ινδολ-5-υλο)-κυκλοπροπανοκαρβοξαμιδιου

Country Status (24)

Country Link
US (1) US20110251253A1 (el)
EP (5) EP4253381A3 (el)
JP (5) JP5734410B2 (el)
CN (3) CN109081804B (el)
AU (3) AU2011230508B2 (el)
BR (1) BR112012024338B1 (el)
CA (2) CA3016080C (el)
CY (3) CY1123794T1 (el)
DK (1) DK2826776T3 (el)
ES (4) ES2951520T3 (el)
FR (1) FR21C1018I2 (el)
HR (2) HRP20230661T1 (el)
HU (3) HUE052759T2 (el)
IL (4) IL222117B (el)
LT (2) LT2826776T (el)
MX (3) MX345541B (el)
NO (1) NO2021021I1 (el)
NZ (3) NZ602665A (el)
PL (2) PL2826776T3 (el)
PT (1) PT2826776T (el)
RS (1) RS61314B1 (el)
RU (2) RU2573830C2 (el)
SI (1) SI2826776T1 (el)
WO (1) WO2011119984A1 (el)

Families Citing this family (102)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100074949A1 (en) 2008-08-13 2010-03-25 William Rowe Pharmaceutical composition and administration thereof
CA2537841A1 (en) 2003-09-06 2005-03-24 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
US7977322B2 (en) 2004-08-20 2011-07-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
CN107501099B (zh) 2004-06-24 2021-03-19 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
WO2007021982A2 (en) 2005-08-11 2007-02-22 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP2395002B1 (en) 2005-11-08 2014-06-18 Vertex Pharmaceuticals Inc. Pharmaceutical composition containing a heterocyclic modulator of atp-binding cassette transporters.
PL1993360T3 (pl) 2005-12-28 2017-08-31 Vertex Pharmaceuticals Incorporated Stałe postacie n-[2,4-bis(1,1-dimetyloetylo)-5-hydroksyfenylo]-1,4- dihydro-4-oksochinolino-3-karboksyamidu
EP2016065B1 (en) 2005-12-28 2012-09-19 Vertex Pharmaceuticals Incorporated 1-(benzo[d][1,3]dioxol-5-yl)-n-(phenyl)cyclopropane-carboxamide derivatives and related compounds as modulators of atp-binding cassette transporters for the treatment of cystic fibrosis
RU2451018C2 (ru) 2006-04-07 2012-05-20 Вертекс Фармасьютикалз Инкорпорейтед Модуляторы атф-связывающих кассетных транспортеров
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
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
AU2008251504B2 (en) 2007-05-09 2013-07-18 Vertex Pharmaceuticals Incorporated Modulators of CFTR
NZ583420A (en) 2007-08-24 2012-06-29 Vertex Pharma Isothiazolopyridinones useful for the treatment of (inter alia) cystic fibrosis
EP3012250B1 (en) 2007-11-16 2017-11-08 Vertex Pharmaceuticals Incorporated Isoquinoline modulators of atp-binding cassette transporters
US8507534B2 (en) 2007-12-07 2013-08-13 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
US20100036130A1 (en) 2007-12-07 2010-02-11 Vertex Pharmaceuticals Incorporated Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
SI2639222T1 (sl) 2007-12-07 2016-12-30 Vertex Pharmaceuticals Incorporated Proces za izdelavo cikloalkilkarboksiamido-piridin benzojskih kislin
NZ620944A (en) 2008-02-28 2015-02-27 Vertex Pharma Heteroaryl derivatives as cftr modulators
SI2615085T1 (sl) 2008-03-31 2015-11-30 Vertex Pharmaceuticals Incorporated Piridilni derivati kot cftr-modulatorji
AU2009296271A1 (en) 2008-09-29 2010-04-01 Vertex Pharmaceuticals Incorporated Dosage units of 3-(6-(1-(2,2-difluorobenzo [d] [1,3] dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
KR101955863B1 (ko) 2009-03-20 2019-03-07 버텍스 파마슈티칼스 인코포레이티드 낭성 섬유증 막횡단 전도도 조절자의 조정자의 제조 방법
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
CA2795748C (en) 2010-04-07 2020-12-08 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
PL3150198T3 (pl) 2010-04-07 2022-01-17 Vertex Pharmaceuticals Incorporated Kompozycje farmaceutyczne kwasu 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-ilo)cyklopropanokarboksamido)-3-metylopirydyn-2-ylo)benzoesowego i ich podawanie
EP3045452A1 (en) * 2010-04-22 2016-07-20 Vertex Pharmaceuticals Inc. Process of producing cycloalkylcarboxamido-indole compounds
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
US20130172375A1 (en) * 2011-12-13 2013-07-04 Hoffmann-La Roche Inc. Pharmaceutical composition
IL265430B2 (en) 2012-02-27 2024-08-01 Vertex Pharma Pharmaceutical preparations containing a solid dispersion of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide and uses thereof
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
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
JP6545148B2 (ja) 2013-03-13 2019-07-17 フラットリー ディスカバリー ラブ，エルエルシー ピリダジノン化合物及び嚢胞性線維症の治療のための方法
CN104415345A (zh) * 2013-08-30 2015-03-18 天津药物研究院 一种多元复合物及其制备方法
JP6963896B2 (ja) 2013-11-12 2021-11-10 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 Ｃｆｔｒ媒介性疾患の処置のための医薬組成物を調製する方法
HRP20230709T1 (hr) 2014-04-15 2023-10-13 Vertex Pharmaceuticals Incorporated Farmaceutski pripravci za liječenje bolesti povezanih s regulatorom provodljivosti transmembrane cistične fibroze
UA125245C2 (uk) 2014-10-06 2022-02-09 Вертекс Фармасьютикалз Інкорпорейтед Модулятори регулятора трансмембранної провідності при муковісцидозі
AU2015330923B2 (en) 2014-10-07 2020-03-12 Vertex Pharmaceuticals Incorporated Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator
LT3212189T (lt) * 2014-10-31 2020-11-25 Abbvie Overseas S.A R.L. Pakeisti chromanai ir naudojimo būdas
CA2968130C (en) 2014-11-18 2022-08-16 Vertex Pharmaceuticals Incorporated Process of conducting high throughput testing high performance liquid chromatography
US10167278B2 (en) 2014-12-31 2019-01-01 Auspex Pharmaceuticals, Inc. Cyclopropanecarboxamide modulators of cystic fibrosis transmembrane conductance regulator
US10196384B2 (en) 2015-03-31 2019-02-05 Vertex Pharmaceuticals (Europe) Limited Deuterated CFTR modulators
CN105130949B (zh) * 2015-09-02 2019-01-29 阜新奥瑞凯新材料有限公司 1-(2,2-二氟苯并[d][1,3]二氧杂环戊烯-5-基)环丙基腈的制备方法
WO2017180794A1 (en) 2016-04-13 2017-10-19 Skyline Antiinfectives, Inc. Deuterated o-sulfated beta-lactam hydroxamic acids and deuterated n-sulfated beta-lactams
US10206915B2 (en) 2016-04-25 2019-02-19 Druggability Technologies Ip Holdco Limited Complexes of Ivacaftor and its salts and derivatives, process for the preparation thereof and pharmaceutical compositions containing them
HUP1600271A2 (hu) 2016-04-25 2017-10-30 Druggability Tech Ip Holdco Ltd Ivacaftor és Lumacaftor sóinak és származékainak komplexei, eljárás azok elõállítására és azok gyógyszerészetileg elfogadható készítményei
US10383865B2 (en) 2016-04-25 2019-08-20 Druggability Technologies Ip Holdco Limited Pharmaceutical combination composition comprising complex formulations of Ivacaftor and Lumacaftor and their salts and derivatives, process for their preparation thereof and pharmaceutical compositions containing them
HUP1600270A2 (hu) 2016-04-25 2017-10-30 Druggability Tech Ip Holdco Ltd Ivacaftornak, sóinak és származékainak komplexei, eljárás azok elõállítására és azok gyógyszerészetileg elfogadott készítményei
PT3519401T (pt) 2016-09-30 2021-12-27 Vertex Pharma Modulador de regulador de condutância transmembranar de fibrose quística, composições farmacêuticas, métodos de tratamento e processo para fazer o modulador
US10399940B2 (en) * 2016-10-07 2019-09-03 Abbvie S.Á.R.L. Substituted pyrrolidines and methods of use
PT3551622T (pt) 2016-12-09 2020-11-12 Vertex Pharma Modulador do regulador da condutância transmembrana da fibrose quística, composições farmacêuticas, métodos de tratamento e processo de fabrico do modulador
US11253509B2 (en) 2017-06-08 2022-02-22 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
WO2019010092A1 (en) 2017-07-01 2019-01-10 Vertex Pharmaceuticals Incorporated COMPOSITIONS AND METHODS FOR TREATING CYSTIC FIBROSIS
WO2019018353A1 (en) 2017-07-17 2019-01-24 Vertex Pharmaceuticals Incorporated METHODS OF TREATING CYSTIC FIBROSIS
WO2019018395A1 (en) 2017-07-17 2019-01-24 Vertex Pharmaceuticals Incorporated METHODS OF TREATING CYSTIC FIBROSIS
CN111051280B (zh) 2017-08-02 2023-12-22 弗特克斯药品有限公司 制备吡咯烷化合物的方法
EP3697774A1 (en) 2017-10-19 2020-08-26 Vertex Pharmaceuticals Incorporated Crystalline forms and compositions of cftr modulators
CN107880011B (zh) * 2017-11-27 2019-08-16 山东省医学科学院药物研究所 鲁玛卡托关键中间体的合成方法
US20210228489A1 (en) 2017-12-04 2021-07-29 Vertex Pharmaceuticals Incorporated Compositions for treating cystic fibrosis
JP7245834B2 (ja) 2017-12-08 2023-03-24 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 嚢胞性線維症膜コンダクタンス制御因子のモジュレーターを作成するためのプロセス
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
MA51828B1 (fr) 2018-02-15 2022-11-30 Vertex Pharma Macrocycles utilisés en tant que modulateurs du régulateur de la conductance transmembranaire de fibrose kystique, compositions pharmaceutiques de ceux-ci, leur utilisation dans le traitement de la fibrose kystique et procédé de fabrication associé
CN110193012B (zh) * 2018-02-27 2022-02-08 江苏恒瑞医药股份有限公司 一种氧代吡啶酰胺类衍生物的药物组合物及其制备方法
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
EP3880197B1 (en) 2018-11-14 2023-02-22 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
CA3067611A1 (en) 2019-01-15 2020-07-15 Apotex Inc. Processes for the preparation of tezacaftor and intermediates thereof
AR118555A1 (es) 2019-04-03 2021-10-20 Vertex Pharma Agentes moduladores del regulador de la conductancia transmembrana de la fibrosis quística
WO2020214921A1 (en) 2019-04-17 2020-10-22 Vertex Pharmaceuticals Incorporated Solid forms of modulators of cftr
US11884672B2 (en) 2019-05-14 2024-01-30 Vertex Pharmaceuticals Incorporated Modulators of alpha-1 antitrypsin
WO2020242935A1 (en) 2019-05-29 2020-12-03 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
US11873300B2 (en) 2019-08-14 2024-01-16 Vertex Pharmaceuticals Incorporated Crystalline forms of CFTR modulators
TW202115092A (zh) 2019-08-14 2021-04-16 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
TW202120517A (zh) 2019-08-14 2021-06-01 美商維泰克斯製藥公司 製備cftr調節劑之方法
WO2021030556A1 (en) 2019-08-14 2021-02-18 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2021140525A1 (en) * 2020-01-07 2021-07-15 Msn Laboratories Private Limited, R&D Center Novel crystalline form of 1-(2,2-difluoro-2h-1,3benzo dioxol-5-yl)-n-{1-[(2r)-2,3-dihydroxypropyl]-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl}cyclopropane-1-carboxamide and its process for the preparation thereof
US20230092495A1 (en) 2020-03-06 2023-03-23 Química Sintética, S.A. Solid forms of tezacaftor and processes for the preparation thereof
WO2022194399A1 (en) 2020-07-13 2022-09-22 Idorsia Pharmaceuticals Ltd Macrocycles as cftr modulators
CR20230120A (es) 2020-08-07 2023-09-01 Vertex Pharma Moduladores del regulador de la conductancia transmembrana de la fibrosis quística
AU2021325923A1 (en) 2020-08-13 2023-04-06 Vertex Pharmaceuticals Incorporated Crystalline forms of CFTR modulators
EP4225446A1 (en) 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2022076629A1 (en) 2020-10-07 2022-04-14 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US20230373939A1 (en) 2020-10-07 2023-11-23 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2022076618A1 (en) 2020-10-07 2022-04-14 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2022076620A1 (en) 2020-10-07 2022-04-14 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US20230373935A1 (en) 2020-10-07 2023-11-23 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2022076626A1 (en) 2020-10-07 2022-04-14 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP4225764A1 (en) 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
MX2023004073A (es) 2020-10-07 2023-07-05 Vertex Pharma Moduladores del regulador de la conductancia transmembrana de la fibrosis quistica.
AU2021358512A1 (en) 2020-10-07 2023-05-18 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
AU2021381509A1 (en) 2020-11-17 2023-06-22 Vertex Pharmaceuticals Incorporated Solid forms of 4-(5-(4-fluorophenyl)-6-tetrahydro-2h-pyran-4-yl)- 1,5-dihydropyrrolo[2,3-f]indazol-7-yl)benzoic acid
IL303519A (en) 2020-12-10 2023-08-01 Vertex Pharma Cystic fibrosis treatment methods
TW202333699A (zh) 2022-02-03 2023-09-01 美商維泰克斯製藥公司 囊腫纖維化之治療方法
AU2023215372A1 (en) 2022-02-03 2024-08-22 Vertex Pharmaceuticals Incorporated Methods of preparing and crystalline forms of (6a,12a)-17-amino-12-methyl-6,15-bis(trifluoromethyl)-13,19-dioxa-3,4,18-triazatricyclo[ 12.3.1.12,5]nonadeca-1(18),2,4,14,16-pentaen-6-ol
WO2023154291A1 (en) 2022-02-08 2023-08-17 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2023196429A1 (en) 2022-04-06 2023-10-12 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2023224931A1 (en) 2022-05-16 2023-11-23 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
WO2023224924A1 (en) 2022-05-16 2023-11-23 Vertex Pharmaceuticals Incorporated Solid forms of a macrocyclic compounds as cftr modulators and their preparation
WO2024031081A1 (en) 2022-08-04 2024-02-08 Vertex Pharmaceuticals Incorporated Compositions for the treatment of cftr-mediated diseases
WO2024056798A1 (en) 2022-09-15 2024-03-21 Idorsia Pharmaceuticals Ltd Macrocyclic cftr modulators
WO2024056791A1 (en) 2022-09-15 2024-03-21 Idorsia Pharmaceuticals Ltd Combination of macrocyclic cftr modulators with cftr correctors and / or cftr potentiators
TW202421636A (zh) 2022-09-15 2024-06-01 瑞士商愛杜西亞製藥有限公司 (3S,7S,10R,13R)-13-苄基-20-氟-7-異丁基-N-(2-(3-甲氧基-1,2,4-㗁二唑-5-基)乙基)-6,9-二甲基-1,5,8,11-四側氧基-10-(2,2,2-三氟乙基)-1,2,3,4,5,6,7,8,9,10,11,12,13,14-十四氫-[1]㗁[4,7,10,14]四氮雜環十七烷并[16,17-f]喹啉-3-甲醯胺的晶型

Family Cites Families (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
US5716981A (en) 1993-07-19 1998-02-10 Angiogenesis Technologies, Inc. Anti-angiogenic compositions and methods of use
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
PT901786E (pt) * 1997-08-11 2007-08-07 Pfizer Prod Inc Disperções farmacêuticas sólidas com biodisponibilidade melhorada
US20020017295A1 (en) 2000-07-07 2002-02-14 Weers Jeffry G. Phospholipid-based powders for inhalation
BR0109050A (pt) * 2000-03-09 2004-04-27 Ono Pharmaceutical Co Derivados de indol, processo para prepapação e uso dos mesmos
US6777400B2 (en) 2000-08-05 2004-08-17 Smithkline Beecham Corporation Anti-inflammatory androstane derivative compositions
US20060083784A1 (en) * 2002-08-07 2006-04-20 Smithkline Beecham Corporation Amorphous pharmaceutical compositions
KR20050061501A (ko) 2002-09-30 2005-06-22 더 리전트 오브 더 유니버시티 오브 캘리포니아 낭종 섬유증 트랜스막 전도도 조절기 단백질 억제제 및이의 용도
JP2004131393A (ja) * 2002-10-08 2004-04-30 Kowa Co 易溶出性製剤
EP1601657A1 (en) 2003-03-12 2005-12-07 Vertex Pharmaceuticals Incorporated Pyrazole modulators of atp-binding cassette transporters
PL3632902T3 (pl) 2003-04-11 2021-12-20 Ptc Therapeutics, Inc. Związek kwasu 1,2,4-oksadiazolobenzoesowego i jego zastosowanie do supresji mutacji nonsensownych i leczenia choroby
WO2004110352A2 (en) 2003-05-16 2004-12-23 The Regents Of The University Of California Compounds having activity in increasing ion transport by mutant-cftr and uses thereof
DE602004022819D1 (de) 2003-06-06 2009-10-08 Vertex Pharma Von atp-bindende kassette transportern
WO2005035514A2 (en) 2003-10-08 2005-04-21 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters containing cycloalkyl or pyranyl groups
CA2545719A1 (en) 2003-11-14 2005-06-02 Vertex Pharmaceuticals Incorporated Thiazoles and oxazoles useful as modulators of atp-binding cassette transporters
WO2005094374A2 (en) 2004-03-30 2005-10-13 The Regents Of The University Of California Hydrazide-containing cftr inhibitor compounds and uses thereof
WO2005120497A2 (en) 2004-06-04 2005-12-22 The Regents Of The University Of California Compounds having activity in increasing ion transport by mutant-cftr and uses thereof
EP2311455B1 (en) 2004-10-13 2015-07-15 PTC Therapeutics, Inc. Compounds for nonsense suppression, and methods for their use
EP2363128B1 (en) 2005-03-11 2016-02-17 Vertex Pharmaceuticals Incorporated Indole modulators of ATP-binding cassette transporters
KR20070114820A (ko) 2005-03-18 2007-12-04 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 돌연변이-ｃｆｔｒ 처리를 보정하는데 활성을 가지는화합물 및 이것의 사용
DK1874306T3 (da) 2005-04-08 2012-10-01 Ptc Therapeutics Inc Sammensætninger af en oralt aktiv 1,2,4-oxadiazol til nonsens-mutationssuppressionsterapi
US8822451B2 (en) 2005-05-24 2014-09-02 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
ZA200802172B (en) * 2005-08-11 2009-06-24 Vertex Pharma Modulators of cystic fibrosis transmembrane conductance regulator
CA2619438A1 (en) * 2005-08-29 2007-03-08 Irwin C. Jacobs Amorphous solid dispersions of 7-chloro-n,n, 5-trimethyl-4-oxo-3-phenyl-3, 5,-dihydro-4h-pyridazino(4,5-b) indole-1-acetamide
CA2624683A1 (en) 2005-10-06 2007-04-19 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
CN101494979A (zh) * 2006-03-20 2009-07-29 沃泰克斯药物股份有限公司 药物组合物
AU2007226984B2 (en) * 2006-03-20 2013-02-21 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions
US7645789B2 (en) * 2006-04-07 2010-01-12 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
RU2451018C2 (ru) * 2006-04-07 2012-05-20 Вертекс Фармасьютикалз Инкорпорейтед Модуляторы атф-связывающих кассетных транспортеров
WO2008064259A2 (en) * 2006-11-21 2008-05-29 Biokey, Inc. Solid dispersion composition comprising fluvastatin
CA2706536C (en) * 2007-11-22 2016-04-19 Tadaaki Sugama Amorphous form of heterocyclic compound, solid dispersion and pharmaceutical preparation each comprising the same, and process for production of the same
US8507534B2 (en) * 2007-12-07 2013-08-13 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
CN102272127A (zh) * 2008-11-06 2011-12-07 弗特克斯药品有限公司 Atp-结合盒转运蛋白调节剂
UA104876C2 (uk) * 2008-11-06 2014-03-25 Вертекс Фармасьютікалз Інкорпорейтед Модулятори atф-зв'язувальних касетних транспортерів
CN102665715A (zh) * 2009-10-22 2012-09-12 沃泰克斯药物股份有限公司 治疗囊性纤维化和其他慢性疾病的组合物
AU2011242454A1 (en) * 2010-04-22 2012-11-08 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions and administrations thereof
EP3045452A1 (en) * 2010-04-22 2016-07-20 Vertex Pharmaceuticals Inc. Process of producing cycloalkylcarboxamido-indole compounds
CN103153287A (zh) * 2010-08-23 2013-06-12 弗特克斯药品有限公司 (R)-1-(2，2-二氟苯并[d][1，3]间二氧杂环戊烯-5-基)-N-(1-(2，3-二羟基丙基)-6-氟-2-(1-羟基-2-甲基丙-2-基)-1H-吲哚-5-基)环丙烷甲酰胺的药物组合物及其施用

Also Published As

Publication number Publication date
SI2826776T1 (sl) 2021-02-26
JP6326570B2 (ja) 2018-05-23
AU2011230508B2 (en) 2016-04-28
IL257542A (en) 2018-04-30
MX347804B (es) 2017-05-15
PL3835297T3 (pl) 2023-09-11
EP4253381A3 (en) 2023-11-01
JP6964702B2 (ja) 2021-11-10
RU2711481C2 (ru) 2020-01-17
RU2015153068A3 (el) 2019-07-17
EP4253381A2 (en) 2023-10-04
IL288388A (en) 2022-01-01
RU2573830C2 (ru) 2016-01-27
CN106083832A (zh) 2016-11-09
ES2804202T3 (es) 2021-02-04
ES2951520T3 (es) 2023-10-23
EP2563778A1 (en) 2013-03-06
BR112012024338A2 (pt) 2020-09-01
EP3181561B1 (en) 2020-05-20
JP2017008120A (ja) 2017-01-12
CA2794559A1 (en) 2011-09-29
JP6913623B2 (ja) 2021-08-04
HUE052759T2 (hu) 2021-05-28
CY2021014I1 (el) 2021-10-15
US20110251253A1 (en) 2011-10-13
JP5734410B2 (ja) 2015-06-17
EP2826776B1 (en) 2020-11-25
CY2021014I2 (el) 2021-10-15
EP3835297B1 (en) 2023-06-07
JP2013523655A (ja) 2013-06-17
CN102892764B (zh) 2016-07-06
CA3016080C (en) 2019-08-20
CY1126143T1 (el) 2023-11-15
CA3016080A1 (en) 2011-09-29
ES2845449T3 (es) 2021-07-26
AU2016208341A1 (en) 2016-08-18
CA2794559C (en) 2019-07-23
LTPA2021508I1 (el) 2021-06-10
EP2563778B1 (en) 2016-08-24
JP2015127334A (ja) 2015-07-09
JP2018048207A (ja) 2018-03-29
NO2021021I1 (no) 2021-05-21
RU2015153068A (ru) 2019-01-17
LT2826776T (lt) 2021-01-11
AU2016208341B2 (en) 2018-05-24
MX370904B (es) 2020-01-09
EP3835297C0 (en) 2023-06-07
MX2012011062A (es) 2013-01-14
IL222117B (en) 2018-02-28
DK2826776T3 (da) 2020-12-14
IL270047B (en) 2022-01-01
RS61314B1 (sr) 2021-02-26
AU2011230508A1 (en) 2012-10-18
ES2604105T3 (es) 2017-03-03
CN109081804B (zh) 2021-12-10
MX345541B (es) 2017-02-03
IL257542B (en) 2020-05-31
PL2826776T3 (pl) 2021-05-31
HRP20230661T1 (hr) 2023-09-29
WO2011119984A1 (en) 2011-09-29
EP3835297A1 (en) 2021-06-16
HUS2100019I1 (hu) 2021-06-28
JP2020094068A (ja) 2020-06-18
FR21C1018I2 (fr) 2023-02-17
HUE062892T2 (hu) 2023-12-28
EP2826776A1 (en) 2015-01-21
NZ602665A (en) 2014-10-31
CN109081804A (zh) 2018-12-25
BR112012024338B1 (pt) 2021-09-28
RU2012145295A (ru) 2014-04-27
CN102892764A (zh) 2013-01-23
HRP20210165T1 (hr) 2021-03-19
FR21C1018I1 (fr) 2021-07-02
AU2018203149A1 (en) 2018-05-24
EP3181561A1 (en) 2017-06-21
NZ700556A (en) 2016-04-29
AU2018203149B2 (en) 2019-07-25
NZ718018A (en) 2017-10-27
PT2826776T (pt) 2021-02-01

Similar Documents

Publication Publication Date Title
CY1123794T1 (el) ΣΤΕΡΕΑ ΔΙΑΣΠΟΡΑ ΑΜΟΡΦΗΣ ΜΟΡΦΗΣ (R)-l-(2,2-ΔΙΦΘΟΡΟΒΕΝΖΟ[D][1,3]ΔΙΟΞΟΛ-5-ΥΛΟ)-Ν-(1-(2,3-ΔΙΥΔΡΟΞΥΠΡΟΠΥΛΟ)-6-ΦΘΟΡΟ-2-(1-ΥΔΡΟΞΥ-2-ΜΕΘΥΛΟΠΡΟΠΑΝ-2-ΥΛΟ)-1Η-ΙΝΔΟΛ-5-ΥΛΟ)-ΚΥΚΛΟΠΡΟΠΑΝΟΚΑΡΒΟΞΑΜΙΔΙΟΥ
CY1122895T1 (el) Στερεες μορφες 3-(6-(1-(2,2-διφθοροβενζο[d][1,3]διοξολ-5-υλο)-κυκλοπροπανοκαρβοξαμιδο)-3-μεθυλοπυριδιν-3-υλο)-βενζοϊκου οξεος
CY1122617T1 (el) Απαλλαγμενες prion συνθεσεις νανοσωματιδιων και μεθοδοι
CY1122330T1 (el) Συνθεσεις δισκιων μηλεϊνικης νερατινιμπης
CY1118454T1 (el) Πρωτοτυποι αναστολεις πυρρολιου της αναγωγασης s-νιτροζογλουταθειονης ως θεραπευτικοι παραγοντες
CY1121070T1 (el) Φαρμακευτικες συνθεσεις για την αγωγη cftr μεσολαβουμενων παθησεων
MX2012012204A (es) Proceso para producir compuestos de cicloalquilcarboxamido-indol.
CY1117728T1 (el) Στερεες μορφες 3-(6-(1-(2,2-διφθοροβενζο[d][1,3]διοξολ-5-υλ) κυκλοπροπανοκαρβοξαμιδο)-3-μεθυλπυριδιν-2-υλ)βενζοϊκου οξεος
EA201070699A1 (ru) Композиции 3-(6-(1-2,2-дифторбензо[d][1,3]диоксол-5-ил)циклопропанкарбоксамидо)-3-метилпиридин-2-ил)бензойной кислоты
UA112514C2 (uk) АНТАГОНІСТИ C5aR
CY1115369T1 (el) Τροποποιητες του ρυθμιστη διαμεμβρανικης αγωγιμοτητας κυστικης ινωσης
CL2011003147A1 (es) Compuestos derivados de n-(1-4-(1h-pirazol-5-il)ftalazina-1-il) piperidina-4-il) benzamida; composicion farmaceutica que los contiene, utiles como antagonista de la trayectoria de hedgehog, en el tratamiento del cancer.
CY1119527T1 (el) Συνθεση για την αναγεννηση φυσιολογικου ιστου απο ινωτικο ιστο
EA201190297A1 (ru) Инъецируемые композиции мелфалана, содержащие производное циклодекстрина, и способы их получения и применения
TN2011000647A1 (en) Fused imidazoles and compositions comprising them for the treatment of parasitic diseases such as e.g. malaria
EA201171063A1 (ru) Фармацевтические составы олмесартана
BRPI0814457A2 (pt) Derivados de imidazolona, composições farmacêuticas, utilização de derivados de imidazolona, e, processo de síntese de derivados de imidazolona
NI201000195A (es) Derivados de quinuclidina como antagonistas de receptores muscarinicos m3.
TR201109686T2 (tr) Olmesartan'ın Farmasötik Bileşimleri.
CY1113835T1 (el) Δραση των εκχυλισματων του φυτου cissampelos pareira εναντι του δαγκειου πυρετου
EA201170843A1 (ru) Предварительно спрессованные быстро распадающиеся лекарственные формы соединений с низкой пероральной биодоступностью
WO2010023196A3 (en) Piperidylpropionamide derivatives useful for the treatment of cns disorders including depression and panic disorder
NZ724488A (en) Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
ITBO20070846A1 (it) Procedimento e macchina per la formazione di scatole.
EA200970792A1 (ru) Аморфный твёрдый раствор, содержащий производное пиразол-3-карбоксамида в аморфной форме и стабилизирующие эксципиенты