PE20221441A1 - Derivados de piridina como moduladores de tmem16a para su uso en el tratamiento de afecciones respiratorias - Google Patents

Derivados de piridina como moduladores de tmem16a para su uso en el tratamiento de afecciones respiratorias

Info

Publication number
PE20221441A1
PE20221441A1 PE2022000119A PE2022000119A PE20221441A1 PE 20221441 A1 PE20221441 A1 PE 20221441A1 PE 2022000119 A PE2022000119 A PE 2022000119A PE 2022000119 A PE2022000119 A PE 2022000119A PE 20221441 A1 PE20221441 A1 PE 20221441A1
Authority
PE
Peru
Prior art keywords
methyl
halo
tmem16a
treatment
respiratory diseases
Prior art date
Application number
PE2022000119A
Other languages
English (en)
Inventor
Stephen Collingwood
Craig Buxton
Jonathan David Hargrave
Peter Ingram
Thomas Beauregard Schofield
Abdul Shaikh
Christopher Stimson
Original Assignee
Tmem16A Ltd
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
Priority claimed from GBGB1910607.9A external-priority patent/GB201910607D0/en
Priority claimed from GBGB2005739.4A external-priority patent/GB202005739D0/en
Application filed by Tmem16A Ltd filed Critical Tmem16A Ltd
Publication of PE20221441A1 publication Critical patent/PE20221441A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pulmonology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)

Abstract

La presente invencion se refiere a un compuesto de formula general (I), el cual incluye en su estructura a los radicales R1, R2, R3, R4, R5, R6, R7, R8, R9 y R10; en donde R1 se selecciona de metilo, fluorometilo, difluorometilo, trifluorometilo, clorodifluorometilo, diclorofluorometilo, etinilo y CN; R2 se selecciona de metilo y CH2OH; R3 se selecciona de H y metilo; R4 es H o halo; R5 se selecciona independientemente de H, halo, C1-3 alquilo y C1-3 haloalquilo, al igual que R7; R6 se selecciona de halo, CN y C1-4 alquilo y a veces se sustituye con uno o mas sustituyentes de halo y OH; R8 es metilo o etilo, entre otros; R9 es OH, CH2OH, metilo, etilo, entre otros; y R10 es H, OH o C1-4 alquilo, etc. Este compuesto es seleccionado de 4-[[2-(4-ter-butil-2-fluoro-5-hidroxi-fenil)acetil]amino]-N-(1-metilciclopropil)piridin-2-carboxamida, entre otros y puede ser utilizado para la fabricacion de un medicamento para el tratamiento o profilaxis de enfermedades respiratorias y otras afecciones moduladas por TMEM16A, tales como sequedad en la boca (xerostomia), hipermotilidad intestinal, colestasis y afecciones oculares.
PE2022000119A 2019-07-24 2020-07-24 Derivados de piridina como moduladores de tmem16a para su uso en el tratamiento de afecciones respiratorias PE20221441A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1910607.9A GB201910607D0 (en) 2019-07-24 2019-07-24 Compounds
GBGB2005739.4A GB202005739D0 (en) 2020-04-20 2020-04-20 Compounds
PCT/GB2020/051778 WO2021014166A1 (en) 2019-07-24 2020-07-24 Pyridine derivatives as tmem16a modulators for use in the treatment of respiratory conditions

Publications (1)

Publication Number Publication Date
PE20221441A1 true PE20221441A1 (es) 2022-09-21

Family

ID=71948615

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022000119A PE20221441A1 (es) 2019-07-24 2020-07-24 Derivados de piridina como moduladores de tmem16a para su uso en el tratamiento de afecciones respiratorias

Country Status (15)

Country Link
US (1) US20220235006A1 (es)
EP (1) EP4003516A1 (es)
JP (1) JP2022541311A (es)
KR (1) KR20220063162A (es)
CN (1) CN114616226A (es)
AU (1) AU2020317036A1 (es)
BR (1) BR112022001164A2 (es)
CA (1) CA3145120A1 (es)
CL (1) CL2022000147A1 (es)
CO (1) CO2022002022A2 (es)
CR (1) CR20220072A (es)
IL (1) IL290035A (es)
MX (1) MX2022000841A (es)
PE (1) PE20221441A1 (es)
WO (1) WO2021014166A1 (es)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CR20220072A (es) * 2019-07-24 2022-06-29 Tmem16A Ltd Derivados de piridina como moduladores de tmem16a para su uso en el tratamiento de afecciones respiratorias

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050176767A1 (en) * 2003-10-30 2005-08-11 Laval Chan Chun Kong Pyridine carboxamide and methods for inhibiting HIV integrase
EP3612180B1 (en) * 2017-04-17 2023-10-11 The Regents of the University of California Substituted 2-acylamino-cycloalkylthiophene-3-carboxylic acid arylamides as inhibitors of calcium-activated chloride channel tmem16a
GB201801355D0 (en) * 2018-01-26 2018-03-14 Enterprise Therapeutics Ltd Compounds
CR20220072A (es) * 2019-07-24 2022-06-29 Tmem16A Ltd Derivados de piridina como moduladores de tmem16a para su uso en el tratamiento de afecciones respiratorias

Also Published As

Publication number Publication date
MX2022000841A (es) 2022-06-08
WO2021014166A1 (en) 2021-01-28
BR112022001164A2 (pt) 2022-03-15
JP2022541311A (ja) 2022-09-22
CL2022000147A1 (es) 2022-10-07
CN114616226A (zh) 2022-06-10
KR20220063162A (ko) 2022-05-17
EP4003516A1 (en) 2022-06-01
IL290035A (en) 2022-03-01
CR20220072A (es) 2022-06-29
CO2022002022A2 (es) 2022-06-10
CA3145120A1 (en) 2021-01-28
US20220235006A1 (en) 2022-07-28
AU2020317036A1 (en) 2022-03-17

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