IL292156B2 - Modified azacils as TRMP8 modulators - Google Patents

Modified azacils as TRMP8 modulators

Info

Publication number
IL292156B2
IL292156B2 IL292156A IL29215622A IL292156B2 IL 292156 B2 IL292156 B2 IL 292156B2 IL 292156 A IL292156 A IL 292156A IL 29215622 A IL29215622 A IL 29215622A IL 292156 B2 IL292156 B2 IL 292156B2
Authority
IL
Israel
Prior art keywords
imidazol
piperidin
propan
methylthio
phenyl
Prior art date
Application number
IL292156A
Other languages
English (en)
Hebrew (he)
Other versions
IL292156A (en
IL292156B1 (en
Original Assignee
Givaudan Sa
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 Givaudan Sa filed Critical Givaudan Sa
Publication of IL292156A publication Critical patent/IL292156A/en
Publication of IL292156B1 publication Critical patent/IL292156B1/en
Publication of IL292156B2 publication Critical patent/IL292156B2/en

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
    • A61K31/435—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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
    • A61K8/4946—Imidazoles or their condensed derivatives, e.g. benzimidazoles
    • 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
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
    • A61K2800/24—Thermal properties
    • A61K2800/244—Endothermic; Cooling; Cooling sensation
    • 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
    • C07B2200/07—Optical isomers
    • 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
    • C07B2200/09—Geometrical isomers

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Birds (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Cosmetics (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Steroid Compounds (AREA)
  • Thermotherapy And Cooling Therapy Devices (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Laser Surgery Devices (AREA)
IL292156A 2019-10-17 2020-10-15 Modified azacils as TRMP8 modulators IL292156B2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2019111690 2019-10-17
PCT/EP2020/079009 WO2021074281A1 (en) 2019-10-17 2020-10-15 Substituted azacyles as trmp8 modulators

Publications (3)

Publication Number Publication Date
IL292156A IL292156A (en) 2022-06-01
IL292156B1 IL292156B1 (en) 2026-01-01
IL292156B2 true IL292156B2 (en) 2026-05-01

Family

ID=72964655

Family Applications (1)

Application Number Title Priority Date Filing Date
IL292156A IL292156B2 (en) 2019-10-17 2020-10-15 Modified azacils as TRMP8 modulators

Country Status (10)

Country Link
US (2) US12528801B2 (enExample)
EP (1) EP4045491A1 (enExample)
JP (1) JP7778688B2 (enExample)
KR (1) KR20220085798A (enExample)
CN (1) CN114555594B (enExample)
BR (1) BR112022005289A2 (enExample)
CO (1) CO2022004130A2 (enExample)
IL (1) IL292156B2 (enExample)
MX (1) MX2022003494A (enExample)
WO (1) WO2021074281A1 (enExample)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
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GB202012170D0 (en) * 2020-08-05 2020-09-16 Givaudan Sa Organic compounds
GB202013383D0 (en) * 2020-08-26 2020-10-07 Givaudan Sa Process
WO2022170519A1 (en) 2021-02-09 2022-08-18 Givaudan Sa Organic compounds
GB202102676D0 (en) 2021-02-25 2021-04-14 Givaudan Sa Compositions
GB202103207D0 (en) 2021-03-08 2021-04-21 Givaudan Sa Organic compounds
GB202105661D0 (en) 2021-04-21 2021-06-02 Givaudan Sa Organic compounds
US20240238183A1 (en) 2021-05-28 2024-07-18 Firmenich Incorporated Compositions that enhance the cooling effect
CN117813077A (zh) * 2021-08-16 2024-04-02 西姆莱斯股份公司 组合物
US20250387310A1 (en) 2022-07-07 2025-12-25 Firmenich Incorporated Compositions that enhance the cooling effect
EP4554572A2 (en) 2022-07-11 2025-05-21 Symrise AG Mixtures and uses of (2e)-3-(1,3-benzodioxol-5-yl)-n-phenyl-n-(tetrahydro-3-furanyl)-2-propenamide
JP2026512978A (ja) 2022-10-27 2026-04-22 フイルメニツヒ ソシエテ アノニム フラボノイド組成物およびその使用
US20260206810A1 (en) 2022-12-22 2026-07-23 Firmenich Sa Natural sweetener compositions and uses thereof
US20260206809A1 (en) 2022-12-22 2026-07-23 Firmenich Sa Natural sweetener compositions containing alkyl lactates and uses thereof
JP2026511252A (ja) 2023-03-28 2026-04-10 フイルメニツヒ ソシエテ アノニム 味改変組成物およびその使用
EP4774272A1 (en) 2023-09-04 2026-07-15 Symrise AG Trpm8 modulators and related method for modulating trpm8 receptors
GB202315636D0 (en) 2023-10-12 2023-11-29 Givaudan Sa Composition
WO2025132323A1 (en) 2023-12-21 2025-06-26 Dsm-Firmenich Ag Compositions comprising a sunscreen active agent
WO2026052684A1 (en) 2024-09-04 2026-03-12 Givaudan Sa Flavour compositions
WO2026087386A1 (en) 2024-10-24 2026-04-30 Firmenich Sa Rosin diester compounds and uses thereof
WO2026092819A1 (en) 2024-10-28 2026-05-07 Symrise Ag Oral care compositions

Citations (4)

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WO1998040400A1 (en) * 1997-03-10 1998-09-17 Basf Aktiengesellschaft Dolastatin 15 derivatives with carbonyl and heterocyclic functionalities at the c-terminus
WO2002036116A2 (en) * 2000-10-30 2002-05-10 Janssen Pharmaceutica N.V. Tripeptidyl peptidase inhibitors
US20100048589A1 (en) * 2008-08-19 2010-02-25 Colburn Raymond W Cold Menthol Receptor Antagonists
EP3315492A1 (en) * 2015-06-23 2018-05-02 Kissei Pharmaceutical Co., Ltd. Pyrazole derivative, or pharmaceutically acceptable salt thereof

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US3988433A (en) 1973-08-10 1976-10-26 The Procter & Gamble Company Oral compositions for preventing or removing stains from teeth
US4083955A (en) 1975-04-02 1978-04-11 The Procter & Gamble Company Processes and compositions for remineralization of dental enamel
US4528180A (en) 1983-03-01 1985-07-09 Schaeffer Hans A Dental preparation, article and method for storage and delivery thereof
US4849213A (en) 1983-03-01 1989-07-18 Schaeffer Hans A Dental preparation, article and method for storage and delivery therof
US5198220A (en) 1989-11-17 1993-03-30 The Procter & Gamble Company Sustained release compositions for treating periodontal disease
US5145666A (en) 1991-10-23 1992-09-08 The Proctor & Gamble Co. Methods of reducing plaque and gingivitis with reduced staining
US5213790A (en) 1991-10-23 1993-05-25 The Procter & Gamble Co. Methods of reducing plaque and gingivitis with reduced staining
US5281410A (en) 1991-10-23 1994-01-25 The Proctor & Gamble Company Methods of reducing plaque and gingivitis with reduced staining
US5242910A (en) 1992-10-13 1993-09-07 The Procter & Gamble Company Sustained release compositions for treating periodontal disease
HUP0500921A2 (en) 2005-10-05 2007-07-30 Richter Gedeon Nyrt Tetrazole derivatives, process for their preparation and their use
HUP0500920A2 (en) * 2005-10-05 2007-07-30 Richter Gedeon Nyrt Oxadiazole derivatives, process for their preparation and their use
GB0704163D0 (en) 2007-03-02 2007-04-11 Quest Int Serv Bv Compositions comprising a physiological coolant
AU2009318056B2 (en) 2008-11-20 2014-07-24 The Procter & Gamble Company Personal care compositions providing enhanced cooling sensation
CN103201279A (zh) 2010-11-05 2013-07-10 赛诺米克斯公司 作为trpm8的调节剂有用的化合物
WO2014037340A1 (de) 2012-09-05 2014-03-13 Bayer Cropscience Ag Verwendung substituierter 2-amidobenzimidazole, 2-amidobenzoxazole und 2-amidobenzothiazole oder deren salze als wirkstoffe gegen abiotischen pflanzenstress
CN106103416B (zh) 2014-03-14 2021-03-02 拉夸里亚创药株式会社 作为trpm8拮抗剂的氮杂螺衍生物
EP3675809B1 (de) 2017-08-31 2023-09-27 Basf Se Verwendung physiologischer kühlwirkstoffe und mittel enthaltend solche wirkstoffe
EP3658109B1 (en) 2017-12-21 2022-12-07 Firmenich SA Cooling and flavor boosting compositions

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998040400A1 (en) * 1997-03-10 1998-09-17 Basf Aktiengesellschaft Dolastatin 15 derivatives with carbonyl and heterocyclic functionalities at the c-terminus
WO2002036116A2 (en) * 2000-10-30 2002-05-10 Janssen Pharmaceutica N.V. Tripeptidyl peptidase inhibitors
US20100048589A1 (en) * 2008-08-19 2010-02-25 Colburn Raymond W Cold Menthol Receptor Antagonists
EP3315492A1 (en) * 2015-06-23 2018-05-02 Kissei Pharmaceutical Co., Ltd. Pyrazole derivative, or pharmaceutically acceptable salt thereof

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
BRESLIN H J ET AL,, RATIONALE, DESIGN, AND SYNTHESIS OF NOVEL PHENYL IMIDAZOLES AS OPIOID RECEPTOR AGONISTS FOR GASTROINTESTINAL DISORDERS, 4 September 2004 (2004-09-04) *
M. JES?S P?REZ DE VEGA ET AL,, TRANSIENT RECEPTOR POTENTIAL MELASTATIN 8 CHANNEL (TRPM8) MODULATION: COOL ENTRYWAY FOR TREATING PAIN AND CANCER, 1 August 2016 (2016-08-01) *

Also Published As

Publication number Publication date
JP7778688B2 (ja) 2025-12-02
KR20220085798A (ko) 2022-06-22
US12528801B2 (en) 2026-01-20
JP2022552401A (ja) 2022-12-15
MX2022003494A (es) 2022-04-25
US20240132487A1 (en) 2024-04-25
EP4045491A1 (en) 2022-08-24
CN114555594A (zh) 2022-05-27
IL292156A (en) 2022-06-01
WO2021074281A1 (en) 2021-04-22
BR112022005289A2 (pt) 2022-09-20
US20260103459A1 (en) 2026-04-16
CO2022004130A2 (es) 2022-07-08
CN114555594B (zh) 2025-03-18
IL292156B1 (en) 2026-01-01

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