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PE20161366A1 - Heterociclil-sulfonas sustituidas con heteroarilo - Google Patents

Heterociclil-sulfonas sustituidas con heteroarilo

Info

Publication number
PE20161366A1
PE20161366A1 PE2016002003A PE2016002003A PE20161366A1 PE 20161366 A1 PE20161366 A1 PE 20161366A1 PE 2016002003 A PE2016002003 A PE 2016002003A PE 2016002003 A PE2016002003 A PE 2016002003A PE 20161366 A1 PE20161366 A1 PE 20161366A1
Authority
PE
Peru
Prior art keywords
heteroaryl
substituted
heterociclyl
sulphones
compounds
Prior art date
Application number
PE2016002003A
Other languages
English (en)
Inventor
Kathy Mackenzie
Marc Rogers
Achim Kless
Stefan Schunk
Nils Damann
Florian Jakob
Melanie Reich
Michael Haurand
Original Assignee
Gruenenthal Chemie
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 Gruenenthal Chemie filed Critical Gruenenthal Chemie
Publication of PE20161366A1 publication Critical patent/PE20161366A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4433Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D309/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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

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)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Se refiere a compuestos de formula I, donde: m es 1 o 2; n es 0 o 1; Y es un enlace o –C(R3)2-; R3 es H, alquilo C1-C6, entre otros; L es –[C(R4)2]x-(X)y-[C(R4)]z-; x es 0, 1 o 2; y es 0 o 1; z es 0 o 1; R4 es H, alquilo C1-C6, entre otros; X es O, S, S(O)2, entre otros; R1 es H, F, Cl, entre otros; R2 es H, F, Cl, entre otros; Ar1 y Ar2 son arilo o heteroarilo sustituidos. Son compuestos preferidos: 3-MetIlsulfonIl-5-[4-metIl-4-[[3-(trifluorometil)fenil]sulfonil]-tetrahidro-piran-2-il]- piridina; 5-Ciclopropil-2-[4-metil-4-[[3-(trifluorometil)fenil]sulfonil]-tetrahidro-piran-2-il]-piridina; entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos son bloqueadores de los canales de calcio dependientes de voltaje, siendo utiles en el tratamiento y/o profilaxis del dolor
PE2016002003A 2014-04-14 2015-04-14 Heterociclil-sulfonas sustituidas con heteroarilo PE20161366A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP14001346 2014-04-14

Publications (1)

Publication Number Publication Date
PE20161366A1 true PE20161366A1 (es) 2017-01-15

Family

ID=50486704

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016002003A PE20161366A1 (es) 2014-04-14 2015-04-14 Heterociclil-sulfonas sustituidas con heteroarilo

Country Status (16)

Country Link
US (2) US9879000B2 (es)
EP (2) EP3131894A1 (es)
JP (1) JP6673850B2 (es)
KR (1) KR20160144487A (es)
CN (1) CN106458956B (es)
AR (1) AR100073A1 (es)
AU (1) AU2015246387B2 (es)
BR (1) BR112016023860A2 (es)
CA (1) CA2945535A1 (es)
CL (1) CL2016002615A1 (es)
EA (1) EA032581B1 (es)
IL (1) IL248250A0 (es)
MX (1) MX2016013447A (es)
PE (1) PE20161366A1 (es)
TW (1) TW201620899A (es)
WO (1) WO2015158427A1 (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
EP3131884A1 (en) 2014-04-14 2017-02-22 Grünenthal GmbH Aryl substituted heterocyclyl sulfones
TW201726128A (zh) * 2015-10-08 2017-08-01 歌林達有限公司 經吡唑基取代之四氫哌喃基碸
TW201718557A (zh) 2015-10-08 2017-06-01 歌林達有限公司 經吡唑基取代之四氫吡喃基碸
JP6678779B2 (ja) 2016-06-13 2020-04-08 ギリアード サイエンシーズ, インコーポレイテッド Fxr(nr1h4)調節化合物
CA2968836C (en) 2016-06-13 2025-09-02 Gilead Sciences, Inc. FXR MODULATING COMPOUNDS (NR1H4)
EP4122464B1 (en) 2017-03-28 2024-05-15 Gilead Sciences, Inc. Therapeutic combinations for treating liver diseases
KR102912146B1 (ko) 2018-12-06 2026-01-14 다이이찌 산쿄 가부시키가이샤 시클로알칸-1,3-디아민 유도체
EP3911647B1 (en) 2019-01-15 2023-12-13 Gilead Sciences, Inc. Isoxazole compound as fxr agonist and pharmaceutical compositions comprising same
AU2020225225B2 (en) 2019-02-19 2022-12-22 Gilead Sciences, Inc. Solid forms of FXR agonists
US20220396560A1 (en) * 2019-10-18 2022-12-15 Fmc Corporation Methods for the preparation of 5-bromo-2-(3-chloro-pyridin-2-yl)-2h-pyrazole-3-carboxylic acid
KR20220084092A (ko) * 2019-10-18 2022-06-21 에프엠씨 코포레이션 5-브로모-2-(3-클로로-피리딘-2-일)-2h-피라졸-3-카복실산의 제조 방법

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1138680A1 (en) * 2000-03-29 2001-10-04 Pfizer Products Inc. Gem substituted sulfonyl hydroxamic acids as MMP inhibitors
WO2007125398A2 (en) 2006-04-27 2007-11-08 Pfizer Japan Inc. : sulfonamide compounds as antagonists of the n-type calcium channel
GB0813142D0 (en) * 2008-07-17 2008-08-27 Glaxo Group Ltd Novel compounds
CN102762534A (zh) * 2009-09-18 2012-10-31 扎里卡斯药品有限公司 作为钙通道阻断剂的芳基砜衍生物
EP3131884A1 (en) 2014-04-14 2017-02-22 Grünenthal GmbH Aryl substituted heterocyclyl sulfones
TW201726128A (zh) 2015-10-08 2017-08-01 歌林達有限公司 經吡唑基取代之四氫哌喃基碸
TW201718557A (zh) 2015-10-08 2017-06-01 歌林達有限公司 經吡唑基取代之四氫吡喃基碸

Also Published As

Publication number Publication date
IL248250A0 (en) 2016-11-30
EA201692049A1 (ru) 2017-04-28
WO2015158427A1 (en) 2015-10-22
AU2015246387B2 (en) 2018-11-22
CL2016002615A1 (es) 2017-04-28
EA032581B1 (ru) 2019-06-28
US20150291572A1 (en) 2015-10-15
TW201620899A (zh) 2016-06-16
KR20160144487A (ko) 2016-12-16
CN106458956B (zh) 2019-06-14
JP6673850B2 (ja) 2020-03-25
EP3131894A1 (en) 2017-02-22
MX2016013447A (es) 2017-01-18
US9926302B2 (en) 2018-03-27
US9879000B2 (en) 2018-01-30
EP3495360A1 (en) 2019-06-12
CN106458956A (zh) 2017-02-22
US20170121314A1 (en) 2017-05-04
AU2015246387A1 (en) 2016-12-01
CA2945535A1 (en) 2015-10-22
JP2017511352A (ja) 2017-04-20
BR112016023860A2 (pt) 2017-08-15
AR100073A1 (es) 2016-09-07

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