AR106295A1 - Tetrahidropiranilsulfonas sustituidas con pirazolilo - Google Patents

Tetrahidropiranilsulfonas sustituidas con pirazolilo

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Publication number
AR106295A1
AR106295A1 ARP160103076A ARP160103076A AR106295A1 AR 106295 A1 AR106295 A1 AR 106295A1 AR P160103076 A ARP160103076 A AR P160103076A AR P160103076 A ARP160103076 A AR P160103076A AR 106295 A1 AR106295 A1 AR 106295A1
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Argentina
Prior art keywords
alkyl
cycloalkyl
membered heterocyclyl
group
heteroaryl
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ARP160103076A
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English (en)
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Michael Dr Koenigs Ren
Dr Reich Melanie
Dr Schunk Stefan
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Gruenenthal Gmbh
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Publication of AR106295A1 publication Critical patent/AR106295A1/es

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    • 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/24—Antidepressants
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular 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
    • C07D405/14—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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente se refiere a tetrahidropiranilsulfonas sustituidas con pirazolilo como bloqueadores de los canales de calcio dependientes de voltaje, a composiciones farmacéuticas que contienen estos compuestos y también a estos compuestos para utilizar en el tratamiento y/o profilaxis del dolor y de otras enfermedades y/o trastornos. Reivindicación 1: Un compuesto de fórmula general (1), donde R¹ se selecciona del grupo que consiste en H o alquilo C₁₋₆; R² se selecciona del grupo que consiste en H o alquilo C₁₋₆; R³ representa L’-R³ᵃ, donde L’ es un enlace o CH₂ y R³ᵃ se selecciona del grupo que consiste en alquilo C₁₋₆ sustituido, cicloalquilo C₃₋₆ o heterociclilo de 3 a 7 miembros, donde dicho alquilo C₁₋₆ sustituido está sustituido con uno o dos sustituyentes seleccionados independientemente del grupo que consiste en OH, OCH₃, S(=O)₂CH₃, N(CH₃)₂, C(=O)NH₂, C(=O)NH(CH₃) y C(=O)N(CH₃)₂; donde dicho cicloalquilo C₃₋₆ y dicho heterociclilo de 3 a 7 miembros están sin sustituir o sustituidos con uno o dos sustituyentes seleccionados independientemente del grupo que consiste en OH, OCH₃, =O, S(=O)₂CH₃, NH₂, NH(CH₃), N(CH₃)₂, C(=O)OH, C(=O)NH₂, C(=O)NH(CH₃) y C(=O)N(CH₃)₂; y donde dicho heterociclilo de 3 a 7 miembros contiene uno o dos heteroátomos o grupos de heteroátomos seleccionados independientemente del grupo que consiste en O, NH, N(CH₃), S(=O) y S(=O)₂; R⁴ representa L-R⁵, donde L es un enlace, CH₂, C(CH₃)₂, O ó S(=O)₂ y R⁵ se selecciona del grupo que consiste en alquilo C₁₋₆, cicloalquilo C₃₋₆ o heterociclilo de 3 a 7 miembros, donde dicho heterociclilo de 3 a 7 miembros se caracteriza porque contiene un heteroátomo o grupo de heteroátomos, seleccionados entre O, NH, N(CH₃), S(=O) y S(=O)₂; donde dicho alquilo C₁₋₆ está sin sustituir o sustituido con uno o dos o tres o cuatro sustituyentes seleccionados independientemente del grupo que consiste en F, Cl, CN, OH, OCH₃, OCFH₂, OCHF₂, OCF₃, S(=O)₂CH₃, S(=O)₂CHF₂, S(=O)₂CF₃, S(=O)₂CH(CH₃)₂, S(=O)₂(c-propilo), NH₂, NH(CH₃), N(CH₃)₂, C(=O)NH₂, C(=O)NH(CH₃) y C(=O)N(CH₃)₂; y donde dicho cicloalquilo C₃₋₆ o dicho heterociclilo de 3 a 7 miembros está sin sustituir o sustituido con uno o dos o tres o cuatro sustituyentes seleccionados independientemente del grupo que consiste en F, Cl, CN, CH₃, CFH₂, CHF₂, CF₃, =O, OH, OCH₃, CH₂OH, CH₂OCH₃, OCFH₂, OCHF₂, OCF₃, S(=O)₂CH₃, S(=O)₂CHF₂, S(=O)₂CF₃, S(=O)₂CH(CH₃)₂, S(=O)₂(c-propilo), NH₂, NH(CH₃), N(CH₃)₂, C(=O)NH₂, C(=O)NH(CH₃) y C(=O)N(CH₃)₂; Ar¹ representa arilo o heteroarilo, donde dicho arilo o dicho heteroarilo está sustituido con cero o uno o dos o tres sustituyentes R⁷, donde cada R⁷ se selecciona independientemente del grupo que consiste en F; Cl; Br; I; NO₂; CN; alquilo C₁₋₆; CF₃; CF₂H; CFH₂; CF₂Cl; CFCl₂; C(O)-H; C(O)-alquilo C₁₋₆; C(O)-OH; C(O)-O-alquilo C₁₋₆; C(O)-N(H)(OH); C(O)-NH₂; C(O)-N(H)(alquilo C₁₋₆); C(O)-N(alquilo C₁₋₆)₂; C(=N-OH)-H; C(=N-OH)-alquilo C₁₋₆; C(=N-O-alquil C₁₋₆)-H; C(=N-O-alquil C₁₋₆)-alquilo C₁₋₆; OH; OCF₃; OCF₂H; OCFH₂; OCF₂Cl; OCFCl₂; O-alquilo C₁₋₆; O-C(O)-alquilo C₁₋₆; O-C(O)-O-alquilo C₁₋₆; O-(CO)-N(H)(alquilo C₁₋₆); O-C(O)-N(alquilo C₁₋₆)₂; O-S(O)₂-alquilo C₁₋₆; O-S(O)₂-OH; O-S(O)₂-O-alquilo C₁₋₆; O-S(O)₂-NH₂; O-S(O)₂-N(H)(alquilo C₁₋₆); O-S(O)₂-N(alquilo C₁₋₆)₂; NH₂; N(H)(alquilo C₁₋₆); N(alquilo C₁₋₆)₂; N(H)-C(O)-alquilo C₁₋₆; N(H)-C(O)-O-alquilo C₁₋₆; N(H)-C(O)-NH₂; N(H)-C(O)-N(H)(alquilo C₁₋₆); N(H)-C(O)-N(alquilo C₁₋₆)₂; N(alquil C₁₋₆)-C(O)-alquilo C₁₋₆; N(alquil C₁₋₆)-C(O)-O-alquilo C₁₋₆; N(alquil C₁₋₆)-C(O)-NH₂; N(alquil C₁₋₆)-C(O)-N(H)(alquilo C₁₋₆); N(alquil C₁₋₆)-C(O)-N(alquilo C₁₋₆)₂; N(H)-S(O)₂OH; N(H)-S(O)₂-alquilo C₁₋₆; N(H)-S(O)₂-O-alquilo C₁₋₆; N(H)-S(O)₂-NH₂; N(H)-S(O)₂-N(H)(alquilo C₁₋₆); N(H)-S(O)₂N(alquilo C₁₋₆)₂; N(alquil C₁₋₆)-S(O)₂-OH; N(alquil C₁₋₆)-S(O)₂-alquilo C₁₋₆; N(alquil C₁₋₆)-S(O)₂-O-alquilo C₁₋₆; N(alquil C₁₋₆)-S(O)₂-NH₂; N(alquil C₁₋₆)-S(O)₂-N(H)(alquilo C₁₋₆); N(alquil C₁₋₆)-S(O)₂-N(alquilo C₁₋₆)₂; SH; SCF₃; SCF₂H; SCFH₂; SCF₂Cl; SCFCl₂; S-alquilo C₁₋₆; S(O)-alquilo C₁₋₆; S(O)₂-alquilo C₁₋₆; S(O)₂-OH; S(O)₂-O-alquilo C₁₋₆; S(O)₂-NH₂; S(O)₂-N(H)(alquilo C₁₋₆); S(O)₂-N(alquilo C₁₋₆)₂; cicloalquilo C₃₋₆; heterociclilo de 3 a 7 miembros; arilo; heteroarilo; O-cicloalquilo C₃₋₆; O-(heterociclilo de 3 a 7 miembros); O-arilo; O-heteroarilo; N(H)-cicloalquilo C₃₋₆; N(H)-(heterociclilo de 3 a 7 miembros); N(H)-arilo; N(H)-heteroarilo; N(alquil C₁₋₆)-cicloalquilo C₃₋₆; N(alquil C₁₋₆)-(heterociclilo de 3 a 7 miembros); N(alquil C₁₋₆)-arilo; N(alquil C₁₋₆)-heteroarilo; C(O)-cicloalquilo C₃₋₆; C(O)-(heterociclilo de 3 a 7 miembros); C(O)-arilo; C(O)-heteroarilo; S(O)₂-cicloalquilo C₃₋₆; S(O)₂-(heterociclilo de 3 a 7 miembros); S(O)₂-arilo; S(O)₂-heteroarilo; S(O)(NR¹³)-cicloalquilo C₃₋₆; S(O)(NR¹³)-(heterociclilo de 3 a 7 miembros); S(O)(NR¹³)-arilo y S(O)(NR¹³)-heteroarilo, donde R¹³ representa H o alquilo C₁₋₆; con la condición de que el compuesto de fórmula general (1) no sea 1-(2-metoxietil)-5-(4-metil-4-((3-(trifluorometil)fenil)sulfonil)tetrahidro-2H-piran-2-il)-3-(trifluorometil)-1H-pirazol, opcionalmente en forma de un estereoisómero único o una mezcla de estereoisómeros, en forma del compuesto libre y/o una sal fisiológicamente aceptable y/o un solvato fisiológicamente aceptable del mismo.
ARP160103076A 2015-10-08 2016-10-07 Tetrahidropiranilsulfonas sustituidas con pirazolilo AR106295A1 (es)

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EP15002880 2015-10-08

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US (1) US10100041B2 (es)
JP (1) JP2018530569A (es)
CN (1) CN108473480A (es)
AR (1) AR106295A1 (es)
AU (1) AU2016336777A1 (es)
BR (1) BR112018007004A2 (es)
CA (1) CA3001949A1 (es)
HK (1) HK1258461A1 (es)
MX (1) MX2018004217A (es)
TW (1) TW201726128A (es)
WO (1) WO2017059966A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2016013451A (es) 2014-04-14 2017-01-18 Gruenenthal Gmbh Heterociclilsulfonas arilo sustituidas.
TW201620899A (zh) 2014-04-14 2016-06-16 歌林達有限公司 經雜芳基取代之雜環碸
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
WO2021076835A1 (en) * 2019-10-18 2021-04-22 Fmc Corporation Methods for the preparation of 5-bromo-2-(3chloro-pyridin-2-yl)-2h-pyrazole-3-carboxylic acid

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007125398A2 (en) 2006-04-27 2007-11-08 Pfizer Japan Inc. : sulfonamide compounds as antagonists of the n-type calcium channel
EP2158183A2 (en) * 2007-05-25 2010-03-03 Vertex Pharmaceuticals Incorporated Ion channel modulators and methods of use
GB0813142D0 (en) 2008-07-17 2008-08-27 Glaxo Group Ltd Novel compounds
NZ598269A (en) * 2009-09-18 2014-12-24 Zalicus Pharmaceuticals Ltd Aryl sulphone derivatives as calcium channel blockers
KR20150042834A (ko) * 2012-08-16 2015-04-21 얀센 파마슈티카 엔.브이. N형 칼슘 채널 차단제로서의 치환된 피라졸
AU2013302468B2 (en) * 2012-08-16 2017-08-24 Janssen Pharmaceutica Nv Substituted pyrazoles as N-type calcium channel blockers
TW201416348A (zh) * 2012-08-29 2014-05-01 Gruenenthal Chemie 以氟甲基取代之吡咯甲醯胺
MX2016013451A (es) * 2014-04-14 2017-01-18 Gruenenthal Gmbh Heterociclilsulfonas arilo sustituidas.
TW201620899A (zh) 2014-04-14 2016-06-16 歌林達有限公司 經雜芳基取代之雜環碸
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

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BR112018007004A2 (pt) 2018-10-16
JP2018530569A (ja) 2018-10-18
CA3001949A1 (en) 2017-04-13
HK1258461A1 (zh) 2019-11-15
US20170101398A1 (en) 2017-04-13
TW201726128A (zh) 2017-08-01
CN108473480A (zh) 2018-08-31
WO2017059966A1 (en) 2017-04-13
AU2016336777A1 (en) 2018-04-12
US10100041B2 (en) 2018-10-16
MX2018004217A (es) 2018-06-13

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