AR100073A1 - Sulfonas heterocíclicas sustituidas con heteroarilos - Google Patents

Sulfonas heterocíclicas sustituidas con heteroarilos

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Publication number
AR100073A1
AR100073A1 ARP150101120A ARP150101120A AR100073A1 AR 100073 A1 AR100073 A1 AR 100073A1 AR P150101120 A ARP150101120 A AR P150101120A AR P150101120 A ARP150101120 A AR P150101120A AR 100073 A1 AR100073 A1 AR 100073A1
Authority
AR
Argentina
Prior art keywords
alkyl
heterocyclyl
cycloalkyl
heteroaryl
aryl
Prior art date
Application number
ARP150101120A
Other languages
English (en)
Inventor
Dr Schunk Stefan
Dr Reich Melanie
Dr Jakob Florian
Dr Damann Nils
Dr Haurand Michael
Dr Kless Achim
Dr Rogers Marc
Dr Sutton Kathy
Original Assignee
Gruenenthal Gmbh
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 Gmbh filed Critical Gruenenthal Gmbh
Publication of AR100073A1 publication Critical patent/AR100073A1/es

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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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic 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
    • A61K31/351—Heterocyclic 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
    • 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
    • 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
    • A61P25/28—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
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic 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
    • C07D309/08—Heterocyclic 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
    • 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
    • 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
    • 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
    • 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

Abstract

Compuestos útiles como bloqueadores de los canales de calcio activados por el voltaje (CaV). Composiciones farmacéuticas que las contienen. Su uso en el tratamiento y/o la profilaxis del dolor y de otras enfermedades y/o trastornos. Reivindicación 1: Un compuesto caracterizado porque es de fórmula general (1), donde m representa 0, 1 ó 2; n denota 0 ó 1; Y se selecciona entre el grupo que consiste en un enlace y -C(R³)₂-; donde cada R³ se selecciona en forma independiente entre el grupo que consiste en H y C₁₋₆-alquilo, o dos R³ forman junto con el átomo de C que los conecta un C₃₋₁₀-cicloalquilo o un heterociclilo de entre 3 y 7 miembros; L es -[C(R⁴)₂]ˣ-(X)ʸ-[C(R⁴)₂]ᶻ-, donde x es 0, 1 ó 2, y es 0 ó 1 y z es 0 ó 1, con la condición de que x ³ y; cada R⁴ se selecciona en forma independiente entre el grupo que consiste en H y C₁₋₆-alquilo, o dos R⁴ forman junto con el átomo de C que los conecta un C₃₋₁₀-cicloalquilo o un heterociclilo de entre 3 y 7 miembros o dos R⁴ forman junto con dos átomos de C adyacentes que los conectan un C₃₋₁₀-cicloalquilo o un heterociclilo de entre 3 y 7 miembros; X se selecciona entre el grupo que consiste en O, S, S(O)₂, N(H) o N(C₁₋₆-alquilo); R¹ se selecciona entre el grupo que consiste en H; F; Cl; CN; C₁₋₆-alquilo; C₁₋₆-alquil-O(R⁵) y C₁₋₆-alquil-N(R⁵)₂; donde cada R⁵ se selecciona en forma independiente entre H o C₁₋₆-alquilo o dos R⁵ forman junto con el átomo de N que los conecta un heterociclilo de entre 3 y 7 miembros; R² se selecciona entre el grupo que consiste en H; F; Cl; CN; C₁₋₆-alquilo; C₁₋₆-alquil-O(R⁶) y C₁₋₆-alquil-N(R⁶)₂; donde cada R⁶ se selecciona en forma independiente entre H o C₁₋₆-alquilo o dos R⁶ forman junto con el átomo de N que los conecta un heterociclilo de entre 3 y 7 miembros; Ar¹ representa arilo o heteroarilo, donde dicho arilo o dicho heteroarilo está sustituido con cero o uno o dos o tres sustituyentes R⁷; Ar² representa heteroarilo, sustituido con cero o uno o dos o tres sustituyentes R⁸; donde cada R⁷ y cada R⁸ se selecciona en forma independiente entre el grupo que consiste en F; Cl; Br; I; NO₂; CN; C₁₋₆-alquilo; CF₃; CF₂H; CFH₂; CF₂Cl; CFCl₂; C(=O)-H; C(=O)-C₁₋₆-alquilo; C(=O)-OH; C(=O)-O-C₁₋₆-alquilo; C(=O)-N(H)(OH); C(=O)-NH₂; C(=O)-N(H)(C₁₋₆-alquilo); C(=O)-N(C₁₋₆-alquilo)₂; C(=N-OH)-H; C(=N-OH)-C₁₋₆-alquilo; C(=N-O-C₁₋₆-alquil)-H; C(=N-O-C₁₋₆-alquil)-C₁₋₆-alquilo; OH; OCF₃; OCF₂H; OCFH₂; OCF₂Cl; OCFCl₂; O-C₁₋₆-alquilo; O-C(=O)-C₁₋₆-alquilo; O-C(=O)-O-C₁₋₆-alquilo; O-(C=O)-N(H)(C₁₋₆-alquilo); O-C(=O)-N(C₁₋₆-alquilo)₂; O-S(=O)₂-C₁₋₆-alquilo; O-S(=O)₂-OH; O-S(=O)₂-O-C₁₋₆-alquilo; O-S(=O)₂-NH₂; O-S(=O)₂-N(H)(C₁₋₆-alquilo); O-S(=O)₂-N(C₁₋₆-alquilo)₂; NH₂; N(H)(C₁₋₆-alquilo); N(C₁₋₆-alquilo)₂; N(H)-C(=O)-C₁₋₆-alquilo; N(H)-C(=O)-O-C₁₋₆-alquilo; N(H)-C(=O)-NH₂; N(H)-C(=O)-N(H)(C₁₋₆-alquilo); N(H)-C(=O)-N(C₁₋₆-alquilo)₂; N(C₁₋₆-alquil)-C(=O)-C₁₋₆-alquilo; N(C₁₋₆-alquil)-C(=O)-O-C₁₋₆-alquilo; N(C₁₋₆-alquil)-C(=O)-NH₂; N(C₁₋₆-alquil)-C(=O)-N(H)(C₁₋₆-alquilo); N(C₁₋₆-alquil)-C(=O)-N(C₁₋₆-alquilo)₂; N(H)-S(=O)₂OH; N(H)-S(=O)₂-C₁₋₆-alquilo; N(H)-S(=O)₂-O-C₁₋₆-alquilo; N(H)-S(=O)₂-NH₂; N(H)-S(=O)₂-N(H)(C₁₋₆-alquilo); N(H)-S(=O)₂N(C₁₋₆-alquilo)₂; N(C₁₋₆-alquil)-S(=O)₂-OH; N(C₁₋₆-alquil)-S(=O)₂-C₁₋₆-alquilo; N(C₁₋₆ alquil)-S(=O)₂-O-C₁₋₆-alquilo; N(C₁₋₆-alquil)-S(=O)₂-NH₂; N(C₁₋₆-alquil)-S(=O)₂-N(H)(C₁₋₆-alquilo); N(C₁₋₆-alquil)-S(=O)₂-N(C₁₋₆-alquilo)₂; SH; SCF₃; SCF₂H; SCFH₂; SCF₂Cl; SCFCl₂; S-C₁₋₆-alquilo; S(=O)-C₁₋₆-alquilo; S(=O)₂-C₁₋₆-alquilo; S(=O)₂-OH; S(=O)₂-O-C₁₋₆-alquilo; S(=O)₂-NH₂; S(=O)₂-N(H)(C₁₋₆-alquilo); S(=O)₂-N(C₁₋₆ alquilo)₂; C₃₋₁₀-cicloalquilo; heterociclilo de entre 3 y 7 miembros; arilo; heteroarilo; O-C₃₋₁₀-cicloalquilo; O-(heterociclilo de entre 3 y 7 miembros); O-arilo; O-heteroarilo; N(H)-C₃₋₁₀-cicloalquilo; N(H)-(heterociclilo de entre 3 y 7 miembros); N(H)-arilo; N(H)-heteroarilo; N(C₁₋₆-alquil)-C₃₋₁₀ cicloalquilo: N(C₁₋₆-alquil)-(heterociclilo de entre 3 y 7 miembros); N(C₁₋₆-alquil)-arilo; N(C₁₋₆-alquil)-heteroarilo; C(=O)-C₃₋₁₀-cicloalquilo; C(=O)-(heterociclilo de entre 3 y 7 miembros); C(=O)-arilo; C(=O)-heteroarilo; S(=O)₂-C₃₋₁₀-cicloalquilo; S(=O)₂-(heterociclilo de entre 3 y 7 miembros); S(=O)₂-arilo; S(=O)₂-heteroarilo; S(=O)(=NR¹³)-C₃₋₁₀-cicloalquilo; S(=O)(=NR¹³)-(heterociclilo de entre 3 y 7 miembros); S(=O)(=NR¹³)-arilo y S(=O)(=NR¹³)-heteroarilo, donde R¹³ representa H o C₁₋₆-alquilo; donde en cada caso dicho C₁₋₆-alquilo puede ser ramificado o lineal; no sustituido o monosustituido o polisustituido; y donde en cada caso dicho C₃₋₁₀-cicloalquilo, heterociclilo de entre 3 y 7 miembros, arilo y heteroarilo puede no estar sustituido o estar monosustituido o polisustituido; opcionalmente en forma de un estereoisómero aislado o una mezcla de estereoisómeros, en forma del compuesto libre y/o una sal aceptable para uso fisiológico y/o un solvato aceptable para uso fisiológico del mismo.
ARP150101120A 2014-04-14 2015-04-14 Sulfonas heterocíclicas sustituidas con heteroarilos AR100073A1 (es)

Applications Claiming Priority (1)

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EP14001346 2014-04-14

Publications (1)

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AR100073A1 true AR100073A1 (es) 2016-09-07

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US (2) US9879000B2 (es)
EP (2) EP3495360A1 (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)

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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
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
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
CA2968836A1 (en) 2016-06-13 2017-12-13 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
KR102269305B1 (ko) 2016-06-13 2021-06-25 길리애드 사이언시즈, 인코포레이티드 Fxr (nr1h4) 조정 화합물
CN110461328A (zh) 2017-03-28 2019-11-15 吉利德科学公司 治疗肝疾病的治疗组合
EP3892278B1 (en) 2018-12-06 2024-02-28 Daiichi Sankyo Company, Limited Cycloalkane-1,3-diamine derivative
DK3911647T3 (da) 2019-01-15 2024-02-26 Gilead Sciences Inc Isoxazol-forbindelse som FXR-agonist og farmaceutiske sammensætninger, der omfatter en sådan
JP2022519906A (ja) 2019-02-19 2022-03-25 ギリアード サイエンシーズ， インコーポレイテッド Ｆｘｒアゴニストの固体形態
CN114641471A (zh) * 2019-10-18 2022-06-17 Fmc公司 用于制备5-溴-2-(3-氯-吡啶-2-基)-2h-吡唑-3-甲酸的方法
KR20220084092A (ko) * 2019-10-18 2022-06-21 에프엠씨 코포레이션 5-브로모-2-(3-클로로-피리딘-2-일)-2h-피라졸-3-카복실산의 제조 방법

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EP1138680A1 (en) * 2000-03-29 2001-10-04 Pfizer Products Inc. Gem substituted sulfonyl hydroxamic acids as MMP inhibitors
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GB0813142D0 (en) * 2008-07-17 2008-08-27 Glaxo Group Ltd Novel compounds
EP2477963A4 (en) * 2009-09-18 2013-02-27 Zalicus Pharmaceuticals Ltd ARYLSULFON DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
EP3131884A1 (en) * 2014-04-14 2017-02-22 Grünenthal GmbH Aryl substituted heterocyclyl sulfones
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
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

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AU2015246387A1 (en) 2016-12-01
CA2945535A1 (en) 2015-10-22
US20170121314A1 (en) 2017-05-04
TW201620899A (zh) 2016-06-16
US20150291572A1 (en) 2015-10-15
CL2016002615A1 (es) 2017-04-28
US9879000B2 (en) 2018-01-30
JP6673850B2 (ja) 2020-03-25
KR20160144487A (ko) 2016-12-16
CN106458956A (zh) 2017-02-22
EP3495360A1 (en) 2019-06-12
EA032581B1 (ru) 2019-06-28
MX2016013447A (es) 2017-01-18
BR112016023860A2 (pt) 2017-08-15
US9926302B2 (en) 2018-03-27
WO2015158427A1 (en) 2015-10-22
AU2015246387B2 (en) 2018-11-22
JP2017511352A (ja) 2017-04-20
EP3131894A1 (en) 2017-02-22
CN106458956B (zh) 2019-06-14
EA201692049A1 (ru) 2017-04-28
IL248250A0 (en) 2016-11-30
PE20161366A1 (es) 2017-01-15

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