BR112015001545A2 - composto, uso de um composto, e, composição farmacêutica - Google Patents

composto, uso de um composto, e, composição farmacêutica

Info

Publication number
BR112015001545A2
BR112015001545A2 BR112015001545A BR112015001545A BR112015001545A2 BR 112015001545 A2 BR112015001545 A2 BR 112015001545A2 BR 112015001545 A BR112015001545 A BR 112015001545A BR 112015001545 A BR112015001545 A BR 112015001545A BR 112015001545 A2 BR112015001545 A2 BR 112015001545A2
Authority
BR
Brazil
Prior art keywords
alkyl
hydrogen
compound
alkoxy
pharmaceutical composition
Prior art date
Application number
BR112015001545A
Other languages
English (en)
Other versions
BR112015001545B1 (pt
Inventor
Louise Walker Ann
Wellaway Christopher
Douault Clement
Matthew Wilson David
Diallo Hawa
Liddle John
Campbell Matthew
David Barker Michael
Stuart Garton Neil
John Sheppard Robert
John Atkinson Stephen
Original Assignee
Glaxo Group 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
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of BR112015001545A2 publication Critical patent/BR112015001545A2/pt
Publication of BR112015001545B1 publication Critical patent/BR112015001545B1/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (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)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

1 / 1 resumo “composto, uso de um composto, e, composiã‡ãƒo farmacãšutica” compostos da fã³rmula (i): (i) em que; r ã© hidrogãªnio ou alquila c ; r ã© hidrogãªnio, alquila c , per- 1 1-6 2 1-6 halometilalquilc -o-, ou alcã³xi c ; r ã© hidrogãªnio, alquila c , ou alcã³xi 0-5 1-6 3 1-6 c alquila c ; r ã© hidrogãªnio, alquila c , per-halometilalquila c ; ou 1-6 1-6 4 1-6 1-6 cicloalquilc - alquila c nã£o substituã­do; a ã© c-r ou n; b ã© c-r ou n; d 3 6 1-6 5 6 ã© c-r ou n; com a condiã§ã£o de que pelo menos um de a, b e d seja n; r ã© 7 5 hidrogãªnio ou alquila c ; r ã© hidrogãªnio ou alquila c ; r ã© hidrogãªnio, 1-6 6 1-6 7 alquila c , alcã³xi c , ou hidrã³xi; r ã© hidrogãªnio ou alquila c , com a 1-6 1-6 8 1-6 condiã§ã£o de que um de r e r seja hidrogãªnio; r ã© hidrogãªnio ou hidrã³xi; 4 8 9 r ã© hidrogãªnio ou alquila c ; e seus sais sã£o inibidores de pad4 e podem 10 1-6 ser usados no tratamento de vã¡rios distãºrbios, por exemplo, artrite reumatã³ide, vasculite, lãºpus eritematoso sistãªmico, colite ulcerativa, cã¢ncer, fibrose cã­stica, asma, lãºpus eritematoso cutã¢neo e psorã­ase.
BR112015001545-0A 2012-07-26 2012-07-26 Composto, composição farmacêutica, e, uso de um composto BR112015001545B1 (pt)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/EP2012/064649 WO2014015905A1 (en) 2012-07-26 2012-07-26 2 - (azaindol- 2 -yl) benz imidazoles as pad4 inhibitors

Publications (2)

Publication Number Publication Date
BR112015001545A2 true BR112015001545A2 (pt) 2017-07-04
BR112015001545B1 BR112015001545B1 (pt) 2022-07-05

Family

ID=49996626

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112015001545-0A BR112015001545B1 (pt) 2012-07-26 2012-07-26 Composto, composição farmacêutica, e, uso de um composto

Country Status (22)

Country Link
US (4) US9127003B2 (pt)
EP (1) EP2877467B1 (pt)
JP (1) JP6063567B2 (pt)
KR (1) KR101916443B1 (pt)
CN (1) CN104470919B (pt)
AU (1) AU2012386257B2 (pt)
BR (1) BR112015001545B1 (pt)
CA (1) CA2879341C (pt)
CY (1) CY1118524T1 (pt)
DK (1) DK2877467T3 (pt)
ES (1) ES2609126T3 (pt)
HR (1) HRP20161530T1 (pt)
HU (1) HUE033294T2 (pt)
IN (1) IN2014KN02935A (pt)
LT (1) LT2877467T (pt)
PL (1) PL2877467T3 (pt)
PT (1) PT2877467T (pt)
RS (1) RS55684B1 (pt)
RU (1) RU2611010C2 (pt)
SI (1) SI2877467T1 (pt)
SM (1) SMT201700052B (pt)
WO (1) WO2014015905A1 (pt)

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ES2770102T3 (es) * 2016-02-23 2020-06-30 Padlock Therapeutics Inc Inhibidores de heteroarilo de PAD4
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ES2828623T3 (es) * 2016-07-27 2021-05-27 Padlock Therapeutics Inc Inhibidores covalentes de PAD4
MA46193A (fr) * 2016-09-12 2019-07-17 Padlock Therapeutics Inc Inhibiteurs hétéroaryles de pad4
US11208386B2 (en) 2016-12-02 2021-12-28 University Of Massachusetts Inhibitors of protein arginine deiminases (PADs) and methods of preparation and use thereof
CN108689946B (zh) * 2017-04-12 2022-10-18 中国科学院上海药物研究所 2-取代硫基乙酰胺类化合物及其制备方法和应用
KR20200094734A (ko) * 2017-09-22 2020-08-07 주빌런트 에피파드 엘엘씨 Pad 억제제로서의 헤테로사이클릭 화합물
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PE20211067A1 (es) * 2018-08-08 2021-06-09 Bristol Myers Squibb Co Benzimidazoles sustituidos como inhibidores de pad4
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WO2021003078A1 (en) * 2019-07-03 2021-01-07 University Of Massachusetts Inhibitors of protein arginine deiminase 1 and methods of preparation and use thereof
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TW202140477A (zh) * 2020-02-12 2021-11-01 美商必治妥美雅史谷比公司 雜環ｐａｄ４抑制劑
CN111265526B (zh) * 2020-04-09 2021-03-19 黑龙江中医药大学 一种治疗胃癌的药物及其制备方法
BR112022021963A2 (pt) 2020-04-30 2022-12-13 Gilead Sciences Inc Inibidores macrocíclicos de peptidilarginina desiminases
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Also Published As

Publication number Publication date
RS55684B1 (sr) 2017-07-31
US9833449B2 (en) 2017-12-05
WO2014015905A1 (en) 2014-01-30
LT2877467T (lt) 2017-01-10
HRP20161530T1 (hr) 2017-02-10
DK2877467T3 (en) 2017-02-13
US20180161316A1 (en) 2018-06-14
KR20150038438A (ko) 2015-04-08
US10039755B2 (en) 2018-08-07
IN2014KN02935A (pt) 2015-05-08
US20150175600A1 (en) 2015-06-25
AU2012386257B2 (en) 2016-09-08
CA2879341A1 (en) 2014-01-30
CN104470919A (zh) 2015-03-25
HUE033294T2 (en) 2017-11-28
AU2012386257A1 (en) 2015-03-12
CY1118524T1 (el) 2017-07-12
US20170119750A1 (en) 2017-05-04
EP2877467B1 (en) 2016-11-02
SI2877467T1 (sl) 2017-02-28
CA2879341C (en) 2019-06-11
US9518054B2 (en) 2016-12-13
ES2609126T3 (es) 2017-04-18
CN104470919B (zh) 2016-07-06
JP2015522628A (ja) 2015-08-06
RU2014152456A (ru) 2016-09-20
US20160009716A1 (en) 2016-01-14
RU2611010C2 (ru) 2017-02-17
PT2877467T (pt) 2017-01-02
SMT201700052B (it) 2017-03-08
EP2877467A1 (en) 2015-06-03
KR101916443B1 (ko) 2018-11-08
US9127003B2 (en) 2015-09-08
PL2877467T3 (pl) 2017-08-31
BR112015001545B1 (pt) 2022-07-05
JP6063567B2 (ja) 2017-01-18

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