BR112015020287A2 - n-(4-(azaindazol-6-il)-fenil)-sulfonamidas e seu uso como agentes farmacêuticos - Google Patents

n-(4-(azaindazol-6-il)-fenil)-sulfonamidas e seu uso como agentes farmacêuticos

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Publication number
BR112015020287A2
BR112015020287A2 BR112015020287A BR112015020287A BR112015020287A2 BR 112015020287 A2 BR112015020287 A2 BR 112015020287A2 BR 112015020287 A BR112015020287 A BR 112015020287A BR 112015020287 A BR112015020287 A BR 112015020287A BR 112015020287 A2 BR112015020287 A2 BR 112015020287A2
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BR
Brazil
Prior art keywords
azaindazol
sulfonamides
phenyl
pharmaceutical agents
sgk
Prior art date
Application number
BR112015020287A
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English (en)
Other versions
BR112015020287B1 (pt
Inventor
Struebing Carsten
Schmidt Friedemann
Kleemann Heinz-Werner
Saas Joachim
Nazare Marc
Halland Nis
Weiss Tilo
Original Assignee
Sanofi 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.)
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Publication date
Application filed by Sanofi Sa filed Critical Sanofi Sa
Publication of BR112015020287A2 publication Critical patent/BR112015020287A2/pt
Publication of BR112015020287B1 publication Critical patent/BR112015020287B1/pt

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    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

resumo patente de invenção: "n-(4-(azaindazol-6-il)-fenil)-sulfona-midas e seu uso como agentes farmacêuticos". a presente invenção refere-se a n-(4-(azaindazol-6-il)-fenil)-sulfonamidas da fórmula i, onde ar, n, x, z, r1, r2 e r3 têm os significados indicados nas reivindicações. os compostos da fórmula i são compostos farmacologicamente ativos valiosos que modulam a atividade de proteína quinase, especificamente a atividade de quinase regulada por soro e glucocorticoide (sgk), em particular da isoforma de quinase regulada por soro e glucocorticoide 1 (sgk-1, sgk1), e são adequados para o tratamento de doenças onde atividade de sgk é inapropriada, por exemplo, distúrbios da articulação degenerativos ou processos inflamatórios tal como osteoartrite ou reumatismo. a invenção refere-se ainda a processos para a preparação dos compostos da fórmula i, seu uso como agentes farmacêuticos e composições farmacêuticas compreendendo os mesmos. 1/1
BR112015020287-0A 2013-03-13 2014-03-12 N-(4-(azaindazol-6-il)-fenil)-sulfonamidas, seu processo de preparação, composição farmacêutica, e uso do mesmo BR112015020287B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13305283.7 2013-03-13
EP13305283 2013-03-13
PCT/EP2014/054770 WO2014140065A1 (en) 2013-03-13 2014-03-12 N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals

Publications (2)

Publication Number Publication Date
BR112015020287A2 true BR112015020287A2 (pt) 2017-07-18
BR112015020287B1 BR112015020287B1 (pt) 2022-12-13

Family

ID=48040124

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BR112015020287-0A BR112015020287B1 (pt) 2013-03-13 2014-03-12 N-(4-(azaindazol-6-il)-fenil)-sulfonamidas, seu processo de preparação, composição farmacêutica, e uso do mesmo

Country Status (24)

Country Link
US (1) US9718825B2 (pt)
EP (1) EP2970259B1 (pt)
JP (1) JP6404241B2 (pt)
KR (2) KR102219160B1 (pt)
CN (1) CN105189502B (pt)
AR (1) AR095279A1 (pt)
AU (1) AU2014230805B2 (pt)
BR (1) BR112015020287B1 (pt)
CA (2) CA3111517A1 (pt)
CY (1) CY1119151T1 (pt)
DK (1) DK2970259T3 (pt)
ES (1) ES2618213T3 (pt)
HR (1) HRP20170337T1 (pt)
HU (1) HUE031540T2 (pt)
IL (1) IL240178A (pt)
LT (1) LT2970259T (pt)
MX (1) MX363658B (pt)
PL (1) PL2970259T3 (pt)
PT (1) PT2970259T (pt)
RU (1) RU2671864C2 (pt)
SG (1) SG11201506093SA (pt)
SI (1) SI2970259T1 (pt)
TW (1) TWI629275B (pt)
WO (1) WO2014140065A1 (pt)

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EP3325100A4 (en) 2015-07-17 2019-02-20 Memorial Sloan-Kettering Cancer Center COMBINED THERAPY USING PDK1 AND PI3K INHIBITORS
JOP20190053A1 (ar) 2016-09-23 2019-03-21 Novartis Ag مركبات أزا إندازول للاستخدام في إصابات الأوتار و/ أو الرباط
TWI651308B (zh) * 2016-09-23 2019-02-21 瑞士商諾華公司 用於肌腱及／或韌帶傷害之吲唑化合物
US11236083B2 (en) 2016-12-07 2022-02-01 Orimos Therapeutics Co., Ltd. Compounds and pharmaceutical compositions for modulating SGK activity, and methods thereof
TWI782056B (zh) * 2017-07-14 2022-11-01 日商鹽野義製藥股份有限公司 具有ｍｇａｔ２抑制活性的縮合環衍生物
KR20200036004A (ko) * 2017-08-01 2020-04-06 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 Jak 키나아제 억제제로서 피라졸로 및 트리아졸로 비시클릭 화합물
WO2020060268A1 (ko) 2018-09-20 2020-03-26 한미약품 주식회사 상피세포 성장인자 수용체 돌연변이 저해 효과를 갖는 신규 융합 피리미딘 골격 설폰아마이드 유도체
CN113498352A (zh) 2019-01-23 2021-10-12 施万生物制药研发Ip有限责任公司 作为jak抑制剂的咪唑并[1,5-a]吡啶、1,2,4-三唑并[4,3-a]吡啶和咪唑并[1,5-a]吡嗪
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JP2024502178A (ja) * 2021-01-13 2024-01-17 スリブ セラピューティクス インコーポレイテッド Ｓｇｋ－１を阻害するためのピラゾロ［３，４－ｄ］ピリミジン－６－イル－スルホンアミド誘導体
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WO2024011316A1 (en) * 2022-07-12 2024-01-18 Thryv Therapeutics Inc. Salts of n-[4-(4-[[2-(dimethylamino)ethyl]amino]-3-methyl-1h-pyrazolo[3,4-d]pyrimidin-6-yl)-2-fluorophenyl]-2,5-difluorobenzenesulfonamide and crystalline forms thereof
WO2024015055A1 (en) * 2022-07-13 2024-01-18 Thryv Therapeutics Inc. Pyrazolo[3,4-d]pyrimidin-6-yl-sulfonamide derivatives for the inhibition of sgk-1 and treatment of cancer

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Also Published As

Publication number Publication date
US20160024097A1 (en) 2016-01-28
CA2901534C (en) 2021-04-27
CA2901534A1 (en) 2014-09-18
IL240178A (en) 2016-08-31
AR095279A1 (es) 2015-09-30
CN105189502A (zh) 2015-12-23
CA3111517A1 (en) 2014-09-18
BR112015020287B1 (pt) 2022-12-13
TW201512194A (zh) 2015-04-01
MX2015011353A (es) 2015-12-16
US9718825B2 (en) 2017-08-01
TWI629275B (zh) 2018-07-11
RU2671864C2 (ru) 2018-11-07
JP6404241B2 (ja) 2018-10-10
AU2014230805B2 (en) 2018-02-15
KR20210021127A (ko) 2021-02-24
EP2970259A1 (en) 2016-01-20
RU2015143000A (ru) 2017-04-20
HRP20170337T1 (hr) 2017-04-21
WO2014140065A1 (en) 2014-09-18
JP2016514116A (ja) 2016-05-19
SI2970259T1 (sl) 2017-05-31
SG11201506093SA (en) 2015-09-29
CY1119151T1 (el) 2018-02-14
LT2970259T (lt) 2017-03-27
EP2970259B1 (en) 2016-12-21
PT2970259T (pt) 2017-03-10
KR20150130443A (ko) 2015-11-23
HUE031540T2 (en) 2017-07-28
KR102219160B1 (ko) 2021-02-23
AU2014230805A1 (en) 2015-09-24
IL240178A0 (en) 2015-09-24
ES2618213T3 (es) 2017-06-21
PL2970259T3 (pl) 2017-06-30
DK2970259T3 (en) 2017-03-20
CN105189502B (zh) 2017-05-31
MX363658B (es) 2019-03-28

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