BR112012006176A2 - inibidores macrocíclicos de jak - Google Patents

inibidores macrocíclicos de jak

Info

Publication number
BR112012006176A2
BR112012006176A2 BR112012006176A BR112012006176A BR112012006176A2 BR 112012006176 A2 BR112012006176 A2 BR 112012006176A2 BR 112012006176 A BR112012006176 A BR 112012006176A BR 112012006176 A BR112012006176 A BR 112012006176A BR 112012006176 A2 BR112012006176 A2 BR 112012006176A2
Authority
BR
Brazil
Prior art keywords
macrocyclic
jak inhibitors
jak
inhibitors
variables
Prior art date
Application number
BR112012006176A
Other languages
English (en)
Inventor
Alam Jahangir
Hanbiao Yang
Michael Soth
Stephen M Lynch
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BR112012006176A2 publication Critical patent/BR112012006176A2/pt

Links

Classifications

    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/18—Bridged 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • 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
    • A61P17/04—Antipruritics
    • 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
    • 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
    • A61P25/28—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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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
    • 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
    • C07D487/22—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 four or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

inibidores macrocíclicos de jak. a presente invenção refere-se ao uso de novos compostos macrocíclicos da fórmula (i) em que as variáveis q, q~ 1~, q~ 2~, q~ 3~ e q~ 4~ são definidas como descritas aqui, o qual inibe jak e são úteis para o tratamento de doenças autoimunes e inflamatórias.
BR112012006176A 2009-09-21 2010-09-17 inibidores macrocíclicos de jak BR112012006176A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US24421609P 2009-09-21 2009-09-21
US37296910P 2010-08-12 2010-08-12
PCT/EP2010/063682 WO2011033053A1 (en) 2009-09-21 2010-09-17 Macrocyclic inhibitors of jak

Publications (1)

Publication Number Publication Date
BR112012006176A2 true BR112012006176A2 (pt) 2015-09-08

Family

ID=43034482

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012006176A BR112012006176A2 (pt) 2009-09-21 2010-09-17 inibidores macrocíclicos de jak

Country Status (11)

Country Link
US (1) US8318764B2 (pt)
EP (1) EP2480554B1 (pt)
JP (1) JP5540100B2 (pt)
KR (1) KR101438293B1 (pt)
CN (1) CN102498113B (pt)
BR (1) BR112012006176A2 (pt)
CA (1) CA2771176A1 (pt)
ES (1) ES2509590T3 (pt)
MX (1) MX2012002385A (pt)
RU (1) RU2012116003A (pt)
WO (1) WO2011033053A1 (pt)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112014007654A8 (pt) * 2011-09-30 2018-06-12 Ipsen Pharma Inibidores de lrrk2 quinase macrocíclicos.
CN102617599B (zh) * 2012-04-10 2014-04-16 江苏先声药物研究有限公司 大环类化合物及其应用
US9165142B1 (en) * 2013-01-30 2015-10-20 Palo Alto Networks, Inc. Malware family identification using profile signatures
WO2018153546A1 (en) * 2017-02-27 2018-08-30 Laboratorios Del Dr. Esteve, S.A. Tetrahydropyran and tetrahydrothiopyran methanone derivatives having multimodal activity against pain
US10764309B2 (en) 2018-01-31 2020-09-01 Palo Alto Networks, Inc. Context profiling for malware detection
US11159538B2 (en) 2018-01-31 2021-10-26 Palo Alto Networks, Inc. Context for malware forensics and detection
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
CN113735856A (zh) * 2020-05-29 2021-12-03 百极弘烨(南通)医药科技有限公司 大环jak抑制剂及其应用
US11956212B2 (en) 2021-03-31 2024-04-09 Palo Alto Networks, Inc. IoT device application workload capture
WO2023208244A1 (zh) * 2022-04-29 2023-11-02 南京明德新药研发有限公司 大环类化合物及其应用

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6235740B1 (en) 1997-08-25 2001-05-22 Bristol-Myers Squibb Co. Imidazoquinoxaline protein tyrosine kinase inhibitors
EP1066286B1 (en) 1998-03-04 2009-04-29 Bristol-Myers Squibb Company Heterocyclo-substituted imidazopyrazine protein tyrosine kinase inhibitors
US7652135B2 (en) 2003-09-23 2010-01-26 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
CN101522682A (zh) * 2006-10-30 2009-09-02 诺瓦提斯公司 作为抗炎剂的杂环化合物
EP2079740B1 (en) * 2006-11-01 2012-12-05 Vertex Pharmaceuticals, Inc. Tricyclic heteroaryl compounds useful as inhibitors of janus kinase
WO2008060248A1 (en) * 2006-11-15 2008-05-22 S*Bio Pte Ltd. Indole sustituted pyrimidines and use thereof in the treatment of cancer
ES2415863T3 (es) 2006-12-22 2013-07-29 Incyte Corporation Heterociclos sustituidos como inhibidores de Janus Quinasas
PT2299821E (pt) 2008-06-10 2016-03-11 Abbvie Inc Compostos tricíclicos

Also Published As

Publication number Publication date
ES2509590T3 (es) 2014-10-17
KR101438293B1 (ko) 2014-09-05
KR20120068940A (ko) 2012-06-27
CN102498113B (zh) 2014-11-26
US8318764B2 (en) 2012-11-27
JP2013505219A (ja) 2013-02-14
CN102498113A (zh) 2012-06-13
US20110071179A1 (en) 2011-03-24
RU2012116003A (ru) 2013-10-27
MX2012002385A (es) 2012-04-02
CA2771176A1 (en) 2011-03-24
WO2011033053A1 (en) 2011-03-24
EP2480554B1 (en) 2014-08-06
JP5540100B2 (ja) 2014-07-02
EP2480554A1 (en) 2012-08-01

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Legal Events

Date Code Title Description
B15I Others concerning applications: loss of priority

Free format text: PERDA DAS PRIORIDADES US 61/244,216 DE 21/09/2009 E US 61/372,969 DE 12/08/2010 REIVINDICADA NO PCT/EP2010/063682, CONFORME AS DISPOSICOES PREVISTAS NA LEI 9.279 DE 14/05/1996 (LPI) ART. 16 7O, ITEM 28 DO ATO NORMATIVO 128/97 E NO ART. 29 DA RESOLUCAO INPI-PR 77/2013. ESTA PERDA SE DEU PELO FATO DE O DEPOSITANTE CONSTANTE DA PETICAO DE REQUERIMENTO DE ENTRADA NA FASE NACIONAL SER DISTINTO DAQUELE QUE DEPOSITOU O PEDIDO ANTERIOR CUJA PRIORIDADE E REIVINDICADA E APRESENTOU COPIA DO CORRESPONDENTE DOCUMENTO DE CESSAO EM 25/05/2012, CONTUDO O PRAZO PARA A APRESENTACAO DA CESSAO DO DIREITO DE PRIORIDADE EXPIRAVA EM 18/05/2012 (60 DIAS APOS A ENTRADA DA FASE NACIONAL DO BRASIL), CONFORME AS DISP

B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 6A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2385 DE 20-09-2016 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.