AR080699A1 - Pirrolopirazinas como inhibidores de jak y syk - Google Patents

Pirrolopirazinas como inhibidores de jak y syk

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Publication number
AR080699A1
AR080699A1 ARP110100907A ARP110100907A AR080699A1 AR 080699 A1 AR080699 A1 AR 080699A1 AR P110100907 A ARP110100907 A AR P110100907A AR P110100907 A ARP110100907 A AR P110100907A AR 080699 A1 AR080699 A1 AR 080699A1
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AR
Argentina
Prior art keywords
lower alkyl
independently
cyano
cycloalkyl
alkoxy
Prior art date
Application number
ARP110100907A
Other languages
English (en)
Inventor
Robert Than Hendricks
Johannes Cornelius Hermann
Rama K Kondru
Yan Lou
Stephen M Lynch
Timothy D Owens
Michael Soth
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Hoffmann La Roche
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Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR080699A1 publication Critical patent/AR080699A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/02Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (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

Estos compuestos inhiben JAK y SYK, resultan utiles para el tratamiento de enfermedades autoinmunologicas e inflamatorias. Reivindicacion 1: Compuesto de formula (1) en la que Y es C(R1)2(C(R1')2)m, m es 0 o 1; cada R1 es H o R1a; cada R1a es, independientemente, alquilo inferior, alcoxi inferior, fenilo, bencilo, heteroarilo, cicloalquilo, heterocicloalquilo o cicloalquil-alquilo inferior, opcionalmente sustituido con uno o más R1a', R1a' es halogeno, alquilo inferior, haloalquilo inferior, alcoxi inferior, hidroxialquilo inferior, oxo, hidroxi o ciano, cada R1' es, independientemente, H, alquilo inferior o haloalquilo inferior, R2 es, independientemente, H o R2a, R2a es, independientemente, alquilo inferior, haloalquilo inferior, alcoxi inferior, hidroxialquilo inferior, ciano, alquilo inferior, cicloalquilo o heterocicloalquilo, o R2a y R1a conjuntamente forman un anillo, opcionalmente sustituido con uno o más de entre halogeno, alquilo inferior, ciano, ciano-alquilo inferior, hidroxi, haloalquilo inferior, hidroxialquilo inferior, alcoxi inferior, alquilamino inferior o dialquilamino inferior, R3 es, independientemente, H o R3a, R3a es, independientemente, alquilo inferior, haloalquilo inferior, alcoxi inferior, hidroxialquilo inferior, ciano-alquilo inferior, C(=O)R3a' o S(=O)2R3a', cada R3a' es, independientemente, H o alquilo inferior, Q es H, halogeno, hidroxi, ciano o Q', Q' es alquilo inferior, alquenilo inferior, alquinilo inferior, cicloalquilo, fenilo, cicloalquenilo, heterocicloalquilo o heteroarilo, opcionalmente sustituidos con uno o más Qa, Qa es Qb o Qc, Qb es halogeno, oxo, hidroxi, -CN, -SCH3, -S(O)2CH3, o -S(=O)CH3, Qc es Qd o Qe; o dos Qa conjuntamente forman un sistema de anillos bicíclico, opcionalmente sustituido con uno o más Qb o Qc; Qd es -O(Qe), -S(=O)2(Qe), -C(=O)N(Qe)2, -S(O)2(Qe), -C(=O)(Qe), -C(=O)O(Qe), -N(Qe)2, N(Qe)C(=O)(Qe), -N(Qe)C(=O)O(Qe), o -N(Qe)C(=O)N(Qe)2; cada Qe es, independientemente, H o Qe', cada Qe' es, independientemente, alquilo inferior, alcoxi inferior, fenilo, bencilo, heteroarilo, cicloalquilo, heterocicloalquilo o cicloalquil-alquilo inferior, opcionalmente sustituido con uno o más Qf, Qf es Qg o Qh, Qg es halogeno, hidroxi, ciano, oxo, o C(=O)(Qh), Qh es alquilo inferior, haloalquilo inferior, alcoxi inferior, amino, fenilo, bencilo, cicloalquilo, heterocicloalquilo o heteroarilo, opcionalmente sustituidos con uno o más Qi, y Qi es halogeno, hidroxi, ciano, alquilo inferior, haloalquilo inferior o alcoxi inferior, o una sal farmacéuticamente aceptable de los mismos.
ARP110100907A 2010-03-22 2011-03-21 Pirrolopirazinas como inhibidores de jak y syk AR080699A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US31599910P 2010-03-22 2010-03-22

Publications (1)

Publication Number Publication Date
AR080699A1 true AR080699A1 (es) 2012-05-02

Family

ID=43983677

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110100907A AR080699A1 (es) 2010-03-22 2011-03-21 Pirrolopirazinas como inhibidores de jak y syk

Country Status (12)

Country Link
US (1) US8481541B2 (es)
EP (1) EP2550274A1 (es)
JP (1) JP5667692B2 (es)
KR (1) KR20130004342A (es)
CN (1) CN102812029A (es)
AR (1) AR080699A1 (es)
BR (1) BR112012023752A2 (es)
CA (1) CA2786402A1 (es)
MX (1) MX2012010610A (es)
RU (1) RU2012142550A (es)
TW (1) TW201136936A (es)
WO (1) WO2011117160A1 (es)

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MX2012013378A (es) * 2010-05-20 2013-01-24 Hoffmann La Roche Derivados de pirrolo [2, 3-b] pirazina-7-carboxamida y sus uso como inhibidores de cinasa janus (jak) y cinasa tirosina del brazo (syk).
EP2571881A1 (en) * 2010-05-20 2013-03-27 F.Hoffmann-La Roche Ag Pyrrolopyrazine derivatives as syk and jak inhibitors
JP6096778B2 (ja) * 2011-09-01 2017-03-15 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト ピロロピラジンキナーゼ阻害剤
KR20140095513A (ko) 2011-11-01 2014-08-01 에프. 호프만-라 로슈 아게 이미다조피리다진 화합물
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TW202334164A (zh) 2022-01-12 2023-09-01 美商戴納立製藥公司 (S)-5-苄基-N-(5-甲基-4-側氧基-2,3,4,5-四氫吡啶並[3,2-b][1,4]氧氮呯-3-基)-4H-1,2,4-三唑-3-甲醯胺的晶型

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Also Published As

Publication number Publication date
US20110230414A1 (en) 2011-09-22
CN102812029A (zh) 2012-12-05
RU2012142550A (ru) 2014-04-27
TW201136936A (en) 2011-11-01
JP2013522337A (ja) 2013-06-13
KR20130004342A (ko) 2013-01-09
JP5667692B2 (ja) 2015-02-12
CA2786402A1 (en) 2011-09-29
EP2550274A1 (en) 2013-01-30
US8481541B2 (en) 2013-07-09
BR112012023752A2 (pt) 2019-09-24
WO2011117160A1 (en) 2011-09-29
MX2012010610A (es) 2012-10-03

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