DOP2012000025A - Derivados de piridina y pirazina como moduladores de cinasa de proteina - Google Patents

Derivados de piridina y pirazina como moduladores de cinasa de proteina

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Publication number
DOP2012000025A
DOP2012000025A DO2012000025A DO2012000025A DOP2012000025A DO P2012000025 A DOP2012000025 A DO P2012000025A DO 2012000025 A DO2012000025 A DO 2012000025A DO 2012000025 A DO2012000025 A DO 2012000025A DO P2012000025 A DOP2012000025 A DO P2012000025A
Authority
DO
Dominican Republic
Prior art keywords
piridine
protein kinase
kinase modulators
pirazine
derivatives
Prior art date
Application number
DO2012000025A
Other languages
English (en)
Inventor
Paul A Barsanti
Cheng Hu
Jeff Jin
Robert Keyes
Robert Kucejko
Xiadong Lin
Yue Pan
Keith Pfister
Martin Sendzik
James Sutton
Original Assignee
Novartis Ag
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42727614&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=DOP2012000025(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of DOP2012000025A publication Critical patent/DOP2012000025A/es

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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
    • A61K31/495—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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • 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
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
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    • A61P13/10—Drugs for disorders of the urinary system of the bladder
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
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    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
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    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three 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
    • C07D241/20—Nitrogen atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Molecular Biology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)

Abstract

La presente invención proporciona un compuesto de la fórmula (I): y las sales farmacéuticamente aceptables, enantiómeros, estereoisómeros, rotámeros, tautómeros, diaestereómeros, o racematos del mismo. También se proporciona un procedimiento para la fabricación de un medicamento útil en el tratamiento de una enfermedad o condición mediada por CDK9.
DO2012000025A 2009-07-30 2012-01-27 Derivados de piridina y pirazina como moduladores de cinasa de proteina DOP2012000025A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US27315409P 2009-07-30 2009-07-30
US35772010P 2010-06-23 2010-06-23

Publications (1)

Publication Number Publication Date
DOP2012000025A true DOP2012000025A (es) 2012-06-15

Family

ID=42727614

Family Applications (1)

Application Number Title Priority Date Filing Date
DO2012000025A DOP2012000025A (es) 2009-07-30 2012-01-27 Derivados de piridina y pirazina como moduladores de cinasa de proteina

Country Status (31)

Country Link
US (3) US8415381B2 (es)
EP (1) EP2459535B1 (es)
JP (2) JP5650735B2 (es)
KR (1) KR101464052B1 (es)
CN (1) CN102482218B (es)
AR (1) AR077505A1 (es)
AU (1) AU2010277588B2 (es)
BR (1) BR112012008074A2 (es)
CA (1) CA2767066A1 (es)
CL (1) CL2012000092A1 (es)
CO (1) CO6612188A2 (es)
CR (1) CR20120051A (es)
CU (1) CU24091B1 (es)
DO (1) DOP2012000025A (es)
EA (1) EA023561B1 (es)
EC (1) ECSP12011638A (es)
ES (1) ES2536479T3 (es)
GE (1) GEP20146101B (es)
GT (1) GT201200022A (es)
IL (2) IL217524A0 (es)
MA (1) MA33540B1 (es)
MX (1) MX2012001281A (es)
MY (1) MY183373A (es)
NI (1) NI201200016A (es)
NZ (1) NZ597551A (es)
PE (1) PE20121127A1 (es)
SG (1) SG177660A1 (es)
TW (1) TW201107307A (es)
UY (1) UY32810A (es)
WO (1) WO2011012661A1 (es)
ZA (1) ZA201109166B (es)

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US8415381B2 (en) * 2009-07-30 2013-04-09 Novartis Ag Heteroaryl compounds and their uses
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
JP2014506878A (ja) * 2011-01-28 2014-03-20 ノバルティス アーゲー Ｃｄｋ９阻害剤としての置換ビ−ヘテロアリール化合物およびそれらの使用
CA2826464C (en) * 2011-03-02 2020-07-28 Lead Discovery Center Gmbh Pharmaceutically active disubstituted triazine derivatives
WO2012117059A1 (en) 2011-03-02 2012-09-07 Lead Discovery Center Gmbh Pharmaceutically active disubstituted pyridine derivatives
MX2013012233A (es) * 2011-04-19 2014-01-23 Bayer Pharma AG 4-aril-n-fenil-1,3,5-triazin-2-aminas sustituidas.
TWI555737B (zh) 2011-05-24 2016-11-01 拜耳知識產權公司 含有硫醯亞胺基團之４－芳基－ｎ－苯基－１，３，５－三氮雜苯－２－胺
EP2527332A1 (en) 2011-05-24 2012-11-28 Bayer Intellectual Property GmbH 4-Aryl-N-phenyl-1,3,5-triazin-2-amines containing a sulfoximine group as CDK9 inhibitors
EP2561867A1 (en) 2011-08-22 2013-02-27 Lead Discovery Center GmbH CDK9 inhibitors in the treatment of midline carcinoma
EP2562265A1 (en) 2011-08-22 2013-02-27 Lead Discovery Center GmbH Susceptibility to selective CDK9 inhibitors
CA2848616A1 (en) 2011-09-16 2013-03-21 Bayer Intellectual Property Gmbh Disubstituted 5-fluoro-pyrimidines
EP2755948B1 (en) 2011-09-16 2016-05-25 Bayer Intellectual Property GmbH Disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group
WO2013059634A1 (en) 2011-10-20 2013-04-25 The Regents Of The University Of California Use of cdk9 inhibitors to reduce cartilage degradation
CN105283453B (zh) 2012-10-18 2018-06-22 拜耳药业股份公司 含砜基的n-(吡啶-2-基)嘧啶-4-胺衍生物
CN104854091B (zh) 2012-10-18 2018-04-03 拜耳药业股份公司 含砜基团的5‑氟‑n‑(吡啶‑2‑基)吡啶‑2‑胺衍生物
US20150259300A1 (en) 2012-10-18 2015-09-17 Bayer Pharma Aktiengesellschaft 4-(ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amines containing a sulfone group
KR102242871B1 (ko) 2012-11-15 2021-04-20 바이엘 파마 악티엔게젤샤프트 술폭시민 기를 함유하는 5-플루오로-n-(피리딘-2-일)피리딘-2-아민 유도체
TW201418243A (zh) 2012-11-15 2014-05-16 Bayer Pharma AG 含有磺醯亞胺基團之ｎ－（吡啶－２－基）嘧啶－４－胺衍生物
JP6371385B2 (ja) 2013-07-04 2018-08-08 バイエル ファーマ アクチエンゲゼルシャフト スルホキシイミン置換５−フルオロ−ｎ−（ピリジン−２−イル）ピリジン−２−アミン誘導体およびそのｃｄｋ９キナーゼ阻害薬としての使用
CN106232596A (zh) 2014-03-13 2016-12-14 拜耳医药股份有限公司 含有砜基团的5‑氟‑n‑(吡啶‑2‑基)吡啶‑2‑胺衍生物
US9790189B2 (en) 2014-04-01 2017-10-17 Bayer Pharma Aktiengesellschaft Disubstituted 5-fluoro pyrimidine derivatives containing a sulfondiimine group
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