ECSP12011638A - Derivados de piridina y pirazina como moduladores de cinasa de proteína - Google Patents

Derivados de piridina y pirazina como moduladores de cinasa de proteína

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Publication number
ECSP12011638A
ECSP12011638A EC2012011638A ECSP12011638A ECSP12011638A EC SP12011638 A ECSP12011638 A EC SP12011638A EC 2012011638 A EC2012011638 A EC 2012011638A EC SP12011638 A ECSP12011638 A EC SP12011638A EC SP12011638 A ECSP12011638 A EC SP12011638A
Authority
EC
Ecuador
Prior art keywords
piridine
protein kinase
kinase modulators
pirazine
derivatives
Prior art date
Application number
EC2012011638A
Other languages
English (en)
Inventor
Paul A Barsanti
Xiaodong Lin
Keith Pfister
Martin Sendzik
Jeff Jin
Cheng Hu
Robert Keyes
Robert Kucejko
Yue Pan
James Sutton
Lifeng Wan
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=ECSP12011638(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 ECSP12011638A publication Critical patent/ECSP12011638A/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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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • 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
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    • 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
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    • 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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    • 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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    • 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
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    • C—CHEMISTRY; METALLURGY
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    • 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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  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Diabetes (AREA)
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  • Biomedical Technology (AREA)
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  • Tropical Medicine & Parasitology (AREA)
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Abstract

La presente invención proporciona un compuesto de la fórmula (I): (I)y las sales farmacéuticamente aceptables, enantiómeros, estereoisómeros, rotámeros, tautómeros, diaestereómeros, o racematos del mismo. También se proporciona un método para el tratamiento de una enfermedad o condición mediada por CDK9.
EC2012011638A 2009-07-30 2012-01-30 Derivados de piridina y pirazina como moduladores de cinasa de proteína ECSP12011638A (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
ECSP12011638A true ECSP12011638A (es) 2012-02-29

Family

ID=42727614

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2012011638A ECSP12011638A (es) 2009-07-30 2012-01-30 Derivados de piridina y pirazina como moduladores de cinasa de proteína

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
WO2012101062A1 (en) * 2011-01-28 2012-08-02 Novartis Ag Substituted bi-heteroaryl compounds as cdk9 inhibitors and their uses
JP5947818B2 (ja) 2011-03-02 2016-07-06 リード ディスカバリー センター ゲーエムベーハー 薬学的活性化二置換ピリジン誘導体
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AU2012244745A1 (en) * 2011-04-19 2013-09-19 Bayer Intellectual Property Gmbh Substituted 4-Aryl-N-phenyl-1,3,5-triazin-2-amines
TW201636330A (zh) 2011-05-24 2016-10-16 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
CN103917527B (zh) 2011-09-16 2017-05-31 拜耳知识产权有限责任公司 二取代的5‑氟‑嘧啶
CN103930399B (zh) 2011-09-16 2016-03-16 拜耳知识产权有限责任公司 包含亚氨基亚磺酰基的二取代的5-氟嘧啶衍生物
WO2013059634A1 (en) 2011-10-20 2013-04-25 The Regents Of The University Of California Use of cdk9 inhibitors to reduce cartilage degradation
HK1209414A1 (en) 2012-10-18 2016-04-01 Bayer Pharma Aktiengesellschaft 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfone group
CN105102434A (zh) 2012-10-18 2015-11-25 拜耳药业股份公司 含砜基团的4-(邻)-氟苯基-5-氟嘧啶-2-基胺
ES2616441T3 (es) 2012-10-18 2017-06-13 Bayer Pharma Aktiengesellschaft Derivados de N-(piridin-2-il))pirimidin-4-amina que contienen un grupo sulfona
ME02880B (me) 2012-11-15 2018-04-20 Bayer Pharma AG Derivati 5-fluoro- n- (piridin -2-il}piridi n- 2 - amina koji sadrze sulfoksiminsku grupu
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
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EP3126338B1 (en) 2014-04-01 2019-09-04 Bayer Pharma Aktiengesellschaft Disubstituted 5-fluoro pyrimidine derivatives containing a sulfondiimine group
US9963464B2 (en) 2014-04-11 2018-05-08 Bayer Pharma Aktiengesellschaft Macrocyclic compounds
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
US10300073B2 (en) 2014-10-14 2019-05-28 The Regents Of The University Of California Use of CDK9 and BRD4 inhibitors to inhibit inflammation
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