AR038259A1 - Derivados sustituidos de aril-1,4-pirazina, composiciones farmaceuticas que los contienen, su uso para la elaboracion de medicamentos, articulo de fabricacion que los comprende, metodo para inhibir la union del crf al receptor de crf1, metodo para clasificar ligandos de receptores del crf y metodo p - Google Patents

Derivados sustituidos de aril-1,4-pirazina, composiciones farmaceuticas que los contienen, su uso para la elaboracion de medicamentos, articulo de fabricacion que los comprende, metodo para inhibir la union del crf al receptor de crf1, metodo para clasificar ligandos de receptores del crf y metodo p

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Publication number
AR038259A1
AR038259A1 ARP020104440A ARP020104440A AR038259A1 AR 038259 A1 AR038259 A1 AR 038259A1 AR P020104440 A ARP020104440 A AR P020104440A AR P020104440 A ARP020104440 A AR P020104440A AR 038259 A1 AR038259 A1 AR 038259A1
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AR
Argentina
Prior art keywords
heterocycloalkyl
substituted
heteroaryl
pyrazine
aryl
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ARP020104440A
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English (en)
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Upjohn Co
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Publication date
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Publication of AR038259A1 publication Critical patent/AR038259A1/es

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    • 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
    • C07D241/18—Oxygen or sulfur atoms
    • 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
    • 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
    • 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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • 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
    • 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
    • C07D401/12—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
    • 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
    • C07D401/14—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/74—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving hormones or other non-cytokine intercellular protein regulatory factors such as growth factors, including receptors to hormones and growth factors
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/575—Hormones
    • G01N2333/5751—Corticotropin releasing factor [CRF] (Urotensin)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/02—Screening involving studying the effect of compounds C on the interaction between interacting molecules A and B (e.g. A = enzyme and B = substrate for A, or A = receptor and B = ligand for the receptor)
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S206/00—Special receptacle or package
    • Y10S206/828—Medicinal content

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Physics & Mathematics (AREA)
  • Food Science & Technology (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • Microbiology (AREA)
  • General Physics & Mathematics (AREA)
  • Endocrinology (AREA)
  • Pathology (AREA)
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  • Cell Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un compuesto que comprende un derivado sustituido de aril-1,4-pirazina de fórmula (1) o un estereoisómero de dicha fórmula, una sal farmacéuticamente aceptable de dicha fórmula, ó un profármaco de dicha fórmula, en donde en la fórmula (1): X se selecciona entre NR3R4, -OR3, -CR3R5R5, -C(O)R3,-S(O)mR3, -NR3C(O)R4, -NR3S(O)mR4, m es 0, 1 ó 2; Ar se selecciona entre arilo, arilo sustituido, heteroarilo, heteroarilo sustituido; R1, R2 y R5 se seleccionan independientemente entre halógeno, -NO2, -CN, -Ra, -ORa, -S(O)mRa, -NRaRa, -C(O)NRaRa, -C(S)NRaRa-S(O)mNRaRa,-NRaS(O)mRa, -NRaC(O)ORa, -OC(O)NRaRa, -NRaC(O)NRaRa, -NRaC(S)NRaRa, -C(O)ORa, -C(S)ORa, y -OC(O)ORa; R3 y R4 se seleccionan independientemente entre Ra, heterocicloalquilo, heterocicloalquilo sustituido, heteroarilo sustituido, arilo sustituido, aril-cicloalquilo, aril-cicloalquilo sustituido, heteroaril-cicloalquilo, heteroaril-cicloalquilo sustituido, aril-heterocicloalquilo, aril-heterocicloalquilo sustituido, heteroaril-heterocicloalquilo, ó heteroaril-heterocicloalquilo sustituido siempre que por lo menos uno entre R3 ó R4 sea heteroarilo, heteroarilo sustituido, aril-cicloalquilo, aril-cicloalquilo sustituido, heteroaril-cicloalquilo, heteroaril-cicloalquilo sustituido, aril-heterocicloalquilo, aril-heterocicloalquilo sustituido, heteroaril-heterocicloalquilo, heteroaril-heterocicloalquilo sustituido, heterocicloalquilo ó heterocicloalquilo sustituido; cada Ra se selecciona entre H, alquilo, cicloalquilo, haloalquilo, arilo, heteroarilo, ó heterocicloalquilo opcionalmente sustituido con 1 a 5 de Rt, -ORt, -S(O)mRt, NRtRt, oxo(=O), tiona (=S), fenilo, heteroarilo, ó heterocicloalquilo en donde fenilo, heteroarilo, y heterocicloalquilo están opcionalmente sustituidos con 1 a 5 grupos seleccionados independientemente entre Rt; y cada Rt se selecciona entre H, halógeno, -NO2, -NH2, -OH, -SH, -CN, -C(O)NH2, -C(O)-NH alquilo, -C(O)N alquilalquilo, -O alquilo, NH alquilo, Nalquilalquilo, -S(O)malquilo, SO2NH2, SO2NHalquilo y SO2N alquilalquilo, alquilo, cicloalquilo, haloalquilo, fenilo, bencilo, heteroarilo, ó heterocicloalquilo en donde fenilo, bencil-heteroarilo y heterocicloalquilo pueden estar opcionalmente sustituidos con alquilo o halógeno, siempre que el compuesto no sea: 2,5-dimetil-3-(2,4-diclorofenil)-6-[(1-metilpiperidin-4-il)oxi]pirazina; 2,5-dimetil-3-(2,4-diclorofenil)-6-(tetrahidrofuran-3-il)oxi]pirazina; 2,5-dimetil-3-(2,4-diclorofenil)-6-(tetrahidro-2H-piran-4-iloxi)pirazina, 2,5-dimetil-3-(2,4-diclorofenil)-6-[(1-metilpiperidin-3-il)oxi]pirazina, 2,5-dimetil-3-(2,4-diclorofenil)-6-[1-etilpiperdin-3-il)oxi]pirazina, 2,5-dimetil-3-(2,4-diclorofenil)-6-(1-piperidin-4-il)oxi]pirazina, 2,5-dimetil-3-(2,4-diclorofenil)-6-piperidin-3-il)oxi]pirazina, 2,5-dimetil-3-(2,4-diclorofenil)-6-[(1-etilpirrolidin-3-il)oxi]pirazina, 2,5-dimetil-3-(2,4-diclorofenil)-6-[(1-metilpirrolidin-3-il)oxi]pirazina, 2,5-dimetil-3-(2,4-diclorofenil)-6-[(pirrolidin-3-il)oxi]pirazina, 2,5-dimetil-3-(2,4-diclorofenil)-6-[(piridin-4-il)oxi]pirazina. También se dan a conocer composiciones farmacéuticas que los contienen, su uso para la elaboración de medicamentos, artículo de fabricación que los comprende, método para inhibir la unión del CRF al receptor CRF1, método para clasificar ligandos de receptores del CRF y método para detectar receptores del CRF en tejidos. Estos compuestos son útiles para la elaboración de medicamentos útiles para el tratamiento de trastornos de ansiedad, depresión y trastornos relacionados con el estrés.
ARP020104440A 2001-11-21 2002-11-19 Derivados sustituidos de aril-1,4-pirazina, composiciones farmaceuticas que los contienen, su uso para la elaboracion de medicamentos, articulo de fabricacion que los comprende, metodo para inhibir la union del crf al receptor de crf1, metodo para clasificar ligandos de receptores del crf y metodo p AR038259A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US33205201P 2001-11-21 2001-11-21
US35854602P 2002-02-21 2002-02-21
US38828502P 2002-06-13 2002-06-13
US41037802P 2002-09-13 2002-09-13

Publications (1)

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AR038259A1 true AR038259A1 (es) 2005-01-12

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ARP020104440A AR038259A1 (es) 2001-11-21 2002-11-19 Derivados sustituidos de aril-1,4-pirazina, composiciones farmaceuticas que los contienen, su uso para la elaboracion de medicamentos, articulo de fabricacion que los comprende, metodo para inhibir la union del crf al receptor de crf1, metodo para clasificar ligandos de receptores del crf y metodo p

Country Status (4)

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US (2) US6992087B2 (es)
AR (1) AR038259A1 (es)
MY (1) MY130489A (es)
TW (1) TWI292758B (es)

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7704995B2 (en) * 2002-05-03 2010-04-27 Exelixis, Inc. Protein kinase modulators and methods of use
CA2548172A1 (en) * 2003-12-04 2005-06-23 Vertex Pharmaceuticals Incorporated Quinoxalines useful as inhibitors of protein kinases
US20060211710A1 (en) * 2005-03-17 2006-09-21 Pfizer Inc Substituted aryl 1,4-pyrazine derivatives
EP1963302B1 (en) * 2005-12-05 2013-02-27 Pfizer Products Inc. Polymorphs of a c-met/hgfr inhibitor
BRPI0619424B1 (pt) * 2005-12-05 2022-02-08 Pfizer Products Inc Uso de inibidores c-met/hgfrs para a fabricação de medicamentos
EP2038261A2 (en) * 2006-06-22 2009-03-25 Mallinckrodt Inc. Pyrazine derivatives with extended conjugation and uses thereof
RU2011123647A (ru) 2008-11-10 2012-12-20 Вертекс Фармасьютикалз Инкорпорейтед Соединения, полезные в качестве ингибиторов atr киназы
CA3013000C (en) * 2008-12-19 2022-12-13 Vertex Pharmaceuticals Incorporated Pyrazine derivatives useful as inhibitors of atr kinase
CA2798760A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated 2-aminopyridine derivatives useful as inhibitors of atr kinase
EP2569286B1 (en) 2010-05-12 2014-08-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
SG185524A1 (en) 2010-05-12 2012-12-28 Vertex Pharma Compounds useful as inhibitors of atr kinase
EP2569287B1 (en) 2010-05-12 2014-07-09 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
EP2568984A1 (en) 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2011143419A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Pyrazines useful as inhibitors of atr kinase
EP2585468A1 (en) 2010-06-23 2013-05-01 Vertex Pharmaceuticals Incorporated Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase
JP2014510151A (ja) 2011-04-05 2014-04-24 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｒキナーゼ（ｔｒａｋｉｎａｓｅ）阻害剤として有用なアミノピラジン化合物
US8822469B2 (en) 2011-06-22 2014-09-02 Vertex Pharmaceuticals Incorporated Pyrrolo[2,3-B]pyrazines useful as inhibitors of ATR kinase
EP2723746A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
JP2014522818A (ja) 2011-06-22 2014-09-08 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｒキナーゼ阻害剤として有用な化合物
CA2850491C (en) 2011-09-30 2020-10-27 Vertex Pharmaceuticals Incorporated Treating pancreatic cancer and non-small cell lung cancer with atr inhibiors
WO2013049726A2 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Processes for making compounds useful as inhibitors of atr kinase
EP2751088B1 (en) 2011-09-30 2016-04-13 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
CA2850564A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8853217B2 (en) 2011-09-30 2014-10-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2013071088A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8841450B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
JP2015502925A (ja) 2011-11-09 2015-01-29 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ａｔｒキナーゼの阻害剤として有用なピラジン化合物
WO2013071090A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2776429A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
MX358818B (es) 2012-04-05 2018-09-05 Vertex Pharma Compuestos utiles como inhibidores de cinasa ataxia telangiectasia mutada y rad3 relacionados (atr) y terapias de combinacion de estos.
WO2014055756A1 (en) 2012-10-04 2014-04-10 Vertex Pharmaceuticals Incorporated Method for measuring atr inhibition mediated increases in dna damage
US8912198B2 (en) 2012-10-16 2014-12-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
CA2891122C (en) 2012-11-14 2021-07-20 The Johns Hopkins University Methods and compositions for treating schizophrenia
ES2946360T3 (es) 2012-12-07 2023-07-17 Vertex Pharma Pirazolo[1,5-a]pirimidinas útiles como inhibidores de ATR quinasa para el tratamiento de enfermedades de cáncer
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
RU2687276C2 (ru) 2013-12-06 2019-05-13 Вертекс Фармасьютикалз Инкорпорейтед Соединения, пригодные для использования в качестве ингибиторов atr киназы
KR101859315B1 (ko) * 2014-05-30 2018-05-18 제이에프이 스틸 가부시키가이샤 열연 강판의 제조 방법, 강판 절단 위치 설정 장치, 강판 절단 위치 설정 방법, 및 강판 제조 방법
LT3152212T (lt) 2014-06-05 2020-05-11 Vertex Pharmaceuticals Inc. Radioaktyviai žymėti 2-amino-6-fluor-n-[5-fluor-piridin-il]- pirazolo[1,5-a]pirimidin-3-karboksamido junginio dariniai, naudingi kaip atr kinazės inhibitoriai, minėto junginio gamybos būdas ir jo skirtingos kietos formos
SG11201610500WA (en) 2014-06-17 2017-01-27 Vertex Pharma Method for treating cancer using a combination of chk1 and atr inhibitors
CA3000684A1 (en) 2015-09-30 2017-04-06 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of dna damaging agents and atr inhibitors
CN111093666A (zh) 2017-07-18 2020-05-01 诺维逊生物股份有限公司 1,8-萘啶酮化合物及其用途
AU2018302179A1 (en) 2017-07-18 2020-02-13 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
WO2019213386A1 (en) * 2018-05-04 2019-11-07 New Mexico Tech University Research Park Corporation Proteasome inhibitors
JP2022517419A (ja) * 2019-01-18 2022-03-08 ニューベイション・バイオ・インコーポレイテッド アデノシンアンタゴニストとしてのヘテロ環式化合物
WO2020150677A1 (en) * 2019-01-18 2020-07-23 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
EP3911324A4 (en) 2019-01-18 2022-08-17 Nuvation Bio Inc. 1,8-NAPHTHYRIDINONE COMPOUNDS AND THEIR USES
WO2020163409A1 (en) * 2019-02-05 2020-08-13 Skyhawk Therapeutics, Inc. Methods and compositions for modulating splicing
JP2022521467A (ja) 2019-02-05 2022-04-08 スカイホーク・セラピューティクス・インコーポレーテッド スプライシングを調節するための方法および組成物
KR20210135507A (ko) 2019-02-06 2021-11-15 스카이호크 테라퓨틱스, 인코포레이티드 스플라이싱을 조절하는 방법 및 조성물

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69701868T2 (de) 1996-03-27 2000-11-02 Akzo Nobel Nv Alkydharze mit niedriger dynamischer viskosität zur verwendung in festkörperreichen beschichtungsmitteln
US5883105A (en) 1996-04-03 1999-03-16 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5880140A (en) 1996-04-03 1999-03-09 Merck & Co., Inc. Biheteroaryl inhibitors of farnesyl-protein transferase
US5872136A (en) 1996-04-03 1999-02-16 Merck & Co., Inc. Arylheteroaryl inhibitors of farnesyl-protein transferase
WO1997036886A1 (en) 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1997036898A1 (en) 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JP2001507699A (ja) 1996-12-30 2001-06-12 メルク エンド カンパニー インコーポレーテッド ファルネシル蛋白トランスフェラーゼ阻害薬
MA26473A1 (fr) 1997-03-01 2004-12-20 Glaxo Group Ltd Composes pharmacologiquement actifs.
PA8467401A1 (es) 1998-02-17 2000-09-29 Pfizer Prod Inc Procedimiento para tratar la insuficiencia cardiaca
MXPA02007868A (es) 2000-02-16 2003-02-10 Neurogen Corp Arilpirazinas sustituidas.

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