AR092266A1 - Inhibidores de ddr2 para el tratamiento de osteoartritis - Google Patents

Inhibidores de ddr2 para el tratamiento de osteoartritis

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Publication number
AR092266A1
AR092266A1 ARP130103053A ARP130103053A AR092266A1 AR 092266 A1 AR092266 A1 AR 092266A1 AR P130103053 A ARP130103053 A AR P130103053A AR P130103053 A ARP130103053 A AR P130103053A AR 092266 A1 AR092266 A1 AR 092266A1
Authority
AR
Argentina
Prior art keywords
group
hal
independently selected
mono
carbon atoms
Prior art date
Application number
ARP130103053A
Other languages
English (en)
Inventor
Dra Wucherer-Plietker Margarita
Dra Werkmann Daniela
Dra Gigout Anne
Dr Kuhn Daniel
Sawatzky Edgar
Original Assignee
Merck Patent Ges Mit Beschränkter Haftung
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 Merck Patent Ges Mit Beschränkter Haftung filed Critical Merck Patent Ges Mit Beschränkter Haftung
Publication of AR092266A1 publication Critical patent/AR092266A1/es

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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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4355—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • 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
    • A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
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    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • 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
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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    • 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
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61P19/00—Drugs for skeletal disorders
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    • 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
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    • A61P25/00—Drugs for disorders of the nervous system
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    • 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]
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    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/68—One oxygen atom attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • 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
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
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    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Reivindicación 1: Compuestos de la fórmula (1), en donde W es O, N, CH₂, CH₂CH₂, CH₂CHOH o -(CH₂)O-; X, Y, Q, U, T son, de modo independiente entre sí, C o N, siempre que uno o varios de X, Y, Q, U y T sean átomos de carbono y que M esté ligado a un átomo de carbono; V es un enlace simple o -CR⁴R⁵-; M es O ó -CR⁴R⁵-; R¹ es heteroarilo, heterociclilo o arilo mono- o bicíclico que contiene 3 a 14 átomos de carbono y 1 ó 4 heteroátomos, seleccionados de modo independiente de N, O y S, que no está sustituido o que está mono-, di- o trisustituido con R⁶; R² es H, A, CN, OH, OA o Hal; R³ es heteroarilo, heterociclilo o arilo mono- o bicíclico que contiene 3 a 14 átomos de carbono y 1 ó 4 heteroátomos, seleccionados de modo independiente de N, O y S, que no está sustituido o que está mono-, di- o trisustituido con R⁷; R⁴, R⁵ están seleccionados, de modo independiente entre sí, del grupo que consiste en H y A; R², R⁶ y R⁷ están seleccionados, de modo independiente entre sí, del grupo que consiste en H, A, =O, OH, OA, Hal, CH₂HaI, CH(Hal)₂, C(Hal)₃, NO₂, (CH₂)ₙCN, (CH₂)ₙNR⁸R⁹, (CH₂)ₙO(CH₂)ₖNR⁸R⁹, (CH₂)ₙNR⁸(CH₂)ₖNR⁸R⁹, (CH₂)ₙO(CH₂)ₖOR¹⁸, (CH₂)ₙNR⁸(CH₂)ₖOR⁹, (CH₂)ₙCOOR¹⁰, (CH₂)ₙCHOR¹⁰, (CH₂)ₙCHONR⁸R⁹, C(O)NR⁸R⁹, C(O)NHANH₂, (CH₂)ₙNR⁸COR¹⁰, (CH₂)ₙNR⁸CONR⁸R⁹, (CH₂)ₙNR⁸SO₂A, (CH₂)ₙSO₂NR⁸R⁹, (CH₂)ₙS(O)ᵘR¹⁰, (CH₂)ₙOC(O)R¹⁰, (CH₂)ₙC(O)R¹⁰, (CH₂)ₙSR⁸, CH=N-OA, CH₂CH=N-OA, (CH₂)ₙNHOA, (CH₂)ₙCH=N-R⁸, (CH₂)ₙOC(O)NR⁸R⁹, (CH₂)ₙNR⁸COOR¹⁰, (CH₂)ₙN(R⁸)CH₂CH₂OR¹⁰, (CH₂)ₙN(R⁸)CH₂CH₂OCF₃, CH₂)ₙN(R⁸)C(R¹⁰)HCOOR⁹, (CH₂)ₙN(R⁸)C(R¹⁰)HCOR⁹, (CH₂)ₙN(R⁸)CH₂CH₂N(R⁹)CH₂COOR⁸, (CH₂)ₙN(R⁸)CH₂CH₂NR⁸R⁹, CH=CHCOOR¹⁰, CH=CHCH₂NR⁸R⁹, CH=CHCH₂NR⁸R⁹, CH=CHCH₂OR¹⁰, (CH₂)ₙN(COOR¹⁰)COOR¹¹, (CH₂)ₙN(CONH₂)COOR¹⁰, (CH₂)ₙN(CONH₂)CONH₂, (CH₂)ₙN(CH₂COOR¹⁰)COOR¹¹, (CH₂)ₙN(CH₂CONH₂)COOR¹⁰, (CH₂)ₙN(CH₂CONH₂)CONH₂, (CH₂)ₙCHR¹⁰COR¹¹, (CH₂)ₙCHR¹⁰COOR¹¹, (CH₂)ₙCHR¹⁰CH₂OR¹¹, (CH₂)ₙOCN y (CH₂)ₙNCO; R⁸, R⁹ están seleccionados, de modo independiente entre sí, del grupo que consiste en H, A, (CH₂)ₘAr¹ y (CH₂)ₘHet o en NR⁸R⁹, R⁸ y R⁹ forman, junto con el átomo de N al que están unidos, un heterociclo de 5, 6 ó 7 miembros que opcionalmente contiene 1 ó 2 heteroátomos adicionales seleccionados de N, O y S; R¹⁰, R¹¹ están seleccionados, de modo independiente entre sí, del grupo que consiste en H, Hal, A, (CH₂)ₘAr² y (CH₂)ₘHet; A está seleccionado del grupo que consiste en alquilo, alquenilo y cicloalquilo; Ar¹, Ar² son, de modo independiente entre sí, residuos de hidrocarburos aromáticos que comprenden 5 a 12 y con preferencia, 5 a 10 átomos de carbono que están opcionalmente sustituidos con uno o varios sustituyentes seleccionados de un grupo que consiste en A, Hal, NO₂, CN, OR¹², NR¹²R¹³, COOR¹², CONR¹²R¹³, NR¹²COR¹³, NR¹²CONR¹²R¹³, NR¹²SO₂A, COR¹², SO₂R¹²R¹³, S(O)ᵘA y OOCR¹²; Het es un residuo heterocíclico mono- o bicíclico saturado, insaturado o aromático que contiene 3 a 14 átomos de carbono y 1 ó 4 heteroátomos, seleccionados de modo independiente de N, O y S, que está opcionalmente sustituido con uno o varios sustituyentes seleccionados de un grupo que consiste en A, Hal, NO₂, CN, OR¹², NR¹²R¹³, COOR¹², CONR¹²R¹³, NR¹²COR¹³, NR¹²CONR¹²R¹³, NR¹²SO₂A, COR¹², SO₂R¹²R¹², S(O)ᵘA y OOCR¹²; R¹², R¹³ están seleccionados, de modo independiente entre sí, del grupo que consiste en H, A y (CH₂)ₘAr³; Ar³ es un hidrocarburo aromático de 5 ó 6 miembros que está opcionalmente sustituido con uno o varios sustituyentes seleccionados de un grupo que consiste en metilo, etilo, propilo, 2-propilo, ter.-butilo, Hal, CN, OH, NH₂ y CF₃; k, u, n y m son, de modo independiente entre sí, 0, 1, 2, 3, 4 ó 5; Hal está seleccionado, de modo independiente entre sí, del grupo que consiste en F, Cl, Br y I; y sus sales, solvatos y estereoisómeros fisiológicamente aceptables, incluyendo sus mezclas en todas las proporciones.
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Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3030250B1 (de) * 2013-08-06 2019-08-28 Merck Patent GmbH Intraartikuläre applikation von pepstatin bei arthrose
WO2016070024A1 (en) * 2014-10-31 2016-05-06 Washington University Ddr2 inhibitors and methods of using
CN107922320A (zh) 2015-08-31 2018-04-17 东丽株式会社 尿素衍生物和其用途
RU2018109256A (ru) * 2015-08-31 2019-10-07 Торэй Индастриз, Инк. Производное мочевины и его применение
MA51285A (fr) 2017-12-18 2021-04-28 Chiesi Farm Spa Dérivés d'azaindole comme inhibiteurs de rho-kinase
WO2019152711A1 (en) 2018-01-31 2019-08-08 Diciphera Pharmaceuticals Llc. Combination therapy for the treatment of gastrointestinal stromal tumors
GB201909194D0 (en) * 2019-06-26 2019-08-07 Ucb Biopharma Sprl Therapeutic agents
WO2021030405A1 (en) 2019-08-12 2021-02-18 Deciphera Pharmaceuticals, Llc Ripretinib for treating gastrointestinal stromal tumors
MX2022001863A (es) 2019-08-12 2022-05-30 Deciphera Pharmaceuticals Llc Metodos para tratar los tumores del estroma gastrointestinal.
HRP20231699T1 (hr) 2019-12-30 2024-05-10 Deciphera Pharmaceuticals, Llc Formulacije inhibitora amorfne kinaze i postupci njihove primjene
IL293864A (en) 2019-12-30 2022-08-01 Deciphera Pharmaceuticals Llc Preparations of 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3- phenylurea
AU2021282320A1 (en) 2020-05-25 2022-12-22 Chiesi Farmaceutici S.P.A. Benzylamine derivatives as DDRs inhibitors
US11779572B1 (en) 2022-09-02 2023-10-10 Deciphera Pharmaceuticals, Llc Methods of treating gastrointestinal stromal tumors

Family Cites Families (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4125828A (en) 1972-08-04 1978-11-14 Med-El Inc. Method and apparatus for automated classification and analysis of cells
US4207554A (en) 1972-08-04 1980-06-10 Med-El Inc. Method and apparatus for automated classification and analysis of cells
DE2346939A1 (de) * 1973-09-18 1975-04-03 Bayer Ag Acylamino-phenyl-acetamidine, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
EP0729459B1 (en) * 1993-11-15 2003-03-12 Schering Corporation Phenyl-alkyl imidazoles as h3-receptor antagonists
AU3577995A (en) * 1994-10-04 1996-04-26 Fujisawa Pharmaceutical Co., Ltd. Urea derivatives and their use as acat-inhibitors
RU2196769C2 (ru) * 1995-08-30 2003-01-20 Джи. Ди. Сирл Энд Ко. Производные аминобензойной кислоты, фармацевтическая композиция
NZ331480A (en) * 1997-09-04 2000-02-28 F 2-(Arylphenyl)amino-imidazoline derivatives and pharmaceutical compositions
US5990147A (en) * 1997-11-07 1999-11-23 Schering Corporation H3 receptor ligands of the phenyl-alkyl-imidazoles type
JP2001522835A (ja) * 1997-11-07 2001-11-20 シェーリング コーポレイション フェニル−アルキル−イミダゾール型のｈ３レセプターリガンド
US7517880B2 (en) * 1997-12-22 2009-04-14 Bayer Pharmaceuticals Corporation Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
US20120046290A1 (en) * 1997-12-22 2012-02-23 Jacques Dumas Inhibition of p38 kinase activity using substituted heterocyclic ureas
NZ525324A (en) * 2000-10-20 2005-03-24 Eisai Co Ltd Nitrogenous aromatic ring compounds
EP1463714A4 (en) * 2001-12-10 2005-10-19 Amgen Inc VANILLOID RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS
TW200406374A (en) * 2002-05-29 2004-05-01 Novartis Ag Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases
US7247741B2 (en) * 2005-01-21 2007-07-24 Ptc Therapeutics, Inc. Acetylamino benzoic acid compounds and their use for nonsense suppression and the treatment of disease
WO2004009533A1 (en) * 2002-07-24 2004-01-29 Ptc Therapeutics, Inc. Acetylamino benzoic acid compounds and their use for nonsense suppression and the treatment of disease
BR0315580A (pt) * 2002-10-24 2005-08-30 Merck Patent Gmbh Derivados de metileno uréia
US7135575B2 (en) * 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
AU2004218463B2 (en) * 2003-03-03 2009-07-16 Array Biopharma, Inc. p38 inhibitors and methods of use thereof
DE10334663A1 (de) * 2003-07-30 2005-03-10 Merck Patent Gmbh Harnstoffderivate
KR20050091462A (ko) 2004-03-12 2005-09-15 한국과학기술연구원 푸로피리미딘 화합물 및 이를 포함하는 ｄｄｒ2 티로신키나아제 활성 저해제
EP1742908B1 (en) * 2004-04-23 2009-11-11 F.Hoffmann-La Roche Ag Non-nucleoside reverse transcriptase inhibitors
US20090105218A1 (en) * 2004-05-29 2009-04-23 7Tm Pharma A/S CRTH2 Receptor Ligands For Therapeutic Use
NZ554017A (en) * 2004-10-12 2010-06-25 Astrazeneca Ab [(Quinazolin-4-yloxy)phenyl]acetamide derivatives
CA2584179C (en) * 2004-10-13 2013-01-29 Wolfgang Staehle N,n'-diphenylurea derivatives which are suitable as kinase inhibitors
EP1809628B1 (de) * 2004-10-13 2011-06-08 Merck Patent GmbH Phenylharnstoffderivate als hemmstoffe von tyrosinkinasen zur behandlung von tumorerkrankungen
EP1824843A2 (en) * 2004-12-07 2007-08-29 Locus Pharmaceuticals, Inc. Inhibitors of protein kinases
EP1856053A1 (en) * 2005-01-14 2007-11-21 Millennium Pharmaceuticals, Inc. Cinnamide and hydrocinnamide derivatives with raf-kinase inhibitory activity
US7888374B2 (en) * 2005-01-28 2011-02-15 Abbott Laboratories Inhibitors of c-jun N-terminal kinases
EP1970375A4 (en) * 2005-11-29 2010-06-02 Toray Industries ARYLMETHYLENE UREE DERIVATIVE AND USE THEREOF
RU2008127486A (ru) * 2005-12-08 2010-01-20 Милленниум Фармасьютикалз, Инк. (Us) Бициклические соединения с ингибиторной активностью в отношении киназы
WO2007109783A2 (en) * 2006-03-23 2007-09-27 Janssen Pharmaceutica, N.V. Substituted pyrimidine kinase inhibitors
US20090203693A1 (en) * 2006-06-29 2009-08-13 Eisai R & D Management Co., Ltd. Therapeutic agent for liver fibrosis
US8450481B2 (en) * 2007-06-14 2013-05-28 The Regents Of The University Of California Compounds for inhibiting protein aggregation, and methods for making and using them
EP2242367A4 (en) * 2008-01-08 2012-07-04 Univ Pennsylvania REL INHIBITORS AND METHODS OF USE
PT2268623E (pt) * 2008-03-17 2015-09-17 Ambit Biosciences Corp Derivados de quinazolina como moduladores de cinase raf e métodos para utilização dos mesmos
DE102008027574A1 (de) * 2008-06-10 2009-12-17 Merck Patent Gmbh Neue Pyrrolidinderivate als MetAP-2 Inhibitoren
EA201200218A1 (ru) 2009-08-06 2012-09-28 Мерк Патент Гмбх Новые бициклические соединения мочевины
EP2937345B1 (en) * 2009-12-29 2018-03-21 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
EP2674161A1 (en) * 2010-11-11 2013-12-18 Akron Molecules GmbH FMO3 inhibitors for treating pain
CA2843330C (en) * 2011-08-03 2016-09-20 National Taiwan University Substituted phenyl- and heteroaryl-phenyl ether agonists of src homology-2 containing protein tyrosine phosphatase-1 and treatment methods using the same

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