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

Inhibidores de ddr2 para el tratamiento de osteoartritis

Info

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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    • 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
    • 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
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • 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
    • 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
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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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    • A61K31/4427—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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    • A61K31/47—Quinolines; Isoquinolines
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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
    • 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
    • C07D213/75—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
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered

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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.
ARP130103053A 2012-08-29 2013-08-28 Inhibidores de ddr2 para el tratamiento de osteoartritis AR092266A1 (es)

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