AR070136A1 - Pirimidil ciclopentanos como inhibidores de la akt proteina quinasa - Google Patents

Pirimidil ciclopentanos como inhibidores de la akt proteina quinasa

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Publication number
AR070136A1
AR070136A1 ARP090100067A ARP090100067A AR070136A1 AR 070136 A1 AR070136 A1 AR 070136A1 AR P090100067 A ARP090100067 A AR P090100067A AR P090100067 A ARP090100067 A AR P090100067A AR 070136 A1 AR070136 A1 AR 070136A1
Authority
AR
Argentina
Prior art keywords
alkyl
cr10r10
aryl
heterocyclyl
optionally substituted
Prior art date
Application number
ARP090100067A
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English (en)
Original Assignee
Array Biopharma Inc
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.)
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Publication date
Application filed by Array Biopharma Inc filed Critical Array Biopharma Inc
Publication of AR070136A1 publication Critical patent/AR070136A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
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    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems

Abstract

Además se proveen métodos para utilizar los compuestos de esta solicitud como inhibidores de Akt proteína quinasa y para el tratamiento de enfermedades mediadas por la Akt, por ejemplo, enfermedades hiperproliferativas tal como cáncer. Reivindicacion 1: Un compuesto de formula (1) y sus tautomeros, enantiomeros resueltos, diastereomeros resueltos, solvatos, metabolitos, sales y prodrogas aceptables para uso farmacéutico, donde: R1 es H, CH3, CH2CH3, CH(CH3)2, CH=CH2, CH2OH, CF3, CHF2, CH2F, o cicloalquilo C3-; R2 es H, OH, OCH3 o F; R3 es H, F o CH3; cada R4 se selecciona independientemente de H, F, CI, Br, I, CN, (CH2)tNR10R10, (CH2)tOR10, (CH2)tC(O)R10, (CH2)tC(O)OR10, (CH2)tC(O)NR10R10, (CH2)tNR10C(O)R10, (CH2)tNR10C(O)OR10, (CH2)tNR10C(O)NR10R10, alquilo C1-6, (CR10R10)tcicloalquiIo C3-8, (CR10R10)theterociclilo C3-6, (CR10R10)tarilo C6-8, O(CR10R10)t arilo C6-8, (CR10R10)theteroarilo C3-6, donde dicho alquilo, cicloalquilo, heterociclilo, arilo y heteroarilo están opcionalmente sustituidos con uno o más F, CI, Br, I, CN, alquilo C1-3, CF3, OH o O(alquilo C1-3); R5 es H, alquilo C1-6, (CR10R10)tOR10, (CR10R10)tNR10R10, (CH2)tcicloalquilo C3-8, (CH2)tarilo C6-8, donde dicho arilo está opcionalmente sustituido con F, CI, Br o I; R6, R7, R8 y R9 se seleccionan independientemente de H, alquilo C1-6, (CR10R10)tOR10, (CR10R10)tarilo C6-8; donde dicho arilo está opcionalmente sustituido con F, CI, Br o I; R10 se selecciona independientemente de H, OH, O(alquilo C1-3), (CH2)tNR11R11, (CH2)tC(O)NR11R11, (CH2)tS(O)NR11R11, (CH2)tS(O)2NR11R11, alquilo C1-6, (CH2)tcicloalquilo C3-8, (CH2)theterociclilo C3-6, (CH2)tarilo C6-8 y (CH2)theteroarilo C3-6, donde dicho alquilo, cicloalquilo, heterociclilo, arilo y heteroarilo están opcionalmente sustituidos con uno o más F, CI, Br, I, CN, alquilo C1-3, CF3, OH, O(alquilo C1-3); o dos R10 se toman juntos para formar oxo o un heterociclilo C3-6; R11 se selecciona independientemente de H, alquilo C1-3, OH, Oalquilo C1-3, NH2, N(alquilo C1-3)2; o dos R11 se toman juntos para formar un heterociclilo C3-6 opcionalmente sustituido con metilo o etilo; m y n son independientemente 1, 2 o 3, siempre que m y n tomados juntos sean 3, 4 o 5; p es 0,1, 2 o 3;y cada t es independientemente 0, 1, 2, 3 o 4.
ARP090100067A 2008-01-09 2009-01-09 Pirimidil ciclopentanos como inhibidores de la akt proteina quinasa AR070136A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US2012508P 2008-01-09 2008-01-09

Publications (1)

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AR070136A1 true AR070136A1 (es) 2010-03-17

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ID=40436385

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Country Status (12)

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US (2) US8324221B2 (es)
EP (1) EP2240483B8 (es)
JP (1) JP5512545B2 (es)
CN (1) CN102015708B (es)
AR (1) AR070136A1 (es)
CA (1) CA2714888C (es)
CL (1) CL2009000035A1 (es)
ES (1) ES2403284T3 (es)
HK (1) HK1149270A1 (es)
PE (1) PE20091315A1 (es)
TW (1) TW200940542A (es)
WO (1) WO2009089454A1 (es)

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PE20091315A1 (es) 2008-01-09 2009-09-21 Array Biopharma Inc Ciclopentanos de pirimidilo como inhibidores de la proteina cinasa akt
US20100048912A1 (en) 2008-03-14 2010-02-25 Angela Brodie Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens, In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
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Also Published As

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JP2011509307A (ja) 2011-03-24
US9346805B2 (en) 2016-05-24
CA2714888A1 (en) 2009-07-16
EP2240483A1 (en) 2010-10-20
TW200940542A (en) 2009-10-01
US20130072500A1 (en) 2013-03-21
EP2240483B1 (en) 2013-02-27
US8324221B2 (en) 2012-12-04
US20110053959A1 (en) 2011-03-03
CN102015708A (zh) 2011-04-13
CA2714888C (en) 2017-03-14
CN102015708B (zh) 2014-03-26
PE20091315A1 (es) 2009-09-21
EP2240483B8 (en) 2013-04-03
WO2009089454A1 (en) 2009-07-16
ES2403284T3 (es) 2013-05-17
JP5512545B2 (ja) 2014-06-04
HK1149270A1 (en) 2011-09-30
CL2009000035A1 (es) 2009-11-27

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