AR061842A1 - Pirimidil ciclopentanos hidroxilados y metoxilados como inhibidores de la proteina quinasa akt - Google Patents

Pirimidil ciclopentanos hidroxilados y metoxilados como inhibidores de la proteina quinasa akt

Info

Publication number
AR061842A1
AR061842A1 ARP070103033A ARP070103033A AR061842A1 AR 061842 A1 AR061842 A1 AR 061842A1 AR P070103033 A ARP070103033 A AR P070103033A AR P070103033 A ARP070103033 A AR P070103033A AR 061842 A1 AR061842 A1 AR 061842A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
phenyl
cycloalkyl
attached form
Prior art date
Application number
ARP070103033A
Other languages
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.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38686743&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR061842(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Array Biopharma Inc filed Critical Array Biopharma Inc
Publication of AR061842A1 publication Critical patent/AR061842A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/06Anti-spasmodics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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

Abstract

También se proporcionan métodos de uso de los compuestos de la presente como inhibidores de la proteína quinasa AKT y para el tratamiento de enfermedades proliferativas tales como el cáncer. Reivindicacion 1: Un compuesto de formula 1 y sus tautomeros, enantiomeros resueltos, diastereomeros resueltos, solvatos, metabolitos y sales, en los cuales: R1 es H, Me, Et, vinilo, CF3, CHF2 o CH2F; R2 es H o Me; R5 es H, Me, Et o CF3; A es como se muestra en formula (2); G es fenilo sustituido en forma opcional con uno a cuatro grupos R9 o un heteroarilo de 5-6 miembros sustituido en forma opcional con un halogeno; R6 y R7 son de manera independiente H, OCH3, cicloalquil C3-6-(CH2), cicloalquil C3-6-(CH2CH2), V-(CH2)0-1 donde V es un heteroarilo de 5-6 miembros, W-(CH2)1-2 donde W es fenilo sustituido en forma opcional con F, CI, Br, I, OMe, CF3 o Me, cicloalquilo C3-6 sustituido en forma opcional con alquilo C1-3 u Oalquilo C1-3, hidroxi-cicloalquilo C3-6, fluor-cicloalquilo C3- 6, CH(CH3)CH(OH)fenilo, heterociclo de 4-6 miembros sustituido en forma opcional con F, OH, alquilo C1-3, ciclopropilmetilo o C(=O)alquilo C1-3 o alquilo C1-6 sustituido en forma opcional con uno o más grupos seleccionados de manera independiente de OH, oxo, Oalquilo C1-6, CN, F, NH2, NHalquilo C1-6, N(alquil C1-6)2, ciclopropilo, fenilo, imidazolilo, piperidinilo, pirrolidinilo, morfolinilo, tetrahidrofuranilo, oxetanilo o tetrahidropiranilo, o R6 y R7 junto con el nitrogeno al cual están unidos forman un anillo heterocíclico de 4-7 miembros sustituido en forma opcional con uno o más grupos seleccionados de manera independiente de OH, halogeno, oxo, CF3, CH2CF3, CH2CH2OH, Oalquilo C1-3, C(=O)CH3, NH2, NHMe, N(Me)2, S(O)2CH3, ciclopropilmetilo y alquilo C1-3; Ra y Rb son H, o Ra es H y Rb y R6 junto con los átomos a los cuales están unidos forman un anillo heterocíclico de 5-6 miembros que tiene uno o dos átomos de nitrogeno en el anillo; Rc y Rd son H o Me, o Rc y Rd junto con el átomo al cual están unidos forman un anillo ciclopropilo; R8 es H, Me, E u OH, o R8 y R6 junto con los átomos a los cuales están unidos forman un anillo heterocíclico de 5-6 miembros que tiene uno o dos átomos de nitrogeno en el anillo; cada R9 es de manera independiente halogeno, alquilo C1-6, cicloalquilo C3-6, O-alquilo C1-6, CF3, OCF3, Salquilo C1-6, CN, OCH2-fenilo, CH2O- fenilo, NH2, NH-alquilo C1-6, N-(alquil C1-6)2, piperidina, pirrolidina, CH2F, CHF2, OCH2F, OCHF2, OH, SO2alquilo C1-6, C(O)NH2, C(O)NHalquilo C1-6 y C(O)N(alquil C1-6)2; R10 es H o Me; y m, n y p son de manera independiente 0 o 1.
ARP070103033A 2006-07-06 2007-07-06 Pirimidil ciclopentanos hidroxilados y metoxilados como inhibidores de la proteina quinasa akt AR061842A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US81871806P 2006-07-06 2006-07-06

Publications (1)

Publication Number Publication Date
AR061842A1 true AR061842A1 (es) 2008-09-24

Family

ID=38686743

Family Applications (3)

Application Number Title Priority Date Filing Date
ARP070103033A AR061842A1 (es) 2006-07-06 2007-07-06 Pirimidil ciclopentanos hidroxilados y metoxilados como inhibidores de la proteina quinasa akt
ARP130104510A AR093810A2 (es) 2006-07-06 2013-12-05 Pirimidil ciclopentanos hidroxilados y metoxilados como inhibidores de la proteina quinasa ak, sus usos, composiciones, kits y formas de dosificacion
ARP170102366A AR109424A2 (es) 2006-07-06 2017-08-25 Pirimidil ciclopentanos hidroxilados y metoxilados como inhibidores de la proteína quinasa akt

Family Applications After (2)

Application Number Title Priority Date Filing Date
ARP130104510A AR093810A2 (es) 2006-07-06 2013-12-05 Pirimidil ciclopentanos hidroxilados y metoxilados como inhibidores de la proteina quinasa ak, sus usos, composiciones, kits y formas de dosificacion
ARP170102366A AR109424A2 (es) 2006-07-06 2017-08-25 Pirimidil ciclopentanos hidroxilados y metoxilados como inhibidores de la proteína quinasa akt

Country Status (35)

Country Link
EP (4) EP2399909B1 (es)
JP (4) JP5266216B2 (es)
KR (5) KR20150051240A (es)
CN (2) CN102816124A (es)
AR (3) AR061842A1 (es)
AT (1) ATE524447T1 (es)
AU (1) AU2007269060B2 (es)
BR (3) BR122013028005B8 (es)
CA (2) CA2656622C (es)
CL (1) CL2007001993A1 (es)
CO (1) CO6150161A2 (es)
CR (1) CR10600A (es)
CY (1) CY1112117T1 (es)
DK (2) DK2402325T3 (es)
ES (3) ES2554228T3 (es)
HK (3) HK1160638A1 (es)
HR (1) HRP20110908T1 (es)
HU (1) HUE026237T2 (es)
IL (2) IL196028A (es)
IN (1) IN2014KN02886A (es)
MA (1) MA31655B1 (es)
MX (4) MX2008016202A (es)
MY (1) MY147364A (es)
NO (1) NO342346B1 (es)
NZ (3) NZ573732A (es)
PL (2) PL2402325T3 (es)
PT (1) PT2049501E (es)
RS (1) RS52212B (es)
RU (2) RU2478632C2 (es)
SG (4) SG185980A1 (es)
SI (2) SI2402325T1 (es)
TW (2) TW201332994A (es)
UA (1) UA95641C2 (es)
WO (1) WO2008006040A1 (es)
ZA (1) ZA200900070B (es)

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY147628A (en) 2006-07-06 2012-12-31 Array Biopharma Inc Cyclopenta [d] pyrimidines as akt protein kinase inhibitors
UA95641C2 (en) * 2006-07-06 2011-08-25 Эррей Биофарма Инк. Hydroxylated cyclopenta [d] pyrimidines as akt protein kinase inhibitors
WO2008006039A1 (en) * 2006-07-06 2008-01-10 Array Biopharma Inc. Dihydrothieno pyrimidines as akt protein kinase inhibitors
US8063050B2 (en) 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
DE602007011628D1 (de) * 2006-07-06 2011-02-10 Array Biopharma Inc Dihydrofuropyrimidine als akt-proteinkinaseinhibitoren
US20110135569A1 (en) 2007-03-20 2011-06-09 Peak Biosciences Inc. Method for therapeutic administration of radionucleosides
CA2692506C (en) 2007-07-05 2015-11-24 Array Biopharma Inc. Pyrimidyl cyclopentanes as akt protein kinase inhibitors
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
US8846683B2 (en) 2007-07-05 2014-09-30 Array Biopharma, Inc. Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
CN103396409B (zh) 2007-07-05 2015-03-11 阵列生物制药公司 作为akt蛋白激酶抑制剂的嘧啶基环戊烷
US8329709B2 (en) * 2008-01-09 2012-12-11 Genentech, Inc. 5H-cyclopenta[D]pyrimidines as AKT protein kinase inhibitors
CA2711699A1 (en) * 2008-01-09 2009-07-16 Array Biopharma Inc. Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors
EP2240455B1 (en) * 2008-01-09 2012-12-26 Array Biopharma, Inc. Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor
ES2403284T3 (es) 2008-01-09 2013-05-17 Array Biopharma, Inc. Pirimidil ciclopentanos como inhibidores de la proteína quinasa AKT
CN103403161A (zh) * 2010-12-23 2013-11-20 基因泰克公司 用于治疗新生物的自噬诱导剂和抑制剂组合疗法
CN103841976A (zh) * 2011-04-01 2014-06-04 基因泰克公司 Akt和mek抑制剂化合物的组合及其使用方法
CA2850175C (en) * 2011-04-01 2021-04-13 Genentech, Inc. Biomarkers for predicting sensitivity to cancer treatments
SG194048A1 (en) * 2011-04-01 2013-11-29 Genentech Inc Combinations of akt inhibitor compounds and chemotherapeutic agents, and methods of use
NZ702935A (en) * 2012-05-17 2017-02-24 Genentech Inc Process for making hydroxylated cyclopentylpyrimidine compounds
NZ702513A (en) * 2012-05-17 2016-09-30 Genentech Inc Amorphous form of an akt inhibiting pyrimidinyl - cyclopentane compound, compositions and methods thereof
WO2013173736A1 (en) * 2012-05-17 2013-11-21 Array Biopharma Inc. Process for making hydroxylated cyclopentylpyrimidine compounds
CA2873661C (en) * 2012-05-17 2020-07-21 Genentech, Inc. Process of making hydroxylated cyclopentapyrimidine compounds and salts thereof
MX350443B (es) * 2012-05-17 2017-09-06 Genentech Inc Proceso para hacer compuestos de aminoácidos.
EP2914260A1 (en) 2012-10-31 2015-09-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for preventing antiphospholipid syndrome (aps)
WO2014089570A1 (en) 2012-12-07 2014-06-12 The General Hospital Corporation Combinations of a pi3k/akt inhibitor compound with an her3/egfr inhibitor compound and use thereof in the treatment of a hyperproliferative disorder
JP6340162B2 (ja) 2012-12-20 2018-06-06 日東電工株式会社 アポトーシス誘導剤
EP4282973A3 (en) 2013-11-15 2024-03-27 F. Hoffmann-La Roche AG Processes for the preparation of pyrimidinylcyclopentane compounds
ES2749100T3 (es) 2014-09-26 2020-03-19 Hoffmann La Roche Procesos para preparar compuestos de (ciclopentil[d]pirimidin-4-il)piperazina
TW202329972A (zh) 2016-08-10 2023-08-01 瑞士商赫孚孟拉羅股份公司 包含Akt蛋白質激酶抑制劑之醫藥組合物
US11472799B2 (en) * 2018-03-06 2022-10-18 Icahn School Of Medicine At Mount Sinai Serine threonine kinase (AKT) degradation / disruption compounds and methods of use
WO2020131765A1 (en) 2018-12-19 2020-06-25 Genentech, Inc. Treatment of breast cancer using combination therapies comprising an akt inhibitor, a taxane, and a pd-l1 inhibitor
BR112021011894A2 (pt) 2018-12-21 2021-09-08 Daiichi Sankyo Company, Limited Composição farmacêutica
CA3127884A1 (en) 2019-01-29 2020-08-06 Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd. Akt inhibitor
EP3946330A1 (en) 2019-03-29 2022-02-09 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of keloid, hypertrophic scars and/or hyperpigmentation disorders
EP3952871A4 (en) * 2019-04-09 2023-06-07 Dana-Farber Cancer Institute, Inc. AKT DEGRADATION BY CONJUGATION OF ATP COMPETITIVE AKT INHIBITOR GDC-0068 WITH E3 LIGASE LIGANDS AND METHODS OF USE
CN115916758A (zh) 2020-06-16 2023-04-04 豪夫迈·罗氏有限公司 用于制备羟基化环戊基嘧啶化合物的方法
CA3186568A1 (en) 2020-07-22 2022-01-27 Changyou MA Salt of dihydropyrido[2,3-d]pyrimidinone derivative, preparation method therefor, and use thereof
TWI750905B (zh) * 2020-11-19 2021-12-21 財團法人國家衛生研究院 噻唑化合物作為蛋白質激酶抑制劑
KR20230035773A (ko) * 2021-09-06 2023-03-14 연세대학교 산학협력단 Akt 신호경로 억제제를 유효성분으로 포함하는 아토피피부염의 예방 또는 치료용 조성물
WO2023043869A1 (en) * 2021-09-15 2023-03-23 Teva Pharmaceuticals International Gmbh Solid state forms of ipatasertib citrate
CN113788834B (zh) * 2021-09-18 2022-11-29 河南奥思恩医药科技有限公司 2,4-二氯-6,7-二氢-5H-吡咯并[3,4-d]嘧啶盐酸盐的制备方法
WO2023109540A1 (zh) * 2021-12-17 2023-06-22 中国医药研究开发中心有限公司 具有akt激酶抑制活性的杂环化合物及其制备方法和医药用途
WO2023187037A1 (en) 2022-03-31 2023-10-05 Astrazeneca Ab Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors in combination with an akt inhibitor for the treatment of cancer

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
NL7112938A (es) * 1970-09-30 1972-04-05
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
CA2276098C (en) * 1997-01-08 2007-05-08 F. Hoffmann-La Roche Ag Tricyclic benzo[e]isoindoles and benzo[h]isoquinolines
ES2152902B1 (es) * 1999-07-27 2001-08-16 Medichem Sa Procedimiento de obtencion de venlafaxina
KR100831116B1 (ko) * 2000-08-18 2008-05-20 밀레니엄 파머슈티컬스 인코퍼레이티드 키나아제 억제제로서의 퀴나졸린 유도체
AU2001292670A1 (en) * 2000-09-15 2002-03-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
IL158186A0 (en) * 2001-03-30 2004-03-28 King Pharmaceuticals Res & Dev Pharmaceutically active compounds and methods of use
DE60231439D1 (de) * 2001-12-06 2009-04-16 Merck & Co Inc Mitotische kinesinhemmer
CA2473510A1 (en) * 2002-01-23 2003-07-31 Bayer Pharmaceuticals Corporation Pyrimidine derivatives as rho-kinase inhibitors
TW200306819A (en) * 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
KR101223914B1 (ko) * 2003-11-21 2013-01-18 어레이 바이오파마 인크. Akt 단백질 키나제 억제제
EP1751133B1 (en) * 2004-04-28 2010-04-14 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of rock and other protein kinases
WO2005113762A1 (en) 2004-05-18 2005-12-01 Pfizer Products Inc. CRYSTAL STRUCTURE OF PROTEIN KINASE B-α (AKT-1) AND USES THEREOF
JP2008538102A (ja) * 2005-03-03 2008-10-09 ザ バーナム インスティテュート フォー メディカル リサーチ バーチャルドッキングアプローチを適用したプロテインキナーゼb阻害剤のスクリーニング方法並びにそれにより見出された化合物及び組成物
MY147628A (en) * 2006-07-06 2012-12-31 Array Biopharma Inc Cyclopenta [d] pyrimidines as akt protein kinase inhibitors
WO2008006039A1 (en) * 2006-07-06 2008-01-10 Array Biopharma Inc. Dihydrothieno pyrimidines as akt protein kinase inhibitors
UA95641C2 (en) * 2006-07-06 2011-08-25 Эррей Биофарма Инк. Hydroxylated cyclopenta [d] pyrimidines as akt protein kinase inhibitors

Also Published As

Publication number Publication date
SI2049501T1 (sl) 2012-01-31
EP2966065A3 (en) 2016-03-02
BR122013028012B8 (pt) 2021-05-25
RU2012155606A (ru) 2014-06-27
EP2399909A1 (en) 2011-12-28
ES2372774T3 (es) 2012-01-26
EP2399909B1 (en) 2015-08-26
IN2014KN02886A (es) 2015-05-08
MY147364A (en) 2012-11-30
EP2049501B1 (en) 2011-09-14
KR101578877B1 (ko) 2016-02-22
JP5266216B2 (ja) 2013-08-21
KR20130141717A (ko) 2013-12-26
KR20150051240A (ko) 2015-05-11
CO6150161A2 (es) 2010-04-20
JP2014231530A (ja) 2014-12-11
EP2049501A1 (en) 2009-04-22
CN101578273B (zh) 2012-11-14
RU2478632C2 (ru) 2013-04-10
EP2966065A2 (en) 2016-01-13
TWI402266B (zh) 2013-07-21
KR101495408B1 (ko) 2015-02-25
CA2836316A1 (en) 2008-01-10
IL196028A (en) 2017-02-28
PL2049501T3 (pl) 2012-02-29
BR122013028005B1 (pt) 2021-04-06
CN102816124A (zh) 2012-12-12
HK1160134A1 (en) 2012-08-10
ATE524447T1 (de) 2011-09-15
NO342346B1 (no) 2018-05-07
EP2402325A3 (en) 2012-06-13
MX366319B (es) 2019-07-05
NZ597647A (en) 2013-08-30
CA2656622A1 (en) 2008-01-10
HK1126768A1 (en) 2009-09-11
CR10600A (es) 2009-02-20
NZ610633A (en) 2014-12-24
KR20130029364A (ko) 2013-03-22
SG10201802127UA (en) 2018-04-27
KR20140093291A (ko) 2014-07-25
NZ573732A (en) 2012-03-30
ES2554228T3 (es) 2015-12-17
NO20090581L (no) 2009-04-06
KR20090030333A (ko) 2009-03-24
AU2007269060A1 (en) 2008-01-10
BR122013028005B8 (pt) 2021-05-25
AR109424A2 (es) 2018-11-28
BRPI0713923B8 (pt) 2021-05-25
HK1160638A1 (en) 2012-08-10
KR101178672B1 (ko) 2012-09-07
ZA200900070B (en) 2010-03-31
JP2009542723A (ja) 2009-12-03
ES2554252T3 (es) 2015-12-17
TW201332994A (zh) 2013-08-16
CL2007001993A1 (es) 2008-06-20
EP2402325A2 (en) 2012-01-04
PL2402325T3 (pl) 2016-01-29
SG184706A1 (en) 2012-10-30
CA2656622C (en) 2017-09-12
DK2049501T3 (da) 2011-12-12
RS52212B (en) 2012-10-31
IL241705A0 (en) 2015-11-30
AU2007269060B2 (en) 2014-02-20
TW200817373A (en) 2008-04-16
BRPI0713923B1 (pt) 2020-09-29
AR093810A2 (es) 2015-06-24
RU2009103900A (ru) 2010-08-20
DK2402325T3 (en) 2015-12-07
WO2008006040A1 (en) 2008-01-10
MX2008016202A (es) 2009-02-11
SG188905A1 (en) 2013-04-30
IL196028A0 (en) 2009-09-01
SI2402325T1 (sl) 2015-12-31
SG185980A1 (en) 2012-12-28
CN101578273A (zh) 2009-11-11
MX2019008117A (es) 2019-09-04
EP2402325B1 (en) 2015-08-26
MX337843B (es) 2016-03-22
CY1112117T1 (el) 2015-11-04
JP5836294B2 (ja) 2015-12-24
MA31655B1 (fr) 2010-09-01
HRP20110908T1 (hr) 2012-02-29
HUE026237T2 (en) 2016-06-28
UA95641C2 (en) 2011-08-25
BR122013028012B1 (pt) 2021-04-06
PT2049501E (pt) 2011-12-30
JP2013177470A (ja) 2013-09-09
BRPI0713923A2 (pt) 2013-07-02
JP2013091670A (ja) 2013-05-16

Similar Documents

Publication Publication Date Title
AR061842A1 (es) Pirimidil ciclopentanos hidroxilados y metoxilados como inhibidores de la proteina quinasa akt
AR061844A1 (es) Pirimidil-ciclopentanos como inhibidores de protein-quinasa akt
ES2528451T3 (es) Inhibidores de esfingosina cinasa
AR070136A1 (es) Pirimidil ciclopentanos como inhibidores de la akt proteina quinasa
PE20210405A1 (es) Derivados de 3-(5-hidroxi-1-oxoisoindolin-2-il)piperidina-2,6-diona y su uso en el tratamiento de enfermedades dependientes de la proteina con dedos de zinc 2 de la familia ikaros (ikzf2)
CY1121699T1 (el) Ενωσεις τριαζινης ως αναστολεις κινασης ρ13 και mtor
ES2515194T3 (es) Derivados de pirrolidina
AR055150A1 (es) Compuestos de isoindol - imido y composiciones que los comprenden y sus metodos de uso
AR081577A1 (es) Derivados de aminopirimidina como moduladores de la lrrk2
AR046394A1 (es) Derivados de quinolinas y quinazolinas, metodo de preparacion de los mismos y composiciones farmaceuticas que los contienen.
AR054529A1 (es) Derivados de benzazepina como moduladores del receptor de 5-hidroxi-triptamina 6
ECSP034865A (es) Resolución óptica de (1-benzilo-4-metilopiperidina-3-il)-metilamina y su uso para la preparación de derivados de pirrolo 2,3-pirimidina como inhibidores de proteina quinasas
AR053120A1 (es) Aminopiridinas como inhibidores de beta secretasa
AR065556A1 (es) Derivados de 3-(( 1,2,4) triazolo (4,3-a) piridin -7-il) benzamida
CO5580765A2 (es) Derivados de ciclohexano espirociclicos
AR070828A1 (es) Derivados de azetidina y ciclobutano como inhibidores de jak
AR043837A1 (es) Pirazoles sustituidos
AR067413A1 (es) Compuestos heterociclicos que contienen ciclopenta[d]pirimidina inhibidores de proteinquinasas akt, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de las mismas para el tratamiento de enfermedades hiperproliferativas, tales como cancer
AR036075A1 (es) Compuestos derivados de pirimidina,triazina,y,pirazina,su uso, un procedimiento para su preparacion y medicamentos que los comprenden
AR048691A1 (es) Compuestos con estructura de alquino con accion antagonista de mch y medicamentos que contienen estos compuestos
CR20190261A (es) Inhibidores de la tirosina quinasa de bruton
AR083798A1 (es) Inhibidores selectivos de glucosidasas y sus usos
AR109991A1 (es) Tratamientos de combinación que comprenden la administración de imidazopirazinonas
AR109990A1 (es) Derivados de imidazopirazinonas inhibidores de pde1
AR055666A1 (es) Inhibidores inntr

Legal Events

Date Code Title Description
FC Refusal