ME00486B - Jedinjenja pirolopirimidina i njihova upotreba - Google Patents

Jedinjenja pirolopirimidina i njihova upotreba

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Publication number
ME00486B
ME00486B MEP-2008-766A MEP76608A ME00486B ME 00486 B ME00486 B ME 00486B ME P76608 A MEP76608 A ME P76608A ME 00486 B ME00486 B ME 00486B
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ME
Montenegro
Prior art keywords
substituted
alkyl
group
groups
compound
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MEP-2008-766A
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English (en)
French (fr)
Inventor
Christopher Thomas Brain
Gebhard Thoma
Moo Je Sung
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Novartis Ag
Astex Therapeutics Ltd
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38779335&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ME00486(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag, Astex Therapeutics Ltd filed Critical Novartis Ag
Publication of ME00486B publication Critical patent/ME00486B/me

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/18—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
    • 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/24—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one nitrogen and one sulfur atom

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Claims (18)

1. Jedinjenje Formule I: ili njegova farmaceutski prihvatljiva so ili solvat, naznačen time, što: isprekidana linija predstavlja dvostruku vezu gde A predstavlja N; gde su R2 i R3 svaki, nezavisno, odabrani iz grupe koja obuhvata vodonik, hidroksil, C1-C3-alkil, C3-C8-cikloalkil, heterociklil, aril, heteroaril, supstituisani C1-C3-alkil, supstituisani C3-C8-cikloalkil, supstituisani heterociklil, supstituisani aril i supstituisani heteroaril; R4 je odabran iz grupe koja obuhvata vodonik, C1-C8-alkil, supstituisani C1-C8-alkil, C3-C8-cikloalkil, supstituisani C3-C8-cikloalkil, aril, supstituisani aril, heteroaril i supstituisani heteroaril; i Y je CR12; R11 je vodonik ili C1-C3-alkil; i R12 je -BC(0)NR13R14; gde je B veza, C1-C3-alkil ili razgranati C1-C3-alkil; gde su R13 i R14 svaki, nezavisno, odabrani iz grupe koja obuhvata vodonik, C1-C3-alkil, C3-C8-cikloalkil, heterociklil, aril, heteroaril, supstituisani alkil, supstituisani cikloalkil, supstituisani heterociklil, supstituisani aril, i supstituisani heteroaril.
2. Jedinjenje iz patentnog zahteva 1, naznačeno time, što je R4 razgranat ili linearni C1-C5-alkil, gde razgranata C1-C5-alkil grupa može biti prekinuta sa jednim ili više heteroatoma, i/ili supstituisana jednim ili više heteroatoma, halogena, C3-C8 cikloalkil grupa, supstituisanih C3-C8 cikloalkil grupa, C3-C8 heterociklil grupa, aril grupa, heteroaril grupa, supstituisanih aril grupa, ili supstituisanih heteroaril grupa.
3.    Jedinjenje iz patentnog zahteva 1, naznačen time, što je R4 odabran iz grupe koja obuhvata vodonik, C1-C8-alkil, C3-C8-cikloalkil, C3-C8- supstituisani cikloalkil, aril, supstituisani aril, heteroaril, i supstituisani heteroaril.
4.    Jedinjenje iz patentnog zahteva 3, naznačeno time, što je R4 je razgranat ili linearni C1-C5-alkil, gde razgranata C1-C5-alkil grupa može biti prekinuta jednim ili više heteroatoma, i/ili supstituisana jednim ili više heteroatoma, halogena, C3-C8 cikloalkil grupa, supstituisanih C3-C8 cikloalkil grupa, C3-C8 hetrociklil grupa, aril grupa, heteroaril grupa, supstituisanih aril grupa, ili supstituisanih heteroaril grupa.
5.    Jedinjenje iz patentnog zahteva 1, naznačeno time, što je R4 odabran iz grupe koja obuhvata vodonik, razgranati C1-C5-alkil, razgranati C1-C5-alkil supstituisan fenilom i C3-C6-cikloalkil.
6.    Jedinjenje iz patentnog zahteva 1, naznačeno time, što R4 može da bude C(H)(CH2CH3)2, C(H)(CH2CH3)Ph, CH2CH3, ciklopropil, ciklopentil ili cikloheksil.
7.    Jedinjenje iz patentnog zahteva 1, naznačeno time, što je R2 u stvari H.
8.    Jedinjenje iz patentnog zahteva 1, naznačeno time, što je R3 aril grupa,    koja    je    dalje nezavisno supstituisana jednom ili više puta halogenom, C1-C4-alkoksi-grupom, Rl5-aminom, R15-heterociklom, ili R15-heteroarilom, gde je R15 veza, C(O), N(H)C(0), N(H)SO2, OC(O) ili (CH2)1-4, gde (CH2)1-4 grupa može biti prekinuta O, N(CH3) ili N(H).
9.    Jedinjenje iz patentnog zahteva 8, naznačeno time, što je aril grupa fenil.
10.    Jedinjenje iz patentnog zahteva 9, naznačeno time, što je fenil grupa nezavisno supstituisana jedan ili više puta sa fluoro, metoksi, dietilaminskom, R15-piperazinil, R15-morfolinil, R15-piperidinil, R15-triazolil, R15-fenil, R15-piridinil, Rl5-piperazinil, R15-indazolil, Rl5-pirolidinil ili R15-imidazolil grupom, gde piperazinil, morfolinil, piperidinil, triazolil, fenil, piridinil, piperazinil, indazolil, pirolidinil ili imidazolil-grupe mogu dalje biti supstituisane C1-C4-alkil grupom, C(O)C1-C4-alkil, S(0)2C1-C4-alkil, OH, C(0)(CH2),.3CN ili N(H)C(0)C1-C4-alkilom.
11. Jedinjenje iz patentnog zahteva 9, naznačeno time, što je fenil grupa supstituisana N(H)C(O)aril, C(O)N(H)C1-C4-alkil, C(0)N(C1-C4-alkil)2 ili C(0)N(H)C3-C6-eikloalkil grupom.
12. Jedinjenje prema bilo kojem od patentnih zahteva 1-12, naznačeno time, što je jedinjenje odabrano iz grupe koja obuhvata
13.    Upotreba jedinjenja prema bilo kojem od patentnih zahteva 1-12 za proizvodnju leka za lečenje poremećaja povezanih sa protein kinazom.
14.    Upotreba prema patentnom zahtevu 13, naznačen time, što je poremećaj povezan sa protein kinazom, kancer odabran iz grupe koja obuhvata kancer mokraćne bešike, glave i vrata, dojke, stomaka, jajnika, kolona, pluća, mozga, larinksa. limfnog sistema, genitourinamog trakta, gastrointestinalnog trakta, jajovoda, prostate, gastrični, koštani, sitnoćelijski plućni, gliom, koiorektalni i kancer pankreasa.
15.    Farmaceutska kompozicija koja obuhvata jeđinjenje prema bilo kojem od patentnih zahteva 1-12, zajedno sa farmaceutski prihvatljivim nosačem i po slobodnom izboru ostalim terapeutskim agensima.
16. Farmaceutska kompozicija koja obuhvata jedinjenje prema bilo kojem od patentnih zahteva 1-iz, koja je prilagodjena za simultanu ili sekvencijalnu primenu sa antiinflamatomim sredstvom, antiproliferativnim sredstvom, hemoterapeutikom, imunosupresantom, anti-kancerskim, citotoksičnim sredstvom ili inhibitorom kinaze različitim od jedinjenja prema bilo kojem od patentnih zahteva 1-12 ili njegova so.
17.    Farmaceutska kompozicija iz patentnog zahteva 15, naznačena time, što se pomenuto jedinjenje prema bilo kojem od patentnih zahteva 1-12 ili njegova so, daje simultano ili sekvencijalno, sa jednim ili više PTK inhibitora, ciklosporinom A, CTLA4-Ig, antitelima iz grupe anti-ICAM-3, anti-IL-2 receptor, anti-CD45RB, anti-CD2, anti-CD3, anti-CD4, anti-CD80, anti-CD86, i monoklonalnim antitelom OKT3, sa sredstvima koja blokiraju interakciju izmedju CD40 i gp39, fuzionim proteinima konstruisanim od CD40 i gp39, inhibitorima NF-kappa B, nesteroidnim antiinflamatomim lekovima, steroidima, jedinjenjima zlata, antiproliferativnim sredstvima, FK506, mikofenolat-mofetilom, citotoksičnim lekovima, inhibitorima TNF-α, antitelima na TNF ili na rastvomi TNF receptor, sa rapamicinom, leflunimidom, inhibitorima ciklooksigenaze-2, paklitakselom, cisplatinom, karboplatinom, doksombicinom, karminomicinom, daunorubicinom, aminopterinom, metotreksatom, metopterinom, mitomicinom C, ekteinascidinom 743, porfiromicinom, 5-fluorouracilom, 6-merkaptopurinom, gemcitabinom, citozin arabinozidom, podofilotoksinom, etopozidom, etopozid fosfatom, tenipozidom, melfalanom, vinblastinom, vinkristinom, leurozidinom, epotilonom, vindezinom, leurozinom, ili sa njihovim derivatima.
18.    Komplet, naznačen time, što obuhvata jedinjenje-modulator protein kinaze prema bilo kojem od patentnih zahteva 1-12, upakovan zajedno sa uputstvom za upotrebu efikasne količine jedinjenja-modulatora protein kinaze za tretman poremećaja povezanih sa protein kinazom.
MEP-2008-766A 2006-05-26 2007-05-24 Jedinjenja pirolopirimidina i njihova upotreba ME00486B (me)

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Application Number Priority Date Filing Date Title
US80860506P 2006-05-26 2006-05-26
PCT/US2007/069595 WO2007140222A2 (en) 2006-05-26 2007-05-24 Pyrrolopyrimidine compounds and their uses

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ME00486B true ME00486B (me) 2011-10-10

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