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ME02125B - Inhibitori protein apoptoze (iap) - Google Patents

Inhibitori protein apoptoze (iap)

Info

Publication number
ME02125B
ME02125B MEP-2012-557A MEP55712A ME02125B ME 02125 B ME02125 B ME 02125B ME P55712 A MEP55712 A ME P55712A ME 02125 B ME02125 B ME 02125B
Authority
ME
Montenegro
Prior art keywords
formula
compound
inhibitors
phenyl
ethyl
Prior art date
Application number
MEP-2012-557A
Other languages
English (en)
French (fr)
Inventor
Fan Yang
Leigh Zawel
Zhuoliang Chen
Yaping Wang
Wojciech Wrona
Gang Liu
Mark G Charest
Feng He
Mark G Palermo
Sushil Kumar Sharma
Christopher Straub
Run-Ming Wang
Yanlin Zhang
Original Assignee
Novartis Ag
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=34962601&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ME02125(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of ME02125B publication Critical patent/ME02125B/me

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    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • A—HUMAN NECESSITIES
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    • A61P35/00—Antineoplastic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D207/06—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
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    • C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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Claims (18)

1. Jedinjenje formule (IV) gde U predstavlja: i u kojoj (a) R1 i R3 predstavljaju metil ili etil; gde R2 može da bude H, metil, etil, hlorometil, dihlorometil ili trifluorometil; gde je R4 C1-C4 alkil; C3-C7 cikloalkil; C3-C7 cikloalkil- C1-C7 alkil; fenil- C1-C7 alkil ili aril; gde R5 predstavlja H; a U ima strukturu formule II u kojoj X predstavlja N; gde R6, R6', R7 i R'7 mogu da budu H; ili R6 predstavlja -C(O)- C1-C4 alkil-fenil i gde R6’, R7 i R'7 predstavljaju H; n je 0, tako da (Ra)n i (Rb)n oba označavaju vezu; Rc predstavlja H; Rd predstavlja Ar1D-Ar2, u kojoj su Ar1 i Ar2 supstituisani i nesupstituisani fenil ili het; i gde je D N(Rh), kada Rh predstavlja H, Me, -CHO, -S02, -C(O), -CHOH, -CF3 ili - SO2CH3; ili gde (b) R1 i R3 predstavljaju metili ili etil; kada R2 predstavlja H, metil, etil, hlorometil, dihlorometil ili trifluorometil; gde R4 može da bude C1-C4 alkil; C3-C7 cikloalkil; C3-C7 cikloalkil- C1-C7 alkil; fenil-C1-C7 alkil ili aril; gde R5 predstavlja H; U ima strukturu formule II u kojoj X predstavlja N; gde R6, R6’, R7 i R'7 mogu da budu H; n je 0, tako da (Ra)n i (Rb)n oba označavaju vezu; Rc predstavlja H; Rd predstavlja Ar1-D-Ar2, u kojoj su Ar1 i Ar2 supstituisani i nesupstituisani fenil ili het; i D je -0-; ili gde (c) R1 i R3 predstavljaju metili ili etil; kada R2 predstavlja H, metil, etil, hlorometil, dihlorometil ili trifluorometil; gde R4 može da bude C1-C4 alkil; C3-C7 cikloalkil; gde R5 predstavlja H; gde U ima strukturu formule II u kojoj X predstavlja N; gde R6, R6', R7 i R’7 predstavljaju H; n je 0, tako da (Ra)n i (Rb)n oba označavaju vezu; gde Rc predstavlja H; Rd predstavlja Ar1-D-Ar2, gde su Ar1 i Ar2 supstituisani i nesupstituisani fenil ili het; i D je C(O)-; gde “ het “ može da bude 5-očlani do 7-očlani heterociklični prsten koji sadrži 1-4 heteroatoma u prstenu koji su odabrani izmedju N, O i S ili 8-očlani do 12-očlani spojeni prsten koji obuhvata jedan 5-očlani do 7-očlani monociklični heterociklični prsten koji sadrži 1, 2 ili 3 heteroatoma u prstenu odabranih od N, O i S, gde pomenuti heterociklični prsten ili spojeni sistem prstenova može da bude nesupstituisan ili supstituisan na atomu ugljenika ili azota, ili njena farmaceutski prihvatljiva so.
2.    Jedinjenje formule (IV) prema patentnom zahtevu 1, naznačen time što D predstavlja N(Rh), i što je R4 metil, etil, hutil. izopropil, t-butil, cikloheksil, -CH2-ciklopentil, -CH2-cikloheksil, -CH2-ciklopropil, fenil ili -CH2-fenil.
3.    Jedinjenje formule (IV) prema patentnom zahtevu 1 ili 2, naznačen time, što D predstavlja N(Rh), i gde su Ar1 i Ar2 supstituisani i nesupstituisani fenil ili het, gde je pomenuta het grupa supstituisani i nesupstituisani triazin, pirimidin, piridin, oksazol, 2, 4-difluorofenil, Cl-fenil ili fluorofenil.
4.    Jedinjenje formule (IV) prema patentnom zahtevu 1, naznačen time, što D predstavlja -O- i gde R4 predstavlja metil, etil, butil, izopropil, t-butil, cikloheksil, -CH2-ciklopentil, -CH2-cikloheksil, -CH2-ciklopropil, fenil ili -CH2-fenil.
5.    Jedinjenje formule (IV) prema patentnom zahtevu 1 ili 4, naznačen time što, D predstavlja -O- i gde su Ar1 and Ar2 supstituisani i nesupstituisani fenil ili het, gde je pomenuta het grupa supstituisani i nesupstituisani pirimidin, piridin, oksazol ili 2-metiloksazol.
6.    Jedinjenje formule (IV) prema patentnom zahtevu 1, naznačen time što D predstavlja C(O), i gde R4 predstavlja izopropil, t-butil, ciklopentil, ili cikloheksil.
7.    Jedinjenje formule (IV) prema patentnom zahtevu 1 ili 6, naznačen time što, D predstavlja C(O), i gde su Ar1 Ar2 supstituisani i nesupstituisani oksazol, tiazol i ozadiazol.
8.    Jedinjenje formule (IV) prema patenentom zahtevu 1, koje je odabrano iz grupe koju čine Primer 6 i primer 195 ili njena farmaceutski prihvatljiva so.
9. Farmaceutska kompozicija koja obuhvata farmaceutski prihvatljivi nosač i terapijski efikasnu količinu jedinjenja formule (IV) prema bilo kojem od patentnih zahteva od 1 do 8.
10.    Jedinjenje formule (IV) prema bilo kojem od patentnih zahteva od 1 do 8 za upotrebu u medicini.
11.    Jedinjenje formule (IV) prema bilo kojem od patentnih zahteva od 1 do 8 za proizvodnju leka za lečenje proliferativnih oboljenja.
12.    Upotreba prema patentnom zahtevu 11, naznačen time, što je proliferativno oboljenje, tumor.
13.    Upotreba jedinjenja prema patentnom zahtevu 11 ili 12, gdeje proliferativno oboljenje odabrano iz grupe koju čine kancer dojke, genitourinarni kancer, kancer pluća, gastrointestinalni kancer, epidermoidni kancer, melanom, kancer jajnika, pankreasa, neuroblastom, rak glave i/ili jezika, kancer bešike, bubrega, mozga ili želudca, tumora usta, tumor pluća, kolorektalni tumor, tumor prostate i multipli mijelom.
14.    Kombinacija jedinjenja formule (IV) prema bilo kojem od patentnih zahteva od 1 do 8 i drugog antiproliferativnog sredstva.
15.    Kombinacija jedinjenja prema patentnom zahtevu 14, naznačen time, što je antiproliferativno sredstvo odabrano iz grupe koju sačinjavaju inhibitori aromataze; antiestrogeni; inhibitori topoizomeraze I; inhibitori topoizomeraze II; sredstva aktivna na mikrotubulama; alkilujuća sredstva; inhibitori histon deacetilaze; jedinjenja koja indukuju procese ćelijske diferencijacije; inhibitori ciklooksigenaze; inhibitori MMP; inhibitori mTOR; antineoplastični antimetaboliti; jedinjenja platine; jedinjenja koja targetuju/smanjuju aktivnost proteinske ili lipidne kinaze i dalja antiangiogena jedinjenja; jedinjenja koja targetuju, smanjuju ili inhibiraju aktivnost proteinske ili lipidne fosfataze; agonisti gonadorelina; anti-androgeni; inhibitori metionin-aminopeptidaze; bisfosfonati; modifikatori biološkog odgovora; antiproliterativna antitela; inhibitori heparanaze; inhibitori Ras onkogenih izoformi; inhibitori telomeraze; inhibitori proteazoma; sredstva koja se koriste u tretmanu hematoloških maligniteta; jedinjenja koja targetuju, smanjuju ili inhibiraju aktivnost Flt-3; inhibitori Hsp90; temozolomid (TEMODAL®); i leukovorin.
16.    Kombinacija jedinjenja prema patentnom zahtevu 15, naznačen time, što je antiproliferativno sredstvo aktivno sredstvo za mikrotubule.
17.    Kombinacija jedinjenja prema patentnom zahtevu 16, naznačen time, što je aktivno sredstvo paklitaksel ili docetaksel.
18.    Jedinjenje formule (IV) prema patentnim zahtevima od 1 do 8, za upotrebu za lečenje bilo kojeg od opisanih indikacija u bilo kojem od patentnih zahteva 11, 12 ili 13.
MEP-2012-557A 2004-04-07 2005-04-06 Inhibitori protein apoptoze (iap) ME02125B (me)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US56018604P 2004-04-07 2004-04-07
PCT/EP2005/003619 WO2005097791A1 (en) 2004-04-07 2005-04-06 Inhibitors of iap
EP10172398A EP2253614B1 (en) 2004-04-07 2005-04-06 Inhibitors of IAP

Publications (1)

Publication Number Publication Date
ME02125B true ME02125B (me) 2013-04-30

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