ME01282B - Jedinjenja pirolopirimidina kao inhibitori cdk - Google Patents

Jedinjenja pirolopirimidina kao inhibitori cdk

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Publication number
ME01282B
ME01282B MEP-2011-25A MEP2511A ME01282B ME 01282 B ME01282 B ME 01282B ME P2511 A MEP2511 A ME P2511A ME 01282 B ME01282 B ME 01282B
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Prior art keywords
ylamino
cyclopentyl
pyrrolo
dimethylcarboxamide
pyridin
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MEP-2011-25A
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English (en)
French (fr)
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Steven Howard
Yue Li
Yipin Lu
Paul Mortenson
Troy Smith
Moo Sung
Steven Woodhead
Wojciech Wrona
Gilbert Besong
Christopher Thomas Brain
Clinton A Brooks
Miles Stuart Congreve
Claudio Dagostin
Guo He
Ying Hou
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Novartis Ag
Astex Therapeutics Ltd
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41171100&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ME01282(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 ME01282B publication Critical patent/ME01282B/me

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    • 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
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    • 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
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    • A—HUMAN NECESSITIES
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Abstract

Prikazana jedinjenja se odnose na lečenja i terapije poremećaja povezanih sa protein kinazom. Takođe postoji potreba za jedinjenj ima koja se mogu koristiti za lečenje ili prevenciju ili poboljšanje jednog ili više simptoma kancera, odbacivanja transplanta, i autoimunih bolesti. Osim toga, postoji potreba za metodama za moduliranje aktivnosti protein kinaza, kao što su CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 i CDK9, primenom jedinjenja koja su ovde data.  

Claims (22)

1. Jedinjenje formule I: ili njegova farmaceutski prihvatljiva so, naznačeno time što: X je CR9, ili N; R1 je C1-8alkil, CN, C(0)0R4 ili CONR5R6, 5-14-člana heteroaril grupa, ili 3-14-člana cikloheteroalkil grupa; R je C1-8alkil, C3-14cikloalkil, ili 5-14- člana heteroaril grupa, i gde R može biti supstituisan jednim ili više C1-8alkil, ili OH; L je veza, C1-8alkilen, C(O), ili C(0)NR10, i gde L može biti supstituisano ili nesupstituisano; Y je H, R11, NR12R13, OH, ili je Y deo sledeće grupe , gde Y je CR9 ili N; gde 0-3 R može biti prisutno, i R je C1-8alkil, okso, halogen, ili dve ili više R mogu formirati premošćenu alkil grupu; W je CR9, ili N; R3 je H, C1-8alkil, C1-8alkilR14, C3-14cikloalkil, C(0)C1-8 alkil, C1-8haloalkil, C1-8alkilOH, C(0)NR14R15, C1-8cijanoalkil, C(0)R14, C0-8alkilC(O)C0-8alkilNR14R15, C0-8alkilC(O)OR14, NR14R15, S02C0-8alkil, C0-8alkilC3-14cikloalkil, C(0)C1-8alkilC3-14cikloalkil, C1-8alkoksi, ili OH koji može biti supstituisan ili nesupstituisan kada R3 nije H. R9 je H ili halogen; R1, R2, R6, R7, R10, R11, R12, R13, R14, i R15 je svaki nezavisno izabran od H, C1-8alkil, C3-14 cikloalkil, 3-14- člane cikloheteroalkil grupe, C6-14aril grupe, 5-14- elane heteroaril grupe, alkoksi, C(0)H, C(N)OH, C(N)OCH3, C(0)C,.3alkil, C1-8alkilNH2, C1-6alkilOH, i gde R1, R2, R6, R7, R10, R11, R12, i R13, R14, i R15kada nisu H mogu biti supstituisani ili nesupstituisani; m i n su nezavsno 0-2; i Gde L, R3, R1, R2, R6, R7 , R10, R11, R12, i R13, R14, i Rl5mogu biti supstituisani sa jednom ili više od C1-8alkil, C2-8alkenil, C2-8alkinil, C3-14cikloalkil, 5-14- člane heteroaril grupe, C6-14aril grupe, 3-14-člane cikloheteroalkil grupe, OH, (O), CN, alkoksi, halogen, ili NH2.
2. Jedinjenje formule I u skladu sa patentnim zahtevom 1, naznačeno time što R3 je H, C1-8alkil, C3-14cikloalkil, C(0)C1-8 alkil, C1-8alkilOH, C1-8cijanoalkil, C0-8alkilC(0)C0-8alkilNR14R15, C0-8alkilC(0)0R14, NR14R15, C1-8alkilC3-i4cikloalkil, C(0)C1-8alkilC3.i4cikloalkil, C0-8alkoksi, C1-8alkilR14, C1-8haloalkil, ili C(0)R14, koji mogu biti supstituisani sa jednim ili više od OH, CN, F, ili NH2, i naznačeno time da je R14 i R15 svaki nezavisno izabran od H, C1-8alkil, C3-14cikloalkil, alkoksi, C(0)C1-3alkil, C1-8alkilNH2, ili C1-6alkilOH.
3. Jedinjenje formule I u skladu sa bilo kojim od patentnih zahteva 1-2, naznačeno time što R3 je H, C1-8alkil, ili C1-8alkilOH.
4. Jedinjenje formule I u skladu sa bilo kojim od patentnih zahteva 1-3, naznačeno time što Y je H, OH, ili je Y deo sledeće grupe , gde Y je N i W je CR9, ili N; gde 0-2 R8 može biti prisutno, i R8 je C1-8alkil, okso, ili dva ili više R8 mogu da formiraju premošćenu alkil grupu.
5.    Jedinjenje formule 1 u skladu sa bilo kojim od patentnih zahteva 1-4, naznačeno time stoje L veza, C1-8alkilen, ili C(0)NH, ili C(O).
6.    Jedinjenje formule I u skladu sa bilo kojim od patentnih zahteva 1-5, naznačeno time što R2je C3-14cikloalkil.
7.    Jedinjenje formule I u skladu sa bilo kojim od patentnih zahteva 1-6, naznačeno time što R je ciklopentan.
8.    Jedinjenje formule I u skladu sa bilo kojim od patentnih zahteva 1-7, naznačeno time što R1 je CN, C(0)0R4, CONR5R6, ili 5-14-člana heteroaril grupa.
9.    Jedinjenje formule I u skladu sa bilo kojim od patentnih zahteva 1-8, naznačeno time što R1 je CONR5R6, i R5 i R6 su C1-8alkil.
10.    Jedinjenje formule I u skladu sa bilo kojim od patentnih zahteva 1 -9, naznačeno time što X je CR9.
11.    Jedinjenje formule I u skladu sa bilo kojim od patentnih zahteva 1-10, naznačeno time što jedno X je N i drugo X je CR9.
12.    Jedinjenje formule I u skladu sa bilo kojim od patentnih zahteva 1-11, naznačeno time što X je CR9 i Y je gde m i n su 1, i Y i W su N.
13. Metod za lečenje bolesti, poremećaja ili sindroma povezanog sa CDK 4 inhibicijom, naznačen time što navedeni metod obuhvata administriranje jedinjenja u skladu sa bilo kojim od patentnih zahteva 1-12 ili njegov prolek ili farmaceutsku kompoziciju koja sadrži jedinjenje formule I ili njegov prolek i farmaceutski prihvatljiv ekscipijens subjektu kome je potreban.
14.    Metod lečenja za koji se traži patentna zaštita u patentnom zahtevu 13, naznačen time što je bolest, poremećaj ili sindrom hiperproliferativan u subjektu, gde je subjekt životinja uključujući ljude, izabran iz grupe koja obuhvata kancer i inflamaciju.
15.    Metod inhibicije ciklin zavisne kinaze (npr. cdk-4), naznačen time što metod obuhvata kontakt kinaze sa kinaza-inhibitomim jedinjenjem u skladu sa bilo kojim od patentnih zahteva 1 do 12.
16.    Metod moduliranja ćelijskog procesa (na primer deobe ćelija) inhibicijom aktivnosti ciklin zavisne kinaze korišćenjem jedinjenja u skladu sa bilo kojim od patentnih zahteva 1 do 12.
17.    Jedinjenje u skladu sa bilo kojim od patentnih zahteva 1 do 12 naznačeno time što se koristi u profilaksi ili tretmanu bolesnog stanja kao što je ovde opisano.
18.    Upotreba jedinjenja u skladu sa bilo kojim od patentnih zahteva 1 do 12 za proizvodnju medikamenta, naznačena time da je medikament za bilo koju ili više upotreba koje su ovde definisane.
19.    Farmaceutska kompozicija naznačena time što sadrži jedinjenje u skladu sa bilo kojim od patentnih zahteva 1 do 12 i farmaceutski prihvatljiv nosač.
20.    Farmaceutska kompozicija naznačena time što sadrži jedinjenje u skladu sa bilo kojim od patentnih zahteva 1 do 12 i farmaceutski prihvatljiv nosač u obliku pogodnom za oralnu primenu.
21.    Jedinjenje formule I(a): ili njegova farmaceutski prihvatljiva so, naznačeno time što: R50 je CONR54R55, ili CN; R51 je C3-14cikloalkil koji može biti nesupstituisan ili supstituisan sa C1-3alkil, ili OH; Z je CH ili N; i V je NR56 ili CHR57; R54 i R55 su nezavsno H, C1-3alkil, R52, R53 R56, i R57 su nezavsno H, C1-8alkil, C3-14cikloalkil, C1-8haloalkil, NR58R59, C(0)OR6°, C(0)C1-8alkil, C0-8alkilC(O)C0-8alkil-NR61R62, C1-8alkoksi, C1-8alkilOR63, C(0)-5-14cikloheteroalkil grupa, C3-14cikloalkil grupa, od kojih svaki kad nije H može biti supstituisan jednim ili više od C1-8alkil, OH, ili CN; R58, R59, R60, R61, R62, i R63 su H ili C1-8alkil.
22. Jedinjenje naznačeno time što je izabrano od: 7-Ciklopentil-2-[5-(3-metil-piperazin-l-il)-piridin-2-ilamino]-7H-pirolo[2,3d]pirimidin-6-karbonitril; 7-Ciklopentil-2-{5-[4-(2-fluoro-etil)-piperazin-l-il]-piridin-2-ilamino}-7H-pirolo[2,3-d]pirimidin-6-d im eti lkarboksam id; 7-Ciklopentil-2-(4-dimetilamino-3,4,5,6-tetrahidro-2H-[l,3']bipiridinil-6'-ilamino)-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 2-[5-(4-Karbamoilmetil-piperazin-l-il)-piridin-2-ilamino]-7-ciklopentil-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 2-{5-[4-(2-Amino-acetil)-piperazin-l-il]-piridin-2-ilamino}-7-ciklopentil-7H-pirolo[2,3-d]pirimidin-6- dimetilkarboksamid; 2-[5-(3-Amino-pirolidin-l-il)-piridin-2-ilamino]-7-ciklopentil-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7- Ciklopentil-2-{5-[4-(2-metoksi-etil)-piperazin-l-il]-piridin-2-ilamino}-7H-pirolo[2,3-d]pirimidin-6- dimetilkarboksamid; 7- Ciklopentil-2-[4-(2-hidroksietil)-3,4,5,6-tetrahidro-2H-[l,2']bipirazinil-5'-ilamino]-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-[5-((R)-3-metil-piperazin-l-il)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-[5-((S)-3-metilpiperazin-l-il)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-[5-(3-metilpiperazin-l-il)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-{5-[4-(3-hidroksipropil)-piperazin-l-il]-piridin-2-ilamino}-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-{5-[4-(pirolidin-l-karbonil)-piperazin-l-il]-piridin-2-ilamino}-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-{5-[4-(2-hidroksi-etil)-piperazin-l-il]-piridin-2-ilamino}-7H-pirolo[2,3-d]pirimidin-6- dimetilkarboksamid; 7- Ciklopentil-2-{5-[4-((S)-2,3-dihidroksipropil)-piperazin-l-il]-piridin-2-ilamino}-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-(5-{4-[2-(2-hidroksietoksi)-etil]-piperazin-l-il}-piridin-2-ilamino)-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-{5-[4-(2-hidroksi-1 -metileti l)-piperazin-1 -il]-piridin-2-ilamino} -7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-{6-[4-(2-hidroksietil)-piperazin-l-il]-piridazin-3-ilamino}-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-{5-[4-(2,3-dihidroksipropil)-piperazin-l-il]-piridin-2-ilamino}-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-CikIopentil-2-{5-[4-((R)-2,3-dihidroksipropil)-piperazin-l-il]-piridin-2-ilamino}-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-CikIopentil-2-(4-dimetilamino-3,4,5,6-tetrahidro-2H-[l,3']bipiridinil-6,-ilamino)-7H-pirolo[2,3-d]pirimidin-6-karbonitriI; 7-Ciklopentil-2-(3,4,5,6-tetrahidro-2H-[l,2']bipirazinil-5'-ilamino)-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-[5-(piperazin-l-karbonil)-piridin-2-iIamino]-7H-pirolo[2,3d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-[5-(4-dimetilaminopiperidin-l-karbonil)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-(r,2,,3',4',5',6'-heksahidro-[3,4']bipiridinil-6-ilamino)-7H-pirolo[2,3d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-[5-((S)-3-metilpiperazin-l-ilmetil)-piridin-2-ilamino]-7Hpirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-{5-[4-((S)-2-hidroksipropil)-piperazin-l-il]-piridin-2-ilamino}-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-{5-[4-((R)-2-hidroksipropil)-piperazin-l-il]-piridin-2-ilamino}-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-(5-piperazin-l-il-piridin-2-ilamino)-7H-pirolo[2,3-d]pirimidin-6-metil karboksamid; 7-Ciklopentil-2-[5-(4-izopropil-piperazin-l-il)-piridin-2-ilamino]-7H-pirolo[2,3d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-[5-(4-izopropil-piperazin-l-karboniI)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6- dimetilkarboksamid; 7- Ciklopentil-2-{5-[4-(4-metil-pentil)-piperazin-l-il]-piridin-2-ilamino}-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-[6-(4-izopropil-piperazin-l-il)-piridazin-3-ilamino]-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-{5-[4-(2-hidroksi-2metilpropi])-piperazin-l-il]-piridin-2-ilamino}-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-[5-(3,3-dimetil-piperazin-l-il)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-[5-(3,8-diaza-biciklo[3.2.1]okt-3-ilmetil)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-(5-piperazin-l-il-piridin-2-ilamino)-7H-pirolo[2,3-d]pirimidin-6- dimetilkarboksamid; 7-Ciklopentil-2-[5-(4-etil-piperazin-l-il)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-[5-(4-ciklopentil-piperazin-l-il)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-(r-izopropil-r,2',3',4',5',6'-heksahidro-[3,4']bipiridinil-6-ilamino)-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-{5-[(R)-4-(2-hidroksietil)-3-metil-piperazin-l-il]-piridin-2-ilamino}-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-{5-[(S)-4-(2-hidroksietil)-3-metil-piperazin-l-il]-piridin-2-ilamino}-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-{5-[4-(2-hidroksietil)-piperazin-l-ilmetil]-piridin-2-ilamino}-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-{5-[4-(2-dimetilaminoacetil)-piperazin-l-il]-piridin-2-ilamino}-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-{5-[4-(2-etil-butil)piperazin-l-il]-piridin-2-ilamino}-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 2-{5-[4-(2-Cikloheksil-acetil)piperazin-l-il]-piridin-2-ilamino}-7-ciklopentil-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-{5-[4-(3-ciklopentil-propionil)-piperazin-l-il]-piridin-2-ilamino}7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-[5-(4-izobutilpiperazin-l-il)-piridin-2-ilamino]-7H-pirolo[2,3d]pirimidin-6-dimetilkarboksamid; Metil estar {4-[6-(7-ciklopentil-6-dimetilkarbamoil-7H-pirolo[2,3-d]pirimidin-2-ilamino)piridin-3-il]-piperazin-l-il}-acetatne kiseline; 7-Ciklopentil-2-{5-[4-(2-izopropoksietil)-piperazin-l-il]-piridin-2-ilamino}-7Hpirolo[2,3-d]pirimidin-6-dimetilkarboksamid; Etil estar {4-[6-(7-ciklopentil-6-dimetilkarbamoil-7H-pirolo[2,3-d]pirimidin-2-ilamino)piridin-3-il]-piperazin-l-il}-acetatne kiseline; ferc-Butil estar 4-(6-{7-ciklopentil-6-[(2-hidroksi-etil)metil-karbamoil]-7H-pirolo[2,3-d]pirimidin-2-ilamino}-piridin-3-il)piperazin-l-karboksilne kiseline; 7-Ciklopentil-2-{5-[4-(2-metil-butil)piperazin-l-il]-piridin-2-ilamino}-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; 7-Ciklopentil-2-[r-(2-hidroksi-etil)-r,2',3',4',5',6'-heksahidro-[3,4']bipiridinil-6-ilamino]-7H-pirolo[2,3-d]pirimidin-6-dimetilkarboksamid; {4-[6-(7-Ciklopentil-6-dimetilkarbamoil-7H-pirolo[2,3-d]pirimidin-2-ilamino)-piridin-3-il]piperazin-l-il}-acetatna kiselina; i 2-{4-[6-(7-Ciklopentil-6-dimetilkarbamoil-7H-pirolo[2,3-d]pirimidin-2-ilamino)-piridin-3-il]-piperazin-l-il}-propionska kiselina; ili njihove farmaceutski prihvatljive soli.
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