SI20975B - N-/5-///5-alkil-2-oksazolil/metil/tio/-2-tiazolil/-karboksamidni inhibitorji ciklodekstrin odvisne kinaze - Google Patents

N-/5-///5-alkil-2-oksazolil/metil/tio/-2-tiazolil/-karboksamidni inhibitorji ciklodekstrin odvisne kinaze Download PDF

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SI20975B
SI20975B SI200020060A SI200020060A SI20975B SI 20975 B SI20975 B SI 20975B SI 200020060 A SI200020060 A SI 200020060A SI 200020060 A SI200020060 A SI 200020060A SI 20975 B SI20975 B SI 20975B
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methyl
medicament
dimethylethyl
oxazolyl
thio
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S David Kimball
Kyoung S Kim
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Bristol Myers Squibb Co
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Abstract

Izum opisuje spojine s formulo (I) in njene enantiomere, diastereomere in farmacevtsko sprejemljivesoli. Spojine s formulo (I) so inhibitorji protein kinaze in so uporabne pri zdravljenju proliferativnih oziroma hitro napredujocih bolezni, kot na primer raka, vnetij in artritisa. Uporabne so tudi pri zdravljenju Alzheimerjeve bolezni, plesavosti povzrocene s kemoterapijo in kardiovaskularnih bolezni.

Description

* V tem dokumentu so objavljeni spremenjeni zahtevki patenta 20975 A. Zahtevki so bili spremenjeni na podlagi ugotovitvene odločbe, izdane po členu 93(1 )(b) Zakona o industrijski lastnini (Uradni list RS, št. 102/04)

Claims (29)

1. Spojina s formulo I in njene enantiomere, diastereoizomere in farmacevtsko sprejemljive soli, značilna po tem, da je:
R alkilni radikal, ki vsebuje od 1 do 12 ogljikovih atornov;
R,i. in R2 sta vsak neodvisno vodik ali alkilni radikal, ki vsebuje od 1 do 12 ogljikovih atomov;
Ra je vodik ali alkilni radikal,, ki vsebuje od 1 do 12 ogljikovih atomov in
Rzi je alkilni radikal, ki vsebuje od 1 do 12 ogljikovih atomov, substituiran 2 eno ali dvema hidroksi skupinama ali - eno NR^Re skupino ali pa sta R3 in R« združena z dušikovim atomom, na katerega sta vezana tako, da tvorita 4- do 7-členske heterociklične obroče, kjer je R3R4 predstavljen s -(CH2)n-, kjer je n celo število 3, 4, 5 ali 6;
R5 in R6 sta vsak neodvisno:
- vodik ali
- alkilni radikal, ki vsebuje od 1 do 12 ogljikovih atomov, po izbiri substituiran s substituenti iz skupine v kateri so: halogen, haloalkil, alkoksi, alkiltio, hidroksi, karboksi, alkilkarbonil, alkoksikarbonil, alkilkarboniloksi, amirto, karbamoil, urea, amidinil in tiol ali cikloalkil, ki vsebuje 3 do 15 ogljikovih atomov ali cikloalkil, ki vsebuje 3 do 15 ogljikovih atomov, substituiran s substituenti iz skupine v kateri so: halogen, alkil, alkoksi, alkil hidroksi, amino, nitro, ciano, tiol in alkiltio ali pa sta R5 in R6 združena z dušikovim atomom, na katerega sta vezana tako, da tvorita 4- do 7-členske heterociklične obroče, kjer je R5R6 predstavljen s -(CH2)m-, kjer je m celo število 3, 4, 5 ali 6; in
X je CH ali N.
2. Spojina po zahtevku 1, značilna po tem, da je: R je terc-butil;
Rx in R2 sta vsak neodvisno vodik ali metil;
R3 je vodik in
R4 je -CH2C (CH3) 2CH2OH, -CH2CH2OH, -C (CH3) 2CH2OH, CH(CH2OH)2, -CH2CH (OH) CH2OH, -CH(CH3)CH2OH ali
-CH2CH2N ali pa sta R3 in R4 združena z dušikovim atomom, na katerega sta vezana tako, da tvorita 5-členski heterociklični obroč, kjer je R3R4 predstavljen s -(CH2)4~; in
X je CH ali N.
3. Spojina po zahtevku 1 s formulo la in njene enantiomere, diastereoizomere in farmacevtsko sprejemljive soli, značilna po tem, da je:
Ri in R2 sta vsak neodvisno vodik ali metil; in
R3 je vodik in
R4 je -CH2C (CH3) 2CH2OH, -CH2CH2OH, -C (CH3) 2CH2OH, CH(CH2OH)2, -CH2CH(OH)CH2OH, -CH (CH3) CH2OH ali
-CH2CH2N
ali pa sta R3 in R4 združena z dušikovim atomom, na katerega sta vezana tako, da tvorita 5-členske heterociklične obroče, kjer je R3R4 predstavljen s
-(CH2)4-.
in njene enantiomere, diastereoizomere in farmacevtsko sprejemljive soli, značilna po tem, da je:
Ri in R2 sta vsak neodvisno vodik ali metil; in R3 je vodik
R4 je -CH2C(CH3)2CH2OH, -CH2CH2OH, -C (CH3) 2CH2OH, -CH(CH2OH)2, -CH2CH (OH) CH2OH, -CH(CH3)CH2OH ali
-CH2CH2N // ali pa sta R3 in R4 katerega sta vezana heterociklične obroče, združena z dušikovim atomom, na tako, da tvorita 5-členske kjer je R3R4 enak -(CH2)4-.
in njene enantiomere, diastereoizomere in farmacevtsko sprejemljive soli, značilna po tem, da je:
Ri in R2 sta vsak neodvisno vodik ali metil; in R3 je vodik in
R4 je -CH2C (CH3) 2CH2OH, -CH2CH2OH, -C (CH3) 2CH2OH, -CH(CH2OH)2, -CH2CH (OH) CH2OH, -CH (CH3) CH2OH ali
-CH2CH2N ali pa sta R3 in R4 združena z dušikovim atomom, na katerega sta vezana tako, da tvorita 5-členske heterociklične obroče, kjer je R3R4 enak - (CH2) 4-.
6. Spojina po zahtevku 1, značilna po tem, da je izbrana iz skupine, ki vsebuje:
N—[5—[[[5— (1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[[[2-hidroksi-l-(hidroksimetil)etil]amino]metil]benzenacetamid;
4-[[(2,3-dihidroksipropil)amino]metil]-N-[
5-[([5-(1, 1dimetiletil)-2-oksazolil]metil]tio]-2-tiazolil] benzenacetamid;
(R) -4-[[(2,3-dihidroksipropil)amino]metil]-N-[5-[[[5- (1,1 dimetiletil)-2-oksazolil]metil]tio]-2-tiazolil]benzenacetamid;
(S) -4- [ [ (2,3-dihidroksipropil)amino]metil]-N-[5-[[[5-(1,1 dimetiletil)-2-oksazolil]metil]tio]-2-tiazolil]benzenacetamid;
N-[5-[[[5-(l,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil-4-[[[3-hidroksi-2,2-dimetilpropil)amino]metil]benzenacetamid;
N—[5—[[[5—(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-(1-pirolidinilmetil)benzenacetamid;
N-[5-[[[5-(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[[(2-hidroksietil)amino]metil]benzenacetamid;
N—[5—[[[5—(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[[(2-(1-pirolidinil)etil)amino]metil]benzenacetamid;
N—[5—[[[5—(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[[(2-hidroksi-l,1-dimetiletil)amino]metil]benzenacetamid;
N-[5-[[[5-(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-3-[[ (2-hidroksietil)amino]metil]benzenacetamid;
N—[5—[[[5— (1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-3-[[(3-hidroksi-2,2-dimetilpropil)amino]metil]benzenacetamid;
N-[5-[[[5 —(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[[(2-hidroksi-l-metiletil) amino]metil]benzenacetamid;
N—[5 —[[[5-(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[1-[(2-hidroksietil)amino]etil]benzenacetamid;
N-[5-[[[5-(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[1-[(2-hidroksi-l-metiletil)amino]etil]benzenacetamid;
(S)-N-[5-[[[5-(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[[(2-hidroksietil)amino]metil]-a-metilbenzenacetamid;
N-[5-[[[5-(l,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-
6- [ [ (2-hidroksietil)amino]metil]-3piridinacetamid; in
N-[5-[[[5-(l,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[[(2-hidroksietil)amino]metil]-a-metilbenzenacetamid;
ter njihove farmacevtsko sprejemljive soli.
7. Spojina po zahtevku 1, značilna po tem, da ima formulo N—[5—[[[5—(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[[[2-hidroksi-l-(hidroksimetil)-etil]amino]metil]benzenacetamid in njene farmacevtsko sprejemljive soli.
8. Spojina po zahtevku 1, značilna po tem, da ima formulo N-[5-[[[5 —(1,1-dimetiletil)-2-oksazolil]metil]tio]-2tiazolil]-4-[[(2-hidroksi-l,1-dimetiletil)amino]metil]benzenacetamid in njene farmacevtsko sprejemljive soli.
9. Spojina po zahtevku 1, značilna po tem, da ima formulo 4-[[(2,3-dihidroksipropil)amino]metil]-N-[5-[[[5-(1,1dimetiletil)-2-oksazolil]metil]tio]-2-tiazolil]benzenacetamid in njene farmacevtsko sprejemljive soli.
10. Spojina po zahtevku 1, značilna po tem, da ima formulo (R)-4-[[(2,3-dihidroksipropil)amino]metil]-N-[5[[[5-(1,1-dimetiletil)-2-oksazolil]metil]tio]-2-tiazolil]benzenacetamid in njene farmacevtsko sprejemljive soli.
ϊ
11. Spojina po zahtevku 1, značilna po tem, da ima formulo (S) -4-[ [ (2,3-dihidroksipropil)amino]metil]-N- [5[[[5-(1,1-dimetiletil)-2-oksazolil]metil]tio]-2-tiazolil]benzenacetamid in njene farmacevtsko sprejemljive soli.
12. Farmacevtska zmes, značilna Po tem, da sestoji iz spoj in po zahtevkih od 1 do 11 in farmacevtsko sprejemljivega nosilca. 13. Farmacevtska zmes, značilna po tem, da vsebuje spoj ine po kateremkoli od zahtevkov od 1 do 11 v kombinaciji
s farmacevtsko sprejemljivim nosilcem in sredstvom proti raku v določeni količini.
14. Farmacevtska zmes, značilna po tem, da vsebuje spojine po kateremkoli od zahtevkov od 1 do 11 v kombinaciji s farmacevtsko sprejemljivim nosilcem in modulatorjem transaktivacij e p53 v določeni količini.
15. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z modulacijo apoptoze.
16. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicijo protein kinaz.
17. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicijo ciklin odvisnih kinaz.
18. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicijo cdc2 (cdkl).
19. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicijo cdk2.
20. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicijo cdk3.
21. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicijo cdk4.
22. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicijo cdk5.
23. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicijo cdk6.
24. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicij o cdk7.
25. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje bolezni, ki se jo zdravi z ihibicij o cdk8.
26. Uporaba spojine po kateremkoli od zahtevkov od 12 do 14 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje proliferativnih bolezni.
27. Uporaba spojine po kateremkoli od zahtevkov od 12 do 14 za izdelavo zdravila, značilna po tem, da_se omenjeno zdravilo uporablja za zdravljenje raka.
28. Uporaba spojine po kateremkoli od zahtevkov od 12 do 14 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje vnetja, vnetnih bolezni črevesja ali zavrnitev presadkov.
29. Uporaba spojine po kateremkoli od zahtevkov od 12 do 14 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje artritisa.
30. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje nepravilnosti povezanih s ciklin odvisnimi kinazami.
31. Uporaba spojine po kateremkoli od zahtevkov od 1 do 11 za izdelavo zdravila, značilna po tem, da se omenjeno zdravilo uporablja za zdravljenje alopecije, trombocitopenij e in mukozitisa povzročenih s kemoterapijo
SI200020060A 1999-12-15 2000-12-07 N-/5-///5-alkil-2-oksazolil/metil/tio/-2-tiazolil/-karboksamidni inhibitorji ciklodekstrin odvisne kinaze SI20975B (sl)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US09/464,511 US6262096B1 (en) 1997-11-12 1999-12-15 Aminothiazole inhibitors of cyclin dependent kinases
US09/616,629 US6214852B1 (en) 1998-10-21 2000-07-26 N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
PCT/US2000/033113 WO2001044241A1 (en) 1999-12-15 2000-12-07 N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases

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Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6262096B1 (en) 1997-11-12 2001-07-17 Bristol-Myers Squibb Company Aminothiazole inhibitors of cyclin dependent kinases
US6414156B2 (en) 1998-10-21 2002-07-02 Bristol-Myers Squibb Company Process for preparing azacycloalkanoylaminothiazoles
US6515004B1 (en) 1999-12-15 2003-02-04 Bristol-Myers Squibb Company N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
US6392053B2 (en) * 1999-12-15 2002-05-21 Bristol-Myers Squibb Company Process for preparing arylacetylaminothiazoles
US6534531B2 (en) * 2000-04-27 2003-03-18 Bristol-Myers Squibb Company Methods for preventing and treating alopecia induced by chemotherapy or radiotherapy
EP1724270A3 (en) * 2001-07-19 2007-01-03 Pfizer Italia S.r.l. Phenylacetamido-thiazole derivatives, process for their preparation and their use as antitumor agents
CA2453294A1 (en) * 2001-07-19 2003-01-30 Paolo Pevarello Phenylacetamido-thiazole derivatives, process for their preparation and their use as antitumor agents
ES2183734B1 (es) * 2001-08-02 2004-06-16 Consejo Sup. Investigaciones Cientificas Derivados de 4-4'-bipiridil-2-2'-bisoxazoles y 4-4'-bipiridil-2-2'-bistiazoles como agentes antineoplasicos.
JP2004538315A (ja) * 2001-08-03 2004-12-24 ノボ・ノルデイスク・エー／エス 新規の２，４−ジアミノチアゾール誘導体
CN1547574A (zh) * 2001-08-03 2004-11-17 ŵ��Ų�ڿ˹�˾ 新型2,4-二氨基噻唑衍生物
TW200401638A (en) * 2002-06-20 2004-02-01 Bristol Myers Squibb Co Heterocyclic inhibitors of kinases
DE10300124A1 (de) * 2003-01-07 2004-07-15 Bayer Ag Verfahren zur Herstellung von Arylalkinen
US20070105114A1 (en) * 2003-07-29 2007-05-10 Martha Li Biomarkers of cyclin-dependent kinase modulation
US7888504B2 (en) * 2006-07-06 2011-02-15 Bristol-Myers Squibb Company Glucokinase activators and methods of using same
WO2008049856A2 (en) * 2006-10-25 2008-05-02 Ingenium Pharmaceuticals Gmbh Methods of treating pain using cdk inhibitors
CA2784807C (en) 2009-12-29 2021-12-14 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
MX342746B (es) * 2011-09-28 2016-10-11 Euro-Celtique S A * Derivados de mostaza de nitrogeno.
US9382239B2 (en) 2011-11-17 2016-07-05 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-terminal kinase (JNK)
AR092790A1 (es) 2012-02-01 2015-05-06 Euro Celtique Sa Derivados bencimidazolicos del acido hidroxamico
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
USRE48175E1 (en) 2012-10-19 2020-08-25 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
EP3057956B1 (en) 2013-10-18 2021-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
US20160264551A1 (en) 2013-10-18 2016-09-15 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
GB201409488D0 (en) 2014-05-28 2014-07-09 Euro Celtique Sa Pharmaceutical composition
GB201409485D0 (en) 2014-05-28 2014-07-09 Euro Celtique Sa Pharmaceutical composition
GB201409471D0 (en) 2014-05-28 2014-07-09 Euro Celtique Sa Pharmaceutical composition
WO2016105528A2 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
US10550121B2 (en) 2015-03-27 2020-02-04 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
EP4019515A1 (en) * 2015-09-09 2022-06-29 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
AU2016426574B2 (en) 2016-10-11 2023-07-13 Euro-Celtique S.A. Hodgkin lymphoma therapy
GB201709405D0 (en) 2017-06-13 2017-07-26 Euro Celtique Sa Compounds for treating ovarian cancer
GB201709406D0 (en) 2017-06-13 2017-07-26 Euro-Cletique S A Compounds for treating TNBC
GB201709403D0 (en) 2017-06-13 2017-07-26 Euro Celtique Sa Compounds for treating sarcoma
GB201709402D0 (en) 2017-06-13 2017-07-26 Euro Celtique Sa Compounds for treating t-pll

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1088049A (en) 1975-06-03 1980-10-21 Takashi Masugi 3-substituted-7-substituted alkanamido-3-cephem-4- carboxylic acid compounds and processes for preparation thereof
CA1201431A (en) 1981-12-17 1986-03-04 Daiei Tunemoto .beta.-LACTAM COMPOUNDS, PROCESS FOR THE PREPARATION THEREOF AND INTERMEDIATE PRODUCTS FOR THE PREPARATION THEREOF
TW205041B (sl) 1989-08-07 1993-05-01 Fujisawa Pharmaceutical Co
US5491157A (en) 1993-05-10 1996-02-13 Eastman Kodak Company Method and composition for the prevention, control and amelioration of soilborne fungi and disease caused thereby
IL112721A0 (en) 1994-03-10 1995-05-26 Zeneca Ltd Azole derivatives
EP0796263A1 (en) 1994-12-09 1997-09-24 Fujisawa Pharmaceutical Co., Ltd. Cephem compounds and pharmaceutical use thereof
IL117620A0 (en) 1995-03-27 1996-07-23 Fujisawa Pharmaceutical Co Heterocyclic compounds processes for the preparation thereof and pharmaceutical compositions containing the same
AUPN801196A0 (en) 1996-02-12 1996-03-07 Fujisawa Pharmaceutical Co., Ltd. New cephem compounds and pharmaceutical use thereof
GEP20032896B (en) 1997-10-27 2003-02-25 Agouron Pharma 4-Aminothiazole Derivatives, Containing Them Pharmaceutical Compositions Inhibiting Cyclin-Dependent Kinases and Methods for Treatment
US6040321A (en) 1997-11-12 2000-03-21 Bristol-Myers Squibb Company Aminothiazole inhibitors of cyclin dependent kinases
GB9823871D0 (en) 1998-10-30 1998-12-23 Pharmacia & Upjohn Spa 2-Amino-thiazole derivatives, process for their preparation, and their use as antitumour agents

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PT1240165E (pt) 2005-09-30
DE60019964T2 (de) 2006-04-27
EP1240165A1 (en) 2002-09-18
CA2394544A1 (en) 2001-06-21
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CN1433415A (zh) 2003-07-30
US6214852B1 (en) 2001-04-10
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PL364884A1 (en) 2004-12-27
DE60019964D1 (en) 2005-06-09
KR20020067547A (ko) 2002-08-22
ATE294800T1 (de) 2005-05-15
WO2001044241A1 (en) 2001-06-21
SI20975A (sl) 2003-02-28
HUP0300974A2 (hu) 2003-08-28
DK1240165T3 (da) 2005-08-08
HUP0300974A3 (en) 2009-03-30
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