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1. WO2007141473 - N-(BENZOYL)-O- [2- (PYRIDIN- 2 -YLAMINO) ETHYL] -L-TYROSINE DERIVATIVES AND RELATED COMPOUNDS AS A5B1 ANTAGONISTS FOR THE TREATMENT OF SOLID TUMORS

Publication Number WO/2007/141473
Publication Date 13.12.2007
International Application No. PCT/GB2007/001697
International Filing Date 10.05.2007
IPC
C07D 213/75 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with 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
72Nitrogen atoms
75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C07D 471/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 213/74 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with 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
72Nitrogen atoms
74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C07D 213/89 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
89with hetero atoms directly attached to the ring nitrogen atom
C07D 235/30 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
235Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02condensed with carbocyclic rings or ring systems
04Benzimidazoles; Hydrogenated benzimidazoles
24with 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 in position 2
30Nitrogen atoms not forming part of a nitro radical
A61K 31/4402 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
4402only substituted in position 2, e.g. pheniramine, bisacodyl
CPC
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 35/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
02specific for leukemia
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
C07D 213/73
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72Nitrogen atoms
73Unsubstituted amino or imino radicals
C07D 213/74
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72Nitrogen atoms
74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C07D 213/75
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72Nitrogen atoms
75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
Applicants
  • ASTRAZENECA AB [SE]/[SE] (AE, AG, AL, AM, AT, AU, AZ, BA, BB, BE, BF, BG, BH, BJ, BR, BW, BY, BZ, CA, CF, CG, CH, CI, CM, CN, CO, CR, CU, CY, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, GR, GT, GW, HN, HR, HU, ID, IE, IL, IN, IS, IT, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MC, MD, MK, ML, MN, MR, MT, MW, MX, MY, MZ, NA, NE, NG, NI, NL, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SI, SK, SL, SM, SN, SV, SY, SZ, TD, TG, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VC, VN, ZA, ZM, ZW)
  • ASTRAZENECA UK LIMITED [GB]/[GB] (MG)
  • ARNOULD, Jean-Claude [FR]/[FR] (UsOnly)
  • DELOUVRIE, Benedicte [FR]/[FR] (UsOnly)
  • DUCRAY, Richard [FR]/[FR] (UsOnly)
  • LAMBERT-VAN DER BREMPT, Christine, Marie, Paul [BE]/[FR] (UsOnly)
Inventors
  • ARNOULD, Jean-Claude
  • DELOUVRIE, Benedicte
  • DUCRAY, Richard
  • LAMBERT-VAN DER BREMPT, Christine, Marie, Paul
Agents
  • GLOBAL INTELLECTUAL PROPERTY
Priority Data
06300576.309.06.2006EP
06301245.412.12.2006EP
07300973.023.04.2007EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) N-(BENZOYL)-O- [2- (PYRIDIN- 2 -YLAMINO) ETHYL] -L-TYROSINE DERIVATIVES AND RELATED COMPOUNDS AS A5B1 ANTAGONISTS FOR THE TREATMENT OF SOLID TUMORS
(FR) DÉRIVÉS DE PHÉNYLALANINE
Abstract
(EN)
The present invention relates to compounds that inhibit of a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to a5b1 antagonists that also exhibit appropriate selectivity profile(s) against other integrins.
(FR)
La présente invention concerne des composés qui inhibent la fonction de a5b1, des procédés pour leur préparation, des compositions pharmaceutiques contenant ceux-ci en tant qu'ingrédient actif, leur utilisation en tant que médicaments et leur utilisation dans la fabrication de médicaments pour utilisation dans le traitement chez des animaux à sang chaud tels que des humains de maladies qui ont une angiogenèse significative de composant vasculaire tel que pour le traitement de tumeurs solides. La présente invention concerne en outre des antagonistes de a5b1 qui présentent en outre des profil(s) de sélectivité appropriés contre d'autres intégrines.
Latest bibliographic data on file with the International Bureau