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VITRONECTIN RECEPTOR ANTAGONISTS, PROCESS FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME AND USE THEREOF IN THE PREPARATION OF MEDICAMENTS FOR TREATMENT OF OSTEOPOROSIS AND INHIBITION OF ANGIOGENESIS
VITRONECTIN RECEPTOR ANTAGONISTS, PROCESS FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME AND USE THEREOF IN THE PREPARATION OF MEDICAMENTS FOR TREATMENT OF OSTEOPOROSIS AND INHIBITION OF ANGIOGENESIS
A compound of the formula wherein: R1 is R7, or A-C0-4 alkyl, A-C2-4 alkenyl, A-C2-4 alkynyl, A-C3-4 oxoalkenyl, A-C3-4 oxoalkynyl, A-C1-4 aminoalkyl, A-C3-4 aminoalkenyl, A-C3-4 aminoalkynyl, optionally substituted by any accessible combination of one or more of R10 or R7; A is H, C3-6 cycloalkyl, Het or Ar; R7 is -COR8, -COCR'2R9, -C(S)R8, -S(O)mOR', -S(O)mNR'R'', 1833 ז' באב התשס" ד - July 25, 2004 -PO(OR'), -PO(OR')2 NO2, or tetrazolyl; each R8 independently is -OR', -NR'R'', -NR'SO2R', -NR'OR', or -OCR'2CO(O)R'; R9 is -OR', -CN, -S(O)rR', -S(O)mNR'2, -C(O)R', C(O)NR'2 or -CO2R'; R10 is H, halo, -OR11, -CN, -NR'R11, -NO2, -CF3, CF3S(O)r-, CO2R', -CONR'2, A-C0-6 alkyl-, A-C1-6 oxoalkyl-, A-C2-6 alkenyl, A-C2-6 alkynyl-, A-C0-6 alkyloxy-, A-C0-6 alkylamino- or A-C0-6 alkyl-S(O)r-; R11 is R', -C(O)R', -C(O)NR'2, -C(O)OR', -S(O)mR', or -S(O)mNR'2; R2 is 1834 ז' באב התשס" ד - July 25, 2004 W is -(CHRg)a-U- (CHRg)b-; U is absent or CO, CRg2, C(=CRg2), S(O)k, O, NRg, CRgORg, CRg(ORk)CRg2, CRg2(ORk), C(O)CRg2, CRg2C(O), CONRi, NRiCO, OC(O), C(O)O, C(S)O, OC(S), C(S)NRg, NRgC(S), S(O)2NRg, NRgS(O)2 N=N, NRgNRg, NRgCRg2, CRg2NRg, CRg2O, OCRg2, C:C or CRg=CRg; G is NRe, S or O; Rg is H, C1-6 alkyl, Het-C0-6 alkyl, C3-7 cycloalkyl-C0-6 alkyl or Ar-C0-6 alkyl; Rk is Rg, -C(O)Rg, or -C(O)ORf; Ri is is H, C1-6 alkyl, Het-C0-6 alkyl, C3-7 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, or C1-6 alkyl substituted by one to three groups chosen from halogen, CN, NRg2, ORg, SRg, CO2Rg, and CON(Rg)2; Rf is H, C1-6 alkyl or Ar-C0-6 alkyl; Re is H, C1-6 alkyl, Ar-C0-6 alkyl, Het-C0-6 alkyl, C3-7 cycloalkyl-C0-6 alkyl, or (CH2)k CO2Rg; Rb and Rc are independently selected from H, C1-6 alkyl, Ar-C0-6 alkyl, Het-C0-6 alkyl, or C3-6 cycloalkyl-C0-6 alkyl, halogen, CF3, ORf, S(O)kRf, CORf, NO2 N(Rf)2, CO(NRf)2, CH2N(Rf)2, or Rb and Rc are joined together to form a five to six membered aromatic or non-aromatic carbocyclic or heterocyclic ring, optionally substituted by up to three substituents chosen from halogen, CF3, C1-4 alkyl, ORf, S(O)kRf, CORf, CO2Rf, OH, NO2, N(Rf)2, CO(NRf)2, and CH2N(Rf)2; or methylenedioxy; Q1, Q2, Q3 and Q4 are independently N or C-Ry, provided that no more than one of Q1, Q2, Q3 and Q4 is N; R' is H, C1-6 alkyl, Ar-C0-6 alkyl or C3-6 cycloalkyl-C0-6 alkyl; R) is R(, -C(O)R' or -C(O)OR'; Ry is H, halo, -ORg, -SRg, -CN, -NRgRk, -NO2, -CF3, CF3S(O)r-, CO2Rg, -CORg or -CONRg2, or C1-6 alkyl optionally substituted by halo, -ORg, -SRg, -NC, -NRgR), -NO2, -CF2, R'S(O)r-, -CO2Rg, -CORg or -CONRg2; a is 0, 1 or 2; b is 0, 1 or 2; k is 0, 1 or 2; m is 1 or 2; r is 0, 1 or 2; s is 0, 1 or 2; u is 0 or 1; and v is 0 or 1; or a pharmaceutically acceptable salt thereof. 1835 ז' באב התשס" ד - July 25, 2004
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