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    43.
    发明专利
    未知

    公开(公告)号：ID19254A

    公开(公告)日：1998-06-28

    申请号：ID973919

    申请日：1997-12-18

    Applicant: HOECHST AG ,  GENENTECH INC

    Inventor： PEYMAN ANUSCHIRWAN DR ,  KNOLLE JOCHEN DR ,  WEHNER VOLKMAR DR ,  BREIPOHL GERHARD DR ,  GOURVEST JEAN-FRANCOIS DR ,  CARNIATO DENIS DR ,  GADEK THOMAS RICHARD DR

    IPC: C07D473/00 ,  A61K31/52 ,  A61P3/00 ,  A61P9/00 ,  A61P13/12 ,  A61P19/00 ,  A61P19/10 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D233/00 ,  C07D239/00 ,  C07D401/12 ,  C07D403/12 ,  C07D473/02 ,  C07D473/26 ,  C07D473/34 ,  C07D473/40

    Abstract: Purine derivatives of formula (I) and (Ia), and their salts, are new. One of R', R" = (CR1R2)nA-(CR1R2)m(CR1R3)i-(CR1R2)qR4 and the other = (CR1R2)rA'-(CR1R2)s(CR1R3)k-(CR1R2)tDE; X = H, NH2, OH, NHCOR6; A, A' = bond, CONR5, NR5CO, C(O), NR5, O, S, SO, SO2, Ar, 2-4C alkynylene, 2-4C alkenylene, or a 3-7 membered ring (optionally containing 1-2 Het and optionally substituted by =O, =S or R3); Ar = 5-14C arylene optionally with 1-5 C replaced by heteroatoms; R1, R2 = H, F, Cl, CN, nitro, 1-10C alkyl, 3-14C cycloalkyl, (3-12C cycloalkyl)(1-8C alkyl), 5-14C aryl, (5-14C aryl)(1-8C alkyl), R7-O-R6, R7-S(O)p-R6 or R7N-R6R61; R3 = H, F, Cl, CN, nitro, 1-14C alkyl, 3-14C cycloalkyl, (3-14C cycloalkyl)(1-8C alkyl), 5-14C aryl, (5-14C aryl)(1-8C alkyl), R7-O-R6, R7-S(O)p-R6, R7N-R6R61, R7OCOR6, R7COR6, R7COOR6, R7OCONR5R6, R7NR5S(O)pR6, R7NR5COOR6, R7NR5COR6, R7NR5CONR5R6, R7NR5S(O)pNR5R6, R7S(O)pR6, R7NS(O)pNR5R6, R7NR6COSR6, R7COR6 or R7CONR5R6, (where alkyl is optionally substituted, and alkyl (sic) and aryl are all optionally substituted, by one or more of F, Cl, Br, CN, NO2, R7NR5R6, R7NR6R61, R7COOR6, R7COR6, ; R7CONR5R6, R7S(O)pNR5R6, R6 or R7OR6); R4 = COR8, CSR8, S(O)pR8, POR8R81, a D- or L-aminoacid or a 4-8-membered saturated or unsaturated heterocycle containing 1-4 Het; R5 = H, 1-10C alkyl, 3-14C cycloalkyl, (3-14C cycloalkyl)-1-8C alkyl, 5-14C aryl or (5-14C aryl)-1-8C alkyl; R6, R61 = H, 1-8C alkyl, 3-14C cycloalkyl, 1-8C alkyl (substituted by 3-14C cycloalkyl or ArH) or ArH; or R6+R61 complete a ring system which may contain Het; R7 = a bond or 1-4C alkylene; R8, R81 = OH, 1-8C alkoxy, (5-14C aryl)(1-8C alkoxy), 5-14C aryloxy, (1-8C alkylcarbonyloxy)(1-4C alkoxy), (5-14C aryl)(1-8C alkyl)carbonyloxy(1-6C alkoxy), NR6R61, 1-8C dialkylaminocarbonylmethyloxy, (5-14C aryl)(1-8C dialkyl)aminocarbonylmethyloxy, 5-14C arylamino or an L or D amino acid; B = bond, O, S, NR5, NR5CO, CONR5, or a 3-7 membered ring (optionally containing 1-2 heteroatoms and optionally substituted by one or two =O, =S or R3); D = bond, NR6, CONR6, NR6CO, SO2NR6, NR6CONR6, NR6CSNR6, NR6S(O)uNR6, NR6COO, NR6N=CR6, NR6S(O)u, (5-14C aryl)CO, (5-14C aryl)S(O)u, N=CR6, CR6=N or CR6=N-NR6; E = H, NR6C(R6)=NR6, C(=NR6)NR6R61, NR6C(=NR6)NR6R61, or a 4-11 membered monocyclic or polycyclic aromatic or non-aromatic ring system (optionally containing 1-4 Het and optionally mono- to tri- substituted by R3, R5, =O, =S or C(=NR6)NR6R61); Het = N, O, S; n, m, s, t = 0-5; i, k = 0 or 1; p, q = 0-2; r = 0-6; u = 1 or 2.

    44.
    发明专利
    未知

    公开(公告)号：DE19653647A1

    公开(公告)日：1998-06-25

    申请号：DE19653647

    申请日：1996-12-20

    Applicant: HOECHST AG ,  GENENTECH INC

    Inventor： WEHNER VOLKMAR DR ,  STILZ HANS-ULRICH DR ,  PEYMAN ANUSCHIRWAN DR ,  KNOLLE JOCHEN DR ,  RUXER JEAN-MARIE DR ,  CARNIATO DENIS DR ,  LEFRANCOIS JEAN-MICHEL ,  GADEK THOMAS RICHARD DR ,  MCDOWELL ROBERT DR

    IPC: C07D239/00 ,  A61K31/155 ,  A61K31/16 ,  A61K31/18 ,  A61K31/33 ,  A61K31/395 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/47 ,  A61K31/472 ,  A61K31/55 ,  A61K38/04 ,  A61P9/00 ,  A61P19/08 ,  A61P19/10 ,  A61P25/00 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07C279/20 ,  C07C279/24 ,  C07C311/64 ,  C07C313/30 ,  C07C327/00 ,  C07D217/24 ,  C07D233/04 ,  C07D235/16 ,  C07D243/06 ,  C07D253/06 ,  C07D253/08 ,  C07D263/52 ,  C07D267/08 ,  C07D277/60 ,  C07D471/02 ,  C07D471/04 ,  C07D487/04 ,  C07K5/04 ,  C07D487/08 ,  A61K38/39

    Abstract: Guanidine and cycloguanidine derivatives of formula A-B-D-E-F-G (I) and their salts are new. A = R R N-C(=NR )NR Z- or a group of formula (a) or (b); Z = C(Q) or S(O)n; Q = O or S; n = 1 or 2; R = 5-10 membered mono- or polycyclic, aromatic or non-aromatic ring (optionally containing 1-4 N, O and/or S and optionally substituted by 1 or more of R -R ); B = direct bond; or alkyl, -CR =CR -, 5-10C aryl, 3-8C cycloalkyl or -C IDENTICAL C- (all optionally mono- or disubstituted by 1-8C alkyl), e.g. Me-Ph-Me or Et-CH=CH-; D, F = direct bond or alkyl, 5-10C aryl, -Q-; -NR -, -CO-NR -, -NR -CO-, -NR -C(Q)-NR -, -O-C(O)-,-C(O)-O-, -C(Q)-, -S(O)n, -S(O)n-NR , -NR -S(O)n, -CR =CR -, -C IDENTICAL C-, -NR -N=CR -, -N=CR -, -R C=N- or -CH(OH)- (all optionally mono- or disubstituted by alkyl, -CR -CR - or 5-6C aryl), e.g. Me-Ph-CH=CH- or Et-O-, and D is optionally linked to B via one of these substituents; E = template of a fibrinogen receptor antagonist; G = -CR R -(CR R )p-(CH2)p-R ; R , R = H; 1-10C alkyl (optionally substituted by 1 or more F); cycloalkyl; cycloalkyl-alkyl; aryl; aryl-alkyl; R OC(O)R ; R R NC(O)R ; or R C(O)R ; R -R = H; F; OH; alkyl; cycloalkyl; cycloalkyl-alkyl; R QR ; R CO2R ; R OC(O)R ; R -5-14C aryl-R ; R N(R )R ; R R NR ; R N(R )CO(O)R ; R S(O)n-N(R )R ; R QC(O)N(R )R ; R C(O)N(R )R ; R N(R )C(O)N(R )R ; R N(R )S(O)N(R )R ; R S(O)nR ; R C(O)R ; R N(R )C(O)R ; or R N(R )S(O)nR ; R = H; Alk; cycloalkyl; cycloalkyl-Alk; aryl; or aryl-Alk; Alk = alkyl (optionally substituted by 1 or more F); R = direct bond or alkyl; R = C(Q)R ; S(O)n-NR ; P(O)nR ; or a 4-8 membered saturated or unsaturated heterocycle containing 1-4 N, O and/or S, e.g. tetrazolyl, imidazolyl, pyrazolyl, oxazolyl or thiadiazolyl; R = OH; alkoxy; aryl-alkoxy; aryloxy; alkylcarbonyloxy-(1-4C) alkoxy; aryl-alkylcarbonyloxy-(1-6C) alkoxy; NH2; NH(alkyl); N(alkyl)2; aryl-alkylamino; dialkylaminocarbonylmethoxy; aryl- dialkylaminocarbonylmethoxy; arylamino; or a L- or D-aminoacid; R -R = H; 1-10C alkyl (optionally substituted by one or more F); 3-12C cycloalkyl; 3-12C cycloalkyl-alkyl; aryl; aryl-alkyl; NH2; R ONR ; R OR ; R OC(O)R ; R R NR ; R -aryl-R ; HO-alkyl-N(R )R ; R N(R )C(O)R ; R C(O)N(R )R ; R C(O)R ; R R N-C(=NR )-NR ; R R N-C(=NR ); or Q; or two adjacent R R substituents form -O-(CH2)n-O- or -OC(CH3)2O-; p, q = 0 or 1; alkyl moieties have 1-8C, cycloalkyl moieties 3-14C and aryl moieties 5-14C unless specified otherwise; compounds where E is a 6-membered aromatic ring (optionally containing 1-4 N and/or 1-4 substituents ) and the compound 4-methyl-3-oxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine are excluded.

    CYCLOALKYL DERIVATIVES, PROCESS OF THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEREOF
    45.
    发明专利
    CYCLOALKYL DERIVATIVES, PROCESS OF THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEREOF 未知

    公开(公告)号：CZ234397A3

    公开(公告)日：1998-03-18

    申请号：CZ234397

    申请日：1997-07-22

    Applicant: HOECHST AG ,  GENENTECH INC

    Inventor： WEHNER VOLKMAR DR ,  KNOLLE JOCHEN DR ,  STILZ HANS ULRICH DR ,  GOURVEST JEAN FRANCOIS DR ,  CARNIATO DENIS DR ,  GADEK THOMAS RICHARD DR ,  MCDOWELL ROBERT DR ,  PITTI ROBERT MAURICE ,  BODARY SARAH CATHERINE DR

    IPC: C07C229/04 ,  A61K31/155 ,  A61K31/197 ,  A61K31/27 ,  A61K31/415 ,  A61K31/445 ,  A61K31/505 ,  A61P9/00 ,  A61P13/02 ,  A61P15/00 ,  A61P19/00 ,  A61P19/08 ,  A61P19/10 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07C251/02 ,  C07C279/20 ,  C07C333/00 ,  C07D233/48 ,  C07D233/54 ,  C07D239/16 ,  C07D239/72 ,  C07D239/84 ,  C07D257/04 ,  C07D211/18 ,  A61K31/19

    Abstract: Substituted cycloalkanes of formula R YABDEF'C(R )(R )(CH2)qR (I) and their salts are new. A = bond, 1-8C alkanediyl, NR C(Q)NR , NR C(Q)Q, NR S(O)nNR , NR S(O)nO, NR S(O)n, 3-12C cycloalkanediyl, C IDENTICAL C, NR CO, CONR , 5-14C arylene-CONR , O, S(O)n, 5-14C arylene, CO, 5-14C arylene-CO, NR , SO2NR , CO2, CR =CR or 5-14C arylene-S(O)n (all optionally mono- or disubstituted by 1-8C alkanediyl (sic), e.g. -1-8C alkanediyl-CONR -1-8C alkanediyl, 1-8C alkanediyl-CONR or CONR -1-8C alkanediyl); Q = O or S; B = bond, 1-10C alkanediyl, CR =CR or C IDENTICAL C (all optionally mono- or disubstituted by 1-8C alkanediyl); D, F' = bond, 1-8C alkanediyl, or Q, NR , CONR , NR CO, NR C(Q)NR , OCO, COO, CQ, S(O)n, S(O)2NR , NR S(O)n, CR =CR , C IDENTICAL C or CH(OH) (all optionally mono- or disubstituted by 1-8C alkanediyl); E = 6-membered aromatic group optionally containing 1-4 N atoms and optionally mono- to tetra-substituted by R , R , F, Cl, Br, I, NO2 and OH; Y = bond or NR ; R = NR C(=NR )R , C(=NR )NR R , NR C(=NR )NR R or a 4-10 membered monocyclic or polycyclic aromatic or non-aromatic ring optionally containing 1-4 N, O and/or S atoms and optionally substituted by 1 or more R , R , R and R ; R , R = H, 1-10C alkyl (optionally substituted by 1 or more F), 3-12C cycloalkyl, 3-12C cycloalkyl-1-8C alkanediyl, 5-14C aryl, 5-14C aryl-1-8C alkanediyl, NH2, R N(R )OR , R OR , R COOR , R -5-14C arylene-R , R NR R , R NR -1-8C hydroxyalkyl, R CONR R , R NR C(O)R , R COR , C(=NR )NR R or 1-18C alkylcarbonyloxy-1-6C alkanediyloxycarbonyl; R = R QR , R OCOR , R COOR , R -5-14C arylene-R , R NR R , R NR R , R OCONR R , R NR S(O)nR , R NR COQR , R NR C(O)R , R N(R )C(O)N(R )R , R N(R )S(O)nN(R )R , R S(O)nR , R C(O)R , R CONR R , R S(O)nNR R , Cy or 1-8C alkyl substituted by Cy; Cy = monocyclic or polycyclic, saturated or mono- or poly-unsaturated 10-18C cycloalkyl optionally substituted by 1 or more Z'; Z' = 1-10C alkyl (optionally substituted by 1 or more F), 3-12C cycloalkyl, 3-12C cycloalkyl-1-8C alkanediyl, 5-14C aryl, 5-14C aryl-1-8C alkanediyl, 1-8C alkoxy, 5-14C aryl-1-8C alkanediyloxy, 5-14C aryloxy, 1-8C alkylcarbonyloxy-1-4C alkanediyloxy, NH2, NH(1-8C alkyl), N(1-8C alkyl)2, 5-14C aryl-1-8C alkanediylamino, 5-14C arylamino, =Q, NO2, OH, F, Cl, Br or I; R = H, F, 1-8C alkyl (optionally substituted by 1 or more F), 3-12C cycloalkyl, 3-12C cycloalkyl-1-8C alkanediyl, 5-14C aryl or 5-14C aryl-1-8C alkanediyl; R = Cy or 1-8C alkyl substituted by Cy; R = bond or 1-8C alkanediyl; R = H, 1-8C alkyl (optionally substituted by 1 or more F, or one 3-12C cycloalkyl or 5-14C aryl), 3-12C cycloalkyl or 5-14C aryl; R = C(Q)R , S(O)nR , P(O)(R )n or a 4-8 membered saturated or unsaturated heterocycle containing 1-4 N, O and/or S atoms; R = OH, 1-8C alkoxy(optionally substituted by 5-14C-aryl), 5-14C aryloxy, 1-8C alkylcarbonyloxy-1-4C alkanediyloxy, 5-14C aryl-1-8C alkanediylcarbonyloxy-1-6C alkanediyloxy, NH2, mono- or di- 1-8C alkylamino, 5-14C aryl-1-8C alkanediylamino, 1-8C dialkylaminocarbonylmethyleneoxy, 5-14C aryl-1-8C dialkylaminocarbonylmethyleneoxy, 5-14C arylamino or the residue of a L- or D-amino acid; R -R = H, 1-10C alkyl (optionally substituted by 1 or more F), 3-12C cycloalkyl, 3-12C cycloalkyl-1-8C alkanediyl, 5-14C aryl, 5-14C aryl-1-8C alkanediyl, NH2, R N(R )OR , R OR , R COOR , R NR R , R NR -1-8C hydroxyalkyl, R CONR R , R COR , NR C(=NR )NR R , C(=NR )NR R , R -5-14C arylene-R , R NR COR or Q; n = 1 or 2; q = 0 or 1.

    47.
    发明专利
    未知

    公开(公告)号：DE4408533A1

    公开(公告)日：1995-09-28

    申请号：DE4408533

    申请日：1994-03-14

    Applicant: HOECHST AG

    Inventor： UHLMANN EUGEN DR ,  BREIPOHL GERHARD DR ,  KNOLLE JOCHEN DR

    IPC: C07C231/02 ,  C07C233/36 ,  C07C233/47 ,  C07C237/12 ,  C07D239/46 ,  C07D239/54 ,  C07D473/18 ,  C07D473/34 ,  C07K1/00 ,  C07K1/04 ,  C07K1/113 ,  C07K5/04 ,  C07K14/00 ,  C07K14/485 ,  C07K14/52 ,  C08G69/06 ,  C08G69/10 ,  C07D473/26 ,  C07D239/545 ,  C07D473/40

    Abstract: A process is claimed for preparing peptide nucleic acid (PNA) oligomers of formula (I). Ro=H, 1-18C alkanoyl, 2-19C alkoxycarbonyl, 3-8C cycloalkanoyl (sic), 7-15C aroyl, 3-13C heteroaroyl or a gp. which enhances the intracellular uptake of the oligomer or interacts with a target nucleic acid during hybridisation; A and Q=amino acid residues; k and m=0-20; B=a nucleotide base, opt. in prodrug form; Qo=OH, NH2 or NHR''; R''=1-18C alkyl, 2-18C aminoalkyl or 2-18C hydroxyalkyl; n=1-50. The process comprises: (a) opt. coupling amino acids (Q') to a support of formula L-(Polymer) by solid-phase synthesis to give (Q')m-L-(Polymer), where L=a linking gp. contg. Qo in latent form and Q'=Q with optional side-chain protection; (b) coupling a cpd. of formula (II) to L-(Polymer) or (Q')m-L-(Polymer), where PG=a base-labile protecting gp. and B'=a nucleotide base with a protected exocyclic amino gp.; (c) removing PG; (d) repeating steps (b) and (c) n-1 times; (e) opt. coupling amino acids (A') to the prod. by solid-phase synthesis, where A'=A with optional side-chain protection, and introducing Ro if Ro is other than H; and (f) cleaving the PNA oligomer from the prod. of formula (III) and simultaneously or subsequently deprotecting B', A' and Q'. Also claimed are cpds. (II) and a process for preparing them.

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