公开(公告)号：JPH10114751A

公开(公告)日：1998-05-06

申请号：JP19715597

申请日：1997-07-23

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 ,  MAC DOWELL ROBERT DR ,  PITTI ROBERT MAURICE ,  BODARY SARAH CATHERINE DR

IPC: C07C229/04 ,  A61K31/19 ,  A61K31/197 ,  A61K31/415 ,  A61K31/445 ,  A61P3/00 ,  A61P9/00 ,  A61P13/02 ,  A61P15/00 ,  A61P19/08 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07C251/02 ,  C07D211/18 ,  C07D233/52 ,  C07D233/54 ,  C07D233/66 ,  C07D257/04

Abstract: PROBLEM TO BE SOLVED: To obtain the subject novel compound which is useful as an inhibitor of bone resorption by osteoclast cells, a tumor growth and metastasis inhibitor, an antiinflammatory agent, a vitronectin receptor antagonist and the like. SOLUTION: This novel compound is one of stereisomers or their mixture represented by the formula; R -Y-A-B-D-E-F-G [A is a single bond, a 1-8C alkanediyl, a 5-14C arylene; B is a single bond, a 1-8C alkanediyl; D is a single bond, a 1-8C alkanediyl, -O-, -OC(O)-; E is a 6-membered aromatic ring which may contains 1-4N atoms; F is same as D; G is a group of formula II (R -R are independently H, F, OH or the like; R is a 4-8-membered heterocyclic ring; p and q are independently 0, 1); Y is a single bond and the like; R is a 4-10-membered monocyclic or polycyclic aromatic group]. Typically, the compound of the formula is cited.

公开(公告)号：DE19629816A1

公开(公告)日：1998-01-29

申请号：DE19629816

申请日：1996-07-24

Applicant: HOECHST AG

Inventor： WEHNER VOLKMAR DR ,  KNOLLE JOCHEN DR ,  STILZ HANS ULRICH DR ,  GOURVEST JEAN-FRANCOIS DR ,  CARNIATO DENIS DR ,  GADEK THOMAS RICHARD DR ,  MAC DOWELL 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 ,  C07C279/22 ,  C07C277/08 ,  C07B41/08 ,  C07B47/00 ,  A61K31/325 ,  C07B51/00 ,  C07D401/12 ,  C07D227/00 ,  C07D247/02 ,  C07D471/04 ,  A61K31/33

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.

公开(公告)号：DE19629817A1

公开(公告)日：1998-01-29

申请号：DE19629817

申请日：1996-07-24

Applicant: HOECHST AG

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

IPC: C07C229/04 ,  A61K31/19 ,  A61K31/197 ,  A61K31/415 ,  A61K31/445 ,  A61P3/00 ,  A61P9/00 ,  A61P13/02 ,  A61P15/00 ,  A61P19/08 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07C251/02 ,  C07D211/18 ,  C07D233/52 ,  C07D233/54 ,  C07D233/66 ,  C07D257/04 ,  C07D471/04 ,  C07D401/14 ,  C07D247/02 ,  C07D227/00 ,  A61K31/33

Abstract: Aromatic compounds of formula R1YABDEF'CR R R )p(CH2)q-R (I) and their salts are new. A = bond, Z, 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 C(O), C(O)NR , 5-14C arylene-C(O)NR , 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, i.e. e.g. 1-8C alkanediyl-CONR -1-8C alkanediyl, 1-8C alkanediyl-CONR or CONR -1-8C alkanediyl); Z = NR -N=CR , N=CR or CR =N; Q = O or S; B = direct bond, 1-8C alkanediyl, CR =CR or C IDENTICAL C (all optionally mono- or disubstituted by 1-8C alkanediyl) or a divalent residue of a 5- or 6-membered saturated or unsaturated ring containing 1 or 2 N atoms (optionally mono- or disubstituted by 1-6C alkyl or Q); D, F' = bond, 1-8C alkanediyl, or Z, Q, NR , CONR , NR CO, NR C(Q)NR , OC(O), C(O)O, CQ, S(O), S(O)2, S(O)2NR , NR S(O), NR S(O)2, 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 (optionally mono- to tetra-substituted by R , R , F, Cl, Br, I, NO2 and OH); Y = bond or NR ; R = NR CR ), 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 (optionally substituted by 1 or more R -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 NR OR , R OR , R COOR , R -5-14C arylene-R , R N(R )2, R NR 1-8C alkanediyl-OH, R CON(R )2, R NR C(O)R , R C(O)R , C(=NR )N(R )2 or (1-18C)alkylcarbonyloxy(1-6)alkanediyloxycarbonyl; R -R = H, F, OH, 1-8C alkyl, 3-12C cycloalkyl, 3-12C-cycloalkyl(1-8C)alkanediyl, R QR , R OCOR , R COOR , R -5-14C arylene-R , etc.; R = H, 1-8C alkyl (optionally substituted by 1 or more F), 3-12C cycloalkyl, 1-8C-alkanediyl-3-12C cycloalkyl, 5-14C aryl or 1-8C alkanediyl-5-14C aryl; R = direct bond or 1-8C alkanediyl; 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, 1-8C alkanediyl-5-14C-aryl, 5-14C aryloxy, 1-4C alkanediyloxycarbonyl1-8C alkylcarbonyloxy, 5-14C aryl-1-8C alkanediylcarbonyloxy-1-6C alkanediyloxy, NH2, NH(1-8C alkyl), N(1-8C alkyl)2, 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, etc.; n = 1 or 2; p, q = 0 or 1; provided that at least 1 of A, D and F' = Z.