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31. 发明专利

DE102009049211A1 Sulfoxide 未知
公开(公告)号：DE102009049211A1
公开(公告)日：2011-04-28
申请号：DE102009049211
申请日：2009-10-13
申请人： MERCK PATENT GMBH
发明人： SCHIEMANN KAI , SCHULTZ MELANIE , STAEHLE WOLFGANG
IPC分类号： C07D249/04 , A61K31/4192 , A61K31/423 , A61K31/496 , A61P35/00 , C07D263/58
摘要： Sulfoxidderivate der Formel Ia bis Im wie beschrieben, sowie ihre pharmazeutisch verwendbaren Salze, Solvate, Enantiomere, Tautomere und Stereoisomere, einschließlich deren Mischungen in allen Verhältnissen zur Behandlung von Tumoren.

32. 发明专利

CA2757368A1 PIPERIDINE AND PIPERAZINE DERIVATIVES AS AUTOTAXIN INHIBITORS 未知
公开(公告)号：CA2757368A1
公开(公告)日：2010-10-14
申请号：CA2757368
申请日：2010-03-03
申请人： MERCK PATENT GMBH
发明人： SCHIEMANN KAI , SCHULTZ MELANIE , STAEHLE WOLFGANG
IPC分类号： C07D211/30 , A61K31/4427 , A61K31/4523 , A61P9/00 , A61P25/28 , A61P27/02 , A61P29/00 , A61P35/00 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/10
摘要： The present invention relates to piperidine and pyrazine derivatives according to formulae (Ia), (Ib) and (II) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.

33. 发明专利

DE102008059578A1 未知
公开(公告)号：DE102008059578A1
公开(公告)日：2010-06-10
申请号：DE102008059578
申请日：2008-11-28
申请人： MERCK PATENT GMBH
发明人： STAEHLE WOLFGANG , KOBER INGO , SCHIEMANN KAI , SCHULTZ MELANIE , WIENKE DIRK
IPC分类号： C07D471/04 , A61K31/435
摘要： Compounds of the formula (I), in which R1, R2, R3, R4, R5, D, Z, X, Y, m and p have the meanings indicated in Claim 1, can and be employed for the treatment of tumours.

34. 发明专利

ZA200806320B Diazepinones 未知
公开(公告)号：ZA200806320B
公开(公告)日：2009-12-30
申请号：ZA200806320
申请日：2008-07-21
申请人： MERCK PATENT GMBH
发明人： SCHULTZ MELANIE , BURGDORF LARS THORE , FINSINGER DIRK , BLAUKAT ANDREE , GREINER HARTMUT , ESDAR CHRISTINA
IPC分类号： A61K20100101 , A61P20100101 , C07D20100101
摘要： Fused-ring diazepinone compounds (I) and their salts, derivatives, solvates and stereoisomers (including mixtures in all proportions) are new. Fused-ring diazepinone compounds of formula (I) and their salts, derivatives, solvates and stereoisomers (including mixtures in all proportions) are new. R 1>', R 1>'', R 1>''', R 1>'''', R 3>, R 4>, R 5>', R 5>'' and R 5>''' : hydrogen, A, R 6>, Ar, OR 6>, SR 6>, OAr, SAr, NR 6> 2, NHAr, hal, nitro, cyano, (CH 2) mCOOR 6>, (CH 2) mCOOAr, (CH 2) mCONR 6> 2, (CH 2) mCONAAr, COA, COR 6>, COAr, S(O) mA, S(O) mAr, NACOA, NACOAr, NASO 2A, NASO 2Ar, SO 2NR 6> 2, SO 2NAAr, M(CH 2) nNR 6> 2, M(CH 2)NAR 6>, M(CH 2) nNA 2, M(CH 2) n(R 6>) n, M(CH 2) n-oxopiperazine, -oxomorpholine or -oxopyrrolidine, M(CH 2) nC(CH 3) n(CH 2) nNR 6> 2, M(CH 2) nMR 6> nSO mA, M(CH 2) nMR 6> 2S(O) mMR 6> 2, M(CH 2) nMR 6> 2S(O) mAr, (CH 2) nM(R 6>) nSO mA, (CH 2) nM(R 6>) nSO mMR 6> 2, (CH 2) nM(R 6>) nSO mAr, M(CH 2) nSO mA, M(CH 2) nSO mNR 6> nA, M(CH 2) nSO mAr, (CH 2) nSO mA, (CH 2) nSO mMR 6> n or (CH 2) nSO mAr, where two adjacent R 1> may together form a saturated or unsaturated 5-6 membered carbo- or hetero-cycle, optionally substituted by 1 or 2 M; R 2>' and R 2>'' : R 6>; R 6> : hydrogen, hal, cyano, amino, nitro, SO 2(sic), 1-4C alkyl (optionally with one CH 2 replaced by O or S atom and/or by NH, NA, CONH, NHCO or CH=CH and/or 1-4 H can be replaced by hal and one Me can be replaced by NH 2, NHR 7>, NR 7> 2, nitro or SO 2; R 7> : Me or Et; n : 0-5; m : 0-2; A : 1-14C linear, branched or cyclic alkyl, optionally with one or two CH 2 replaced by O or S and/or by NH, CONH, NHCO, CO or CH=CH and/or 1-7 H can be replaced by hal and 1 or 2 Me replaced by R 6>; Ar : mono- or di-nuclear homo- or hetero-cycle with 1-4 N, O and/or S and 5-10 basic atoms, optionally substituted 1-3 times by carbonyl, hal, A, hydroxy, OA, NH 2, NHA, NA 2, nitro, cyano, OCN, SCN, COOH, COOA, CONH 2, CONHA, CONA 2, NHCOA, NHCONH 2, NHSO 2A, CHO, COA, SO 2NH 2 and/or S(O) mA; hal : fluoro, chloro, bromo or iodo; X : CR 1>, CHR 5>, N, NR 1>, O or S and at least one is CR 1> or CHR 1> and O or S can not be directly linked to N, NR 1>, O or S; Y : NR 4>, O or S; Z : CR 1>, CHR 5>, N, NR 5>, O or S, at least one must be CR 5> or CHR 5> and O or S can not be linked directly to N, NR 5>, O or S; Q : CR 5>, CHR 5> or bond; M : NH, O or S, and ? : indicates a single or double bond. Independent claims are included for the following: (1) method for preparing (I) and (2) kit comprising, in separate packages, (I) and another pharmaceutical. [Image] ACTIVITY : Cytostatic; Antiarteriosclerotic; Antidiabetic; Ophthalmological; Antiinflammatory. MECHANISM OF ACTION : Inhibition of kinases, specifically the serine-threonine kinase PDK1. The compound 3-methyl(1-methylpiperidin-4-yl)amino)-5,10-dihydro-2,4,5,10-tetra-aza-dibenzo[a,d]cyclohepta-11-one has IC50 against PDK1 of 2.3 mu M.

35. 发明专利

CA2704803A1 7-AZAINDOLE DERIVATIVES AS SELECTIVE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS 未知
公开(公告)号：CA2704803A1
公开(公告)日：2009-05-14
申请号：CA2704803
申请日：2008-10-01
申请人： MERCK PATENT GMBH
发明人： CARNIATO DENIS , SCHULTZ MELANIE , ROCHE DIDIER , HALLAKOU-BOZEC SOPHIE
IPC分类号： C07D471/04 , A61K31/33 , A61P25/00
摘要： The present invention relates to 7-azaindole derivatives of formula (I) as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11 ß-HSD-1 ) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.

36. 发明专利

CA2701519A1 PIPERIDINE AND PIPERAZINE DERIVATIVES 未知
公开(公告)号：CA2701519A1
公开(公告)日：2009-04-16
申请号：CA2701519
申请日：2008-09-19
申请人： MERCK PATENT GMBH
发明人： SCHIEMANN KAI , SCHULTZ MELANIE , BLAUKAT ANDREE , KOBER INGO
IPC分类号： C07D209/34 , A61K31/404 , A61K31/416 , A61K31/4184 , A61K31/4192 , A61K31/423 , A61K31/428 , A61K31/433 , A61P35/00 , C07D235/26 , C07D249/18 , C07D263/58 , C07D277/68 , C07D413/12 , C07D417/12 , C07D471/10 , C07D491/10 , C07D498/10
摘要： The invention relates to compounds of formula (I), in which R1, R2, R3, D, G, Q and W are defined as cited in claim (1). Said compounds can be used for treating tumours.

37. 发明专利

AU2006334820A1 Diazepinones 未知
公开(公告)号：AU2006334820A1
公开(公告)日：2007-07-19
申请号：AU2006334820
申请日：2006-11-28
申请人： MERCK PATENT GMBH
发明人： GREINER HARTMUT , ESDAR CHRISTINA , FINSINGER DIRK , BURGDORF LARS THORE , SCHULTZ MELANIE , BLAUKAT ANDREE
IPC分类号： C07D487/04 , A61K31/5517 , A61P35/00
摘要： Fused-ring diazepinone compounds (I) and their salts, derivatives, solvates and stereoisomers (including mixtures in all proportions) are new. Fused-ring diazepinone compounds of formula (I) and their salts, derivatives, solvates and stereoisomers (including mixtures in all proportions) are new. R 1>', R 1>'', R 1>''', R 1>'''', R 3>, R 4>, R 5>', R 5>'' and R 5>''' : hydrogen, A, R 6>, Ar, OR 6>, SR 6>, OAr, SAr, NR 6> 2, NHAr, hal, nitro, cyano, (CH 2) mCOOR 6>, (CH 2) mCOOAr, (CH 2) mCONR 6> 2, (CH 2) mCONAAr, COA, COR 6>, COAr, S(O) mA, S(O) mAr, NACOA, NACOAr, NASO 2A, NASO 2Ar, SO 2NR 6> 2, SO 2NAAr, M(CH 2) nNR 6> 2, M(CH 2)NAR 6>, M(CH 2) nNA 2, M(CH 2) n(R 6>) n, M(CH 2) n-oxopiperazine, -oxomorpholine or -oxopyrrolidine, M(CH 2) nC(CH 3) n(CH 2) nNR 6> 2, M(CH 2) nMR 6> nSO mA, M(CH 2) nMR 6> 2S(O) mMR 6> 2, M(CH 2) nMR 6> 2S(O) mAr, (CH 2) nM(R 6>) nSO mA, (CH 2) nM(R 6>) nSO mMR 6> 2, (CH 2) nM(R 6>) nSO mAr, M(CH 2) nSO mA, M(CH 2) nSO mNR 6> nA, M(CH 2) nSO mAr, (CH 2) nSO mA, (CH 2) nSO mMR 6> n or (CH 2) nSO mAr, where two adjacent R 1> may together form a saturated or unsaturated 5-6 membered carbo- or hetero-cycle, optionally substituted by 1 or 2 M; R 2>' and R 2>'' : R 6>; R 6> : hydrogen, hal, cyano, amino, nitro, SO 2(sic), 1-4C alkyl (optionally with one CH 2 replaced by O or S atom and/or by NH, NA, CONH, NHCO or CH=CH and/or 1-4 H can be replaced by hal and one Me can be replaced by NH 2, NHR 7>, NR 7> 2, nitro or SO 2; R 7> : Me or Et; n : 0-5; m : 0-2; A : 1-14C linear, branched or cyclic alkyl, optionally with one or two CH 2 replaced by O or S and/or by NH, CONH, NHCO, CO or CH=CH and/or 1-7 H can be replaced by hal and 1 or 2 Me replaced by R 6>; Ar : mono- or di-nuclear homo- or hetero-cycle with 1-4 N, O and/or S and 5-10 basic atoms, optionally substituted 1-3 times by carbonyl, hal, A, hydroxy, OA, NH 2, NHA, NA 2, nitro, cyano, OCN, SCN, COOH, COOA, CONH 2, CONHA, CONA 2, NHCOA, NHCONH 2, NHSO 2A, CHO, COA, SO 2NH 2 and/or S(O) mA; hal : fluoro, chloro, bromo or iodo; X : CR 1>, CHR 5>, N, NR 1>, O or S and at least one is CR 1> or CHR 1> and O or S can not be directly linked to N, NR 1>, O or S; Y : NR 4>, O or S; Z : CR 1>, CHR 5>, N, NR 5>, O or S, at least one must be CR 5> or CHR 5> and O or S can not be linked directly to N, NR 5>, O or S; Q : CR 5>, CHR 5> or bond; M : NH, O or S, and ? : indicates a single or double bond. Independent claims are included for the following: (1) method for preparing (I) and (2) kit comprising, in separate packages, (I) and another pharmaceutical. [Image] ACTIVITY : Cytostatic; Antiarteriosclerotic; Antidiabetic; Ophthalmological; Antiinflammatory. MECHANISM OF ACTION : Inhibition of kinases, specifically the serine-threonine kinase PDK1. The compound 3-methyl(1-methylpiperidin-4-yl)amino)-5,10-dihydro-2,4,5,10-tetra-aza-dibenzo[a,d]cyclohepta-11-one has IC50 against PDK1 of 2.3 mu M.

38. 发明专利

CA2630203A1 3, 6-DIHYDRO-2-OXO-6H-(1,3,4)THIADIAZINE DERIVATIVES 未知
公开(公告)号：CA2630203A1
公开(公告)日：2007-05-24
申请号：CA2630203
申请日：2006-10-25
申请人： MERCK PATENT GMBH
发明人： SCHADT OLIVER , BLAUKAT ANDREE , DORSCH DIETER , SCHULTZ MELANIE
IPC分类号： C07D285/18 , A61K31/54 , A61K31/541 , A61P35/00 , C07D417/12
摘要： The invention relates to compounds of formula (I), in which R1, R2, Q and B are defined as cited in claim 1. Said compounds are inhibitors of tyrosine kinases, in particular of Met kinase, and can be used, among other things, for treating tumours.

39. 发明专利

ES2880623T3 Derivados de piperidina y piperazina como inhibidores de autotaxina 未知
公开(公告)号：ES2880623T3
公开(公告)日：2021-11-25
申请号：ES13002080
申请日：2010-03-03
申请人： MERCK PATENT GMBH
发明人： SCHIEMANN KAI , SCHULTZ MELANIE , STAEHLE WOLFGANG
IPC分类号： A61K31/4427 , A61K31/4523
摘要： Compuesto según la fórmula (Ia) **(Ver fórmula)** donde: W1, W2 juntos forman independientemente «-N=N-, -C(O)-O-, -C(O)-S-, -C(O)-N(R5)-, -C(S)-N(R5a)-, -N=C[N(R8)(R9)]-»; Y1 se selecciona independientemente a partir del grupo compuesto por «-C(O)-, -N(R10)-C(O)-, -C(O)-N(R11)-»; Y2 se selecciona independientemente a partir del grupo compuesto por «-C(R12)(R13)-, -O-, -N(R14)-, -C(O)-, -C(O)-NH-, enlace sencillo»; Y3 se selecciona independientemente a partir del grupo compuesto por «-O-, -C(O)-, enlace sencillo»; Z1 se selecciona independientemente a partir del grupo compuesto por «O»; L se selecciona independientemente a partir del grupo compuesto por: **(Ver fórmula)** B se selecciona independientemente a partir del grupo compuesto por «heterociclilo, arilo, heteroarilo», donde el «heterociclilo, arilo, heteroarilo» puede estar sustituido independientemente con uno o más sustituyentes idénticos o diferentes seleccionados a partir del grupo compuesto por: (i) «hidrógeno, alquilo, alquilo (C9-C30), cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, halógeno, -F, -Cl, -Br, -I, -CN, -CF3, -SF3, -N3, -NH2, -NHX1, -NX2X3, -NO2, -OH, =O, -OCF3, -SCF3, -OCHF2, -SCHF2, -SH, -O-SO3H, -OP(O)(OH)2, -CHO, -COOH, -C(O)NH2, -SO3H, -P(O)(OH)2, -C(O)-X4, -C(O)O-X5, -C(O)NH-X6, -C(O)NX7X8, -O-X9, -O(-X10-O)a-H (a = 1, 2, 3, 4, 5), -O(-X11-O)b-X12 (b = 1, 2, 3, 4, 5), -OC(O)-X13, -OC(O)-O-X14, -OC(O)-NHX15, -O-C(O)-NX16X17, -OP(O)(OX18)(OX19), -OSi(X20)(X21)(X22), -OS(O2)-X23, -NHC(O)-NH2, -NHC(O)-X24, -NX25C(O)-X26, -NH-C(O)-O-X27, -NH-C(O)-NH-X28, -NH-C(O)-NX29X30, -NX31-C(O)-O-X32, -NX33-C(O)-NH-X34, -NX35-C(O)-NX36X37, -NHS(O2)-X38, -NX39S(O2)-X40, -S-X41, -S(O)-X42, -S(O2)-X43, -S(O2)NH-X44, -S(O2)NX45X46, -S(O2)O-X47, -P(O)(OX48)(OX49), -Si(X50)(X51)(X52), -C(NH)-NH2, -C(NX53)-NH2, -C(NH)-NHX54, -C(NH)-NX55X56, -C(NX57)-NHX58, -C(NX59)-NX60X61, -NH-C(O)-NH-O-X62, -NH-C(O)-NX63-O-X64, -NX65-C(O)-NX66-O-X67, -N(-C(O)-NH-O-X68)2, -N(-C(O)-NX69-O-X70)2, -N(-C(O)-NH-O-X71)(-C(O)-NX72-O-X73), -C(S)-X74, -C(S)-O-X75, -C(S)-NH-X76, -C(S)-NX77X78, -C(O)-NH-O-X79, -C(O)-NX80-O-X81, -C(S)-NH-O-X82, -C(S)-NX83-O-X84, -C(O)-NH-NH-X85, -C(O)-NH-NX86X87, -C(O)-NX88-NX89X90, -C(S)-NH-NH-X91, -C(S)-NH-NX92X93, -C(S)-NX94-NX95X96, -C(O)-C(O)-O-X97, -C(O)-C(O)-NH2, -C(O)-C(O)-NHX98, -C(O)-C(O)-NX99X100, -C(S)-C(O)-O-X101, -C(O)-C(S)-O-X102, -C(S)-C(S)-O-X103, -C(S)-C(O)-NH2, -C(S)-C(O)-NHX104, -C(S)-C(O)-NX105X106, -C(S)-C(S)-NH2, -C(S)-C(S)-NHX107, -C(S)-C(S)-NX108X109, -C(O)-C(S)-NH2, -C(O)-C(S)-NHX110, -C(O)-C(S)-NX111X112»; donde X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12, X13, X14, X15, X16, X17, X18, X19, X20, X21, X22, X23, X24, X25, X26, X27, X28, X29, X30, X31, X32, X33, X34, X35, X36, X37, X38, X39, X40, X41, X42, X43, X44, X45, X46, X47, X48, X49, X50, X51, X52, X53, X54, X55, X56, X57, X58, X59, X60, X61, X62, X63, X64, X65, X66, X67, X68, X69, X70, X71, X72, X73, X74, X75, X76, X77, X78, X79, X80, X81, X82, X83, X84, X85, X86, X87, X88, X89, X90, X91, X92, X93, X94, X95, X96, X97, X98, X99, X100, X101, X102, X103, X104, X105, X106, X107, X108, X109, X110, X111 y X112 se seleccionan independientemente entre sí a partir del grupo compuesto por: «alquilo, alquilo (C9-C30), cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, arilalquilo, heteroarilo, heteroaril- alquilo» y donde alternativamente X7, X8 y/o X16, X17 y/o X29, X30 y/o X36, X37 y/o X45, X46 y/o X55, X56 y/o X60, X61 y/o X77, X78 y/o X86, X87 y/o X89, X90 y/o X92, X93 y/o X95, X96 y/o X99, X100 y/o X105, X106 y/o X108, X109 y/o X111, X112, respectivamente, juntos también pueden formar un «heterociclilo»; donde, opcionalmente, los sustituyentes anteriores del grupo de sustituyentes (i) pueden estar sustitui- dos a su vez independientemente entre sí con uno o más sustituyentes V idénticos o diferentes; R1, R2, R3, R4, R5, R5a, R8, R9, R10, R11, R12, R13 y R14 se seleccionan independientemente entre sí a partir del grupo compuesto por: «V»; V se selecciona independientemente a partir del grupo compuesto por: (i) «hidrógeno, alquilo, alquilo (C9-C30), cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, halógeno, -F, -Cl, -Br, -I, -CN, -CF3, -SF3, -N3, -NH2, -NHA1, -NA2A3, -NO2, -OH, =O, -OCF3, -SCF3, -OCHF2, -SCHF2, -SH, -O-SO3H, -OP(O)(OH)2, -CHO, -COOH, -C(O)NH2, -SO3H, -P(O )(OH)2, -C(O)-A4, -C(O)O-A5, -C(O)NH-A6, -C(O)NA7A8, -O-A9, -O(-A10-O)a-H (a = 1, 2, 3, 4, 5), -O(-A11-O)b-A12 (b = 1, 2, 3, 4, 5), -OC(O)-A13, -OC(O)-O-A14, -OC(O)-NHA15, -O-C(O)-NA16A17, -OP(O)(OA18)(OA19), -OSi(A20)(A21)(A22), -OS(O2)-A23, -NHC(O)-NH2, -NHC(O)-A24, -NA25C(O)-A26, -NH-C(O)-O-A27, -NH-C(O)-NH-A28, -NH-C(O)-NA29A30, -NA31-C(O)-O-A32, -NA33-C(O)-NH-A34, -NA35-C(O)-NA36A37, -NHS(O2)-A38, -NA39S(O2)-A40, -S-A41, -S(O)-A42, -S(O2)-A43, -S(O2)NH-A44, -S(O2)NA45A46, -S(O2)O-A47, -P(O)(OA48)(OA49), -Si(A50)(A51)(A52), -C(NH)-NH2, -C(NA53)-NH2, -C(NH)-NHA54, -C(NH)-NA55A56, -C(NA57)-NHA58, -C(NA59)-NA60A61, -NH-C(O)-NH-O-A62, -NH-C(O)-NA63-O-A64, -NA65-C(O)-NA66-O-A67, -N(-C(O)-NH-O-A68)2, -N(-C(O)-NA69-O-A70)2, -N(-C(O)-NH-O-A71)(-C(O)-NA72-O-A73), -C(S)-A74, -C(S)-O-A75, -C(S)-NH-A76, -C(S)-NA77A78, -C(O)-NH-O-A79, -C(O)-NA80-O-A81, -C(S)-NH-O-A82, -C(S)-NA83-O-A84, -C(O)-NH-NH-A85, -C(O)-NH-NA86A87, -C(O)-NA88-NA89A90, -C(S)-NH-NH-A91, -C(S)-NH-NA92A93, -C(S)-NA94-NA95A96, -C(O)-C(O)-O-A97, -C(O)-C(O)-NH2, -C(O)-C(O)-NHA98, -C(O)-C(O)-NA99A100, -C(S)-C(O)-O-A101, -C(O)-C(S)-O-A102, -C(S)-C(S)-O-A 103, -C(S)-C(O)-NH2, -C(S)-C(O)-NHA104, -C(S)-C(O)-NA105A106, -C(S)-C(S)-NH2, -C(S)-C(S)-NHA 107, -C(S)-C(S)-NA108A109, -C(O)-C(S)-NH2, -C(O)-C(S)-NHA110, -C(O)-C(S)-NA111A112»; donde A1, A2, A3, A4, A5, A6, A7, A8, A9, A10, A11, A12, A13, A14, A15, A16, A17, A18, A19, A20, A21, A22, A23, A24, A25, A26, A27, A28, A29, A30, A31, A32, A33, A34, A35, A36, A37, A38, A39, A40, A41, A42, A43, A44, A45, A46, A47, A48, A49, A50, A51, A52, A53, A54, A55, A56, A57, A58, A59, A60, A61, A62, A63, A64, A65, A66, A67, A68, A69, A70, A71, A72, A73, A74, A75, A76, A77, A78, A79, A80, A81, A82, A83, A84, A85, A86, A87, A88, A89, A90, A91, A92, A93, A94, A95, A96, A97, A98, A99, A100, A101, A102, A103, A104, A105, A106, A107, A108, A109, A110, A111 y A112 se seleccionan independientemente entre sí a partir del grupo compuesto por: «alquilo, alquilo (C9-C30), cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, arilalquilo, heteroarilo, heteroaril- alquilo» y donde alternativamente A7, A8 y/o A16, A17 y/o A29, A30 y/o A36, A37 y/o A45, A46 y/o A55, A56 y/o A60, A61 y/o A77, A78 y/o A86, A87 y/o A89, A90 y/o A92, A93 y/o A95, A96 y/o A99, A100 y/o A105, A106 y/o A108, A109 y/o A111, A112, respectivamente, juntos también pueden formar un «heterociclilo»; donde, opcionalmente, los sustituyentes anteriores del grupo de sustituyentes (i) pueden estar sustitui- dos a su vez independientemente entre sí con uno o más sustituyentes V idénticos o diferentes; m es 0; n es independientemente 0, 1, 2 o 3; o es 0; y las sales, solvatos y estereoisómeros de los mismos fisiológicamente aceptables, incluidas sus mezclas en todas las proporciones.

40. 发明专利

CA2757368C PIPERIDINE AND PIPERAZINE DERIVATIVES AS AUTOTAXIN INHIBITORS 未知
公开(公告)号：CA2757368C
公开(公告)日：2019-03-12
申请号：CA2757368
申请日：2010-03-03
申请人： MERCK PATENT GMBH
发明人： SCHIEMANN KAI , SCHULTZ MELANIE , STAEHLE WOLFGANG
IPC分类号： C07D211/30 , A61K31/4427 , A61K31/4523 , A61P9/00 , A61P25/28 , A61P27/02 , A61P29/00 , A61P35/00 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/10
摘要： The present invention relates to piperidine and pyrazine derivatives according to formulae (Ia), (Ib) and (II) as autotaxin in-hibitors and the use of such com-pounds for the treatment and/or pro-phylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propa-gated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.

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