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31. 发明专利

GB2377933A Succinic acid derivatives useful as integrin antagonists 未知
公开(公告)号：GB2377933A
公开(公告)日：2003-01-29
申请号：GB0116577
申请日：2001-07-06
申请人： BAYER AG
发明人： ROELLE THOMAS , LEHMANN THOMAS , ALBERS MARKUS , HESLER GERHARD , MUELLER GERHARD , FISCHER RUEDIGER , TAJIMI MASAOMI , ZIEGELBAUER KARL , BACON KEVIN , HASEGAWA HARUKI , OKIGAMI HIROMI
IPC分类号： A61P9/10 , A61P11/06 , A61P29/00 , A61P37/00 , C07C233/55 , C07C275/40 , C07C275/42 , A61K31/17
摘要： The present invention relates to compounds of the general formula (I), wherein the symbols are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of pharmaceutical compositions for the treatment of e.g. inflammatory diseases. Intermediates of the general formula (I') are also claimed.

32. 发明专利

AU1592602A Aliphatic, cyclic amino carboxylic acids as integrin antagonists 未知
公开(公告)号：AU1592602A
公开(公告)日：2002-04-22
申请号：AU1592602
申请日：2001-10-08
申请人： BAYER AG
发明人： ROLLE THOMAS , LEHMANN THOMAS , ALBERS MARKUS , HESSLER GERHARD , MULLER GERHARD , TAJIMI MASAOMI , ZIEGELBAUER KARL , BACON KEVIN , HASEGAWA HARUKI , OKIGAMI HIROMI
IPC分类号： A61P3/10 , A61P9/10 , A61P11/06 , A61P11/08 , A61P19/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07C275/40 , C07C323/60 , C07C275/00

33. 发明专利

CA2424951A1 BETA-AMINO ACID DERIVATIVES AS INTEGRIN RECEPTOR ANTAGONISTS 未知
公开(公告)号：CA2424951A1
公开(公告)日：2002-04-18
申请号：CA2424951
申请日：2001-10-08
申请人： BAYER AG
发明人： BACON KEVIN , ZIEGELBAUER KARL , MULLER GERHARD , TAJIMI MASAOMI , FISCHER RUDIGER , LEHMANN THOMAS , ROLLE THOMAS , ALBERS MARKUS , OKIGAMI HIROMI , HASEGAWA HARUKI , HEBLER GERHARD
IPC分类号： A61P1/04 , A61K31/192 , A61P3/10 , A61P9/10 , A61P11/00 , A61P11/06 , A61P25/00 , A61P29/00 , A61P37/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07C235/84 , C07C273/18 , C07C275/40 , C07D277/30
摘要： The present invention relates to compounds of the general formula (I), processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of pharmaceutical compositions for t he treatment of inflammatory diseases.

34. 发明专利

DE10006453A1 New piperidylcarboxylic acid derivatives, are integrin antagonists useful for treating inflammatory, autoimmune or immunological diseases, e.g. atherosclerosis, asthma, diabetes, rheumatoid arthritis or transplant rejection 未知
公开(公告)号：DE10006453A1
公开(公告)日：2001-08-16
申请号：DE10006453
申请日：2000-02-14
申请人： BAYER AG
发明人： FISCHER RUEDIGER , LEHMANN THOMAS , MUELLER GERHARD , HESLER GERHARD , TAJIMI MASAOMI , ZIEGELBAUER KARL , OKIGAMI HIROMI , HASEGAWA HARUKI , KOMURA HIROSHI , MIZOGUCHI MANAMI
IPC分类号： A61P37/08 , C07D207/16 , C07D211/34 , C07D211/60 , C07D211/62 , C07D263/58 , C07D403/04 , C07D413/12 , C07D487/04 , C07D211/32 , A61K31/5355 , C07K14/78
摘要： Piperidylcarboxylic acid derivatives and analogs (I) are new. Piperidylcarboxylic acid derivatives and analogs of formula (I) and their salts are new: [Image] R1 + R2group completing a 4-8 membered (un)saturated ring (optionally containing 1 N and/or 1 or 2 of O and S as heteratom(s)), optionally fused with a 4-8 membered (un)saturated or aromatic ring (also optionally containing 1 N and/or 1 or 2 of O and S as heteratom(s)), both rings being optionally substituted (os) by 1 or 2 -R11-R12-R13-Z groups and/or by 1 or 2 of R18, halo, NO2, NH2, CN or oxo; R11irect bond, O, S, NR14, alkyl, alkenyl, alkynyl, aryl, cycloalkyl or Het1 (all os by 1 or 2 R14); R14H, alkyl, alkenyl, alkynyl, aryl, cycloalkyl or Het1 (all os by 1-3 of T, OT, Ph, Cy, halo, NO2, CN or oxo); Het14-9 membered (un)saturated heterocycle containing 1-3 of O, S and N as heteroatom(s); T : 1-4C alkyl; Cy : 3-6C cycloalkyl; R12direct bond, O, S, NR14, alkyl, alkenyl or alkynyl (all os by alkyl, alkenyl, alkynyl or R14); R13direct bond, alkyl, alkenyl or alkynyl (all os by 1 or 2 R14); Z : H, COORz1, CONRz2Rz3, SO2NRz2Rz3, S(O)ORz1, SO2ORz1, P(O)Rz1(ORz3), P(O)(ORz1)(ORz3) or 5-tetrazolyl; Rz2C(O)Rz4, SO2Rz4, T, 2-6C alkenyl, 2-6C alkynyl, Cy or aryl (all os by 1-3 of halo, NO2, CN or oxo); Rz4T, 2-6C alkenyl, 2-6C alkynyl, Cy or aryl (all os by 1-3 of halo, NO2, CN or oxo); Rz1, Rz3H, T, 2-6C alkenyl, 2-6C alkynyl, Cy or aryl (all os by 1-3 of T, OT, halo, NO2 or CN); R18T, OT, Ph or Cy (all os by 1-5 halo); R3 -R5H, alkyl, alkenyl, alkynyl, aryl, cycloalkyl or Het2 (all os by 1-3 R31 and/or by one of cycloalkyl, aryl, 4-9C heteroaryl or Het2 (itself os by 1-3 R31)); or R3 + R4 or R4 + R5group completing a 4-7 membered (un)saturated ring (optionally containing 1-3 of N, O and S as heteratom(s)), os by 1 or 2 of T, Ph, CH2Ph, cycloalkyl, halo, NO2, CN or oxo and optionally fused with a 3-7 membered carbocyclic or heterocyclic, (un)saturated or aromatic ring; Het24-9 membered (un)saturated heterocycle containing 1 or 2 of O, S and N as heteroatom(s); R31T, CF3, OCF3, OR32, SR32, NR33, R34, C(O)R32, S(O)R32, SO2R32, COOR32, OC(O)R32, CONR33R34, NR32COR32, SO2NR33R34, NR32SO2R32, NR32CONR33R34, NR32COOR32, OCONR33R34, halo, CN, NO2 or oxo; R32H, T, Cy or aryl (all os by one of T, OT, Ph, Cy, halo); R33, R34H, T, Cy or aryl; or NR33R344-7 membered ring (optionally containing 1 or 2 additional O, S or N heteroatom(s) and/or 1 or 2 double bonds); R6phenyl or 5- or 6-membered heteroaryl (containing 1-3 of O, N and S as heteroatom(s)), both optionally fused with a 5-8 membered (un)saturated ring (optionally containing 1-3 of O, N and S as heteroatom(s)) and os by 1 or 2 of alkyl, alkenyl, alkynyl, aryl or cycloalkyl (themselves os by 1-3 R61); and X : bond, CRx1Rx2, O or NRx3; or X + R6group completing a 4-7 membered ring (optionally containing 1 or 2 additional O, S or N heteroatom(s) and/or 1 or 2 double bonds), os by 1 or 2 of T, Ph, CH2Ph, cycloalkyl, OT, NH2, halo, NO2, CN or oxo; R61T, CF3, OCF3, OR62, SR62, NR62R63, C(O)R62, S(O)R62, SO2R62, COOR62, OC(O)R62, CONR62R63, NR63COR62, SO2NR62R63, NR63SO2R62, NR63CONR62R64, NR63COOR62, OCONR62R63, halo, CN, NO2 or oxo; R62H, T, Cy, aryl or Het1 (all os by 1-3 R65); R65T, CF3, OCF3, OR66, SR66 or NR67R68; R66H, T, Cy or aryl (all os by 1-3 of T, OT, Ph, CH2Ph, Cy, OH, NH2, halo, NO2, CN, CF3 or OCF3); R67, R68H, T, Cy, aryl or Het2 (all os as for R66); or NR67R684-7 membered ring (optionally containing 1 or 2 additional O, S or N heteroatom(s) and/or 1 or 2 double bonds), os by 1 or 2 of T, OT, Ph, CH2Ph, Cy, OH, NH2, halo, NO2, CN, CF3, OCF3 or oxo; R63, R64H, bond, T, Cy, aryl or Het2 (all os by 1-3 of T, CF3, OCF3, OR66, SR66 or NR67R68); or NR62R63 or NR63R644-7 membered ring (optionally containing 1 or 2 additional O, S or N heteroatom(s) and/or 1 or 2 double bonds), os by 1 or 2 of T, OT, Ph, CH2Ph, Cy, OH, NH2, halo, NO2, CN, CF3, OCF3 or oxo and/or os by 1-3 R65; A : C(O), C(O)-C(O), SO, SO2, P(O)Ra1, 2- or 4-pyrimidinyl, 2-pyridyl, 2- or 4-imidazolyl, 2-benzimidazolyl or phenylene; or 2-thiazolyl, 2-oxazolyl, 3-pyrazolyl, 3-isothiazolyl, 3-isoxazolyl, 4H-1,2,4-triazol-3-yl, 1,3,4-thiadiazol-2-yl, 1,3,4-oxadiazol-2-yl, 1,2,4-thiadiazol-5-yl, 1,2,4-oxadiazol-3-yl, 1,2,4-thiadiazol-3-yl, 1,2,4-oxadiazol-3-yl, 4,5-dihydro-thiazol-2-yl, 4,5-dihydro-imidazol-2-yl, benzothiazol-2-yl, benzoxazol-2-yl, pyrazin-2-yl or pyridazin-3-yl (where the bonding position indicated is the bond to N(R5), X being bonded to another ring C); rings systems in A being os by T, OT, halo, NO2, NH2, CN or CN; Ra1T or OT; Rx1 - Rx3bond, H, T, 2-4C alkenyl or 2-4 C alkynyl; Y' : bond, C(O), S(O), SO2, O, S, CRy1Ry2 or NRy3; Ry1 - Ry3bond, H, T, 2-4C alkenyl or 2-4 C alkynyl (all os by 1 or 2 of T, Ph, CH2Ph, cycloalkyl, OT, NH2, halo, NO2, CN or oxo; D : N or CRd1; Rd1as Ry1; With the following provisos: (1) if R13 is a bond then R12 cannot be a heteroatoms; (2) R11 and R12 cannot both be heteroatoms; and (3) Y' and D cannot both be heteroatoms; unless specified otherwise alkyl moieties have 1-10C, alkenyl or alkynyl moieties 2-10C, cycloalkyl moieties 3-7C and aryl moieties 6C or 10C. An INDEPENDENT CLAIM is included for the preparation of (I). - ACTIVITY : Antiinflammatory; immunosuppressive; antiarteriosclerotic; antiasthmatic; antiallergic; antidiabetic; neuroprotective; cardiant; antirheumatic; antiarthritic. - MECHANISM OF ACTION : Integrin antagonist. (I) are especially alpha 4beta 1 integrin antagonists, but may also show alpha 4beta 7 and/or alpha 4beta 9 antagonist activity. 2-(1-(2-(2-(4-((2-Toluidinocarbonyl)-amino)-phen yl)-acetyl)-L-leucine)-2-piperidinyl)-acetic acid (Ia) had IC50 0.5 mu M or less in a Jurkat-VCAM-1 in vitro assay.

36. 发明专利

DE19962936A1 New beta-aminoacid amide derivatives, are integrin antagonists useful for treating inflammatory, autoimmune or immunological disorders e.g. asthma, diabetes or rheumatoid arthritis 未知
公开(公告)号：DE19962936A1
公开(公告)日：2001-06-28
申请号：DE19962936
申请日：1999-12-24
申请人： BAYER AG
发明人： ALBERS MARKUS , LEHMANN THOMAS , ROELLE THOMAS , MUELLER GERHARD , HESLER GERHARD , TAJIMI MASAOMI , ZIEGELBAUER KARL , OKIGAMI HIROMI , HASEGAWA HARUKI
IPC分类号： A61K31/445 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61P1/04 , A61P3/10 , A61P9/10 , A61P11/06 , A61P25/28 , A61P29/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D211/60 , C07D211/96 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/06 , C07D409/06 , C07D409/12 , C07D409/14 , A61K31/452 , C07D211/90 , C07D413/02 , C07D417/02
摘要： N,N'-Disubstituted beta -aminoacid amide derivatives (I) are new. beta -Aminoacid derivatives of formula (I) and their salts are new. R1 - R5, R7-R9 = H, 1-10C alkyl, 2-10C alkenyl, 6C or 10C aryl, 3-7C cycloalkyl or Het1; Het1 = 4-9 membered saturated or unsaturated heterocyclyl containing 1 or 2 of O, S and N heteroatom(s), optionally substituted by 1-3 R10 and additionally optionally monosubstituted by 3-7C cycloalkyl, 6C or 10C aryl, 4-9C heteroaryl or Het2; Het2 = 4-9 membered heterocyclyl containing 1 or 2 of O, S and N as heteroatom(s), optionally substituted by 1-3 R10; R10 = T, CF3, OCF3, OR11, SR11, NR13R14, COR11, SOR11, SO2R11, COOR11, OCOR11, CONR13R14, NR11COR11, SO2NR13R14, NR11SO2R11, NR11CONR13R14, NR11COOR11, OCONR13R14, halo, CN, NO2 or =O; T = 1-4C alkyl; R11 = H, T, 3-6C cycloalkyl or 6C or 10C aryl (optionally substituted (os) by T, OT, Ph, 3-6C cycloalkyl, halo, NO2 or CN); R13, R14 = H, T, 3-6C cycloalkyl or 6C or 10C aryl, or NR13R14 = 4-7 membered heterocyclyl, optionally containing 1 or 2 additional O, S or N heteroatoms and/or 1 or 2 double bonds; R6 = H, 1-10C alkyl, 2-10C alkenyl, 6C or 10C aryl, 3-7C cycloalkyl or Het3; Het3 = 4-9 membered saturated or unsaturated heterocyclyl containing 1 or 2 of O, S and N heteroatom(s), os by 1-3 R31 and additionally os by one of 3-7C cycloalkyl, 6C or 10C aryl, 4-9C heteroaryl or Het4; Het4 = 4-9 membered heterocyclyl containing 1 or 2 of O, S and N heteroatom(s), os by 1-3 R10 or fused to benzo; R31 = T, CF3, OCF3, OR32, SR32, NR33R34, COR32, SOR32, SO2R32, COOR32, OCOR32, CONR33R34, NR32COR32, SO2NR33R34, NR32SO2R32, NR32CONR33R34, NR32COR32, OCONR33R34, halo, CN, NO2 or =O; R32 = H, T, 3-6C cycloalkyl or 6C or 10C aryl (os by 1-3 of T, 1-4C alkoxy, Ph, 3-6C cycloalkyl, halo, NO2 or CN); R33, R34 = H, T, 3-6C cycloalkyl, 6C or 10C aryl or Het5, or NR33R34 = 4-7 membered heterocycle, optionally containing 1 or 2 additional O, S or N heteroatoms and/or 1 or 2 double bonds and os by 1 or 2 of T, Ph, benzyl, 3-7C cycloalkyl, OT, halo, NO2, CN or =O; Het5 = 4-9 membered saturated or unsaturated heterocyclyl containing 1 or 2 of O, S and N as heteroatom(s), os by 1 or 2 of T, Ph, 3-7C cycloalkyl, OT, halo, NO2 or CN, or R1 + R2, R4 + R2 or R6 + R12 = a group completing a 4-7 membered heterocycle, optionally containing 1 or 2 additional O, S or N heteroatoms and/or 1 or 2 double bonds, optionally substituted by 1 or 2 of T, Ph, benzyl, 3-7C cycloalkyl, OT, halo, NO2, CN or =O and optionally fused with a 3-7 membered homocyclic or heterocyclic, saturated or unsaturated ring, or R1 + R4, R1 + R5 or R3 + R4 = a group completing a 4-7 membered ring, optionally containing 1 or 2 O, S or N heteroatoms and/or 1 or 2 double bonds, optionally substituted by 1 or 2 of T, Ph, benzyl, 3-7C cycloalkyl, OT, halo, NO2, CN or =O and optionally fused with a 3-7 membered homocyclic or heterocyclic, saturated or unsaturated ring; A = (i) C(O), C(O)-C(O)-, C(S), SO, SO2, PO, PO2, 2- or 4-pyrimidyl, 2-pyridyl, 2- or 4-imidazolyl or 2-benzimidazolyl; or (ii) 4- or 5-(X)-thiazol-2-yl, 4- or 5-(X)-oxazol-2-yl, 4- or 5-(X)-pyrazol-3-yl, 4- or 5-(X)-isothiazol-3-yl, 4- or 5-(X)-isoxazol-3-yl, 5-(X)-4H-1,2,4-triazol-3-yl, 5-(X)-1,3,4-thiadiazol-2-yl, 5-(X)-1,3,4-oxadiazol-2-yl, 3-(X)-1,2,4-thiadiazol-5-yl, 3-(X)-1,3,4-oxadiazol-5-yl, 5-(X)-1,2,4-thiadiazol-3-yl, 5-(X)-1,3,4-oxadiazol-3-yl, 4- or 5-(X)-4,5-dihydrothiazol-2-yl, 4- or 5-(X)-4,5-dihydroimidazol-2-yl, 4-, 5-,6- or 7-benzothiazol-2-yl, 4-, 5-,6- or 7-benzoxazol-2-yl, 3-, 5- or 6-(X)-pyrazin-2-yl or 4-, 5- or 6-(X)-pyridazin-3-yl (all os in the ring by T, OT, halo, NO2 or CN); X = a direct bond, O or NR12; R12 = H, T, 2-4C alkenyl, 2-4C alkynyl (os by Ph) or group forming a ring with R6 (as described above); Y = O or S; Z' = COOR47, CONR48R49, SO2NR48R49, SO(OR47), SO2(OR47), P(O)R47(OR49), P(O)(OR47)(OR49) or 5-tetrazolyl; R48 = COR50 or SO2R50; R50 = T, 2-6C alkenyl, 2-6C alkynyl, 3-6C cycloalkyl or 6C or 10C aryl (os by 1-3 of halo, NO2 or CN), and R47, R49 = H, polymeric resin, T, 2-6C alkenyl, 2-6C alkynyl, 3-6C cycloalkyl or 6C or 10C aryl (os by 1-3 of T, OT, halo, NO2 or CN).

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