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    • 82. 发明专利
      DE10129717A1 Combination preparation containing nucleoside compound and 5-sulfonyl-2-phenylacetamido-thiazole derivative, useful as antiviral agent effective againts herpes viruses, especially herpes simplex 未知
    • Combination preparation containing nucleoside compound and 5-sulfonyl-2-phenylacetamido-thiazole derivative, useful as antiviral agent effective againts herpes viruses, especially herpes simplex
    • DE10129717A1
    • 2003-01-02
    • DE10129717
    • 2001-06-22
    • BAYER AG
    • KLEYMANN GERALD , BETZ ULRICH , FISCHER RUEDIGER , HENDRIX MARTIN , BENDER WOLFGANG , ECKENBERG PETER , HANDKE GABRIELE , SCHNEIDER UDO , SCHOHE-LOOP RUDOLF , BAUMEISTER JUDITH , HENNINGER KERSTIN , JENSEN AXEL , KELDENICH JOERG , WEBER OLAF
    • A61K31/426 , A61K31/522
    • New combination preparations (A) contain (a) nucleoside compounds (specifically acyclovir or penciclovir) and (b) 5-aminosulfonyl-2-phenylacetamido-thiazole derivatives (I) or 5-halosulfonyl-2-phenylacetamido-thiazole derivatives (IV). New combination preparations (A) contain nucleoside compounds (specifically acyclovir, penciclovir or their prodrugs) and (b) thiazole derivatives of formula (I) (or their salts) or (IV). R1 = H, halo, alkyl, alkoxy, aminoalkyl or haloalkyl; R2, R3 = H, alkoxy, cycloalkyl or biphenylaminocarbonyl; alkyl (optionally substituted (os) by 1-3 of 3-6C cycloalkyl, alkoxy, halo, OH, NH2, trialkylsilyloxy, 3,4-methylenedioxyphenyl, tetrahydrofuran-2-yl, -N(R'2)COOtBu, Het1, Het2 or aryl (os by OH or alkoxy)); -P(O)(OR8)(OR9), -COCH(NH2)-R10, -CHR11-OCOR12 or -CH(NH2)-R10; or NR2R3 = 5- or 6-membered saturated heterocycle, optionally containing a further O heteroatom; R'2, R8, R9 = H or 1-4C alkyl; Het1 = C- or N-bonded 5- or 6-membered aromatic heterocycle containing 1-3 of S, N and/or O as heteroatom(s)); Het2 = C- or N-bonded 3-8 membered, saturated or unsaturated, non-aromatic heterocycle containing 1-3 of S, N and/or O as heteroatom(s)); R10 = side-chain of a naturally occurring aminoacid; R11 = 1-4C alkyl; R12 = H, 1-4C alkyl or -CH(NH2)-R10; R4 = H, acyl, 2-6C alkenyl or cycloalkyl; or alkyl (os by 1-3 of halo, OH, cycloalkyl, acyl, alkoxy, COOH, NHCOOtBu, OEt, -CH2CH2OEt, phenoxy, aryl or NR13R14); or alkyl substituted by optionally benzo-fused Het1, 2-(R16)-pyrrolidino, tetrahydrofuran-2-yl, benzo-1,4-dioxan-2-yl, 2-oxo-pyrrolidino or -OCOR17R18; R13, R14 = H, acyl, alkyl, CONH2, mono- or dialkylaminoalkyl, mono- or dialkylaminocarbonyl, aryl or alkoxycarbonyl; or NR13R14 = 5- or 6-membered saturated heterocyclyl, optionally containing a further O, S or NR15 heteroatom and os by =O; R15 = H or 1-4C alkyl; R16 = H or alkyl; R17, R18 = H; or alkyl or aryl (both os by 1-3 of OH, alkoxy or halo); R5, R7 = H, alkyl, halo, NH2, mono- or dialkylamino or alkanoylamino; R6 = phenyl (os by 1-3 groups R'6); R'6 = halo, aryl (os by 1-3 of alkanoyl, alkoxy, alkyl, halo, alkoxycarbonyl, NO2, haloalkyl, haloalkoxy, NH2, alkylthio, OH, COOH, CONH2, mono- or dialkylaminocarbonyl, mono- or dialkanoylamino, alkoxycarbonylamino, alkylsulfoxy, alkylsulfonyl, trialkylsilyloxy, Het2 or CN), alkoxy (os by 1-6 F, but not perfluorinated), alkoxycarbonyl, alkylthio, OH, COOH, alkyl (os by tetrahydrofuran-2-yl), Het1 (os by 1-3 of alkanoyl, alkoxy, alkyl, halo, alkoxycarbonyl, NO2, haloalkyl, haloalkoxy, NH2, alkylthio, OH, COOH, CONH2, mono- or dialkylaminocarbonyl, mono- or dialkanoylamino, alkoxycarbonylamino, alkylsulfoxy, alkylsulfonyl, Het2 (mono- or bicyclic) or CN), Het2 (mono- or bicyclic; and os by 1-3 of =O, halo, OH, alkoxycarbonyl, alkoxycarbonylamino, alkyl, haloalkyl or hydroxyalkyl), 2-6C alkenyl, OR19, NR20R21, CONR22R23, carbazole, dibenzofuran, dibenzothiophene, xanthene or 9,10-dihydroacridine; R19 = phenyl (os by NR24R25) or alkyl (os by 1-3 of OH or halo); R24, R25 = H, alkyl or acyl; R20, R21 = H, CONH2, mono- or dialkylaminocarbonyl, phenyl, acyl or alkyl (os by alkoxy or acyl; or by phenyl or Het1 (both os by 1-3 of halo or OH)); R22, R23 = H or alkyl; D = halogen; alkyl moieties or acyl groups have 1-6C, cycloalkyl moieties 3-8C and aryl moieties 6-10C unless specified otherwise.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 85. 发明专利
      DE10039265A1 New 2-acylamino-5-aminosulfonyl-1,3-thiazole derivatives, useful as antiviral agents, especially for treatment or prophylaxis of herpes simplex virus infections 未知
    • New 2-acylamino-5-aminosulfonyl-1,3-thiazole derivatives, useful as antiviral agents, especially for treatment or prophylaxis of herpes simplex virus infections
    • DE10039265A1
    • 2002-02-21
    • DE10039265
    • 2000-08-11
    • BAYER AG
    • FISCHER RUEDIGER , KLEYMANN GERALD , BETZ ULRICH , BAUMEISTER JUDITH , BENDER WOLFGANG , ECKENBERG PETER , HANDKE GABRIELE , HENDRIX MARTIN , HENNINGER KERSTIN , JENSEN AXEL , KELDENICH JOERG , SCHNEIDER UDO , WEBER OLAF
    • C07D277/54 , C07D417/12 , C07D521/00 , C07F7/18 , C07F9/6539 , A61K31/426
    • 2-Acylamino-5-aminosulfonyl-1,3-thiazole derivatives (I) are new. Thiazole derivatives of formula (I) and their salts are new. R1 = H, halo, alkyl, alkoxy, aminoalkyl or haloalkyl; R2, R3 = H, alkoxy, cycloalkyl or biphenylaminocarbonyl; alkyl (optionally substituted (os) by 1-3 of 3-6C cycloalkyl, alkoxy, halo, OH, NH2, trialkylsilyloxy, 3,4-methylenedioxyphenyl, tetrahydrofuran-2-yl, -N(R'2)-COOCMe3, Het1, Het2 or aryl (itself os by OH or alkoxy); -COCH(R10)-NH2; or -CH(R11)-OCOR12; or NR2R3 = 5- or 6-membered saturated heterocycle optionally containing O; R'2, R8, R9 = H or 1-4C alkyl; Het1 = optionally N-bonded 5- or 6-membered aromatic heterocycle containing 1-3 of S, N and O as heteroatom(s); Het2 = optionally N-bonded 3-8 membered saturated or unsaturated non-aromatic heterocycle containing 1-3 of S, N and O as heteroatom(s); R10 = side-chain of a naturally occurring alpha -amino acid; R11 = 1-4C alkyl; R12 = H, 1-4C alkyl or -CHR10-NH2; R4 = H, 1-6C acyl, 2-6C alkenyl or cycloalkyl; or alkyl os by (i) 1-3 of halo, OH, cycloalkyl, 1-6C acyl, alkoxy, COOH, -NHCOOCMe3, -(OCH2CH2)nOEt, OPh, aryl or NR13R14 or (ii) Het1 (optionally fused with benzo), 1-(R16)-2-pyrrolidinyl, tetrahydrofuran-2-yl, benzo-1,4-dioxan-2-yl, 2-oxo-1-pyrrolidinyl or -OCONR17R18; n = 0 or 1; R13, R14 = H, 1-6C acyl, alkyl, CONH2, mono- or dialkylaminoalkyl, mono- or dialkylaminocarbonyl, aryl or alkoxycarbonyl; or NR13R14 = 5- or 6-membered saturated heterocycle optionally containing O, S or NR15 as additionally heteroatom and os by oxo; R15 = H or 1-4C alkyl; R17, R18 = H; or alkyl or aryl (both os by 1-3 of OH, alkoxy and halo); R5, R7 = H, alkyl, halo, NH2, mono- or dialkylamino or (1-6C) alkanoylamino; R6 = phenyl, os by 1-3 Q; Q = halo, aryl (os by 1-3 Q'), alkoxy (os by 1-6 F), alkoxycarbonyl, alkylthio, OH, COOH, alkyl (os by tetrahydrofuran-2-yl), Het1 (os by 1-3 Q'), mono- or bicyclic Het2 (os by 1-3 of oxo, halo, OH, alkoxycarbonyl, alkoxycarbonylamino, alkyl, haloalkyl and hydroxyalkyl), 2-6C alkenyl, OR19, NR20R21, CONR22R23, carbazole, dibenzofuran, dibenzothiepin, xanthene or 9,10-dihydroacridine; Q' = (1-6C) alkanoyl, alkoxy, alkyl, halo, alkoxycarbonyl, NO2, haloalkyl, haloalkoxy, NH2, alkylthio, OH, COOH, CONH2, mono- or dialkylaminocarbonyl, mono- or di-(1-6C alkanoyl)-amino, alkoxycarbonylamino, alkylsulfoxy, alkylsulfonyl, trialkylsilyloxy, CN or mono- or bicyclic Het2; R19 = phenyl (os by NR24R25) or alkyl (os by 1-3 of OH or halo); R24, R25 = H, alkyl or 1-6C acyl; R20, R21 = H, CONH2, mono- or dialkylaminocarbonyl, phenyl, 1-6C acyl or alkyl (where alkyl is os by alkoxy, 1-6C acyl, phenyl or Het1; and phenyl and Het1 are os by one or more of halo and/or OH); R22, R23 = H or alkyl; and D' = halogen. alkyl moieties have 1-6C, cycloalkyl moieties 3-8C and aryl moieties 6-10C unless specified otherwise. Independent claims are included for: (i) the preparation of (I); (ii) new sulfonyl halide intermediates of formula (IV); and (iii) the use of N-(5-(aminosulfonyl)-1,3-thiazol-2-yl)-acetamide, N-(5-(aminosulfonyl)-1,3-thiazol-2-yl)-2-phenylacetamide or N-(5-(aminosulfonyl)-1,3-thiazol-2-yl)-2-(1,1'-biphenyl)-4-ylacetamide derivatives for the preparation of medicaments.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 86. 发明专利
      DE19959958A1 New 2-ureido-thiazole-5-sulfonic acid amide derivatives useful as antiviral agents, especially against herpes simplex infections 未知
    • New 2-ureido-thiazole-5-sulfonic acid amide derivatives useful as antiviral agents, especially against herpes simplex infections
    • DE19959958A1
    • 2001-08-30
    • DE19959958
    • 1999-12-13
    • BAYER AG
    • FISCHER RUEDIGER , KLEYMANN GERALD , BAUMEISTER JUDITH , BENDER WOLFGANG , BETZ ULRICH , ECKENBERG PETER , HANDKE GABRIELE , HENDRIX MARTIN , SCHNEIDER UDO , WEBER OLAF , HENNINGER KERSTIN , JENSEN AXEL , KELDENICH JOERG
    • C07D277/54 , C07D417/12 , C07D487/04 , C07D521/00 , A61K31/425 , C07D295/06
    • 2-Ureido-thiazole-5-sulfonic acid amide derivatives (I) and their salts are new. 2-Ureido-thiazole-5-sulfonic acid amide derivatives of formula (I) and their salts are new. [Image] R1H, halo or 1-6C alkyl, alkoxy, aminoalkyl or haloalkyl; R2, R3H, 3-8C cycloalkyl, biphenylaminocarbonyl; or 1-6C alkyl (optionally substituted by 1-3 3-6C cycloalkyl, 1-6C alkoxy, halo, OH, 2-tetrahydrofuranyl or 5-benzo[1,3]dioxolyl; 5-6 membered heteroaryl containing 1-3 N, O and/or S, optionally bonding through N; or 3-8 membered non-aromatic heterocycle containing 1-3 N, O and/or S, optionally bonded through N and optionally substituted by OH or 1-6C alkoxy); or NR2R35-6 membered saturated heterocycle, optionally containing an O atom; R4H, 1-6C acyl or 2-6C alkenyl; or 1-6C alkyl (optionally substituted by either 1-3 halo, OH, 1-6C acyl, 1-6C alkoxy, phenoxy, 6-10C aryl or NR7R8; or by 5-6 membered heteroaryl (containing 1-3 N, O and/or S optionally bonded via N), 2-tetrahydrofuranyl, 1-R10-2-pyrrolidinyl, 2,3-dihydro-benzo[1,4]dioxin-2-yl or (R11)(R12)NC(=O)O); R7, R8H, 1-6C acyl, 1-6C alkyl, carbamoyl, mono- or di-1-6C alkylamino-1-6C alkyl, mono- or di- 1-6C alkylaminocarbonyl, 6-10C aryl or 1-6C alkoxycarbonyl; or NR7R85-6 membered heteroaryl optionally containing additional O, S or NR9heteroatoms (optionally substituted by oxo); R9H or 1-4C alkyl; R11, R12H; or 1-6C alkyl or 6-10C aryl, both optionally substituted by 1-3 OH, 1-6C alkoxy or halo; R62-oxo-3-ethyl-3H-benzoxazol-6-yl; or phenyl (optionally substituted by 1-3 halo, 6-10C aryl (itself optionally substituted by halo, NO2, NH2, OH, COOH, carbamoyl, mono- or di-1-6C alkylcarbonyl, mono- or di- 1-6C acylamino or CN; or 1-6C alkanoyl, alkoxy, alkyl, alkoxycarbonyl, haloalkyl, haloalkoxy, alkylthio, alkylsulfoxy or alkylsulfonyl), 1-6C alkoxy, 1-6C alkoxycarbonyl, 1-6 alkylthio, OH, COOH, fluorinated 1-6C alkoxy (with 1-6 F atoms), a group of formula (i)-(iii), 1-6C alkyl (optionally substituted by 2-tetrahydrofuranyl), 5-6 membered heteroaryl containing 1-3 O, N and/or S (optionally bonded through N and optionally substituted by 1-3 halo, NO2, NH2, OH, COOH, carbamoyl, mono- or di-1-6C alkylaminocarbonyl, mono- or di- 1-6C acylamino or CN; or 1-6C alkanoyl, alkoxy, alkyl, alkoxycarbonyl, haloalkoxy, alkylthio, alkylsulfoxy or alkylsulfonyl), 3-8C non-aromatic mono- or bi-cyclic heterocycle containing 1-3 O, N and/or S (optionally bonded through N and optionally substituted by 1-3 oxo, halo, OH or 1-6C alkoxycarbonyl, alkoxycarbonylamino, alkyl, haloalkyl or hydroxyalkyl) or OR14, NR15R16 or CONR17R18); R14phenyl (optionally substituted by NR19R20), 1-6C alkyl (optionally substituted by 1-3 OH) or an isoquinolin derivative of formula (iv); R15, R16H, carbamoyl, mono- or di- 1-6C alkylaminocarbonyl, phenyl or 1-6C acyl; or 1-6C alkyl (optionally substituted by 1-6C alkoxy, 1-6C acyl; or phenyl or 5-6 membered heteroaryl with 1-3 O, N and/or S heteroatoms (themselves optionally substituted by 1-3 halo and/or OH); R5, R10, R13, R17, R18H or 1-6C alkyl;; R19, R20H, 1-6C alkyl or 1-6C acyl. [Image] [Image] Independent claims are included for: (1) intermediates of formula (II); (2) preparation of (I); and (3) use of 2-[(aminocarbonyl)amino]-1,3-thiazol-5-sulfonamide derivatives (A) for preparation of medicaments [Image] A : halo. ACTIVITY : Virucide. 2-{[2-(Dimethylamino)ethyl][4-(ethoxyanilino)carbonyl]amino}-N,4-dimethyl-1,3-thiazol-5-sulfonamide (Ia) had IC50 values of 0.2 MicroM for herpes simplex virus (HSV) 1F and 1 MicroM for HSV-2G. A similar compound, 2-(3-biphenyl-4-yl-1-methyl-ureido)-4-methyl-thiazole-5-sulfonic acid methylamide had corresponding IC50 values of 1 nM and 5 nM respectively. Zovirax had IC50 values of 1 MicroM and 3 MicroM respectively. MECHANISM OF ACTION : None given.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 87. 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
    • 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
    • DE10006453A1
    • 2001-08-16
    • DE10006453
    • 2000-02-14
    • BAYER AG
    • FISCHER RUEDIGER , LEHMANN THOMAS , MUELLER GERHARD , HESLER GERHARD , TAJIMI MASAOMI , ZIEGELBAUER KARL , OKIGAMI HIROMI , HASEGAWA HARUKI , KOMURA HIROSHI , MIZOGUCHI MANAMI
    • A61P37/08 , C07D207/16 , C07D211/34 , C07D211/60 , C07D211/62 , C07D263/58 , C07D403/04 , C07D413/12 , C07D487/04 , C07D211/32 , A61K31/5355 , C07K14/78
    • 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.
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