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1. 发明申请

WO0076966A3 INDOLINYLAMIDE DERIVATIVES AND THE USE THEREOF AS ANTIVIRAL DRUGS 审中-公开
标题翻译： INDOLINYLAMIDDERIVATE及其作为抗病毒药物
公开(公告)号：WO0076966A3
公开(公告)日：2001-07-19
申请号：PCT/EP0005114
申请日：2000-06-05
申请人： BAYER AG , HANDKE GABRIELE , BAUMEISTER JUDITH , BENDER WOLFGANG , BETZ ULRICH , BRANDS MICHAEL , ECKENBERG PETER , FISCHER RUEDIGER , HENDRIX MARTIN , HENNINGER KERSTIN , JENSEN AXEL , KELDENICH JOERG , KLEYMANN GERALD , MAESSEN JUTTA , SCHNEIDER UDO , WEBER OLAF
发明人： HANDKE GABRIELE , BAUMEISTER JUDITH , BENDER WOLFGANG , BETZ ULRICH , BRANDS MICHAEL , ECKENBERG PETER , FISCHER RUEDIGER , HENDRIX MARTIN , HENNINGER KERSTIN , JENSEN AXEL , KELDENICH JOERG , KLEYMANN GERALD , MAESSEN JUTTA , SCHNEIDER UDO , WEBER OLAF
IPC分类号： C07D209/08 , C07D401/12 , C07D403/12 , C07D405/12 , A61K31/404 , A61P31/12
CPC分类号： C07D401/12 , C07D209/08 , C07D403/12 , C07D405/12
摘要： The invention relates to compounds of general formula (I), to a method for the production thereof and to the use of said compounds as medicaments, particularly as antiviral drugs.
摘要翻译：本发明betrifftneue通式（I）化合物，它们的制备方法以及它们作为药物的用途，尤其是作为抗病毒药物的方法。

2. 发明申请

WO0240455A8 SUBSTITUTED AMIDOALKYL URACILS AND THEIR USE AS INHIBITORS OF THE POLY(ADP-RIBOSE) SYNTHETASE (PARS) 审中-公开
标题翻译：取代AMIDOALKYLURACILE及其作为聚（ADP-核糖）合成酶抑制剂（PARS）
公开(公告)号：WO0240455A8
公开(公告)日：2002-07-18
申请号：PCT/EP0112694
申请日：2001-11-02
申请人： BAYER AG , ALBRECHT BARBARA , GERISCH MICHAEL , HANDKE GABRIELE , JENSEN AXEL , KRAHN THOMAS , NICKL WERNER , OEHME FELIX , SCHLEMMER KARL-HEINZ , STEINHAGEN HENNING
发明人： ALBRECHT BARBARA , GERISCH MICHAEL , HANDKE GABRIELE , JENSEN AXEL , KRAHN THOMAS , NICKL WERNER , OEHME FELIX , SCHLEMMER KARL-HEINZ , STEINHAGEN HENNING
IPC分类号： C07D239/96 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D491/04 , C07D495/04 , C07D519/00 , C07D521/00 , A61K31/517 , A61K31/519
CPC分类号： C07D231/12 , C07D233/56 , C07D239/96 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D491/04 , C07D495/04
摘要： The invention relates to novel amidoalkyl uracil derivatives of formula (I), to a method for the production thereof, and to their use as medicament active substances for the prophylaxis and/or treatment of medical disorders.
摘要翻译：还有被描述为用于治疗疾病的Amidoalkyluracil式（I）的新衍生物预防和/或治疗的药物活性化合物，它们的制备和它们的用途的方法。

3. 发明申请

WO0206247A8 SUBSTITUTED AMIDOALKYL-URACILS AS PARP INHIBITORS 审中-公开
标题翻译：取代的酰胺基 - 尿嘧啶作为PARP抑制剂
公开(公告)号：WO0206247A8
公开(公告)日：2002-02-21
申请号：PCT/EP0107670
申请日：2001-07-05
申请人： BAYER AG , HAERTER MICHAEL , ALBRECHT BARBARA , GERISCH MICHAEL , HANDKE GABRIELE , HUETTER JOACHIM , JENSEN AXEL , KRAHN THOMAS , MITTENDORF JOACHIM , OEHME FELIX , SCHLEMMER KARL HEINZ , STEINHAGEN HENNING
发明人： HAERTER MICHAEL , ALBRECHT BARBARA , GERISCH MICHAEL , HANDKE GABRIELE , HUETTER JOACHIM , JENSEN AXEL , KRAHN THOMAS , MITTENDORF JOACHIM , OEHME FELIX , SCHLEMMER KARL-HEINZ , STEINHAGEN HENNING
IPC分类号： A61P9/10 , C07D239/96 , C07D401/06 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D411/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/04 , C07D491/048 , C07D491/052 , C07D495/04 , C07D513/04 , A61K31/517 , A61K31/519 , C07D401/12
CPC分类号： C07D401/06 , C07D239/96 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D411/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/04 , C07D495/04 , C07D513/04
摘要： The invention relates to novel PARP inhibitors in the form of amidoalkyl-uracil derivatives of formula (I), to a method for producing them and to their use as active agents of medicaments, for preventing and/or treating ischaemia and reperfusion damage.
摘要翻译：还有被描述为在式（I）的酰胺基烷基 - 尿嘧啶衍生物的形式预防和/或治疗缺血再灌注损伤的新的PARP抑制剂的药物活性化合物，它们的制备和它们的用途的方法。

4. 发明专利

PL356484A1 THIAZOLYL AMIDE DERIVATIVES 未知
公开(公告)号：PL356484A1
公开(公告)日：2004-06-28
申请号：PL35648400
申请日：2000-12-12
申请人： BAYER AG
发明人： FISCHER RUDIGER , KLEYMANN GERALD , BETZ ULRICH , BAUMEISTER JUDITH , BENDER WOLFGANG , ECKENBERG PETER , HANDKE GABRIELE , HENRIX MARTIN , HENNINGER KERSTIN , JENSEN AXEL , KELDENICH JORG , SCHNEIDER UDO , WEBER OLAF
IPC分类号： A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/497 , A61K31/506 , C07D277/20 , A61K31/5377 , A61K31/695 , A61P1/16 , A61P11/00 , A61P25/00 , A61P27/02 , A61P31/12 , A61P31/22 , C07B61/00 , C07D277/54 , C07D417/12 , C07D521/00 , C07F7/18 , C07F9/6539
摘要： The present invention relates to novel compounds, to a process for their preparation and to their use as medicaments, in particular as antiviral medicaments.

5. 发明专利

AU8200701A Inverse thiazolyl amide derivatives 未知
公开(公告)号：AU8200701A
公开(公告)日：2002-02-18
申请号：AU8200701
申请日：2001-07-23
申请人： BAYER AG
发明人： HENDRIX MARTIN , KLEYMANN GERALD , BETZ ULRICH , BAUMEISTER JUDITH , BENDER WOLFGANG , ECKENBERG PETER , FISCHER RUDIGER , HANDKE GABRIELE , HENNINGER KERSTIN , JENSEN AXEL , KELDENICH JORG , SCHNEIDER UDO , WEBER OLAF
IPC分类号： A61P31/12 , C07D277/36 , A61K31/425

6. 发明专利

DE10038022A1 未知
公开(公告)号：DE10038022A1
公开(公告)日：2002-02-14
申请号：DE10038022
申请日：2000-08-04
申请人： BAYER AG
发明人： HENDRIX MARTIN , KLEYMANN GERALD , BETZ ULRICH , BAUMEISTER JUDITH , BENDER WOLFGANG , ECKENBERG PETER , FISCHER RUEDIGER , HANDKE GABRIELE , HENNINGER KERSTIN , JENSEN AXEL , KELDENICH JOERG , SCHNEIDER UDO , WEBER OLAF
IPC分类号： A61P31/12 , C07D277/36 , A61K31/425 , C07D417/12 , C07D417/14
摘要： The invention relates to novel compounds, namely inverse thiazolyl amide derivatives of the formula (I). The invention also relates to methods for producing said derivatives, and to their use as medicaments, especially as antiviral medicaments.

7. 发明专利

DE19962532A1 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
公开(公告)号：DE19962532A1
公开(公告)日：2001-07-05
申请号：DE19962532
申请日：1999-12-23
申请人： BAYER AG
发明人： 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
IPC分类号： C07D277/54 , C07D417/12 , C07D521/00 , C07F7/18 , C07F9/6539 , A61K31/425
摘要： 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.

8. 发明专利

DE19927415A1 未知
公开(公告)号：DE19927415A1
公开(公告)日：2000-12-21
申请号：DE19927415
申请日：1999-06-16
申请人： BAYER AG
发明人： HANDKE GABRIELE , BAUMEISTER JUDITH , BENDER WOLFGANG , BETZ ULRICH , BRANDS MICHAEL , ECKENBERG PETER , FISCHER RUEDIGER , HENDRIX MARTIN , HENNINGER KERSTIN , JENSEN AXEL , KELDENICH JOERG , KLEYMANN GERALD , MAESEN JUTTA , SCHNEIDER UDO , WEBER OLAF
IPC分类号： C07D209/08 , C07D401/12 , C07D403/12 , C07D405/12 , A61K31/405
摘要： The invention relates to novel compounds, to a method for the production thereof and to the use of said compounds as medicaments, particularly as antiviral medicaments.

9. 发明专利

HK1057552A1 Thiazolyl amide derivatives 未知
公开(公告)号：HK1057552A1
公开(公告)日：2004-04-08
申请号：HK04100401
申请日：2004-01-19
申请人： BAYER AG
发明人： FISCHER RUDIGER , KLEYMANN GERALD , BETZ ULRICH , BAUMEISTER JUDITH , BENDER WOLFGANG , ECKENBERG PETER , HANDKE GABRIELE , HENDRIX MARTIN , HENNINGER KERSTIN , JENSEN AXEL , KELDENICH JORG , SCHNEIDER UDO , WEBER OLAF
IPC分类号： C07D277/20 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/695 , A61P1/16 , A61P11/00 , A61P25/00 , A61P27/02 , A61P31/12 , A61P31/22 , C07B61/00 , C07D277/54 , C07D417/12 , C07D521/00 , C07F7/18 , C07F9/6539 , C07D , C07F , A61K , A61P
摘要： The present invention relates to novel compounds, to a process for their preparation and to their use as medicaments, in particular as antiviral medicaments.

10. 发明专利

DE10056312A1 New 1-(N-substituted amidoalkyl) bicyclic uracil derivatives useful as medicaments for treating ischemia or reperfusion damage, are poly-(ADP-ribose)-synthetase inhibitors 未知
公开(公告)号：DE10056312A1
公开(公告)日：2002-05-16
申请号：DE10056312
申请日：2000-11-14
申请人： BAYER AG
发明人： ALBRECHT BARBARA , GERISCH MICHAEL , HANDKE GABRIELE , JENSEN AXEL , KRAHN THOMAS , NICKL WERNER , OEHME FELIX , SCHLEMMER KARL-HEINZ , STEINHAGEN HENNING
IPC分类号： C07D239/96 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D491/04 , C07D495/04 , C07D519/00 , C07D521/00 , A61K31/505 , C07D213/74 , C07D247/00 , C07D295/205 , C07D417/12
摘要： 1-(N-Substituted amidoalkyl) 5,6-fused bicyclic uracil derivatives (I) are new. 1-(N-Substituted amidoalkyl) 5,6-fused bicyclic uracil derivatives of formula (I) and their salts, hydrates, hydrated salts and solvates are new. A = J, CH2-J, J-CH2, CH=CHCH2, CH2CH=CH, CH2CH2-J, J-CH2CH2 or CH2-J-CH2; J = CH2, O or S; E, G = 1-6C alkylene or 3-8C cycloalkylene (optionally substituted by one or more of 1-4C alkoxy, OH or NH2); T = direct bond or CH2; U, V = direct bond or CC (sic); or 6-10C arylene or 5-7 membered heterocyclene (containing 1-3 of O, S and N as heteroatom(s)), both optionally substituted by 1-3 of NO2, CN, halo, R, 3-8C cycloalkyl, OR, CF2, OCHF2, OCF3, OH, NH2, NHR, N(R)2, COOR, SO2NH2, SO2R, SO2NHR, SO2N(R)2 or OCOR; W = direct bond, O, S, COO, OCO or NR4; R4 = H or R; X = O, S or NR5; Y1 = H and Y2 = OH; or Y1 + Y2 = =O, =S or =NR6; R5, R6 = H, R or CH2Ph; R1 = H, R (optionally substituted by one or more halo) or 3-8C cycloalkyl; R2 = H or COOR; R3 = 6-10C aryl or 5-13 membered heterocyclyl (containing 1-4 of O, S and N as heteroatom(s)), both optionally substituted by 1-3 of NO2, CN, halo, R, 3-8C cycloalkyl, OR, CF2, OCHF2, OCF3, OH, =O, NH2, NHR, N(R)2, CH2NHR, CH2N(R)2, COOR, SO2NH2, SO2R, SO2NHR, SO2N(R)2, OCOR or CH2R7; R7 = 5-7 membered heterocycle containing 1-3 of O, S and N as heteroatom(s); and R = 1-6C alkyl. An Independent claim is also included for the preparation of (I).

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