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1. 发明申请

WO2010072602A1 SUBSTITUTED AMIDINE COMPOUNDS FOR COMBATING ANIMAL PESTS 审中-公开
标题翻译：用于组合动物疫苗的取代的氨基化合物
公开(公告)号：WO2010072602A1
公开(公告)日：2010-07-01
申请号：PCT/EP2009/067037
申请日：2009-12-14
申请人： BASF SE , KAISER, Florian , KÖRBER, Karsten , POHLMAN, Matthias , GROß, Steffen , DESHMUKH, Prashant , DICKHAUT, Joachim , BANDUR, Nina, Gertrud , VON DEYN, Wolfgang , CULBERTSON, Deborah, L. , ANSPAUGH, Douglas, D. , BRAUN, Franz-Josef , EBUENGA, Cecille
发明人： KAISER, Florian , KÖRBER, Karsten , POHLMAN, Matthias , GROß, Steffen , DESHMUKH, Prashant , DICKHAUT, Joachim , BANDUR, Nina, Gertrud , VON DEYN, Wolfgang , CULBERTSON, Deborah, L. , ANSPAUGH, Douglas, D. , BRAUN, Franz-Josef , EBUENGA, Cecille
IPC分类号： C07D261/04 , C07D413/12 , C07D213/78 , C07C257/18 , C07C257/22 , C07C259/18 , C07D413/04 , C07D413/10 , C07D413/14 , A01N43/80
CPC分类号： C07D261/04 , A01N43/80 , A01N43/82 , C07C257/18 , C07C257/22 , C07C259/18 , C07C2601/02 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14
摘要： The invention relates to substituted amidine compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the substituted amidine compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such substituted amidine compounds. The substituted amidine compounds of the present invention are defined by formula (I) wherein A 1 to A 4 , B 1 to B 3 , R 1 to R 3 , (R 4 ) p , (R 5 ) q , X and Y are defined as in the description.
摘要翻译：本发明涉及式（I）的取代的脒化合物，其涉及其对映体，非对映异构体和盐以及包含这些化合物的组合物。本发明还涉及取代的脒化合物，其盐或包含它们的组合物用于对抗动物害虫的用途。此外，本发明还涉及应用这种取代的脒化合物的方法。本发明的取代的脒化合物由式（I）定义，其中A1至A4，B1至B3，R1至R3，（R4）p，（R5）q，X和Y如说明书所定义。

2. 发明申请

WO2008070831A3 BISBENZAMIDINES AND BISBENZAMIDOXIMES FOR THE TREATMENT OF HUMAN AFRICAN TRYPANOSOMIASIS 审中-公开
标题翻译：用于治疗人类非特异性血管瘤的双嘧斯汀和双嘧达莫
公开(公告)号：WO2008070831A3
公开(公告)日：2008-08-28
申请号：PCT/US2007086773
申请日：2007-12-07
申请人： XAVIER UNIVERSITY OF LOUISIANA , HUANG TIEN L , VANDEN EYNDE JEAN-JACQUES , MAYENCE ANNIE , BACCHI CYRUS , DONKOR ISAAC O , KODE NAGESWARA
发明人： HUANG TIEN L , VANDEN EYNDE JEAN-JACQUES , MAYENCE ANNIE , BACCHI CYRUS , DONKOR ISAAC O , KODE NAGESWARA
IPC分类号： A01N37/52 , A61K31/155
CPC分类号： C07D295/155 , A61K31/167 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/551 , C07C257/18 , C07C259/18 , C07D271/06 , C07D271/07 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/10
摘要： Disclosed are bisbenzamidine and bisbenzamidoxime compounds useful for treatment of treatment of trypanosomiasis. The compounds disclosed are useful for treating mammals infected with parasitic hemoflagellates, in particular Trypanosoma brucei gambiense and Trypanosoma brucei rho
摘要翻译：公开了可用于治疗锥虫病的双苄脒和双苄脒肟化合物。所公开的化合物可用于治疗感染寄生性血栓病毒的哺乳动物，特别是布鲁斯氏锥虫和布鲁斯锥虫（Trypanosoma brucei rho）

3. 发明申请

WO2006021833A2 BISBENZAMIDINES FOR THE TREATMENT OF PNEUMONIA 审中-公开
标题翻译：用于治疗肺炎的双苄嘧啶
公开(公告)号：WO2006021833A2
公开(公告)日：2006-03-02
申请号：PCT/IB2004/004468
申请日：2004-11-24
申请人： UNIVERSITY OF CINCINNATI , WALZER, Peter, D. , CUSHION, Melanie, T. , MAYENCE, Annie , HUANG, Tien, Liang , VANDEN EYNDE, Jean, Jacques
发明人： WALZER, Peter, D. , CUSHION, Melanie, T. , MAYENCE, Annie , HUANG, Tien, Liang , VANDEN EYNDE, Jean, Jacques
CPC分类号： C07D233/02 , C07C257/18 , C07C259/18 , C07C2601/02 , C07D233/24 , C07D233/48 , C07D235/30 , C07D239/14 , C07D243/08 , C07D295/112 , C07D295/135 , C07D295/155 , C07D317/28 , C07D401/14 , C07D403/14
摘要： A method of combating infectious agents, such as Pneumocystis pneumonia, and a method of treating a subject in need of such treatment is disclosed. The method comprises administering to the subject a bis-benzamidoxime of formula (I) wherein the linker is a di-substituted cyclic moiety of any ring size and may contain at least one heteroatom; the aromatic group is 1,2-; 1,3-; or 1,4- disubstituted; R is selected from the group consisting of a hydrogen, a linear or branched alkyl group, containing from 1 to 20 carbon atoms; R' is selected from the group consisting of a hydrogen, a linear or branched alkyl group containing from one to twenty carbon atoms, an aromatic ring, a cycloalkyl group containing three to eight carbon atoms, or a hydroxyl group; alternatively, R and R' may form a cyclic structure that can be fused to another cyclic system; or a pharmaceutically acceptable salt thereof. Pharmaceutical formulations and active compounds useful in the practice of the present invention are also disclosed.
摘要翻译：一种抗感染剂的方法，例如

4. 发明申请

WO2005033065A1 NOVEL AMIDINE COMPOUNDS FOR TREATING MICROBIAL INFECTIONS 审中-公开
标题翻译：用于治疗微生物感染的新型氨基化合物
公开(公告)号：WO2005033065A1
公开(公告)日：2005-04-14
申请号：PCT/US2003/027963
申请日：2003-09-05
申请人： UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL , GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC. , TIDWELL, Richard, R. , BOYKIN, David , BRUN, Reto , STEPHENS, Chad, E. , KUMAR, Arvind
发明人： TIDWELL, Richard, R. , BOYKIN, David , BRUN, Reto , STEPHENS, Chad, E. , KUMAR, Arvind
IPC分类号： C07C257/00
CPC分类号： C07C257/18 , C07C259/18 , C07D235/20 , C07D307/52 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D409/14
摘要： Novel amidine and diamidine compounds are useful in the treatment of microbial infections, including mycobacterial, fungal and protozoal infections. Pharmaceutical formulations comprising these compounds can be used in methods of treating microbial infections.
摘要翻译：新型脒和脒化合物可用于治疗微生物感染，包括分枝杆菌，真菌和原生动物感染。包含这些化合物的药物制剂可用于治疗微生物感染的方法。

5. 发明申请

WO01096366A3 Dipeptide inhibitors for the blood-clotting factorxa 审中-公开
标题翻译：用于血液凝固因子的二肽抑制剂
公开(公告)号：WO01096366A3
公开(公告)日：2002-04-25
申请号：PCT/EP2001/006814
申请日：2001-06-15
IPC分类号： A61K38/00 , A61P7/02 , A61P9/00 , A61P43/00 , C07C257/18 , C07C259/18 , C07K5/06 , C07K5/068 , A61K38/04 , C07C257/00
CPC分类号： C07C259/18 , C07C257/18 , C07K5/0606 , C07K5/06069 , C07K5/06086
摘要： The invention relates to derivatives of amidino-benzylamine, especially derivatives of 4-amidino-benzylamine, with two bonded amino acids. These derivatives represent a novel group of highly active and very selective F Xa-inhibitors for treating cardiovascular diseases and thrombotic events.

6. 发明申请

WO01090051A1 PHENYLGLYCINE DERIVATIVES 审中-公开
标题翻译：苯乙烯衍生物
公开(公告)号：WO01090051A1
公开(公告)日：2001-11-29
申请号：PCT/EP2001/005633
申请日：2001-05-17
IPC分类号： A61K31/155 , A61K31/198 , A61K31/216 , A61K31/341 , A61P7/02 , A61P7/04 , A61P9/00 , A61P9/10 , A61P29/00 , A61P35/00 , C07C257/18 , C07C257/20 , C07C259/18 , C07C269/00 , C07C271/64 , C07C273/18 , C07C275/56 , C07D307/20 , C07D317/36
CPC分类号： C07D317/36 , C07C257/18 , C07C259/18 , C07D307/20
摘要： The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula (I) wherein X and R to R are as defined in the description and in the claims, as well as hydrates or solvates and/or physiologically acceptable salts thereof and/or physiologically acceptable esters thereof.
摘要翻译：本发明涉及式（I）的新型N-（4-甲脒基 - 苯基） - 甘氨酸衍生物，其中X和R 1至R 5如说明书和权利要求书中所定义，以及水合物或溶剂化物和/或其生理上可接受的盐和/或其生理上可接受的酯。

7. 发明申请

WO99064397A1 DOUBLE PRODRUGS OF POTENT GPIIb/IIIa ANTAGONISTS 审中-公开
标题翻译： GPIIb / IIIa拮抗剂的双重产物
公开(公告)号：WO99064397A1
公开(公告)日：1999-12-16
申请号：PCT/US1999/011799
申请日：1999-06-07
IPC分类号： C07C259/18 , C07D207/26 , C07D207/273 , A61K31/40
CPC分类号： C07D207/273 , C07C259/18
摘要： The present invention relates to double prodrugs of pharmacologically active glycoprotein IIb/IIIa antagonists of formula (I), wherein R1 is selected from the group consisting of lower alkyl of about 2 to about 8 carbon atoms, cycloalkyl, and aralkyl; R is selected from the group consisting of alkoxy, formula (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), wherein R is H or alkyl; and formula (k), wherein R is H or alkyl; and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及式（I）的药理学活性糖蛋白IIb / IIIa拮抗剂的双重前药，其中R 1选自约2至约8个碳原子的低级烷基，环烷基和芳烷基; 式（a），（b），（c），（d），（e），（f），（g），（h），（i），（j）其中R 50为H或烷基; 和式（k），其中R 50是H或烷基; 及其药学上可接受的盐。

8. 发明申请

WO99014188A1 NOVEL BENZAMIDOXIM DERIVATIVES, INTERMEDIATE PRODUCTS AND METHODS FOR PREPARING THEM, AND THEIR USE AS FUNGICIDES 审中-公开
标题翻译：新benzamideoxime衍生物，及其中间产品和工艺及其作为杀菌剂
公开(公告)号：WO99014188A1
公开(公告)日：1999-03-25
申请号：PCT/EP1998/005618
申请日：1998-09-05
IPC分类号： A01N37/52 , A01N43/10 , C07C259/18 , C07D333/24
CPC分类号： A01N43/10 , A01N37/52 , C07C259/18 , C07D333/24
摘要： The invention concerns benzamidoxim derivatives of formula (I) in which the substituents have the following meanings: R represents hydrogen or fluorine; R represents C1-C6 phenyl-alkyl, bearing on the cyclic phenyl compound one or several substituents selected in the group comprising halogen, C1-C4 alkyl, C1-C4 alkyl halide, C1-C4 alkoxy or C1-C4 alkoxy halide, or C1-C4 thienyl-alkyl, optionally bearing one or several substituents selected in the group comprising halogen, C1-C4 alkyl, C1-C4 alkyl halide, C1-C4 alkoxy or C1-C4 alkoxy halide, or C1-C4 pyrazol-alkyl, optionally bearing one or several substituents selected in the group comprising halogen, C1-C4 alkyl, C1-C4 alkyl halide, C1-C4 alkoxy or C1-C4 alkoxy halide.
摘要翻译：式（I），其中取代基具有以下含义的苄胺肟衍生物：R t <1>是氢或氟，R <2>苯基-C 1 -C 6 - 烷基，其包含选自苯环上的组中的一个或多个取代可以从携带卤素，C1-C4烷基，C1-C4卤代烷基，C1-C4烷氧基或C1-C4卤代烷氧基，或噻吩基-C 1 -C 4 - 烷基，其中任选地一个或多个取代基选自由可以从携带卤素，C1-C4烷基，C1-C4卤代烷基，C1-C4烷氧基或C1-C4卤代烷氧基，或吡唑基-C 1 -C 4 - 烷基，其中任选地一个或多个取代基选自由可以从卤素，C1-C4烷基，C1-C4卤代烷基，C1-C4烷氧基或C1-C4卤代烷氧基携带。

9. 发明申请

WO99000127A1 ANTITHROMBOTIC AGENTS 审中-公开
公开(公告)号：WO99000127A1
公开(公告)日：1999-01-07
申请号：PCT/US1998/013424
申请日：1998-06-26
IPC分类号： C07D333/40 , A61K31/00 , A61K31/167 , A61K31/196 , A61K31/216 , A61K31/27 , A61K31/381 , A61K31/4035 , A61K31/423 , A61K31/445 , A61K31/4545 , A61P7/02 , C07C257/18 , C07C259/18 , C07C271/64 , C07C271/66 , C07D209/44 , C07D211/60 , C07D261/20 , C07D333/38 , C07D401/04 , A61K31/38 , A61K31/165 , A61K31/40 , A61K31/42 , C07C233/64 , C07D211/32 , C07D333/06
CPC分类号： C07C271/66 , A61K31/00 , C07C257/18 , C07C259/18 , C07C271/64 , C07D209/44 , C07D211/60 , C07D261/20 , C07D333/38
摘要： This application relates to a compound of formula (I) (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

10. 发明申请

WO99000121A1 ANTITHROMBOTIC AGENTS 审中-公开
标题翻译：抗血栓药物
公开(公告)号：WO99000121A1
公开(公告)日：1999-01-07
申请号：PCT/US1998/013427
申请日：1998-06-26
IPC分类号： C07D295/18 , A61K31/167 , A61K31/18 , A61K31/216 , A61K31/235 , A61K31/27 , A61K31/36 , A61K31/381 , A61K31/403 , A61K31/4035 , A61K31/42 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/445 , A61K31/4465 , A61K31/4525 , A61K31/4535 , A61K31/4545 , A61K31/5375 , A61P7/02 , C07C233/75 , C07C233/80 , C07C235/42 , C07C235/56 , C07C235/84 , C07C237/40 , C07C237/42 , C07C237/44 , C07C257/18 , C07C259/18 , C07C307/10 , C07C311/08 , C07C311/09 , C07C311/16 , C07C311/21 , C07C317/44 , C07C317/50 , C07C323/62 , C07D209/48 , C07D209/58 , C07D209/64 , C07D209/66 , C07D211/22 , C07D211/34 , C07D211/46 , C07D211/62 , C07D211/78 , C07D211/96 , C07D213/30 , C07D213/56 , C07D213/70 , C07D213/74 , C07D213/75 , C07D233/60 , C07D261/10 , C07D277/20 , C07D277/38 , C07D277/56 , C07D295/185 , C07D307/84 , C07D307/85 , C07D317/58 , C07D317/66 , C07D333/68 , C07D333/70 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/14 , C07D417/06 , A61K31/165 , A61K31/335 , A61K31/34 , A61K31/38 , A61K31/40 , A61K31/525 , C07C233/64 , C07C307/02 , C07D209/56 , C07D211/32 , C07D211/82 , C07D265/30 , C07D317/46 , C07D333/56 , C07D357/80
CPC分类号： C07D209/48 , C07C233/75 , C07C235/56 , C07C237/40 , C07C237/42 , C07C237/44 , C07C257/18 , C07C259/18 , C07C307/10 , C07C311/08 , C07C311/09 , C07C311/16 , C07C311/21 , C07C317/44 , C07C317/50 , C07C2603/18 , C07D209/58 , C07D209/64 , C07D211/22 , C07D211/34 , C07D211/46 , C07D211/62 , C07D211/78 , C07D211/96 , C07D213/30 , C07D213/56 , C07D213/70 , C07D213/75 , C07D261/10 , C07D277/56 , C07D295/185 , C07D307/85 , C07D317/58 , C07D333/70 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/14 , C07D417/06
摘要： This application relates to a compound of formula (I) (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
摘要翻译：本发明涉及如说明书中所定义的式（I）化合物（或其前药或其药学上可接受的盐或其前药），含有该化合物的药物组合物，该化合物作为Xa因子抑制剂的用途，制备该化合物的方法以及用于制备所述化合物的中间体。

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