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21. 发明授权

US07074787B2 Microbiocidal N-phenyl-N-[4-(4-pyridyl-2-pyrimidin-2-yl]-amine derivatives 失效
公开(公告)号：US07074787B2
公开(公告)日：2006-07-11
申请号：US10451930
申请日：2001-12-20
申请人： Martin Eberle , Hugo Ziegler , Fredrik Cederbaum , Peter Ackermann , Anita Schnyder
发明人： Martin Eberle , Hugo Ziegler , Fredrik Cederbaum , Peter Ackermann , Anita Schnyder
IPC分类号： C07D401/04 , C07D413/04 , A01N43/54
CPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D419/14
摘要： The invention relates to novel N-phenyl-4-(4-pyridyl)-2-pyrimidineamine derivatives of the general formula (I) wherein the sum of (m+p) together is 0, 1, 2 or 3; n and q are independently of each other 0 or 1, and the sum of (m+p+q) together is 1, 2, 3 or 4; R1 is hydrogen, halogen, alkoxy, haloalkyl, haloalkoxy or alkyl; R2 is hydrogen, C1–C6-alkyl, C1–C6-haloalkyl or C1–C6-alkoxy; R2A is hydrogen, C1–C6-alkyl, C3–C4-alkenyl or C3–C4-alkynyl; each of R3, R4, R5 and R6 is, independently of the others, hydrogen, C1–C6-alkyl, C1–C6-haloalkyl, hydroxy-C1–C6-alkyl or C1–C6-alkoxy-C1–C6-alkyl, or the ring members CR3R4 or CR5R6 or CR2R2A are independently of each other a carbonyl group (C═O) or a group C═S; X is C═O, C═S, S═O or O═S═O; Y is O, S, C═O, CH2, —N(R8)—, —O—N(R8)—, —N(R8)—O— or NH—; R7 is hydrogen, C1–C4-alkyl, C3–C4-alkenyl, C3–C4-alkynyl, —CH2OR8, CH2SR8, —C(O)R8, —C(O)OR8, SO2R8, SOR8 or SR8; and R8 is C1–C8-alkyl, C1–C8-alkoxyalkyl, C1–C8 haloalkyl or phenylC1–C2-alkyl wherein the phenyl may be substituted by up to three groups selected from halo or C1–C4-alkyl; or a salt thereof. The invention also relates to the preparation of the compounds and to agrochemical compositions comprising at least one of those compounds as active ingredient as well as the preparation of the said compositions and to the use of the compounds or of the compositions in controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi.

22. 发明授权

US07951957B2 Substituted benzimidazoles and their use for inducing apoptosis 有权
标题翻译：取代的苯并咪唑及其诱导凋亡的用途
公开(公告)号：US07951957B2
公开(公告)日：2011-05-31
申请号：US12173869
申请日：2008-07-16
申请人： Martin Eberle , Felix Bachmann , Alessandro Strebel , Subho Roy , Sudhir Srivastava , Goutam Saha
发明人： Martin Eberle , Felix Bachmann , Alessandro Strebel , Subho Roy , Sudhir Srivastava , Goutam Saha
IPC分类号： A61K31/4184 , C07D403/04
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04
摘要： The invention relates to compounds of formula (I) wherein R represents aryl or heteroaryl, X is a bond, a carbonyl group, a derivative of a carbonyl group, an ethylene group or an ethylenecarbonyl group, R1 is optionally substituted amino or hydroxy, and the substituents R2 to R6 have the meanings given in the specification, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to intermediates, to the use of a compounds of formula (I) as a medicament and for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same.
摘要翻译：本发明涉及式（I）化合物，其中R表示芳基或杂芳基，X为键，羰基，羰基衍生物，亚乙基或亚乙基羰基，R 1为任选取代的氨基或羟基，以及取代基R 2至R 6具有本说明书中给出的含义，这些化合物的合成方法，含有式（I）化合物的药物组合物，中间体，使用式（I）化合物作为药物，和用于制备用于治疗肿瘤和自身免疫疾病的药物组合物，以及使用这样的式（I）化合物或含有其的药物组合物治疗肿瘤和自身免疫性疾病的方法。

23. 发明授权

US07368479B2 Alpha-sulfonylamino-acetonitriles 有权
公开(公告)号：US07368479B2
公开(公告)日：2008-05-06
申请号：US10517977
申请日：2003-06-18
申请人： Martin Eberle , Daniel Stierli , Urs Müller
发明人： Martin Eberle , Daniel Stierli , Urs Müller
IPC分类号： A61K31/275 , C07C255/00
CPC分类号： C07D207/27 , A01N41/06 , A01N43/36 , A01N43/40 , A01N43/50 , A01N43/56 , A01N43/653 , A01N43/78 , C07C311/13 , C07C317/20 , C07C323/20 , C07D213/30 , C07D213/643 , C07D213/85 , C07D231/12 , C07D233/54 , C07D239/26 , C07D239/42 , C07D239/60 , C07D241/42 , C07D249/08 , C07D271/10 , C07D277/24 , C07D277/34 , C07D277/36 , C07D277/42 , C07D285/08 , C07D285/12 , C07D295/205 , C07D295/215
摘要： The invention relates to α-sulfonylamino-acetonitrile derivatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein Ar1, and Ar2 independently of each other stand for an optionally substituted aryl or heteroaryl group, R1, and R2 stand independently of each other for hydrogen, optionally substituted C1,-C5alkyl, optionally substituted C2-C5alkenyl, C2-C5alkynyl or optionally substituted C3-C6cycloalkyl; R3 designates hydrogen, C3-C5alkenyl, C3-C5alkynyl or optionally substituted C1,-C5alkyl; R4 is optionally substituted C1,-C5alkyl, optionally substituted C2-C5alkenyl, C2-C5alkynyl or optionally substituted C3-C6cycloalkyl; R5 and R6 are independently of each other hydrogen or optionally substituted C1-C5alkyl, optionally substituted C2-C5alkenyl, C2-C5alkynyl or optionally substituted C3-C6cycloalkyl; R7, and R8 are independently of each other hydrogen or optionally substituted C1,-C5alkyl, optionally substituted C2-C5alkenyl, C2-C5alkynyl or optionally substituted C3-C6cycloalkyl; W designates a bridge selected from —O— —S(O)m— or —NR3—; X designates a direct bond or a bridge selected from —O—, —S(O)m— or —NR3—; a and b independently of each other stand for a number 1, 2 or 3; and c and m independently of each other stand for a number zero, 1 or 2. These compounds possess useful plant protecting properties and may advantageously be employed in agricultural practice for controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi.

24. 发明申请

US20070060570A1 Sulfopyrroles 有权
标题翻译：硫磺吡咯
公开(公告)号：US20070060570A1
公开(公告)日：2007-03-15
申请号：US10557664
申请日：2004-05-24
申请人： Martin Eberle , Daniel Obrecht , Philipp Ermert , Franck Lach , Anatol Luther , Felix Bachmann , Alessandro Strebel
发明人： Martin Eberle , Daniel Obrecht , Philipp Ermert , Franck Lach , Anatol Luther , Felix Bachmann , Alessandro Strebel
IPC分类号： A61K31/55 , A61K31/454 , A61K31/4015 , A61K31/4025 , C07D403/02
CPC分类号： C07D401/04 , C07D207/48 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： The invention relates to compounds of formula (I) wherein R1 represents aryl, aralkyl or heteroaryl, R2 is aryl or heteroaryl and R3 is aryl, heteroaryl or optionally substituted aminomethyl, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to the use of a compounds of formula (I) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using compounds of formula (I) or of pharmaceutical compositions containing same.
摘要翻译：本发明涉及其中R 1表示芳基，芳烷基或杂芳基，R 2是芳基或杂芳基和R 3'的式（I）化合物，是将芳族，杂芳基或任选取代的氨基甲基与合成式（I）化合物的药物组合物的合成方法，涉及式（I）化合物用于制备用于治疗肿瘤和自身免疫疾病，以及使用式（I）化合物或含有其的药物组合物治疗肿瘤和自身免疫性疾病的方法。

25. 发明授权

US06949669B2 Organic compounds 失效
标题翻译：有机化合物
公开(公告)号：US06949669B2
公开(公告)日：2005-09-27
申请号：US10181878
申请日：2001-01-23
申请人： Gerald Wayne Craig , Martin Eberle , Martin Zeller , Steven Scott Bondy , Daniel Dennis Comer , Soan Cheng , Julie Elizabeth Penzotti , Peter Grootenhuis , Jürg Ehrler
发明人： Gerald Wayne Craig , Martin Eberle , Martin Zeller , Steven Scott Bondy , Daniel Dennis Comer , Soan Cheng , Julie Elizabeth Penzotti , Peter Grootenhuis , Jürg Ehrler
IPC分类号： A01N37/34 , A01N37/38 , A01N37/40 , A01N37/48 , A01P13/00 , C07C17/14 , C07C43/215 , C07C43/225 , C07C43/23 , C07C47/575 , C07C49/84 , C07C69/734 , C07C69/736 , C07C69/76 , C07C205/35 , C07C205/37 , C07C217/48 , C07C217/60 , C07C217/76 , C07C251/48 , C07C255/37 , C07C255/46 , C07C255/54 , C07D209/48 , C07C255/01 , C07C255/45 , C07C255/49
CPC分类号： C07D209/48 , A01N37/38 , A01N37/40 , A01N37/48 , C07C17/14 , C07C43/215 , C07C43/225 , C07C43/23 , C07C47/575 , C07C49/84 , C07C69/734 , C07C69/736 , C07C69/76 , C07C205/35 , C07C205/37 , C07C217/48 , C07C217/60 , C07C217/76 , C07C251/48 , C07C255/37 , C07C255/46 , C07C255/54 , C07C2601/02 , C07C25/02
摘要： Compounds of general formula (I) wherein the substituents are as defined in claim 1 are suitable for use as herbicides
摘要翻译：其中取代基如权利要求1中所定义的通式（I）的化合物适合用作除草剂

26. 发明申请

US20050156082A1 Apparatus and method for lighter-than-air aircraft 失效
标题翻译：用于轻型飞机的装置和方法
公开(公告)号：US20050156082A1
公开(公告)日：2005-07-21
申请号：US10752425
申请日：2004-01-06
申请人： Martin Eberle , Tim Rabel
发明人： Martin Eberle , Tim Rabel
IPC分类号： B64B1/02 , B64B1/58 , B64B1/66 , B64F1/14
CPC分类号： B64F1/14 , B64B1/58 , B64B1/66
摘要： An apparatus and associated method for launching and recovering a lighter-than-air aircraft are provided. The aircraft includes an envelope that is substantially filled before launch with a lift gas and a second gas. The lift gas and second gas are substantially separated in the envelope by a boundary layer of mixed gas, formed by the lift and second gases. The aircraft is supported by one or more masts as the lift gas is injected to achieve the required buoyancy for launch. The aircraft is then released and rises, for example, in an inclined orientation. As the aircraft climbs, the lift gas expands in the envelope, and the second gas is vented therefrom. During horizontal descent, air can be pumped into the envelope to maintain the envelope in a substantially filled configuration. The air and lift gas can be mixed to avoid sloshing and pooling.
摘要翻译：提供了一种用于发射和恢复轻型飞机的装置和相关方法。该飞机包括一个信封，其在发射之前用提升气体和第二个气体基本上被填充。提升气体和第二气体通过由升力和第二气体形成的混合气体的边界层在壳体中基本分离。飞机由一个或多个桅杆支撑，因为提升气体被注入以实现所需的浮力用于发射。然后飞机被释放并且例如以倾斜的方向上升。当飞机爬升时，提升气体在信封中膨胀，并且第二气体从其中排出。在水平下降期间，可以将空气泵送到信封中，以将信封保持在基本上充满的配置。空气和提升气体可以混合，以避免晃动和汇集。

27. 发明申请

US20050038059A1 Thiazolyl substituted aminopyrimidines as plant protection agents 失效
标题翻译：噻唑基取代的氨基嘧啶作为植物保护剂
公开(公告)号：US20050038059A1
公开(公告)日：2005-02-17
申请号：US10491231
申请日：2002-09-19
申请人： Urs Mueller , Martin Eberle , Christian Pillonel , William Lutz , Peter Stanetty
发明人： Urs Mueller , Martin Eberle , Christian Pillonel , William Lutz , Peter Stanetty
IPC分类号： A01N43/78 , A01N53/00 , C07D417/04 , C07D417/14 , A61K31/506
CPC分类号： C07D417/04 , A01N43/78 , A01N53/00 , C07D417/14
摘要： Compounds of formula (I), or a salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, and R8 are specified organic redicals; and compositions containing them, processes for making them and their use as fungicides.
摘要翻译：式（I）化合物或其盐，其中R1，R2，R3，R4，R5，R6，R7和R8是指定的有机红; 含有它们的组合物，制备它们的方法及其作为杀真菌剂的用途。

28. 发明授权

US5807863A 2-(4-pyrazolyloxy-pyrimidin-5-yl) acetic acid derivatives 失效
标题翻译： 2-（4-吡唑氧基 - 嘧啶-5-基）乙酸衍生物
公开(公告)号：US5807863A
公开(公告)日：1998-09-15
申请号：US715980
申请日：1996-09-19
申请人： Martin Eberle , Clemens Lamberth , Fritz Schaub
发明人： Martin Eberle , Clemens Lamberth , Fritz Schaub
IPC分类号： C07D239/34 , A01N43/54 , A01N43/56 , A01N43/76 , A01N43/78 , C07D231/02 , C07D231/08 , C07D231/10 , C07D231/22 , C07D239/24 , C07D401/14 , C07D403/12 , C07D409/14 , C07D413/14 , C07D417/14
CPC分类号： C07D401/14 , A01N43/56 , A01N43/76 , A01N43/78 , C07D231/08 , C07D231/22 , C07D403/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要： This invention relates to novel 2-(4-pyrazolyloxy-pyrimidin-5-yl) acetic acid derivatives of formula I ##STR1## wherein R.sub.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.3-6 cycloalkyl, or di-C.sub.1-4 alkylamino, R.sub.2 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, or di-C.sub.1-4 alkyl-amino, R.sub.3 is hydrogen or methyl, R.sub.4 is aryl, aryl-C.sub.1-4 alkyl, heteroaryl, or heteroaryl-C.sub.1-4 alkyl, wherein each of the aromatic rings may be optionally substituted; and X is CH or nitrogen; the use of such compounds for the control of phytopathogens, compositions for facilitating such use, and the preparation of the compounds of formula I.
摘要翻译：本发明涉及式I（I）的新的2-（4-吡唑氧基 - 嘧啶-5-基）乙酸衍生物，其中R 1是氢，C 1-4烷基，C 1-4烷氧基，C 1-4烷硫基，C 3-6环烷基，或二-C 1-4烷基氨基，R 2是氢，C 1-4烷基，C 1-4烷氧基，C 1-4烷硫基或二-C 1-4烷基 - 氨基，R 3是氢或甲基，R 4是芳基，芳基-C 1-4烷基，杂芳基或杂芳基-C 1-4烷基，其中每个芳环可以任选被取代; X为CH或氮; 使用这些化合物来控制植物病原体，促进这种用途的组合物和式I化合物的制备。

29. 发明授权

US5783580A .alpha.-pyrimidinyl acrylic acid derivatives 失效
标题翻译： α-嘧啶基丙烯酸衍生物
公开(公告)号：US5783580A
公开(公告)日：1998-07-21
申请号：US652865
申请日：1996-05-23
申请人： Martin Eberle , Fritz Schaub , Gerald Wayne Craig
发明人： Martin Eberle , Fritz Schaub , Gerald Wayne Craig
IPC分类号： A01N43/54 , A01N43/78 , A01N43/80 , C07D239/46 , C07D239/52 , C07D405/12 , C07D413/12 , C07D417/12 , C07D521/00 , C07D239/47
CPC分类号： C07D239/47 , A01N43/54 , A01N43/78 , A01N43/80 , C07D231/12 , C07D233/56 , C07D239/52 , C07D249/08 , C07D405/12 , C07D413/12 , C07D417/12
摘要： This invention relates to compounds of formula I ##STR1## wherein R.sup.1 is C.sub.1-4 alkoxy or --NR.sup.8 R.sup.9 ; R.sup.2 is heteroaryl, heteroaryloxy or a group ##STR2## R.sup.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, cyano, nitro or halogen; R.sup.4 is hydrogen, halogen, C.sub.1-4 alkoxy or C.sub.1-4 alkyl; R.sup.5 is hydrogen or methyl; R.sup.7 is hydrogen or methyl; R.sup.8 and R.sup.9 are independently C.sub.1-4 alkyl or together C.sub.3-6 alkylene; E is C.sub.1-3 alkylene; X is CH or nitrogen; and Y is OCH.sub.3, NH.sub.2, NHCH.sub.3 or N(CH.sub.3).sub.2.
摘要翻译：本发明涉及式Ⅰ化合物其中R 1是C 1-4烷氧基或-NR 8 R 9; R 2是杂芳基，杂芳氧基或基团R 3是氢，C 1-4烷基，C 1-4烷氧基，氰基，硝基或卤素; R4是氢，卤素，C1-4烷氧基或C1-4烷基; R5是氢或甲基; R7是氢或甲基; R 8和R 9独立地为C 1-4烷基或C 3-6亚烷基; E为C1-3亚烷基; X是CH或氮; Y是OCH 3，NH 2，NHCH 3或N（CH 3）2。

30. 发明授权

US08288421B2 Phenylaminopyridines 有权
标题翻译：苯基氨基吡啶
公开(公告)号：US08288421B2
公开(公告)日：2012-10-16
申请号：US11662047
申请日：2005-09-05
申请人： Martin Eberle , Felix Bachmann , Alessandro Strebel , Subho Roy , Goutam Saha , Godhuli Nandi
发明人： Martin Eberle , Felix Bachmann , Alessandro Strebel , Subho Roy , Goutam Saha , Godhuli Nandi
IPC分类号： A61K31/44 , A61P43/00 , C07D213/04
CPC分类号： C07D213/74 , C07D241/20 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The invention relates to novel substituted 3-phenylamino-5-(3-aminophenyl)pyridines and corresponding pyrazines of formula (I), wherein A is CH or N, R1 represents C(═O)R9, S(═O)2R10, P(═O)(OR11)2, optionally substituted phenyl or optionally substituted heteroaryl, and the other substituents have the meaning described in the specification, processes for the preparation thereof, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of neoplastic diseases and autoimmune diseases, and a method for the treatment of such a diseases.
摘要翻译：本发明涉及式（I）的新的取代的3-苯基氨基-5-（3-氨基苯基）吡啶和相应的吡嗪，其中A是CH或N，R1代表C（= O）R 9，S（= O）2 R 10， P（= O）（OR 11）2，任选取代的苯基或任选取代的杂芳基，其它取代基具有说明书中描述的含义，其制备方法，含有它们的药物组合物，其用途任选地与一种或用于治疗肿瘤性疾病和自身免疫性疾病的更多其它药物活性化合物，以及治疗这种疾病的方法。

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