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1. 发明申请

WO2008131859A3 USE OF CYCLICALLY SUBSTITUTED FUROPYRIMIDINE DERIVATIVES FOR TREATING PULMONARY ARTERIAL HYPERTONIA 审中-公开
标题翻译： VERWENDIMG环状的取代furopyrimidine衍生物对肺动脉高血压的治疗
公开(公告)号：WO2008131859A3
公开(公告)日：2009-07-16
申请号：PCT/EP2008003008
申请日：2008-04-16
申请人： BAYER SCHERING PHARMA AG , LAMPE THOMAS , BECKER EVA-MARIA , KAST RAIMUND , BECK HARTMUT , JESKE MARIO , SCHUHMACHER JOACHIM , STOLL FRIEDERIKE , KLEIN MARTINA , AKBABA METIN , KNORR ANDREAS , STASCH JOHANNES-PETER , BAERFACKER LARS , HILLISCH ALEXANDER , KARIG GUNTER , MEININGHAUS MARK , SCHLEMMER KARL-HEINZ , SCHOHE-LOOP RUDOLF
发明人： LAMPE THOMAS , BECKER EVA-MARIA , KAST RAIMUND , BECK HARTMUT , JESKE MARIO , SCHUHMACHER JOACHIM , STOLL FRIEDERIKE , KLEIN MARTINA , AKBABA METIN , KNORR ANDREAS , STASCH JOHANNES-PETER , BAERFACKER LARS , HILLISCH ALEXANDER , KARIG GUNTER , MEININGHAUS MARK , SCHLEMMER KARL-HEINZ , SCHOHE-LOOP RUDOLF
IPC分类号： A61K31/519 , A61P9/12 , A61P11/00
CPC分类号： A61K31/519
摘要： The invention relates to the use of cyclically substituted furopyrimidine derivatives of formula (I) for the treatment and/or prophylaxis of pulmonary arterial hypertonia and other forms of pulmonary hypertonia and to the use of said derivatives for producing medicaments for the treatment and/or prophylaxis of pulmonary arterial hypertonia and other forms of pulmonary hypertonia.
摘要翻译：本申请涉及使用式（I）为肺动脉高血压和其他形式的肺动脉高压以及它们用于制备药物用于治疗肺动脉高血压的治疗和/或预防中的用途在治疗和/或预防的环状取代furopyrimidine衍生物的和其他形式的肺动脉高压。

2. 发明申请

WO2008131858A2 USE OF ACYCLICALLY SUBSTITUTED FUROPYRIMIDINE DERIVATIVES FOR TREATING PULMONARY ARTERIAL HYPERTONIA 审中-公开
标题翻译：取代无环furopyrimidine衍生物用于肺动脉高压BENHANDLUNG USE
公开(公告)号：WO2008131858A2
公开(公告)日：2008-11-06
申请号：PCT/EP2008003007
申请日：2008-04-16
申请人： BAYER HEALTHCARE AG , LAMPE THOMAS , BECKER EVA-MARIA , KAST RAIMUND , BECK HARTMUT , JESKE MARIO , SCHUHMACHER JOACHIM , STOLL FRIEDERIKE , KLEIN MARTINA , AKBABA METIN , KNORR ANDREAS , STASCH JOHANNES-PETER , BAERFACKER LARS , HILLISCH ALEXANDER , KARIG GUNTER , MEININGHAUS MARK , SCHLEMMER KARL-HEINZ , SCHOHE-LOOP RUDOLF
发明人： LAMPE THOMAS , BECKER EVA-MARIA , KAST RAIMUND , BECK HARTMUT , JESKE MARIO , SCHUHMACHER JOACHIM , STOLL FRIEDERIKE , KLEIN MARTINA , AKBABA METIN , KNORR ANDREAS , STASCH JOHANNES-PETER , BAERFACKER LARS , HILLISCH ALEXANDER , KARIG GUNTER , MEININGHAUS MARK , SCHLEMMER KARL-HEINZ , SCHOHE-LOOP RUDOLF
IPC分类号： A61K31/519 , A61P9/12 , A61P11/00
CPC分类号： A61K31/519
摘要： The invention relates to the use of acyclically substituted furopyrimidine derivatives of formula (I) for the treatment and/or prophylaxis of pulmonary arterial hypertonia and other forms of pulmonary hypertonia and to the use of said derivatives for producing medicaments for the treatment and/or prophylaxis of pulmonary arterial hypertonia and other forms of pulmonary hypertonia.
摘要翻译：本申请涉及使用无环的用于治疗和/或肺动脉高血压和其他形式的肺动脉高压以及它们用于制备药物用于治疗肺动脉高血压的治疗和/或预防中的用途预防取代的式（I）的Furopyrimidin-衍生物和其他形式的肺动脉高压。

3. 发明申请

WO2012084857A3 METHOD FOR PRODUCING 2-(TRIAZINYLCARBONYL) SULFONANILIDES 审中-公开
标题翻译： 2-（三苄基羰基）磺酰苯胺的制备方法
公开(公告)号：WO2012084857A3
公开(公告)日：2012-08-16
申请号：PCT/EP2011073287
申请日：2011-12-19
申请人： BAYER CROPSCIENCE AG , KARIG GUNTER , FORD MARK JAMES , SIEGEL KONRAD
发明人： KARIG GUNTER , FORD MARK JAMES , SIEGEL KONRAD
IPC分类号： C07D403/04 , A01N43/66 , C07D251/20
CPC分类号： C07D251/20 , A01N43/66 , C07D403/04
摘要： The invention relates to a method, which is based on the oxidative ring opening of a compound with an oxindole structure, for producing substituted 2-(triazinylcarbonyl) sulfonanilides of formula (1-1) proceeding from an N-sulfonyl-substituted 3-triazinyl oxindole of formula (2-1), to the thus produced 2-(triazinylcarbonyl) sulfonanilides of formula (1-1), and to the use thereof as intermediate products for the synthesis of fine chemicals and active substances in the agricultural field. Furthermore, the invention relates to a multistage method for producing N-alkyl-N-[2-(1,3,5-triazin-2-ylcarbonyl)phenyl]alkansulfonamides of formula (4-1) proceeding from a 3-(alkylsulfanyl)-1,3-dihydro-2H-indol-2-on of formula (7-1), wherein the multistage method also has said oxidative opening as a sub-step, and to the 2-(triazinylcarbonyl) sulfonanilides of formula (1-1), said sulfonanilides being obtained by means of the oxidative ring opening and used as intermediates in the multistage method.
摘要翻译：本申请涉及一种方法，该方法是基于具有Oxindolstruktur的化合物的氧化开环，制备式（1-1）的取代的2-（Triazinylcarbonyl）sulfonaniliden的制备从N-3-sulfonylsubstituierten Triazinyloxindol启动式（2-1）和如此制备的式（1-1）的2-（三嗪基 - 羰基）磺酰苯胺及其作为用于合成农业中的精细化学品和活性成分的中间体的用途。此外，本发明涉及一种多级方法用于制备N-烷基-N- [2-（1,3,5-三嗪-2-基羰基）苯基]从3-（烷基硫基）启动式（4-1）的alkanesulfonamides -1,3-二氢-2H-吲哚-2-酮的式（7-1），其中，所述多阶段工艺包括如步骤的一部分的，所述式氧化开环和通过氧化开环得到的2-（Triazinylcarbonyl）磺酰苯胺（1-1），它们在多阶段过程中用作中间体。

4. 发明申请

WO2012084855A3 METHOD FOR PRODUCING TRIAZINYL-SUBSTITUTED OXINDOLES 审中-公开
标题翻译：用于生产TRIAZINYLSUBSTITUIERTEN吲哚酮
公开(公告)号：WO2012084855A3
公开(公告)日：2012-09-07
申请号：PCT/EP2011073283
申请日：2011-12-19
申请人： BAYER CROPSCIENCE AG , KARIG GUNTER , FORD MARK JAMES , SIEGEL KONRAD
发明人： KARIG GUNTER , FORD MARK JAMES , SIEGEL KONRAD
IPC分类号： C07D403/04
CPC分类号： C07D403/04 , A01N43/66 , C07D403/12 , C07D405/04
摘要： The invention relates to a method for producing triazinyl-substituted oxindoles of formula (3) and the salts thereof by reacting an oxindole (1) with a triazine (2) in the presence of a carbonate, a hydroxide, a phosphate, or a mixture of a plurality of said compounds, to the compounds of the general formula (3) and the salts (3'') thereof, and to the use of both for producing plant protecting agents.
摘要翻译：一种用于通过羟吲哚（1）用在碳酸盐，氢氧化物，磷酸盐或几种上述化合物的混合物，和一般的化合物的存在下的三嗪（2）反应，从而制造式（3）的triazinylsubstituierten羟吲哚和它们的盐的过程式（3）和它们的盐（3“”）和用于作物保护剂的制备中的用途两者。

5. 发明申请

WO2010127786A8 METHOD FOR PRODUCING OXINDOLES AND ORTHO-SUBSTITUTED ANILINES AND THE USE THEREOF AS INTERMEDIATE PRODUCTS FOR SYNTHESES 审中-公开
标题翻译：用于生产的羟吲哚和邻位取代的苯胺及其用作合成中间体
公开(公告)号：WO2010127786A8
公开(公告)日：2011-11-10
申请号：PCT/EP2010002566
申请日：2010-04-27
申请人： BAYER CROPSCIENCE AG , FORD MARK JAMES , KARIG GUNTER
发明人： FORD MARK JAMES , KARIG GUNTER
IPC分类号： C07C319/20 , C07C323/58 , C07D209/30 , C07D209/34
CPC分类号： C07D209/34 , C07C323/58
摘要： The invention relates to a method for producing oxindoles and ortho-substituted anilines and the use thereof as intermediate products for syntheses. Method for producing compounds of the formula (4): wherein a mixture of an aniline (compound of the formula Q) is converted with a thioether (compound of the formula W) in the presence of a chlorinating agent and an organic solvent at a reaction temperature in the range from -60° to -10°C. In a subsequent method, said compound is further converted in the presence of an acid catalyst to the indole of the formula (7) or the oxindole of the formula (8).
摘要翻译：一种用于吲哚酮和邻 - 取代的苯胺的制备以及它们作为中间体的式I化合物的制备使用用于合成处理方法（4）：其中苯胺（式Q的化合物）与硫醚（式W的化合物）的混合物中：在氯化剂的在-60℃-10℃之间和°的范围存在下和在反应温度下的有机溶剂在随后的过程中，该化合物进一步与式（7）的吲哚或式（8）的在酸催化剂的存在下的羟吲哚进行反应。

6. 发明申请

WO2006063811A3 SUBSTITUTED 1,2,4-TRIAZIN-5(2H)-ONES 审中-公开
标题翻译：取代的1,2,4-三嗪-5（2H） - 酮
公开(公告)号：WO2006063811A3
公开(公告)日：2006-09-08
申请号：PCT/EP2005013431
申请日：2005-12-14
申请人： BAYER HEALTHCARE AG , HENDRIX MARTIN , ZIMMERMANN KATJA , HIRTH-DIETRICH CLAUDIA , KARIG GUNTER , KARTHAUS DAGMAR , RAABE MARTIN , WEBER OLAF , ZAISS SIEGFRIED
发明人： HENDRIX MARTIN , ZIMMERMANN KATJA , HIRTH-DIETRICH CLAUDIA , KARIG GUNTER , KARTHAUS DAGMAR , RAABE MARTIN , WEBER OLAF , ZAISS SIEGFRIED
IPC分类号： C07D253/06 , A61K31/53 , A61P9/10 , A61P17/06 , A61P29/00 , C07D401/12
CPC分类号： C07D401/12 , C07D253/07 , C07D253/075
摘要： The invention relates to substituted 1,2,4-triazin-5(2H)-ones, to a method for the production thereof, and to their use for producing medicaments for treating and/or preventing diseases, particularly chronic inflammatory diseases, for example, rheumatoid diseases and cardiovascular diseases, such as dyslipidaemias, arteriosclerosis, and coronary heart diseases.
摘要翻译：本发明涉及取代的1,2,4-三嗪-5（2H） - 酮和它们的制备方法和它们用于制备药物用于治疗和/或预防疾病的用途，特别是慢性炎症性疾病如流程疾病类风湿性疾病，和心血管疾病，如血脂异常，动脉粥样硬化和冠心病心脏疾病。

7. 发明申请

WO2008019784A8 AVERMECTIN DERIVATIVES 审中-公开
标题翻译：阿维菌素衍生物
公开(公告)号：WO2008019784A8
公开(公告)日：2009-07-23
申请号：PCT/EP2007006991
申请日：2007-08-08
申请人： BAYER CROPSCIENCE AG , JESCHKE PETER , KARIG GUNTER , VELTEN ROBERT , FISCHER REINER , MALSAM OLGA , GOERGENS ULRICH , ARNOLD CHRISTIAN , SANWALD ERICH , HARDER ACHIM , TURBERG ANDREAS
发明人： JESCHKE PETER , KARIG GUNTER , VELTEN ROBERT , FISCHER REINER , MALSAM OLGA , GOERGENS ULRICH , ARNOLD CHRISTIAN , SANWALD ERICH , HARDER ACHIM , TURBERG ANDREAS
IPC分类号： C07H17/08 , A01N43/90 , C07H13/02
CPC分类号： C07H17/08 , A01N43/90 , C07H13/02
摘要： Disclosed are novel avermectin derivatives of formula (I), wherein -C22R1-A-C23R2, R3, R4, and R5 have the meanings indicated in the description, methods for producing said substances, the use thereof for controlling animal pests, novel intermediate products, and the production thereof.
摘要翻译：式（I）的新除虫菌素衍生物，其中-C22R1-A-C23R2，R3，R4和R5具有说明书中给出的含义，用于制备这些物质和它们在防治动物害虫，以及新的中间体和它们的制备使用的方法。

8. 发明申请

WO2008019784A3 AVERMECTIN DERIVATIVES 审中-公开
标题翻译：阿维菌素衍生物
公开(公告)号：WO2008019784A3
公开(公告)日：2008-09-25
申请号：PCT/EP2007006991
申请日：2007-08-08
申请人： BAYER CROPSCIENCE AG , JESCHKE PETER , KARIG GUNTER , VELTEN ROBERT , FISCHER REINER , MALSAM OLGA , GOERGENS ULRICH , ARNOLD CHRISTIAN , SANWALD ERICH , HARDER ACHIM , TURBERG ANDREAS
发明人： JESCHKE PETER , KARIG GUNTER , VELTEN ROBERT , FISCHER REINER , MALSAM OLGA , GOERGENS ULRICH , ARNOLD CHRISTIAN , SANWALD ERICH , HARDER ACHIM , TURBERG ANDREAS
IPC分类号： C07H17/08 , A01N43/90 , C07H13/02
CPC分类号： C07H17/08 , A01N43/90 , C07H13/02
摘要： Disclosed are novel avermectin derivatives of formula (I), wherein -C 22 R 1 -A-C 23 R 2 , R 3 , R 4 , and R 5 have the meanings indicated in the description, methods for producing said substances, the use thereof for controlling animal pests, novel intermediate products, and the production thereof.
摘要翻译：式（I），其中-C _{22 - [R ^{1 -A-C _{23 - [R ^{2 ，R的新除虫菌素衍生物 ^{3 ，R ^{4 和R ^{5 具有说明书中给出的含义，用于制备这些物质和它们的用途，用于控制动物害虫的方法和新的中间体和它们的制备。}}}}}}}

9. 发明申请

WO2006063813A3 3-ARYLALKYL-SUBSTITUTED AND 3-HETEROARYLALKYL-SUBSTITUTED-1,2,4-TRIAZIN-5(2H)-ONES 审中-公开
标题翻译： 3-芳基烷基-AND-3-杂芳基烷基取代-1,2,4-三嗪-5（2H） - 酮
公开(公告)号：WO2006063813A3
公开(公告)日：2006-09-21
申请号：PCT/EP2005013434
申请日：2005-12-14
申请人： BAYER HEALTHCARE AG , HENDRIX MARTIN , ZIMMERMANN KATJA , HIRTH-DIETRICH CLAUDIA , KARIG GUNTER , KARTHAUS DAGMAR , RAABE MARTIN , WEBER OLAF , ZAISS SIEGFRIED
发明人： HENDRIX MARTIN , ZIMMERMANN KATJA , HIRTH-DIETRICH CLAUDIA , KARIG GUNTER , KARTHAUS DAGMAR , RAABE MARTIN , WEBER OLAF , ZAISS SIEGFRIED
IPC分类号： C07D253/06 , A61K31/53 , C07D403/12 , C07D409/12
CPC分类号： C07D409/06 , C07D253/07 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D409/14 , C07D451/14
摘要： The invention relates to 3-arylalkyl-substituted and 3-heteroarylalkyl-substituted-1,2,4-triazin-5(2H)-ones, to a method for the production thereof, and to their use for producing medicaments for treating and/or preventing diseases, particularly chronic inflammatory diseases for example, rheumatoid diseases and cardiovascular diseases, such as dyslipidaemias, arteriosclerosis, and coronary heart diseases.
摘要翻译：本发明涉及3-芳基烷基和杂3-取代-1,2,4-三嗪-5（2H） - 酮和它们的制备方法和它们用于制备药物用于治疗和/或预防疾病的用途，特别流程慢性炎性疾病，如疾病类风湿性疾病，和心血管疾病，如血脂异常，动脉粥样硬化和冠心病心脏疾病。

10. 发明专利

IL216051A Method for producing oxindoles and ortho-substituted anilines and the use thereof as intermediate products for syntheses 未知
公开(公告)号：IL216051A
公开(公告)日：2015-03-31
申请号：IL21605111
申请日：2011-10-30
申请人： FORD MARK JAMES , KARIG GUNTER , BAYER IP GMBH , BAYER CROPSCIENCE AG
发明人： FORD MARK JAMES , KARIG GUNTER
摘要： Preparing ortho-substituted aniline compound (I), comprises reacting a mixture comprising substituted aniline compound (II) and thioether derivative (III), in presence of a chlorinating agent and an organic solvent at a reaction temperature of -65[deg] C, preferably -50 to -20[deg] C and obtaining the ortho-substituted aniline compound. Preparing ortho-substituted aniline compound of formula (I), comprises reacting a mixture comprising substituted aniline compound of formula (II) and thioether derivative of formula (R1-S-C(R2)(H)(R3)) (III), in presence of a chlorinating agent and an organic solvent at a reaction temperature of -65[deg] C, preferably -50 to -20[deg] C and obtaining the ortho-substituted aniline compound. R1 : 1-6C alkyl, substituted alkyl, substituted aryl or aryl, preferably 1-4C alkyl; R3 : electron withdrawing- or activating group comprising -CO-R1, -CO-X, SO(n 1>)-R1, -CN, -NO 2, aryl or heteroaryl; either R2 : H, 1-6C alkyl, substituted alkyl, substituted aryl or aryl; and R21 : R2 or residue other than R2; or R2R21 : ring; X : OR1, SR1, NR2R21; n 1> : 0-2; R4 : halo, CF 3, CN, NO 2or COY1, preferably 2-F; Y1 : OR1, SR1, NR2R22; R22 : R2 or residue other than R2; n : 1-4, preferably 1; and R5 : R2. Independent claims are also included for: (1) preparing substituted indole compound of formula (IV) and substituted oxindole compound of formula (V), comprising converting (I) in presence of an acid catalyst, with or without the isolation of (I) (optional for (IV) and preferred for (V)), and obtaining (IV) or (V); (2) an intermediate comprising ortho-substituted aniline compound of formula (VI); and (3) end products comprising substituted indole- and substituted oxindole compound of formula (VII) and (VIII). R6 : 1-6C alkyl, substituted alkyl, substituted aryl or aryl, preferably 1-4C alkyl or OH; R7 : 2-6C alkyl, preferably benzyl; R8 : H; R9 : CO 2Ra; Ra : 1-6C alkyl or optionally benzyl ester; R10 : 2-F; and R11 : H, 1-4C alkyl; R12 : 7-F; and R13 : 1-6C alkyl or optionally benzyl or OH. [Image] [Image] [Image].

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