公开(公告)号：US09936700B2

公开(公告)日：2018-04-10

申请号：US15029533

申请日：2014-10-20

申请人： BAYER CROPSCIENCE AKTIENGESELLSCHAFT

发明人： Bernd Alig ,  Joerg Greul ,  Ruediger Fischer ,  Hans-Georg Schwarz ,  Niklas Tim Bretschneider ,  Uta Bretschneider ,  Reiner Fischer ,  Daniela Portz ,  Olga Malsam ,  Peter Loesel ,  Kerstin Ilg ,  Angela Becker ,  Ulrich Goergens ,  Stefan Herrmann ,  Claudia Welz

IPC分类号： A01N43/60 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04 ,  C07D241/40 ,  C07D491/04 ,  A01N43/90 ,  C07D213/50 ,  C07D491/056

CPC分类号： A01N43/60 ,  A01N43/90 ,  C07D213/50 ,  C07D241/40 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04 ,  C07D491/04 ,  C07D491/056

摘要： The invention relates to novel compounds of the formula (I) in which R1, R2, R3, R4, R5, R6, Y1 and Y2 have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as acaricides and/or insecticides for controlling animal pests. The compounds of the formula (I) are also suitable as nematicides for plant-damaging pests and/or anthelminthics for endoparasites in humans and animals.

公开(公告)号：US20140039189A1

公开(公告)日：2014-02-06

申请号：US14047043

申请日：2013-10-07

申请人： Joerg KLEY ,  Daniel HAERLE ,  Guenter LINZ ,  Sandra STEHLE

发明人： Joerg KLEY ,  Daniel HAERLE ,  Guenter LINZ ,  Sandra STEHLE

IPC分类号： C07C231/14 ,  C07C233/11 ,  C07D403/12 ,  C07D233/48 ,  C07D241/28 ,  C07D241/44

CPC分类号： C07C231/14 ,  C07C231/00 ,  C07C231/10 ,  C07C233/11 ,  C07C235/28 ,  C07D233/48 ,  C07D241/06 ,  C07D241/28 ,  C07D241/40 ,  C07D241/44 ,  C07D261/08 ,  C07D403/12

摘要： The present invention relates to a novel process for the preparation of compounds of general formula (I) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.

摘要翻译： 本发明涉及一种制备通式（I）化合物及其盐的新方法，特别是其与无机或有机酸和碱的生理上可接受的盐，其具有有价值的药理学性质，特别是对上皮的抑制作用 钠通道，其用于治疗疾病，特别是肺和气道疾病的用途。

公开(公告)号：US08222417B2

公开(公告)日：2012-07-17

申请号：US12666802

申请日：2008-06-24

申请人： Ryo Suzuki ,  Ayako Mikami ,  Hiroaki Tanaka ,  Hiroshi Fukushima

发明人： Ryo Suzuki ,  Ayako Mikami ,  Hiroaki Tanaka ,  Hiroshi Fukushima

IPC分类号： C07D215/38 ,  A61K31/04

CPC分类号： C07D209/08 ,  C07D215/08 ,  C07D215/18 ,  C07D215/20 ,  C07D215/48 ,  C07D223/16 ,  C07D241/40 ,  C07D265/36 ,  C07D279/16

摘要： The present invention provides compounds having excellent 11β-HSD1 inhibitory activity.A compound represented by the following formula (I): [wherein X1 represents an oxygen atom, or the formula —(CR11R12)p—, etc., Y1 represents a hydrogen atom, a hydroxyl group, etc., Z1 represents an oxygen atom or the formula —(NR14)—, R1 represents a hydrogen atom, a halogen atom, a cyano group, a C1-4 alkyl group, a C1-4 alkyl group substituted with 1 to 3 halogen atoms, a C1-4 alkoxy group, a C1-4 alkoxycarbonyl group, a carboxyl group, a carbamoyl group, or an amino group, and m represents an integer of 1 or 2, and R2 represents a hydrogen atom or a C1-4 alkyl group, and n represents an integer of 1 or 2].

摘要翻译： 本发明提供具有优异的11＆amp; b -HSD1抑制活性的化合物。 由下式（I）表示的化合物：[其中X1表示氧原子，或式 - （CR11R12）p-等，Y1表示氢原子，羟基等，Z1表示氧原子 或式 - （NR14） - ，R1表示氢原子，卤素原子，氰基，C1-4烷基，被1〜3个卤素原子取代的C1-4烷基，C1-4烷氧基 ，C 1-4烷氧基羰基，羧基，氨基甲酰基或氨基，m表示1或2的整数，R 2表示氢原子或C 1-4烷基，n表示整数 1或2]。

公开(公告)号：US20100179325A1

公开(公告)日：2010-07-15

申请号：US12666802

申请日：2008-06-28

申请人： Ryo Suzuki ,  Ayako Mikami ,  Hiroaki Tanaka ,  Hiroshi Fukushima

发明人： Ryo Suzuki ,  Ayako Mikami ,  Hiroaki Tanaka ,  Hiroshi Fukushima

IPC分类号： C07D215/38 ,  C07D209/04

CPC分类号： C07D209/08 ,  C07D215/08 ,  C07D215/18 ,  C07D215/20 ,  C07D215/48 ,  C07D223/16 ,  C07D241/40 ,  C07D265/36 ,  C07D279/16

摘要： The present invention provides compounds having excellent 11β-HSD1 inhibitory activity.A compound represented by the following formula (I): [wherein X1 represents an oxygen atom, or the formula —(CR11R12)p—, etc., Y1 represents a hydrogen atom, a hydroxyl group, etc., Z1 represents an oxygen atom or the formula —(NR14)—, R1 represents a hydrogen atom, a halogen atom, a cyano group, a C1-4 alkyl group, a C1-4 alkyl group substituted with 1 to 3 halogen atoms, a C1-4 alkoxy group, a C1-4 alkoxycarbonyl group, a carboxyl group, a carbamoyl group, or an amino group, and m represents an integer of 1 or 2, and R2 represents a hydrogen atom or a C1-4 alkyl group, and n represents an integer of 1 or 2].

摘要翻译： 本发明提供具有优异的11＆amp; b -HSD1抑制活性的化合物。 由下式（I）表示的化合物：[其中X1表示氧原子，或式 - （CR11R12）p-等，Y1表示氢原子，羟基等，Z1表示氧原子 或式 - （NR14） - ，R1表示氢原子，卤素原子，氰基，C1-4烷基，被1〜3个卤素原子取代的C1-4烷基，C1-4烷氧基 ，C 1-4烷氧基羰基，羧基，氨基甲酰基或氨基，m表示1或2的整数，R 2表示氢原子或C 1-4烷基，n表示整数 1或2]。

公开(公告)号：US20170191990A1

公开(公告)日：2017-07-06

申请号：US15438859

申请日：2015-08-21

申请人： Roche Diagnostics Operations, Inc.

发明人： Peter Gebauer ,  Dieter Heindi ,  Carina Horn ,  Maksim Fomin

IPC分类号： G01N33/52 ,  C07D241/42 ,  C07D403/06 ,  G01N33/50

CPC分类号： G01N33/52 ,  C07D241/40 ,  C07D241/42 ,  C07D401/06 ,  C07D403/06 ,  G01N33/5005

摘要： The present invention relates to a chemical compound or a salt or solvate thereof being a phenazine-, phenanthridine-, phenanthroline-, quinoline-, quinoxaline-, acridine- isoquinoline-, pyrazine- or pyridine-derivative comprising a conjugated π-system and a π-acceptor group, and to uses thereof. The present invention further relates to a chemistry matrix and to a test element comprising the chemical compound of the present invention. The present invention also relates to a method of determining the amount of an analyte in a test sample, comprising contacting said test sample with a chemical compound, with a chemistry matrix, or with a test element of the invention and estimating the amount of redox equivalents liberated or consumed by the chemical compound, by the chemical compound comprised in said chemistry matrix, or by the chemical compound comprised in said test element, in the presence of said test sample, thereby determining the amount of an analyte in said test sample. Moreover, the present invention relates to a system comprising a test element according to the present invention and a device comprising a sensor for measuring the amount of redox equivalents liberated or consumed.

公开(公告)号：US20160227779A1

公开(公告)日：2016-08-11

申请号：US15029533

申请日：2014-10-20

申请人： BAYER CROPSCIENCE AKTIENGESELLSCHAFT

发明人： Bernd Alig ,  Joerg Greul ,  Ruediger Fischer ,  Hans-Georg Schwarz ,  Niklas Tim Bretschneider ,  Uta Bretschneider ,  Reiner Fischer ,  Daniela Portz ,  Olga Malsam ,  Peter Loesel ,  Kerstin Ilg ,  Angela Becker ,  Ulrich Goergens ,  Stefan Herrmann ,  Claudia Welz

IPC分类号： A01N43/60 ,  C07D213/50 ,  C07D491/056 ,  A01N43/90

CPC分类号： A01N43/60 ,  A01N43/90 ,  C07D213/50 ,  C07D241/40 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04 ,  C07D491/04 ,  C07D491/056

摘要： The invention relates to novel compounds of the formula (I) in which R1, R2, R3, R4, R5, R6, Y1 and Y2 have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as acaricides and/or insecticides for controlling animal pests. The compounds of the formula (I) are also suitable as nematicides for plant-damaging pests and/or anthelminthics for endoparasites in humans and animals.

摘要翻译： 本发明涉及其中R1，R2，R3，R4，R5，R6，Y1和Y2具有上述含义的式（I）的新化合物与多种制备方法和中间体及其用途 用于控制动物害虫的杀螨剂和/或杀虫剂。 式（I）的化合物也适用于人和动物内寄生虫的植物损害性害虫和/或抗血清活性的杀线虫剂。

公开(公告)号：US09359380B2

公开(公告)日：2016-06-07

申请号：US14205508

申请日：2014-03-12

申请人： Vertex Pharmaceuticals Incorporated

发明人： John Patrick Maxwell ,  Paul S. Charifson ,  Qing Tang ,  Steven M. Ronkin ,  Katrina Lee Jackson ,  Albert Charles Pierce ,  David J. Lauffer ,  Pan Li ,  Simon Giroux ,  Jinwang Xu ,  Kevin M. Cottrell ,  Mark A. Morris ,  Nathan D. Waal ,  John J. Court ,  Wenxin Gu ,  Hongbo Deng

IPC分类号： C07D513/04 ,  C07D498/00 ,  C07D241/40 ,  C07D405/12 ,  C07D471/04 ,  C07D417/12 ,  C07D413/12 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D473/40 ,  C07D475/00 ,  C07D487/04 ,  C07D491/048 ,  C07D498/08 ,  C07D241/42 ,  C07D413/04 ,  C07D241/44 ,  C07D491/052

CPC分类号： A61K31/5377 ,  A61K31/506 ,  A61K31/5386 ,  C07D241/40 ,  C07D241/42 ,  C07D241/44 ,  C07D271/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D473/40 ,  C07D475/00 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  C07D491/056 ,  C07D491/08 ,  C07D498/08 ,  C07D513/04

摘要： The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

公开(公告)号：US20130296557A1

公开(公告)日：2013-11-07

申请号：US13980108

申请日：2012-01-23

申请人： Prabal Sengupta ,  Hemant Ashvinbhai Chokshi ,  Chetan Surjitsingh Puri ,  Sabbirhusen Yusufbhai Chimanwala ,  Varun Anilkumar Mehta ,  Dipali Manubhai Desai ,  Trinadha Rao Chitturi ,  Rajamannar Thennati

发明人： Prabal Sengupta ,  Hemant Ashvinbhai Chokshi ,  Chetan Surjitsingh Puri ,  Sabbirhusen Yusufbhai Chimanwala ,  Varun Anilkumar Mehta ,  Dipali Manubhai Desai ,  Trinadha Rao Chitturi ,  Rajamannar Thennati

IPC分类号： C07D487/04 ,  C07D215/14 ,  C07D241/40

CPC分类号： C07D241/40 ,  C07C243/38 ,  C07D213/56 ,  C07D215/12 ,  C07D215/14 ,  C07D231/12 ,  C07D239/74 ,  C07D277/64 ,  C07D401/06 ,  C07D401/12 ,  C07D409/06 ,  C07D417/06 ,  C07D471/04 ,  C07D487/04

摘要： The present invention relates to novel diarylacetylene hydrazide compounds of formula (I) or pharmaceutically acceptable salt thereof, as tyrosine kinase inhibitors, the process for their preparation, and to the use of the compounds of formula (I) in the preparation of pharmaceutical compositions for the therapeutic treatment of disorders related to tyrosine kinases, in warm-blooded animals

摘要翻译： 本发明涉及式（I）的新型二芳基乙炔酰肼化合物或其药学上可接受的盐作为酪氨酸激酶抑制剂，其制备方法以及式（I）化合物在制备药物组合物中的用途 在温血动物中治疗与酪氨酸激酶相关的疾病

公开(公告)号：US4696933A

公开(公告)日：1987-09-29

申请号：US701012

申请日：1985-02-12

申请人： Tobias O. Yellin ,  David J. Gilman

发明人： Tobias O. Yellin ,  David J. Gilman

IPC分类号： A61K31/41 ,  A61K31/415 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61K31/505 ,  A61P1/04 ,  A61P43/00 ,  C07D213/70 ,  C07D213/73 ,  C07D213/75 ,  C07D213/76 ,  C07D231/38 ,  C07D239/42 ,  C07D239/46 ,  C07D239/47 ,  C07D241/40 ,  C07D249/04 ,  C07D249/14 ,  C07D277/20 ,  C07D277/48 ,  C07D401/12

CPC分类号： C07D213/76 ,  C07D239/42 ,  C07D239/47 ,  C07D241/40 ,  C07D249/04 ,  C07D277/48

摘要： The invention relates to amide derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention there is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 is a hydrogen or 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkyl, 3-6C alkenyl, 3-6C alkynyl, 1-6C alkanoyl, 6-10C aryl, 7-11C aralkyl or 7-11C aroyl, the aryl, aralkyl and aroyl radical being optionally substituted; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene, or a 1-8C alkylene into which is optionally inserted one or two groups; D is O or S; and R.sup.2 and R.sup.3 are hydrogen or a variety of radicals described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.

公开(公告)号：US10060907B2

公开(公告)日：2018-08-28

申请号：US15438859

申请日：2015-08-21

申请人： Roche Diagnostics Operations, Inc.

发明人： Peter Gebauer ,  Dieter Heindl ,  Carina Horn ,  Maksim Fomin

IPC分类号： G01N33/52 ,  G01N33/50 ,  C07D241/42 ,  C07D403/06

CPC分类号： G01N33/52 ,  C07D241/40 ,  C07D241/42 ,  C07D401/06 ,  C07D403/06 ,  G01N33/5005

摘要： The present invention relates to a chemical compound or a salt or solvate thereof being a phenazine-, phenanthridine-, phenanthroline-, quinoline-, quinoxaline-, acridine-isoquinoline-, pyrazine- or pyridine-derivative comprising a conjugated π-system and a π-acceptor group, and to uses thereof. The present invention further relates to a chemistry matrix and to a test element comprising the chemical compound of the present invention. The present invention also relates to a method of determining the amount of an analyte in a test sample, comprising contacting said test sample with a chemical compound, with a chemistry matrix, or with a test element of the invention and estimating the amount of redox equivalents liberated or consumed by the chemical compound, by the chemical compound comprised in said chemistry matrix, or by the chemical compound comprised in said test element, in the presence of said test sample, thereby determining the amount of an analyte in said test sample. Moreover, the present invention relates to a system comprising a test element according to the present invention and a device comprising a sensor for measuring the amount of redox equivalents liberated or consumed.