公开(公告)号：US09029365B2

公开(公告)日：2015-05-12

申请号：US13727009

申请日：2012-12-26

Applicant: George Philip Lahm ,  Thomas Paul Selby ,  Thomas Martin Stevenson

Inventor： George Philip Lahm ,  Thomas Paul Selby ,  Thomas Martin Stevenson

IPC: A01N43/56 ,  A01N43/16 ,  C07C251/76 ,  C07D213/77 ,  C07D231/06 ,  C07D231/08 ,  C07D231/14 ,  C07D231/16 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  A01N43/707 ,  A01N37/38

CPC classification number: A01N43/56 ,  A01N37/38 ,  A01N43/16 ,  A01N43/707 ,  C07C251/76 ,  C07D213/77 ,  C07D231/06 ,  C07D231/08 ,  C07D231/14 ,  C07D231/16 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14

Abstract: This invention provides a composition comprising a first compound selected from Formula 1, an N-oxide or an agriculturally suitable salt thereof; and a second compound selected from neonicotinoids, wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure.

Abstract translation: 本发明提供一种组合物，其包含选自式1的第一化合物，N-氧化物或其农业上合适的盐; 和选自新烟碱类的第二化合物，其中R1，R2，R3，R4a，R4b和R5如本公开所定义。

公开(公告)号：US20150119242A1

公开(公告)日：2015-04-30

申请号：US14399544

申请日：2013-05-06

Applicant: BAYER CROPSCIENCE AG

Inventor： Simon Maechling ,  Mazen Es-Sayed ,  Peter Dahmen ,  Ulrike Wachendorff-Neumann ,  David Bernier ,  Lionel Carles ,  Christophe Dubost ,  Jean-Pierre Vors ,  Stephane Brunet ,  Helene Lachaise

IPC: A01N43/56 ,  C07C251/50 ,  C07C211/60 ,  C07D231/14

CPC classification number: C07C211/60 ,  A01N43/56 ,  C07C251/44 ,  C07C251/50 ,  C07D231/14 ,  C07D231/16

Abstract: The present invention relates to novel pyrazole(thio)tetrahydronaphthyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.

Abstract translation: 本发明涉及新颖的吡唑（硫代）四氢萘基甲酰胺，制备这些化合物的方法，包括这些化合物的组合物，以及其作为生物活性化合物的用途，特别是用于控制作物保护中的有害微生物和保护 材料

公开(公告)号：US09012657B2

公开(公告)日：2015-04-21

申请号：US14009483

申请日：2012-06-18

Applicant: Masamune Okamoto ,  Hideaki Imura ,  Naoto Takada

Inventor： Masamune Okamoto ,  Hideaki Imura ,  Naoto Takada

IPC: C07D231/10 ,  C07D231/28 ,  C07D231/14

CPC classification number: C07D231/28 ,  C07D231/14

Abstract: A method for producing a pyrazole compound of the general formula (5) includes reacting a 2-acyl-3-aminoacrylic acid ester of the general formula (1) with a hydrazine of the general formula (4) in the presence of a base where R1, R2, R3 and R4 each independently represent an alkyl group wherein R5 represents an alkyl group or an aryl group wherein R1, R4 and R5 have the same meanings as above. It is possible by this production method to produce the 1,3-disubstituted pyrazol-4-carboxylic acid ester at a high yield and selectivity and with less discoloration.

Abstract translation: 制备通式（5）的吡唑化合物的方法包括在碱的存在下使通式（1）的2-酰基-3-氨基丙烯酸酯与通式（4）的肼反应， R 1，R 2，R 3和R 4各自独立地表示烷基，其中R 5表示烷基或芳基，其中R 1，R 4和R 5具有与上述相同的含义。 通过这种制备方法可以以高产率和选择性和较少的变色产生1,3-二取代的吡唑-4-羧酸酯。

公开(公告)号：US20150065543A1

公开(公告)日：2015-03-05

申请号：US14521689

申请日：2014-10-23

Applicant: Paul Allegretti ,  Seok-Ki Choi ,  Roland Gendron ,  Paul R. Fatheree ,  Keith Jendza ,  Robert Murray McKinnell ,  Darren McMurtrie ,  Brooke Olson

Inventor： Paul Allegretti ,  Seok-Ki Choi ,  Roland Gendron ,  Paul R. Fatheree ,  Keith Jendza ,  Robert Murray McKinnell ,  Darren McMurtrie ,  Brooke Olson

IPC: C07D513/14 ,  C07D233/64 ,  C07D213/64 ,  C07D233/70 ,  C07D231/14 ,  C07D249/08 ,  C07D233/68 ,  C07D403/10

CPC classification number: C07D233/70 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/417 ,  A61K31/4188 ,  A61K31/4196 ,  A61K31/4412 ,  A61K45/00 ,  A61K45/06 ,  C07D207/36 ,  C07D207/46 ,  C07D213/64 ,  C07D213/89 ,  C07D231/14 ,  C07D233/64 ,  C07D233/68 ,  C07D233/90 ,  C07D249/08 ,  C07D255/02 ,  C07D401/12 ,  C07D403/10 ,  C07D513/04 ,  C07D513/14

Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract translation: 本发明涉及具有下式的化合物：其中：Ar，r，Y，Z，Q，W，X和R5-7如说明书中所定义，及其药学上可接受的盐。 这些化合物具有AT1受体拮抗剂活性和neprilysin抑制活性。 本发明还涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。

公开(公告)号：US08946236B2

公开(公告)日：2015-02-03

申请号：US13961765

申请日：2013-08-07

Applicant: Bayer CropScience AG

Inventor： Bernd Alig ,  Ruediger Fischer ,  Christian Funke ,  Rudolf F. Ernst Gesing ,  Achim Hense ,  Olga Malsam ,  Mark Wilhelm Drewes ,  Ulrich Goergens ,  Tetsuya Murata ,  Katsuaki Wada ,  Christian Arnold ,  Erich Sanwald

IPC: A01N43/653 ,  A01N43/56 ,  A01N43/80 ,  A01N43/54 ,  A01N43/713 ,  C07D231/14 ,  C07D403/06 ,  C07D405/14 ,  C07D413/14 ,  C07D401/14

CPC classification number: C07D231/14 ,  A01N43/54 ,  A01N43/56 ,  A01N43/653 ,  A01N43/713 ,  A01N43/80 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D413/14

Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.

Abstract translation: 本发明涉及式（I）的新的杀虫剂，其中R1，R2，R3，R4，R5，R6，A，Q和n可以具有说明书中所述的定义，涉及制备它们的多种方法， 用作活性化合物，更具体地说是用作害虫防治组合物。

公开(公告)号：US08933246B2

公开(公告)日：2015-01-13

申请号：US13738230

申请日：2013-01-10

Applicant: BASF SE

Inventor： Maximilian Dochnahl ,  Gunter Lipowsky

IPC: C07D231/10 ,  C07D231/20 ,  C07D231/14

CPC classification number: C07D231/20 ,  C07D231/14

Abstract: The present invention to a process for preparing 1-phenylpyrazoles of the formula I in which each R1 is independently selected from chlorine, fluorine, alkyl, haloalkyl, alkoxy and haloalkoxy; n is 1, 2 or 3; each R2 is independently selected from cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and alkoxycarbonyl; m is 0, 1 or 2; A is alkyl, aryl or aryl-C1-C4-alkyl, where A optionally bears 1, 2, 3 or 4 substituents comprising reacting a phenyl halide of the formula (II) with a pyrazole derivative of the formula (III) in which X is chlorine, iodine or bromine; and R1, n, R2, m and A are each as defined above, in the presence of a base and a catalytic system comprising a ligand and a metal compound selected from palladium compounds, iron compounds and copper compounds.

Abstract translation: 本发明涉及一种制备式I的1-苯基吡唑的方法，其中每个R 1独立地选自氯，氟，烷基，卤代烷基，烷氧基和卤代烷氧基; n为1,2或3; 每个R 2独立地选自氰基，硝基，卤素，烷基，卤代烷基，烷氧基，卤代烷氧基，烷硫基和烷氧基羰基; m为0,1或2; A是烷基，芳基或芳基-C 1 -C 4烷基，其中A任选地带有1,2,3或4个取代基，包括使式（II）的苯基卤与式（III）的吡唑衍生物反应，其中X 是氯，碘或溴; 在碱和催化体系的存在下，R 1，n，R 2，m和A各自如上所定义，所述催化体系包含配体和选自钯化合物，铁化合物和铜化合物的金属化合物。

公开(公告)号：US20140371213A1

公开(公告)日：2014-12-18

申请号：US14281360

申请日：2014-05-19

Applicant: ASTEX THERAPEUTICS, LTD.

Inventor： Valerio BERDINI ,  Michael Alistair O'BRIEN ,  Maria Grazia CARR ,  Theresa Rachel EARLY ,  Adrian Liam GILL ,  Gary TREWARTHA ,  Alison Jo-Anne WOOLFORD ,  Andrew James WOODHEAD ,  Paul Graham WYATT

IPC: C07D231/38 ,  A61K31/415 ,  C07D231/40 ,  C07D403/12 ,  A61K31/4155 ,  A61K31/541 ,  A61K31/4439 ,  A61K31/4196 ,  A61K31/454 ,  A61K31/496 ,  A61K31/4178 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/12

CPC classification number: C07D231/38 ,  A61K31/415 ,  A61K31/4152 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C04B35/632 ,  C07D231/14 ,  C07D231/40 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D453/02 ,  C07D471/04

Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C═O, NRg(C═O) or O(C═O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).

Abstract translation: 本发明提供式（O）的化合物或其盐或互变异构体或N-氧化物或溶剂合物，用于预防或治疗疾病状态和病症，例如由细胞周期蛋白依赖性激酶和糖原合酶激酶-3介导的癌症。 在式（0）中：X为基团R 1 -A-NR 4 - 或5或6元碳环或杂环; A是键，SO 2，C = O，NR g（C = O）或O（C = O），其中R g是氢或任选被羟基或C 1-4烷氧基取代的C 1-4烃基; Y是长度为1,2或3个碳原子的键或亚烷基链; R1是氢; 具有3-12个环成员的碳环或杂环基; 或任选被一个或多个选自卤素（例如氟），羟基，C 1-4烃氧基，氨基，单或二-C 1-4烃基氨基的取代基取代的C 1-8烃基，以及具有3至 12个环成员，并且其中烃基的1或2个碳原子可以任选地被选自O，S，NH，SO，SO 2的原子或基团取代; R2是氢; 卤素; C 1-4烷氧基（如甲氧基）; 或任选被卤素（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的C 1-4烃基; R 3选自具有3至12个环成员的氢和碳环和杂环基; 和R 4是氢或任选被卤素（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的C 1-4烃基。

公开(公告)号：US08912342B2

公开(公告)日：2014-12-16

申请号：US13759107

申请日：2013-02-05

Applicant: Westfaelische Wilhelms Universitaet Muenster

Inventor： Frank Glorius ,  Mamta Suri

IPC: C07D231/12 ,  C07D231/14 ,  C07D405/04

CPC classification number: C07D231/14 ,  C07D231/12 ,  C07D405/04

Abstract: A method of synthesizing Pyrazoles by means of the oxidative conversion of Enamines with suitable N-containing carboxylic acid derivatives in the presence of copper ions and 2-picolinic acid derivatives is provided.

Abstract translation: 提供了一种通过在铜离子和2-吡啶甲酸衍生物存在下用适当的含有N的羧酸衍生物对Enamine进行氧化转化来合成吡唑的方法。

公开(公告)号：US20140348850A1

公开(公告)日：2014-11-27

申请号：US14460679

申请日：2014-08-15

Applicant: JOSLIN DIABETES CENTER

Inventor： Edward P. Feener ,  Allen Clermont

IPC: C07K16/40 ,  C07D401/06 ,  A61K31/415 ,  C07D231/14 ,  A61K31/341 ,  C07D307/68 ,  A61K31/4192 ,  C07D249/04 ,  A61K31/381 ,  C07D333/38 ,  A61K31/426 ,  C07D277/56 ,  A61K31/4436 ,  C07D409/04 ,  A61K31/40 ,  C07D207/34 ,  A61K39/395 ,  A61K38/00 ,  A61K38/02 ,  A61K45/06 ,  A61K31/4439

CPC classification number: C07K16/40 ,  A61K31/195 ,  A61K31/341 ,  A61K31/381 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/426 ,  A61K31/4436 ,  A61K31/4439 ,  A61K38/005 ,  A61K38/02 ,  A61K39/3955 ,  A61K45/06 ,  C07D207/34 ,  C07D231/14 ,  C07D249/04 ,  C07D277/56 ,  C07D307/68 ,  C07D333/38 ,  C07D401/06 ,  C07D409/04

Abstract: The present invention relates to methods of reducing blood pressure in a subject by administering a plasma kallikrein inhibitor.

Abstract translation: 本发明涉及通过施用血浆激肽释放酶抑制剂降低受试者的血压的方法。

公开(公告)号：US08871947B2

公开(公告)日：2014-10-28

申请号：US14145073

申请日：2013-12-31

Applicant: KingChem LLC

Inventor： Zheqing Wang ,  Angang Wang

IPC: C07C67/343 ,  C07D231/14 ,  C07C67/313 ,  C07C67/36

CPC classification number: C07D231/14 ,  C07C67/313 ,  C07C67/343 ,  C07C67/36 ,  C07C69/732 ,  C07C69/738 ,  C07C69/716

Abstract: The present disclosure provides a novel and economically advantageous process for preparation of compounds of Formula I, such as alkyl 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid ester. The process includes acidification of the sodium enolate of alkyl difluoroacetoacetate by carbonic acid generated in situ by reacting carbon dioxide with water. The disclosure also includes promoting the ring closure reaction in which alkyl 2-alkomethylene-4,4-difluoro-3-oxobutyrate is reacted with methylhydrazine in two phase system with a weak base such as Na2CO3 or K2CO3.

Abstract translation: 本公开内容提供了制备式I化合物的新颖且经济上有利的方法，例如3-二氟甲基-1-甲基-1H-吡唑-4-甲酸烷基酯。 该方法包括通过二氧化碳与水反应原位产生的碳酸来酸化二氟乙酰乙酸烷基酯的烯醇化钠。 本公开还包括促进闭环反应，其中2-烷基亚甲基-4,4-二氟-3-氧代丁酸烷基酯与二碱系中的甲基肼与弱碱如Na 2 CO 3或K 2 CO 3反应。