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1. 发明授权

US10526316B2 Quinoxaline and pyridopyrazine derivatives as PI3Kβ inhibitors 有权
公开(公告)号：US10526316B2
公开(公告)日：2020-01-07
申请号：US15766887
申请日：2016-10-07
申请人： Janssen Pharmaceutica NV
发明人： Patrick Rene Angibaud , Olivier Alexis Georges Querolle , Didier Jean-Claude Berthelot , Christophe Meyer , Matthieu Philippe Victor Willot , Lieven Meerpoel , Thierry Francois Alain Jean Jousseaume
IPC分类号： C07D403/10 , C07D487/04 , C07D495/10 , C07D498/10 , C07D471/04 , C07D241/42 , C07D403/12 , C07D403/14 , C07D413/10 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D413/04 , C07D413/06 , C07D241/14 , C07D417/04 , C07D487/02 , C07D491/10 , C07D513/10
摘要： The present invention relates to substituted quinoxaline and pyridopyrazine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3Kβ inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

2. 发明申请

US20110136831A1 N-2-(Hetero)Arylethylcarboxamide Derivative, and Pest-Controlling Agent Comprising the Same 有权
标题翻译： N-2-（杂）芳基乙酰基甲酰胺衍生物和包含它的害虫控制剂
公开(公告)号：US20110136831A1
公开(公告)日：2011-06-09
申请号：US12225361
申请日：2007-03-20
申请人： Masatsugu Oda , Yoshihiro Matsuzaki , Koji Tanaka , Eiji Takizawa , Motohiro Haseba , Nobutaka Kuroki , Akiyuki Suwa , Kenji Oshima
发明人： Masatsugu Oda , Yoshihiro Matsuzaki , Koji Tanaka , Eiji Takizawa , Motohiro Haseba , Nobutaka Kuroki , Akiyuki Suwa , Kenji Oshima
IPC分类号： A01N43/60 , C07D213/56 , C07D241/14 , C07D327/06 , C07D231/12 , C07D277/24 , C07D307/34 , C07D333/38 , A01N43/40 , A01N43/32 , A01N43/56 , A01N43/78 , A01N43/08 , A01N43/10 , A01P5/00 , A01P15/00
CPC分类号： C07D241/24 , A01N37/18 , A01N37/40 , A01N43/08 , A01N43/10 , A01N43/32 , A01N43/40 , A01N43/56 , A01N43/60 , A01N43/78 , A01N47/02 , C07D213/82 , C07D231/14 , C07D277/20 , C07D277/56 , C07D307/56 , C07D327/06 , C07D333/38
摘要： An N-2-(hetero)arylethylcarboxamide derivative represented by the formula (I) wherein R1 and R2 are each independently a hydrogen atom etc., R3 and R4 are each independently a hydrogen atom etc., each Y is independently a halogen atom; a (C1-C6)alkyl group optionally substituted by halogen atom(s) etc., n is an integer of 1 to 5, A is a specific substituted cyclic group, E is C—H; C—Y (Y is as defined above); or a nitrogen atom, a salt thereof, and a pest controlling agent containing the derivative or salt as an active ingredient show superior performance as compared to the prior art technique, and are is useful particularly as plant disease controlling agents or nematocides having a broad control spectrum at a low dose.
摘要翻译：由式（I）表示的N-2-（杂）芳基乙基甲酰胺衍生物，其中R 1和R 2各自独立地为氢原子等，R 3和R 4各自独立地为氢原子等，各Y独立地为卤素原子; 任选被卤素原子取代的（C1-C6）烷基等，n为1〜5的整数，A为特定的取代环状基团，E为C-H; C-Y（Y如上定义）; 或氮原子，其盐和含有该衍生物或盐的害虫控制剂作为活性成分，与现有技术相比表现出优异的性能，特别适用于具有广泛控制的植物病害防治剂或杀线虫剂频谱在低剂量。

3. 发明授权

US5914344A Substituted carboxanilide derivative and plant disease control agent comprising same as active ingredient 失效
标题翻译：取代的羧酰苯胺衍生物和包含与活性成分相同的植物病害防治剂
公开(公告)号：US5914344A
公开(公告)日：1999-06-22
申请号：US908187
申请日：1997-08-07
申请人： Yukihiro Yoshikawa , Kanji Tomiya , Naofumi Tomura , Hiroyuki Katsuta , Osamu Takahashi , Shunichi Inami , Yuji Yanase , Junro Kishi , Hideo Kawashima
发明人： Yukihiro Yoshikawa , Kanji Tomiya , Naofumi Tomura , Hiroyuki Katsuta , Osamu Takahashi , Shunichi Inami , Yuji Yanase , Junro Kishi , Hideo Kawashima
IPC分类号： C07D231/14 , A01N43/26 , A01N43/56 , A01N43/78 , C07C211/45 , C07D213/82 , C07D231/16 , C07D241/14 , C07D263/34 , C07D277/20 , C07D277/30 , C07D277/56 , C07D307/68 , C07D309/28 , C07D327/06 , C07D333/24 , A61K31/415
CPC分类号： A01N43/56 , A01N43/78 , C07C211/45 , C07D231/14 , C07D277/56
摘要： A substituted carboxanilide derivative represented by the formula (1): ##STR1## wherein A is a hydrogen atom or methyl, B is a methyl or ethyl, and Het is 1-methyl-3-substituted-4-pyrazolyl or 2-methyl-4-substituted-5-triazoyl group, exhibits a disease control effect against Botrytis cinerea, Powdery mildew, Pyricularia oryzae of rice plant and other various plant diseases, is excellent in residual effect, has also activity against resistant strain for conventional chemicals, particularly exerts control effects against Botrytis cinerea at a lower dosage as compared with a prior art, is also safe for crops, and thus is useful as a plant control agent.
摘要翻译：由式（1）表示的取代的羧酰苯胺衍生物：其中A是氢原子或甲基，B是甲基或乙基，Het是1-甲基-3-取代-4-吡唑基或2-甲基-4-取代的 -5-三唑酰基对植物灰葡萄孢，白粉病，稻瘟病等多种植物病害具有防治效果，残留效果优异，对常规化学品的抗性菌株也具有抗菌活性，特别是对抗与现有技术相比，较低剂量的灰葡萄孢属对于作物也是安全的，因此可用作植物控制剂。

4. 发明授权

US5663341A Process for making HIV protease inhibitors 失效
标题翻译：制造HIV蛋白酶抑制剂的方法
公开(公告)号：US5663341A
公开(公告)日：1997-09-02
申请号：US487903
申请日：1995-06-07
申请人： Kai Rossen , David Askin , Paul Reider , Richard J. Varsolona , Ralph Volante
发明人： Kai Rossen , David Askin , Paul Reider , Richard J. Varsolona , Ralph Volante
IPC分类号： C07D241/14 , A61K31/495 , A61P31/12 , C07D241/04 , C07D401/06 , C07D405/06 , C07D491/04 , C07D491/048
CPC分类号： C07D401/06 , C07D241/04 , C07D491/04
摘要： A process for racemization of optically pure or enriched piperazine-2-tert-butylcarboxamide and its derivatives comprising reacting the optically pure or enriched piperazine compound with a racemizing agent selected from a strong base, an anhydrous metal salt or a carboxylic acid, in a solvent at a temperature range of between room temperature and 250.degree. C. The piperazine carboxamide derivatives are key intermediates in the preparation of HIV protease inhibitor compounds, including Compound J.
摘要翻译：光学纯的或富集的哌嗪-2-叔丁基羧酰胺及其衍生物的外消旋化方法，包括使光学纯的或富集的哌嗪化合物与选自强碱，无水金属盐或羧酸的外消旋化合物在溶剂中反应在室温至250℃的温度范围内。哌嗪甲酰胺衍生物是制备HIV蛋白酶抑制剂化合物的关键中间体，包括化合物J.

5. 发明授权

US5491238A Process for making HIV protease inhibitors 失效
公开(公告)号：US5491238A
公开(公告)日：1996-02-13
申请号：US458379
申请日：1995-06-02
申请人： David Askin , Ralph P. Volante , Kan K. Eng
发明人： David Askin , Ralph P. Volante , Kan K. Eng
IPC分类号： C07D241/04 , C07D241/14 , C07D263/52 , C07D413/06 , C07D213/06
CPC分类号： C07D263/52 , C07D413/06
摘要： Intermediates of structural formula ##STR1## can be made by reacting glycidol or an activated derivative thereof with an amide. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.

6. 发明授权

US5442059A 9-[(substituted glycyl)amido)]-6-demethyl-6-deoxytetracyclines 失效
标题翻译： 9 - [（取代甘氨酰）酰氨基）] - 6-脱甲基-6-脱氧四环素
公开(公告)号：US5442059A
公开(公告)日：1995-08-15
申请号：US928590
申请日：1992-08-13
申请人： Phaik-Eng Sum , Ving J. Lee , Raymond T. Testa
发明人： Phaik-Eng Sum , Ving J. Lee , Raymond T. Testa
IPC分类号： A61K31/65 , A61P31/00 , A61P31/04 , C07C20060101 , C07C237/26 , C07C239/18 , C07C239/20 , C07C255/50 , C07C271/22 , C07C323/29 , C07D207/06 , C07D207/14 , C07D207/16 , C07D207/30 , C07D209/02 , C07D211/14 , C07D211/56 , C07D213/40 , C07D213/74 , C07D221/22 , C07D231/12 , C07D231/14 , C07D241/04 , C07D241/14 , C07D249/02 , C07D249/04 , C07D249/08 , C07D265/28 , C07D279/04 , C07D295/14 , C07D295/15 , C07D295/215 , C07D295/24 , C07D307/33 , C07D333/20 , C07D333/36 , C07F15/00 , C07C231/12 , C07C233/64
CPC分类号： C07D213/40 , C07C237/26 , C07C239/18 , C07C239/20 , C07C271/22 , C07D295/15 , C07D295/215 , C07D295/24 , C07D333/20 , C07C2103/46
摘要： The invention provides compounds of the formula: ##STR1## wherein R, and R.sup.1 and W are defined in the specification. These compounds are useful as antibiotic agents.
摘要翻译：本发明提供下式的化合物：说明书。这些化合物可用作抗生素。

7. 发明授权

US4910202A Aminomethylphenolic pyrazines 失效
标题翻译：氨甲基苯酚吡嗪
公开(公告)号：US4910202A
公开(公告)日：1990-03-20
申请号：US198946
申请日：1988-05-26
申请人： John A. Schwartz
发明人： John A. Schwartz
IPC分类号： C07D241/28 , A61K20060101 , A61K31/495 , A61K31/4965 , A61P7/10 , C07D20060101 , C07D241/14 , C07D241/26
CPC分类号： C07D241/26
摘要： This invention comprises novel pyrazine amides which are useful as eukalemic diuretics.

8. 发明授权

US4849009A 2-arylmethyliminopyrazines pyrazines, compositions and method of combating undesirable plant growth and of regulating plant growth 失效
公开(公告)号：US4849009A
公开(公告)日：1989-07-18
申请号：US92257
申请日：1987-09-02
申请人： Helmut Zondler , Wolfgang Eckhardt , Robert Nyfeler
发明人： Helmut Zondler , Wolfgang Eckhardt , Robert Nyfeler
IPC分类号： A01N43/54 , A01N43/60 , C07D239/42 , C07D241/14 , C07D241/20 , C07D405/12
CPC分类号： C07D239/42 , A01N43/54 , A01N43/60 , C07D241/20 , C07D405/12
摘要： 2-Arylmethyliminopyrazines of the formula I ##STR1## in which R.sub.1 is SR.sub.2 ; OR.sub.2 ; O--CHR.sub.10 R.sub.2 ; N(R.sub.3)(CHR.sub.10 R.sub.4); N(R.sub.11)(CHR.sub.10 R.sub.4) or NR.sub.3 R.sub.4 ; R.sub.2 is C.sub.1 -C.sub.10 - alkyl which is unsubstituted or substituted by hydroxyl, mercapto, C.sub.1 -C.sub.4 -alkoxycarbonyl, mercaptoalkoxy, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylcarbonyl, mono- or di-C.sub.1 -C.sub.4 -alkylamino, C.sub.1 -C.sub.4 -haloalkoxy, tri-(C.sub.1 -C.sub.4 -alkoxy)-silyl, cyano, nitro or phenyl; C.sub.1 -C.sub.4 -haloalkyl; C.sub.3 -C.sub.8 -alkenyl; (3-methyl-oxetan-3-yl)methyl; C.sub.3 -C.sub.8 -alkynyl; or a radical from the group comprising phenyl, benzyl, C.sub.3 -C.sub.7 -cycloalkyl, furanyl or furfuryl which is unsubstituted or mono-, di- or trisubstituted by identical or different substituents from the group comprising halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkylcarbonyl, nitro, C.sub.1 -C.sub.4 -alkoxy and C.sub.1 -C.sub.4 -haloalkyl; R.sub.3 and R.sub.4 independently of one another are hydrogen; a phenyl or benzyl radical which is unsubstituted or mono-, di-, tri- or tetrasubstituted by identical or different substituents from the group comprising halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkylcarbonyl, nitro, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkylthio and C.sub.1 -C.sub.4 -haloalkylthio; C.sub.1 -C.sub.8 -alkyl; or C.sub.3 -C.sub.6 -cycloalkyl; or R.sub.3 and R.sub.4, together with the nitrogen atom, form a saturated 5- or 6-membered heterocyclic ring which contains up to two heteroatoms from the group comprising N, O and S and can be mono- or disubstituted by C.sub.1 -C.sub.4 -allkyl; R.sub.5 is hydrogen; halogen; C.sub.1 -C.sub.8 -alkyl; C.sub.1 -C.sub.4 -alkoxy; C.sub.1 -C.sub.4 -haloalkyl; nitro; cyano; C.sub.1 -C.sub.4 -haloalkoxy; phenylthio; di-C.sub.1 -C.sub.4 -alkylamino; phenyl; or is phenoxy which is unsubstituted or substituted by the radicals R.sub.8 and R.sub.9 ; and R.sub.6, R.sub.7, R.sub.8 and R.sub.9 independently of one another are hydrogen; halogen; C.sub.1 -C.sub.8 -alkyl; C.sub.1 -C.sub.4 -haloalkyl; C.sub.1 -C.sub.4 -alkoxy; C.sub.1 -C.sub.4 -haloalkoxy; nitro; cyano; or di-C.sub.1 -C.sub.4 -alkylamino; and R.sub.10 and R.sub.11 independently of one another are C.sub.1 -C.sub.4 -alkyl; and salts of compounds of the formula I with acids and bases, process for their preparation and herbicidal or plant growth-regulating compositions containing compounds of the formula I.

9. 发明授权

US3954753A 2-Aroyl-3-amino pyrazines and the 3(-2haloacetamide derivatives thereof 失效
标题翻译： 2-芳酰基-3-氨基吡嗪及其3（ - 2-卤代乙酰胺衍生物）
公开(公告)号：US3954753A
公开(公告)日：1976-05-04
申请号：US549566
申请日：1975-02-13
申请人： George Francis Field , Leo Henryk Sternbach , Armin Walser
发明人： George Francis Field , Leo Henryk Sternbach , Armin Walser
IPC分类号： C07D241/20 , C07D401/06 , C07D403/06 , C07D487/04 , C07D241/14
CPC分类号： C07D401/06 , C07D241/20 , C07D403/06 , C07D487/04
摘要： Novel pyrazino-1,4-diazepines are disclosed together with processes for their preparation and novel intermediates used in these processes. These novel diazepines are useful as sedatives, muscle-relaxants and anti-convulsants.
摘要翻译：公开了新的吡嗪-1,4-二氮杂及其制备方法和用于这些方法的新型中间体。这些新的二氮杂类药物可用作镇静剂，肌肉松弛剂和抗惊厥药。

10. 发明申请

US20210213011A1 CGRP RECEPTOR ANTAGONISTS 有权
公开(公告)号：US20210213011A1
公开(公告)日：2021-07-15
申请号：US17139299
申请日：2020-12-31
申请人： Heptares Therapeutics Limited
发明人： John Andrew Christopher , Miles Stuart Congreve , Sarah Joanne Bucknell , Francesca Deflorian , Mark Pickworth , Jonathan Stephen Mason
IPC分类号： A61K31/496 , C07D401/14 , C07D498/10 , C07D241/14 , C07D471/04 , C07D498/20
摘要： The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.

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