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1. 发明申请

WO2021030554A1 PROCESS OF MAKING CFTR MODULATORS 审中-公开
公开(公告)号：WO2021030554A1
公开(公告)日：2021-02-18
申请号：PCT/US2020/046116
申请日：2020-08-13
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： ANGELL, Paul , COCHRAN, John E. , LITTLER, Benjamin J. , SIESEL, David Andrew , URBINA, Armando , ANDERSON, Corey Don , CLEMENS, Jeremy J. , CLEVELAND, Thomas , COON, Timothy Richard , FRIEMAN, Bryan , HADIDA RUAH, Sara Sabina , MCCARTNEY, Jason , MILLER, Mark Thomas , PARASELLI, Prasuna , PIERRE, Fabrice , SWIFT, Sara E. , ZHOU, Jinglan
IPC分类号： C07D207/08 , C07D207/09 , C07D213/61 , C07D213/62 , C07D213/70 , C07D213/74 , C07D231/20 , C07D401/04 , C07D401/14 , C07D513/22
摘要： The disclosure provides processes for synthesizing Compound I, and pharmaceutically acceptable salts thereof.

2. 发明申请

WO2017086966A1 MOLECULES HAVING PESTICIDAL UTILITY, PESTICIDAL COMPOSITIONS, AND PROCESSES, RELATED THERETO 审中-公开
标题翻译：具有杀虫剂用途，杀虫剂组合物和工艺的分子，与其相关的
公开(公告)号：WO2017086966A1
公开(公告)日：2017-05-26
申请号：PCT/US2015/061521
申请日：2015-11-19
申请人： DOW AGROSCIENCES LLC
发明人： GOMEZ, Luis E. , SRIGIRIRAJU, Lakshmipathi , ROY, Agamananda
IPC分类号： A61K31/44 , C07D401/04 , C07D213/62
CPC分类号： C07D401/04 , A01N43/56
摘要： This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests.
摘要翻译：本公开涉及具有杀节肢动物门纲，软体动物门和线虫纲害虫的杀虫剂应用的分子领域，含有这种分子的杀虫组合物，以及使用这种杀虫组合物对抗这些害虫的方法。

3. 发明申请

WO2017086965A1 MOLECULES HAVING PESTICIDAL UTILITY, PESTICIDAL COMPOSITIONS, AND PROCESSES, RELATED THERETO 审中-公开
公开(公告)号：WO2017086965A1
公开(公告)日：2017-05-26
申请号：PCT/US2015/061516
申请日：2015-11-19
申请人： DOW AGROSCIENCES LLC
发明人： GOMEZ, Luis E. , TRULLINGER, Tony K. , HUNTER, Ricky , SRIGIRIRAJU, Lakshmipathi , YI, Jee-Hwan , RUSHTON, Mary
IPC分类号： A61K31/44 , C07D401/04 , C07D213/62
CPC分类号： C07D401/04 , A01N43/56
摘要： This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests.

4. 发明申请

WO2012170377A1 PROCESS FOR PREPARING [(3-HYDROXYPYRIDINE-2-CARBONYL)AMINO]ALKANOIC ACIDS, ESTERS AND AMIDES 审中-公开
标题翻译：制备[（3-羟基吡啶-2-羰基）氨基]亚烷基酸，酯和胺的方法
公开(公告)号：WO2012170377A1
公开(公告)日：2012-12-13
申请号：PCT/US2012/040833
申请日：2012-06-05
申请人： AKEBIA THERAPEUTICS INC. , LANTHIER, Christopher, M. , GORIN, Boris , OUDENES, Jan , DIXON, Craig, Edward , LU, Alan, Quigbo , COPP, James, Densmore , JANUSZ, John, Michael
发明人： LANTHIER, Christopher, M. , GORIN, Boris , OUDENES, Jan , DIXON, Craig, Edward , LU, Alan, Quigbo , COPP, James, Densmore , JANUSZ, John, Michael
IPC分类号： C07D213/62
CPC分类号： C07D213/81 , C07D213/79 , C07D213/803
摘要： Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino} acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, [(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino} acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibitors or for treating conditions wherein prolyl hydroxylase inhibition is desired.
摘要翻译：公开了制备[（3-羟基吡啶-2-羰基）氨基] - 链烷酸，衍生物，特别是5-芳基取代和5-杂芳基取代的[（3-羟基吡啶-2-羰基）氨基}乙酸的方法。还公开了制备[（3-羟基吡啶-2-羰基） - 氨基]乙酸的前药的方法，例如[（3-羟基吡啶-2-羰基）氨基}乙酸酯和{[3-羟基吡啶-2 - 羰基]氨基}乙酸酰胺。所公开的化合物可用作脯氨酰羟化酶抑制剂或用于治疗需要脯氨酰羟化酶抑制的条件。

5. 发明申请

WO00037438A1 NOVEL THIO-AMINOTETRALIN COMPOUNDS USEFUL IN PAIN MANAGEMENT 审中-公开
标题翻译：新型硫胺素化合物有助于疼痛管理
公开(公告)号：WO00037438A1
公开(公告)日：2000-06-29
申请号：PCT/SE1999/002401
申请日：1999-12-17
IPC分类号： A61K31/135 , A61K31/165 , A61K31/196 , A61K31/216 , A61K31/4402 , A61K31/505 , A61K31/662 , A61P25/04 , C07B53/00 , C07B55/00 , C07C53/18 , C07C323/30 , C07C323/31 , C07C323/37 , C07C323/52 , C07C323/58 , C07C323/60 , C07C323/61 , C07C323/65 , C07D213/70 , C07D239/38 , C07D249/10 , C07D249/14 , C07F9/40 , C07C323/10 , A61K31/095 , A61K31/4196 , A61P29/00 , C07D213/62 , C07D239/32
CPC分类号： C07D249/14 , C07C323/30 , C07C323/37 , C07C323/52 , C07C323/60 , C07C323/65 , C07C2602/10 , C07F9/4006
摘要： The present invention relates to novel thio-aminotetralin compounds of formula (I) wherein Z, X, R1, R2, R3, R4, R5, and R6 are defined herein. The compounds are useful in pain management.
摘要翻译：本发明涉及式（I）的新型硫代 - 氨基四氢萘化合物，其中Z，X，R 1，R 2，R 3，R 4，R 5和R 6在本文中定义。这些化合物可用于疼痛管理。

6. 发明申请

WO98053819A1 THERAPEUTIC AGENT FOR ERECTION FAILURE 审中-公开
标题翻译：治疗失败的治疗药物
公开(公告)号：WO98053819A1
公开(公告)日：1998-12-03
申请号：PCT/JP1998/002378
申请日：1998-05-29
IPC分类号： A61K9/00 , A61K31/00 , A61K31/4745 , A61K31/519 , C07D487/06 , A61K31/435 , A61K31/12 , A61K31/165 , A61K31/235 , A61K31/40 , A61K31/415 , A61K31/44 , A61K31/505 , A61K31/52 , A61K38/08 , A61K45/00 , C07D209/08 , C07D209/88 , C07D213/62 , C07D213/72 , C07D217/02 , C07D217/24 , C07D235/06 , C07D235/08 , C07D235/24 , C07D239/34 , C07D239/42 , C07D239/84 , C07D239/91 , C07D239/94 , C07D471/00 , C07D471/04 , C07D471/06 , C07D471/14 , C07D473/18 , C07D473/24 , C07D473/30 , C07D487/04 , C07D487/14 , C07D491/048 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D519/00
CPC分类号： C07D487/06 , A61K9/0043 , A61K9/0056 , A61K31/00 , A61K31/4745 , A61K31/519
摘要： A therapeutic agent for erection failure and gynecoid incompetence, which is free from the problems involved in oral administration and direct injection, is safe, and exhibits excellent effect. A therapeutic agent for erection failure and gynecoid incompetence for intranasal administration, percutaneous administration, or mucosal administration, such as oral mucosal administration or penis mucosal administration, characterized by containing as the active ingredient at least one compound having cyclic GMP phosphodiesterase inhibitory activity or salt thereof.
摘要翻译：勃起功能衰竭和妇科无能的治疗剂不含口服和直接注射所涉及的问题，是安全的，效果显着。用于鼻内给药，经皮给药或粘膜给药如口腔粘膜给药或阴茎粘膜给药的勃起衰竭和妇科无能的治疗剂，其特征在于含有至少一种具有环状GMP磷酸二酯酶抑制活性的化合物或其盐。

7. 发明申请

WO98042661A1 AROMATIC AND HETEROCYCLIC NITRATO DERIVATIVES 审中-公开
标题翻译：芳香和杂环NITRATO衍生物
公开(公告)号：WO98042661A1
公开(公告)日：1998-10-01
申请号：PCT/IL1998/000144
申请日：1998-03-26
IPC分类号： A61K31/21 , A61K31/222 , A61K31/385 , A61K31/426 , A61K31/4365 , A61K31/44 , A61P9/08 , A61P9/10 , C07C321/10 , C07C321/28 , C07C323/12 , C07C323/19 , C07C323/20 , C07C323/56 , C07C323/62 , C07C327/32 , C07D213/70 , C07D213/79 , C07D213/80 , C07D213/82 , C07D277/14 , C07D277/20 , C07D277/56 , C07D339/04 , C07D339/08 , C07D495/04 , C07C323/42 , C07D213/62 , C07D213/78 , C07D277/06 , C07D327/06 , C07D339/02 , C07D401/12 , C07D471/04 , C07D487/04
CPC分类号： C07D213/70 , C07C323/12 , C07C323/19 , C07C323/56 , C07C323/62 , C07C327/32 , C07D213/80 , C07D213/82 , C07D277/14 , C07D339/04 , C07D339/08 , C07D495/04
摘要： An organic compound is provided which contains at least one nitric oxide donor group and at least one group being, or being adapted to be converted in vivo to a free sulfhydryl group. A preferred compound contains at least one sulfhydryl group, either in the reduced -SH form or in the oxidized -S-S-disulfide form.
摘要翻译：提供了一种有机化合物，其含有至少一个一氧化氮供体基团和至少一个基团，或适于在体内转化为游离巯基。优选的化合物含有至少一个以还原-SH形式或氧化的-S-S-二硫化物形式的巯基。

8. 发明申请

WO1986001202A1 PYRIDONE ESTERS AS INOTROPIC AGENTS 审中-公开
标题翻译：作为无机物质的甜玉米饼
公开(公告)号：WO1986001202A1
公开(公告)日：1986-02-27
申请号：PCT/US1985001468
申请日：1985-08-01
申请人： AMERICAN HOSPITAL SUPPLY CORPORATION
发明人： AMERICAN HOSPITAL SUPPLY CORPORATION , STOUT, David, M. , YAMAMOTO, Diane, M. , BARCELON-YANG, Cynthia
IPC分类号： C07D213/62
CPC分类号： C07D213/80 , C07C45/70 , C07C49/175 , C07D213/62 , C07D213/85 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/06 , C07D413/04
摘要： Compounds of formula (I) wherein R is hydrogen, lower alkyl, halo, cyano, hydroxy, amino, lower alkylamino, -CH2NH2, -CH2OH or -COOR''; R' is hydrogen, lower cycloalkyl or lower alkyl; R'' is lower alkenyl, lower alkynyl, lower cycloalkyl, -(W)nY wherein W is straight or branched chain lower alkyl or lower alkenyl, n is 0 to 5, and Y is Ar, lower cycloalkyl, lower alkenyl, lower alkynyl, -COOZ wherein Z is lower alkyl, a compound of formula (II), or NAB wherein A and B are, independently, lower alkyl, benzyl or substituted benzyl, and Ar is 2, 3 or 4-pyridyl, pyridazinyl, pyrimidinyl, quinolyl, isoquinolyl, phthalazinyl, quinazolinyl, thiazolyl, phenyl, benzyl, furyl, tetrahydrofuryl or thienyl, unsubstituted or substituted with lower alkyl, lower alkoxy, halo, amino, or -CF3; R''' is -COOR'', a compound of formulas (III) and X is oxygen or nitrogen; or a pharmaceutically acceptable salt thereof, and their use in the treatment of impaired ventricular myocardial contractility. The compounds exhibit cardiotonic activity.
摘要翻译：式（I）的化合物，其中R是氢，低级烷基，卤素，氰基，羟基，氨基，低级烷基氨基，-CH 2 NH 2，-CH 2 OH或-COOR“ R'是氢，低级环烷基或低级烷基; R“是低级烯基，低级炔基，低级环烷基， - （W）nY其中W是直链或支链低级烷基或低级烯基，n是0-5，Y是Ar，低级环烷基，低级烯基，低级炔基，其中Z为低级烷基的-COOZ，式（II）的化合物或NAB，其中A和B独立地为低级烷基，苄基或取代的苄基，Ar为2,3或4-吡啶基，哒嗪基，嘧啶基，喹啉基，异喹啉基，酞嗪基，喹唑啉基，噻唑基，苯基，苄基，呋喃基，四氢呋喃基或噻吩基，未取代或被低级烷基，低级烷氧基，卤素，氨基或-CF 3取代。 R“是-COOR”，式（III）和X的化合物是氧或氮; 或其药学上可接受的盐，以及它们在治疗心室心肌收缩受损中的应用。化合物表现出强心活性。

9. 发明申请

WO2015092412A1 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2015092412A1
公开(公告)日：2015-06-25
申请号：PCT/GB2014/053756
申请日：2014-12-18
申请人： ISIS INNOVATION LIMITED
发明人： SCHOFIELD, Christopher Joseph , RYDZIK, Anna , MCDONOUGH, Michael , CHOWDHURY, Rasheduzzaman
IPC分类号： C07D215/20 , C07D213/62
CPC分类号： C07D215/20 , C07D213/62
摘要： A compound which is a pyridine or isoquinoline derivative of formula (I), or a pharmaceutically acceptable salt thereof, which is useful in the inhibition of γ- butyrobetaine hydroxylase (BBOX). The compounds are particularly useful in treatment of cardiovascular disease and diabetes. (I)
摘要翻译：作为式（I）的吡啶或异喹啉衍生物或其药学上可接受的盐，可用于抑制γ-丁酸甜菜碱羟化酶（BBOX）的化合物。该化合物特别可用于治疗心血管疾病和糖尿病。（一世）

10. 发明申请

WO2014098259A1 PEST CONTROL AGENT 审中-公开
标题翻译：虫控制剂
公开(公告)号：WO2014098259A1
公开(公告)日：2014-06-26
申请号：PCT/JP2013/085022
申请日：2013-12-19
申请人： ISHIHARA SANGYO KAISHA, LTD.
发明人： KIRIYAMA, Kazuhisa , MATSUMOTO, Masahiro , YOSHIDA, Kotaro , BOLDBAATAR, DamdinSuren , JUKUROGI, Tatsuya , UMEMOTO, Nao , KANI, Tatsuya , MATSUDA, Yoko , TANAKA, Kumiko , KANUMA, Michiko , SHIMADA, Tatsuya
IPC分类号： A01N43/40 , C07D213/72 , C07D213/73 , C07D213/74 , C07D213/75 , C07D401/02 , C07D213/24 , C07D213/60 , C07D213/61 , C07D213/62 , C07D213/70
CPC分类号： C07D213/16 , A01N43/40 , C07D213/24 , C07D213/60 , C07D213/61 , C07D213/62 , C07D213/70 , C07D213/72 , C07D213/73 , C07D213/74 , C07D213/75 , C07D401/06
摘要： Objects of the present invention are to provide a compound which is highly active against pests, to provide a pest control agent comprising the compound, and to provide a method for controlling a pest by applying the compound. The present invention provides a 4-(arylethynyl)pyridine or a salt thereof, a pest control agent which comprises the 4-(arylethynyl)pyridine or salt thereof as an active ingredient, and a method for controlling a pest by applying the 4-(arylethynyl)pyridine or salt thereof in an effective amount.
摘要翻译：本发明的目的是提供一种对害虫具有高度活性的化合物，以提供包含该化合物的害虫控制剂，并提供通过施用化合物来控制害虫的方法。本发明提供一种4-（芳基乙炔基）吡啶或其盐，其包含4-（芳基乙炔基）吡啶或其盐作为活性成分的害虫控制剂，以及通过施用4-（芳基乙炔基）吡啶或其盐。

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