公开(公告)号：US08710234B2

公开(公告)日：2014-04-29

申请号：US14033005

申请日：2013-09-20

Applicant: Mitsui Chemicals, Inc.

Inventor： Kei Yoshida ,  Takeo Wakita ,  Hiroyuki Katsuta ,  Akiyoshi Kai ,  Yutaka Chiba ,  Kiyoshi Takahashi ,  Hiroko Kato ,  Nobuyuki Kawahara ,  Michikazu Nomura ,  Hidenori Daido ,  Junji Maki ,  Shinichi Banba

IPC: C07D213/04 ,  A01N43/40

CPC classification number: C07D333/38 ,  A01N37/22 ,  A01N37/44 ,  A01N43/08 ,  A01N43/10 ,  A01N43/12 ,  A01N43/16 ,  A01N43/30 ,  A01N43/40 ,  A01N43/42 ,  A01N43/54 ,  A01N43/56 ,  A01N43/58 ,  A01N43/60 ,  A01N43/78 ,  A01N43/80 ,  C07C237/42 ,  C07C237/48 ,  C07C317/40 ,  C07C323/42 ,  C07C327/48 ,  C07D207/34 ,  C07D207/416 ,  C07D213/64 ,  C07D213/73 ,  C07D213/81 ,  C07D213/82 ,  C07D213/89 ,  C07D215/52 ,  C07D231/14 ,  C07D231/16 ,  C07D239/28 ,  C07D239/30 ,  C07D241/24 ,  C07D261/18 ,  C07D263/34 ,  C07D275/03 ,  C07D277/56 ,  C07D307/24 ,  C07D307/68 ,  C07D307/84 ,  C07D307/85 ,  C07D309/08 ,  C07D309/28 ,  C07D317/46 ,  C07D317/62 ,  C07D333/68

Abstract: A compound represented by Formula (1): The compound can be used as insecticides.

Abstract translation: 由式（1）表示的化合物：该化合物可以用作杀虫剂。

公开(公告)号：US08658689B2

公开(公告)日：2014-02-25

申请号：US13589867

申请日：2012-08-20

Applicant: Gregory D. Cuny ,  Xin Teng ,  Junying Yuan ,  Alexei Degterev ,  John A. Porco, Jr.

Inventor： Gregory D. Cuny ,  Xin Teng ,  Junying Yuan ,  Alexei Degterev ,  John A. Porco, Jr.

IPC: A61K31/40 ,  C07D207/36

CPC classification number: C07D417/12 ,  C07D207/34 ,  C07D231/14 ,  C07D241/24 ,  C07D263/34 ,  C07D277/56 ,  C07D285/06 ,  C07D307/68 ,  C07D307/84 ,  C07D333/38

Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-α) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-α induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.

Abstract translation: 本发明具有抑制肿瘤坏死因子α（TNF-α）诱导的人工坏死的一系列杂环衍生物。 本发明的杂环化合物由式（I）和（Ia） - （Ie）描述，并且显示出抑制人Jurkat T细胞的FADD缺陷型变体中的TNF-α诱导的人工死亡。 本发明还涉及以本发明化合物为特征的药物组合物。 本发明的化合物和组合物也可以用于治疗棘球菌根可能起重要作用的病症。

公开(公告)号：US20130317100A1

公开(公告)日：2013-11-28

申请号：US13884179

申请日：2011-11-11

Applicant: Frank Richter ,  Erwin Schreiner ,  Samo Pirc ,  Anton Copar

Inventor： Frank Richter ,  Erwin Schreiner ,  Samo Pirc ,  Anton Copar

IPC: C07D307/81 ,  A61K31/343

CPC classification number: C07D307/81 ,  A61K31/343 ,  C07D307/82 ,  C07D307/84

Abstract: The present invention relates to a process for the preparation of 3-aroyl-5-aminobenzofuran derivatives useful as antiarrhythmic drugs which avoids the use of nitro intermediates.

Abstract translation: 本发明涉及一种制备可用作抗心律失常药物的3-芳酰基-5-氨基苯并呋喃衍生物的方法，其避免使用硝基中间体。

公开(公告)号：US20130296296A1

公开(公告)日：2013-11-07

申请号：US13758098

申请日：2013-02-04

Applicant: ASTRAZENECA AB

Inventor： Johan ANDERSSON ,  Helena GYBACK ,  Anh JOHANSSON ,  Christian Erik LINDE ,  Jonas MALMSTROM ,  Gunnar NORDVALL ,  Tatjana WEIGELT ,  Gitte TERP

IPC: C07D405/12 ,  C07D417/14 ,  C07D307/85 ,  C07D405/14

CPC classification number: C07D405/12 ,  C07D307/84 ,  C07D307/85 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to compounds of formula (I), wherein R1 is heteroaryl or heterocyclyl, optionally substituted; R2 is C1-4alkyl, heterocyclyl, C1-4alkylaryl, C1-4alkylheteroaryl, carbocyclyl, C1-4alkylheterocyclyl, heterocyclyl-heteroaryl, aryl-heterocyclyl, carbocyclyl-heteroaryl, heterocyclyl-aryl, optionally substituted; R3 is hydrogen or C1-4alkyl, or R2 and R3 may together with the nitrogen atom, form a saturated ring system containing 4, 5 or 6 ring forming atoms, and optionally substituted; R4 is hydrogen, halogen, methyl or methoxy; to pharmaceutical composition containing said compounds and to the use of said compounds in therapy, for instance in treating cognitive disorders. The present invention further relates to new intermediates useful in the preparation thereof.

Abstract translation: 本发明涉及式（I）化合物，其中R 1是杂芳基或任选被取代的杂环基; R 2是C 1-4烷基，杂环基，C 1-4烷基芳基，C 1-4烷基杂芳基，碳环基，C 1-4烷基杂环基，杂环基 - 杂芳基，芳基 - 杂环基，碳环基 - 杂芳基，杂环基 - 芳基，任选取代的; R 3是氢或C 1-4烷基，或者R 2和R 3可以与氮原子一起形成含有4,5或6个成环原子的饱和环系，并且任选被取代; R4是氢，卤素，甲基或甲氧基; 含有所述化合物的药物组合物和所述化合物在治疗中的用途，例如用于治疗认知障碍。 本发明还涉及可用于其制备的新中间体。

公开(公告)号：US20130287727A1

公开(公告)日：2013-10-31

申请号：US13870782

申请日：2013-04-25

Applicant: INSCENT, INC.

Inventor： Daniel F. Woods ,  Spiros Dimitratos

IPC: A01N43/40 ,  C07D207/12 ,  C07D207/24 ,  C07D211/74 ,  G06F17/18 ,  C07D307/83 ,  C07D307/84 ,  A01N43/36 ,  A01N43/12 ,  C07D211/42 ,  C07D307/82

CPC classification number: A01N43/40 ,  A01N33/18 ,  A01N35/06 ,  A01N35/10 ,  A01N37/32 ,  A01N43/12 ,  A01N43/36 ,  A01N43/38 ,  A01N43/60 ,  A01N43/78 ,  A01N43/82 ,  A01N43/90 ,  C07D207/12 ,  C07D207/24 ,  C07D211/42 ,  C07D211/74 ,  C07D307/82 ,  C07D307/83 ,  C07D307/84 ,  G06F17/18

Abstract: The present specification discloses psyllid attractants, compositions comprising such attractants, lures, traps and other devices using such attractants, methods and uses to attract, capture and/or kill psyllids using such attractants, compositions and/or lures, traps and/or other devices, and methods and uses for monitoring a psyllid population using such attractants, compositions and/or lures, traps and/or other devices.

Abstract translation: 本说明书公开了木质链引诱剂，包含这种引诱剂的组合物，诱饵，陷阱和使用这种引诱剂的其它装置，使用这种引诱剂，组合物和/或诱饵，捕集器和/或其它装置吸引，捕获和/或杀死木脂蛋白的方法和用途 以及使用这种引诱剂，组合物和/或诱饵，捕集器和/或其他装置监测木质部种群的方法和用途。

公开(公告)号：US08168825B2

公开(公告)日：2012-05-01

申请号：US10587990

申请日：2004-12-24

Applicant: Kei Yoshida ,  Takeo Wakita ,  Hiroyuki Katsuta ,  Akiyoshi Kai ,  Yutaka Chiba ,  Kiyoshi Takahashi ,  Hiroko Kato ,  Nobuyuki Kawahara ,  Michikazu Nomura ,  Hidenori Daido ,  Junji Maki ,  Shinichi Banba

Inventor： Kei Yoshida ,  Takeo Wakita ,  Hiroyuki Katsuta ,  Akiyoshi Kai ,  Yutaka Chiba ,  Kiyoshi Takahashi ,  Hiroko Kato ,  Nobuyuki Kawahara ,  Michikazu Nomura ,  Hidenori Daido ,  Junji Maki ,  Shinichi Banba

IPC: C07C233/65 ,  A01N37/18

CPC classification number: C07D333/38 ,  A01N37/22 ,  A01N37/44 ,  A01N43/08 ,  A01N43/10 ,  A01N43/12 ,  A01N43/16 ,  A01N43/30 ,  A01N43/40 ,  A01N43/42 ,  A01N43/54 ,  A01N43/56 ,  A01N43/58 ,  A01N43/60 ,  A01N43/78 ,  A01N43/80 ,  C07C237/42 ,  C07C237/48 ,  C07C317/40 ,  C07C323/42 ,  C07C327/48 ,  C07D207/34 ,  C07D207/416 ,  C07D213/64 ,  C07D213/73 ,  C07D213/81 ,  C07D213/82 ,  C07D213/89 ,  C07D215/52 ,  C07D231/14 ,  C07D231/16 ,  C07D239/28 ,  C07D239/30 ,  C07D241/24 ,  C07D261/18 ,  C07D263/34 ,  C07D275/03 ,  C07D277/56 ,  C07D307/24 ,  C07D307/68 ,  C07D307/84 ,  C07D307/85 ,  C07D309/08 ,  C07D309/28 ,  C07D317/46 ,  C07D317/62 ,  C07D333/68

Abstract: An object of the present invention is to provide a compound represented by Formula (1): wherein A1, A2, A3 and A4 each represent a carbon atom, a nitrogen atom or an oxidized nitrogen atom; R1 and R2 each represent a hydrogen atom, an optionally substituted alkyl group or an optionally substituted C1-C4 alkylcarbonyl group; G1 and G2 each represent an oxygen atom or a sulfur atom; X, which may be identical or different each other, represents a hydrogen atom, a halogen atom, a C1-C3 alkyl group or a trifluoromethyl group; n is an integer of 0 to 4; and Q1 represents an optionally substituted phenyl group, an optionally substituted naphthyl group or an optionally substituted heterocyclic group; Q2 represents a phenyl group or heterocyclic group having one or more substituents, at least one of the substituent being any of a C1-C4 haloalkoxy group, a C2-C6 perfluoroalkyl group, a C1-C6 perfluoroalkylthio group, a C1-C6 perfluoroalkylsulfinyl group and a C1-C6 perfluoroalkylsulfonyl group, an insecticide comprising the compound as the active ingredient, and a process for preparation thereof.

Abstract translation: 本发明的目的是提供由式（1）表示的化合物：其中A1，A2，A3和A4各自表示碳原子，氮原子或氧化的氮原子; R 1和R 2各自表示氢原子，任选取代的烷基或任选取代的C 1 -C 4烷基羰基; G1和G2各自表示氧原子或硫原子; X可以相同或不同，表示氢原子，卤素原子，C1-C3烷基或三氟甲基; n为0〜4的整数。 并且Q 1表示任选取代的苯基，任选取代的萘基或任选取代的杂环基; Q2表示具有一个或多个取代基的苯基或杂环基，所述取代基中的至少一个为C1-C4卤代烷氧基，C2-C6全氟烷基，C1-C6全氟烷硫基，C1-C6全氟烷基亚磺酰基 和C1-C6全氟烷基磺酰基，其包含该化合物作为活性成分的杀虫剂及其制备方法。

公开(公告)号：US08163751B2

公开(公告)日：2012-04-24

申请号：US12748951

申请日：2010-03-29

Applicant: Hartmut Strobel ,  Paulus Wohlfart ,  Alena Safarova ,  Armin Walser ,  Teri Suzuki ,  Karl Schönafinger ,  Ramalinga M. Dharanipragada

Inventor： Hartmut Strobel ,  Paulus Wohlfart ,  Alena Safarova ,  Armin Walser ,  Teri Suzuki ,  Karl Schönafinger ,  Ramalinga M. Dharanipragada

IPC: A61K31/495 ,  A61K31/44 ,  C07D241/36 ,  C07D513/02

CPC classification number: C07D213/81 ,  C07C233/58 ,  C07C233/65 ,  C07C233/66 ,  C07C233/74 ,  C07C233/76 ,  C07C235/42 ,  C07C235/54 ,  C07C235/84 ,  C07C237/38 ,  C07C237/42 ,  C07C255/57 ,  C07C255/60 ,  C07C309/66 ,  C07C309/73 ,  C07C311/08 ,  C07C311/16 ,  C07C311/21 ,  C07C317/44 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2602/08 ,  C07D207/34 ,  C07D213/56 ,  C07D213/82 ,  C07D215/48 ,  C07D235/08 ,  C07D241/24 ,  C07D249/04 ,  C07D261/18 ,  C07D295/185 ,  C07D307/78 ,  C07D307/84 ,  C07D317/60 ,  C07D333/24 ,  C07D401/06

Abstract: The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1-R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B is CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description. These compounds are useful in the upregulation of endothelial nitric oxide synthase (eNOS), and may therefore be useful for the manufacture of medicaments for the treatment of cardiovascular diseases, stable or unstable angina pectoris, coronary heart disease, Prinzmetal angina, acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease, endothelial dysfunction, atherosclerosis, restenosis, endothelial damage after PTCA, hypertension, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular hypertension, chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, diabetes or diabetes complications, nephropathy or retinopathy, angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, osteoporosis, restricted memory performance, a restricted ability to learn, or for the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives.

Abstract translation: 本发明涉及根据通式（I）的酰化茚满基胺，其中R 1 -R 4具有在描述中给出的含义，A是CH 2，CHOH或CH-（C 1 -C 3 - 烷基），B是CH 2或CH- （C 1 -C 3 - 烷基），R 5是可以被描述中所列取代基取代的芳基或杂芳基。 这些化合物可用于内皮一氧化氮合酶（eNOS）的上调，因此可用于制备用于治疗心血管疾病，稳定或不稳定型心绞痛，冠心病，Prinzmetal心绞痛，急性冠状动脉综合征， 心脏衰竭，心肌梗塞，中风，血栓形成，外周动脉闭塞性疾病，内皮功能障碍，动脉粥样硬化，再狭窄，PTCA后的内皮损伤，高血压，原发性高血压，肺动脉高压，继发性高血压，肾血管性高血压，慢性肾小球肾炎，勃起功能障碍，室性心律失常， 糖尿病或糖尿病并发症，肾病或视网膜病变，血管生成，支气管哮喘，慢性肾功能衰竭，肝硬化，骨质疏松症，受限记忆能力，受限的学习能力或降低绝经后妇女的心血管危险或摄入避孕药 。

公开(公告)号：US08101590B2

公开(公告)日：2012-01-24

申请号：US11513972

申请日：2006-08-31

Applicant: Phaik-Eng Sum ,  Tarek Suhayl Mansour ,  David Brian How ,  Darrin William Hopper ,  Matthew Douglas Vera ,  Joshua James Sabatini ,  Jaechul Shim

Inventor： Phaik-Eng Sum ,  Tarek Suhayl Mansour ,  David Brian How ,  Darrin William Hopper ,  Matthew Douglas Vera ,  Joshua James Sabatini ,  Jaechul Shim

IPC: A61K31/65 ,  C07C237/26

CPC classification number: C07D333/38 ,  C07C237/26 ,  C07C271/22 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2603/46 ,  C07C2603/74 ,  C07D207/416 ,  C07D209/42 ,  C07D213/81 ,  C07D213/82 ,  C07D215/48 ,  C07D307/68 ,  C07D307/84 ,  C07D317/34

Abstract: This invention provides compounds of Formula I having the structure where R1, R2, R3 and A are defined in the specification or a pharmaceutically acceptable salt thereof useful as antibacterial agents. Compounds according to Formula (II): where Q, R4, R5, R6 and R10 and A are defined in the specification are useful as chemical intermediates.

Abstract translation: 本发明提供式I化合物，其具有在说明书中定义R1，R2，R3和A的结构或其药学上可接受的盐作为抗菌剂。 根据式（II）的化合物：其中Q，R 4，R 5，R 6和R 10和A在说明书中定义可用作化学中间体。

公开(公告)号：US08080582B2

公开(公告)日：2011-12-20

申请号：US12542833

申请日：2009-08-18

Applicant: Hardy Chan ,  Chung Faye Chao ,  Vallapa Soong

Inventor： Hardy Chan ,  Chung Faye Chao ,  Vallapa Soong

IPC: A61K31/343 ,  C07D307/80

CPC classification number: C07D405/14 ,  C07D307/84

Abstract: The present application discloses derivatives of 8-epiblechnic acid and use thereof in treating a disease related to endothelin receptor A or endothelin-1 (ET-1) over-expression, such as hypertension, cancer, atherosclerosis, and myocardial infarction.

Abstract translation: 本申请公开了8-表意醇酸的衍生物及其在治疗与内皮素受体A或内皮素-1（ET-1）过表达相关的疾病如高血压，癌症，动脉粥样硬化和心肌梗死的疾病中的用途。

公开(公告)号：US08048887B2

公开(公告)日：2011-11-01

申请号：US12554193

申请日：2009-09-04

Applicant: Kap-Sun Yeung ,  Kyle E. Parcella ,  John A. Bender ,  Brett R. Beno ,  Katharine A. Grant-Young ,  Ying Han ,  Piyasena Hewawasam ,  John F. Kadow ,  Andrew Nickel

Inventor： Kap-Sun Yeung ,  Kyle E. Parcella ,  John A. Bender ,  Brett R. Beno ,  Katharine A. Grant-Young ,  Ying Han ,  Piyasena Hewawasam ,  John F. Kadow ,  Andrew Nickel

IPC: A61K31/506 ,  C07D405/02

CPC classification number: C07D307/84 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12 ,  C07D453/00 ,  C07D491/10

Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.