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71. 发明申请

US20160145210A1 SUBSTITUTED PYRIDINES AS SODIUM CHANNEL BLOCKERS 有权
公开(公告)号：US20160145210A1
公开(公告)日：2016-05-26
申请号：US14961026
申请日：2015-12-07
申请人： Purdue Pharma L.P.
发明人： Laykea Tafesse , Jiangchao Yao
IPC分类号： C07D213/50 , C07D213/56 , C07D213/57
CPC分类号： C07D213/50 , C07D213/24 , C07D213/30 , C07D213/46 , C07D213/56 , C07D213/57 , C07D213/81
摘要： The invention relates to substituted pyridine and pyrimidine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1, R2a, R2b, A1, A2, X, and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.

72. 发明申请

US20160130214A1 1,3-DIAMINOCYCLOPENTANE CARBOXAMIDE DERIVATIVES 有权
标题翻译： 1,3-二氨基环戊烷羧酰胺衍生物
公开(公告)号：US20160130214A1
公开(公告)日：2016-05-12
申请号：US14898491
申请日：2014-05-09
申请人： MERCK PATENT GMBH
发明人： Christos TSAKLAKIDIS , Wolfgang STAEHLE , Birgitta LEUTHNER , Paul CZODROWSKI , Thomas FUCHSS
IPC分类号： C07C233/79 , A61K31/423 , C07D213/56 , A61K31/451 , A61K31/166 , C07C231/10 , C07D277/66 , A61K31/428 , C07D235/18 , A61K31/4184 , C07D487/04 , A61K31/519 , C07D233/58 , A61K31/4164 , C07C255/60 , A61K31/277 , C07C253/30 , C07D403/04 , A61K31/501 , C07D263/57
CPC分类号： C07C233/79 , A61K31/166 , A61K31/277 , A61K31/4164 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/451 , A61K31/501 , A61K31/519 , C07C231/10 , C07C235/42 , C07C253/30 , C07C255/57 , C07C255/60 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07D209/08 , C07D209/14 , C07D209/30 , C07D209/34 , C07D209/42 , C07D213/56 , C07D215/12 , C07D231/12 , C07D231/56 , C07D233/26 , C07D233/58 , C07D235/06 , C07D235/18 , C07D235/26 , C07D249/18 , C07D263/57 , C07D277/62 , C07D277/66 , C07D309/04 , C07D317/50 , C07D319/18 , C07D401/04 , C07D403/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D498/04
摘要： Compounds of the formula I in which R1, R4, R6, R, X1, X2, X3, X4, q and W have the meanings indicated in claim 1, are inhibitors of fatty acid synthase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
摘要翻译：其中R 1，R 4，R 6，R 4，X 1，X 2，X 3，X 4，q和W具有权利要求1所示含义的式Ⅰ化合物是脂肪酸合成酶的抑制剂，特别可用于治疗疾病如癌症，心血管疾病，中枢神经系统损伤和不同形式的炎症。

73. 发明授权

US09334259B2 Aryloxyacetamide compound and pesticide 有权
标题翻译：芳氧基乙酰胺化合物和农药
公开(公告)号：US09334259B2
公开(公告)日：2016-05-10
申请号：US14377052
申请日：2013-02-12
申请人： Nippon Soda Co., Ltd.
发明人： Hironori Furukawa , Daisuke Hanai , Tetsuo Tamai , Yasuyuki Shiinoki
IPC分类号： C07D401/12 , A01N43/40 , A01N43/54 , C07D215/20 , C07D239/26 , C07D417/12 , C07C381/10 , C07D213/40 , C07D213/68 , A01N41/06 , A01N43/42 , A01N43/78 , C07D213/56 , C07D277/62
CPC分类号： C07D401/12 , A01N41/06 , A01N43/40 , A01N43/42 , A01N43/54 , A01N43/78 , C07C381/10 , C07D213/40 , C07D213/56 , C07D213/68 , C07D215/20 , C07D239/26 , C07D277/62 , C07D417/12
摘要： The present invention provides a pesticide comprising an aryloxyacetamide compound represented by formula (IV) (wherein in formula (IV), R1a represents an alkyl group or the like, R2 to R5 independently represents an alkyl group, X represents a halogen atom or the like, n represents an integer of 0 to 5, Z represents an oxygen atom or a sulfur atom) or salt thereof as an active ingredient.
摘要翻译：本发明提供一种农药，其含有式（IV）所示的芳氧基乙酰胺化合物（式中，式（IV）中，R 1a表示烷基等，R 2〜R 5独立地表示烷基，X表示卤素原子等，n表示0〜5的整数，Z表示氧原子或硫原子）或其盐作为有效成分。

74. 发明授权

US09296716B2 Androgen receptor ligands 有权
标题翻译：雄激素受体配体
公开(公告)号：US09296716B2
公开(公告)日：2016-03-29
申请号：US14360081
申请日：2012-11-23
申请人： David George Lloyd , Darren Fayne , Mary Jane Meegan , Miriam Carr , Gemma Karena Kinsella , Laura Caboni , Wiliam Nicholas Jagoe , Billy Egan , Fernando Blanco , D. Clive Williams
发明人： David George Lloyd , Darren Fayne , Mary Jane Meegan , Miriam Carr , Gemma Karena Kinsella , Laura Caboni , Wiliam Nicholas Jagoe , Billy Egan , Fernando Blanco , D. Clive Williams
IPC分类号： C07D307/91 , C07D209/56 , C07D307/92 , A61K31/166 , A61K31/175 , A61K31/343 , C07C251/86 , C07D213/56 , C07D307/54
CPC分类号： C07D307/92 , A61K31/166 , A61K31/175 , A61K31/343 , C07C251/86 , C07D213/56 , C07D307/54
摘要： Non ligand binding pocket antagonists for the human androgen receptor. The androgen receptor (AR) is a member of the Nuclear Receptor (NR) family and its role is to modulate the biological effects of the endogenous androgens, testosterone (tes) and dihydrotestosterone (DHT). Synthetic androgens and anti-androgens have therapeutic value in the treatment of various androgen dependent conditions, from regulation of male fertility to prostate cancer. Current treatment of prostate cancer (PCa) typically involves administration of ‘classical’ antiandrogens, competitive inhibitors of natural AR ligands, DHT and tes, for the ligand binding pocket (LBP) in the C-terminal ligand binding domain (LBD) of the AR. However, prolonged LBP-targeting can often lead to androgen resistance and alternative therapies and therapeutic strategies are urgently required. Disclosed herein are a class of non-steroidal, small molecule AR antagonists which inhibit the transcriptional activity of the AR by non LBP-mediated modulation. The novel class reported demonstrates full (‘true’) antagonism in AR with low micromolar potency, high selectivity over both the Estrogen Receptors alpha and beta (ERα and ERβ) and the Glucocorticoid Receptor (GR) and only micromolar partial antagonism in the Progesterone Receptor (PR). Data provide compelling evidence for such non-LBP intervention as an alternative approach to classical PCa therapy. (Formula I).
摘要翻译：用于人雄激素受体的非配体结合口袋拮抗剂。雄激素受体（AR）是核受体（NR）家族的成员，其作用是调节内源雄激素，睾丸激素（tes）和二氢睾酮（DHT）的生物学作用。合成雄激素和抗雄激素在治疗各种雄激素依赖性病症方面具有治疗价值，从调节男性生殖力到前列腺癌。前列腺癌（PCa）的当前治疗通常涉及对AR的C-末端配体结合结构域（LBD）中的配体结合口袋（LBP）施用“经典”抗雄激素，天然AR配体的竞争性抑制剂，DHT和tes 。然而，长期的LBP靶向通常可导致雄激素抵抗，迫切需要替代疗法和治疗策略。本文公开了一类非甾体的小分子AR拮抗剂，其通过非LBP介导的调节来抑制AR的转录活性。报道的新一代报道在AR中具有低的（“真实”）拮抗作用，具有低微摩尔效力，对雌激素受体α和β（ERα和ER和bgr）和糖皮质激素受体（GR）的高选择性，而孕激素中仅有微摩尔部分拮抗作用受体（PR）。数据为这种非LBP干预提供了令人信服的证据，作为经典PCa治疗的替代方法。（式I）。

75. 发明授权

US09278961B2 Pyridyl inhibitors of hedgehog signalling 有权
公开(公告)号：US09278961B2
公开(公告)日：2016-03-08
申请号：US12960609
申请日：2010-12-06
申请人： Janet L. Gunzner , Daniel Sutherlin , Mark S. Stanley , Liang Bao , Georgette M. Castanedo , Rebecca L. Lalonde , Shumei Wang , Mark E. Reynolds , Scott J. Savage , Kimberly Malesky , Michael S. Dina , Michael F. T. Koehler
发明人： Janet L. Gunzner , Daniel Sutherlin , Mark S. Stanley , Liang Bao , Georgette M. Castanedo , Rebecca L. Lalonde , Shumei Wang , Mark E. Reynolds , Scott J. Savage , Kimberly Malesky , Michael S. Dina , Michael F. T. Koehler
IPC分类号： C07D213/38 , C07D417/12 , C07D401/14 , A61K31/44 , C07D213/40 , C07D213/56 , C07D213/70 , C07D213/75 , C07D213/81 , C07D213/82 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/04 , C07F9/58
CPC分类号： C07D213/16 , C07D213/38 , C07D213/40 , C07D213/56 , C07D213/70 , C07D213/75 , C07D213/81 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07F9/58
摘要： The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.

76. 发明申请

US20160052911A1 HETEROARYL COMPOUNDS AS SODIUM CHANNEL BLOCKERS 有权
标题翻译：异氟醚化合物作为钠通道阻塞剂
公开(公告)号：US20160052911A1
公开(公告)日：2016-02-25
申请号：US14928945
申请日：2015-10-30
申请人： Purdue Pharma L.P.
发明人： Jiangchao Yao
IPC分类号： C07D401/12 , C07D239/26 , C07D213/643 , C07D213/56
CPC分类号： C07D401/12 , C07D213/56 , C07D213/57 , C07D213/643 , C07D213/65 , C07D239/26
摘要： The invention relates to aryl substituted compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein Het, G, A, R, and n are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
摘要翻译：本发明涉及式（I）的芳基取代的化合物及其药学上可接受的盐，前体药物或溶剂合物，其中Het，G，A，R和n如说明书所述定义。本发明还涉及式I化合物用于治疗对钠通道阻断有反应的病症。本发明的化合物特别适用于治疗疼痛。

77. 发明授权

US09265768B2 Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols as phosphodiesterase inhibitors 有权
标题翻译： 1-苯基-2-吡啶基烷基醇的衍生物作为磷酸二酯酶抑制剂
公开(公告)号：US09265768B2
公开(公告)日：2016-02-23
申请号：US14164527
申请日：2014-01-27
申请人： Chiesi Farmaceutici S.p.A.
发明人： Elisabetta Armani , Gabriele Amari , Carmelida Capaldi , Oriana Esposito , Ilaria Peretto
IPC分类号： C07D211/82 , A61K31/435 , A61K31/5377 , C07D213/89 , C07D213/69 , A61K31/44 , A61K31/4439 , A61K31/496 , A61M15/00 , A61M16/14 , C07D213/55 , C07D213/56 , C07D401/12 , C07D413/12 , C07D417/12
CPC分类号： A61K31/5377 , A61K31/44 , A61K31/4439 , A61K31/496 , A61M15/0045 , A61M15/009 , A61M16/14 , C07D213/55 , C07D213/56 , C07D213/69 , C07D213/89 , C07D401/12 , C07D413/12 , C07D417/12
摘要： The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
摘要翻译：本发明涉及磷酸二酯酶4（PDE4）酶的抑制剂。更具体地，本发明涉及作为1-苯基-2-吡啶基烷基醇的衍生物的化合物，制备这些化合物的方法，含有它们的组合物及其治疗用途。

78. 发明授权

US09254284B2 Apoptosis signal-regulating kinase inhibitor 有权
标题翻译：细胞凋亡信号调节激酶抑制剂
公开(公告)号：US09254284B2
公开(公告)日：2016-02-09
申请号：US14254342
申请日：2014-04-16
申请人： Gilead Sciences, Inc.
发明人： Gregory Notte
IPC分类号： A61K31/44 , C07D213/56 , A61K31/4439 , C07D401/14 , C07D233/56 , C07D401/04
CPC分类号： C07D401/14 , A61K9/0053 , A61K9/20 , A61K31/4439 , A61K45/06 , C07D213/56 , C07D233/56 , C07D401/04
摘要： The present invention relates to a compound of formula (I): The compound has apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis.
摘要翻译：本发明涉及式（I）化合物：该化合物具有凋亡信号调节激酶（“ASK1”）抑制活性，因此可用于治疗肾病，糖尿病性肾病和肾纤维化等疾病。

79. 发明申请

US20160024009A1 Novel Sulfonamide TRPA1 Receptor Antagonists 有权
标题翻译：新型磺酰胺TRPA1受体拮抗剂
公开(公告)号：US20160024009A1
公开(公告)日：2016-01-28
申请号：US14772622
申请日：2014-03-06
申请人： ARIO PHARMA LIMITED
发明人： Francesca Fruttarolo , Maria Giovanna Pavani , Serena Bencivenni , Raffaele Gatti , Mauro Napoletano
IPC分类号： C07D213/56 , C07C311/19 , C07D401/04 , C07D409/14 , C07D213/89 , C07C311/20 , C07D213/64 , C07D213/73 , C07D333/34 , C07D409/12 , C07D213/74
CPC分类号： C07D213/56 , C07C311/19 , C07C311/20 , C07D213/40 , C07D213/64 , C07D213/73 , C07D213/74 , C07D213/89 , C07D333/34 , C07D401/04 , C07D409/12 , C07D409/14
摘要： The invention discloses compounds of Formula (I). The compounds of formula (I) are TRPA1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of TRPA1 receptors.
摘要翻译：本发明公开了式（I）的化合物。式（I）化合物是TRPA1拮抗剂，可用作药物组合物的活性成分，用于治疗通过抑制TRPA1受体而改善的疼痛和其它症状。

80. 发明授权

US09221843B2 Heteroaryl inhibitors of PDE4 有权
标题翻译： PDE4的杂芳基抑制剂
公开(公告)号：US09221843B2
公开(公告)日：2015-12-29
申请号：US14349688
申请日：2013-10-24
申请人： Tetra Discovery Partners, LLC
发明人： Mark E. Gurney , Timothy J. Hagen , Xuesheng Mo , A. Samuel Vellekoop , Donna L. Romero , Robert F. Campbell , Joel R. Walker , Lei Zhu
IPC分类号： C07D213/24 , C07D239/26 , A61K31/4418 , C07F5/02 , C07D213/72 , C07D403/12 , C07D413/14 , C07D213/74 , C07D221/04 , C07D409/04 , C07D409/14 , C07D413/12 , C07D495/04 , C07D213/56 , A61K45/06 , A61K31/435 , A61K31/505 , A61K31/517 , A61K31/53 , A61K31/69 , C07D239/70 , C07D251/22 , C07D401/12 , C07D405/04
CPC分类号： C07F5/027 , A61K31/435 , A61K31/44 , A61K31/4418 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/53 , A61K31/5377 , A61K31/69 , A61K45/06 , C07D213/56 , C07D213/72 , C07D213/74 , C07D221/04 , C07D239/26 , C07D239/70 , C07D251/22 , C07D251/30 , C07D251/42 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/04 , C07D409/04 , C07D409/14 , C07D413/12 , C07D413/14 , C07D495/04 , C07F5/025
摘要： The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.
摘要翻译：本发明涉及用作治疗或预防疾病的磷酸二酯酶4（PDE4）抑制剂的化合物和方法。

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