公开(公告)号：US09381228B2

公开(公告)日：2016-07-05

申请号：US12303343

申请日：2007-06-08

Applicant: Tracy Robson ,  Andrea Valentine ,  Martin Gerard O'Rourke ,  David Hirst

Inventor： Tracy Robson ,  Andrea Valentine ,  Martin Gerard O'Rourke ,  David Hirst

IPC: A61K6/00 ,  A61K31/00 ,  A61K38/00 ,  A61K38/16 ,  A61K38/17 ,  A61K39/00 ,  A61K39/395 ,  C07K1/00 ,  A61K31/7105 ,  C07K14/705 ,  A61K45/06

CPC classification number: C07K14/705 ,  A61K9/127 ,  A61K31/00 ,  A61K31/4412 ,  A61K31/7105 ,  A61K38/1709 ,  A61K38/177 ,  A61K39/3955 ,  A61K45/06 ,  A61K47/551 ,  A61K47/60 ,  C12N9/90 ,  C12Y502/01008 ,  A61K2300/00

Abstract: Disclosed are methods and compositions that employ FKBP-L polypeptides for modulating angiogenesis and/or tumor metastasis. The FKBP-L polypeptides may be used for the treatment of disorders mediated by angiogenesis such as cancer.

Abstract translation: 公开了使用FKBP-L多肽调节血管生成和/或肿瘤转移的方法和组合物。 FKBP-L多肽可用于治疗由血管生成如癌症介导的病症。

公开(公告)号：US20160136174A1

公开(公告)日：2016-05-19

申请号：US14945147

申请日：2015-11-18

Applicant: Celgene Corporation

Inventor： Benjamin M. COHEN ,  John F. TRAVERSE ,  Jean XU ,  Ying LI

IPC: A61K31/5377

CPC classification number: A61K31/5377 ,  A61K31/4035 ,  A61K31/4412 ,  C07D401/04

Abstract: Salts and solid forms of 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a stereoisomer thereof, are disclosed. Compositions comprising and methods of using the salts and solid forms are also disclosed.

Abstract translation: 公开了3-（4 - （（4-（吗啉代甲基）苄基）氧基）-1-氧代异吲哚啉-2-基）哌啶-2,6-二酮的盐和固体形式。 还公开了组合物和使用盐和固体形式的方法。

公开(公告)号：US09334527B2

公开(公告)日：2016-05-10

申请号：US14290642

申请日：2014-05-29

Applicant: EPIZYME, INC.

Inventor： Kevin Wayne Kuntz ,  Sarah Kathleen Knutson ,  Timothy James Nelson Wigle

IPC: A61P35/00 ,  C12Q1/68 ,  C07D473/34 ,  C12Q1/48 ,  G01N33/50 ,  G01N33/574 ,  A61K31/711 ,  A61K38/17 ,  C07D405/12 ,  A61P35/02

CPC classification number: A61K31/5377 ,  A61K31/4412 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/551 ,  A61K31/7076 ,  A61K31/711 ,  A61K38/17 ,  C07D405/12 ,  C07D473/34 ,  C12Q1/48 ,  C12Q1/68 ,  G01N33/5011 ,  G01N33/57426 ,  G01N2333/91011 ,  G01N2333/91017 ,  G01N2800/52 ,  Y10T436/143333

Abstract: The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.

公开(公告)号：US20160120986A1

公开(公告)日：2016-05-05

申请号：US14926949

申请日：2015-10-29

Applicant: Textile-Based Delivery, Inc.

Inventor： David Anderson ,  Jordan Schindler ,  Erik Scott Goebel

IPC: A61K47/34 ,  A61K9/70 ,  A61K31/573 ,  A61K47/32 ,  A61K31/203 ,  A61K31/122 ,  A61K31/12 ,  A61K31/4412 ,  A61K31/343 ,  A61K31/555

CPC classification number: A61K9/70 ,  A61K9/0024 ,  A61K9/0092 ,  A61K31/12 ,  A61K31/122 ,  A61K31/203 ,  A61K31/343 ,  A61K31/4166 ,  A61K31/4412 ,  A61K31/555 ,  A61K31/573 ,  A61K31/616 ,  A61K47/34 ,  A61M37/00

Abstract: Disclosed herein are delivery systems including coated and uncoated yarns, yarn precursors, threads, fibers, and other substrates for the constant or near-constant release of active compounds, as well as methods for manufacturing such delivery systems. The yarns, yarn precursors, threads, fibers, and other substrates can include a cross-linked hydrophobic elastomer and an active compound. One or more coatings that are impermeable or substantially impermeable to the active compound may partially or fully occlude the yarn or substrate to control release rates of the active compound. The delivery systems may be used in a variety of applications, including the making of articles of clothing, textiles, and fabrics, and may be used in methods of treating various conditions and diseases.

Abstract translation: 本文公开了包括涂覆和未涂覆的纱线，纱线前体，丝线，纤维和用于活性化合物的恒定或接近恒定释放的其它基底的递送系统，以及用于制造这种递送系统的方法。 纱线，纱线前体，丝线，纤维和其它基底可以包括交联的疏水弹性体和活性化合物。 对活性化合物不可渗透或基本不渗透的一种或多种涂层可以部分或完全闭塞纱线或底物以控制活性化合物的释放速率。 递送系统可以用于各种应用，包括制造衣服，纺织品和织物，并且可以用于治疗各种病症和疾病的方法中。

公开(公告)号：US20160102059A1

公开(公告)日：2016-04-14

申请号：US14872527

申请日：2015-10-01

Applicant: RESPIVERT LIMITED ,  TOPIVERT PHARMA LIIMITED

Inventor： Thomas Matthew BAKER ,  Matthew Colin Thor FYFE ,  Geraint JONES ,  Stephen Malcolm THOM

IPC: C07D213/74 ,  A61K31/5377 ,  C07D401/12 ,  A61K31/4545 ,  A61K31/496 ,  C07D413/12 ,  A61K31/551 ,  C07D239/47 ,  A61K31/541 ,  A61K31/553 ,  A61K31/506 ,  A61K31/4439 ,  A61K31/635 ,  C07H19/048 ,  A61K31/706 ,  C07D405/12 ,  C07D453/02 ,  A61K31/4375 ,  C07F9/58 ,  A61K31/675 ,  A61K31/44

CPC classification number: C07D213/74 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K31/553 ,  A61K31/635 ,  A61K31/675 ,  A61K31/7052 ,  A61K31/706 ,  A61K45/06 ,  C07D213/80 ,  C07D239/47 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D453/02 ,  C07F9/58 ,  C07F9/59 ,  C07F9/6512 ,  C07F9/65583 ,  C07H13/08 ,  C07H15/26 ,  C07H19/048 ,  A61K2300/00

Abstract: There are provided compounds of formula I, wherein R1A to R1E, R2 to R4, R5a, L and X1 to X3 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

Abstract translation: 提供式I化合物，其中R1A至R1E，R2至R4，R5a，L和X1至X3具有说明书中给出的含义，哪些化合物具有抗炎活性（例如通过抑制一个或多个成员：家族 的p38丝裂原活化蛋白激酶; Syk激酶;以及Src家族酪氨酸激酶的成员），并且用于治疗，包括药物组合，特别是治疗炎性疾病，包括肺，眼和眼的炎性疾病 肠子

公开(公告)号：US20160097078A1

公开(公告)日：2016-04-07

申请号：US14944796

申请日：2015-11-18

Applicant: ISIS INNOVATION LIMITED

Inventor： Patrick Henry Maxwell ,  Christopher William Pugh ,  Peter John Ratcliffe ,  Christopher Joseph Schofield

IPC: C12Q1/26 ,  C07C323/60 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07C235/80 ,  C07C327/32

CPC classification number: A61K31/455 ,  A01K2217/05 ,  A61K31/137 ,  A61K31/14 ,  A61K31/165 ,  A61K31/166 ,  A61K31/185 ,  A61K31/192 ,  A61K31/194 ,  A61K31/195 ,  A61K31/197 ,  A61K31/198 ,  A61K31/21 ,  A61K31/221 ,  A61K31/223 ,  A61K31/225 ,  A61K31/235 ,  A61K31/24 ,  A61K31/265 ,  A61K31/327 ,  A61K31/44 ,  A61K31/4412 ,  A61K38/00 ,  A61K39/3955 ,  C07C235/80 ,  C07C323/60 ,  C07C327/32 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07K14/4702 ,  C07K16/40 ,  C07K2317/30 ,  C12N9/0071 ,  C12Q1/26 ,  C12Q1/34 ,  G01N33/573 ,  G01N2333/90245 ,  G01N2500/04 ,  G01N2500/20

Abstract: A novel class of hydroxylases is described having the amino acid sequence of SEQ ID NO: 2, 4, 6 and 8, and variants and fragments thereof having HIF hydroxylation activity. The polypeptides of the invention have in particular prolyl hydroxylase activity. An assay method monitors the interaction of the HIF hydroxylase with a substrate. Modulators of HIF hydroxylase are provided for use in the treatment of a condition associated with increased or decreased HIF levels or activity or for the treatment of a condition where it is desirable to modulate HIF levels or activity.

公开(公告)号：US20160074375A1

公开(公告)日：2016-03-17

申请号：US14951313

申请日：2015-11-24

Applicant: INTERMUNE, INC.

Inventor： Gakuji Kiyonaka ,  Yoshihiro Furuya ,  Yusuke Suzuki

IPC: A61K31/4418 ,  A61K9/28 ,  A61K9/20

CPC classification number: A61K31/4418 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/28 ,  A61K9/2813 ,  A61K9/282 ,  A61K9/2866 ,  A61K31/4412 ,  C07D213/64

Abstract: A tablet characterized by comprising 5-methyl-1-phenyl-2-(1H)-pyridone as the main ingredient and, based on the main ingredient, 10 to 50 wt. % excipient, 5 to 40 wt. % disintegrator, 1 to 10 wt. % binder, 0.5 to 5 wt. % lubricant, 2 to 6 wt. % coating basis, and 0.05 to 3 wt. % light-shielding agent, wherein the odor or bitterness of the 5-methyl-1-phenyl-2-(1H)-pyridone is masked and the light stability is improved.

公开(公告)号：US09283213B2

公开(公告)日：2016-03-15

申请号：US14598202

申请日：2015-01-15

Applicant: N30 Pharmaceuticals, Inc.

Inventor： Xicheng Sun ,  Jian Qiu

IPC: C07D401/00 ,  C07D419/00 ,  C07D213/22 ,  C07D417/04 ,  C07D417/14 ,  C07D417/00 ,  C07D405/00 ,  C07D403/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  A61K31/4412 ,  C07D211/88 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14 ,  C07D211/86 ,  C07D409/04 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444

CPC classification number: A61K31/4412 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  C07D211/86 ,  C07D211/88 ,  C07D401/04 ,  C07D401/14 ,  C07D409/04 ,  C07D409/14

Abstract: The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and/or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.

Abstract translation: 本发明涉及可用作S-亚硝基谷胱甘肽还原酶（GSNOR）抑制剂和/或神经激肽-3（NK3）受体拮抗剂的新型二氢吡啶-2（1H） - 酮化合物，包含这些化合物的药物组合物，以及制备和使用 一样。

公开(公告)号：US09278930B2

公开(公告)日：2016-03-08

申请号：US14628261

申请日：2015-02-22

Applicant: Aerpio Therapeutics Inc.

Inventor： Robert Shalwitz ,  Joseph H. Gardner

IPC: A61K31/4412 ,  C07D211/96 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  C07D213/02 ,  C07D213/69 ,  C07D401/06 ,  C07D401/14 ,  C07D417/06 ,  C07D491/113 ,  A61K31/4427 ,  A61K31/444 ,  A61K45/06 ,  C07D211/86

CPC classification number: C07D211/96 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K45/06 ,  C07D211/86 ,  C07D213/02 ,  C07D213/69 ,  C07D401/06 ,  C07D401/14 ,  C07D417/06 ,  C07D491/113 ,  Y02A50/401 ,  Y02A50/465 ,  Y02A50/47 ,  Y02A50/471 ,  Y02A50/473 ,  Y02A50/475 ,  Y02A50/478 ,  Y02A50/481

Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1α) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1α prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1α.

Abstract translation: 本文公开了用于控制缺氧诱导型转录因子1-α（HIF-1α）的活性和与其相关的疾病，病症或综合征，尤其是外周血管疾病（PVD），冠状动脉疾病（CAD），心脏 失败，缺血和贫血。 还公开了包含HIF-1α脯氨酰羟化酶抑制剂的药物组合物，其用于治疗与其相关的HIF-1α的活性的疾病，病症和/或综合征。

公开(公告)号：US09259409B2

公开(公告)日：2016-02-16

申请号：US13981360

申请日：2012-01-24

Applicant: Fabrizio G. Mastronardi

Inventor： Fabrizio G. Mastronardi

IPC: A01N37/08 ,  A61K31/215 ,  A01N37/34 ,  A61K31/275 ,  A61K31/216 ,  A61K31/165 ,  A61K45/06 ,  C07C405/00 ,  A61K31/16 ,  A61K31/4196 ,  A61K31/4412 ,  A61K31/4706 ,  A61K31/53 ,  A61K31/5575

CPC classification number: A61K31/5575 ,  A61K31/16 ,  A61K31/165 ,  A61K31/216 ,  A61K31/4196 ,  A61K31/4412 ,  A61K31/4706 ,  A61K31/53 ,  A61K45/06 ,  C07C405/00 ,  A61K2300/00

Abstract: The present invention relates to methods and compositions for the treatment of neuropsychiatric conditions (e.g., bipolar disorder) by administration of prostaglandin or prostaglandin derivatives (e.g., latanoprost) to a subject (e.g., a human).

Abstract translation: 本发明涉及通过向受试者（例如人）施用前列腺素或前列腺素衍生物（例如拉坦前列素）来治疗神经精神状况（例如双相性精神障碍）的方法和组合物。