公开(公告)号：US12036195B2

公开(公告)日：2024-07-16

申请号：US17850014

申请日：2022-06-27

Applicant: Nanyang Technological University

Inventor： Ho Sup Yoon ,  Sreekanth Rajan ,  Hui Ting Toh ,  Xuewei Liu ,  Hui Yao

IPC: A61K31/191 ,  C07C59/90 ,  C07K14/705 ,  G16B35/20

CPC classification number: A61K31/191 ,  C07C59/90 ,  C07K14/70567 ,  G16B35/20

Abstract: Co-crystals comprising the Nuclear receptor related 1 protein-ligand binding domain (Nurr1-LBD) and a cyclopentenone prostaglandin are provided. Also provided are methods of identifying or designing Nurr1-modulating ligands and compounds based on the crystal structures described herein as well as the applications of said ligands and compounds as Nurr1 modulators or medicaments.

公开(公告)号：US20180297934A1

公开(公告)日：2018-10-18

申请号：US15823448

申请日：2017-11-27

Applicant: KINDEX PHARMACEUTICALS, INC.

Inventor： Veera KONDA ,  Jan URBAN ,  Anuradha DESAI ,  Clinton J. DAHLBERG ,  Brian J. CARROLL

IPC: C07C225/14 ,  C07C49/743 ,  C07C49/707 ,  C07C69/612 ,  C07C69/28 ,  A61K31/122 ,  C07C69/78 ,  C07C69/96 ,  C07C59/90 ,  A61K31/135 ,  C07C251/42

CPC classification number: C07C225/14 ,  A61K31/122 ,  A61K31/135 ,  C07C49/707 ,  C07C49/743 ,  C07C59/90 ,  C07C69/02 ,  C07C69/22 ,  C07C69/28 ,  C07C69/612 ,  C07C69/614 ,  C07C69/78 ,  C07C69/96 ,  C07C251/42 ,  C07C2601/08 ,  C07C2601/10

Abstract: The present application provides novel tetrahydro-isohumulone (THIAA) derivatives and substantially enantiomerically pure compositions and pharmaceutical formulations thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPARγ, inhibit inflammation, and treat conditions associated with inflammation and conditions responsive to PPARγ modulation such as diabetes.

公开(公告)号：US20180184651A1

公开(公告)日：2018-07-05

申请号：US15738928

申请日：2016-06-28

Applicant: KING ABDULLAH UNIVERSITY OF SCIENCE AND TECHNOLOGY

Inventor： Salim AL-BABILI

IPC: A01N35/02 ,  C07C49/242 ,  C07C59/90 ,  C07C62/38 ,  A01N37/42

CPC classification number: A01N35/02 ,  A01N37/42 ,  A01N49/00 ,  C07C49/242 ,  C07C59/90 ,  C07C62/38 ,  C07C2601/16

Abstract: New plant growth regulators, including compounds and compositions, and methods of use including for promoting root growth. The compounds are carotenoid oxidation products, and a preferred example is 3-OH-β-apo-13-Carotenone. A method comprising promoting the growth of at least one plant with use of an effective amount of at least one composition comprising an effective amount of at least one compound which is represented by A-B-C, wherein B is a bivalent polyene moiety, A is a monovalent moiety linked to B by a six-membered carbon ring, wherein the ring has at least one substituent linked to the ring by an oxygen atom, and C is a monovalent moiety linked to B by a carbonyl group. Synergistic effects can be used with combinations of compounds.

公开(公告)号：US09781930B2

公开(公告)日：2017-10-10

申请号：US14794415

申请日：2015-07-08

Applicant: Valent BioSciences Corporation

Inventor： Gary T. Wang ,  Daniel Heiman ,  Gregory D. Venburg ,  Eiki Nagano ,  Marci Surpin ,  Joseph H. Lustig

IPC: C07C69/738 ,  C07D277/64 ,  C07C231/12 ,  C07C255/31 ,  C07C51/16 ,  C07C253/30 ,  C07C67/44 ,  C07C235/78 ,  C07C59/90 ,  A01N37/42 ,  A01N43/78 ,  A01N53/00

CPC classification number: A01N37/42 ,  A01N43/78 ,  A01N53/00 ,  C07B2200/07 ,  C07C51/16 ,  C07C59/90 ,  C07C67/44 ,  C07C69/738 ,  C07C231/12 ,  C07C235/78 ,  C07C253/30 ,  C07C255/31 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/16 ,  C07D277/64

Abstract: The invention relates to a novel class of (S)-3′-substituted-abscisic acid derivatives and (±)-3′-substituted-abscisic acid derivatives, and methods of synthesizing the derivatives.

公开(公告)号：US20170247311A1

公开(公告)日：2017-08-31

申请号：US15509225

申请日：2015-09-08

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yan Shi ,  Ying Wang ,  Peter T.W. Cheng ,  Shung C. Wu

IPC: C07C59/72 ,  A61K31/192 ,  C07D213/64 ,  A61K31/4418 ,  C07D213/70 ,  C07D271/06 ,  A61K31/4245 ,  C07D213/65 ,  C07D277/24 ,  A61K31/426 ,  C07D307/79 ,  A61K31/343 ,  C07D213/68 ,  C07D237/14 ,  A61K31/50 ,  C07D309/12 ,  A61K31/351 ,  A61K45/06

CPC classification number: C07C59/72 ,  A61K31/192 ,  A61K31/343 ,  A61K31/351 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/4418 ,  A61K31/50 ,  A61K45/06 ,  C07C59/90 ,  C07C62/34 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2602/50 ,  C07C2603/50 ,  C07D213/64 ,  C07D213/643 ,  C07D213/65 ,  C07D213/68 ,  C07D213/70 ,  C07D237/14 ,  C07D271/06 ,  C07D277/24 ,  C07D307/79 ,  C07D309/12

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.

公开(公告)号：US09676698B2

公开(公告)日：2017-06-13

申请号：US15178112

申请日：2016-06-09

Applicant: LEO Laboratories Limited

Inventor： Thomas Hogberg ,  Gunnar Grue-Sorensen ,  Xifu Liang ,  Anne Marie Horneman ,  Anders Klarskov Petersen

IPC: C07C49/00 ,  C07C67/00 ,  C07C69/00 ,  C07D319/00 ,  C07C67/08 ,  C07C67/297 ,  C07D319/08 ,  C07C49/753 ,  C07C59/90 ,  C07F7/18 ,  C07C67/14 ,  C07D317/70 ,  C07D493/08

CPC classification number: C07C67/08 ,  C07C49/753 ,  C07C59/90 ,  C07C67/14 ,  C07C67/297 ,  C07C2603/86 ,  C07C2603/98 ,  C07D317/70 ,  C07D319/08 ,  C07D493/08 ,  C07F7/1804 ,  Y02P20/55 ,  C07C69/533

Abstract: The present invention relates to methods of producing ingenol-3-angelate (I) from ingenol (II). Furthermore, the invention relates to intermediates useful for the synthesis of ingenol-3-angelate (I) from ingenol (II) and to methods of producing said intermediates.

公开(公告)号：US20170057941A1

公开(公告)日：2017-03-02

申请号：US15088964

申请日：2016-04-01

Applicant: Allergan, Inc.

Inventor： Yariv Donde ,  Jeremiah H. Nguyen

IPC: C07D333/40 ,  C07D333/38 ,  C07C59/90

CPC classification number: C07D333/40 ,  C07C59/56 ,  C07C59/90 ,  C07C65/19 ,  C07C323/52 ,  C07C2601/10 ,  C07D213/30 ,  C07D213/55 ,  C07D277/56 ,  C07D307/68 ,  C07D333/24 ,  C07D333/38 ,  C07D409/04 ,  C07D409/10

Abstract: Disclosed herein is a compound of the formula Therapeutic methods, compositions, and medicaments, related thereto are also disclosed.

Abstract translation: 还公开了与此相关的治疗方法，组合物和药物。

公开(公告)号：US20170036987A1

公开(公告)日：2017-02-09

申请号：US15301697

申请日：2015-04-06

Applicant: Sanford-Burnham Medical Research Institute

Inventor： Raveendra Panickar DHANYA ,  Douglas J. SHEFFLER ,  Nicholas D. P. COSFORD

IPC: C07C65/40 ,  C07D311/16 ,  C07C69/92 ,  C07C255/56 ,  C07D257/04 ,  C07F5/04 ,  C07C259/10 ,  C07C311/51 ,  C07F5/02 ,  C07C251/48 ,  C07D271/07 ,  C07D285/08 ,  C07D295/16 ,  C07C235/46 ,  C07C49/84 ,  C07D213/50 ,  C07D295/26 ,  C07C235/54 ,  C07D307/54 ,  C07D213/55 ,  C07D277/24 ,  C07D333/24 ,  C07D241/12 ,  C07D285/12 ,  C07D239/26 ,  C07D307/68 ,  C07D213/80 ,  C07D213/79 ,  C07D241/24 ,  C07D213/64 ,  C07D213/70 ,  C07C59/90

CPC classification number: C07C65/40 ,  C07C49/84 ,  C07C59/90 ,  C07C65/05 ,  C07C65/10 ,  C07C69/92 ,  C07C235/46 ,  C07C235/54 ,  C07C251/48 ,  C07C255/56 ,  C07C259/10 ,  C07C311/51 ,  C07C2601/02 ,  C07C2601/08 ,  C07D213/50 ,  C07D213/55 ,  C07D213/64 ,  C07D213/68 ,  C07D213/70 ,  C07D213/79 ,  C07D213/80 ,  C07D239/26 ,  C07D241/12 ,  C07D241/24 ,  C07D257/04 ,  C07D271/06 ,  C07D271/07 ,  C07D277/24 ,  C07D285/08 ,  C07D285/12 ,  C07D295/108 ,  C07D295/16 ,  C07D295/26 ,  C07D307/42 ,  C07D307/54 ,  C07D307/68 ,  C07D311/16 ,  C07D333/24 ,  C07F5/025 ,  C07F5/04 ,  C07F7/025

Abstract: Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor positive allosteric modulators (PAMS), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

Abstract translation: 本文提供的是小分子活性代谢型谷氨酸亚型2和-3受体阳性变构调节剂（PAMS），包含该化合物的组合物，以及使用包含该化合物的化合物和组合物的方法。

公开(公告)号：US09562025B2

公开(公告)日：2017-02-07

申请号：US15044685

申请日：2016-02-16

Applicant: Allianz Pharmascience Ltd.

Inventor： Charles Shih ,  Qian Shi ,  Hui-Kang Wang

IPC: C07C49/255 ,  C07C69/618 ,  C07D295/192 ,  A61K31/00 ,  C07D295/16 ,  C07C309/65 ,  C07D277/46 ,  C07C235/78 ,  A61K31/12 ,  A61K31/165 ,  A61K31/426 ,  A61K31/5375 ,  A61K31/255 ,  C07C59/90 ,  C07C69/738 ,  C07C235/74 ,  C07D277/44

CPC classification number: C07D295/16 ,  A61K31/12 ,  A61K31/165 ,  A61K31/255 ,  A61K31/426 ,  A61K31/5375 ,  C07C49/255 ,  C07C59/90 ,  C07C69/618 ,  C07C69/738 ,  C07C235/74 ,  C07C235/78 ,  C07C309/65 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D277/44 ,  C07D277/46 ,  C07D295/192 ,  Y10S514/884

Abstract: The present invention relates to compounds having at least one (substituted phenyl)-propenal moiety. The compounds are useful in treating a subject suffering from an androgen receptor-associated medical condition, e.g., inflammation, acne, alopecia, hirsutism, wound, Spinal and Bulbar Muscular Atrophy (SBMA, Kennedy's Disease), unwanted immune response, immune disorder, or cancer.

Abstract translation: 本发明涉及具有至少一个（取代的苯基） - 丙烯酸部分的化合物。 这些化合物可用于治疗患有雄激素受体相关医学状况的受试者，例如炎症，痤疮，脱发，多毛症，伤口，脊髓和Bulbar肌肉萎缩（SBMA，肯尼迪氏病），不想要的免疫应答，免疫疾病或 癌症。

公开(公告)号：US20160237012A1

公开(公告)日：2016-08-18

申请号：US15045259

申请日：2016-02-17

Applicant: Golden Biotechnology Corporation

Inventor： Sheng-Yung LIU ,  Chih-Ming Chen

IPC: C07C39/19 ,  C07C37/14 ,  C07D307/33 ,  C07C69/96 ,  C07C68/00 ,  C07C49/743 ,  C07C57/42

CPC classification number: C07C39/19 ,  C07C35/18 ,  C07C35/21 ,  C07C35/48 ,  C07C49/248 ,  C07C49/743 ,  C07C49/753 ,  C07C59/90 ,  C07C69/013 ,  C07C69/017 ,  C07C69/145 ,  C07C69/16 ,  C07C69/96 ,  C07C215/44 ,  C07C225/20 ,  C07C323/17 ,  C07C2601/16 ,  C07D307/33 ,  C07F7/1804

Abstract: Provided herein are compositions and processes of making of anticancer compounds useful for cancer treatments. These cyclohexenone compounds show an unexpected result against certain cancer cells compared to their known analogs.

Abstract translation: 本文提供了可用于癌症治疗的抗癌化合物的制备的组合物和方法。 与其已知的类似物相比，这些环己烯酮化合物对某些癌细胞显示出意想不到的结果。