公开(公告)号：US20240308951A1

公开(公告)日：2024-09-19

申请号：US18379142

申请日：2023-10-11

Applicant: Acucela Inc.

Inventor： Claes Olof BAVIK ,  Susan Hayes HENRY ,  Ryo KUBOTA ,  Vladimir A. KUKSA

IPC: C07C215/08 ,  A61K31/137 ,  A61K31/138 ,  A61K31/35 ,  A61K31/765 ,  A61K45/06 ,  C07C211/27 ,  C07C217/20 ,  C07C323/32 ,  C07D309/06

CPC classification number: C07C215/08 ,  A61K31/137 ,  A61K31/138 ,  A61K31/35 ,  A61K31/765 ,  A61K45/06 ,  C07C211/27 ,  C07C217/20 ,  C07C323/32 ,  C07D309/06

Abstract: Methods are provided herein for the treatment of ophthalmic diseases or conditions such as an ophthalmic disease or disorder associated with diabetes in a patient. Also provided herein are methods of treating retinopathy of prematurity in a patient. Further, provided herein are methods for treating wet age-related macular degeneration in a patient. The methods comprise administration of compounds disclosed herein to a patient in need thereof that inhibit or slow one or more signs or symptoms of such conditions.

公开(公告)号：US11446261B2

公开(公告)日：2022-09-20

申请号：US16865195

申请日：2020-05-01

Applicant: Acucela Inc.

Inventor： Ian L. Scott ,  Vladimir A. Kuksa ,  Mark W. Orme ,  Thomas L. Little, Jr. ,  Anna Gall ,  Feng Hong

IPC: A61K31/137 ,  C07C217/60 ,  C07C217/62 ,  C07C217/64 ,  C07C217/72 ,  C07C225/16 ,  C07C229/38 ,  C07C233/18 ,  C07C235/08 ,  C07C251/86 ,  C07C279/08 ,  C07C317/28 ,  C07C323/25 ,  C07D277/24 ,  C07D309/06 ,  C07C217/20 ,  C07C215/20 ,  C07C309/06 ,  C07C217/84 ,  C07C323/33 ,  A61K31/165 ,  A61K31/222

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

公开(公告)号：US20220281803A1

公开(公告)日：2022-09-08

申请号：US17612013

申请日：2020-05-18

Applicant: SINGAPORE HEALTH SERVICES PTE LTD ,  AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH ,  TAN TOCK SENG HOSPITAL PTE LTD

Inventor： Thet Tun AUNG ,  Jianguo LI ,  Jun Jie KOH ,  Lakshminarayanan RAJAMANI ,  Roger BEUERMAN ,  Tiang Hwee Donald TAN ,  Mercy Halleluyah PERIAYAH ,  Chandra Shekhar VERMA ,  Swaine CHEN ,  Timothy BARKHAM

IPC: C07C217/20 ,  A61P31/04 ,  A61K47/02 ,  C07C279/14 ,  C07D213/30 ,  C07D233/60 ,  C07D405/14

Abstract: The present invention relates to a compound comprising a hydrophobic moiety, a linker and N-containing moiety. The present invention also relates to the method of synthesizing the compound and the use of the compound as an antibiotic or an adjuvant for an antibiotic.

公开(公告)号：US20210171435A1

公开(公告)日：2021-06-10

申请号：US16934715

申请日：2020-07-21

Applicant: Acucela Inc.

Inventor： Claes Olof BAVIK ,  Susan Hayes HENRY ,  Ryo KUBOTA ,  Vladimir A. KUKSA

IPC: C07C215/08 ,  C07C323/32 ,  A61K31/35 ,  A61K31/138 ,  A61K45/06 ,  C07C211/27 ,  A61K31/765 ,  C07C217/20 ,  C07D309/06 ,  A61K31/137

Abstract: Methods are provided herein for the treatment of ophthalmic diseases or conditions such as an ophthalmic disease or disorder associated with diabetes in a patient. Also provided herein are methods of treating retinopathy of prematurity in a patient. Further, provided herein are methods for treating wet age-related macular degeneration in a patient. The methods comprise administration of compounds disclosed herein to a patient in need thereof that inhibit or slow one or more signs or symptoms of such conditions.

公开(公告)号：US20190183816A1

公开(公告)日：2019-06-20

申请号：US16043019

申请日：2018-07-23

Applicant: Acucela Inc.

Inventor： Ian L. SCOTT ,  Vladimir A. KUKSA ,  Mark W. ORME ,  Thomas L. LITTLE, JR. ,  Anna GALL ,  Feng HONG

IPC: A61K31/137 ,  C07C317/28 ,  C07C217/84 ,  C07C217/20 ,  C07C217/60 ,  C07C217/62 ,  C07C217/64 ,  A61K31/222 ,  A61K31/165 ,  C07C323/33 ,  C07C215/20 ,  C07D309/06 ,  C07D277/24 ,  C07C323/25 ,  C07C309/06 ,  C07C279/08 ,  C07C251/86 ,  C07C235/08 ,  C07C233/18 ,  C07C229/38 ,  C07C225/16 ,  C07C217/72

CPC classification number: A61K31/137 ,  A61K31/165 ,  A61K31/222 ,  C07C215/20 ,  C07C217/20 ,  C07C217/60 ,  C07C217/62 ,  C07C217/64 ,  C07C217/72 ,  C07C217/84 ,  C07C225/16 ,  C07C229/38 ,  C07C233/18 ,  C07C235/08 ,  C07C251/86 ,  C07C279/08 ,  C07C309/06 ,  C07C317/28 ,  C07C323/25 ,  C07C323/33 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/42 ,  C07D277/24 ,  C07D309/06

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

公开(公告)号：US09481660B2

公开(公告)日：2016-11-01

申请号：US14246741

申请日：2014-04-07

Applicant: Jonathan Daniel Heller ,  Qingqi Chen ,  Rocio Alejandra Lopez ,  Amanda Jean Morris

Inventor： Jonathan Daniel Heller ,  Qingqi Chen ,  Rocio Alejandra Lopez ,  Amanda Jean Morris

IPC: C07C33/26 ,  C07D295/088 ,  C07C37/50 ,  C07C39/367 ,  C07C43/225 ,  C07C43/23 ,  C07C47/27 ,  C07C47/273 ,  C07C217/20 ,  C07D277/24 ,  C07C39/21 ,  C07C43/205 ,  C07C217/54

CPC classification number: C07D295/088 ,  C07C37/50 ,  C07C39/21 ,  C07C39/367 ,  C07C43/2055 ,  C07C43/225 ,  C07C43/23 ,  C07C47/27 ,  C07C47/273 ,  C07C217/20 ,  C07C217/54 ,  C07C255/33 ,  C07D277/24 ,  C07C39/16

Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.

Abstract translation: 本发明涉及去甲二氢愈创木酸衍生物化合物，即丁烷桥改性的二氢愈创木酸（NDGA）化合物和丁烷桥改性的四-O-取代的NDGA化合物，含有它们的药物组合物，制备它们的方法及其使用方法和试剂盒 包括它们用于治疗疾病和病症，特别是由HIV感染，HPV感染或HSV感染引起的或与病毒感染相关的疾病，诸如各种类型的关节炎和炎症性肠病的炎性疾病， 代谢疾病，如糖尿病和高血压，或增殖性疾病，如各种类型的癌症。

公开(公告)号：US09359298B2

公开(公告)日：2016-06-07

申请号：US14368066

申请日：2012-12-18

Applicant: INSTITUTE OF MEDICINAL BIOTECHNOLOGY, CHINESE ACADEMY OF MEDICAL SCIENCES

Inventor： Zhuorong Li ,  Xingyue Ji ,  Situ Xue ,  Guanghui Zheng ,  Yuhuan Li ,  Peizhen Tao ,  Jiandong Jiang

IPC: C07D213/30 ,  C07D213/68 ,  C07D213/55 ,  C07D213/64 ,  C07D213/65 ,  C07D213/69 ,  C07C65/28 ,  C07C69/92 ,  C07C51/09 ,  C07C65/105 ,  C07C65/19 ,  C07C43/215 ,  C07C43/23 ,  C07D213/80 ,  C07D311/58 ,  C07C275/00 ,  C07C275/54 ,  C07C279/22 ,  C07C281/02 ,  C07D333/16 ,  C07D333/24 ,  C07D233/60 ,  C07D233/90 ,  C07C217/20 ,  C07C217/22 ,  C07D241/04 ,  C07C229/08 ,  C07C235/46 ,  C07C235/62 ,  C07C235/64 ,  C07D207/16 ,  C07D211/58 ,  C07C69/157 ,  C07C69/36 ,  C07C39/21 ,  C07C51/353 ,  C07C51/36 ,  C07C41/18 ,  C07C67/30 ,  C07C231/12

CPC classification number: C07D213/30 ,  C07C39/21 ,  C07C41/18 ,  C07C43/215 ,  C07C43/23 ,  C07C51/09 ,  C07C51/353 ,  C07C51/36 ,  C07C65/105 ,  C07C65/19 ,  C07C65/28 ,  C07C67/30 ,  C07C69/157 ,  C07C69/36 ,  C07C69/92 ,  C07C217/20 ,  C07C217/22 ,  C07C229/08 ,  C07C231/12 ,  C07C235/46 ,  C07C235/62 ,  C07C235/64 ,  C07C275/00 ,  C07C275/54 ,  C07C279/22 ,  C07C281/02 ,  C07C2601/02 ,  C07C2601/14 ,  C07D207/16 ,  C07D211/58 ,  C07D213/55 ,  C07D213/64 ,  C07D213/65 ,  C07D213/68 ,  C07D213/69 ,  C07D213/80 ,  C07D233/60 ,  C07D233/90 ,  C07D241/04 ,  C07D311/58 ,  C07D333/16 ,  C07D333/24 ,  C07C65/24

Abstract: Provided are cajanine structure analogous compounds, synthesis method and pharmacological effects thereof, the compounds of the present invention having the structure as represented by general formulas I, II, III, IV and V. Also provided are pharmaceutical compositions containing the compounds as active ingredient, and uses thereof; the compounds of the present invention having the pharmacological activities such as anti-virus, anti-virus-infection, nerve protection, anti-metabolic-diseases and the like. Also provided is a chemical total synthesis preparation method of the natural products cajanine, cajanine A and cajanine C. The present invention lays a foundation for the in-depth study and development of the compounds as clinical drugs in the future.

Abstract translation: 本发明提供的是具有由通式I，II，III，IV和V表示的结构的本发明化合物的cajanine结构类似化合物，其合成方法和药理作用。还提供了含有化合物作为活性成分的药物组合物， 及其用途; 具有抗病毒，抗病毒感染，神经保护，抗代谢疾病等药理活性的本发明化合物。 还提供了天然产物cajanine，cajanine A和cajanine C的化学全合成制备方法。本发明为将来化合物作为临床药物的深入研究奠定了基础。

公开(公告)号：US09079825B2

公开(公告)日：2015-07-14

申请号：US13291948

申请日：2011-11-08

Applicant: Ian L. Scott ,  Vladimir A. Kuksa ,  Mark W. Orme ,  Thomas Little ,  Anna Gall ,  Feng Hong

Inventor： Ian L. Scott ,  Vladimir A. Kuksa ,  Mark W. Orme ,  Thomas Little ,  Anna Gall ,  Feng Hong

IPC: C09B11/02 ,  C07C211/00 ,  C07C215/20 ,  C07C217/20 ,  C07C217/60 ,  C07C217/62 ,  C07C217/64 ,  C07C217/72 ,  C07C225/16 ,  C07C229/38 ,  C07C233/18 ,  C07C235/08 ,  C07C251/86 ,  C07C279/08 ,  C07C317/28 ,  C07C323/25 ,  C07D277/24 ,  C07D309/06

CPC classification number: A61K31/137 ,  A61K31/165 ,  A61K31/222 ,  C07C215/20 ,  C07C217/20 ,  C07C217/60 ,  C07C217/62 ,  C07C217/64 ,  C07C217/72 ,  C07C217/84 ,  C07C225/16 ,  C07C229/38 ,  C07C233/18 ,  C07C235/08 ,  C07C251/86 ,  C07C279/08 ,  C07C309/06 ,  C07C317/28 ,  C07C323/25 ,  C07C323/33 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/42 ,  C07D277/24 ,  C07D309/06

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

公开(公告)号：US07423185B2

公开(公告)日：2008-09-09

申请号：US10545380

申请日：2004-01-30

Applicant: Junichi Kobayashi ,  Tetsuya Nakamura ,  Ritsu Suzuki ,  Hideyuki Muranaka ,  Tomonaga Ozawa ,  Yuichiro Kai ,  Takehiro Ishikawa ,  Tatsuhiro Kondo ,  Tetsuro Tamai ,  Satoshi Akahane

Inventor： Junichi Kobayashi ,  Tetsuya Nakamura ,  Ritsu Suzuki ,  Hideyuki Muranaka ,  Tomonaga Ozawa ,  Yuichiro Kai ,  Takehiro Ishikawa ,  Tatsuhiro Kondo ,  Tetsuro Tamai ,  Satoshi Akahane

IPC: C07C217/14 ,  C07C217/20 ,  C07D307/79 ,  A61K31/195 ,  A61P1/00 ,  A61P1/16 ,  A61P3/04

CPC classification number: C07D307/79 ,  A61K31/195 ,  C07C217/18 ,  C07C217/20 ,  C07C323/62 ,  C07C2601/04

Abstract: The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen or lower alkyl; R3, R4, R5 and R6 are each hydrogen, halogen, lower alkyl or lower alkoxy; R7 and R8 are each hydrogen, halogen, lower alkyl, halo-lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, cyano, a hydroxyl group, lower acyl, carboxy or the like; R9 is —C(O)—R10, -A1-C(O)—R10, —O-A2-C(O)—R10 or a tetrazol-5-yl group, which exhibit potent and selective β3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

Abstract translation: 本发明提供由通式（I）表示的化合物或其药学上可接受的盐，其中R 1和R 2各自为氢或低级烷基; R 3，R 4，R 5和R 6各自为氢，卤素，低级烷基或低级烷氧基 ; R 7和R 8各自为氢，卤素，低级烷基，卤代低级烷基，低级烷氧基，环烷基，芳基，杂芳基，氰基，羟基，低级酰基 ，羧基等; R 9是-C（O）-R 10，-A 1 -C（O）-R 10 O > - O 2 -C（O）-R 10或四唑-5-基，其显示出有效和选择性的β3肾上腺素受体刺激活性。 本发明还提供含有所述化合物的药物组合物及其用途。

公开(公告)号：US20050214952A1

公开(公告)日：2005-09-29

申请号：US11005558

申请日：2004-12-06

Applicant: Samuel Stupp ,  James Hulvat ,  Marina Sofos ,  Keisuke Tajima

Inventor： Samuel Stupp ,  James Hulvat ,  Marina Sofos ,  Keisuke Tajima

IPC: C07C20060101 ,  C07C45/44 ,  C07C45/71 ,  C07C47/575 ,  C07C217/20 ,  C07C217/54 ,  C07F9/40 ,  C09K19/16 ,  C09K19/58 ,  H01L21/00 ,  H01L51/00 ,  H01L51/50

CPC classification number: C07C217/20 ,  C07C45/44 ,  C07C45/71 ,  C07C47/575 ,  C07F9/4056 ,  C09K19/16 ,  C09K19/582 ,  C09K2019/168 ,  H01L51/0038 ,  H01L51/0071 ,  H01L51/0073 ,  H01L51/0076 ,  H01L51/5012

Abstract: Amphiphilic oligo(p-phenylene vinylene) compounds and methods of use en route to self-assembled composites and device fabrication.

Abstract translation: 两亲寡聚（对亚苯基亚乙烯基）化合物和使用途径，途经自组装复合材料和器件制造。