公开(公告)号：US12102628B2

公开(公告)日：2024-10-01

申请号：US17706225

申请日：2022-03-28

申请人： Seinda Pharmaceutical Guangzhou Corporation

发明人： Hui Ouyang ,  Yong Qiu

IPC分类号： A61P27/02 ,  A61K9/00 ,  A61K31/06 ,  A61K31/216 ,  A61K31/222 ,  A61K31/24 ,  A61K31/4168 ,  A61K31/417 ,  A61K31/439 ,  A61K31/4406 ,  A61K31/46 ,  A61K31/498 ,  A61K31/551 ,  A61K31/5513 ,  A61P27/10 ,  C07C217/20 ,  C07C219/10 ,  C07D213/04 ,  C07D235/02 ,  C07D403/04 ,  C07D403/12 ,  C07D471/08 ,  C07D487/04 ,  C07D491/18

CPC分类号： A61K31/46 ,  A61K9/0048 ,  A61K31/24 ,  A61K31/4168 ,  A61K31/417 ,  A61K31/498 ,  A61K31/551 ,  A61P27/10

摘要： Compositions and methods useful in slowing, inhibiting, or regressing the progression of myopia, while minimizing pupil dilation and light sensitivity are provided herein. Provided compositions can include a muscarinic receptor antagonist and a miotic agent.

公开(公告)号：US11786497B2

公开(公告)日：2023-10-17

申请号：US16299560

申请日：2019-03-12

申请人： Techfields Pharma Co., Ltd.

发明人： Chongxi Yu

IPC分类号： A61K31/215 ,  A61K47/54 ,  A61K31/21 ,  A61K31/216 ,  A61K31/4453 ,  C07C219/10 ,  G01N33/50 ,  A61K31/221

CPC分类号： A61K31/215 ,  A61K31/21 ,  A61K31/216 ,  A61K31/221 ,  A61K31/4453 ,  A61K47/54 ,  C07C219/10 ,  G01N33/502 ,  C07C2601/16 ,  C07C2602/10

摘要： The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of retinoids and retinoid-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

公开(公告)号：US11634379B2

公开(公告)日：2023-04-25

申请号：US16906985

申请日：2020-06-19

申请人： Acuitas Therapeutics, Inc.

发明人： Steven M. Ansell ,  Xinyao Du

IPC分类号： C07C229/24 ,  A61K9/127 ,  C07C219/10 ,  A61K47/18 ,  A61K47/22 ,  C07C219/06 ,  C07C219/08 ,  C07C229/16 ,  C07D295/13 ,  C08G65/333 ,  A61K38/48 ,  A61K47/24 ,  A61K47/28 ,  A61K48/00 ,  C07C235/06 ,  C07C227/16

摘要： Compounds are provided having the following structure: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6, R7, R8, R9, L1, L2, a, b, c, d and e are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.

公开(公告)号：US09738593B2

公开(公告)日：2017-08-22

申请号：US14732218

申请日：2015-06-05

申请人： Acuitas Therapeutics Inc.

发明人： Steven M. Ansell ,  Xinyao Du

IPC分类号： C07C219/06 ,  A61K47/18 ,  A61K47/22 ,  C07C219/08 ,  C07C229/16 ,  C07D295/13 ,  C08G65/333 ,  A61K9/127 ,  C07C219/10

CPC分类号： C07C229/24 ,  A61K9/1272 ,  A61K38/4846 ,  A61K47/18 ,  A61K47/22 ,  A61K47/24 ,  A61K47/28 ,  A61K48/0041 ,  C07C219/06 ,  C07C219/08 ,  C07C219/10 ,  C07C227/16 ,  C07C229/16 ,  C07C235/06 ,  C07D295/13 ,  C08G65/33306 ,  C12Y304/21022

摘要： Compounds are provided having the following structure: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6, R7, R8, R9, L1, L2, a, b, c, d and e are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.

公开(公告)号：US6107410A

公开(公告)日：2000-08-22

申请号：US217902

申请日：1998-12-22

申请人： Michinori Waki ,  Kenji Miyamoto ,  Yoshihiro Motani

发明人： Michinori Waki ,  Kenji Miyamoto ,  Yoshihiro Motani

IPC分类号： C07C217/08 ,  C07C219/10 ,  C07C229/22 ,  C07C233/51 ,  C07C237/08 ,  C07C237/12 ,  C07K5/06 ,  C07K5/083 ,  C08B37/00 ,  C08B37/08 ,  C08L5/08 ,  C08F8/32

CPC分类号： C07C217/08 ,  C07C219/10 ,  C07C229/22 ,  C07C233/51 ,  C07C237/08 ,  C07C237/12 ,  C07K5/06026 ,  C07K5/0806 ,  C08B37/003 ,  C08B37/0063 ,  C08L5/08

摘要： The invention provides a cinnamic acid derivative having a novel spacer introduced into cinnamic acid which is photodimerizable, a cinnamic acid-polysaccharide derivative photocurable with high sensitivity and efficiency obtainable by introducing the above cinnamic acid derivative into a host polysaccharide such as a glycosaminoglycan, and a photocrosslinked cinnamic acid-polysaccharide derivative obtainable by exposing the same cinnamic acid-polysaccharide derivative to ultraviolet light irradiation.

公开(公告)号：US6025444A

公开(公告)日：2000-02-15

申请号：US863933

申请日：1997-05-27

申请人： Michinori Waki ,  Kenji Miyamoto ,  Yoshihiro Motani

发明人： Michinori Waki ,  Kenji Miyamoto ,  Yoshihiro Motani

IPC分类号： C07C217/08 ,  C07C219/10 ,  C07C229/22 ,  C07C233/51 ,  C07C237/08 ,  C07C237/12 ,  C07K5/06 ,  C07K5/083 ,  C08B37/00 ,  C08B37/08 ,  C08L5/08 ,  C08F8/32

CPC分类号： C07C217/08 ,  C07C219/10 ,  C07C229/22 ,  C07C233/51 ,  C07C237/08 ,  C07C237/12 ,  C07K5/06026 ,  C07K5/0806 ,  C08B37/003 ,  C08B37/0063 ,  C08L5/08

摘要： The invention provides a cinnamic acid derivative having a novel spacer introduced into cinnamic acid which is photodimerizable, a cinnamic acid-polysaccharide derivative photocurable with high sensitivity and efficiency obtainable by introducing the above cinnamic acid derivative into a host polysaccharide such as a glycosaminoglycan, and a photocrosslinked cinnamic acid-polysaccharide derivative obtainable by exposing the same cinnamic acid-polysaccharide derivative to ultraviolet light irradiation.

摘要翻译： 本发明提供了一种肉桂酸衍生物，其具有引入肉桂酸中的新型间隔基，其可被光可定向化，肉桂酸 - 多糖衍生物可以通过将上述肉桂酸衍生物引入宿主多糖如糖胺聚糖中而获得，其具有高灵敏度和高效率可光固化， 通过将相同的肉桂酸 - 多糖衍生物暴露于紫外线照射而获得的光交联肉桂酸 - 多糖衍生物。

公开(公告)号：US5629422A

公开(公告)日：1997-05-13

申请号：US343393

申请日：1994-11-22

申请人： Hugo Camenzind

发明人： Hugo Camenzind

IPC分类号： C07D215/06 ,  C07C217/08 ,  C07C219/10 ,  C07D279/22 ,  C08K5/10 ,  C08K5/105 ,  C08K5/17 ,  C08L101/00 ,  C10M133/08 ,  C10M133/14 ,  C10M133/40 ,  C10M135/36 ,  C10N30/10 ,  C10N40/25 ,  C07C69/76 ,  C07D221/02

CPC分类号： C07C217/08 ,  C07C219/10 ,  C07D279/22 ,  C08K5/17 ,  C10M133/14 ,  C10M133/40 ,  C10M135/36 ,  C10M2201/02 ,  C10M2215/064 ,  C10M2215/065 ,  C10M2215/22 ,  C10M2215/221 ,  C10M2215/225 ,  C10M2215/226 ,  C10M2215/30 ,  C10M2219/108 ,  C10N2240/08 ,  C10N2240/401 ,  C10N2240/402 ,  C10N2240/403 ,  C10N2240/404 ,  C10N2240/405 ,  C10N2240/406 ,  C10N2240/407 ,  C10N2240/408 ,  C10N2240/409

摘要： New compounds of the formula I are described which are active, for example, as antioxidants, and also a process for their preparation: ##STR1## R.sub.1 and R.sub.2 are independently of one another C.sub.1 -C.sub.20 alkyl, allyl, methallyl, unsubstituted or C.sub.1 -C.sub.8 alkyl-substituted C.sub.5 -C.sub.12 cycloalkyl, C.sub.5 -C.sub.8 cycloalkenyl, phenyl or C.sub.7 -C.sub.9 phenylalkyl, A is a direct bond, --CH.sub.2 --, --(CH.sub.2).sub.2 -- or --CH.sub.2 --CH(CH.sub.3)--, E is --(CH.sub.2).sub.2 --, --CHR.sub.6 --CH.sub.2 -- or --CH.sub.2 CHR.sub.6 --, n is 1, 2 or 3, R.sub.3 is C.sub.1 -C.sub.18 alkyl or is C.sub.1 -C.sub.18 alkyl which is interrupted by --O-- or --S--, unsubstituted or C.sub.1 -C.sub.8 alkyl-substituted C.sub.5 -C.sub.12 cycloalkyl, phenyl, naphthyl, C.sub.7 -C.sub.9 phenylalkyl, C.sub.7 -C.sub.18 alkylphenyl or is of the formula ##STR2## R.sub.4 is phenyl, naphthyl, C.sub.7 -C.sub.9 phenylalkyl, C.sub.7 -C.sub.18 alkylphenyl or is a radical of the formula ##STR3## or NR.sub.3 R.sub.4 is a group of the formula ##STR4## R.sub.5 is hydrogen, C.sub.1 -C.sub.18 alkyl, allyl, methallyl, unsubstituted or C.sub.1 -C.sub.8 alkyl-substituted C.sub.5 -C.sub.12 cycloalkyl, phenyl or naphthyl, R.sub.6 is hydrogen, C.sub.1 -C.sub.20 alkyl or C.sub.2 -C.sub.20 alkyl which is interrupted by --O--, --S--, --NR.sub.7 -- or --C(O)O--, and R.sub.7 is hydrogen or C.sub.1 -C.sub.6 alkyl.

摘要翻译： 描述了具有活性的新的式I化合物，例如作为抗氧化剂，以及它们的制备方法：（I）R 1和R 2彼此独立地为C 1 -C 20烷基，烯丙基，甲代烯丙基，未取代的或未取代的 C 1 -C 8烷基取代的C 5 -C 12环烷基，C 5 -C 8环烯基，苯基或C 7 -C 9苯基烷基，A是直接键，-CH 2 - ， - （CH 2）2 - 或-CH 2 -CH（CH 3） - ，E是 - （CH 2 ）2-，-CHR 6 -CH 2 - 或-CH 2 CHR 6 - ，n为1,2或3，R 3为C 1 -C 18烷基或被-O-或-S-间隔的C 1 -C 18烷基，未取代或C 1 -C 8烷基 - 取代的C 5 -C 12环烷基，苯基，萘基，C 7 -C 9苯基烷基，C 7 -C 18烷基苯基或具有下式的化合物：R 4是苯基，萘基，C 7 -C 9苯基烷基，C 7 -C 18烷基苯基，或者是下式的基团：IMAGE> C 1 -C 18烷基，烯丙基，甲代烯丙基，未取代的或C 1 -C 8烷基取代的C 5 -C 12环烷基，苯基或萘基，R 6是氢，C 1 -C 20烷基或C 2 -C 20烷基，其被-O - ， - S-， NR7-或-C（O）O-，R7是氢或C1- C6烷基。

公开(公告)号：US4633007A

公开(公告)日：1986-12-30

申请号：US832503

申请日：1986-02-21

申请人： Michael Preiss

发明人： Michael Preiss

IPC分类号： C07C69/738 ,  B01J31/00 ,  C07B61/00 ,  C07C67/00 ,  C07C201/00 ,  C07C205/56 ,  C07C213/00 ,  C07C219/10 ,  C07C253/00 ,  C07C255/57 ,  C07C301/00 ,  C07C303/22 ,  C07C309/58 ,  C07C143/525 ,  C07C79/38 ,  C07C121/76

CPC分类号： C07C201/12

摘要： A process for the preparation of a benzylidene compound of the formula ##STR1## in which R.sup.1 is hydrogen or one or two substituents independently selected from the group consisting of nitro, cyano, halogen, SO.sub.3 H, alkyl, alkoxy and fluorinated alkyl, each with 1 to 4 C atoms and two or three fluorine substituents, andR.sup.3 is alkyl with 1 to 10 C atoms, which is optionally interrupted by an oxygen in the chain or is optionally substituted by fluorine, chlorine, hydroxyl or a methylbenzylamine group, comprising reacting an acetal of the formula ##STR2## in which R.sup.2 each independently is alkyl with 1 to 6 C atoms, which is optionally substituted by phenyl, or the two radicals R.sup.2 conjointly form an alkylene radical with 1-6 C atoms,with a .beta.-ketocarboxylic acid ester of the formulaCH.sub.3 CO--CH.sub.2 --COOR.sup.3in the presence of an acid at a temperature between about 40.degree. and 120.degree..

摘要翻译： 制备式“IMAGE”的亚苄基化合物的方法，其中R 1是氢或一个或两个独立地选自硝基，氰基，卤素，SO 3 H，烷基，烷氧基和氟化烷基的取代基，各自具有1 至4个C原子和两个或三个氟取代基，R3是具有1至10个C原子的烷基，其任选被链中的氧中断或任选被氟，氯，羟基或甲基苄胺基取代，包括使 其中R 2各自独立地为具有1至6个C原子的烷基，其任选被苯基取代，或两个基团R 2与1-6个C原子一起形成亚烷基，与β-酮羧酸 在酸存在下，在约40至120℃的温度下，式CH 3 CO-CH 2 -COOR 3的酸酯。

公开(公告)号：US4381313A

公开(公告)日：1983-04-26

申请号：US268221

申请日：1981-05-29

申请人： Jean Heusser ,  Max Glasbrenner

发明人： Jean Heusser ,  Max Glasbrenner

IPC分类号： C07C69/614 ,  A61K31/19 ,  A61K31/21 ,  A61K31/215 ,  A61P29/00 ,  C07C17/32 ,  C07C51/00 ,  C07C57/30 ,  C07C59/64 ,  C07C67/00 ,  C07C69/734 ,  C07C213/00 ,  C07C219/10 ,  C07D295/088 ,  C07C101/00

CPC分类号： C07D295/088 ,  C07C17/32 ,  C07C57/30 ,  C07C59/64 ,  Y10S514/887 ,  Y10S514/916

摘要： Novel phenylalkanoic compounds of the formula I ##STR1## wherein R.sub.1 and R.sub.2 independently from each other represent hydrogen or alkyl with 1 to 8 carbon atoms, salts of such compounds and salts thereof, therapeutic uses of the phenylalkanoic compounds, or of the pharmacologically safe salts thereof for treating inflammatory diseases, tussive states, pain symptoms and pyretic diseases and pharmaceutical composition containing the phenylalkanoic compounds or the pharmacologically safe salts together with a carrier and an optional adjuvant or additive.

摘要翻译： 式I的新型苯基链烷酸化合物其中R 1和R 2彼此独立地表示氢或具有1至8个碳原子的烷基，这些化合物及其盐的盐，苯基链烷酸化合物的治疗用途或 用于治疗炎性疾病，咳嗽状态，疼痛症状和热解病的药物安全的盐以及含有苯基链烷酸化合物或药理学上安全的盐以及载体和任选的佐剂或添加剂的药物组合物。

公开(公告)号：US10723692B2

公开(公告)日：2020-07-28

申请号：US16132287

申请日：2018-09-14

申请人： Acuitas Therapeutics, Inc.

发明人： Steven M. Ansell ,  Xinyao Du

IPC分类号： C07C229/24 ,  A61K9/127 ,  C07C219/10 ,  A61K47/18 ,  A61K47/22 ,  C07C219/06 ,  C07C219/08 ,  C07C229/16 ,  C07D295/13 ,  C08G65/333 ,  A61K38/48 ,  A61K47/24 ,  A61K47/28 ,  A61K48/00 ,  C07C235/06 ,  C07C227/16

摘要： Compounds are provided having the following structure: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6, R7, R8, R9, L1, L2, a, b, c, d and e are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.