公开(公告)号：US20230227393A1

公开(公告)日：2023-07-20

申请号：US18155431

申请日：2023-01-17

申请人： Versitech Limited ,  Laboratory for Synthetic Chemistry and Chemical Biology Limited

发明人： Chi Ming Che ,  Tingting Wang ,  Haixu Wang

IPC分类号： C07C50/04 ,  C07C50/30 ,  C07C50/12 ,  C07C50/36 ,  C07C50/34 ,  B01J31/40

CPC分类号： C07C50/04 ,  C07C50/30 ,  C07C50/12 ,  C07C50/36 ,  C07C50/34 ,  B01J31/4023

摘要： Methods for asymmetric cis-dihydroxylation (“AD”) of quinones to produce cis-diols of quinones with high yield (i.e. a yield ≥30%) and high enantioselectivity (i.e. an enantiometric excess ≥30%) are disclosed. The method uses an iron-based catalyst, such as one or more Fe(II) complexes, as the catalyst, and can be performed under mild reaction conditions (e.g. a temperature ≤50° C. at 1 atom in open air). The method generally includes: (i) maintaining a reaction mixture at a temperature for a period of time sufficient to form a product, where the reaction mixture contains a quinone, one or more iron-based catalyst(s), and a solvent, and where the product contains a chiral cis-diol. Optionally, the method also includes adding an oxidant into the reaction mixture prior to and/or during step (i), such as a hydrogen peroxide solution.

公开(公告)号：US10322186B2

公开(公告)日：2019-06-18

申请号：US16235964

申请日：2018-12-28

申请人： Foamix Pharmaceuticals Ltd.

发明人： Dov Tamarkin ,  Elana Gazal ,  Irakliy Papiashvili ,  Yohan Hazot ,  David Schuz ,  Rita Keynan

IPC分类号： A61K8/18 ,  A61K35/50 ,  A61K31/65 ,  C07C50/36 ,  C07C237/26 ,  A61K47/44 ,  A61Q17/04 ,  A61K9/00 ,  A61K9/12 ,  A61K47/24 ,  A61K45/06 ,  A61K47/10 ,  A61K8/36 ,  A61K8/34 ,  A61Q19/10 ,  A61Q19/00 ,  A61K8/31 ,  A61K47/02 ,  A61K31/192 ,  A61K31/137 ,  A61K47/12 ,  A61K31/593 ,  A61K31/573 ,  A61K31/57 ,  A61K31/4164 ,  A61K47/06

摘要： A topical therapeutic hydrophobic breakable composition includes a carrier comprising (a) about 60% to about 99% by weight of at least one hydrophobic oil; (b) at least one viscosity-modifying agents selected from the group consisting of a fatty alcohol, a fatty acid and a wax; and (c) a tetracycline antibiotic, characterized in that at least part of the tetracycline antibiotic is suspended in the composition; the viscosity of the composition is at least about 30% higher than the viscosity of the carrier without the tetracycline antibiotic; and is higher than the viscosity or the hydrophobic oil and the tetracycline antibiotic without the viscosity modifying agents. The tetracycline is chemically stable in the composition for at least six months; wherein more than about 90% of the tetracycline has not broken down. The composition is packaged as a breakable foam that breaks easily upon application of shear force.

公开(公告)号：US6150414A

公开(公告)日：2000-11-21

申请号：US970229

申请日：1992-11-02

申请人： Daniel Meruelo ,  Gad Lavie ,  Yehuda Mazur

发明人： Daniel Meruelo ,  Gad Lavie ,  Yehuda Mazur

IPC分类号： A61K31/047 ,  A61K31/12 ,  A61K31/122 ,  A61K31/13 ,  A61K31/19 ,  A61K31/215 ,  A61K31/22 ,  A61K31/505 ,  A61K31/70 ,  A61P31/12 ,  A61P43/00 ,  C07C39/12 ,  C07C39/17 ,  C07C50/36 ,  C07D221/18 ,  C07D471/04 ,  C07D493/04 ,  A01N37/10 ,  A01N35/00

CPC分类号： C07C39/12 ,  A61K31/12 ,  A61K31/122 ,  A61K31/70

摘要： Disclosed herein are antiviral agents, pharmaceutical formulations comprising effective amounts of these agents and methods for treating mammals suffering from infections caused by viruses. The agents are analogs, isomers, homologs, derivatives and salts of aromatic polycyclic diones.

摘要翻译： 本文公开了抗病毒剂，包含有效量的这些药剂的药物制剂和用于治疗患有由病毒引起的感染的哺乳动物的方法。 这些试剂是芳族多环二酮的类似物，异构体，同系物，衍生物和盐。

公开(公告)号：US06093834A

公开(公告)日：2000-07-25

申请号：US237639

申请日：1999-01-26

申请人： Leonhard Feiler

发明人： Leonhard Feiler

IPC分类号： C07D221/18 ,  C07C50/36 ,  C07C51/00 ,  C07C51/06 ,  C07C51/54 ,  C07D311/78 ,  C07D311/96 ,  C09B5/62 ,  C09D11/00

CPC分类号： C09B5/62 ,  C07C51/54 ,  C07D311/78

摘要： Preparation of perylene-3,4-dicarboxylic acid anhydrides of the general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 can each be independently of one another hydrogen, halogen, C.sub.1 -C.sub.20 alkyl, C.sub.3 -C.sub.4 cycloalkyl, C.sub.1 -C.sub.20 alkoxy, phenyl, phenyloxy or phenylthio, where phenyl can in each case be mono- or polysubstituted by halogen, C.sub.1 -C.sub.20 alkyl, C.sub.3 -C.sub.14 cycloalkyl and/or C.sub.1 -C.sub.20 alkoxy; --NR.sup.5.sub.2 or --OR.sup.5, wherein R.sup.5 is hydrogen or C.sub.1 -C.sub.20 alkyl, or one of the pairs R.sup.1 /R.sup.2 and R.sup.3 /R.sup.4 each in 6,7- or 1,12-position is a bridge having the bridge atoms or bridge atom groups --O--, --S--, S.dbd.O, SO.sub.2 or --NR.sup.6, wherein R.sup.6 is hydrogen, C.sub.1 -C.sub.20 alkyl or C.sub.3 -C.sub.14 cycloalkyl, by treating a perylene-3,4-dicarboximide of formula II ##STR2## (a) in a first step with a base and, (b) in a second step, reacting the resultant anion with an alkylation agent R.sup.7 --X, X being halogen and R.sup.7 being unsubstituted or phenyl-substituted C.sub.1 -C.sub.20 alkyl, to the corresponding carboximide and,(c) in a third step, treating the alkylated carboximide first with a base and, after the treatment with a base, obtaining the perylene-3,4-dicarboxylic acid anhydride I by acidifying the reaction mixture, andnovel perylene-3,4-dicarboxylic acid anhydrides, novel N-alkylperylene-3,4-dicarboxylic acid imides and possibilities for the application of the compounds prepared according to this invention.

摘要翻译： 制备通式Ⅰ的苝-3,4-二羧酸酐其中R 1，R 2，R 3和R 4各自独立地为氢，卤素，C 1 -C 20烷基，C 3 -C 4环烷基，C 1 -C 20烷氧基，苯基，苯氧基 或苯硫基，其中每种情况下苯基可被卤素，C 1 -C 20烷基，C 3 -C 14环烷基和/或C 1 -C 20烷氧基单取代或多取代; -NR 52或-OR 5，其中R 5是氢或C 1 -C 20烷基，或者每个6,7或1,12位中的一对R 1 / R 2和R 3 / R 4是具有桥原子或桥原子基团的桥 -O-，-S-，S = O，SO 2或-NR 6，其中R 6是氢，C 1 -C 20烷基或C 3 -C 14环烷基，通过在第一步中处理式II（a）的苝-3,4-二甲酰亚胺 与碱反应，（b）在第二步中，使所得阴离子与烷基化试剂R7-X，X为卤素，R7为未取代的或苯基取代的C1-C20烷基反应至相应的甲酰亚胺，和（c） 第三步，首先用碱处理烷基化的酰亚胺化物，在用碱处理后，通过酸化反应混合物得到苝-3,4-二羧酸酐I，并加入新的苝-3,4-二羧酸酐 ，新型N-烷基亚丙基-3,4-二羧酸酰亚胺以及应用根据本发明制备的化合物的可能性。

公开(公告)号：US5824654A

公开(公告)日：1998-10-20

申请号：US300725

申请日：1994-09-02

申请人： Gad Lavie ,  Alfred M. Prince

发明人： Gad Lavie ,  Alfred M. Prince

IPC分类号： C07C50/36 ,  C07C50/38 ,  C07C69/00 ,  A61K48/00 ,  C09B3/40 ,  C12N5/00

CPC分类号： C07C69/00 ,  C07C50/36 ,  C07C50/38 ,  C07C2103/00

摘要： The invention provides improved methods for delivery of nucleic acids to cells, which comprise forming ternary complexes between a hydrophobic, membrane-binding anion such as hypericin; a polycation such as polylysine; and a nucleic acid such as DNA; and contacting cells with the tenary complexes. Also provided are pharmaceutical formulations comprising these ternary complexes and a pharmaceutically acceptable carrier or diluent. The methods and compositions find use in mediating DNA uptake into cells, including gene therapy applications.

摘要翻译： 本发明提供了将核酸递送至细胞的改进方法，其包括在疏水性的膜结合阴离子例如金丝桃素之间形成三元复合物; 聚阳离子如聚赖氨酸; 和核酸如DNA; 并使细胞与助剂络合物接触。 还提供了包含这些三元配合物和药学上可接受的载体或稀释剂的药物制剂。 该方法和组合物可用于介导DNA吸收进入细胞，包括基因治疗应用。

公开(公告)号：US5488119A

公开(公告)日：1996-01-30

申请号：US135775

申请日：1993-10-12

申请人： Evelyn Fischer-Reimann ,  Walter Fischer

发明人： Evelyn Fischer-Reimann ,  Walter Fischer

IPC分类号： C07C46/00 ,  C07C50/36 ,  C07C69/00 ,  C07C69/94 ,  C07C255/56 ,  C07C317/24 ,  C08F20/10 ,  C08F20/30 ,  C08F220/30 ,  C08F246/00 ,  C09K9/00 ,  C09K9/02 ,  G03C1/73 ,  C07C50/22 ,  C07C49/617

CPC分类号： C07C69/00 ,  C08F20/30 ,  C08F220/30 ,  C08F246/00 ,  C09K9/02 ,  G03C1/73 ,  G03C1/733 ,  C07C2103/00

摘要： Compounds of formulae I and II ##STR1## wherein D is H or --OR wherein R is phenyl and R.sub.1 to R.sub.4 are H or a substituent such as phenylthio, and one of the substituents R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is a group of formula III--E-CR.sub.5 =C(R.sub.6).sub.2 (III)or R is substituted by a group of formula III, wherein E is a direct bond or --X-C(O)-- wherein X is a linking group, and R.sub.5 and R.sub.6 are each independently of the other H, halogen, C.sub.1 -C.sub.12 alkyl or C.sub.6 -C.sub.10 aryl, can be polymerised to homopolymers or copolymers. The monomers and polymers are reversible photochromic systems which can be used as color indicators, as photochemically modifiable color filters, or for the optical storage of information.

摘要翻译： 式I和II的化合物其中D为H或-OR，其中R为苯基且R 1至R 4为H或取代基如苯硫基，并且一个取代基R 1，R 2 ，R 3和R 4是式III-E-CR 5 = C（R 6）2（III）的基团或R被式III的基团取代，其中E是直接键或-XC（O） - ，其中X是 连接基团和R 5和R 6各自独立地为H，卤素，C 1 -C 12烷基或C 6 -C 10芳基，可以聚合成均聚物或共聚物。 单体和聚合物是可逆的光致变色系统，其可以用作颜色指示剂，作为光化学改性的滤色器，或用于信息的光学存储。

公开(公告)号：US5180758A

公开(公告)日：1993-01-19

申请号：US743373

申请日：1991-08-26

申请人： Walter Cabri ,  Ilaria Candiani ,  Silvia De Bernardinis ,  Franco Francalanci

发明人： Walter Cabri ,  Ilaria Candiani ,  Silvia De Bernardinis ,  Franco Francalanci

IPC分类号： B01J27/128 ,  B01J31/12 ,  C07B61/00 ,  C07C46/00 ,  C07C49/423 ,  C07C49/727 ,  C07C50/36 ,  C07C50/38

CPC分类号： C07C46/00 ,  Y02P20/55

摘要： 4-substituted anthracyclinones of general formula (I): ##STR1## wherein R represents a hydrogen atom or a COOR.sub.1 group in which R.sub.1 may be a hydrogen atom or an optionally substituted C.sub.1 -C.sub.10 alkyl group, which are intermediates in the preparation of antitumor anthracycline glycosides, are prepared by:(i)(a) reacting a 4-demethyl-4-sulfonyl-7-deoxy-13-dioxolanyl daunomycinone of formula (V): ##STR2## wherein R' represents an alkyl group having from 1 to 10 carbon atoms optionally substituted by one or more halogen atoms or an aryl group optionally substituted by halogen, alkyl, alkoxy or nitro, in a reducing environment with a catalytic amount of a compound of formula (VIII):ML.sub.n L'.sub.m wherein M represents a transition metal atom, L and L', which may be the same or different, each represent an anion or a neutral molecule and n and m may vary from 0 to 4, such as to obtain a compound of formula (VII): ##STR3## wherein R represents hydrogen; or (b) carbonylating a 4-demethyl-4-sulfonyl-7-deoxy-13-dioxolanyl daunomycinone of formula (V) as defined above, with carbon monoxide in the presence of a nucleophile R.sub.1 OH wherein R.sub.1 is as defined above, an organic or inorganic base and as catalyst a compound of formula (VIII) as defined above, such as to obtain a compound of formula (VII) as shown above wherein R represents a COOR.sub.1 group; and(ii) introducing an .alpha.-hydroxy group at the 7-position and removing the 13-oxo protecting group by acid hydrolysis from the resultant compound of formula (VII).

公开(公告)号：US5097051A

公开(公告)日：1992-03-17

申请号：US473538

申请日：1990-02-01

申请人： Johan W. Scheeren ,  Joannes F. M. DeBie ,  Dirk DeVos

发明人： Johan W. Scheeren ,  Joannes F. M. DeBie ,  Dirk DeVos

IPC分类号： C07C45/45 ,  C07C49/753 ,  C07C49/757 ,  C07C50/34 ,  C07C50/36 ,  C07C217/12 ,  C07C323/12 ,  C07F7/18

CPC分类号： C07F7/1852

摘要： The invention provides novel cyclic triketone compounds of the formulae ##STR1## wherein S is H, alkyl or alkoxy and R* is a group of the formule ##STR2## wherein R.sup.1 is methyl and R.sub.2 is an alkyl group containing at least 2 carbon atoms or R.sup.1 is an alkyl group having 1-4 carbon atoms and R.sup.2 is an aryl group, a hetero aryl group, a --CH.sub.2 OR' group, a --CH.sub.2 N

公开(公告)号：US5037970A

公开(公告)日：1991-08-06

申请号：US501869

申请日：1990-03-28

申请人： Francesco Angelucci ,  Sergio Penco ,  Ermes Vanotti ,  Federico Arcamone

发明人： Francesco Angelucci ,  Sergio Penco ,  Ermes Vanotti ,  Federico Arcamone

IPC分类号： C07C50/38 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07C45/00 ,  C07C46/00 ,  C07C50/36 ,  C07C67/00 ,  C07D407/04 ,  C07H15/252

CPC分类号： C07D407/04 ,  C07H15/252

摘要： A compound of the formula ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxy group, one of R.sub.2 and R.sub.3 represents a hydrogen atom, the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxy group and X is a hydrogen atom or a trifluoro acetyl group. The N-trifluoroacetyl 7S:9S and 7R:9R derivatives of the .alpha.-glycosides of formula XV can be separated by chromatography on silica gel to obtain, after mild alkaline hydrolysis the wanted 7S:9S .alpha.-glycosides (R.sub.1 =H) as free bases and can eventually be transformed into their corresponding doxorubicin derivatives (R.sub.1 =OH) by known procedures.

公开(公告)号：US4710320A

公开(公告)日：1987-12-01

申请号：US753860

申请日：1985-07-11

申请人： Makoto Hattori ,  Masao Nishikuri ,  Yasuyoshi Ueda

发明人： Makoto Hattori ,  Masao Nishikuri ,  Yasuyoshi Ueda

IPC分类号： C07C46/00 ,  C07C45/00 ,  C07C50/34 ,  C07C50/36 ,  C07C67/00 ,  C09B1/503 ,  C09B1/54 ,  C07C97/26

CPC分类号： C09B1/547 ,  C09B1/503

摘要： 1-Amino-2-phenoxy-4-hydroxyanthraquinones, which are useful as a red disperse dye for polyester fibers, and also useful as an intermediate for the production of other red disperse dyes, are produced in a high yield and purity by reacting a 1-amino-2-halogeno-4-hydroxyanthraquinone with a phenol compound in a sulfane solvent in the presence of an acid binding agent.

摘要翻译： 可用作聚酯纤维的红色分散染料，也可用作生产其它红色分散染料的中间体的1-氨基-2-苯氧基-4-羟基蒽醌以高产率和纯度通过使 1-氨基-2-卤代-4-羟基蒽醌与酚化合物在硫酸溶剂中在酸结合剂存在下反应。