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02-02-2012 дата публикации

Novel lipids and compositions for the delivery of therapeutics

Номер: US20120027796A1

Автор: David Butler, Jayaprakash K. Narayanannair, Kallanthottathil G. Rajeev, Laxmab Eltepu, Muthiah Manoharan, Muthusamy Jayaraman

Принадлежит: Alnylam Pharmaceuticals Inc

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: (Formula (I) or (XXXV)).

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Номер записи: 1

19-04-2012 дата публикации

Novel lipids and compositions for the delivery of therapeutics

Номер: US20120095075A1

Автор: David Butler, Kallanthottathil G. Rajeev, Laxman Eltepu, Muthiah Manoharan, Muthusamy Jayaraman, Narayanannair K. Jayaprakash

Принадлежит: Alnylam Pharmaceuticals Inc

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure:

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Номер записи: 2

05-07-2012 дата публикации

Compositions, Synthesis, and Methods of Using Cycloalkylmethylamine Derivatives

Номер: US20120172426A1

Автор: Kouacou Adiey, Laxminarayan Bhat

Принадлежит: Reviva Pharmaceuticals Inc

The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.

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Номер записи: 3

21-03-2013 дата публикации

QUATERNARY DIALKANOLAMINE ESTERS

Номер: US20130071343A1

Автор: Gruening Burghard, Herrwerth Sascha, Koehle Hans-Juergen, Ulrich-Brehm Isabella

Принадлежит: EVONIK GOLDSCHMIDT GMBH

The invention relates to novel quaternary ammonium compounds of the esterquat type, to a method for the production thereof, and to the use thereof in formulations. 2. The quaternary dialkanolamine ester as claimed in claim 1 , wherein{'sub': 5', '11', '7', '15', '9', '19', '11', '23', '13', '27, 'acyl radicals from group (a) are selected from CHCO—, CHCO—, CHCO—, CHCO— and CHCO—,'} {'sub': 19', '39', '21', '43', '23', '47, 'CHCO—, CHCO— and CHCO— and'}, 'acyl radicals from group (b) are selected from'}acyl radicals from group (c) are selected from acyl radicals of the carboxylic acids which are additionally present in technical mixtures of the carboxylic acids which determine the acyl radical from groups (a) and (b).3. The quaternary dialkanolamine ester as claimed in claim 1 , wherein{'sub': 11', '23, 'acyl radicals from group (a) are selected from CHCO—,'} {'sub': 19', '39', '21', '43', '23', '47, 'CHCO—, CHCO—, CHCO— in a weight ratio of 4-8:85-99:0-3.'}, 'acyl radicals from group (b) are selected from'}4. The quaternary dialkanolamine ester as claimed in claim 1 , wherein the acyl radicals from groups (a) to (c) are determined via the acyl radicals of a mixture consisting oftechnical lauric acid andtechnical behenic acid.5. The quaternary dialkanolamine ester as claimed in claim 1 , wherein the numerical average of the molar ratio of the acyl radicals from group (a) to acyl radicals from group (b) is 1:0.5 to 4.6. A process for preparing quaternary dialkanolamine esters claim 1 , comprising the process steps of{'sub': 2', '2', '4', '3', '6', '4', '8, 'claim-text': (d) carboxylic acid containing 6 to 14 carbon atoms', '(e) carboxylic acid containing 20 to 24 carbon atoms and optionally', '(f) carboxylic acid which contains 3 to 28 carbon atoms and is not included in groups (d) and (e),, 'A) reacting an alkyldialkanolamine in which the two alkanol groups are selected from the group consisting of —CHOH, —CHOH, —CHOH and —CHOH and the alkyl group is selected from ...

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Номер записи: 4

28-03-2013 дата публикации

QUATERNARY DIALKANOLAMINE ESTERS

Номер: US20130078208A1

Автор: Gruening Burghard, Herrwerth Sascha, Koehle Hans-Juergen, Ulrich-Brehm Isabella

Принадлежит: EVONIK GOLDSCHMIDT GMBH

The invention relates to novel quaternary ammonium compounds of the esterquat type, to a method for the production thereof, and to the use thereof in formulations. 2. The quaternary dialkanolamine ester as claimed in claim 1 , wherein{'sub': 5', '11', '7', '15', '9', '19', '11', '23', '13', '27, 'acyl radicals from group (a) are selected from CHCO—, CHCO—, CHCO—, CHCO— and CHCO—,'}{'sub': 15', '29', '17', '33', '17', '31', '17', '29', '19', '37', '19', '31', '19', '29, 'acyl radicals from group (b) are selected from CHCO—, CHCO—, CHCO—, CHCO—, CHCO—, CHCO— and CHCO—,'}{'sub': 19', '39', '21', '43', '23', '47, 'acyl radicals from group (c) are selected from CHCO—, CHCO— and CHCO— and'}acyl radicals from group (d) are selected from acyl radicals of the carboxylic acids which are additionally present in technical mixtures of the carboxylic acids which determine the acyl radical from groups (a), (b) and (c).3. The quaternary dialkanolamine ester as claimed in claim 1 , wherein{'sub': 11', '23, 'acyl radicals from group (a) are selected from CHCO—,'}{'sub': 15', '29', '17', '33', '17', '31', '17', '29', '19', '37, 'acyl radicals from group (b) are selected from CHCO—, CHCO, CHCO—, CHCO— and CHCO— in a weight ratio of 3-7:68-76:5-13:1-3:0-2,'}{'sub': 19', '39', '21', '43', '23', '47, 'acyl radicals from group (c) are selected from CHCO—, CHCO—, CHCO— in a weight ratio of 4-8:85-99:0-3.'}4. A quaternary dialkanolamine ester as claimed in claim 1 , wherein the acyl radicals from groups (a) to (d) are determined via the acyl radicals of a mixture consisting oftechnical lauric acid,technical oleic acid andtechnical behenic acid.5. A quaternary dialkanolamine ester as claimed in claim 1 , wherein the numerical average of the molar ratio of the sum of acyl radicals from group (a) and group (b) to acyl radicals from group (c) is 1:0.67 to 4.6. A process for preparing quaternary dialkanolamine esters claim 1 , comprising the process steps of{'sub': 2', '2', '4', '3', '6', '4', '8 ...

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Номер записи: 5

23-05-2013 дата публикации

"green" diester amines and personal care products

Номер: US20130129656A1

Автор: Abel G. Pereira, Duane St. Amour, Erik Gunderman, Farahdia Edouard

Принадлежит: Croda Inc

Diester tertiary amines and quats and their methods of synthesis are disclosed. Also disclosed are personal care compositions comprising the disclosed compounds.

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Номер записи: 6

23-05-2013 дата публикации

METHODS AND COMPOSITIONS FOR DELIVERY OF ACTIVE AGENTS

Номер: US20130129785A1

Автор: Manoharan Muthiah, Rajeev Kallanthottathil G.

Принадлежит: ALNYLAM PHARMACEUTICALS, INC

A lipid particle can include a cationic lipid. Synthesis of the cationic lipid can include a ylide-based reaction, such as a Wittig reaction or sulfur ylide reaction. In some cases, the synthesis can also include a Michael addition or a related addition reaction. 2. The compound of claim 1 , wherein X are Y are alkyl.3. The compound of claim 3 , wherein X and Y are both methyl.4. The compound of claim 1 , wherein Lis a linear alkylene unit.5. The compound of claim 1 , wherein Lis a linear alkylene unit.6. The compound of claim 5 , wherein Lcontains one or more double bonds and one or more cycloalkylene groups.7. The compound of claim 1 , wherein Rand Rare each claim 1 , independently claim 1 , C-Calkyl or C-Calkenyl.8. The compound of claim 7 , wherein one of Rand Ris a linear C-Calkyl or C-Calkenyl group and the other of Rand Ris a branched C-Calkyl or C-Calkenyl group.9. The compound of claim 1 , wherein Z is —C(O)O— claim 1 , —C(O)N(R)— claim 1 , —O(CO)N(R) claim 1 , —C(O)N(R)C(O)O— claim 1 , or —N(R)C(O)N(R)—.10. The compound of claim 1 , wherein Ris H or alkyl.11. The compound of claim 1 , wherein{'sub': 1', '4, 'X and Y are each, independently, C-Calkyl;'}{'sup': 1', '2, 'sub': 2', '10, 'Land Lare each, independently, an C-Clinear or branched alkylene linking unit, which may optionally contain one or more double bonds and further may optionally be interrupted by one or more heteroatoms and/or one or more cycloalkylene groups;'}{'sub': 1', '2', '10', '30, 'Rand Rare each, independently, a C-Caliphatic group, which may optionally contain one or more double bonds, and may optionally be interrupted by one or more heteroatoms and/or one or more cycloalkylene groups;'}{'sup': 3', '3', '3', '3', '3', '3', '3', '3, 'Z is —C(O)O—, —OC(O)—, —C(O)N(R)—, —N(R)C(O)—, —O(CO)N(R), —N(R)C(O)O—, —C(O)N(R)C(O)O—, —OC(O)N(R)C(O)— or —N(R)C(O)N(R)—;'}{'sup': '3', 'sub': 1', '4, 'each occurrence of Ris independently H or C-Calkyl; and'}{'img': [{'@id': 'CUSTOM-CHARACTER-00003', '@ ...

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Номер записи: 7

29-08-2013 дата публикации

TRANS-2-DECENOIC ACID DERIVATIVE AND PHARMACEUTICAL AGENT CONTAINING THE SAME

Номер: US20130225837A1

Автор: Furukawa Shoei, Iinuma Munekazu, Matsumoto Tomonori, Naiki Mitsuru, SUGIMOTO Hachiro

Принадлежит:

An object of the present invention is to provide a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof and to provide a pharmaceutical agent which contains said compound as an active ingredient and has a highly safe neurotrophic factor-like activity or an alleviating action for side effect induced by administration of anti-cancer agents. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof which is the compound of the present invention is specifically represented by the formula (1): 2. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein Y′ is —O— and W1′ is dialkylaminoalkyl group claim 1 , alkylthioalkyl group claim 1 , alkoxyalkyl group claim 1 , dialkoxyalkyl group or dialkylaminoalkoxyalkyl group.3. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein Y′ is —NR′—.4. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof according to claim 3 , wherein R′ is dialkylaminoalkyl group and W2′ is hydrogen atom claim 3 , alkyl group or dialkylaminoalkyl group.5. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof according to claim 3 , wherein R′ is alkyl group and W2′ is alkyl group which is same as or different from R′ (except the case where both R′ and W2′ are ethyl group).6. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof according to claim 3 , wherein R′ is hydrogen atom and W2′ is alkyl group (except 2-methylpropyl group and 2-methylbutyl group) claim 3 , cyclohexyl group or pyrrolidinealkyl group.7. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein Y′ is —S— and W3′ is alkyl group claim 1 , cycloalkyl group claim 1 , phenylalkyl group or dialkylaminoalkyl group.9. The pharmaceutical agent according to claim 8 , wherein Y is ...

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Номер записи: 8

29-08-2013 дата публикации

ESTERAMINES AND DERIVATIVES FROM NATURAL OIL METATHESIS

Номер: US20130225859A1

Автор: ALLEN Dave R., Bernhardt Randal J., Brown Aaron, Damashek Anatoliy A., Holland Brian, Malec Andrew D., Masters Ronald A., Nepras Marshall J., Skelton Patti, Whitlock Laura Lee, Wolfe Patrick Shane

Принадлежит: STEPAN COMPANY

Esteramine compositions and their derivatives are disclosed. The esteramines comprise a reaction product of a metathesis-derived C-Cmonounsaturated acid, octadecene-1,18-dioic acid, or their ester derivatives with a tertiary alkanolamine. Derivatives made by quaternizing, sulfonating, alkoxylating, sulfating, and/or sulfitating the esteramines are also disclosed. In one aspect, the ester derivative of the C-Cmonounsaturated acid or octadecene-1,18-dioic acid is a lower alkyl ester. In other aspects, the ester derivative is a modified triglyceride made by self-metathesis of a natural oil or an unsaturated triglyceride made by cross-metathesis of a natural oil with an olefin. The esteramines and derivatives are valuable for a wide variety of end uses, including cleaners, fabric treatment, hair conditioning, personal care (liquid cleansing products, conditioning bars, oral care products), antimicrobial compositions, agricultural uses, and oil field applications. 1. An esteramine comprising a reaction product of a metathesis-derived C-Cmonounsaturated acid , octadecene-1 ,18-dioic acid , or their ester derivatives with a tertiary alkanolamine.2. A derivative made by one or more of quaternizing claim 1 , sulfonating claim 1 , alkoxylating claim 1 , sulfating claim 1 , and sulfitating the esteramine of .3. The esteramine of wherein the acid or ester derivative reactant has at least 1 mole % of trans-Δunsaturation.4. The esteramine of wherein the alkanolamine is selected from the group consisting of triethanolamine claim 1 , N-methyldiethanolamine claim 1 , N claim 1 ,N-dimethylethanol-amine claim 1 , and alkoxylated derivatives thereof.6. The esteramine of wherein the ester derivative is a modified triglyceride made by self-metathesis of a natural oil.7. The esteramine of wherein the natural oil is selected from the group consisting of soybean oil claim 6 , palm oil claim 6 , rapeseed oil claim 6 , algal oil claim 6 , and mixtures thereof.8. A derivative made by one or ...

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Номер записи: 9

12-09-2013 дата публикации

AMINES HAVING SECONDARY ALIPHATIC AMINO GROUPS

Номер: US20130237681A1

Автор: BURCKHARDT Urs

Принадлежит: SIKA TECHNOLOGY AG

The present invention relates to novel amides having secondary amino groups, a process for preparing them, adducts of these amines and their uses. The amides can be prepared in a simple way from readily available starting materials. They and their adducts have, in particular, a low viscosity and are suitable as constituent of polyurethane and polyurea compositions having excellent processability and high flexibility, and also as constituent of epoxy resin compositions, in particular coatings. 2. The amine of formula (I) according to claim 1 , wherein Rand Reach stand for a methyl radical and/or Rstands for a hydrogen atom.3. The amine of formula (I) according to claim 1 , wherein Rstands for a hydrogen atom or for a hydrocarbon radical with 1 to 12 carbon atoms claim 1 , optionally containing an ether oxygen.4. The amine of formula (I) according to claim 1 , wherein Rstands for a hydrogen atom or a linear or branched alkyl radical with 1 to 11 carbon atoms claim 1 , optionally with cyclic fractions and optionally with at least one heteroatom or for a mono- or polyunsaturated linear or branched hydrocarbon radical with 5 to 11 carbon atoms or for an optionally substituted aromatic or heteroaromatic six-membered ring.5. The amine of formula (I) according to claim 1 , wherein Xstands for a phenyl claim 1 , biphenyl or naphthyl radical claim 1 , where this radical is optionally substituted claim 1 , with linear or branched alkyl radicals with 1 to 6 carbon atoms claim 1 , with alkoxy groups with 1 to 6 carbon atoms claim 1 , with ester groups with 1 to 6 carbon atoms or with nitrilo groups.7. The method of synthesis of an amine of formula (I) according to claim 6 , wherein the process is carried out in such a way that at one amine PA of formula (II) is condensed with at least one aldehyde ALD of formula (III) to form an aldimine which is then hydrogenated.8. The method according to claim 6 , wherein the amine PA of formula (II) is selected from the group consisting of 1 ...

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Номер записи: 10

24-10-2013 дата публикации

CATIONIC LIPID

Номер: US20130280305A1

Автор: Era Tomohiro, Kuboyama Takeshi, Naoi Tomoyuki, Yagi Nobuhiro

Принадлежит:

The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) 2. The cationic lipid according to claim 1 , wherein Land Lare —O— or —O—CO— claim 1 , and Rand Rare dodecyl claim 1 , tetradecyl claim 1 , hexadecyl claim 1 , octadecyl claim 1 , icosyl claim 1 , docosyl claim 1 , tetracosyl claim 1 , (Z)-tetradec-9-enyl claim 1 , (Z)-hexadec-9-enyl claim 1 , (Z)-octadec-6-enyl claim 1 , (Z)-octadec-9-enyl claim 1 , (E)-octadec-9-enyl claim 1 , (Z)-octadec-11-enyl claim 1 , (9Z claim 1 ,12Z)-octadec-9 claim 1 ,12-dienyl claim 1 , (9Z claim 1 ,12Z claim 1 ,15Z)-octadec-9 claim 1 ,12 claim 1 ,15-trienyl claim 1 , (Z)-icos-11-enyl claim 1 , (11Z claim 1 ,14Z)-icos-11 claim 1 ,14-dienyl claim 1 , 3 claim 1 ,7 claim 1 ,11-trimethyldodeca-2 claim 1 ,6 claim 1 ,10-trienyl or 3 claim 1 ,7 claim 1 ,11 claim 1 ,15-tetramethylhexadec-2-enyl.3. The cationic lipid according to claim 1 , wherein Land Lare —CO—O— claim 1 , and Rand Rare tridecyl claim 1 , pentadecyl claim 1 , heptadecyl claim 1 , nonadecyl claim 1 , heneicosyl claim 1 , tricosyl claim 1 , (Z)-tridec-8-enyl claim 1 , (Z)-pentadec-8-enyl claim 1 , (Z)-heptadec-5-enyl claim 1 , (Z)-heptadec-8-enyl claim 1 , (E)-heptadec-8-enyl claim 1 , (Z)-heptadec-10-enyl claim 1 , (8Z claim 1 ,11Z)-heptadec-8 claim 1 ,11-dienyl claim 1 , (8Z claim 1 ,11Z claim 1 ,14Z)-octadec-8 claim 1 ,11 claim 1 ,14-trienyl claim 1 , (Z)-nonadec-10-enyl claim 1 , (10Z claim 1 ,13Z)-nonadec-10 claim 1 ,13-dienyl claim 1 , (11Z claim 1 ,14Z)-icos-11 claim 1 ,14-dienyl claim 1 , 2 claim 1 ,6 claim 1 ,10-trimethylundec-1 claim 1 ,5 claim 1 ,9-trienyl or 2 claim 1 ,6 claim 1 ,10 claim 1 ,14-tetramethylpentadec-1-enyl.4. The cationic lipid according to claim 1 , wherein a and b are both 0 or 1.5. The cationic lipid according to claim 1 , wherein Lis a single bond claim 1 , Ris a hydrogen atom claim 1 , methyl claim 1 , pyrrolidin-3-yl claim 1 , piperidin-3-yl claim 1 , piperidin-4- ...

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Номер записи: 11

20-02-2014 дата публикации

Patterning process and resist composition

Номер: US20140051026A1

Автор: Jun Hatakeyama, Koji Hasegawa, Masayoshi Sagehashi, Teppei Adachi

Принадлежит: Shin Etsu Chemical Co Ltd

A negative pattern is formed by coating a resist composition comprising a polymer comprising recurring units having a tertiary ester type acid labile group having a plurality of methyl or ethyl groups on alicycle and an acid generator onto a substrate, prebaking, exposing to high-energy radiation, baking, and developing in an organic solvent developer so that the unexposed region of resist film is dissolved away and the exposed region of resist film is not dissolved. The resist composition exhibits a high dissolution contrast during organic solvent development and forms a fine hole or trench pattern of dimensional uniformity.

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Номер записи: 12

03-04-2014 дата публикации

STABLE CRYSTAL MODIFICATIONS OF DOTAP CHLORIDE

Номер: US20140093558A1

Автор: Hedinger Alfred, Platscher Michael Wilhelm

Принадлежит: Merck Patent GmBH

The present invention relates to crystal modifications of racemic (2R,S)- and enantiomerically pure (2R)-resp. (2S)-DOTAP chloride, to processes for the preparation thereof, and to the use thereof for the preparation of pharmaceutical compositions. 1. Crystalline (2R ,S)- , (2S)- or (2R)-DOTAP chloride ,which crystalline (2R,S)-DOTAP chloride has one of the following characteristics:2 theta values comprising at least values of about 12.6, about 19.5, about 20.2, about 21.5 and about 25.2; or2 theta values comprising at least values of about 6.5, about 12.6, about 13.4, about 19.5, about 20.2, about 21.5, about 25.2 and about 29.8; oran X-ray powder diffraction pattern;orwhich crystalline (2S)-DOTAP chloride has one of the following characteristics:2 theta values comprising at least values of about 12.8, about 19.5, about 19.8, about 20.2, and about 21.6;2 theta values comprising at least values of about 6.5, about 12.8, about 19.5, about 19.8, about 20.2, about 20.7, about 21.6 and about 25.3; oran X-ray powder diffraction pattern;orwhich crystalline (2R)-DOTAP chloride has one of the following characteristics:2 theta values comprising at least values of about 12.8, about 19.5, about 19.8, about 20.3, and about 21.6;2 theta values comprising at least values of about 6.6, about 12.8, about 19.5, about 19.8, about 20.3, about 20.8, about 21.6 and about 25.3; oran X-ray powder diffraction pattern.2. Crystalline (2R ,S)- , (2S)- or (2R)-DOTAP chloride , which has a stability of higher than 99% by weight and Area-% determined by HPLC when stored at 25° C. for 36 months or at 40° C. for 12 months.3. Crystalline (2R ,S)- , (2S)- or (2R)-DOTAP chloride , which has a chemical purity of at least about 95% determined by HPLC.4. Crystalline (2R claim 1 ,S)- claim 1 , (2S)- or (2R)-DOTAP chloride according to claim 1 , which has a melting point of higher than 160° C. and a melting enthalpy of more than −130 J/g.5. A pharmaceutical composition comprising crystalline (2R claim 1 , ...

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Номер записи: 13

02-01-2020 дата публикации

Biodegradable compound, lipid particles, composition and kit comprising lipid particles

Номер: US20200000723A1

Автор: Eiichi Akahoshi, Katsuyuki Naito, Mitsuko Ishihara

Принадлежит: Toshiba Corp

[Problem] To provide a biodegradable compound having a structure decomposed in a cell, lipid particles containing the compound, and a pharmaceutical composition comprising the lipid particles. [Solution] The compound of the embodiment is represented by the formula (1): P—[X—R—Y—R′-Q] 2 (1). In the formula, P is an alkyleneoxy having an ether bond, X is a divalent linking group having a tertiary amine structure, R is a divalent linking group, R′ is a single bond or a C 1 to C 6 alkylene, and Q is a liposoluble vitamin residue, a sterol residue, or a C 12 to C 22 aliphatic hydrocarbon group. The structure of the compound contains at least one biodegradable group. From the compound in combination with other lipids such as a lipid capable of reducing aggregation, lipid particles can be formed. Further, the compound can be used for a pharmaceutical composition to deliver an activator into cells.

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Номер записи: 14

07-01-2016 дата публикации

NOVEL HIGH PENETRATION DRUGS AND THEIR COMPOSITIONS THEREOF FOR TREATMENT OF PARKINSON DISEASES

Номер: US20160002157A1

Автор: Xu Lina, Yu Chongxi

Принадлежит:

One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. The HPCs/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 HPCs/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. 2. A pharmaceutical composition comprising a high penetration prodrug according to ; a compound comprising a structure selected from the group consisting of Structure NSAID-1 claim 1 , Structure NSAID-2 claim 1 , Structure NSAID-3 claim 1 , Structure NSAID-4 claim 1 , Structure NSAID-5 claim 1 , Structure NSAID-6 claim 1 , Structure NSAID-7 claim 1 , Structure NSAID-8 claim 1 , Structure NSAID-9 claim 1 , Structure NSAID-10 claim 1 , Structure NSAID-11 claim 1 , Structure NSAID-12 claim 1 , and Structure NSAID-13; an aromatic-L-amino-acid decarboxylase inhibitor selected from the group consisting of carbidopa claim 1 , benserazide claim 1 , difluromethyldopa claim 1 , and α-methyldopa; a catechol-O-methyl transferase inhibitor selected from the group consisting of entacapone and tolcapone; and a pharmaceutically acceptable carrier.3. The pharmaceutical composition according to claim 2 , the pharmaceutically acceptable carrier being selected from the group consisting of alcohol claim 2 , acetone claim 2 , ester claim 2 , cellulose claim 2 , mannitol claim 2 , croscarmellose sodium claim 2 , vegetable oil claim 2 , ...

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Номер записи: 15

05-01-2017 дата публикации

DIAMINE CROSSLINKING AGENTS, CROSSLINKED ACIDIC POLYSACCHARIDES AND MEDICAL MATERIALS

Номер: US20170001948A1

Автор: Funayama Sho, Takahashi Katsuya, Takezawa Akihiro, Yasuda Yosuke

Принадлежит: Seikagaku Corporation

The invention provides a diamine crosslinking agent for acidic polysaccharides consisting of a diamine compound having a primary amino group at both terminals and an ester or thioester bond in the molecule, wherein the number of atom in the linear chain between at least one of the amino groups and the carbonyl carbon in the ester or thioester is 1 to 5; in particular, a diamine crosslinking agent for acidic polysaccharides which is represented by the general formula (I) below: 1. A diamine crosslinking agent for acidic polysaccharides consisting of diamine compounds having a primary amino group at both terminals and an ester or thioester bond in the molecule , wherein the number of atom in the linear chain between at least one of the amino groups and the carbonyl carbon in the ester or thioester is 1 to 5.3. The diamine crosslinking agent according to claim 2 , wherein Z is an oxygen atom.4. The diamine crosslinking agent according to claim 3 , wherein the number of atoms in the linear chain between the amino groups at both terminals is 5 to 8.5. The diamine crosslinking agent according to claim 3 , wherein the number of atoms in the linear chain between the amino groups at both terminals is 5 or 6.6. The diamine crosslinking agent according to claim 2 , wherein:{'sup': '1', 'Ris a hydrogen atom, or a substituted or unsubstituted alkyl group;'}{'sup': 2', '3', '4', '5, 'Ris a hydrogen atom, a —CONRRgroup or a —COORgroup;'}X is a single bond or an alkylene group which may be substituted by halogen;Y is a substituted or unsubstituted alkylene group;{'sup': 1', '5, 'the substituent(s) in Ris selected from the group consisting of methyl groups, phenyl groups, indolyl groups, —COORgroups and —S—Me groups; and'}{'sup': '5', 'the substituent(s) in Y is selected from the group consisting of methyl groups, phenyl groups and —COORgroups.'}7. The diamine cros slinking agent according to claim 2 , wherein:{'sup': 7', '8, 'X is a single bond; Y is a >CRRgroup; and'}{'sup': 7', ' ...

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Номер записи: 16

03-01-2019 дата публикации

Lipids and Lipid Compositions for the Delivery of Active Agents

Номер: US20190002393A1

Автор: BECKWITH Rohan Eric John, Brito Luis, DECHRISTOPHER Brian Addison, Gamber Gabriel Grant, Geall Andrew, ZABAWA Thomas

Принадлежит:

This invention provides for a compound of formula (I): 7. The compound claim 1 , or salt thereof claim 1 , according to claim 1 , wherein the compound is selected from the group consisting of:2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)benzyl 4-(dimethylamino)butanoate;((2-(((4-(dimethylamino)butanoyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-(((3-(dimethylamino)propanoyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-(((1-methylpiperidine-4-carbonyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-((((3-(dimethylamino)propoxy)carbonyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-((((3-(diethylamino)propoxy)carbonyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);3-(dimethylamino) propyl 4-methyl-2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)benzyl carbonate;4-methyl-2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)benzyl 4-(dimethylamino)butanoate;(9Z,9′Z,12Z,12′Z)-((2-(((4-(dimethylamino)butanoyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(butane-4,1-diyl) bis(octadeca-9,12-dienoate);4-(dimethylamino) butyl 4-methyl-2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)benzyl carbonate;((2-(((1-ethylpiperidine-4-carbonyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-(((1-isopropylpiperidine-4-carbonyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-((2-(1-methylpiperidin-4-yl)acetoxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-(((4-(pyrrolidin-1-yl)butanoyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)benzyl (3-(dimethylamino)propyl) carbonate;(9Z,9′Z,12Z,12′Z)-((2-(((4-(dimethylamino)butanoyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(ethane-2,1-diyl) bis(octadeca-9,12-dienoate);2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)benzyl 3-(dimethylamino)propanoate;2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy) ...

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Номер записи: 17

14-01-2016 дата публикации

Onium salt, liquid composition containing said onium salt and cellulose, and cellulose recovery method

Номер: US20160009669A1

Автор: Syuko SAKUGAWA, Yuko KOGA

Принадлежит: Koei Chemical Co Ltd

The invention relates to an onium salt, a liquid composition containing the onium salt and cellulose, and a method for recovering cellulose. The invention makes it possible to provide an onium salt having an extremely high ability to dissolve cellulose at temperatures of 100° C. or lower. It also makes it possible to provide a liquid composition containing this onium salt and cellulose, as a composition suitable for the recovery of cellulose, and a method for recovering cellulose efficiently by using such a liquid composition containing the onium salt and cellulose.

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Номер записи: 18

11-01-2018 дата публикации

RECLAMATION OF NOBLE PRODUCTS IN A METHOD FOR PRODUCING (METH)ACRYLIC ESTER

Номер: US20180009736A1

Автор: CABON Yves, DUBUT Fanny, RIFLADE Benoit

Принадлежит:

The invention relates to a method for producing a (meth)acrylic ester with improved productivity, by transesterfication of a light alkyl (meth)acrylate with a heavy alcohol. The method of the invention includes the recycling of noble products recovered after the thermal treatment of heavy fractions generated during the synthesis, said thermal treatment being carried out in the presence of a dialkyl phthalate, the alkyl chain of which corresponds to that of the light alkyl (meth)acrylate. The invention applies to the production of N,N-dimethyaminoethyl acrylate from ethyl acrylate. 1. A process for recovering unreacted reagents and (meth)acrylic ester products from a heavy (meth)acrylic fraction generated during production of a (meth)acrylic ester by transesterification reaction of a light C-Calkyl (meth)acrylate with a heavy alcohol in the presence of a catalyst , the heavy fraction comprising at least unreacted reagents and (meth)acrylic ester products and Michael adducts resulting from addition reactions on the (meth)acrylic double bonds and also the catalyst , said process comprising heat treating said heavy fraction at a temperature sufficient to crack the Michael adducts into their constituent components , recovering unreacted reagents and (meth)acrylic ester products in the form of a distillate , and eliminating fluid final residue by means of a pump , wherein the heat treatment is carried out in the presence of at least one dialkyl phthalate , the alkyl chain of which corresponds to that of the light alkyl (meth)acrylate.2. The process as claimed in claim 1 , wherein the light alkyl (meth)acrylate is methyl acrylate and the dialkyl phthalate is dimethyl phthalate.3. The process as claimed in claim 1 , wherein the light alkyl (meth)acrylate is ethyl acrylate and the dialkyl phthalate is diethyl phthalate.4. The process as claimed in claim 1 , wherein the light alkyl (meth)acrylate is butyl acrylate and the dialkyl phthalate is dibutyl phthalate.5. The process ...

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Номер записи: 19

03-02-2022 дата публикации

STIMULATION OF AN IMMUNE RESPONSE BY CATIONIC LIPIDS

Номер: US20220031650A1

Автор: Bedu-Addo Frank, Chen Weihsu, Conn Gregory, HUANG Leaf, Johnson Kenya, Yan Weili

Принадлежит:

The present invention provides compositions and methods for stimulating an immune response using cationic lipids alone or in combination with antigens. 1. A method of treating a coronavirus infection in a mammal , the method comprising administering at least one cationic lipid together with at least one coronavirus-associated antigen , wherein the cationic lipid is administered to the mammal in an amount sufficient to activate the MAP kinase signaling pathway to elicit an immunostimulatory adjuvant effect , wherein a mouse dose of cationic lipid is between 10 nmol and about 400 nmol , and wherein the mammal dose of cationic lipid is determined from the mouse dose.2. The method of wherein the cationic lipid is a nonsteroidal cationic lipid comprising at least one fatty acid or alkyl chain.3. The method of wherein the cationic lipid is selected from the group consisting of DOTAP claim 1 , DOTMA claim 1 , DOEPC claim 1 , and combinations thereof.4. The method of wherein the cationic lipid is DOTAP.5. The method of wherein the immunostimulatory adjuvant effect results in the attenuation or curing of the coronavirus infection.6. The method of wherein the antigen is modified to increase its hydrophobicity claim 1 , wherein the antigen is modified via conjugation to a lipid chain or via conjugation to one or more hydrophobic amino acids.7. The method of wherein the coronavirus-associated antigen is a lipidated antigen.8. The method of wherein the coronavirus-associated antigen is lipidated with palmitic acid.9. The method of wherein the palmitic acid is linked to the coronavirus-associated antigen via a spacer claim 8 , wherein the spacer is an amino acid sequence of K-S-S.10. A method of reducing the regulatory T-cell population in a mammal in need thereof claim 8 , the method comprising administering to the mammal at least one cationic lipid and at least one coronavirus-associated antigen claim 8 , wherein a mouse dose of cationic lipid is between 10 nmol and about 400 ...

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Номер записи: 20

18-01-2018 дата публикации

FLUORINE-CONTAINING ETHER MONOCARBOXYLIC ACID AMINOALKYL ESTER AND A METHOD FOR PRODUCING THE SAME

Номер: US20180016223A1

Автор: KOKIN Keisuke

Принадлежит:

A fluorine-containing ether monocarboxylic acid aminoalkyl ester represented by the general formula: 2. The fluorine-containing ether monocarboxylic acid aminoalkyl ester according to claim 1 , wherein a is an integer of 4 to 10 claim 1 , and b is an integer of 1 to 3.4. The method for producing the fluorine-containing ether monocarboxylic acid aminoalkyl ester according to claim 3 , wherein after completion of the reaction claim 3 , the reaction mixture is treated with an alkali metal hydroxide aqueous solution. The present invention relates to a fluorine-containing ether monocarboxylic acid aminoalkyl ester and a method for producing the same. More particularly, the present invention relates to a fluorine-containing ether monocarboxylic acid aminoalkyl ester that is imparted with flexibility in a molecular chain due to an ether bond in a molecule, and that is effectively used as a synthetic raw material, etc.; and also relates to a method for producing the same.Heretofore, the present applicant has proposed various fluoroethers having a terminal alkylamino group, to which flexibility in the molecular chain is imparted by an ether linkage in the molecule, or fluorine-containing polyether carboxylic acid amides (see Patent Documents 1 to 7). Further, the present applicant has also proposed fluorine-containing acid fluoride compounds having COOH, CONH, or the like at the molecular end (see Patent Document 8).However, there has been hardly observed finding on fluorine-containing ether carboxylic acid esters having an amino group at the end of the ester group.Patent Document 1: WO 2007/026513Patent Document 2: JP-A-2008-255042Patent Document 3: JP-A-2009-1709Patent Document 4: JP-A-2010-254736Patent Document 5: JP-A-2011-202055Patent Document 6: JP-A-2011-213837Patent Document 7: JP-A-2013-32455Patent Document 8: JP-A-2008-255035Patent Document 9: JP-A-3-284642Patent Document 10: JP-A-62-270546An object of the present invention is to provide a fluorine-containing ether ...

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Номер записи: 21

16-01-2020 дата публикации

Prodrugs of Fumarates and Their Use in Treating Various Diseases

Номер: US20200016111A1

Автор: Duncan Scott, Hencken Christopher P., Sanrame Carlos N., Wynn Thomas Andrew, Zeidan Tarek A.

Принадлежит:

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. 111-. (canceled)13. A pharmaceutical composition comprising the compound of claim 12 , or a pharmaceutically acceptable salt thereof.14. A method of treating multiple sclerosis in a subject in need thereof claim 12 , comprising administering to the subject a therapeutically effective amount of the compound of .15. A method of treating multiple sclerosis in a subject in need thereof claim 13 , comprising administering to the subject a therapeutically effective amount of a composition of . This application is a continuation of U.S. application Ser. No. 16/145,703, filed Sep. 28, 2018, which is a continuation of U.S. application Ser. No. 15/704,219, filed Sep. 14, 2017, now U.S. Pat. No. 10,117,846, issued Nov. 6, 2018, which is a continuation of U.S. application Ser. No. 15/295,370, filed Oct. 17, 2016, now U.S. Pat. No. 9,775,823, issued Oct. 3, 2017, which is a continuation of U.S. application Ser. No. 14/212,745, filed Mar. 14, 2014, now U.S. Pat. No. 9,505,776, issued Nov. 29, 2016, which claims the benefit of U.S. Provisional Application No. 61/934,365, filed Jan. 31, 2014 and U.S. Provisional Application No. 61/782,445, filed Mar. 14, 2013, the contents of which are incorporated herein by reference in their entireties.The present invention relates to various prodrugs of monomethyl fumarate. In particular, the present invention relates to derivatives of monomethyl fumarate which offer improved properties relative to dimethyl fumarate. The invention also relates to methods of treating various diseases.Fumaric acid esters (FAEs) are approved in Germany for the treatment of psoriasis, are being evaluated in the United States for the treatment of psoriasis and multiple sclerosis, and have been proposed for use in treating a wide range of immunological, autoimmune, and inflammatory diseases and conditions.FAEs and other fumaric acid derivatives have been proposed for use ...

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Номер записи: 22

16-01-2020 дата публикации

Compositions of oxygenated amines and quinone methides as antifoulants for vinylic monomers

Номер: US20200017656A1

Автор: Anahita Khanlari, Jonathan MASERE, Lisheng Xu

Принадлежит: ECOLAB USA INC

Described are compositions and methods for inhibiting polymerization of a monomer (e.g., styrene) composition a quinone methide polymerization retarder and an oxygen-containing amine compound that is a tertiary amine or hydroxylamine. In a mixture, the oxygen-containing amine compound improves the efficacy of the quinone methide polymerization retarder and provides greater antipolymerant activity. In turn, the mixture reduces or prevents apparatus fouling and improves the purity of monomer streams.

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Номер записи: 23

28-01-2016 дата публикации

ESTERAMINES AND DERIVATIVES FROM NATURAL OIL METATHESIS

Номер: US20160023989A1

Автор: Allen Dave R, Bernhardt Randal J, Brown Aaron, Dameshek Anatoliy A, Holland Brian, Malec Andrew D, Masters Ronald A, Nepras Marshall J, Skelton Patti, Whitlock Laura Lee, Wolfe Patrick Shane

Принадлежит:

Esteramine compositions and their derivatives are disclosed. The esteramines comprise a reaction product of a metathesis-derived C-Cmonounsaturated acid, octadecene-1,18-dioic acid, or their ester derivatives with a tertiary alkanolamine. Derivatives made by quaternizing, sulfonating, alkoxylating, sulfating, and/or sulfitating the esteramines are also disclosed. In one aspect, the ester derivative of the C-Cmonounsaturated acid or octadecene-1,18-dioic acid is a lower alkyl ester. In other aspects, the ester derivative is a modified triglyceride made by self-metathesis of a natural oil or an unsaturated triglyceride made by cross-metathesis of a natural oil with an olefin. The esteramines and derivatives are valuable for a wide variety of end uses, including cleaners, fabric treatment, hair conditioning, personal care (liquid cleansing products, conditioning bars, oral care products), antimicrobial compositions, agricultural uses, and oil field applications. 1. An esteramine or an esteramine derivative made by one or more of quaternizing , sulfonating , alkoxylating , sulfating , or sulfitating the esteramine , wherein the esteramine comprises a reaction product of a metathesis-derived C-Cmonounsaturated acid , octadecene-1 ,18-dioic acid , or their ester derivatives with a tertiary alkanolamine; said esteramine having the formula:{'br': None, 'sup': 1', '2, 'sub': 3-m', '2', 'n', '3', 'z', 'm, '(R)—N—[(CH)—(CHCH)—O—CO—R]'}where:{'sup': 1', '2', '3', '4', '3', '4, 'sub': 1', '6', '2', '7', '2', '7', '2', '7', '2', '1', '7, 'Ris C-Calkyl; Ris —(CH)—CH═CHRor —(CH)—CH═CH—(CH)—COR; Ris hydrogen or C-Calkyl; Ris substituted or unsubstituted alkyl, aryl, alkenyl, oxyalkylene, polyoxyalkylene, glyceryl ester, or a mono- or divalent cation; m=1-3; n=1-4; z=0 or 1; and when z=0, n=2-4;'}{'sup': 3', '9, 'sub': 1', '7, 'and wherein when Ris C-Calkyl, the acid or ester derivative reactant has at least 25 mole % of trans-Δunsaturation.'}2. (canceled)3. The esteramine or ...

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Номер записи: 24

10-02-2022 дата публикации

Nucleoside-Modified RNA For Inducing an Adaptive Immune Response

Номер: US20220040285A1

Автор: Hope Michael J., Pardi Norbert, Tam Ying, Weissman Drew

Принадлежит:

The present invention relates to compositions and methods for inducing an adaptive immune response in a subject. In certain embodiments, the present invention provides a composition comprising a nucleoside-modified nucleic acid molecule encoding an antigen, adjuvant, or a combination thereof. For example, in certain embodiments, the composition comprises a vaccine comprising a nucleoside-modified nucleic acid molecule encoding an antigen, adjuvant, or a combination thereof. 1. A composition for inducing an adaptive immune response in a subject , the composition comprising at least one nucleoside-modified RNA encoding at least one antigen.2. The composition of claim 1 , wherein the at least one isolated nucleoside-modified RNA comprises at least one selected from the group consisting of pseudouridine and 1-methyl-pseudouridine.3. (canceled)4. The composition of claim 1 , wherein the at least one antigen comprises at least one selected from the group consisting of a viral antigen claim 1 , a bacterial antigen claim 1 , a fungal antigen claim 1 , a parasitic antigen claim 1 , a tumor-associated antigen claim 1 , and a tumor-specific antigen5. The composition of claim 1 , wherein the at least one antigen comprises an antigen selected from the group consisting of an HIV antigen and an influenza antigen.6. The composition of claim 5 , wherein the antigen comprises an antigen selected from the group consisting of HIV envelope (Env) and influenza hemagglutinin (HA).78-. (canceled)9. The composition of claim 1 , wherein the composition further comprises an adjuvant.10. The composition of claim 1 , wherein the at least one nucleoside-modified RNA further encodes at least one adjuvant.11. The composition of claim 1 , further comprising a lipid nanoparticle (LNP).12. The composition of claim 11 , wherein the at least one nucleoside-modified RNA is encapsulated within the LNP.13. The composition of claim 1 , wherein the composition is a vaccine.2044-. (canceled) This application ...

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Номер записи: 25

25-01-2018 дата публикации

METHOD FOR PRODUCING 2-AMINOETHYLMETHACRYLATE HYDROCHLORIDE

Номер: US20180022692A1

Автор: IIDA Yuri, Sato Hideyuki, TAKEMOTO Masaki

Принадлежит: MITSUBISHI GAS CHEMICAL COMPANY, INC.

Provided is a method for producing 2-aminoethyl methacrylate hydrochloride that, according to one embodiment, includes a step (A) for reacting a ketimine compound of 2-aminoethyl methacrylate with water and hydrogen chloride and obtaining a mixture containing 2-aminoethyl methacrylate hydrochloride, wherein in the step (A), the ratio of the total amount of hydrogen chloride to the total amount of ketimine compound of 2-aminoethyl methacrylate is 1.0-1.5 expressed in terms of equivalents, and the ratio of the total amount of water to the total amount of ketimine compound of 2-aminoethyl methacrylate is 1.0-2.0 expressed in terms of equivalents. 2. The method for producing 2-aminoethyl methacrylate hydrochloride according to claim 1 , wherein Rand Rin Formula (1) above each independently represent an alkyl group with a carbon number of 1-4.3. The method for producing 2-aminoethyl methacrylate hydrochloride according to claim 2 , wherein claim 2 , in Formula (1) above claim 2 , Rrepresents a methyl group and Rrepresents an ethyl group or an isobutyl group.4. The method for producing 2-aminoethyl methacrylate hydrochloride according to claim 3 , wherein Rin Formula (1) above represents an isobutyl group.5. The method for producing 2-aminoethyl methacrylate hydrochloride according to claim 3 , wherein Rin Formula (1) above represents an ethyl group.6. The method for producing 2-aminoethyl methacrylate hydrochloride according to claim 1 , wherein hydrogen chloride is hydrogen chloride gas.7. The method for producing 2-aminoethyl methacrylate hydrochloride according to claim 1 , wherein the reaction of the ketimine compound of 2-aminoethyl methacrylate represented by Formula (1) with water and hydrogen chloride is carried out such that the ratio of the accumulated supply amount of hydrogen chloride to the accumulated supply amount of the ketimine compound of 2-aminoethyl methacrylate is maintained at 1.0 or higher in equivalent ratio throughout the whole period from the ...

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Номер записи: 26

01-02-2018 дата публикации

Method for preparing 4-isopropylamino-1-butanol

Номер: US20180029973A1

Автор: Chi Ma, Fanghui TANG, Qiang JIA

Принадлежит: Seasons Biotechnology (taizhou) Co Ltd

The present invention relates to a preparation method of 4-isopropylamino-1-butanol, in which using cheap and readily available tetrahydrofuran and acetic acid solution of hydrogen bromide as starting materials to prepare a novel intermediate of 4-isopropylamino-1-acetoxyl butane and further obtain the target product. The present invention has advantages of convenient process operations, mild reaction conditions, economical and environment-friendly benefits, and suitability for industrial production to obtain the product with high purity and high yield.

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Номер записи: 27

30-01-2020 дата публикации

P62-zz chemical inhibitor

Номер: US20200031761A1

Автор: Garson David Roodman, Kyaw-Zeyar Myint, Noriyoshi Kurihara, Xiang-qun XIE

Принадлежит: ID4PHARMA LLC

A method for treating a p62-mediated disease (e.g., multiple myeloma) in a subject, the method comprising administering to the subject a therapeutically effective amount of at least one p62-ZZ inhibitor compound.

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Номер записи: 28

06-02-2020 дата публикации

COMPOSITION, METHOD AND USE

Номер: US20200040270A1

Автор: Roberts Martin, Ross Alan Norman

Принадлежит: INNOSPEC LIMITED

A quaternary ammonium salt of formula (I): wherein X is a linking group; Y is O, NH or NRwherein Ris H or an optionally substituted hydrocarbyl group; Q is a moiety that includes a quaternary ammonium cation; A is an anion; Ris an optionally substituted alkylene group; Ris hydrogen or an optionally substituted hydrocarbyl group; and n is 0 or a positive integer; provided that n is not 0 when Ris hydrogen. 3. (canceled)5. The salt according to wherein the quaternary ammonium salt additive is prepared by reacting:(a) a hydrocarbyl substituted dicarboxylic acid or anhydride thereof; with{'sup': 3', '2, 'sub': 'n', '(b) an alcohol of formula R(OR)OH;'}(c) a reactive alcohol or amine including a tertiary amino group; and(d) a quaternising agent.6. The salt according to wherein X is an optionally substituted alkylene or arylene group and Ris an optionally substituted hydrocarbyl group.7. The salt according to wherein n is 0 and Ris an optionally substituted alkyl or alkenyl group having 4 to 40 carbon atoms.8. The salt according to wherein each Ris ethylene or propylene.9. The salt according to wherein Ris hydrogen and n is at least 1.10. The salt according to wherein Ris an optionally substituted alkyl group having 4 to 40 carbon atoms and n is from 1 to 40.12. The salt according to wherein Ris an optionally substituted alkylene group having 1 to 6 carbon atoms claim 11 , Ris Cto Calkyl claim 11 , Ris Cto Calkyl and Ris an unsubstituted Cto Calkyl group or a hydroxy substituted Cto Calkyl group.13. The salt according to wherein Ais a carboxylate anion.14. The salt according to wherein the quaternary ammonium salt additive is prepared by reacting:(a) an optionally substituted succinic acid or anhydride thereof;{'sup': 2', '3, 'sub': 'n', '(b) an alcohol of formula H(OR)OH or ROH;'}(c) a reactive alcohol including a tertiary amino group; and(d) a quaternising agent.15. The salt according to wherein the quaternary ammonium salt additive is prepared by reacting:{'sub': 20', ...

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Номер записи: 29

15-02-2018 дата публикации

PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES

Номер: US20180042881A1

Автор: Duncan Scott, Hencken Christopher P., Sanrame Carlos N., Wynn Thomas Andrew, Zeidan Tarek A.

Принадлежит:

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. 1. (canceled)3. A pharmaceutical composition comprising a crystalline form of and a pharmaceutically acceptable carrier.4. A method of treating multiple sclerosis in a subject in need thereof claim 2 , comprising administering to the subject a therapeutically effective amount of a crystalline form of .5. A method of treating multiple sclerosis in a subject in need thereof claim 3 , comprising administering to the subject a therapeutically effective amount of a composition of . This application is a continuation of U.S. application Ser. No. 15/704,219, filed Sep. 14, 2017, which is a continuation of U.S. application Ser. No. 15/295,370, filed Oct. 17, 2016, now U.S. Pat. No. 9,775,823, issued Oct. 3, 2017, which is a continuation of U.S. application Ser. No. 14/212,745, filed Mar. 14, 2014, now U.S. Pat. No. 9,505,776, issued Nov. 29, 2016, which claims the benefit of U.S. Provisional Application No. 61/934,365, filed Jan. 31, 2014 and U.S. Provisional Application No. 61/782,445, filed Mar. 14, 2013, the contents of which are incorporated herein by reference in their entireties.The present invention relates to various prodrugs of monomethyl fumarate. In particular, the present invention relates to derivatives of monomethyl fumarate which offer improved properties relative to dimethyl fumarate. The invention also relates to methods of treating various diseases.Fumaric acid esters (FAEs) are approved in Germany for the treatment of psoriasis, are being evaluated in the United States for the treatment of psoriasis and multiple sclerosis, and have been proposed for use in treating a wide range of immunological, autoimmune, and inflammatory diseases and conditions.FAEs and other fumaric acid derivatives have been proposed for use in treating a wide-variety of diseases and conditions involving immunological, autoimmune, and/or inflammatory processes including psoriasis (Joshi ...

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Номер записи: 30

01-05-2014 дата публикации

LIPID CONTAINING FORMULATIONS

Номер: US20140121393A1

Автор: Akinc Akin, Jayaprakash Narayanannair K., Jayaraman Muthusamy, MAIER Martin, Manoharan Muthiah, Rajeev Kallanthottathil G.

Принадлежит: TEKMIRA PHARMACEUTICALS CORPORATION

Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described. 2. The compound of claim 1 , wherein Ris H claim 1 , methyl claim 1 , ethyl claim 1 , isopropyl claim 1 , or 2-hydroxyethyl and Ris H claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , or isopropyl.3. The compound of claim 1 , wherein both m and n are 1.4. The compound of claim 1 , wherein both Land Lare —OC(O)— or —C(O)O—.5. The compound of claim 1 , wherein both Land Lare —N(R)C(O)N(R)—.6. The compound of claim 1 , wherein both Land Lare —OC(O)N(R)— or —N(R)C(O)O—.7. The compound of claim 1 , wherein Lis —NRC(O)— and Lis —S—S—.8. The compound of claim 1 , wherein Lis —OC(O)— and Lis —S—S—.9. The compound of claim 1 , wherein Lis —OC(O)N(R) or —N(R)C(O)O— and Lis —S—S—.10. The compound of claim 1 , wherein Lis —N(R)C(O)N(R)— and L2 is —S—S—.11. The compound of claim 1 , wherein L-Rand L-Rare taken together to form an acetal claim 1 , a ketal claim 1 , or an orthoester.12. The compound of claim 1 , wherein both Rand Rare C-Calkyl.13. The compound of claim 12 , wherein each Land Lare independently —S—S— claim 12 , —OC(O)N(R)— or —N(R)C(O)O—.14. The compound of claim 1 , wherein each Rand Rare independently C-Calkenyl.19. A preparation comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof. This application is a divisional application of U.S. patent application Ser. No. 13/211,094, filed on Aug. 16, 2011, which is a continuation application of U.S. patent application Ser. No. 12/056,230, filed on Mar. 26, 2008, which application issued as U.S. Pat. No. 8,034,376 on Oct. 11, 2011, which is a continuation application of International Patent Application No. PCT/US2007/080331, filed on Oct. 3, 2007, and claims priority to U.S. Provisional Application No. 60/828,022 filed on Oct. 3, 2006 and U.S. Provisional Application No. 60/870,457 filed on Dec. 18, 2006. The entire content ...

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Номер записи: 31

19-02-2015 дата публикации

Compound having acridan ring structure, and organic electroluminescent device

Номер: US20150048351A1

Автор: Eiji Takahashi, Makoto Nagaoka, Naoaki Kabasawa, Norimasa Yokoyama

Принадлежит: Hodogaya Chemical Co Ltd

An organic compound with characteristics excelling in hole-injecting/transporting performance and having an electron blocking ability, a highly stable thin-film state, and excellent heat resistance is provided as material for an organic electroluminescent device of high efficiency and high durability, and the organic electroluminescent device of high efficiency and high durability is provided using this compound. The compound of a general formula (Chemical Formula 1) having a substituted acridan ring structure is used as a constituent material of at least one organic layer in the organic electroluminescent device that includes a pair of electrodes and one or more organic layers sandwiched between the pair of electrodes.

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Номер записи: 32

03-03-2022 дата публикации

Novel high penetration drugs and their compositions thereof for treatment of parkinson diseases

Номер: US20220064157A1

Автор: Chongxi Yu, Lina Xu

Принадлежит: Techfields Pharma Co Ltd

One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. The HPCs/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 HPCs/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.

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Номер записи: 33

25-02-2016 дата публикации

Biological buffers with wide buffering ranges

Номер: US20160052868A1

Автор: Thomas P. Daly

Принадлежит: TPAT IP LLC

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

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Номер записи: 34

10-03-2022 дата публикации

NOVEL LIPIDS AND LIPID NANOPARTICLE FORMULATIONS FOR DELIVERY OF NUCLEIC ACIDS

Номер: US20220072155A1

Автор: Ansell Steven M., Du Xinyao

Принадлежит:

Compounds are provided having the following structure: 140.-. (canceled)42. A lipid nanoparticle comprising the compound of .43. The lipid nanoparticle of claim 42 , further comprising a messenger RNA.44. A pharmaceutical composition comprising the compound of and one or more pharmaceutically acceptable carriers claim 41 , diluents or excipients.45. A pharmaceutical composition comprising the lipid nanoparticle of and one or more pharmaceutically acceptable carriers claim 42 , diluents or excipients.46. A pharmaceutical composition comprising the lipid nanoparticle of and one or more pharmaceutically acceptable carriers claim 43 , diluents or excipients. The present invention generally relates to novel cationic lipids that can be used in combination with other lipid components, such as neutral lipids, cholesterol and polymer conjugated lipids, to form lipid nanoparticles with oligonucleotides, to facilitate the intracellular delivery of therapeutic nucleic acids (e.g. oligonucleotides, messenger RNA) both in vitro and in vivo.There are many challenges associated with the delivery of nucleic acids to affect a desired response in a biological system. Nucleic acid based therapeutics have enormous potential but there remains a need for more effective delivery of nucleic acids to appropriate sites within a cell or organism in order to realize this potential. Therapeutic nucleic acids include, e.g., messenger RNA (mRNA), antisense oligonucleotides, ribozymes, DNAzymes, plasmids, immune stimulating nucleic acids, antagomir, antimir, mimic, supermir, and aptamers. Some nucleic acids, such as mRNA or plasmids, can be used to effect expression of specific cellular products as would be useful in the treatment of, for example, diseases related to a deficiency of a protein or enzyme. The therapeutic applications of translatable nucleotide delivery are extremely broad as constructs can be synthesized to produce any chosen protein sequence, whether or not indigenous to the system. ...

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Номер записи: 35

01-03-2018 дата публикации

Derivatives of sobetirome

Номер: US20180057472A1

Автор: Andrew PLACZEK, James Matthew MEINIG, Sky Ferrara, Tapasree BANERJI, Thomas S. Scanlan

Принадлежит: Oregon Health Science University

Ester derivatives of sobetirome with enhanced CNS distribution are disclosed.

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Номер записи: 36

08-03-2018 дата публикации

PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES

Номер: US20180064673A1

Автор: Duncan Scott, Hencken Christopher P., Sanrame Carlos N., Wynn Thomas Andrew, Zeidan Tarek A.

Принадлежит:

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. 2. The composition of claim 1 , wherein Ris methyl.3. The composition of claim 1 , wherein Lis an unsubstituted C-Calkyl.4. The composition of claim 3 , wherein Lis an unsubstituted C-Calkyl.5. The composition of claim 4 , wherein Lis an unsubstituted Calkyl.6. The composition of claim 1 , wherein Ris an unsubstituted C-Calkyl claim 1 , unsubstituted C-Calkenyl claim 1 , or unsubstituted C-Calkynyl.7. The composition of claim 6 , wherein Ris an unsubstituted C-Calkyl.8. The composition of claim 7 , wherein Ris an unsubstituted C-Calkyl.9. The composition of claim 8 , wherein Ris an unsubstituted C-Calkyl.10. The composition of claim 9 , wherein Ris methyl. This application is a continuation of U.S. application Ser. No. 15/295,370, filed Oct. 17, 2016 which is a continuation of U.S. application Ser. No. 14/212,745, filed Mar. 14, 2014, now U.S. Pat. No. 9,505,776, issued Nov. 29, 2016, which claims the benefit of U.S. Provisional Application No. 61/934,365, filed Jan. 31, 2014 and U.S. Provisional Application No. 61/782,445, filed Mar. 14, 2013, the contents of which are incorporated herein by reference in their entireties.The present invention relates to various prodrugs of monomethyl fumarate. In particular, the present invention relates to derivatives of monomethyl fumarate which offer improved properties relative to dimethyl fumarate. The invention also relates to methods of treating various diseases.Fumaric acid esters (FAEs) are approved in Germany for the treatment of psoriasis, are being evaluated in the United States for the treatment of psoriasis and multiple sclerosis, and have been proposed for use in treating a wide range of immunological, autoimmune, and inflammatory diseases and conditions.FAEs and other fumaric acid derivatives have been proposed for use in treating a wide-variety of diseases and conditions involving immunological, autoimmune, and/or ...

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Номер записи: 37

08-03-2018 дата публикации

LIPID CONTAINING FORMULATIONS

Номер: US20180065918A1

Автор: Akinc Akin, Jayaraman Muthusamy, MAIER Martin, Manoharan Muthiah, NAIR Jayaprakash K., Rajeev Kallanthottathil G.

Принадлежит: Arbutus Biopharma Corporation

Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described. 3. A preparation comprising a compound of .4. An association complex comprising a preparation of .5. An association complex comprising a preparation of .6. The association complex of claim 4 , further comprising a therapeutic agent.7. The association complex of claim 6 , wherein the therapeutic agent is nucleic acid.8. The association complex of claim 6 , wherein the therapeutic agent is siRNA.9. The association complex of claim 6 , wherein the therapeutic agent is mRNA.10. The association complex of claim 5 , further comprising a therapeutic agent.11. The association complex of claim 10 , wherein the therapeutic agent is nucleic acid.12. The association complex of claim 10 , wherein the therapeutic agent is siRNA.13. The association complex of claim 10 , wherein the therapeutic agent is mRNA.14. A method of treating a mammal comprising administering to said mammal a therapeutic amount of an association complex of .15. A method of treating a mammal comprising administering to said mammal a therapeutic amount of an association complex of . This application is a Continuation application of U.S. patent application Ser. No. 14/149,496, filed on Jan. 7, 2014, which is a Divisional application of U.S. patent application Ser. No. 13/211,094, filed on Aug. 16, 2011, issued as U.S. Pat. No. 8,642,076 on Feb. 4, 2014, which is a continuation application of U.S. patent application Ser. No. 12/056,230, filed on Mar. 26, 2008, issued as U.S. Pat. No. 8,034,376 on Oct. 11, 2011, which is a continuation application of International Patent Application No. PCT/US2007/080331, filed on Oct. 3, 2007, which claims priority to U.S. Provisional Application No. 60/828,022 filed on Oct. 3, 2006 and U.S. Provisional Application No. 60/870,457 filed on Dec. 18, 2006. The entire content of each of these applications is hereby ...

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Номер записи: 38

05-03-2020 дата публикации

Biological Buffers with Wide Buffering Ranges

Номер: US20200071582A1

Автор: Daly Thomas

Принадлежит:

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability. 2. The biological buffer and its salts of wherein A═D═—CH3 and m=1.3. The biological buffer and its salts of wherein A═D═—CH2OH and m=1.4. The biological buffer and its salts of wherein A═D—CH2O(CH2CH2CH2N)H and n=m=1.5. The biological buffer and its salts of wherein A═—CH2CH3 claim 1 , D═—CH2O(CH2CH2CH2N)H and n=m=1.6. The biological buffer and its salts of wherein A═—CH3 claim 1 , D═—CH2O(CH2CH2CH2N)H and n=m=1.7. The biological buffer and its salts of wherein A is —CH3 and D is —CH2CH3.9. The quaternary ammonium compound and its salts of wherein A═D═—CH3 claim 8 , E═—CH2OH claim 8 , R═R′═—CH3 and G═—H.10. The quaternary ammonium compound and its salts of wherein A═D═E═—CH2OH claim 8 , R═R′═—CH3 and G═—H.11. The quaternary ammonium compound and its salts of wherein A═D═—CH3 claim 8 , E═—CH2OH claim 8 , R═R′═—CH3 and G═—CH2CH3.12. The quaternary ammonium compound and its salts of wherein A═D═E═—CH2OH claim 8 , R═R′=—CH3 and G═—CH2CH3. This is a continuation of U.S. application Ser. No. 15/649,869 filed Jul. 14, 2017 and other previous parent applications claimed in the Application Data Sheet. U.S. application Ser. No. 15/649,869 is hereby incorporated by reference in its entirety.The present invention relates generally to the field of amines and more particularly to a classes of amines used as buffers in biological systems.Amines are very useful compounds in the buffering of biological systems. Each class of amine has various limitations which require choosing an amine ...

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Номер записи: 39

18-03-2021 дата публикации

Lipids and lipid compositions for the delivery of active agents

Номер: US20210078936A1

Автор: Andrew Geall, Delai Chen, Frédéric ZECRI, Gabriel GAMBER, Kevin Love, Luis Brito, Thomas ZABAWA

Принадлежит: NOVARTIS AG

or a pharmaceutically acceptable salt thereof, wherein R1-R4, L1, n and p are defined herein. The compounds of formula (X) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

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Номер записи: 40

24-03-2016 дата публикации

FORMULATION COMPRISING ESTER QUATS BASED ON ISOPROPANOLAMINE AND TETRAHYDROXYPROPYL ETHYLENEDIAMINE

Номер: US20160083333A1

Автор: Koehle Hans-Juergen, Schwab Peter, Seidel Kurt, Wenk Hans Henning, Westerholt Ursula

Принадлежит:

The invention relates to cosmetic formulations comprising specific ester quats based on isopropanolamine or tetrahydroxypropyl ethylenediamine, and to the use of these ester quats in cosmetics. 2. The cosmetic formulation according to claim 1 , wherein Ris selected from the acyl residues of acids selected from oleic acid claim 1 , elaidic acid claim 1 , vaccenic acid claim 1 , gadoleic acid claim 1 , icosenoic acid claim 1 , cetoleic acid claim 1 , erucic acid claim 1 , nervonic acid claim 1 , linolic acid claim 1 , alpha-linolenic acid claim 1 , gamma-linolenic acid claim 1 , calendulic acid claim 1 , punicic acid claim 1 , alpha-elaeostearic acid claim 1 , beta-elaeostearic acid claim 1 , arachidonic acid claim 1 , timnodonic acid claim 1 , clupanodonic acid and cervonic acid.3. The cosmetic formulation according to claim 1 , wherein in general formula I) a=b=2.4. The cosmetic formulation according to claim 1 , wherein no fatty acids or fatty acid salts are present.5. The cosmetic formulation according to claim 1 , further comprising:0.5 to 20% by weight of at least one fatty alcohol,where the percentages by weight refer to the total formulation.6. The cosmetic formulation according to claim 5 , wherein said fatty alcohol is selected from octanol claim 5 , decanol claim 5 , lauryl alcohol claim 5 , isolauryl alcohol claim 5 , anteisolauryl alcohol claim 5 , myristyl alcohol claim 5 , isomyristyl alcohol claim 5 , cetyl alcohol claim 5 , palmoleyl alcohol claim 5 , stearyl alcohol claim 5 , isostearyl alcohol claim 5 , anteisostearyl alcohol claim 5 , eicosanol claim 5 , petroselinyl alcohol claim 5 , Guerbet alcohol claim 5 , arachyl alcohol claim 5 , gadoleyl alcohol claim 5 , behenyl alcohol claim 5 , erucyl alcohol claim 5 , hectacosanol claim 5 , octacosanol claim 5 , and melissyl alcohol claim 5 , and mixtures thereof.7. The cosmetic formulation according to claim 1 , further comprising: at least one counterion to the compound of general formula I) selected ...

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Номер записи: 41

31-03-2022 дата публикации

PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES

Номер: US20220096419A1

Автор: Duncan Scott, Hencken Christopher P., Sanrame Carlos N., Wynn Thomas Andrew, Zeidan Tarek A.

Принадлежит:

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. 2. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof.3. A method of treating multiple sclerosis in a subject in need thereof claim 1 , comprising administering to the subject a therapeutically effective amount of the compound of .4. A method of treating multiple sclerosis in a subject in need thereof claim 2 , comprising administering to the subject a therapeutically effective amount of the composition of . This application is a continuation of U.S. application Ser. No. 16/790,849, filed Feb. 14, 2020, which is a continuation of U.S. application Ser. No. 16/524,498, filed Jul. 29, 2019, now U.S. Pat. No. 10,596,140, issued Mar. 24, 2020, which is a continuation of U.S. application Ser. No. 16/145,703, filed Sep. 28, 2018, now U.S. Pat. No. 10,406,133, issued Sep. 10, 2019, which is a continuation of U.S. application Ser. No. 15/704,219, filed Sep. 14, 2017, now U.S. Pat. No. 10,117,846, issued Nov. 6, 2018, which is a continuation of U.S. application Ser. No. 15/295,370, filed Oct. 17, 2016, now U.S. Pat. No. 9,775,823, issued Oct. 3, 2017, which is a continuation of U.S. application Ser. No. 14/212,745, filed Mar. 14, 2014, now U.S. Pat. No. 9,505,776, issued Nov. 29, 2016, which claims the benefit of U.S. Provisional Application No. 61/934,365, filed Jan. 31, 2014 and U.S. Provisional Application No. 61/782,445, filed Mar. 14, 2013, the conterts of which are incorporated herein by reference in their entireties.The present invention relates to various prodrugs of monomethyl fumarate. In particular, the present invention relates to derivatives of monomethyl fumarate which offer improved properties relative to dimethyl fumarate. The invention also relates to methods of treating various diseases.Fumaric acid esters (FAEs) are approved in Germany for the treatment of psoriasis, are being evaluated in the United ...

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Номер записи: 42

25-03-2021 дата публикации

Compound or salt thereof and lipid particles

Номер: US20210085604A1

Автор: Hirofumi Fukunaga, Issei Doi, Kazuhiro TSUNA, Kimihiko Sato, Masahiko Yamamoto, Motomasa TAKAHASHI, Shintaro TANABE, Taisuki ENDO, Yasutaka Tasaki

Принадлежит: Fujifilm Corp

An object of the present invention is to provide a compound or a salt thereof constituting lipid particles that can achieve a high nucleic acid encapsulation rate and excellent delivery of nucleic acids, and to provide lipid particles that can achieve a high nucleic acid encapsulation rate and excellent delivery of nucleic acids. According to an aspect of the present invention, a compound represented by Formula (1) or a salt thereof is provided. In the formula, X represents —NR 1 — or —O—, R represents a hydrogen atom, a hydrocarbon group, or the like, R 2 and R 3 each independently represent a hydrogen atom, a hydrocarbon group, or the like, R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 each independently represent a hydrogen atom or an alkyl group, groups in any one or more pairs among R 4 and R 5 , R 10 and R 5 , R 5 and R 12 , R 4 and R 6 , R 5 and R 6 , R 6 and R 7 , R 6 and R 10 , R 12 and R 7 , and R 7 and R 8 may be linked to each other to form a 4- to 7-membered ring which may contain an O atom, a, b, c, and d are each independently represent an integer of 0 to 3, a+b is equal to or greater than 1, and c+d is equal to or greater than 1.

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Номер записи: 43

21-03-2019 дата публикации

METHOD OF PREPARATION OF 4-ISOPROPYLAMINO-1-BUTANOL

Номер: US20190084921A1

Автор: Jia Qiang, Ma Chi, Tang Fanghui

Принадлежит:

The present invention relates to a preparation method of 4-isopropylamino-1-butanol, in which using cheap and readily available tetrahydrofuran and acetic acid solution of hydrogen bromide as starting materials to prepare a novel intermediate of 4-isopropylamino-1-acetoxyl butane and further obtain the target product. The present invention has advantages of convenient process operations, mild reaction conditions, economical and environment-friendly benefits, and suitability for industrial production to obtain the product with high purity and high yield. 1. 4-isopropylamino-1-acetoxyl butane represented by formula (II): The present invention is a divisional application of U.S. application Ser. No. 15/552,772, filed Aug. 22, 2017, which is a U.S. national phase of International Application No. PCT/CN2016/000180 under 35 U.S.C. § 371. The teaching in these related applications are incorporated herein in its entirety by reference.The present invention relates to the technical field of chemical synthesis in pharmaceutical industry, specifically, it relates to a preparation method of 4-isopropylamino-1-butanol and a novel intermediate thereof.4-isopropylamino-1-butanol is an important intermediate in pharmaceutical industry, and its structural formula is represented by formula (I):4-isopropylamino-1-butanol was widely used in the pharmaceutical synthesis, for example, Patent Document WO2002088084A1 disclosed a four-step reaction using 4-isopropylamino-1-butanol as the raw material to prepare pulmonary hypertension drug of selexipag. This document was incorporated by reference into the present application.Journal of Organic Chemistry (1961), Vol. 26, P 1744-1747 disclosed a preparation method of 4-isopropylamino-1-butanol, which comprised: (1) reacted succinic anhydride with isopropyl amine to obtain 3-isopropyl carbamoyl propionic acid; (2) reduced 3-isopropylcarbamoyl propionic acid with lithium aluminum hydride to obtain 4-isopropylamino-1-butanol.This method had ...

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Номер записи: 44

02-04-2015 дата публикации

Stimulation of An Immune Response By Cationic Lipids

Номер: US20150093410A1

Автор: Bedu-Addo Frank, Chen Weihsu, Conn Gregory, HUANG Leaf, Johnson Kenya, Yan Weili

Принадлежит:

The present invention provides compositions and methods for stimulating an immune response using cationic lipids alone or in combination with antigens. 128.-. (canceled)29. An immunomodulator composition comprising at least one cationic lipid in a dose sufficient to induce an immune response in a mammal ,wherein the dose of cationic lipid in mice is between about 10 nmol and about 600 nmol, andwherein the dose of cationic lipid in the mammal is determined from the mouse dose.301. The immunomodulator composition of claim , wherein the cationic lipid is selected from the group consisting of DOTAP , DOTMA , DOEPC , and combinations thereof.311. The immunomodulator composition of claim , wherein the cationic lipid is DOTAP.321. The immunomodulator composition of claim further comprising an antigen.334. The immunomodulator composition of claim , wherein the antigen is a microbial antigen.344. The immunomodulator composition of claim , wherein the antigen is a tumor-associated antigen.354. The immunomodulator composition of claim , wherein the antigen is an HPV antigen.361. The immunomodulator composition of claim further comprising an additional therapeutic agent.37. A pharmaceutical formulation comprising at least one cationic lipid in a dose sufficient to induce an immune response in a mammal ,wherein the dose of cationic lipid in mice is between about 10 nmol and about 600 nmol, andwherein the dose of cationic lipid in the mammal is determined from the mouse dose.389. The pharmaceutical formulation of claim , wherein the cationic lipid is selected from the group consisting of DOTAP , DOTMA , DOEPC , and combinations thereof.399. The pharmaceutical formulation of claim , wherein the cationic lipid is DOTAP.409. The pharmaceutical formulation of claim further comprising an antigen.4112. The pharmaceutical formulation of claim , wherein the antigen is a microbial antigen.4212. The pharmaceutical formulation of claim , wherein the antigen is a tumor-associated antigen. ...

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Номер записи: 45

12-05-2022 дата публикации

REDUCING AGENT MONOMER FOR PREPARING STYRENE-ACRYLIC EMULSION BY OXIDATION-REDUCTION REACTION AT ROOM TEMPERATURE, AND SYNTHESIS METHOD THEREOF

Номер: US20220144986A1

Автор: HUANG Wenyan, JIANG Bibiao, JIANG LI, JIANG Qimin, SUN Qiujie, XUE Xiaoqiang, Yang Hongjun

Принадлежит: CHANGZHOU UNIVERSITY

A reducing agent monomer for preparing a styrene-acrylic emulsion by an oxidation-reduction reaction at room temperature and a synthesis method thereof are disclosed. Maleic anhydride (MAH) and dimethylethanolamine (DMEA) are used as raw materials to synthesize the reducing agent monomer: 4-(2-(dimethylamino)ethoxy)-4-oxobut-2-enoic acid, and the synthesis method involves inexpensive easily-available raw materials, simple synthesis conditions, and easy purification. With the synthesized reducing agent monomer as a reducing agent, potassium persulfate (KPS) as an oxidizing agent, water as a dispersion medium, sodium dodecyl sulfate (SDS) as an emulsifier, and styrene, butyl acrylate (BA), and methylmethacrylate (MMA) as comonomers, free-radical microemulsion polymerization is conducted at room temperature to obtain a styrene-acrylic emulsion. In the synthesis of the styrene-acrylic emulsion, a monomer conversion rate is high, and a styrene-acrylic emulsion with a high molecular weight and a branched structure can be obtained at room temperature. 1. (canceled)2. (canceled)3. (canceled)4. Use of a reducing agent monomer synthesized by a synthesis method of the reducing agent monomer for preparing a styrene-acrylic emulsion by an oxidation-reduction reaction at room temperature , wherein an oxidation-reduction initiation system is formed from the reducing agent monomer and a persulfate;the synthesis method comprises:using maleic anhydride (MAH) and dimethylethanolamine (DMEA) as raw materials to synthesize the reducing agent monomer: 4-(2-(dimethylamino)ethoxy)-4-oxobut-2-enoic acid; anda preparation method of the styrene-acrylic emulsion comprises:{'sub': '2', 'adding a pH regulator, an emulsifier, the reducing agent monomer, and a dispersion medium (HO) into a reaction flask, and stirring a resulting mixture for 3 min to 4 min to allow thorough dissolution;'}adding comonomers having styrene, butyl acrylate (BA), and methylmethacrylate (MMA), and pre-emulsifying with ...

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Номер записи: 46

26-03-2020 дата публикации

DNP and DNP Prodrug Treatment of Neuromuscular, Neurodegenerative, Autoimmune, Developmental, Traumatic Brain Injury, Concussion, Dry Eye Disease, Hearing Loss and/or Metabolic Diseases

Номер: US20200093831A1

Автор: Albayati Zaineb, ALONSO Robert, Crooks Peter Anthony, Geisler John Gerard, Penthala Narsimha Reddy

Принадлежит:

A composition and method of treatment of neuromuscular, neuromuscular degenerative, neurodegenerative, autoimmune, developmental, traumatic, hearing loss related, and/or metabolic diseases, including spinal muscular atrophy (SMA) syndrome (SMA1, SMA2, SMA3, and SMA4, also called Type I, II, III and IV), traumatic brain injury (TBI), concussion, keratoconjunctivitis sicca (Dry Eye Disease), glaucoma, Sjogren's syndrome, rheumatoid arthritis, post-LASIK surgery, anti-depressants use, Wolfram Syndrome, and Wolcott-Rallison syndrome. The composition is selected from the group consisting of 2,3-DNP, 2,4-DNP, 2,5-DNP, 2,6-DNP, 3,4-DNP, or 3,5-DNP, bipartite 2,3-dinitrophenol, 2,4-dinitrophenol, 2,5-dinitrophenol, 2,6-dinitrophenol, 3,4-dinitrophenol, or 3,5-dinitrophenol (2,3-DNP, 2,4-DNP, 2,5-DNP, 2,6-DNP, 3,4-DNP, or 3,5-DNP) prodrugs; Gemini prodrugs, bioprecursor molecules, and combinations thereof. A dose of the composition for treatment of neurodegenerative diseases may be from about 0.01 mg/kg of body weight to about 50 mg/kg of body weight of the patient in need of treatment. A dose of the composition for treatment of metabolic diseases may be from about 1 mg/70 kg of body weight to about 100 mg/70 kg of body weight of the patient in need of treatment, and a maximum dose per day is about 200 mg/70 kg of body weight of the patient in need of treatment. 146-. (canceled)48. The composition of claim 47 , wherein the prodrug is stable at a pH of 1-2.49. The composition of claim 47 , wherein the prodrug is stable at a pH of 4.5.50. The composition of claim 47 , wherein the prodrug is stable at a pH of 5-9.51. A depot nanoparticle formulation comprising the composition of .52. A method of treatment of neuromuscular diseases claim 47 , neuromuscular degenerative diseases claim 47 , muscle wasting diseases claim 47 , neurodegenerative diseases claim 47 , autoimmune diseases claim 47 , developmental diseases claim 47 , traumatic diseases of CNS claim 47 , hearing loss ...

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Номер записи: 47

23-04-2015 дата публикации

COMPOSITIONS AND METHODS FOR THE TREATMENT OF FIBROMYALGIA PAIN

Номер: US20150111966A1

Автор: Kandula Mahesh

Принадлежит:

The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of fibromyalgia pain may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of injury, post-operative pain, osteoarthritis, rheumatoid arthritis, multiple sclerosis, spinal cord injury, migraine, HIV related neuropathic pain, post herpetic neuralgia, diabetic neuropathy, bipolar depression, stress, cancer pain, and lower back pain. 2. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.3. The pharmaceutical composition of claim 2 , wherein said pharmaceutical composition is formulated to treat the underlying etiology with an effective amount administering the patient in need by oral administration claim 2 , delayed release or sustained release claim 2 , transmucosal claim 2 , syrup claim 2 , topical claim 2 , parenteral administration claim 2 , injection claim 2 , subdermal claim 2 , oral solution claim 2 , rectal administration claim 2 , buccal administration or transdermal administration.4. A method of treating fibromyalgia pain and pain as the underlying etiology claim 3 , the method comprising administering to a patient in need thereof an effective amount of .5. The method of claim 4 , wherein the fibromyalgia pain and pain as the underlying etiology is selected from injury claim 4 , post-operative pain claim 4 , osteoarthritis claim 4 , rheumatoid arthritis claim 4 , multiple sclerosis claim 4 , spinal cord injury claim 4 , migraine claim 4 , depression claim 4 , HIV related neuropathic pain claim 4 , post herpetic neuralgia claim 4 , diabetic neuropathy claim 4 , bipolar depression claim 4 , stress ...

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Номер записи: 48

04-05-2017 дата публикации

Novel lipids and lipid nanoparticle formulations for delivery of nucleic acids

Номер: US20170119904A1

Автор: Steven M. Ansell, Xinyao Du

Принадлежит: Acuitas Therapeutics Inc

Compounds are provided having the following structure: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R 1 , R 2 , R 3 , L 1 , L 2 , G 1 , G 2 and G 3 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.

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Номер записи: 49

25-08-2022 дата публикации

ITACONIC ACID DERIVATIVES AND USES THEREOF INTREATING AN INFLAMMATORY DISEASE OR A DISEASE ASSOCIATED WITH AN UNDESIRABLE IMMUNE RESPONSE

Номер: US20220265595A1

Автор: COOKE Michael Liam, Cousin David, Fyfe Matthew Colin Thor, Teobald Barry John, THOM Stephen Malcolm, WAUGH Thomas Michael

Принадлежит:

The invention relates to compounds of formula (IW-1) and to their use in treating or preventing an inflammatory disease or a disease associated with an undesirable immune response: wherein R, R, Rand Rare as defined herein. 26-. (canceled)824-. (canceled)25. The compound or pharmaceutically acceptable salt and/or solvate thereof according to claim 1 , wherein Ris Ccycloalkyl.2628-. (canceled)29. The compound or pharmaceutically acceptable salt and/or solvate thereof according to claim 25 , wherein Ris cyclobutyl.3033-. (canceled)34. The compound or pharmaceutically acceptable salt and/or solvate thereof according to claim 1 , wherein Ris 4-10 membered heterocyclyl.3551-. (canceled)52. The compound or pharmaceutically acceptable salt and/or solvate thereof according to claim 1 , wherein Ris substituted by Rand/or Rwhen Ris methyl claim 1 , Ccycloalkyl claim 1 , 4-7 membered heterocyclyl claim 1 , phenyl or 5-6 membered heteroaryl.5358-. (canceled)59. The compound or pharmaceutically acceptable salt and/or solvate thereof according to claim 52 , wherein Ris Chaloalkyl.6079-. (canceled)80. The compound or pharmaceutically acceptable salt and/or solvate thereof according to claim 1 , wherein Ris Calkyl.81179-. (canceled)181. (canceled)182. The compound according to which is a compound selected from the group consisting of:1-(2-cyanoethyl) 4-octyl 2-methylenesuccinate;1-(2-(methylsulfonyl)ethyl) 4-octyl 2-methylenesuccinate;4-octyl 1-(3,3,3-trifluoropropyl) 2-methylenesuccinate;4-octyl 1-(oxetan-3-yl) 2-methylenesuccinate;4-octyl 1-(2-(2-oxopyrrolidin-1-yl)ethyl) 2-methylenesuccinate;1-(3-(dimethylamino)-3-oxopropyl) 4-octyl 2-methylenesuccinate;4-butyl 1-(2-(methylsulfonyl)ethyl) 2-methylenesuccinate;1-(2-cyanoethyl) 4-butyl 2-methylenesuccinate;1-(2-(2,5-dioxopyrrolidin-1-yl)ethyl) 4-octyl 2-methylenesuccinate;1-(2-cyanoethyl) 4-methyl 2-methylenesuccinate;1-(2-cyanoethyl) 4-hexyl 2-methylenesuccinate;4-methyl 1-(2-(methylsulfonyl)ethyl) 2-methylenesuccinate;4-octyl 1 ...

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Номер записи: 50

27-05-2021 дата публикации

ESTERAMINE SALTS

Номер: US20210154117A1

Автор: Ebert Sophia, LUDOLPH Bjoern, MARCZEWSKI Dawid

Принадлежит:

The present invention relates to an esteramine salt according to the general formula (I): 2. The esteramine salt according to claim 1 , wherein{'sup': '1', 'sub': 4', '30, 'Ris C-C-alkyl,'}{'sup': '2', 'sub': 3', '12, 'Ris C-C-alkylene and'}{'sup': 3', '3, 'sub': 2', '30', '1', '30, 'Ris C-C-alkyl or at least monosubstituted aryl and the substituents are independently selected from C-C-alkyl under the proviso that Ris not para toluenyl.'}3. The esteramine salt according to claim 1 , wherein{'sup': '1', 'sub': 6', '21, 'Ris C-C-alkyl,'}{'sup': '2', 'sub': 3', '6, 'Ris C-C-alkylene and'}{'sup': 3', '3, 'sub': 6', '18', '1', '30, 'Ris C-C-alkyl or at least monosubstituted phenyl and the substituents are independently selected from C-C-alkyl under the proviso that Ris not para toluenyl.'}4. The esteramine salt according to claim 1 , wherein{'sup': '1', 'i) Ris a mixture of at least two individual substituents and/or'}{'sup': '1', 'sub': 4', '30', '4', '30, 'ii) Ris unsubstituted straight-chain or branched C-C-alkyl or C-C-alkenyl.'}5. The esteramine salt according to claim 1 , wherein{'sup': '3', 'sub': 8', '16, 'i) Ris monosubstituted phenyl and the substituent is in para position and selected from C-C-alkyl, and/or'}{'sup': '3', 'ii) Ris a mixture of at least two individual substituents.'}6. The esteramine salt according to claim 1 , wherein{'sup': '2', 'sub': 2', '12, 'i) Ris straight-chain C-C-alkylene, or'}{'sup': 2', '7', '9', '11', '5', '7, 'sub': 2', 'm', '2', 'o', '2', '3', '2', '2', 'p', '2', '2', 'r, 'claim-text': [{'sup': 5', '7', '9', '11, 'R, R, Rand Rare independently of each other selected from H or methyl,'}, 'm is an integer from 1 to 10,', 'n is an integer from 2 to 6,', 'o is an integer from 0 to 5,', 'p is an integer from 1 to 3,', 'is an integer from 1 to 3., 'ii) Ris —(CH—CHR—O)—CH—CHR—, —(CHR)—CHR—CHR—O—(CH)— or —(CH—CH)—O—(CH—CH)—,'}7. A process for preparing an esteramine salt according to claim 1 ,wherein a monocarboxylic acid or an ester ...

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Номер записи: 51

23-04-2020 дата публикации

Lipid nanoparticle formulations

Номер: US20200121809A1

Автор: Barbara Mui, Christopher J. BARBOSA, Jia Ching Paulo Lin, Michael J. Hope, Steven M. Ansell, Thomas D. Madden, Xinyao Du

Принадлежит: Individual

Improved formulations of lipid nanoparticles are provided. Use of the lipid nanoparticles for delivery of a therapeutic agent and methods for their preparation are also provided.

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Номер записи: 52

03-06-2021 дата публикации

Novel lipids and compositions for the delivery of therapeutics

Номер: US20210162053A1

Автор: David Butler, Jayaprakash K. Nair, Kallanthottathil G. Rajeev, Laxman Eltepu, Martin Maier, Muthiah Manoharan, Muthusamy Jayaraman

Принадлежит: Arbutus Biopharma Corp

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure (I) wherein R1 and R2 are each independently for each occurrence optionally substituted C10-C30 alkyl, optionally substituted C10-C30 alkenyl, optionally substituted C10-C30 alkynyl, optionally substituted C10-C30 acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10 alkyl, optionally substituted C2-C10 alkenyl, optionally substituted C2-C10 alkynyl, alkylheterocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; E is O, S, N(Q), C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O)2N(Q), S(O)2, N(Q)S(O)2, SS, O═N, aryl, heteroaryl, cyclic or heterocycle; and, Q is H, alkyl, ω-aminoalkyl, ω-(substituted)aminoalkyl, ω-phosphoalkyl or ω-thiophosphoalkyl.

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Номер записи: 53

21-05-2015 дата публикации

COMPOSITIONS AND METHODS FOR THE TREATMENT OF NEUROLOGICAL DISEASES

Номер: US20150141500A1

Автор: Kandula Mahesh

Принадлежит:

The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of depressive disorders, anxiety disorders, attention deficit hyperactivity disorder, migraine prophylaxis, eating disorders, bipolar disorder, post-herpetic neuralgia, insomnia, ankylosing spondylitis, recurring biliary dyskinesia, nocturnal enuresis, cyclic vomiting syndrome, post-traumatic stress disorder (PTSD) and neuropathy. 2. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.3. The pharmaceutical composition of claim 2 , wherein said pharmaceutical composition is formulated to treat the underlying etiology with an effective amount administering the patient in need by oral administration claim 2 , delayed release or sustained release claim 2 , transmucosal claim 2 , syrup claim 2 , topical claim 2 , parenteral administration claim 2 , injection claim 2 , subdermal claim 2 , oral solution claim 2 , rectal administration claim 2 , buccal administration or transdermal administration.4. A method of treating neurological diseases as the underlying etiology claim 3 , the method comprising administering to a patient in need thereof an effective amount of .5. The method of claim 4 , wherein the neurological disease as the underlying etiology is selected from depressive disorders claim 4 , anxiety disorders claim 4 , attention deficit hyperactivity disorder claim 4 , migraine prophylaxis claim 4 , eating disorders claim 4 , bipolar disorder claim 4 , post-herpetic neuralgia claim 4 , insomnia claim 4 , ankylosing spondylitis ...

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Номер записи: 54

09-05-2019 дата публикации

N,N-DIMETHYLAMINOETHYL ACRYLATE COMPOSITION STABILIZED IN RESPECT OF DISCOLORING EFFECTS

Номер: US20190135731A1

Автор: DUBUT Fanny, MAGET Sandra, RIFLADE Benoit

Принадлежит:

The invention relates to the use of 2,6,-di-tert-butyl-4-methylphenol at a moiety of 25 to 200 ppm for stabilizing N,N-dimethylaminoethyl acrylate in respect of discoloring effects. The invention also relates to an N,N-dimethylaminoethyl acrylate stabilized in said manner and to a method for producing the same. 1. A composition of N ,N-dimethylaminoethyl acrylate that is stabilized with respect to coloration , comprising from 25 to 200 ppm of 2 ,6-di-tert-butyl-4-methylphenol.2. The composition as claimed in having a coloration of less than 100 Apha.3. The composition as claimed in further comprising at least one polymerization inhibitor claim 1 , selected from the group consisting of hydroquinone claim 1 , hydroquinone methyl ether (MEHQ) and mixtures thereof.4. A process for the continuous production of a composition of N claim 1 ,N-dimethylaminoethyl acrylate that is stabilized with respect to coloration claim 1 , according to claim 1 , said process comprising the steps of transesterifying a light acrylate selected from the group consisting methyl acrylate and ethyl acrylate claim 1 , with dimethylaminoethanol in the presence of a catalyst claim 1 , followed by a treatment for purifying a reaction mixture comprising a final distillation of purified N claim 1 ,N-dimethylaminoethyl acrylate claim 1 , wherein 25 to 200 ppm of 2 claim 1 ,6-di-tert-butyl-4-methylphenol are introduced at an outlet of the distilled gaseous stream of purified N claim 1 ,N-dimethylaminoethyl acrylate claim 1 , before condensation of final product.5. The process of claim 4 , comprising the following steps:a) transesterifying a light acrylate selected from the group consisting methyl acrylate and ethyl acrylate, with dimethylaminoethanol in the presence of a transesterification catalyst and at least one polymerization inhibitor, a corresponding azeotropic mixture of light acrylate/light alcohol being drawn off continuously during the reaction; at the top, a stream composed essentially of N, ...

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Номер записи: 55

04-06-2015 дата публикации

Pharmaceutically Acceptable Salts of Fatty Acids

Номер: US20150152034A1

Автор: Coughlan David, Downes Bill, Manku Mehar

Принадлежит:

The present disclosure provides pharmaceutically acceptable stable salt forms of 15-lipoxygenase products, such as 15-HETrE lysine salt, compositions comprising same and methods of making and using same. 1. A salt of a 15-lipoxygenase product.2. The salt of claim 1 , wherein the salt is a pharmaceutically acceptable salt.3. The salt of claim 1 , wherein the salt comprises a lysine salt of the 15-lipoxygenase product.4. The salt of claim 1 , wherein the salt comprises a sodium salt of the 15-lipoxygenase product.5. The salt of claim 1 , wherein the salt comprises an ornithine salt of the 15-lipoxygenase product.6. The salt of claim 1 , wherein the salt comprises a piperazine salt of the 15-lipoxygenase product.7. The salt of claim 1 , wherein the salt comprises a meglumine salt of the 15-lipoxygenase product.8. The salt of further comprising the 15-lipoxygenase product in free acid form.9. The salt of claim 1 , wherein the salt is selected from the group consisting of: sodium claim 1 , lysine claim 1 , ornithine claim 1 , piperazine claim 1 , meglumine claim 1 , and combinations thereof.10. The salt of claim 1 , wherein the 15-lipoxygenase product is selected from the group consisting of: 13-HODE claim 1 , 15-HETrE claim 1 , 15-OHEPA claim 1 , 15-HETE claim 1 , and combinations thereof.11. 15-Hydroxy-5 claim 1 ,8 claim 1 ,11 claim 1 ,13-eicosatetraenoic acid lysine salt.12. A pharmaceutical composition comprising a salt form of a 15-lipoxygenase product.13. The pharmaceutical composition of further comprising an excipient.14. The pharmaceutical composition of claim 12 , wherein after storage for at least about 4 weeks claim 12 , the pharmaceutical composition comprises at least about 98% claim 12 , at least about 99% claim 12 , or about 100% of an initial amount of the salt form of the 15-lipoxygenase product.15. The pharmaceutical composition of claim 12 , wherein after storage for at least about 10 weeks or at least 24 weeks claim 12 , the pharmaceutical ...

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Номер записи: 56

02-06-2016 дата публикации

COMPOSITIONS AND METHODS FOR THE TREATMENT OF MULTIPLE SCLEROSIS

Номер: US20160152553A1

Автор: Kandula Mahesh

Принадлежит:

The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing multiple sclerosis may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of multiple sclerosis and psoriasis. 3. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.4. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.5. The pharmaceutical composition of claim 3 , wherein said pharmaceutical composition is formulated to treat the underlying etiology with an effective amount administering the patient in need by oral administration claim 3 , delayed release or sustained release claim 3 , transmucosal claim 3 , syrup claim 3 , topical claim 3 , parenteral administration claim 3 , injection claim 3 , subdermal claim 3 , oral solution claim 3 , rectal administration claim 3 , buccal administration or transdermal administration.6. The pharmaceutical composition of claim 4 , wherein said pharmaceutical composition is formulated to treat the underlying etiology with an effective amount administering the patient in need by oral administration claim 4 , delayed release or sustained release claim 4 , transmucosal claim 4 , syrup claim 4 , topical claim 4 , parenteral administration claim 4 , injection claim 4 , subdermal claim 4 , oral solution claim 4 , rectal administration claim 4 , buccal administration or transdermal administration.7. Compounds and compositions of claim 5 , wherein said compounds and compositions are formulated for the treatment of neurodegenerative diseases claim 5 , multiple sclerosis claim 5 , psoriasis and ...

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Номер записи: 57

08-06-2017 дата публикации

Fatty amides and derivatives from natural oil metathesis

Номер: US20170158617A1

Автор: Aaron Brown, Andrew D. Malec, Brian Holland, Brian Sook, Dave R. Allen, Dennis S. Murphy, Gary Luebke, Gregory Wallace, Irene Shapiro, Kelly Buchek, Laura Lee Whitlock, Lena Titievsky, Marcos Alonso, Michael R. Terry, Michael Wiester, Patrick Shane Wolfe, Patti Skelton, Randal J. Bernhardt, Renee Luka, Ronald A. Masters, Sangeeta Ganguly-Mink

Принадлежит: Stepan Co

Fatty amide compositions and their derivatives are disclosed. The fatty amides comprise a reaction product of a metathesis-derived C 10 -C 17 monounsaturated acid, octadecene-1,18-dioic acid, or their ester derivatives with a primary or secondary amine. Derivatives made by reducing, quaternizing, sulfonating, alkoxylating, sulfating, and sulfitating the fatty amide are also included. The amine reactant can be diethylenetriamine or (2-aminoethyl)ethanolamine, which provide imidazoline amides or esters, respectively. In one aspect, the ester derivative of the C 10 -C 17 monounsaturated acid or octadecene-1,18-dioic acid is a lower alkyl ester. In other aspects, the ester derivative is a modified triglyceride made by self-metathesis of a natural oil or an unsaturated triglyceride made by cross-metathesis of a natural oil with an olefin. The compositions are valuable for cleaners, fabric treatment, hair conditioning, personal care, antimicrobial compositions, agricultural uses, and oil field applications.

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Номер записи: 58

29-09-2022 дата публикации

Lipids for delivery of charged material, formulations thereof and method for making same

Номер: US20220304929A1

Автор: Joshua Zaifman, Marco A. Ciufolini, Sam Chen, Yuen Yi Tam

Принадлежит: Integrated Nanotherapeutics Inc, University of British Columbia

Disclosed herein is a lipid having a net charge at physiological pH, and being covalently attached to a lipid moiety. The lipid moiety comprises a hydrocarbon structure having two or more linked hydrocarbon chains, optionally having cis or trans C═C, at least one of said chains being covalently attached to the head group optionally via the linker region. The hydrocarbon chains are bonded to one another at a branch point at an internal carbon of the chain attached to the linker region, which branch point comprises a functional group having an electronegative atom. The hydrocarbon chains each have between 1 and 40 carbon atoms, wherein the hydrocarbon structure in total comprises between 10 and 150 carbon atoms. Advantageously, the hydrocarbon structure may assume a generally flared shape for enhanced delivery of cargo molecules. Further provided are delivery vehicles comprising the lipids.

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Номер записи: 59

29-09-2022 дата публикации

NEW QUATERNARY AMMONIUM COMPOUNDS

Номер: US20220306570A1

Автор: BACK Olivier, Mastroianni Sergio

Принадлежит:

The invention concerns new quaternary ammonium compounds with surfactant properties and improved biodegradability. 2. The compound in accordance with claim 1 , wherein the compound comprises one or two groups X and two and only two groups R.3. The compound in accordance with wherein n+n′ is 1.4. The compound in accordance with wherein n+n′ is 2.5. The compound in accordance with am claim 1 , wherein n′ is 1 and Y is a C-Caliphatic group.6. The compound in accordance with claim 1 , wherein A is represented by A-6 claim 1 , m claim 1 , m′ claim 1 , m″ and m′″ are 0 claim 1 , Zto Zare O and wherein the compound comprises two groups R and one group X.7. The compound in accordance with wherein n is 0 and n′ is 1.8. The compound in accordance with wherein n is 1.9. The compound in accordance with claim 1 , wherein A is represented by A-3 or A-4 claim 1 , m claim 1 , m′ claim 1 , m″ claim 1 , m′″ and k′″ are 0 and two of substituents Qto Qare represented by groups X with both X attached to the same carbon atom of linker A and two groups R attached to the same or to different carbon atoms of linker A.10. The compound in accordance with claim 1 , wherein A is represented by A-1 claim 1 , m and m′ are 1 claim 1 , m″ and m′″ are 0 claim 1 , k is 0 and two substituents Qto Qare represented by groups X with both groups X being attached to the —(CH)and —(CH)′— groups directly attached to the nitrogen atom of linker A.11. The compound in accordance with claim 1 , wherein A is represented by A-2 claim 1 , k′ is 0 claim 1 , k″ is 1 claim 1 , m is 1 claim 1 , m′ claim 1 , m″ and m′″ are 0 and two of substituents Qto Qare represented by groups X attached to two adjacent carbon atoms of linker A.12. The compound in accordance with claim 1 , wherein A is represented by A-5 claim 1 , m claim 1 , m′ claim 1 , m″ claim 1 , m′″ and k″″ are 0 claim 1 , two of substituents Qto Qare X with each carbon atom of linker A carrying one group X and one group R wherein X and R might be the same or ...

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Номер записи: 60

25-06-2015 дата публикации

P62-zz chemical inhibitor

Номер: US20150175607A1

Автор: Garson David Roodman, Kyaw-Zeyar Myint, Noriyoshi Kurihara, Xiang-qun XIE

Принадлежит: University of Pittsburgh

A method for treating a p62-mediated disease (e.g., multiple myeloma) in a subject, the method comprising administering to the subject a therapeutically effective amount of at least one p62-ZZ inhibitor compound.

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Номер записи: 61

18-09-2014 дата публикации

DYRK1 INHIBITORS AND USES THEREOF

Номер: US20140275064A1

Автор: Besson Thierry, Casagrande Anne-Sophie, Desire Laurent, Foucourt Alicia, Leblond Bertrand

Принадлежит: DIAXONHIT

The present invention relates to novel thiazolo[5,4-f]quinazoline compounds and methods that are useful in the amelioration, treatment or control of Down's syndrome or early Alzheimer's disease or in the amelioration, treatment or control of cancers, especially solid tumors. More specifically, the invention relates to DYRK1A and/or DYRK1B inhibitors and to methods for preparing such compounds. 113-. (canceled)15. The compound according to claim 14 , wherein:Y is a sulfur atom;A is NH;{'sub': 5', '6, 'A is NH and B is a NRRgroup;'}{'sub': '5', 'A is NH and B is a ORgroup;'}{'sub': '3', 'A is NH and B is a OCHgroup;'}{'sub': '2', 'A is O and B is NH;'}R6 is a hydrogen atom;R2 is a hydrogen atom;R3 is an unsubstituted alkyl group, an alkyl group substituted by an alkoxyl group, an alkyl group substituted by a cycloalkyl group, or an alkyl group substituted by an aryl or a heteroaryl group;R3 is an unsubstituted aryl group or an aryl group substituted by at least one group selected from halogen atoms and alkoxyl groups; orR4, R6 and R7 are hydrogen atoms.16. The compound according to claim 14 , wherein R3 is a substituted or unsubstituted aryl or heteroaryl group.17. The compound according to claim 14 , wherein:Y is a sulphur atom;A is NH;B is a OR5 group wherein R5 is an unsubstituted (C1-C8)alkyl group;R2, R4, R7 and R8 are hydrogen atoms; andR3 is an ethyl group substituted by a (C1-C4)alkoxy group or an aryl group substituted with one or two substituents selected from the group consisting of a (C1-C4)alkyl, a halogen atom and a (C1-C4)alkoxy group.18. The compound according to claim 14 , selected from the group consisting of:9-(3-Chloro-4-fluorophenylamino)-N-(2-morpholinoethyl)thiazolo[5,4-f]quinazoline-2-carboximidamide (compound 1);9-(3-Chloro-4-fluorophenylamino)-N-(2-(piperidin-1-yl)ethyl)thiazolo[5,4-f]quinazoline-2-carboximidamide (compound 2);9-(3-Chloro-4-fluorophenylamino)-N-(2-(pyrrolidin-1-yl)ethyl)thiazolo[5,4-f]quinazoline-2-carboximidamide (compound 3 ...

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Номер записи: 62

07-07-2016 дата публикации

BIS(PERFLUOROETHER CARBOXYLIC ACID ALKYL)AMINO ESTER AND METHOD FOR PRODUCING THE SAME

Номер: US20160194275A1

Автор: KOKIN Keisuke

Принадлежит:

A bis(perfluoroether carboxylic acid alkyl)amino ester represented by the general formula: {CFO[CF(CF)CFO]CF(CF)COO(CH)}NR, wherein R is a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, an aryl group, or an aralkyl group; preferably an alkyl group having 1 to 6 carbon atoms or an aryl group; n is an integer of 1 to 3; a is an integer of 0 to 20, preferably an integer of 1 to 6; and b is an integer of 1 to 12, preferably an integer of 1 to 4. The bis(perfluoroether carboxylic acid alkyl)amino ester having an amino group at the end of the ester group is produced by reacting a perfluoroether carboxylic acid fluoride compound of the formula: CFO[CF(CF)CFO]CF(CF)COF and a bis(hydroxyalkyl)amine compound of the formula: HO(CH)NR(CH)OH at a molar ratio of 2:1 in the presence of an alkali metal fluoride. 1: A bis(perfluoroether carboxylic acid alkyl)amino ester represented by the general formula:{'br': None, 'sub': n', '2n+1', '3', '2', 'a', '3', '2', 'b', '2, '{CF[CF(CF)CFO]CF(CF)COO(CH)}NR\u2003\u2003[I]'}wherein R is a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, or a phenyl group; n is an integer of 1 to 3; a is an integer of 0 to 20; and b is an integer of 1 to 12.2: A method for producing the bis(perfluoroether carboxylic acid alkyl)amino ester according to claim 1 , the method comprising reacting a perfluoroether carboxylic acid fluoride compound represented by the general formula:{'br': None, 'sub': n', '2n+1', '3', '2', 'a', '3, 'CFO[CF(CF)CFO]CF(CF)COF\u2003\u2003[II]'} {'br': None, 'sub': 2', 'b', '2', 'b, 'HO(CH)NR(CH)OH\u2003\u2003[III]'}, 'wherein n is an integer of 1 to 3, and a is an integer of 0 to 20; and a bis(hydroxyalkyl)amine compound represented by the general formulawherein R is a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, or a phenyl group; and b is an integer of 1 to 12; in the presence of an alkali metal fluoride.3: The method for producing the bis(perfluoroether carboxylic acid alkyl)amino ester according ...

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Номер записи: 63

07-07-2016 дата публикации

STEREOSELECTIVE SYNTHESIS OF DIOLS AND TRIOLS BY MANNICH REACTION AND THEIR USE IN THE SYNTHESIS OF CARFILZOMIB

Номер: US20160194354A1

Автор: HÖFERL-PRANTZ Kathrin, Wilhelm Thorsten

Принадлежит:

It is provided an improved process for preparing Carfilzomib, including novel compounds that can be used as intermediates in the process for preparing Carfilzomib. 3. The method according to claim 2 , wherein the compound of Formula 9 is converted into Carfilzomib by the steps ofg1.1) epoxide formation by base addition, andh1.1) oxidation of the secondary alcohol.4. The method according to claim 2 , further comprising the steps ofg1.2) oxidation of the secondary alcohol in the compound of Formula 9, andh1.2) epoxide formation by base addition.7. The method according to claim 6 , wherein the base is pyridine claim 6 , triethylamine or sodium/potassium tert-butanolate.8. The method according to claim 6 , wherein the compound of Formula 3 is 2 claim 6 ,2-Dimethyl-1 claim 6 ,3-dioxan-5-one or 1 claim 6 ,5-Dioxaspiro[5.5]undecan-3-one.9. The method according to claim 6 , wherein step a) is carried out with (L)-Alanine as catalyst.10. The method according to claim 6 , wherein step b) is carried out with a Grignard reagent.1217.-. (canceled)18. The method according to claim 3 , wherein the base is pyridine claim 3 , triethylamine or sodium/potassium tert-butanolate.19. The method according to claim 1 , wherein the compound of Formula 3 is 2 claim 1 ,2-Dimethyl-1 claim 1 ,3-dioxan-5-one or 1 claim 1 ,5-Dioxaspiro[5.5]undecan-3-one.20. The method according to claim 1 , wherein step a) is carried out with (L)-Alanine as catalyst.21. The method according to claim 1 , wherein step b) is carried out with a Grignard reagent. Carfilzomib is a tetrapeptide epoxy ketone and a selective proteasome inhibitor. It is an analog of epoxomicin.The US FDA approved it for relapsed and refractory multiple myeloma. It is marketed under the trade name Kyprolis®.The chemical name of Carfilzomib is (S)-4-Methyl-N—((S)-1-(((S)-4-methyl-1-((R)-2-methyloxiran-2-yl)-1-oxopentan-2-yl)amino)-1-oxo-3-phenylpropan-2-yl)-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamide, represented by the ...

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Номер записи: 64

16-07-2015 дата публикации

Use of cannabidiol prodrugs in topical and transdermal administration with microneedles

Номер: US20150197484A1

Автор: Audra Lynn Stinchcomb, Dana Carmel Hammell, Jeffery Lynn Howard, Miroslaw Jerzy Golinski, Stan Lee Banks

Принадлежит: Zynerba Pharmaceuticals Inc

Described herein are microneedle drug delivery systems comprising a pharmaceutical compositions comprising pharmaceutically active agents (e.g., cannabidiol and prodrugs of cannabidiol) and microneedle arrays suitable for local and systemic delivery of the active agent to a mammal. Also described herein are methods of using a microneedle transdermal or topical drug delivery systems comprising pharmaceutical compositions, comprising cannabidiol and prodrugs of cannabidiol, and microneedle arrays in the treatment disease, including pancreatitis and pancreatic cancer.

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Номер записи: 65

11-06-2020 дата публикации

Derivatives of sobetirome

Номер: US20200181103A1

Автор: Andrew PLACZEK, James Matthew MEINIG, Sky Ferrara, Tapasree BANERJI, Thomas S. Scanlan

Принадлежит: Oregon Health Science University

Ester derivatives of sobetirome with enhanced CNS distribution are disclosed.

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Номер записи: 66

20-07-2017 дата публикации

Method of Producing Epoxy Compound and Catalyst Composition for Epoxidation Reaction

Номер: US20170204077A1

Автор: Hosokawa Akemi, KUSAKA Haruhiko

Принадлежит: MITSUBISHI CHEMICAL CORPORATION

A method of producing an epoxy compound, which comprises reacting hydrogen peroxide with a compound having a carbon-carbon double bond, in the presence of at least one of a tungsten compound and a molybdenum compound; and an onium salt comprising 20 or more carbon atoms and one or more of substituents convertible to a functional group containing an active hydrogen or a salt thereof. 125-. (canceled)27: The onium salt according to claim 26 , which is represented by formula (8) claim 26 , formula (9) claim 26 , or formula (10).28: A catalyst composition claim 26 , comprising:a tungsten compound, a molybdenum compound, or both; and{'claim-ref': {'@idref': 'CLM-00026', 'claim 26'}, 'the onium salt according to .'}29: The catalyst composition according to claim 28 , further comprising a phosphoric acid claim 28 , a phosphonic acid claim 28 , or both claim 28 , which is different from the onium salt.31: The composition according to claim 30 , wherein said epoxy compound α is a compound represented by any one of the following formulae (13) claim 30 , (14) or (15):{'br': None, 'sup': '1', 'sub': 'm1', '(A)-(OG)\u2003\u2003(13)'}{'sup': '1', 'claim-text': {'br': None, 'sub': m2', 'n2', 'm2, 'sup': 21', '2', '22', '2', '21, '(GO)-(A)-[X-(A)]-X-(A)-(OG)\u2003\u2003(14)'}, 'wherein in formula (13), G represents a glycidyl group which is a 2,3-epoxypropanyl group, and said glycidyl group may be substituted with an alkyl group, a phenyl group or an alkoxycarbonyl group; Arepresents an m1-valent aromatic or aliphatic hydrocarbon group that may have a substituent; and m1 represents an integer of 1 or more; provided that a plurality of G contained in one molecule may be same or different;'}{'sup': 21', '22', '21', '22', '2', '22', '2', '21', '22', '2, 'claim-text': {'br': None, 'sup': 3', '3, 'sub': m3', 'n3, 'H-[(A(OG))-X]—H\u2003\u2003(15)'}, 'wherein in formula (14), G represents a glycidyl group, and said glycidyl group may be substituted with an alkyl group, a phenyl group or ...

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Номер записи: 67

28-07-2016 дата публикации

Novel lipids and compositions for the delivery of therapeutics

Номер: US20160213785A1

Автор: David Butler, Jayaprakash K. Narayanannair, Kallanthottathil G. Rajeev, Laxman Eltepu, Muthiah Manoharan, Muthusamy Jayaraman

Принадлежит: Tekmira Pharmaceuticals Corp

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures:

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Номер записи: 68

06-08-2015 дата публикации

Derivatives of Betulin

Номер: US20150218142A1

Автор: Hatcher Mark Andrew, JOHNS Brian Alvin, Martin Michael Tolar, Tabet Elie Amine, Tang Jun

Принадлежит: GlaxoSmithKline LLC

The present invention relates to compounds characterized by having a structure according to the following Formula I: 2. The compound of claim 1 , wherein Land Lare both [C(RR)].3. The compound of claim 1 , wherein Land Lare both —CH—.4. The compound of claim 1 , wherein each instance of q is independently 1 claim 1 , 2 claim 1 , or 3.5. The compound of claim 1 , wherein q is 1.6. The compound of claim 1 , wherein W is O.7. The compound of claim 1 , wherein W is a bond.8. The compound of claim 1 , wherein when W is a bond claim 1 , then Ris —H.9. The compound of claim 1 , wherein when W is O claim 1 , then Ris —H.10. The compound of claim 1 , wherein Qin the A group is absent and Qin the A group is —CH— and the Q in the Formula I structure is —C(═O)—.11. The compound of claim 1 , wherein Ris —H.12. The compound of claim 1 , wherein Ris —(CH)NRR.13. The compound of claim 1 , wherein Ris (dimethylamino)ethyl.14. The compound of claim 1 , wherein each instance of r is independently 0 claim 1 , 1 claim 1 , 2 claim 1 , or 3.15. The compound of claim 1 , wherein r is 2.17. The compound of claim 1 , wherein X is a monocyclic (C-C)aryl.18. The compound of claim 1 , wherein X is phenyl.19. The compound of claim 1 , wherein Ris —H.20. The compound of claim 1 , wherein each instance of m is independently 0 or 1.21. The compound of claim 1 , wherein m is 0.22. The compound of claim 1 , wherein m is 1.23. The compound of claim 1 , wherein n is 1.24. The compound of claim 1 , wherein Rand R are both —H.25. The compound of claim 1 , wherein Rand Rare both (C-C)alkyl.26. The compound of claim 1 , wherein Ris methyl.27. The compound of claim 1 , wherein Ris methyl.28. The compound of claim 1 , wherein Rand Rare both methyl.29. The compound of claim 1 , wherein Ris halo.30. The compound of claim 1 , wherein Ris selected from chloro claim 1 , bromo claim 1 , or fluoro.31. The compound of claim 1 , wherein Ris chloro.32. The compound of claim 1 , wherein Ris absent.33. The compound of ...

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Номер записи: 69

04-07-2019 дата публикации

PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES

Номер: US20190201367A1

Автор: Duncan Scott, Hencken Christopher P., Sanrame Carlos N., Wynn Thomas Andrew, Zeidan Tarek A.

Принадлежит:

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. 110-. (canceled)12. A pharmaceutical composition comprising the compound of claim 11 , or a pharmaceutically acceptable salt thereof.13. A method of treating multiple sclerosis in a subject in need thereof claim 11 , comprising administering to the subject a therapeutically effective amount of the compound of .14. A method of treating multiple sclerosis in a subject in need thereof claim 12 , comprising administering to the subject a therapeutically effective amount of a composition of . This application is a continuation of U.S. application Ser. No. 15/704,219, filed Sep. 14, 2017, which is a continuation of U.S. application Ser. No. 15/295,370, filed Oct. 17, 2016, now U.S. Pat. No. 9,775,823, issued Oct. 3, 2017, which is a continuation of U.S. application Ser. No. 14/212,745, filed Mar. 14, 2014, now U.S. Pat. No. 9,505,776, issued Nov. 29, 2016, which claims the benefit of U.S. Provisional Application No. 61/934,365, filed Jan. 31, 2014 and U.S. Provisional Application No. 61/782,445, filed Mar. 14, 2013, the contents of which are incorporated herein by reference in their entireties.The present invention relates to various prodrugs of monomethyl fumarate. In particular, the present invention relates to derivatives of monomethyl fumarate which offer improved properties relative to dimethyl fumarate. The invention also relates to methods of treating various diseases.Fumaric acid esters (FAEs) are approved in Germany for the treatment of psoriasis, are being evaluated in the United States for the treatment of psoriasis and multiple sclerosis, and have been proposed for use in treating a wide range of immunological, autoimmune, and inflammatory diseases and conditions.FAEs and other fumaric acid derivatives have been proposed for use in treating a wide-variety of diseases and conditions involving immunological, autoimmune, and/or inflammatory processes including ...

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Номер записи: 70

12-08-2021 дата публикации

Biological buffers with wide buffering ranges

Номер: US20210246344A1

Автор: Thomas Daly

Принадлежит: Individual

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range. Derivatives that result in polyamines that have the same pKa yield a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

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Номер записи: 71

27-08-2015 дата публикации

QUATERNARY FATTY ACID ESTERS AS CORROSION INHIBITORS

Номер: US20150240365A1

Автор: Monk Keith A.

Принадлежит: ECOLAB USA INC.

Corrosion inhibitor compositions, methods of inhibiting or reducing corrosion, and methods of manufacturing corrosion inhibitor compositions are disclosed herein. In certain methods, the corrosion inhibitor compositions may be added to an aqueous industrial system having at least one surface. The aqueous industrial system may be a water recirculating system, a cooling water system, a boiler water system, a pulp slurry, a papermaking process, a ceramic slurry, a mixed solid/liquid system, or an oil-field system. A method of manufacturing a corrosion inhibitor composition may include reacting an alkanolamine with a fatty acid to form a fatty acid ester reaction product and reacting the fatty acid ester reaction product with an alkyl halide or an acrylate. 2. The corrosion inhibitor composition of claim 1 , wherein the CHgroup of the general structure is selected from the group consisting of a linear alkyl group claim 1 , a branched alkyl group claim 1 , a cyclic alkyl group claim 1 , a saturated alkyl group claim 1 , and an unsaturated alkyl group.3. The corrosion inhibitor composition of claim 1 , wherein the CHgroup is selected from the group consisting of CH claim 1 , CH claim 1 , CH claim 1 , CH claim 1 , CH claim 1 , CH claim 1 , CH claim 1 , CH claim 1 , and CH.4. The corrosion inhibitor composition of claim 1 , wherein x is 12 claim 1 , 13 claim 1 , 14 claim 1 , 15 claim 1 , 16 claim 1 , 17 claim 1 , or 18.5. The corrosion inhibitor composition of claim 1 , wherein R is selected from the group consisting of ethyl claim 1 , n-butyl claim 1 , ethylacetate claim 1 , and propanediol.7. A method of inhibiting corrosion comprising adding an effective amount of a corrosion inhibitor composition comprising a hydrolysable functional group to an aqueous industrial system having at least one surface and inhibiting corrosion of the at least one surface.8. The method of claim 7 , wherein the effective amount is from about 1 ppm to about 200 ppm.9. The method of claim 7 , ...

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Номер записи: 72

17-08-2017 дата публикации

NON-IONIC AMPHIPHILES AND METHODS OF MAKING THE SAME

Номер: US20170233337A1

Автор: Stensrud Kenneth

Принадлежит:

Sugar-derived tetrol, non-ionic amphiphilic amine-esters are prepared facilely and efficaciously in a few steps. The process is initiated by the esterification of a sugar-derived tetrol with a fatty acid chloride, then, undergoing triflate esterification followed by nucleophilic displacement of the aforementioned hydrophilic amine. Each synthetic pathway is efficient and affords modest to high yields of target amphiphiles, which are valorized as practicable surfactant surrogates to petroleum incumbents. 2) The compound of claim 1 , where said carbon side chain is between 8 and 30 carbons.3) A method of making a compound of claim 1 , comprising contacting a reduced hexane polyol with a fatty acid chloride in the presence of a nucleophilic base under ambient conditions.4) The method of claim 3 , wherein the fatty acid chloride is C-C.5) The method of claim 3 , wherein the nucleophilic base is at least one of pyridine claim 3 , dimethylaminopyridine claim 3 , imidazole or a tertiary amine.6) The method of claim 3 , wherein the reduced hexane polyol is contacted with the fatty acid chloride at a temperature of from about 0° C. to about 50° C.7) The method of claim 3 , wherein the reduced hexane polyol is contacted with the fatty acid chloride at a temperature of about 25° C.9) The compound of claim 8 , wherein said carbon side chain is between 8 and 30 carbons.10) The compound of claim 8 , wherein the moiety of the sulfonated hexane ester is selected from the group consisting of p-toluenesulfonyl (tosyl) claim 8 , methanesulfonyl claim 8 , (mesyl) claim 8 , ethanesulfonate (esyl) claim 8 , benzenesulfonate (besyl) claim 8 , p-bromobenzenesulfonate (brosyl) claim 8 , and triflouromethanesulfonic anhydride (triflate).11) A method of making a compound of claim 8 , comprising contacting an esterified claim 8 , reduced hexane polyol with a sulfonating agent to form the sulfonate ester moiety.12) The method of claim 11 , wherein the sulfonating agent selected from the group ...

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Номер записи: 73

25-08-2016 дата публикации

Derivatives of sobetirome

Номер: US20160244418A1

Автор: Andrew PLACZEK, James Matthew MEINIG, Sky Ferrara, Tapasree BANERJI, Thomas S. Scanlan

Принадлежит: Oregon Health Science University

Ester derivatives of sobetirome with enhanced CNS distribution are disclosed.

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Номер записи: 74

01-08-2019 дата публикации

Carbondisulfide Derived Zwitterions

Номер: US20190233372A1

Автор: Thomas Daly

Принадлежит: Thomas Daly

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

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Номер записи: 75

23-09-2021 дата публикации

Surfactants for agricultural products

Номер: US20210289776A1

Автор: Edward Asirvatham

Принадлежит: Advansix Resins and Chemicals LLC

Agricultural products, such as pesticides, plant growth regulators, fungicides, herbicides, and insecticides, may be formulated to include one or more surfactants, from one or more surfactant classes, such as derivatives of amino acids that have surface-active properties.

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Номер записи: 76

07-09-2017 дата публикации

COMPOUNDS AND COMPOSITIONS FOR TREATING HIV WITH DERIVATIVES OF BETULIN

Номер: US20170252356A1

Автор: JOHNS Brian Alvin

Принадлежит:

The present invention relates to compounds characterized by having a structure according to the following Formula I: 1128-. (canceled)134. The method according to claim 133 , wherein the administering is performed separately.135. The method according to claim 133 , wherein the administering is performed simultaneously.137. The method according to claim 136 , wherein the administering is performed separately.138. The method according to claim 136 , wherein the administering is performed simultaneously.140. The method according to claim 139 , wherein the administering is performed separately.141. The method according to claim 139 , wherein the administering is performed simultaneously.143. The method according to claim 142 , wherein the administering is performed separately.144. The method according to claim 142 , wherein the administering is performed simultaneously. This is a Continuation application of U.S. application Ser. No. 14/461,731 filed 18 Aug. 2014, now abandoned, which is a Continuation application of U.S. patent application Ser. No. 13/714,627, now granted U.S. Pat. No. 9,102,685, which claims priority to US Provisonal Application No. 61/576,448 filed 16 Dec. 2011, which is hereby incorporated by reference in its entirety.The present invention relates to compounds, pharmaceutical compositions, and methods of use thereof for (i) inhibiting HIV replication in a subject infected with HIV, or (ii) treating a subject infected with HIV, by administering such compounds.Human immunodeficiency virus type 1 (HIV-1) leads to the contraction of acquired immune deficiency disease (AIDS). The number of cases of HIV continues to rise, and currently over twenty-five million individuals worldwide suffer from the virus. Presently, long-term suppression of viral replication with antiretroviral drugs is the only option for treating HIV-1 infection. Indeed, the U.S. Food and Drug Administration has approved twenty-five drugs over six different inhibitor classes, which have ...

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Номер записи: 77

14-09-2017 дата публикации

Biological Buffers with Wide Buffering Ranges

Номер: US20170260435A1

Автор: Thomas P. Daly

Принадлежит: Individual

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

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Номер записи: 78

04-12-2014 дата публикации

Derivatives of Betulin

Номер: US20140357643A1

Автор: Brian Alvin Johns

Принадлежит: GlaxoSmithKline LLC

The present invention relates to compounds characterized by having a structure according to the following Formula I: , or a pharmaceutically acceptable salt thereof. Compounds of the present invention are useful for the treatment or prevention of HIV.

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Номер записи: 79

28-09-2017 дата публикации

Lipids and Lipid Compositions for the Delivery of Active Agents

Номер: US20170275243A1

Автор: BECKWITH Rohan Eric John, Brito Luis, DECHRISTOPHER Brian Addison, Gamber Gabriel Grant, Geall Andrew, ZABAWA Thomas

Принадлежит: NOVARTIS AG

This invention provides for a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R, R, Rand Rare defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues. 7. The compound claim 1 , or salt thereof claim 1 , according to claim 1 , wherein the compound is selected from the group consisting of:2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)benzyl 4-(dimethylamino)butanoate;((2-(((4-(dimethylamino)butanoyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-(((3-(dimethylamino)propanoyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-(((1-methylpiperidine-4-carbonyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-((((3-(dimethylamino)propoxy)carbonyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-((((3-(diethylamino)propoxy)carbonyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);3-(dimethylamino)propyl 4-methyl-2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)benzyl carbonate;4-methyl-2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)benzyl 4-(dimethylamino)butanoate;(9Z,9′Z,12Z,12′Z)-((2-(((4-(dimethylamino)butanoyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(butane-4,1-diyl) bis(octadeca-9,12-dienoate);4-(dimethylamino)butyl 4-methyl-2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)benzyl carbonate;((2-(((1-ethylpiperidine-4-carbonyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-(((1-isopropylpiperidine-4-carbonyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-((2-(1-methylpiperidin-4-yl)acetoxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);((2-(((4-(pyrrolidin-1-yl)butanoyl)oxy)methyl)-1,4-phenylene)bis(oxy))bis(octane-8,1-diyl) bis(decanoate);2,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)benzyl (3-(dimethylamino)propyl) carbonate;(9Z, ...

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Номер записи: 80

05-09-2019 дата публикации

NOVEL LIPIDS AND LIPID NANOPARTICLE FORMULATIONS FOR DELIVERY OF NUCLEIC ACIDS

Номер: US20190270697A1

Автор: Ansell Steven M., Du Xinyao

Принадлежит:

Compounds are provided having the following structure: 153-. (canceled)55. The compound of claim 54 , wherein Rand Rare each independently straight claim 54 , saturated alkyl chains containing from 12 to 16 carbon atoms.56. The compound of claim 54 , wherein Rand Rare each straight claim 54 , saturated alkyl chains containing 12 carbon atoms.57. The compound of claim 54 , wherein Rand Rare each straight claim 54 , saturated alkyl chains containing 14 carbon atoms.58. The compound of claim 54 , wherein Rand Rare each straight claim 54 , saturated alkyl chains containing 16 carbon atoms.59. The compound of claim 54 , wherein z ranges from 30 to 60.60. The compound of claim 54 , wherein z is 45.61. The compound of claim 54 , wherein z is selected such that an average molecular weight of (II) is about 2500 g/mol.63. The compound of claim 62 , wherein n is 45.66. The compound of claim 65 , wherein n is 45.69. The compound of claim 68 , wherein n is 45.71. A lipid nanoparticle comprising the compound of .72. The lipid nanoparticle of claim 71 , wherein Rand Rare each independently straight claim 71 , saturated alkyl chains containing from 12 to 16 carbon atoms.73. The lipid nanoparticle of claim 71 , wherein Rand Rare each straight claim 71 , saturated alkyl chains containing 12 carbon atoms.74. The lipid nanoparticle of claim 71 , wherein Rand Rare each straight claim 71 , saturated alkyl chains containing 14 carbon atoms.75. The lipid nanoparticle of claim 71 , wherein Rand Rare each straight claim 71 , saturated alkyl chains containing 16 carbon atoms.76. The lipid nanoparticle of claim 71 , wherein z ranges from 30 to 60.77. The lipid nanoparticle of claim 71 , wherein z is 45.78. The lipid nanoparticle of claim 71 , wherein z is selected such that an average molecular weight of (II) is about 2500 g/mol.80. The lipid nanoparticle of claim 79 , wherein n is 45.83. The lipid nanoparticle of claim 82 , wherein n is 45.86. The lipid nanoparticle of claim 85 , wherein n is ...

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Номер записи: 81

09-12-2021 дата публикации

Aminoalkyl (meth)acrylate stabilisation

Номер: US20210380523A1

Автор: Clement Bellini, Patrice Defer, Yves CABON

Принадлежит: Arkema France SA

The present invention relates to the use of a stabilizing composition comprising at least one N-oxyl compound and at least one polymerization inhibitor other than an N-oxyl compound, for inhibiting transesterification catalyst degradation in a process for the synthesis of aminoalkyl (meth)acrylates. Preferably, the transesterification catalyst is a titanium organometallic compound and the stabilising composition comprises at least one N-oxyl derivative and at least one polymerization inhibitor chosen from phenolic compounds and phenothiazine compounds in a weight ratio of between 1 and 10, preferably between 4 and 10, limits inclusive.

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Номер записи: 82

05-10-2017 дата публикации

Novel lipids and lipid nanoparticle formulations for delivery of nucleic acids

Номер: US20170283367A1

Автор: Steven M. Ansell, Xinyao Du

Принадлежит: Acuitas Therapeutics Inc

Compounds are provided having the following structure: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R 1a , R 1b , R 2a , R 2b , R 3a , R 3b , R 4a , R 4b , R 5 , R 6 , R 7 , R 8 , R 9 , L 1 , L 2 , 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.

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Номер записи: 83

22-10-2015 дата публикации

PRODRUGS OF MONOMETHYL FUMARATE (MMF)

Номер: US20150299103A1

Автор: Albrecht Wolfgang, GUSERLE Richard, MAIER Annemarie, RABE Sebastian, SELIG Roland

Принадлежит:

The present invention relates to novel compounds for use as a medicament. In particular, the present invention relates to novel prodrugs of monomethyl fumarate (MMF) suitable as a medicament, preferably in the treatment and/or prevention of systemic diseases, autoimmune diseases, inflammatory diseases, for example multiple sclerosis and psoriasis. 2. Compound according to claim 1 , wherein L in Formula (I) is a linear alkanediyl group.4. Compound according to or claim 1 , wherein Rin Formula (I) is alkyl with 1 to 6 carbon atoms or cyclic alkyl with 3 to 6 carbon atoms.7. Compound according to claim 1 , wherein Rand Rin Formula (IV) are independently hydrogen claim 1 , alkyl with 1 to 6 carbon atoms or cyclic alkyl with 3 to 6 carbon atoms.8. Compound according to or claim 1 , wherein Rand Rare independently hydrogen or methyl.9. Compound according to any one of claim 1 , or claim 1 , wherein c and d are independently 0 or 1.109. Compound according to any one of claim 1 , to claim 1 , wherein Rand Rindependently are hydrogen or alkyl with 1 to 6 carbon atoms.12. Compound according to claim 1 , wherein R claim 1 , R claim 1 , Rand Rin Formula (V) independently are hydrogen claim 1 , alkyl with 1 to 6 carbon atoms or cyclic alkyl with 3 to 6 carbon atoms claim 1 , and Ris hydrogen claim 1 , cyclic alkyl with 3 to 6 carbon atoms or alkyl with 1 to 6 carbon atoms wherein alkyl with 1 to 6 carbon atoms can be substituted preferably with one or more of the following group: amino claim 1 , NH—C(NH)NH claim 1 , carboxamide claim 1 , carboxylic acid claim 1 , hydroxy claim 1 , imidazole claim 1 , indole claim 1 , mercapto claim 1 , methylthio claim 1 , phenyl claim 1 , hydroxyphenyl claim 1 , and wherein one of Rand Rtogether with Roptionally belong to a 5 or 6-membered heteroaliphatic ring.13. Compound according to or claim 1 , wherein Rand Rare hydrogen14. Compound according to any one of claim 1 , or claim 1 , wherein Rand Rare independently hydrogen or methyl.1514. ...

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Номер записи: 84

11-10-2018 дата публикации

Lipids and Lipid Compositions for the Delivery of Active Agents

Номер: US20180290965A1

Автор: Andrew Geall, Delai Chen, Frédéric ZECRI, Gabriel Grant GAMBER, Kevin Love, Luis Brito, Thomas ZABAWA

Принадлежит: NOVARTIS AG

This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R 1 -R 4 , L 1 , n and p are defined herein. The compounds of formula (X) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

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Номер записи: 85

20-10-2016 дата публикации

CATIONIC LIPID

Номер: US20160304487A1

Автор: Era Tomohiro, Kuboyama Takeshi, Naoi Tomoyuki

Принадлежит:

The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) 127-. (canceled)29. The cationic lipid according to claim 28 , wherein Land Lare —O— or —O—CO— claim 28 , and Rand Rare dodecyl claim 28 , tetradecyl claim 28 , hexadecyl claim 28 , octadecyl claim 28 , icosyl claim 28 , docosyl claim 28 , tetracosyl claim 28 , (Z)-tetradec-9-enyl claim 28 , (Z)-hexadec-9-enyl claim 28 , (Z)-octadec-6-enyl claim 28 , (Z)-octadec-9-enyl claim 28 , (E)-octadec-9-enyl claim 28 , (Z)-octadec-11-enyl claim 28 , (9Z claim 28 ,12Z)-octadec-9 claim 28 ,12-dienyl claim 28 , (9Z claim 28 ,12Z claim 28 ,15Z)-octadec-9 claim 28 ,12 claim 28 ,15-trienyl claim 28 , (Z)-icos-11-enyl claim 28 , (11Z claim 28 ,14Z)-icos-11 claim 28 ,14-dienyl claim 28 , 3 claim 28 ,7 claim 28 ,11-trimethyldodeca-2 claim 28 ,6 claim 28 ,10-trienyl or 3 claim 28 ,7 claim 28 ,11 claim 28 ,15-tetramethylhexadec-2-enyl.30. The cationic lipid according to claim 28 , wherein Land Lare —CO—O— claim 28 , and Rand Rare tridecyl claim 28 , pentadecyl claim 28 , heptadecyl claim 28 , nonadecyl claim 28 , heneicosyl claim 28 , tricosyl claim 28 , (Z)-tridec-8-enyl claim 28 , (Z)-pentadec-8-enyl claim 28 , (Z)-heptadec-5-enyl claim 28 , (Z)-heptadec-8-enyl claim 28 , (E)-heptadec-8-enyl claim 28 , (Z)-heptadec-10-enyl claim 28 , (8Z claim 28 ,11Z)-heptadec-8 claim 28 ,11-dienyl claim 28 , (8Z claim 28 ,11Z claim 28 ,14Z)-octadec-8 claim 28 ,11 claim 28 ,14-trienyl claim 28 , (Z)-nonadec-10-enyl claim 28 , (10Z claim 28 ,13 Z)-nonadec-10 claim 28 ,13-dienyl claim 28 , (11Z claim 28 ,14Z)-icos-11 claim 28 ,14-dienyl claim 28 , 2 claim 28 ,6 claim 28 ,10-trimethylundec-1 claim 28 ,5 claim 28 ,9-trienyl or 2 claim 28 ,6 claim 28 ,10 claim 28 ,14-tetramethylpentadec-1-enyl.31. The cationic lipid according to any one of to claim 28 , wherein a and b are both 0 or 1.32. The cationic lipid according to any one of or claim 28 , wherein Lis a single bond ...

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Номер записи: 86

18-10-2018 дата публикации

IONIC OLIGOMER AND POLYMERIZABLE COMPOSITION CONTAINING SAME FOR TEMPORARY-USE WATER-FRAGMENTABLE MATERIALS

Номер: US20180298217A1

Автор: Beaudrais Sylvain, DUQUENNE Christophe, MONNIER Guillaume

Принадлежит:

An oligomer bearing at least one crosslinkable ethylenic unsaturation and at least one ionic bond, comprises in its structure at least one aminoacrylate group and at least one tertiary amine in a form salified with at least one carboxylic acid. Also described are a process for preparing a solution of the oligomer in a reactive diluent, a crosslinkable composition comprising the oligomer, the use thereof as binder in crosslinkable compositions for temporary-use water-removable materials in coatings, hydrogels and 3D object printing, and the crosslinked material which results from polymerizing the oligomer. As a temporary-use material, the cured oligomer can be easily removed after a temporary function, by simple cleaning with water and optionally at a suitable temperature greater than the glass transition temperature of the crosslinked product. 1. A polymerizable , oligomer bearing at least one ethylenic unsaturation and at least one ammonium carboxylate ionic bond and comprising in its structure or in its composition:{'sub': '2', 'P) at least one precursor oligomer bearing at least one tertiary amine function in the form of an aminoacrylate group resulting from the addition of A) at least one amine compound according to A1) bearing at least one primary amine function (—NH) and/or secondary amine function (—NH) and optionally at least one tertiary amine function and/or according to A2) bearing at least one secondary amine function (—NH) and optionally at least one tertiary amine function, on B) at least one hydrophilic acrylate compound with as a result the formation of said at least one aminoacrylate group, and'}C) at least one carboxylic acid compound attached to said precursor oligomer P by at least one ammonium carboxylate ionic bond with at least one of said aminoacrylate groups and optionally at feast one of said tertiary amine functions of said amine compound A).3. The oligomer of claim 2 , wherein said hydrophilic acrylate compound B) is a mixture of ...

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Номер записи: 87

17-09-2020 дата публикации

STORAGE-STABLE ENZYME PREPARATIONS, THEIR PRODUCTION AND USE

Номер: US20200291334A1

Автор: HUEFFER Stephan, KELLERMEIER Matthias, Marcos Alejandra Garcia, Spangenberg Oliver, WOLWERTZ Susanne

Принадлежит:

Described herein is a liquid enzyme preparation containing

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Номер записи: 88

03-11-2016 дата публикации

Lipids and Lipid Compositions for the Delivery of Active Agents

Номер: US20160317458A1

Автор: Brito Luis, Chen Delai, Gamber Gabriel Grant, Geall Andrew, Love Kevin, ZABAWA Thomas, ZECRI Frederic

Принадлежит:

This invention provides for a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R-R, n, p, Land Lare defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues. 12. The compound claim 1 , or salt thereof claim 1 , according to claim 1 , wherein the compound is selected from:2-(10-dodecyl-3-ethyl-8,14-dioxo-7,9,13-trioxa-3-azaoctadecan-18-yl)propane-1,3-diyl dioctanoate;2-(9-dodecyl-2-methyl-7,13-dioxo-6,8,12-trioxa-2-azaheptadecan-17-yl)propane-1,3-diyl dioctanoate;2-(9-dodecyl-2-methyl-7,13-dioxo-6,8,12-trioxa-2-azapentadecan-15-yl)propane-1,3-diyl dioctanoate;2-(10-dodecyl-3-ethyl-8,14-dioxo-7,9,13-trioxa-3-azahexadecan-16-yl)propane-1,3-diyl dioctanoate;2-(8-dodecyl-2-methyl-6,12-dioxo-5,7,11-trioxa-2-azaheptadecan-17-yl)propane-1,3-diyl dioctanoate;2-(10-dodecyl-3-ethyl-8,14-dioxo-7,9,13-trioxa-3-azanonadecan-19-yl)propane-1,3-diyl dioctanoate;2-(9-dodecyl-2-methyl-7,13-dioxo-6,8,12-trioxa-2-azaoctadecan-18-yl)propane-1,3-diyl dioctanoate;2-(8-dodecyl-2-methyl-6,12-dioxo-5,7,11-trioxa-2-azaoctadecan-18-yl)propane-1,3-diyl dioctanoate;2-(10-dodecyl-3-ethyl-8,14-dioxo-7,9,13-trioxa-3-azaicosan-20-yl)propane-1,3-diyl dioctanoate;2-(9-dodecyl-2-methyl-7,13-dioxo-6,8,12-trioxa-2-azanonadecan-19-yl)propane-1,3-diyl dioctanoate;3-(((3-(diethylamino)propoxy)carbonyl)oxy)pentadecyl 4,4-bis(octyloxy)butanoate;3-(((3-(diethylamino)propoxy)carbonyl)oxy)pentadecyl 4,4-bis((2-ethylhexyl)oxy)butanoate;3-(((3-(diethylamino)propoxy)carbonyl)oxy)pentadecyl 4,4-bis((2-propylpentyl)oxy)butanoate;3-(((3-(ethyl(methyl)amino)propoxy)carbonyl)oxy)pentadecyl 4,4-bis((2-propylpentyl)oxy)butanoate;3-(((3-(dimethylamino)propoxy)carbonyl)oxy)pentadecyl 4,4-bis((2-propylpentyl)oxy)butanoate;3-(((3-(diethylamino)propoxy)carbonyl)oxy)pentadecyl 6,6-bis(octyloxy)hexanoate;3-(((3-(diethylamino)propoxy)carbonyl)oxy)pentadecyl 6,6-bis(hexyloxy) ...

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Номер записи: 89

02-11-2017 дата публикации

Biological Buffers with Wide Buffering Ranges

Номер: US20170313920A1

Автор: Daly Thomas P.

Принадлежит:

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability. 2. The biological buffer and its salts of wherein A=D=—CH3 and m=1.3. The biological buffer and its salts of wherein A=D=—CH2OH and m=1.4. The biological buffer and its salts of wherein A=D-CH2O(CH2CH2CH2N)H and n=m=1.5. The biological buffer and its salts of wherein A=—CH2CH3 claim 1 , D=—CH2O(CH2CH2CH2N)H and n=m=1.6. The biological buffer and its salts of wherein A=—CH3 claim 1 , D=—CH2O(CH2CH2CH2N)H and n=m=1.7. The biological buffer and its salts of wherein A is —CH3 and D is —CH2CH3.9. The quaternary ammonium compound and its salts of wherein A=D=—CH3 claim 8 , E=—CH2OH claim 8 , R=R′=—CH3 and G=—H.10. The quaternary ammonium compound and its salts of wherein A=D=E=—CH2OH claim 8 , R=R′=—CH3 and G=—H.11. The quaternary ammonium compound and its salts of wherein A=D=—CH3 claim 8 , E=—CH2OH claim 8 , R=R′=—CH3 and G=—CH2CH3.12. The quaternary ammonium compound and its salts of wherein A=D=E=—CH2OH claim 8 , R=R′=—CH3 and G=—CH2CH3.14. The surfactant of wherein A is —H and D is —CH3.15. The surfactant of wherein A is —CH3 and D is chosen from —CH3 claim 13 , —CH2CH3 claim 13 , —CH2CH2CH3 claim 13 , —CH2OH.16. The surfactant of wherein A is —CH3 and D is chosen from —CH2CH2CH3 claim 13 , —CH2OH.17. The surfactant of wherein A is —CH3 and D is —CH2OH. This is a continuation of application Ser. No. 15/255,654 filed Sep. 2, 2016 and other previous parent applications claimed in the Application Data Sheet. application Ser. No. 15/255,654 is hereby incorporated by reference ...

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Номер записи: 90

10-11-2016 дата публикации

DERIVATIVES OF TARTARIC ACID

Номер: US20160326090A1

Автор: Albrecht Wolfgang, GUSERLE Richard, MAIER Annemarie, RABE Sebastian, SELIG Roland

Принадлежит: ratiopharm GmbH

The present invention relates to novel compounds, e.g. for use as a medicament. In particular, the present invention relates to novel medicaments, preferably in the treatment and/or prevention of systemic diseases, autoimmune diseases, and/or inflammatory diseases, for example multiple sclerosis and psoriasis. 2. Compound according to claim 1 , wherein Rand Rin Formula (I) are OR and OR wherein R and R′ can be independently hydrogen claim 1 , alkyl with 1 to 6 carbon atoms or cyclic alkyl with 3 to 6 carbon atoms.3. Compound according to claim 1 , wherein in Formula (I) Rand Rare OR and OR and wherein OR and OR are identical.4. Compound according to claim 1 , wherein Rand Rin Formula (I) are OR′ and OR and wherein R′ and R are hydrogen claim 1 , ethyl or isopropyl.6. Compound according to claim 1 , wherein Rand Rin Formula (I) are NRR and NRR claim 1 , wherein R claim 1 , R claim 1 , R and R independently are hydrogen claim 1 , alkyl with 1 to 6 carbon atoms or cyclic alkyl with 3 to 6 carbon atoms.7. Compound according to claim 6 , wherein one of R and R and one of R and R are hydrogen.8. Compound according to claim 1 , wherein Rand Rin Formula (I) together are NRforming a cyclic imide claim 1 , wherein Ris hydrogen or alkyl with 1 to 3 carbon atoms.9. Compound according to claim 1 , wherein Rand Rin Formula (II) are not both trans —(CH)—O—CO—CH═CH—COOCH.10. Compound according to claim 1 , wherein one of Rand Rin Formula (II) is trans —(CH)—O CO—CH═CH—COOCH.12. Compound according to claim 1 , wherein Rand Rin Formula (II) are each independently —(CH)—ORor —(CH)—CO—R claim 1 , whereinn′ and n″ are each independently 1, 2 or 3,{'sup': '5', 'Ris hydrogen,'}{'sup': 6', '7', '7', '8', '9', '8', '9, 'Ris ORwherein Ris hydrogen or alkyl with 1 to 4 carbon atoms, or NRR, wherein Rand Rare each independently hydrogen or alkyl with 1 to 4 carbon atoms.'}13. Compound according to claim 1 , wherein in Rand Rare each independently —(CH)—OR claim 1 , whereinn′ is independently 1 ...

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Номер записи: 91

19-11-2015 дата публикации

Carbondisulfide Derived Zwitterions

Номер: US20150329486A1

Автор: Daly Thomas P.

Принадлежит:

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

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Номер записи: 92

17-10-2019 дата публикации

NOVEL LIPIDS AND LIPID NANOPARTICLE FORMULATIONS FOR DELIVERY OF NUCLEIC ACIDS

Номер: US20190314524A1

Автор: Ansell Steven M., Du Xinyao

Принадлежит:

Compounds are provided having the following structure: 25-. (canceled)7. The compound of claim 6 , wherein n is an integer ranging from 2 to 12.8. The compound of claim 7 , wherein n is 3 claim 7 , 4 claim 7 , 5 or 6.9. The compound of claim 6 , wherein y and z are each independently an integer ranging from 2 to 10.10. The compound of claim 6 , wherein y and z are each independently an integer ranging from 4 to 9.1112-. (canceled)14. The compound of claim 13 , wherein a is an integer from 8 to 12.15. The compound of claim 13 , wherein at least one occurrence of Ris H.16. The compound of claim 13 , wherein Ris H at each occurrence.17. The compound of claim 13 , wherein at least one occurrence of Ris C-Calkyl.18. The compound of claim 17 , wherein C-Calkyl is methyl claim 17 , ethyl claim 17 , n-propyl claim 17 , iso-propyl claim 17 , n-butyl claim 17 , iso-butyl claim 17 , tert-butyl claim 17 , n-hexyl or n-octyl.20. The compound of claim 1 , wherein Ris OH.21. The compound of claim 1 , wherein Ris CN.22. The compound of claim 1 , wherein Ris —C(═O)OR claim 1 , —OC(═O)Ror —NHC(═O)R.23. The compound of claim 22 , wherein Ris methyl or ethyl.25. A composition comprising the compound of and a therapeutic agent.26. The composition of claim 25 , further comprising one or more excipient selected from neutral lipids claim 25 , steroids and polymer conjugated lipids.27. The composition of claim 26 , wherein the composition comprises one or more neutral lipids selected from DSPC claim 26 , DPPC claim 26 , DMPC claim 26 , DOPC claim 26 , POPC claim 26 , DOPE and SM.28. The composition of claim 27 , wherein the neutral lipid is DSPC.29. The composition of claim 25 , wherein the molar ratio of the compound to the neutral lipid ranges from about 2:1 to about 8:1.30. The composition of claim 26 , wherein the steroid is cholesterol.31. The composition of claim 30 , wherein the molar ratio of the compound to cholesterol ranges from 5:1 to 1:1.32. The composition of claim 26 , ...

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Номер записи: 93

03-12-2015 дата публикации

Cationic lipid

Номер: US20150343062A1

Автор: Takeshi Kuboyama, Tomohiro Era, Tomoyuki Naoi

Принадлежит: Kyowa Hakko Kirin Co Ltd

The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: R 1 and R 2 are, the same or different, alkenyl, etc, and X 1 and X 3 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X 3 is absent or is alkyl, etc, Y is absent or anion, a and b are, the same or different, 0 to 3, and L 3 is a single bond, etc, R 3 is alkyl, etc, L 1 and L 2 are —O—, —CO—O— or —O—CO—), a composition comprising the cationic lipid and a nucleic acid, and a method for introducing a nucleic acid into a cell by using the composition comprising the cationic lipid and the nucleic acid, and the like.

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Номер записи: 94

23-11-2017 дата публикации

Novel high penetration drugs and their compositions thereof for treatment of parkinson diseases

Номер: US20170334908A1

Автор: Chongxi Yu, Lina Xu

Принадлежит: Techfields Pharma Co Ltd

One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. The HPCs/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 HPCs/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.

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Номер записи: 95

22-10-2020 дата публикации

PROCESS FOR PREPARING DIMETHYLAMINOALKYL (METH)ACRYLATES

Номер: US20200331845A1

Автор: KRILL Steffen, Krüger Torsten, SCHÜTZ Thorben, Treskow Marcel

Принадлежит: EVONIK OPERATIONS GMBH

The present invention relates to a process for preparing dimethylaminoalkyl (meth)acrylates from alkyl (meth)acrylate and dimethylaminoalkanol. It likewise relates to the use of a catalyst system comprising a solution of a lithium alkoxide in alcohol in the preparation of a dimethylaminoalkyl (meth)acrylate. 115-. (canceled)16. A process for preparing dimethylaminoalkyl (meth)acrylate , comprising reacting a mixture comprising: (a) alkyl (meth)acrylate , (b) dimethylaminoalkanol and (c) a catalyst system comprising a solution of a lithium alkoxide in alcohol to produce said dimethylaminoalkyl (meth)acrylate , wherein the catalyst system contains no alkaline earth metal compounds.17. The process of claim 16 , wherein during the reaction claim 16 , additional amounts of (a) the alkyl (meth)acrylate claim 16 , (b) the dimethylaminoalkanol and claim 16 , optionally claim 16 , (c) the catalyst system are added to the reaction mixture and the dimethylaminoalkyl (meth)acrylate which forms is removed partly or completely from the reaction mixture.18. The process of claim 16 , wherein the dimethylaminoalkanol is selected from the group consisting of: 2-dimethylamino-1-ethanol claim 16 , 3-dimethylamino-1-propanol claim 16 , 4-dimethylamino-1-butanol claim 16 , 5-dimethylamino-1-pentanol claim 16 , 6-dimethylamino-1-hexanol claim 16 , 7-dimethylamino-1-heptanol claim 16 , and 8-dimethylamino-1-octanol.19. The process of claim 16 , wherein the alkyl (meth)acrylate is selected from the group consisting of: methyl (meth)acrylate claim 16 , ethyl(meth)acrylate claim 16 , propyl (meth)acrylate claim 16 , butyl (meth)acrylate claim 16 , pentyl (meth)acrylate claim 16 , hexyl (meth)acrylate claim 16 , heptyl (meth)acrylate claim 16 , and octyl (meth)acrylate.20. The process of claim 16 , wherein the dimethylaminoalkanol is 2-dimethylamino-1-ethanol and the alkyl (meth)acrylate is methyl methacrylate.21. The process of claim 16 , wherein the lithium alkoxide is selected from the ...

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Номер записи: 96

22-10-2020 дата публикации

Carbondisulfide Derived Zwitterions

Номер: US20200331853A1

Автор: Daly Thomas

Принадлежит:

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability. The present invention relates generally to the field of amines and more particularly to a classes of amino zwitterions.Amines are extremely useful compounds in the buffering of biological systems. Each class of amine has various limitations which require choosing an amine based on multiple factors to select the best amine. For example, pH buffering range is typically most important, but issues of chelation, pH range stability, and solubility also come into play. Typically, a suboptimal buffer will result in yields that are well below the potential yield. The present invention improves the yields in fermentation and purification, and improves shelf stability of proteins and amino acids.The present invention relates to amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form amine derivatives and polyamines and derivatives with differing pKa's extend the buffering range; derivatives that result in polyamines that have the same pKa yield a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability and reduced conductivity.Several drawings and illustrations have been presented to aid in understanding the invention. The scope of the present invention is not limited to what is shown in the figuresThe reaction of carbon disulfide ...

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Номер записи: 97

07-12-2017 дата публикации

DERIVATIVES OF BETULIN

Номер: US20170348324A1

Автор: Hatcher Mark Andrew, JOHNS Brian Alvin, Martin Michael Tolar, Tabet Elie Amine, Tang Jun

Принадлежит:

The present invention relates to compounds characterized by having a structure according to the following Formula I: 2. The compound of claim 1 , wherein Land Lare both [C(RR)].3. The compound of claim 1 , wherein Land Lare both —CH—.4. The compound of claim 1 , wherein each instance of q is independently 1 claim 1 , 2 claim 1 , or 3.5. The compound of claim 1 , wherein q is 1.6. The compound of claim 1 , wherein W is O.7. The compound of claim 1 , wherein W is a bond.8. The compound of claim 1 , wherein when W is a bond claim 1 , then Ris —H.9. The compound of claim 1 , wherein when W is O claim 1 , then Ris —H.10. The compound of claim 1 , wherein Qin the A group is absent and Q claim 1 , in the A group is —CH— and the Q in the Formula I structure is C(═O)11. The compound of claim 1 , wherein Ris —H.12. The compound of claim 1 , wherein Ris —(CH)NRR.13. The compound of claim 1 , wherein Ris (dimethylamino)ethyl.14. The compound of claim 1 , wherein each instance of r is independently 0 claim 1 , 1 claim 1 , 2 claim 1 , or 3.15. The compound of claim 1 , wherein r is 2.17. The compound of claim 1 , wherein X is a monocyclic (C-C)aryl.18. The compound of claim 1 , wherein X is phenyl.19. The compound of claim 1 , wherein Ris —H.20. The compound of claim 1 , wherein each instance of m is independently 0 or 1.21. The compound of claim 1 , wherein m is 0.22. The compound of claim 1 , wherein m is 1.23. The compound of claim 1 , wherein n is 1.24. The compound of claim 1 , wherein Rand R are both —H.25. The compound of claim 1 , wherein Rand Rare both (C-C)alkyl.26. The compound of claim 1 , wherein Ris methyl.27. The compound of claim 1 , wherein Ris methyl.28. The compound of claim 1 , wherein Rand Rare both methyl.29. The compound of claim 1 , wherein Ris halo.30. The compound of claim 1 , wherein Ris selected from chloro claim 1 , bromo claim 1 , or fluoro.31. The compound of claim 1 , wherein Ris chloro.32. The compound of claim claim 1 , wherein Ris absent.33. The ...

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Номер записи: 98

07-12-2017 дата публикации

CATIONIC LIPID

Номер: US20170349532A1

Автор: Era Tomohiro, Kuboyama Takeshi, Naoi Tomoyuki, Yagi Nobuhiro

Принадлежит: KYOWA HAKKO KIRIN CO., LTD.

The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) 128-. (canceled)30. The method according to claim 29 , wherein the cationic lipid forms a complex between a combination of the cationic lipid with a neutral lipid and/or a polymer and the nucleic acid.31. The method according to claim 29 , wherein the nucleic acid is a nucleic acid having an activity of suppressing the expression of the target gene by utilizing RNA interference (RNAi).32. The method according to claim 31 , wherein the target gene is a gene associated with tumor or inflammation.33. A method for introducing the nucleic acid into a cell by using the composition obtained by the method according to .34. The method according to claim 33 , wherein the cell is a cell at a tumor or inflammation site of a mammal.35. The method according to claim 33 , wherein the cell is a cell in the liver claim 33 , lungs claim 33 , kidneys or spleen of a mammal.36. The method according to claim 33 , wherein the method of the introduction into a cell is a method of introduction into a cell by intravenous administration.37. A method for treating cancer or inflammatory disease claim 32 , comprising a step of administering the composition obtained by the method according to .38. The method according to claim 37 , wherein the method of administration is intravenous administration.39. A medicament comprising the composition obtained by the method according to .40. The medicament according to claim 39 , which is for intravenous administration. The present invention relates to a novel cationic lipid that allows, for example, nucleic acid to be easily introduced into cells, and to a novel composition comprising the cationic lipid, and the like.Cationic lipids are amphiphilic molecules that generally contain a lipophilic region containing one or more hydrocarbon groups, and a hydrophilic region containing at least one positively charged polar head ...

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Номер записи: 99

14-12-2017 дата публикации

Low Molecular Weight Dry Powder Polymer for Use as Paper-Making Dry Strength Agent

Номер: US20170355846A1

Автор: Cheng Weiguo, Cramm Jeffrey, HUANG Heqing, Jordan David, Lowe Robert M., Wei Mingli

Принадлежит: ECOLAB USA INC.

The invention provides an associative polymer, a powder, and a process for making a powder comprising, networking one or more associative polymer(s) and one or more optional surfactant(s) to form a wet gel, and forming a powder from the wet gel, wherein the associative polymer(s) have a weight average molecular weight of from about 10 kDa to about 2,000 kDa. 1184-. (canceled)185. A powder comprisingone or more associative polymer(s) comprising one or more associative monomer unit(s) and one or more additional monomer unit(s) selected from at least one of a cationic monomer unit, an anionic monomer unit, a nonionic monomer unit, a zwitterionic monomer unit, or a combination thereof, and optionally one or more surfactant(s),wherein the associative polymer(s) have a weight average molecular weight of from about 10 kDa to about 2,000 kDa.186. The powder of claim 185 , wherein the one or more associative monomer unit(s) is derived from an acrylate monomer claim 185 , an acrylamide monomer claim 185 , or a combination thereof.187. The powder of claim 186 , wherein the one or more associative polymer(s) comprises a nonionic associative monomer unit.190. The powder of claim 189 , wherein the nonionic monomer unit is derived from lauryl polyethoxy (25) methacrylate claim 189 , cetyl polyethoxy (25) methacrylate claim 189 , stearyl polyethoxy (25) methacrylate claim 189 , behenyl polyethoxy (25) methacrylate claim 189 , or a combination thereof.193. The powder of claim 192 , wherein the organic group is a C-Calkyl group.194. The powder of claim 185 , wherein the additional monomer unit is derived from a monomer selected from 2-(dimethylamino)ethyl acrylate (“DMAEA”) claim 185 , 2-(dimethylamino)ethyl methacrylate (“DMAEM”) claim 185 , 3-(dimethylamino)propyl methacrylamide (“DMAPMA”) claim 185 , 3-(dimethylamino)propyl acrylamide (“DMAPA”) claim 185 , 3-methacrylamidopropyl-trimethyl-ammonium chloride (“MAPTAC”) claim 185 , 3-acrylamidopropyl-trimethyl-ammonium chloride (“ ...

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Номер записи: 100

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