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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 3497. Отображено 100.
29-03-2012 дата публикации

Cyclic olefin compound, photoreactive polymer, and alignment layer comprising the same

Номер: US20120076954A1
Принадлежит: LG Chem Ltd

Disclosed therein are a cyclic olefin compound, a photoreactive polymer, and an alignment layer comprising the photoreactive polymer, where the cyclic olefin compound can be used to provide the photoreactive polymer having not only excellences in liquid crystal alignment and alignment rate but also readiness for change in the alignment direction depending on the polarization direction.

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26-07-2012 дата публикации

Methods and compositions for heavy metal detoxification

Номер: US20120189721A1
Принадлежит: Metaproteomics Llc

Compositions and methods for enhancing heavy metal detoxification are described. The compositions and methods described provide enhanced activity of key detoxification systems including that the induction of phase II detoxification enzymes, such as glutathione S-transferases (GSTs), and NADPH quinone reductase (NQO1) activity.

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06-09-2012 дата публикации

Compounds, compositions and methods for the treatment of amyloid diseases and synucleinopathies such as alzheimer's disease, type 2 diabetes and parkinson's disease

Номер: US20120225890A1
Принадлежит: ProteoTech Inc

Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.

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25-10-2012 дата публикации

Composition, use, and preservation method

Номер: US20120269739A1
Принадлежит: LOreal SA

The invention relates to a cosmetic, pharmaceutical, dermatological, nutraceutical or oral cosmetic composition having, as main preserving system, a mild preserving system formed from compounds with a broad antimicrobial spectrum, which have only one pKa, the said pKa being greater than or equal to 10, the said mild preserving system being present in a content strictly greater than or equal to 1% by weight relative to the weight of the said composition. The invention also relates to the use, in a cosmetic, dermatological or pharmaceutical composition, of at least one compound of formula (I), as a preserving agent:

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25-04-2013 дата публикации

COMPOSITIONS AND METHODS FOR DETECTING AMYLOID-BETA-DEGRADING ENZYME ACTIVITY

Номер: US20130102498A1
Принадлежит: Academia Sinica

Novel substrates for detection of activity of amyloid beta degrading enzyme, such as Neprilysin (NEP) and insulin degrading enzyme (IDE), associated with Alzheimer's disease, are provided. A quenched fluorogenic peptide substrate containing the first seven residues of the Aβpeptide plus a C-terminal Cys residue to detect neprilysin activity with a fluorophore attached to the C-terminal Cys and a quencher linked to the N-terminus of the peptide is disclosed. An assay system sensitive to endopeptidase activity of NEP and IDE, but insensitive to other Aβ-degrading enzymes is disclosed. Active compounds are identified by a cell-based assay system for high-throughput screening. 1. A peptide substrate for detection of amyloid-β degrading enzyme activity , the substrate comprising:(a) a peptide of the sequence DAEFRHDC (SEQ ID NO: 1) comprising residues 1-7 of the amyloid-β peptide and a cysteine residue at the C-terminal end, or an analog or derivative thereof, wherein the peptide comprises a cleavage site for an amyloid-β degrading enzyme;(b) a quencher coupled to the N-terminal end of the peptide; and(c) a fluorophor coupled with the C-terminal end of the peptide.2. The substrate of claim 1 , wherein the amyloid-β degrading enzyme is selected from the group consisting of neprilysin (NEP) and insulin degrading enzyme (IDE).3. The substrate of claim 1 , wherein the fluorophore is selected from the group consisting of fluorescein claim 1 , fluorescein derivatives claim 1 , rhodamines claim 1 , tetramethylrhodamines claim 1 , coumarins claim 1 , resorufins claim 1 , pyrenes claim 1 , anthracenes claim 1 , phenylenes claim 1 , phthalocyanines claim 1 , cyanines claim 1 , xanthenes claim 1 , amidopyrylium dyes claim 1 , oxazines claim 1 , quadrain dyes claim 1 , carbopyronines claim 1 , NBD derivatives claim 1 , BODIPY fluorophores claim 1 , ALEXA fluorophores claim 1 , ALEXA-350 claim 1 , lanthanide chelates claim 1 , metalloporphyrins claim 1 , NIR fluorophores claim 1 , ...

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16-05-2013 дата публикации

VINYLOGOUS CHALCONE DERIVATIVES AND THEIR MEDICAL USE

Номер: US20130123367A1
Принадлежит: MEDIZINISCHE UNIVERSITAT WIEN

The present invention relates to vinylogous chalcone derivatives, in particular the compounds of formula (I) as described and defined herein, pharmaceutical compositions comprising these compounds, and their medical use, including their use in the treatment or prevention of cancer, in particular malignant hematological diseases/disorders. 2. The compound of claim 1 , wherein Ris selected from hydrogen claim 1 , halogen claim 1 , —NO claim 1 , —OH claim 1 , —O(Calkyl) claim 1 , —SH claim 1 , or —S(Calkyl) claim 1 , and Ris hydrogen.3. The compound of claim 1 , wherein Rand Rare mutually linked to form a group —CH═CH—.4. The compound of any of to claim 1 , wherein Ris hydrogen claim 1 , and Ris selected from hydrogen claim 1 , halogen claim 1 , —NO claim 1 , —OH claim 1 , —O(Calkyl) claim 1 , —SH claim 1 , or —S(Calkyl).5. The compound of any of to claim 1 , wherein Rand Rare mutually linked to form a group —CH— or —CH—CH—.6. The compound of any of to claim 1 , wherein Rand Rare each hydrogen.7. The compound of any of to claim 1 , wherein each Ris independently selected from halogen claim 1 , —NO claim 1 , —OH claim 1 , —O(Calkyl) claim 1 , —SH claim 1 , or —S(Calkyl).8. The compound of any of to claim 1 , wherein each Ris independently selected from halogen claim 1 , —NO claim 1 , —OH claim 1 , —O(Calkyl) claim 1 , —SH claim 1 , or —S(Calkyl).9. The compound of any of to claim 1 , wherein n is 1.10. The compound of any of to claim 1 , wherein m is 1 or 3.12. A pharmaceutical composition comprising the compound of any of to and a pharmaceutically acceptable excipient for use in the treatment or prevention of cancer.13. A method of treating or preventing cancer claim 1 , the method comprising the administration of the compound of any of to or the pharmaceutical composition of to a subject in need of such a treatment or prevention.14. The compound of any of to or the pharmaceutical composition of or the method of claim 1 , wherein the cancer is a malignant hematological ...

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05-09-2013 дата публикации

USE OF SUBSTITUTED METHOXYALKOXYPHENYLALKYL DERIVATIVES AS PRESERVATIVE, PRESERVING METHOD, COMPOUNDS AND COMPOSITION

Номер: US20130230473A1
Принадлежит: L'OREAL

The present invention relates to the use as a preserving agent, in particular in cosmetic or dermatological composition, of at least one compound of formula (I): in which:—X represents ═O or —OH;—R1 represents a hydrogen atom or a methyl;—R2 represents a hydrogen atom, a methyl or an ethyl;—R3 represents a C1-C12, saturated or unsaturated, linear hydrocarbon-based radical, optionally substituted with a hydroxyl group (OH); with the exclusion of the compound of formula (I) in which X represents ═O, R1=methyl, R2=H and R3=—(CH)—CH. The invention also relates to certain novel compounds and to the cosmetic or dermatological compositions comprising same. 2. Use according to claim 1 , in which the compounds correspond to formula (I) claim 1 , in which:R3 is a C1-C6, saturated or unsaturated, linear hydrocarbon-based radical, optionally substituted with a hydroxyl group (OH) and/orR2 represents a hydrogen atom.3. Use according to claim 1 , in which R3 is saturated.5. Use according to claim 1 , in which the compound of formula (I) claim 1 , alone or as a mixture claim 1 , is present in a proportion of from 0.01 to 10% by weight claim 1 , in particular 0.1 to 5% by weight claim 1 , relative to the weight of the composition.6. Use according to claim 1 , in which the composition comprises a physiologically acceptable medium which comprises at least one ingredient chosen from fatty substances; water; C2-C6 alcohols; glycols claim 1 , ketones; thickeners claim 1 , emulsifiers claim 1 , surfactants claim 1 , gelling agents claim 1 , active cosmetic agents claim 1 , fragrances claim 1 , fillers claim 1 , colorants claim 1 , moisturizers claim 1 , vitamins and polymers.7. Use according to claim 1 , in which the composition is in the form of a care or makeup product; of an aftershave gel or lotion; of a hair-removing cream; of a suntan or self-tanning composition; of a body or hair hygiene composition; of a dermatological composition; of a solid cosmetic composition; of an aerosol ...

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19-09-2013 дата публикации

COMPOUNDS, COMPOSITIONS AND METHODS FOR THE TREATMENT OF AMYLOID DISEASES AND SYNUCLEINOPATHIES SUCH AS ALZHEIMER'S DISEASE, TYPE 2 DIABETES, AND PARKINSON'S DISEASE

Номер: US20130245128A1
Принадлежит:

The use of 3,4,3′,4′-tetrahydroxychalcone in the treatment of amyloid diseases, especially Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease. 1. A method of treating the formation , deposition , accumulation , or persistence of synuclein fibrils , comprising treating the fibrils with an effective amount of 3 ,4 ,3′ ,4′-tetrahydroxychalcone.2. The method of where the synuclein fibrils are α-synuclein fibrils.3. A method of treating the formation claim 1 , deposition claim 1 , accumulation claim 1 , or persistence of amyloid fibrils claim 1 , comprising treating the fibrils with an effective amount of 3 claim 1 ,4 claim 1 ,3′ claim 1 ,4′-tetrahydroxychalcone.4. The method of where the amyloid fibrils are Aβ amyloid fibrils.5. The method of where the amyloid fibrils are IAPP amyloid fibrils.6. A method of inhibiting and/or relieving an amyloid disease or a synucleinopathy in a mammal suffering therefrom claim 3 , comprising administration to the mammal of a therapeutically effective amount of 3 claim 3 ,4 claim 3 ,3′ claim 3 ,4′-tetrahydroxychalcone.7. The method of where the synucleinopathy is a disease associated with the formation claim 6 , deposition claim 6 , accumulation claim 6 , or persistence of synuclein fibrils.8. The method of where the synucleinopathy is a disease associated with the formation claim 6 , deposition claim 6 , accumulation claim 6 , or persistence of α-synuclein fibrils.9. The method of where the synucleinopathy is selected from the group of diseases consisting of Parkinson's disease claim 6 , familial Parkinson's disease claim 6 , Lewy body disease claim 6 , the Lewy body variant of Alzheimer's disease claim 6 , dementia with Lewy bodies claim 6 , multiple system atrophy claim 6 , and the Parkinsonism-dementia complex of Guam.10. The method of where the synucleinopathy is Parkinson's disease.11. The method of where the ...

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03-10-2013 дата публикации

Compounds with (1E, 6E)-1,7-bis-(3,4-dimethoxyphenyl)-4,4-disubstituted-hepta-1,6-diene-3,5-dione structural scaffold, their biological activity, and uses thereof

Номер: US20130261121A1
Принадлежит:

The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof. 2. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is an androgen receptor associated medical condition that is induced claim 1 , caused or mediated by a normal or abnormal androgen receptor.3. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is inflammation.4. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is acne.5. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is alopecia.6. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is hirsutism.7. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is a wound.8. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated ...

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07-11-2013 дата публикации

GGA AND GGA DERIVATIVES COMPOSITIONS THEREOF AND METHODS FOR TREATING NEURODEGENERATIVE DISEASES INCLUDING PARALYSIS INCLUDING THEM

Номер: US20130296323A1
Принадлежит: COYOTE PHARMACEUTICALS, INC.

This invention relates to geranylgeranyl acetone (GGA) derivatives and the use of GGA, its isomers, and GGA derivatives in methods for inhibiting neural death, increasing neural activity, increasing axon growth and cell viability, and increasing the survival rate of subjects administered the GGA or GGA derivatives. 3. A novel compound of Table 1 or a pharmaceutically acceptable salt thereof.4. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable excipient.5. A pharmaceutical composition comprising a sufficient amount of 5E claim 1 , 9E claim 1 , 13E geranylgeranyl acetone or a GGA derivative of claim 1 , and optionally at least one pharmaceutical excipient claim 1 , wherein the sufficient amount is an amount which provides for a dosing of about 1 mg/kg/day to about 12 mg/kg/day to the patient.6. The pharmaceutical composition of claim 5 , wherein the 5E claim 5 , 9E claim 5 , 13E geranylgeranyl acetone is synthetic 5E claim 5 , 9E claim 5 , 13E geranylgeranyl acetone.7. A composition for increasing the expression and/or release of one or more neurotransmitters from a neuron at risk of developing pathogenic protein aggregates associated with AD or ALS claim 5 , said composition comprising a protein aggregate inhibiting amount of GGA or a GGA derivative.8. A composition for increasing the expression and/or release of one or more neurotransmitters from a neuron at risk of developing extracellular pathogenic protein aggregates claim 5 , said composition comprising an extracellular protein aggregate inhibiting amount of GGA or a GGA derivative.10. The method of claim 10 , wherein said pre-contacted neuron exhibits one or more of:(i) a reduction in the axon growth ability,(ii) a reduced expression level of one or more neurotransmitters,(iii) a reduction in the formation of synapses, and(iv) a reduction in electrical excitability.11. The method of claim 9 , wherein the neurostimulation comprises one or more of:(i) enhancing or inducing ...

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07-11-2013 дата публикации

Novel Dihydroxybenzene Derivatives and Antiprotozoal Agent Comprising Same as Active Ingredient

Номер: US20130296422A1
Принадлежит: ARIGEN PHARMACEUTICALS, INC.

Novel compounds below are useful for preventing or treating diseases caused by protozoans. At least one of a compound represented by Formula (I) 2. The compound claim 1 , optical isomer thereof claim 1 , and pharmaceutically acceptable salt thereof of claim 1 , wherein the one or more substituents of Rare each any one of —COOH claim 1 , —COORa (wherein Ra represents a Calkyl group) claim 1 , —CHO claim 1 , —COOCHCH(OH)CHOH claim 1 , —COO—CH—Rb (wherein Rb represents a group formed by removing one hydrogen atom on a carbon atom of aromatic hydrocarbons claim 1 , such as benzene claim 1 , naphthalene claim 1 , and anthracene) claim 1 , —O—CO-Rc (wherein Rc represents a Calkyl group) claim 1 , —OH claim 1 , —O-Rd (Rd represents a Calkyl group) claim 1 , —O—CH—O—CH claim 1 , —HET (HET represents a group formed by removing one hydrogen atom on a carbon or nitrogen atom of heterocyclic compounds) claim 1 , and —O-HET (HET is defined as above).4. The pharmaceutical composition of claim 3 , wherein the one or more substituents of Ris any one of —COOH claim 3 , —COORa (wherein Ra represents a Calkyl group) claim 3 , —CHO claim 3 , —COOCHCH(OH)CHOH claim 3 , —COO—CH—Rb (wherein Rb represents a group formed by removing one hydrogen atom on a carbon atom of aromatic hydrocarbons claim 3 , such as benzene claim 3 , naphthalene claim 3 , and anthracene) claim 3 , —O—CO-Rc (wherein Rc represents a Calkyl group) claim 3 , —OH claim 3 , —O-Rd (wherein Rd represents a Calkyl group) claim 3 , —O—CH—O—CH claim 3 , —HET (wherein HET represents a group formed by removing one hydrogen atom on a carbon or nitrogen atom of heterocyclic compounds) claim 3 , and —O-HET (wherein HET is defined as above).5. The pharmaceutical composition of or claim 3 , further comprising glycerol.7Trypanosoma.. The agent of claim 6 , wherein the protozoans is8Cryptosporidium.. The agent of claim 6 , wherein the protozoans is9. The agent of any one of to claim 6 , further comprising glycerol.11. The kit of ...

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07-11-2013 дата публикации

Novel Curcumin and Tetrahydrocurcumin Derivatives

Номер: US20130296527A1

The invention relates to novel curcumin and tetrahydrocurcumin derivatives, which have been modified at one phenolic group to incorporate more-reactive groups. The curcumin and tetrahydrocurcumin derivatives are in the form of monomers, dimmers, and polymers.

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21-11-2013 дата публикации

Phenolic compound having carbonyl as neighboring group and application thereof

Номер: US20130306909A1
Принадлежит: JNC Corp, JNC Petrochemical Corp

To provide a liquid crystal compound having a large negative value of dielectric anisotropy (Δ∈). A compound is represented by formula (1): wherein, in formula (1), R 1 and R 2 are hydrogen, halogen or alkyl having 1 to 10 carbons, and in the alkyl, at least one of —CH 2 — may be replaced by —O—, at least one of —(CH 2 ) 2 — may be replaced by —CH═CH—, and at least one of hydrogen may be replaced by halogen; ring A 1 and ring A 2 are 1,4-cyclohexylene or 1,4-phenylene; Z 1 is a single bond, —(CH 2 ) 2 —, —CH 2 O—, —OCH 2 —, —CF 2 O—, —OCF 2 —, —COO—, or —OCO—; Y is halogen, —CF 3 , —CF 2 H or —CH 2 F; and m, n and p are 0, 1 or 2, and a sum (m+n) of m and n is 0, 1 or 2.

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19-12-2013 дата публикации

Compounds with (1E, 6E)-1,7-bis-(3,4-dimethoxyphenyl)-4,4-disubstituted-hepta-1,6-diene-3,5-dione structural scaffold, their biological activity, and uses thereof

Номер: US20130338160A1
Принадлежит:

The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof. 2. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is an androgen receptor associated medical condition that is induced claim 1 , caused or mediated by a normal or abnormal androgen receptor.3. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is inflammation.4. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is acne.5. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is alopecia.6. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is hirsutism.7. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated medical condition is a wound.8. The pharmaceutical composition according to claim 1 , wherein said androgen receptor associated ...

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30-01-2014 дата публикации

Pyrimidine derivatives and use thereof as pesticides

Номер: US20140031373A1
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to novel substituted pyrimidine derivatives, to processes for preparing these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.

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30-01-2014 дата публикации

Solid Forms of Curcumin

Номер: US20140031403A1
Принадлежит:

The present invention provides forms of curcumin and the pharmaceutical compositions thereof. The forms of curcumin disclosed herein are curcumin polymorph Form III, curcumin-2-aminobenzimidazole co-crystal, and curcumin-L-lysine co-crystal. Further, the invention provides methods inhibiting cancer cells and HSV-1 using these curcumin novel solid forms. 1. A co-crystal form of curcumin , wherein the co-crystal form is curcumin-2-aminobenzimidazole.2. The co-crystal form of claim 1 , wherein curcumin-2-aminobenzimidazole exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees-2-theta at about 6.2 claim 1 , about 9.0 claim 1 , about 12.3 claim 1 , about 14.5 claim 1 , about 17.3 claim 1 , about 18.0 claim 1 , about 19.0 claim 1 , about 20.0 claim 1 , about 21.2 claim 1 , about 24.5 claim 1 , about 25.05 claim 1 , and about 27.1 claim 1 , and further exhibits an endothermic transition with an onset of about 118.1° C. as measured by differential scanning calorimetry.3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. A co-crystal form of curcumin claim 1 , wherein the co-crystal form is curcumin-L-lysine.9. The co-crystal form of claim 8 , wherein curcumin-L-lysine is an amorphous form of curcumin co-crystal; and exhibits a first exotherm at onset 36.7° C. with peak 43.6° C. claim 8 , a second exotherm at onset 93.7° C. with peak 97.8° C. claim 8 , and an endotherm at onset 135.5° C. with peak 136.0° C.10. (canceled)11. (canceled)12. (canceled)13. (canceled)14. (canceled)15. A polymorph form of curcumin claim 8 , wherein the polymorph form is Form III.16. The polymorph form of claim 15 , wherein Form III exhibits X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2-theta at about 9.56 claim 15 , about 14.51 claim 15 , about 17.90 claim 15 , and about 26.86 claim 15 , and exhibits an endothermic transition with an onset of about 162.6° C. as measured by differential scanning calorimetry. ...

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06-02-2014 дата публикации

Compounds, compositions and methods for the treatment of amyloid diseases and synucleinopathies such as alzheimer's disease, type 2 diabetes, and parkinson's disease

Номер: US20140038980A1
Принадлежит: ProteoTech Inc

Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.

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06-02-2014 дата публикации

Polymorphs and amorphous forms of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoromethyl)sulfinyl]-1h-pyrazole-3-carbonitrile

Номер: US20140039026A1
Автор: Sharona Zamir
Принадлежит: Makhteshim Chemical Works Ltd

The present invention relates to novel crystalline polymorphs, solvate pseudomorphs and amorphous form of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoromethyl)sulfinyl]-1H-pyrazole-3-carbonitrile (fipronil). The present invention also provides methods for preparing the novel polymorphs, pseudomorphs and amorphous form, as well as insecticidal or pesticidal compositions comprising same, and methods of use thereof as pesticidal agents.

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06-02-2014 дата публикации

Compositions and processes of preparing and using the same

Номер: US20140039182A1
Принадлежит: PURDUE RESEARCH FOUNDATION

The present invention relates to compositions, for example, the DBU/Hexafluoroacetone hydrate salt, and processes of preparing and using the same for the modification of chemical compounds via the release of trifluoroacetate. The DBU/Hexafluoroacetone hydrate salt can perform trifluoromethylation reactions on chemical compounds, such as carbonyl group-containing compounds.

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20-02-2014 дата публикации

Lipophilic Curcumin Analogs And Methods Of Inhibiting HIV-1, Treating Latent HIV In The Brain, And Preventing HIV-Mediated Cognitive Decline And HIV Dementia

Номер: US20140051742A1
Принадлежит:

Compounds having formulas (I) to (VIII), salts thereof, or combinations thereof and pharmaceutical compositions comprising one or more these compounds are described herein for the treatment of HIV and neurodegenerative effects caused by HIV. Also provided herein are methods and a kit for inhibiting HIV-1, treating latent HIV in the brain, and preventing HIV-mediated cognitive decline and HIV dementia comprising administering the compounds having the formulas (I) to (VIII) and pharmaceutical compositions comprising the compounds having these formulas. The compounds having formulas I through VIII are curcumin analogs which are advantageously characterized as having anti-retroviral, neuroprotective, anti-glucosidase, and anti-HIV integrase properties. In one aspect, the pharmaceutical composition is delivered intranasally. 2. The method according to claim 1 , wherein the pharmaceutical composition is intranasally administered.3. The method according to claim 1 , wherein the pharmaceutical composition further comprises an antiviral agent other than at least one compound of formulas (I) to (VIII).4. The method according to claim 3 , wherein the antiviral agent is selected from the group consisting of nucleoside reverse transcriptase inhibitors claim 3 , nonnucleoside reverse transcriptase inhibitors claim 3 , protease inhibitors claim 3 , integrase inhibitors claim 3 , fusion inhibitors claim 3 , chemokine receptor antagonists claim 3 , and combinations thereof.5. The method according to claim 1 , wherein the analog is dispersed into a pharmaceutically acceptable oil.8. A compound having any of formulas (II) to (VIII) as defined in .9. A pharmaceutical composition comprising at least one compound having any of formulas (II) through (VIII) as defined in .10. The pharmaceutical composition according to claim 9 , further comprising a pharmaceutically acceptable excipient claim 9 , diluent claim 9 , and/or carrier.11. The pharmaceutical composition according to claim 9 , ...

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27-03-2014 дата публикации

VIRAL INHIBITOR COMPOSITION FOR IN VIVO THERAPEUTIC USE

Номер: US20140088193A1
Автор: Coppens Christine
Принадлежит: CESA ALLIANCE S.A.

The present invention concerns a pharmaceutical composition comprising a compound of formula A being (2,3(dihydroxy), 5[3(1,2)butadiene], 1(3hydroxy,3methyl,4pentene)benzene) and/or a compound of formula B being (2,3(dihydroxy), 5[3(1,2)butadiene], 2[2methylbutane]benzenal) and/or a compound of formula C being (2,3(dihydroxy), 5[3(1,2)butadiene], 2hydroxy,3butene benzoate) or a combination thereof for use as a medicament or for in vivo use in treatment and prevention of diseases caused by DNA enveloped viruses, DNA non-enveloped viruses, RNA enveloped viruses and RNA non-enveloped viruses. 3. Composition according to or composition for use according to , wherein the compounds are selected from the group consisting in:the compound of formula A alone, orthe compound of formula B alone, orthe compound of formula C alone, orthe compound of formula A and the compound of formula B, orthe compound of formula A and the compound of formula C, orthe compound of formula B and the compound of formula C, orthe compound of formula A and the compound of formula B and the compound of formula C.4. Composition according to or composition for use according to , wherein each compound is administered at a dose higher than or equal to 0.1 mg per administering.5. Composition according to or composition for use according to , wherein each compound is administered at a dose comprised between 0.1 mg and 5000 mg per administering.6. Composition according to or , wherein the dose is administered at least one time per day.7macadamia. Composition according to or composition for use according to or composition according to , wherein a base oil such as olive oil , or oil is added.8. Composition according to or composition for use according to , wherein the composition is used as a prophylactic.9. Composition according to or composition for use according to , wherein the composition is used as a viral inhibitor within the body.10. Composition according to or composition for use according to , ...

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06-01-2022 дата публикации

Half-Curcuminoids as Amyloid-Beta PET Imaging Agents

Номер: US20220001036A1
Принадлежит:

Provided herein are curcumin analogues that are able to interact with amyloid beta (Aβ) and to attenuate the copper-induced crosslinking of Aβ. Also provided herein are methods of using the compounds as imaging agents of amyloid beta and for the treatment of diseases associated with amyloid beta. Methods of preparing unlabeled and radiolabeled compounds useful for interacting with amyloid beta and pharmaceutical compositions are also provided. 2. The method of claim 1 , wherein the imaging technique is selected from the group consisting of fluorescence imaging claim 1 , positron emission tomography imaging claim 1 , magnetic resonance imaging claim 1 , single-photon emission computed tomography claim 1 , positron emission tomography with computed tomography imaging claim 1 , and positron emission tomography with magnetic resonance imaging.3. The method of claim 1 , wherein the imaging technique is selected from the group consisting of fluorescence imaging claim 1 , position emission tomography imaging claim 1 , and single-photon emission computed tomography.5. The method of claim 1 , wherein:{'sup': 4', '5, 'X is BRR;'}{'sup': 1', '1A, 'sub': '6-10', 'Ris selected from the group consisting of Caryl and 5-10 membered heteroaryl, each of which may be optionally substituted by 1, 2, 3, or 4 independently selected Rgroups;'}{'sup': 1A', 'N1', 'N2', '6, 'sub': 1-6', '1-6', '1-6', '1-6', '6-10', '1-6', '1-6', '6-10, 'each Ris independently selected from the group consisting of halo, Calkyl, Chaloalkyl, Calkoxy, Chaloalkoxy, NRR, and Caryl, wherein the Calkyl, Calkoxy, and Caryl are each optionally substituted by 1, 2, 3, or 4 independently selected Rgroups;'}{'sup': 2', '2A, 'sub': 1-6', '3-6, 'Ris selected from the group consisting of Calkyl, Ccycloalkyl, and phenyl, each of which may be optionally substituted by 1, 2, 3, or 4 independently selected Rgroups;'}{'sup': '3', 'Ris H;'}{'sup': 4', '5, 'Rand Rare each halo; and'}m is 1.6. The method of claim 5 , wherein:{'sup ...

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02-01-2020 дата публикации

METHOD FOR PRODUCING CYCLOPROPYL-SUBSTITUTED ACETOPHENONES

Номер: US20200002259A1
Автор: SCHOTES Christoph
Принадлежит: Bayer CropScience Aktiengesellschaft

A method is described for preparing cyclopropyl-substituted acetophenones of the general formula (I). 2: The method according to claim 1 , wherein Xis chlorine.3: The method according to claim 1 , wherein Xis bromine.4: The method according to claim 1 , wherein Ris 4-chlorine.5: The method according to claim 1 , wherein Ris methyl.6: The method according to claim 1 , wherein Xis chlorine claim 1 , Xis bromine claim 1 , Ris 4-chlorine and Ris methyl.8: The compound according to claim 7 , wherein Xis bromine claim 7 , Ris 4-chlorine and Ris methyl.10: The compound according to claim 9 , wherein Ris 4-chlorine and Ris methyl. The invention relates to a method for preparing cyclopropyl-substituted acetophenones and also to two compounds which are used in the method.Cyclopropyl-substituted acetophenones are important intermediates for the synthesis of agrochemically active substances such as cyproconazole and have already been prepared by diverse routes. Examples include here two syntheses related to the method according to the invention:CN 101857576A (2010) discloses a method in which the cyclopropyl-substituted acetophenone 1-(4-chlorophenyl)-2-cyclopropylpropan-1-one is prepared by adding 4-chlorobenzylmagnesium chloride to cyclopropyl methyl ketone, followed by eliminating the resulting hydroxyl group, hydroboration and oxidation initially to the benzylic alcohol, then further to give 1-(4-chlorophenyl)-2-cyclopropylpropan-1-one. A disadvantage of this method is the hydroboration reaction, which is safety-critical and is also expensive.CN102603508B likewise describes the preparation of 1-(4-chlorophenyl)-2-cyclopropylpropan-1-one but starting from methyl 2-chloro-2-(4-chlorophenyl)acetate. This is reacted with a strong base and methyl cyclopropyl ketone to give a glycidyl ester, which rearranges after saponification and acidification to give 1-(4-chlorophenyl)-2-cyclopropylpropan-1-one. A disadvantage here is the use of methyl 2-chloro-2-(4-chlorophenyl)acetate as ...

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14-01-2016 дата публикации

Lipophilic Curcumin Analogs And Methods Of Inhibiting HIV-1, Treating Latent HIV In The Brain, And Preventing HIV-Mediated Cognitive Decline And HIV Dementia

Номер: US20160009623A1
Принадлежит:

Compounds having formulas (I) to (VIII), salts thereof, or combinations thereof and pharmaceutical compositions comprising one or more these compounds are described herein for the treatment of HIV and neurodegenerative effects caused by HIV. Also provided herein are methods and a kit for inhibiting HIV-1, treating latent HIV in the brain, and preventing HIV-mediated cognitive decline and HIV dementia comprising administering the compounds having the formulas (I) to (VIII) and pharmaceutical compositions comprising the compounds having these formulas. The compounds having formulas I through VIII are curcumin analogs which are advantageously characterized as having anti-retroviral, neuroprotective, anti-glucosidase, and anti-HIV integrase properties. In one aspect, the pharmaceutical composition is delivered intranasally. 114-. (canceled)16. The compound according to claim 15 , wherein the compound is of formula (II) or pharmaceutically acceptable salt thereof.17. The compound according to claim 15 , wherein the compound is of formula (III) or pharmaceutically acceptable salt thereof.18. The compound according to claim 15 , wherein the compound is of formula (IV) or pharmaceutically acceptable salt thereof.19. The compound according to claim 15 , wherein the compound is of formula (V) or pharmaceutically acceptable salt thereof.20. The compound according to claim 15 , wherein the compound is of formula (VI) or pharmaceutically acceptable salt thereof.21. The compound according to claim 15 , wherein the compound is of formula (VII) or pharmaceutically acceptable salt thereof.22. The compound according to claim 15 , wherein the compound is of formula (VIII) or pharmaceutically acceptable salt thereof.23. A pharmaceutical composition comprising at least one compound of any of formulas (II) through (VIII) or a pharmaceutically acceptable salt thereof as defined in .24. The pharmaceutical composition according to claim 23 , further comprising a pharmaceutically acceptable ...

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08-01-2015 дата публикации

THERAPEUTIC CURCUMIN DERIVATIVES

Номер: US20150011494A1
Принадлежит:

Curcumin analogues and methods are provided for treatment of disease. 114-. (canceled)15. A method for identifying a therapeutic curcumin derivative , comprising:contacting a cell comprising at least one of NF-κB, AP-1 or GSTP1-1 with a curcumin derivative;contacting the cell with an activator of NF-κB, AP-1 or GSTP1-1; anddetermining the effect of the curcumin derivative on cell activation;wherein a curcumin derivative that reduces cell activation is identified as an therapeutic curcumin derivative.16. The method of claim 15 , wherein the activator comprises TNF-α claim 15 , IL-1 claim 15 , PMA or an MAPK kinase.17. The method of claim 15 , wherein the cell is an adipocyte or endothelial cell.18. The method of claim 15 , wherein the cell is a brain cell.19. The method of claim 18 , wherein the brain cell is a glial cell.20. A method for identifying a therapeutic curcumin derivative claim 18 , comprising:contacting a solution comprising an Aβ peptide with a curcumin derivative; anddetermining the effect of the curcumin derivative on aggregation of the Aβ peptide;wherein a curcumin derivative that reduces aggregation of the Aβ peptide is identified as a therapeutic curcumin derivative.21. The method of claim 20 , wherein the effect of the curcumin derivative on aggregation of the Aβ peptide is determined by an immunological assay.22. A method of treating a subject afflicted with cancer or a precancerous condition claim 20 , the method comprising administering to the subject a therapeutically effective amount of a composition comprising a curcumin derivative selected from the group consisting of:{'sup': 1', '2', '1', '2, '(a) Ar-L-Ar(Formula I); wherein L is a divalent linking group comprising an alkylene or an alkenylene comprising 3, 4, 5, 6, or 7 backbone carbon atoms, wherein one or more of the backbone carbon atoms form part of a carbonyl or secondary alcohol; and Arand Arare each independently aryl groups; and'}{'sup': 1', '11', '1', '11, '(b) Ar-L-R(Formula IV ...

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08-01-2015 дата публикации

ANTI-INVASIVE COMPOUNDS

Номер: US20150011620A1
Принадлежит:

The present invention relates to the field of anti-invasive compounds and methods for predicting the anti-invasive activity of said compounds, as well as their use in the prevention and/or treatment of diseases associated with undesired cell invasion; in particular, this invention relates to the field of anti-invasive chalcone-like compounds. 114.-. (canceled)16. The method according to claim 15 , wherein:x and y are independently selected from 1 or 2, andat least one of x and y is 1.17. The method according to claim 15 , wherein:{'sub': l', '2', '3', '2', '3, 'Ais C, one of Aand Ais C and the other one of Aand Ais O;'}{'sub': 1', '2', '3', '1-6, 'R, R, and Rare each independently selected from —H, -halo, and —O—Calkyl;'}{'sub': 4', '5', '6, 'R, R, and Rare each H;'}x is 2; andy is 1.19. The method according to claim 15 , wherein the compound has Formula Ia claim 15 , wherein:{'sub': 1', '2', '3', '1-6, 'R, R, and R, are each independently selected from —H, -halo, and —O—Calkyl;'}{'sub': 4', '5, 'R, and Rare each H; and'}{'sub': '6', 'Ris halo.'}23. The method according to ; wherein said compound is selected from:(2E)-3-(4-fluorophenyl)-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one;(2E)-3-(4-chlorophenyl)-1-(4-methoxyphenyl)prop-2-en-1-one;(2E)-1-(4-methoxyphenyl)-3-(2,4,6-trimethoxyphenyl)prop-2-en-1-one;(2E)-3-(3-fluorophenyl)-1-(4-fluorophenyl)prop-2-en-1-one;(2E)-3-(furan-2-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one;(2E)-1-(2,6-dimethoxyphenyl)-3-(furan-2-yl)prop-2-en-1-one;(2E)-1-(4-fluorophenyl)-3-(furan-3-yl)prop-2-en-1-one; and(2E)-1,3-di(furan-2-yl)prop-2-en-1-one.24. The method according to claim 15 , wherein the compound is formulated as part of a pharmaceutical composition further comprising a pharmaceutically acceptable carrier claim 15 , excipient and/or diluent claim 15 , and optionally an adjuvant.25. The method according to claim 15 , wherein the invasion of tumor cells into the surrounding tissue is inhibited in a subject having a condition ...

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18-01-2018 дата публикации

INK COMPOSITION FOR ORGANIC LIGHT-EMITTING DEVICE, ORGANIC LIGHT-EMITTING DEVICE INCLUDING FILM FORMED BY USING THE INK COMPOSITION, AND METHOD OF MANUFACTURING THE ORGANIC LIGHT-EMITTING DEVICE

Номер: US20180019411A1
Принадлежит:

An ink composition for an organic light-emitting device, the ink composition including a luminescent host material and a solvent, wherein the luminescent host material includes at least one compound represented by Formula (1), and wherein the solvent includes at least one selected from an aromatic ether, an aromatic ester, and an aromatic ketone: 4. The ink composition of claim 1 , whereinthe luminescent host material comprises at least one compound having a biscarbazole backbone.6. The ink composition of claim 5 , wherein{'sub': 1', '2', '63, 'L, L, and Lare each independently selected froma single bond; and{'sub': 3', '2', '2', '1', '20', '1', '20, 'a phenylene group, a fluorenylene group, a spiro-bifluorenylene group, a carbazolylene group, a dibenzofuranylene group, and a dibenzothiophenylene group, each substituted or unsubstituted with at least one selected from deuterium, —CD, —CDH, —CDH, a C-Calkyl group, a C-Calkoxy group, a phenyl group, a biphenyl group, a fluorenyl group, a spiro-bifluorenyl group, a dimethylfluorenyl group, a diphenylfluorenyl group, a carbazolyl group, a phenylcarbazolyl group, a biphenylcarbazolyl group, a dibenzofuranyl group, a phenyldibenzofuranyl group, a diphenyldibenzofuranyl group, a dibenzothiophenyl group, a phenyldibenzothiophenyl group, and a diphenyldibenzothiophenyl group,'}a1, a2, and a63 are each independently 1, 2, or 3,{'sub': 1', '2', '63, 'A, A, and Aare each independently selected from{'sub': 3', '2', '2', '1', '20', '1', '20, 'hydrogen, deuterium, —CD, —CDH, —CDH, a C-Calkyl group, and a C-Calkoxy group; and'}{'sub': 3', '2', '2', '1', '20', '1', '20, 'a phenyl group, a fluorenyl group, a spiro-bifluorenyl group, a carbazolyl group, a dibenzofuranyl group, and a dibenzothiophenyl group, each substituted or unsubstituted with at least one selected from deuterium, —CD, —CDH, —CDH, a C-Calkyl group, a C-Calkoxy group, a phenyl group, a biphenyl group, a fluorenyl group, a spiro-bifluorenyl group, a dimethylfluorenyl ...

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22-01-2015 дата публикации

GGA AND GGA DERIVATIVES COMPOSITIONS THEREOF AND METHODS FOR TREATING NEURODEGENERATIVE DISEASES INCLUDING PARALYSIS INCLUDING THEM

Номер: US20150025077A1
Принадлежит: COYOTE PHARMACEUTICALS, INC.

This invention relates to geranylgeranyl acetone (GGA) derivatives and the use of GGA, its isomers, and GGA derivatives in methods for inhibiting neural death, increasing neural activity, increasing axon growth and cell viability, and increasing the survival rate of subjects administered the GGA or GGA derivatives. 3. A novel compound of Table 1 or a pharmaceutically acceptable salt thereof.43. A pharmaceutical composition comprising a compound of any one of - and a pharmaceutically acceptable excipient.53. A pharmaceutical composition comprising a sufficient amount of 5E claims 1 , 9E claims 1 , 13E geranylgeranyl acetone or a GGA derivative of any one of - claims 1 , and optionally at least one pharmaceutical excipient claims 1 , wherein the sufficient amount is an amount which provides for a dosing of about 1 mg/kg/day to about 12 mg/kg/day to the patient.6. The pharmaceutical composition of claim 5 , wherein the 5E claim 5 , 9E claim 5 , 13E geranylgeranyl acetone is synthetic 5E claim 5 , 9E claim 5 , 13E geranylgeranyl acetone.7. A composition for increasing the expression and/or release of one or more neurotransmitters from a neuron at risk of developing pathogenic protein aggregates associated with AD or ALS claim 5 , said composition comprising a protein aggregate inhibiting amount of GGA or a GGA derivative.8. A composition for increasing the expression and/or release of one or more neurotransmitters from a neuron at risk of developing extracellular pathogenic protein aggregates claim 5 , said composition comprising an extracellular protein aggregate inhibiting amount of GGA or a GGA derivative.10. The method of claim 10 , wherein said pre-contacted neuron exhibits one or more of:(i) a reduction in the axon growth ability,(ii) a reduced expression level of one or more neurotransmitters,(iii) a reduction in the formation of synapses, and(iv) a reduction in electrical excitability.11. The method of claim 9 , wherein the neurostimulation comprises one or more ...

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24-01-2019 дата публикации

Opsin-Binding Ligands, Compositions and Methods of Use

Номер: US20190023649A1
Принадлежит: BIKAM PHARMACEUTICALS, INC.

Compounds and compositions are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed. 115-. (canceled)17. The method of claim 16 , wherein said visual cycle product is a toxic visual cycle product.18. The method of claim 17 , wherein said toxic visual cycle product is lipofuscin or N-retinylidene-N-retinylethanolamine (A2E).19. The method of claim 16 , wherein said compound reduces mislocalization of said opsin protein.20. The method of claim 16 , wherein said opsin protein is present in a cell.21. The method of claim 20 , wherein said cell is a cone cell or rod cell.22. The method of claim 20 , wherein said cell is present in a mammalian eye.23. A method of inhibiting the formation or accumulation of a visual cycle product claim 20 , comprising contacting an opsin protein with a compound selected from the group consisting of:3-(trifluoromethyl)-N-((2,6,6-trimethylcyclohex-1-enyl)methyl)aniline hydrochloride (Compound 1);3-methyl-N-((2,6,6-trimethylcyclohex-1-enyl)methyl)aniline (Compound 2);3-((2,6,6-trimethylcyclohex-1-enyl)methylamino)benzamide (Compound 3);3-((2,6,6-trimethylcyclohex-1-enyl)methylamino)benzonitrile (Compound 4);3-chloro-N-((2,6,6-trimethylcyclohex-1-enyl)methyl)aniline (Compound 5);1-methyl-3-((2,6,6-trimethylcyclohex-1-enyl)methoxy)benzene (Compound 6);1-fluoro-3-((2,6,6-trimethylcyclohex-1-enyl)methoxy)benzene (Compound 7);1-chloro-3-((2,6,6-trimethylcyclohex-1-enyl)methoxy)benzene (Compound 8);1-(trifluoromethyl)-3-((2,6,6-trimethylcyclohex- ...

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24-01-2019 дата публикации

SYNTHESIS OF CANNABINOIDS

Номер: US20190023680A1
Принадлежит: UNIVERSITY OF SOUTH FLORIDA

Provided are synthesis processes and intermediates for preparing cannabinoids and analogs. 2. The process of claim 1 , wherein step (a) is present.6. The process of claim 2 , wherein step (a) comprises mixing potassium bis(trimethylsilyl)amide (KHMDS) with the compound of formula (II).7. The process of claim 1 , wherein Ris —(CH)-CH.8. The process of claim 1 , wherein Rand Rare —OCH.9. The process of claim 1 , wherein Rand Rare each —CH.10. The process of claim 1 , wherein Ris hydroxyl claim 1 , —CH claim 1 , or —OCH.11. The process of claim 1 , wherein step (b) comprises mixing the compound of formula (III) with (1 claim 1 ,3 -Bi s(2 claim 1 ,4 claim 1 , 6-trimethylphenyl)-2-imidazolidinylidene)dichloro(phenylmethylene)(tricyclohexylphosphine)ruthenium.13. The process of claim 12 , wherein Ris C-Calkoxy.14. The process of claim 12 , wherein the cannabinoid is Δ-tetrahydrocannabinol (THC).16. The process of claim 15 , wherein Ris C-Calkyl.17. The process of claim 15 , wherein the cannabinoid is cannabidiol (CBD).19. The compound of claim 18 , wherein Ris —(CH)-CHor —(CH)-CH.21. The compound of claim 20 , wherein Ris —(CH)-CHor —(CH)-CH. This application claims the benefit of and priority to U.S. Provisional Patent Application No. 62/535,388, filed on Jul. 21, 2017, the entire content of which is incorporated herein by reference in its entirety.The present disclosure relates to synthesis methods for cannabinoids and analogues.Cannabinoids are compounds isolated from plants of the genus Cannabis, which are known for their psychotropic properties. There are more than 100 known cannabinoids present in varying amounts depending on the strain of the plant. The cannabinoids exert their physiological properties through their interaction with a series of receptors known as the cannabinoid receptors. Two of the primary cannabinoid receptors are CB1 and CB2, which are expressed in unique quantities in different tissues throughout the body. There is evidence that additional ...

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23-01-2020 дата публикации

POGOSTONE DERIVATIVES AND METHODS OF USING THE SAME

Номер: US20200024246A1
Принадлежит: Hamyard Associates LLC

Described are novel derivatives of pogostone and methods of using the same. 2. The pogostone derivative of wherein the structure is selected from a group consisting of Formula 1 claim 1 , Formula 2 claim 1 , Formula 3 claim 1 , Formula 4 claim 1 , Formula 5 claim 1 , Formula 6 claim 1 , Formula 7 claim 1 , Formula 8 claim 1 , Formula 9 claim 1 , Formula 10 claim 1 , Formula 11 claim 1 , Formula 12 claim 1 , Formula 13 claim 1 , Formula 14 claim 1 , Formula 15 claim 1 , Formula 16 claim 1 , Formula 17 claim 1 , Formula 18 claim 1 , Formula 19 claim 1 , Formula 20 claim 1 , Formula 21 claim 1 , Formula 22 claim 1 , Formula 23 claim 1 , Formula 24 claim 1 , Formula 25 claim 1 , Formula 26 claim 1 , Formula 27 claim 1 , Formula 28 claim 1 , Formula 29 claim 1 , Formula 30 claim 1 , Formula 31 claim 1 , Formula 32 claim 1 , Formula 33 claim 1 , Formula 34 claim 1 , Formula 35 claim 1 , Formula 36 claim 1 , Formula 37 claim 1 , Formula 38 claim 1 , Formula 39 claim 1 , Formula 40 claim 1 , Formula 41 claim 1 , Formula 42 claim 1 , Formula 43 claim 1 , Formula 44 claim 1 , Formula 45 claim 1 , Formula 46 claim 1 , Formula 47 claim 1 , and Formula 48.4. The compound of claim 3 , wherein Ra substituted or unsubstituted C-Cunbranched or branched alkyl.5. The compound of claim 3 , wherein Ris a methyl group.6. The compound of claim 3 , wherein Rcomprises a unsubstituted C-Cunbranched or branched cycloalkyl.7. The compound of claim 3 , wherein the compound has the structure of Formula 4 claim 3 , Formula 5 claim 3 , or Formula 9.9. The compound of claim 8 , wherein Ris a substituted or unsubstituted C-Cunbranched or branched alkyl.10. The compound of claim 8 , wherein Ris a hydrogen.11. The compound of claim 8 , wherein X is an oxygen.12. The compound of claim 8 , wherein X is a nitrogen.13. The compound of claim 8 , wherein the compound has the structure of Formula 13 claim 8 , Formula 14 claim 8 , Formula 16 claim 8 , Formula 17 claim 8 , Formula 19 claim 8 , Formula 20 claim ...

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28-01-2021 дата публикации

COMPOUNDS AS MODULATORS OF TLR2 SIGNALING

Номер: US20210024539A1
Принадлежит: Neuropore Therapies, Inc.

The present disclosure relates to compounds, pharmaceutical compositions comprising such compounds, and use of such compounds in methods of treatment or in medicaments for treatment of inflammatory diseases and certain neurological disorders that are related to inflammatory signaling processes, including but not limited to misfolded proteins. 3. The compound of claim 1 , or a tautomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Y is —C(O)—.4. The compound of claim 1 , or a tautomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Y is absent.5. The compound of any one of - claim 1 , or a tautomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Gand Gare each CR.6. The compound of any one of - claim 1 , or a tautomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Gis CF claim 1 , CCl claim 1 , or CBr.7. The compound of any one of - claim 1 , or a tautomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Gis CF claim 1 , CCl claim 1 , or CBr.8. The compound of any one of - claim 1 , or a tautomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Gand Gare each CH.9. The compound of any one of - claim 1 , or a tautomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Gis CH and Gis N.10. The compound of any one of - claim 1 , or a tautomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Gis N and Gis CH.11. The compound of any one of - claim 1 , or a tautomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Ris —OH and Ris selected from the group consisting of —C(O)R claim 1 , —S(O)R claim 1 , —S(O)R claim 1 , —NHC(O)R claim 1 , ...

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29-01-2015 дата публикации

WATER-SOLUBLE FLUORESCENCE COMPOUND AND METHOD FOR PREPARING THE SAME

Номер: US20150031867A1
Принадлежит:

The present invention provides a water-soluble fluorescent compound of resveratrone 6-O-β-glucoside [(E)-4-(8-hydroxy-6-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)naphthalen-2-yl)but-3-en-2-one] and its derivatives of Formula 1 which have at least one water-soluble substituent, and a method for preparing the same by a photochemical reaction of resveratrol 3-O-β-glucoside and its derivatives of having Formula 3 which are not fluorescent. Said new water-soluble fluorescent compounds has single-photon absorptive characteristics and/or two-photon absorptive characteristics as well as no or little toxicity, and can be usefully utilized in fields that requires water-soluble fluorescent characteristics (diagnosis, fluorescent probe, in vivo imaging, display, etc.). 3. The fluorescent compound according to claim 1 , wherein Ris hydrogen atom.5. The method according to claim 4 , characterized in that the compound of Formula 3 is selected from the group consisting of trans-isomer claim 4 , cis-isomer and mixture thereof.6. The method according to claim 4 , characterized in that ascorbic acid claim 4 , polyphenol or mixture thereof is further added before the UV irradiation.7. The method according to claim 4 , characterized in that it is conducted under Natmosphere (Npurging).8. (canceled) The present invention relates to a water-soluble fluorescent compound, a method for preparing the same, and its use.There are cases where light is emitted from a substance at a low temperature at which the substance can not emit any visible ray by thermal radiation. Such lighting phenomenon is referred to as luminescence. Luminescence means the emission of light having a wavelength which correspond to the energy difference when a substance is converted to a stable state having low energy from an unstable state having high energy. Thus, in order to make a substance emit such light, it is necessary to make the substance to an unstable excited state having ...

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01-02-2018 дата публикации

IONONE STABILISERS FOR NITROCELLULOSE-BASED PROPELLANTS

Номер: US20180029951A1
Принадлежит: PB CLERMONT SA

The present disclosure is directed to a nitrocellulose-based propellant composition comprising: (a) a nitrate ester-based propellant comprising nitrocellulose; and (b) a stabiliser comprising a non-aromatic compound (12) consisting of a general ionone formula (12-I), (12-II), (12-III) or (12-IV): 2. The propellant composition according to claim 1 , wherein the nitrate ester-based propellant consists of nitrocellulose alone as a single base or of a mixture comprising nitrocellulose in combination with at least a blasting oil and/or at least one energetic additive as a double or higher base.3. The propellant composition according to claim 1 , wherein the non-aromatic compound is a substance capable of reacting by H-abstraction with radical groups formed by degradation of the nitrate ester to form a first by-product capable of further reacting with NOx and/or alkoxy groups formed by degradation of the nitrate ester to form a second by-product comprising no NNO groups.4. The propellant composition according to claim 3 , wherein the second by-product is capable of reaction with radical groups formed by degradation of the nitrate ester for forming third and subsequent by-products capable of reacting with such radical alkoxy groups or with NOx.5. The propellant composition according to claim 2 , wherein the blasting oil comprises at least a nitrated polyol obtainable by nitration of polyol selected from a group consisting of glycerol claim 2 , glycol claim 2 , diethylene glycol claim 2 , triethylene glycol and metriol claim 2 , and wherein the at least one energetic additive is an energetic plasticizer selected from the group of nitramines claim 2 , including butyl-NENA claim 2 , dinitrodiazaalkane (DNDA) claim 2 , or is an explosive comprising RDX claim 2 , HMX claim 2 , FOX-7 claim 2 , FOX-12 claim 2 , CL20.7. The propellant composition according to claim 1 , wherein the non-aromatic compound is present in the composition in an amount comprised between 0.1 and 5.0 wt. % ...

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31-01-2019 дата публикации

PROCESS FOR PREPARING BIPHENYL COMPOUNDS

Номер: US20190032098A1
Принадлежит:

A process is provided for preparing a compound having the formula (I): 2. The process of claim 1 , wherein the water-miscible solvent is acetone.3Trametes versicolor.. The process of claim 1 , wherein the laccase is from4. The process of claim 1 , wherein the amount of laccase for one gram of compound of formula (II) is from 1.5 mg to 75 mg.5. The process of claim 1 , wherein the solution of the compound of formula (II) in a water-miscible solvent is prepared by adding said compound of formula (II) in said water-miscible solvent claim 1 , and adding a buffer solution.6. The process according to claim 5 , wherein the amount of water-miscible solvent is comprised between 5% and 10% of volume in comparison with the total volume of the mixture formed by said solvent and the buffer solution.7. The process of claim 1 , wherein the addition of an oxygen source according to a) is carried out for a sufficient time to saturate the solution in dissolved oxygen.8. The process of claim 1 , wherein the solution of the compound of formula (II) in the water-miscible solvent used for b) is saturated in oxygen.9. The process of claim 1 , wherein the pH of the solution of the compound of formula (II) in the water-miscible solvent is comprised between 4 and 7.10. The process of claim 1 , wherein step c) is a step of recovering the compound of formula (I) by centrifugation or filtration.11. The process of claim 1 , wherein the amount of laccase for one gram of compound of formula (II) is from 3 mg to 15 mg.12. The process of claim 5 , wherein the buffer solution is a sodium acetate buffer.13. The process of claim 7 , wherein the addition of an oxygen source according to step a) is carried out for 5 minutes. This application is a continuation of U.S. patent application Ser. No. 15/516,318, filed Mar. 31, 2017, which is a 371 application of International Application PCT/EP2015/072957, filed Oct. 5, 2015, and which claims the benefit of European Patent Office application Serial No. ...

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04-02-2021 дата публикации

CO-CRYSTALS

Номер: US20210032210A1
Принадлежит:

The present document is directed to co-crystals of resveratrol and/or curcumin with piperazine and their use in medicine and/or as food and feed supplements. 1. A resveratrol-piperazine co-crystal , Form 1 , characterized by having an XRPD pattern comprising peaks at 4.48 , 13.32 , 16.96 , 18.88 , 19.16 , and 22.84 °2θ±0.2 °2θ.2. The resveratrol-piperazine co-crystal claim 1 , Form 1 claim 1 , according to claim 1 , characterized by having an XRPD pattern according to Table 1.3. The resveratrol-piperazine co-crystal claim 1 , Form 1 claim 1 , according to or claim 1 , characterized by having an XRPD pattern as shown in .4. The resveratrol-piperazine co-crystal claim 1 , Form 1 claim 1 , according to any one of the preceding claims claim 1 , characterized by having a fusion temperature Tof 201° C.±5° C.5. The resveratrol-piperazine co-crystal claim 1 , Form 1 claim 1 , according to any one of the preceding claims claim 1 , characterized by having a DSC thermogram as shown in .6. A method for producing the resveratrol-piperazine co-crystal claim 1 , Form 1 claim 1 , as defined in any one of the preceding claims claim 1 , said method comprising the steps of:a) dispensing resveratrol in acetone or acetonitrile;b) adding piperazine in acetone or acetonitrile to the dispensed resveratrol of step a) thereby providing a resveratrol-piperazine mixture;c) optionally diluting the resveratrol-piperazine mixture obtained in step b) with acetone or acetonitrile;d) heating the resveratrol-piperazine mixture obtained in step b) or c) at a temperature within the range of from about 30° C. to about 50° C. under stirring for about 10-30 minutes thereby providing a resveratrol-piperazine suspension;e) allowing the resveratrol-piperazine suspension obtained in step d) to settle;f) separating a solid phase obtained in step e); andg) drying the separated solid phase of step f).7. A method for producing the resveratrol-piperazine co-crystal claim 1 , Form 1 claim 1 , as defined in any one ...

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11-02-2016 дата публикации

COMPOUNDS AND MATRICES FOR USE IN BONE GROWTH AND REPAIR

Номер: US20160038641A1
Принадлежит: HUMAN BIOMOLECULAR RESEARCH INSTITUTE

Compositions of small molecules, matrices, and isolated cells including methods of preparation, and methods for differentiation, transdifferentiation, and proliferation of animal cells into the osteoblast blast cell lineage were described. Examples of osteogenic materials that were administered to cells or co-cultured with cells are represented by compounds of Formula II, IV, and VI independently or preferably in combination with a matrix to afford bone cells. Small molecule-stimulated cells were also combined with a matrix, placed with a cellular adhesive or material carrier and implanted to a site in an animal for bone repair. Matrix pretreated with compounds of Formula II, IV, and VI were also used to cause cells to migrate to the matrix that is of use for therapeutic purposes. 1113. The composition of any one of - claims 1 , wherein the isolated cells capable of differentiating into bone cells are isolated human bone marrow-derived mesenchymal stem cells claims 1 , human mesenchymal stem cells of adipose tissue claims 1 , human mesenchymal stem cells of blood claims 1 , human mesenchymal stem cells of bone allograft or autograft tissues claims 1 , human mesenchymal stem cells of dental pulp claims 1 , human pericytes claims 1 , human myoblasts claims 1 , and human chondrocytes claims 1 , human osteoprogenitor cells claims 1 , urine stem cells claims 1 , or their respective progenitor cells such as stem cell isolated from amniotic fluid or cord blood claims 1 , embryonic stem cells claims 1 , and induced pluripotent stem cells.123. The composition of - wherein the calcium phosphate matrix is a tricalcium phosphate ceramic or is oseoinductive.137. The composition of - wherein the calcium phosphate matrix is a tricalcium phosphate ceramic or is oseoinductive.14. The composition of compound 8-10 wherein the calcium phosphate matrix is a tricalcium phosphate ceramic or is oseoinductive.1510. The compositions of any one of - further comprising a calcium phosphate ...

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11-02-2016 дата публикации

THERAPEUTIC CURCUMIN DERIVATIVES

Номер: US20160039734A1
Принадлежит:

Curcumin analogues and methods are provided for treatment of disease. 1. A method of treating a subject afflicted with Alzheimer's disease or type 2 diabetes , the method comprising administering to the subject a therapeutically effective amount of a composition comprising a curcumin derivative selected from the group consisting of:{'sup': 1', '2', '1', '2, '(a) Ar-L-Ar(Formula I); wherein L is a divalent linking group comprising an alkylene or an alkenylene comprising 3, 4, 5, 6, or 7 backbone carbon atoms, wherein one or more of the backbone carbon atoms form part of a carbonyl or secondary alcohol; and Arand Arare each independently aryl groups; and'}{'sup': 1', '11', '1', '11, '(b) Ar-L-R(Formula IV); wherein L is a divalent linking group comprising an alkylene or an alkenylene comprising 3, 4, 5, 6, or 7 backbone carbon atoms, wherein one or more of the backbone carbon atoms form part of a carbonyl or secondary alcohol; Aris an aryl group; and Ris an alkyl group, a heterocyclic group, or a hydrogen.'}221.-. (canceled)22. A method of treating a subject afflicted with cancer or a precancerous condition , the method comprising administering to the subject a therapeutically effective amount of a composition comprising a curcumin derivative selected from the group consisting of:{'sup': 1', '2', '1', '2, '(a) Ar-L-Ar(Formula I); wherein L is a divalent linking group comprising an alkylene or an alkenylene comprising 3, 4, 5, 6, or 7 backbone carbon atoms, wherein one or more of the backbone carbon atoms form part of a carbonyl or secondary alcohol; and Arand Arare each independently aryl groups; and'}{'sup': 1', '11', '1', '11, '(b) Ar-L-R(Formula IV); wherein L is a divalent linking group comprising an alkylene or an alkenylene comprising 3, 4, 5, 6, or 7 backbone carbon atoms, wherein one or more of the backbone carbon atoms form part of a carbonyl or secondary alcohol; Aris an aryl group; and Ris an alkyl group, a heterocyclic group, or a hydrogen.'}2328.-. ( ...

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09-02-2017 дата публикации

NITRIFICATION INHIBITORS

Номер: US20170036969A1
Принадлежит:

The present invention relates to novel nitrification inhibitors of formula I. Moreover, the invention relates to the use of these novel nitrification inhibitors for reducing nitrification, as well as agrochemical mixtures and compositions comprising the nitrification inhibitors. Further encompassed by the present invention are methods for reducing nitrification comprising the treatment of plants, soil and/or loci with said nitrification inhibitors, and methods for treating a fertilizer or a composition by applying said nitrification inhibitor. 116-. (canceled)18: The compound of claim 17 , wherein in said compound of formula I claim 17 , A is phenyl or a 6-membered hetaryl claim 17 , preferably phenyl claim 17 , wherein the aromatic ring may in each case be unsubstituted or may be partially or fully substituted by substituents claim 17 , which are independently of each other selected from R.19: The compound of claim 17 , wherein in said compound of formula I claim 17 , Rand Rboth represent hydrogen.20: The compound of claim 17 , wherein in said compound of formula I claim 17 , Ris hydrogen claim 17 , C-C-haloalkyl or ethinylhydroxymethyl claim 17 , and preferably Ris hydrogen.21: The compound of claim 17 , wherein in said compound of formula I claim 17 , R claim 17 , if present claim 17 , is{'sup': a', 'b', 'c', '1', 'c', '1', 'c', '1', 'c', '1', 'a', 'b', '2', '1', '2', '1', 'a', 'b', 'g', 'd', 'e', 'f, 'sub': 2', '2', '1', '6', '2', '6', '1', '4', '1', '4', '2', '4', '1', '2', '2', '4, '(i) halogen, CN, NRR, OR, C(═Y)R, C(═Y)OR, C(═Y)SR, C(═Y)NRR, YC(═Y)R, YC(═Y)NRR, NRN═C(R)(R), S(═O)R, NO, C-C-alkyl, C-C- C-C-haloalkyl, C-C-alkoxy, C-C-alkynyl-C-C-hydroxyalkyl, C-C-alkynyloxy;'}{'sub': 2', '4', '2', '4', '1', '4', '2', '4, 'sup': 1', 'c', '2', '1', 'c, '(ii) C-C-alkenylene-C(═Y)R, C-C-alkenylene-Y—C(═Y)R, wherein the C-C-alkylene or C-C-alkenylene chain may in each case be unsubstituted or may be partially or fully substituted by CN or halogen;'}{'sup': 'h', '( ...

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24-02-2022 дата публикации

COMPOUNDS HAVING S1P5 RECEPTOR AGONISTIC ACTIVITY

Номер: US20220055986A1
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

A compound represented by the general formula (V) 3. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein{'sub': 3', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'sup': 6', '6', '6, 'L is (1) —O—(C2-7 alkyl), (2) —O—(C2-7 alkenyl), (3) —O—(C2-7 alkynyl), (4) —O—(C1-5 alkylene)-OCH, (5) —O—(C1-4 alkylene)-OCHCH, (6) —CHO—(C1-6 alkyl), (7) —CHO—(C2-6 alkenyl), (8) —CHO—(C2-6 alkynyl), (9) —CHCHO—(C1-5 alkyl), (10) —CHCHO—(C2-5 alkenyl), (11) —CHCHO—(C2-5 alkynyl), (12) —S—(C2-7 alkyl), (13) —S—(C2-7 alkenyl), (14) —S—(C2-7 alkynyl), (15) —NR—(C2-7 alkyl), (16) —NR—(C2-7 alkenyl), (17) —NR—(C2-7 alkynyl), (18) a C3-8 alkyl group, (19) a C3-8 alkenyl group, or (20) a C3-8 alkynyl group,'}{'sup': '6', 'Rrepresents a hydrogen atom or a C1-4 alkyl group, and'}wherein a carbon atom in each group is optionally substituted with 1 to 3 halogen atoms.4. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein L is a branched or linear chain group in which the number of atoms in the main chain is 4 to 7.5. The compound or a pharmaceutically acceptable salt thereof according to claim 2 , wherein{'sub': 3', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'sup': 6', '6', '6, 'L is (1) —O—(C3-6 alkyl), (2) —O—(C3-6 alkenyl), (3) —O—(C3-6 alkynyl), (4) —O—(C1-4 alkylene)-OCH, (5) —O—(C1-3 alkylene)-OCHCH, (6) —CHO—(C2-5 alkyl), (7) —CHO—(C2-5 alkenyl), (8) —CHO—(C2-5 alkynyl), (9) —CHCHO—(C1-4 alkyl), (10) —CHCHO—(C2-4 alkenyl), (11) —CHCHO—(C2-4 alkynyl), (12) —S—(C3-6 alkyl), (13) —S—(C3-6 alkenyl), (14) —S—(C3-6 alkynyl), (15) —NR—(C3-6 alkyl), (16) —NR—(C3-6 alkenyl), (17) —NR—(C3-6 alkynyl), (18) a C4-7 alkyl group, (19) a C4-7 alkenyl group, or (20) a C4-7 alkynyl group,'}{'sup': '6', 'Rrepresents a hydrogen atom or a C1-4 alkyl group, and'}wherein a carbon atom in each group is optionally substituted with 1 to 3 halogen atoms.6. The compound or a pharmaceutically acceptable salt thereof ...

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25-02-2021 дата публикации

CURCUMIN ANALOGUES AS ZINC CHELATORS AND THEIR USES

Номер: US20210053905A1
Принадлежит:

This invention provides a compound having the structure 134-. (canceled)43. The method of wherein Ris methoxy claim 40 , —ORor —NRR claim 40 , wherein Ris H claim 40 , Calkyl claim 40 , Calkenyl claim 40 , or Calkynyl;{'sub': 16', '17', '1-10', '2-10', '2-10, 'Rand Rare each, independently, H, Calkyl, Calkenyl, Calkynyl, aryl, heteroaryl, or heterocyclyl;'}or a salt thereof.44. The method of claim 40 , wherein{'sub': 14', '16', '17, 'Ras —NRR,'}{'sub': 16', '17, 'wherein Rand Rare each, independently, H or aryl;'}{'sub': 2', '3', '4', '5', '6', '7', '8', '9', '10', '11', '28', '29', '28, 'R, R, R, R, R, R, R, R, R, and Rare each independently, H, —NRR, or —OR,'}{'sub': 28', '29', '1-10, 'wherein Rand Rare each, H or Calkyl;'}or a salt thereof.45. The method of claim 40 , wherein{'sub': '14', 'Ris —NH-phenyl;'}{'sub': 2', '8', '9', '7', '10', '11, 'R, R, R, R, R, and Rare each H;'}{'sub': 3', '4', '8', '9', '3, 'R, R, R, and Rare each, independently, H, —OH, or —OCH; or a salt thereof.'}48. The method of wherein the matrix metalloproteinase (MMP) is MMP-1 claim 35 , MMP-2 claim 35 , MMP-3 claim 35 , MMP-7 claim 35 , MMP-8 claim 35 , MMP-9 claim 35 , MMP-12 claim 35 , MMP-13 claim 35 , or MMP-14.50. The method of wherein the cytokine is TNF-α claim 49 , IL-1β claim 49 , MCP-1 claim 49 , or IL-6.51. The method of wherein the production of a cytokine is induced by an endotoxin claim 49 , lipopolysaccharide (LPS) claim 49 , a hormone claim 49 , or a cholesterol complex.54. The method of wherein the population of cells is a population of human cells. This application claims the benefit of U.S. Provisional Application No. 61/216,392, filed May 15, 2009, the content of which is hereby incorporated by reference in its entirety.Throughout this application, certain publications are referenced in parentheses. Full citations for these publications may be found immediately preceding the claims. The disclosures of these publications in their entireties are hereby incorporated by ...

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22-02-2018 дата публикации

CYCLOBENZOINS

Номер: US20180050974A1
Автор: Ji Qing, MILJANIC Ognjen
Принадлежит: UNIVERSITY OF HOUSTON SYSTEM

One-step cyanide-catalyzed benzoin condensations for synthesizing shape persistent cyclobenzoin macrocycles. Selected dialdehydes, and cyanide salts are reacted in aqueous solvents to form such cyclobenzoin macrocycles. 2. The method of claim 1 , wherein said solvent is an alcohol.3. The method of claim 2 , wherein said alcohol is selected from the group consisting of 2-methoxyethanol; ethanol; methanol; propanol claim 2 , butanol claim 2 , pentanol isomers claim 2 , and glycols.4. The method of claim 2 , wherein said solvent is in a 1:1 molar ratio with HO.5. The method of claim 1 , wherein said dialdehyde is selected from the group consisting of isophthaldehyde; tetraphthaldehyde; phthaldehyde claim 1 , and aromatic analogs thereof claim 1 , wherein one or more substituted or unsubstituted aromatic or hetoroaromatic rings claim 1 , and/or triple bonds are inserted between two formyl groups.6. The method of wherein said dialdehyde is at a concentration of between 0.1M to 1M.7. The method of claim 5 , wherein said dialdehyde is isophthaldehyde in a concentration of about 0.5M.8. The method of claim 5 , wherein said dialdehyde is tetraphthaldehyde in a concentration of about 0.17M.9. The method of claim 1 , wherein said reacting a dialdehyde and a cyanide salt comprises refluxing under nitrogen gas at a temperature of about 100° C. for about 48 hrs.10. The method of claim 1 , wherein said cyanide salt is selected from the group consisting of NaCN claim 1 , cyanide salts of metals; and thiazolium salts.11. The method of claim 7 , wherein said cyclobenzoin macrocycle is cyclotribenzoin or a cyclotetrabenzoin.12. (canceled)13. The method of claim 1 , wherein said cyclobenzoin macrocycle forms a microporous three-dimensional organic framework claim 1 , or a one dimensional nanotube channel.14. (canceled)15. The method of claim 1 , wherein said cyclobenzoin macrocycle is porous.16. The method of claim 12 , wherein said cyclotetrabenzoin comprises a Langmuir surface area ...

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10-03-2022 дата публикации

Compounds, Compositions, and Methods for use in Treating Autophagy-Associated Disorders

Номер: US20220073444A1
Автор: Henderson Ian
Принадлежит:

The invention provides compounds and methods of treating autophagy mediated diseases and disorders and related pharmaceutical compositions, diagnostics, screening techniques and kits. 2. The compound of claim 1 , wherein the compound is selected from the group consisting of:N-(3,4-dimethoxypheny)-1,8-Dioxa-3-aza-2,4-dihydro-2H-5-phenyl-anthracen-7-one,N-(3,4-dimethoxybenzyl)-1,8-Dioxa-3-aza-2,4-dihydro-2H-5-methyl-anthracen-7-one,N-benzyl-1,8-Dioxa-3-aza-3,4dihydro-2H-anthracen-7-one series, andN-(3,4-dimethoxypheny)-1,8-Dioxa-3-aza-2,4-dihydro-2H-5-methyl-anthracen-7-one.4. The compound of claim 3 , wherein the compound is selected from the group consisting of:3-(4-methoxyphenyl)-1,5-bis(2-methoxyphenyl)-1,5-pentanedione,3-(4-hydroxyphenyl)-1,5-bis(2-methoxyphenyl)-1,5-pentanedione,3-(4-methoxyphenyl)-1,5-bis (2-methoxyphenyl)-1,5-pentanedione,3-(4-allyloxyphenyl)-1,5-bis(2-methoxyphenyl)-1,5-pentanedione,3-(4- hydroxyphenyl)-1,5-bis(2-methoxyphenyl)-1,5-pentanedione,3-(3,4,5-trimethoxymethoxyphenyl)-1,5-bis(2-methoxyphenyl)-1,5-pentanedione,3-(4-allyloxyphenyl)-1,5-bis(2-methoxyphenyl)-1,5-pentanedione, and3-(4-dimethylaminophenyl)-1,5- bis(2-methoxyphenyl)-1,5-pentanedione.5. A method of using the compound of to treat an autophagy-mediated disease state or condition.6. A method of using the compound of to treat an autophagy-mediated disease state or condition.7. The method claim 5 , wherein the autophagy-mediated disease state or condition is cancer claim 5 , lysosomal storage diseases claim 5 , Alzheimer's disease claim 5 , Parkinson's disease and other ataxias such as Huntington's disease; a chronic inflammatory disease such as Crohn's disease claim 5 , diabetes I claim 5 , diabetes II claim 5 , metabolic syndrome claim 5 , an inflammation-associated metabolic disorder claim 5 , liver disease claim 5 , renal disease claim 5 , cardiovascular disease claim 5 , muscle degeneration and atrophy claim 5 , frailty in aging claim 5 , spinal cord injury claim 5 , ...

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20-02-2020 дата публикации

Sweetness and Taste Improvement of Steviol Glycoside and Mogroside Sweeteners with Dihydrochalcones

Номер: US20200054058A1
Принадлежит:

Compositions and consumables comprising certain sweeteners and at least one dihydrochalcone of Formula I are provided herein, wherein the at least one sweetener is selected from certain steviol glycoside and/or mogroside sweeteners in sweetening amounts. The at least one dihydrochalcone enhances the sweetness of the consumable and optionally modulates one or more taste attributes to make the consumable taste more like a sucrose-sweetened consumable. Methods of enhancing the sweetness of a consumable, methods of making a consumable taste more like a sucrose-sweetened consumable and methods of preparing consumables are also detailed herein. 2. The beverage of claim 1 , wherein the dihydrochalcone is selected from hesperetin dihydrochalcone claim 1 , phloretin claim 1 , neohesperidin dihydrochalcone claim 1 , hesperetin dihydrochalcone-4′-β-D-glucoside and combinations thereof.3. The beverage of claim 1 , wherein the steviol glycoside is selected from the group consisting of rebaudioside M claim 1 , rebaudioside D claim 1 , rebaudioside A claim 1 , rebaudioside N claim 1 , rebaudioside O claim 1 , rebaudioside E claim 1 , steviolmonoside claim 1 , steviolbioside claim 1 , rubusoside claim 1 , dulcoside B claim 1 , dulcoside A claim 1 , rebaudioside B claim 1 , rebaudioside G claim 1 , stevioside claim 1 , rebaudioside C claim 1 , rebaudioside F claim 1 , rebaudioside I claim 1 , rebaudioside H claim 1 , rebaudioside L claim 1 , rebaudioside K claim 1 , rebaudioside J claim 1 , rebaudioside M2 claim 1 , rebaudioside D2 claim 1 , rebaudioside S claim 1 , rebaudioside T claim 1 , rebaudioside U claim 1 , rebaudioside V claim 1 , rebaudioside W claim 1 , rebaudioside Z1 claim 1 , rebaudioside Z2 claim 1 , rebaudioside IX claim 1 , enzymatically glucosylated steviol glycosides and combinations thereof.4. The beverage of claim 1 , wherein the mogroside is selected from the group consisting of grosmogroside I claim 1 , mogroside IA claim 1 , mogroside IE claim 1 , 11- ...

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15-05-2014 дата публикации

Hydroformylation method having improved catalyst stability in reaction

Номер: US20140135533A1
Принадлежит: LG Chem Ltd

Disclosed is a hydroformylation method having improved catalyst stability in a reaction. Advantageously, provided is a hydroformylation method in which a specific α,β-unsaturated carbonyl compound is incorporated during a hydroformylation reaction to prevent alkyl phosphite decomposed from a phosphite ligand from acting as a catalyst poison, thereby improving a yield of reaction and inhibiting decomposition of ligand and catalyst.

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28-02-2019 дата публикации

INDENE DERIVATIVES AND USES THEREOF

Номер: US20190062298A1
Принадлежит:

The present invention relates to compounds of formula (I): 2. The compound according to claim 1 , wherein Rand R claim 1 , independently of each other claim 1 , are hydrogen claim 1 , hydroxyl claim 1 , alkyl claim 1 , alkoxy claim 1 , methoxy-acetate claim 1 , phosphate claim 1 , valine claim 1 , Gly-Ser claim 1 , —OC(O)CHOC(O)CH claim 1 , —OC(O)CHOCH claim 1 , —OCHC(O)C(CH) claim 1 , —OCHC(O)NHor —OCHC(O)OH.3. The compound according to claim 1 , wherein Rand R claim 1 , together with the carbon atoms to which they are attached claim 1 , form a 5 to 6-membered ring with one or two ring carbons replaced independently by oxygen or nitrogen.4. The compound according to claim 1 , wherein Ris hydroxyl.5. The compound according to claim 1 , wherein R is hydroxyl.6. The compound according to claim 1 , wherein both Rand Rare hydroxyl.7. The compound according to claim 1 , wherein Ris alkoxy.8. The compound according to claim 1 , wherein Ris alkoxy.9. The compound according to claim 1 , wherein both Rand Rare alkoxy.10. The compound according to claim 1 , wherein Ris hydrogen claim 1 , hydroxyl claim 1 , halogen claim 1 , cyano claim 1 , —COOH claim 1 , —C(O)NH claim 1 , —C(O)CHCH claim 1 , —C(O)-alkoxy claim 1 , alkyl claim 1 , alkoxy claim 1 , halo-lower alkyl claim 1 , carboxyl claim 1 , amide claim 1 , ester or nitrile.11. The compound according to claim 1 , wherein Ris amide.12. The compound according to claim 1 , wherein Ris —CF.13. The compound according to claim 1 , wherein Ris alkenyl.14. The compound according to claim 1 , wherein Ris alkenyl optionally mono or bi-substituted independently with hydrogen claim 1 , halogen claim 1 , hydroxyl claim 1 , —OCH-phenyl claim 1 , cycloalkyl claim 1 , —OCH-halophenyl or —OCH-phenylhaloalkyl.16. A pharmaceutical composition claim 1 , comprising a therapeutically effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.17. A ...

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10-03-2016 дата публикации

METHYLENE BETA-DIKETONE MONOMERS, METHODS FOR MAKING METHYLENE BETA-DIKETONE MONOMERS, POLYMERIZABLE COMPOSITIONS AND PRODUCTS FORMED THEREFROM

Номер: US20160068618A1
Принадлежит:

The present teachings are directed at 1,1-disubstituted alkene monomers (e.g., methylene beta-diketone monomers), methods for producing the same, and compositions and products formed therefrom. In the method for producing the monomer, a beta-diketone is preferably reacted with a source of formaldehyde in a modified Knoevenagel reaction optionally in the presence of an acidic or basic catalyst, and optionally in the presence of an acidic or non-acidic solvent, to form reaction complex. The reaction complex may be an oligomeric complex. The reaction complex is subjected to vaporization in order to isolate the monomer. The monomer(s) may be employed in compositions and products, including monomer-based products (e.g., inks, adhesives, coatings, sealants or reactive molding) and polymer-based products (e.g., fibers, films, sheets, medical polymers, composite polymers and surfactants). 2. The polymerizable composition of claim 1 , wherein the amount of ketals in the polymerizable composition is less than about 10 ppm and the amount of latent acid-forming impurities in the polymerizable composition is less than about 10 ppm.3. The polymerizable composition of including a stabilizing amount of at least one stabilizer selected from the group consisting of an acidic stabilizer claim 1 , a vapor phase stabilizer claim 1 , and a free radical stabilizer.4. The polymerizable composition of claim 3 , wherein the polymerizable composition is an adhesive claim 3 , a coating claim 3 , or a sealant.5. The polymerizable composition of claim 3 , wherein the at least one stabilizer includes the acidic stabilizer selected from trifluoromethane sulfonic acid claim 3 , maleic acid claim 3 , methane sulfonic acid claim 3 , difluoro acetic acid claim 3 , trichloroacetic acid claim 3 , phosphoric acid claim 3 , dichloroacetic acid claim 3 , and chlorodifluoro acid.6. The polymerizable composition of claim 3 , wherein the at least one stabilizer includes the vapor phase stabilizer selected ...

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27-02-2020 дата публикации

Anti-Inflammatory Composition

Номер: US20200062684A1
Принадлежит:

It is an object of the present invention to provide a composition having an anti-inflammatory action. The present invention relates to an anti-inflammatory composition, a prostaglandin E2 production inhibitory composition, and a nitric oxide production inhibitory composition, which are useful as food or beverage or pharmaceutical products.The present invention also relates to a novel compound having a prostaglandin E2 production inhibitory activity and a nitric oxide production inhibitory activity.Prostaglandin E2 (PGE2) is generated in leukocytes (macrophages), mast cells, endothelial cells, platelets and the like. Arachidonic acid existing as a structural component of a cell membrane phospholipid is cleaved by phospholipase, and is passed through a cyclooxygenase pathway, thereby synthesizing PGE2. In the process of inflammation, the aforementioned pathway is activated, and generation of PGE2 is thereby increased.PGE2 released from specific cells acts on target cells present in the vicinity thereof, and induces an inflammatory reaction in the target cells. PGE2 is one chemical mediator for amplifying an inflammatory reaction in an inflamed site, and activates the inflammatory reaction in the inflamed site.Nitric oxide (NO) is generated in the process of inflammation by type II nitric oxide synthase (iNOS) of leukocytes (macrophages) induced by an inflammatory cytokine or bacterial endotoxin (Non Patent Literature 1). Excessively generated NO is converted to peroxynitrous acid, which then exhibits a cytotoxic action such as DNA damage or LDL oxidation (Non Patent Literature 2). Thus, it is important to suppress excessive generation of NO due to inflammation. In addition, since NO activates an intracellular signal pathway for promoting inflammation, such as an NF-κB pathway (Non Patent Literature 3), suppression of NO generation is also important for exhibiting an anti-inflammatory action (Patent Literature 1).Inflammation is provoked by stimulating factors such as ...

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11-03-2021 дата публикации

METHOD FOR PRODUCING 2-ACETYL-4H,9H-NAPHTHO[2,3-B]FURAN-4,9-DIONE

Номер: US20210070724A1
Принадлежит: Sumitomo Dainippon Pharma Co., Ltd.

The invention addresses the problem of providing a method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione that is suited to industrial production. The invention provides a method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione by reacting 3-bromo-3-buten-2-one and 2-hydroxy-1,4-naphthoquinone in the presence of a solvent, then obtaining crystals of 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione by adding an alcohol-based solvent and/or water to the reaction system, and treating the crystals by using a specific adsorbent in the presence of a solvent. 139-. (canceled)40. A compound of 2-acetyl-4H ,9H-naphtho[2 ,3-b]furan-4 ,9-dione which is obtained by a process comprising the following step (d):(d) dissolving 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione in a non-alcohol-based solvent C, followed by adding an adsorbent to purify the 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione.41. The compound according to claim 40 , further comprising the following step (e) after the step (d):(e) removing the adsorbent used in the step (d) and evaporating the non-alcohol-based solvent C.42. The compound according to claim 41 , further comprising the following step (f) after the step (e):(f) crystallizing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione obtained in the step (e) by adding at least one crystallization solvent D selected from the group consisting of a hydrocarbon-based solvent, an alcohol-based solvent, an acid-based solvent, an ester-based solvent, an ether-based solvent, and water, to obtain 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione.43. The compound according to claim 42 , further comprising the following step (g) after the step (f):(g) slurrying 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione obtained in the step (f) with ethyl acetate to form a crystal of 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione.44. The compound according to claim 40 , wherein the non-alcohol-based solvent C used in the step (d) is at least one selected from the group consisting ...

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05-06-2014 дата публикации

Fungicidal substituted 2-[2-halogenalkyl-4-(phenoxy)-phenyl]-1-[1,2,4]triazol-1-yl-ethanol compounds

Номер: US20140155262A1
Принадлежит: BASF SE

The present invention relates to substituted 2-[2-halogenalkyl-4-(phenoxy)-phenyl]-1-[1,2,4]triazol-1-yl-ethanol compounds of formula I as defined in the description, and the N-oxides, and salts thereof, their preparation and intermediates for preparing them. The invention also relates to the use of these compounds for combating harmful fungi and seed coated with at least one such compound and also to compositions comprising at least one such compound. 113-. (canceled)15. The compound according to claim 14 , wherein Ris hydrogen claim 14 , C-C-alkyl claim 14 , allyl claim 14 , C-C-alkynyl claim 14 , cyclopropyl claim 14 , phenyl claim 14 , benzyl claim 14 , phenylethenyl or phenylethynyl.16. The compound according to claim 14 , wherein Ris hydrogen claim 14 , C-C-alkyl claim 14 , allyl claim 14 , propargyl or benzyl.17. The compound according to claim 14 , wherein m is 1 claim 14 , 2 or 3 and Ris selected from F and Cl.18. The compound according to claim 14 , wherein n=0 claim 14 , Ris hydrogen claim 14 , Ris 4-Cl and Ris selected from the group consisting of H claim 14 , CH claim 14 , CHCH claim 14 , CHCHCH claim 14 , CHC≡C—CH claim 14 , CHC≡CH claim 14 , isopropyl claim 14 , cyclopropyl and CF claim 14 , and compounds wherein n=0 claim 14 , Ris CH claim 14 , Ris 4-Cl and Ris selected from H claim 14 , CH claim 14 , CHCH claim 14 , isopropyl and cyclopropyl claim 14 , and the compound wherein n=0 claim 14 , Ris H claim 14 , Ris 2 claim 14 ,4-Cland Ris H claim 14 , and the compound wherein n=0 claim 14 , Ris H claim 14 , Ris 4-F and Ris CH claim 14 , and the compounds wherein n=0 claim 14 , Ris CH claim 14 , Ris 4-Cl and Ris selected from CHCH claim 14 , and CHCH═CH claim 14 , and the compounds wherein n=0 claim 14 , Ris methyl-propargyl claim 14 , Ris 4-Cl and Ris selected from CHCH claim 14 , and CHC≡CH.22. An agrochemical composition comprising an auxiliary and at least one compound of formula I claim 14 , as defined in claim 14 , an N-oxide or an agriculturally ...

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24-03-2016 дата публикации

METHOD FOR THE PREPARATION OF alpha-SUBSTITUTED ACRYL ALDEHYDES

Номер: US20160083409A1
Принадлежит:

The invention discloses simple and rapid method for the preparation of α-substituted acryl aldehydes. More particularly, the invention discloses a method for the preparation of α-substituted acryl aldehydes via a gold-catalysed [1,3] rearrangement of the allenyl ethers with a record turnover frequency of 4600 hat 0.05 mol % of the catalyst concentration in homogeneous gold(I) catalysis. The α-substituted acryl aldehydes synthesized by the instant process are used as building blocks in organic synthesis. 2. The process according to claim 1 , wherein the Au(I) complex is selected from the group consisting of AuCl; AuBr claim 1 , AuCl(PPh); AuCl(PMe); AuCl(Biphenyl(tBu)).3. The process according to claim 2 , wherein claim 2 , the Au(I) complex is AuCl(PPh).4. The process according to claim 1 , wherein claim 1 , the Au(I) complex is used in an amount of 0.05 mol % in homogeneous catalysis.5. The process according to claim 1 , wherein claim 1 , the process comprises addition of a silver salt to facilitate the [1 claim 1 , 3] O→C rearrangement.6. The process according to claim 1 , wherein claim 1 , the silver salt is selected from the group consisting of AgSbF; AgOAc; AgOTf and AgNTf.7. The process according to claim 1 , wherein claim 1 , the silver salt is AgSbF.8. The process according to claim 1 , wherein claim 1 , the molar ratio of Au [I] complex and additive is in the range of 1:6 to 1:3 claim 1 , more preferably the molar ratio is 1:3.10. The process according to claim 1 , wherein claim 1 , the α-substituted acryl aldehydes of Formula 2 comprises(i) 2-(4-Methoxybenzyl)acrylaldehyde;(ii) 2-((4-Methoxyphenyl)(phenyl)methyl)acrylaldehyde;(iii) 3-(4-Methoxyphenyl)-2-methylene-4-phenylbutanal;(iv) 3-(4-Methoxyphenyl)-2-methyleneheptanal′(v) 2-(2,4-Dimethoxybenzyl)acrylaldehyde;(vi) 2-((2,4-Dimethoxyphenyl)(phenyl)methyl)acrylaldehyde;(vii) 2-(3,4-Dimethoxybenzyl)acrylaldehyde;(viii) 2-((3,4-Dimethoxyphenyl)(phenyl)methyl)acrylaldehyde;(ix) 3-(3,4-Dimethoxyphenyl)-2- ...

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26-03-2015 дата публикации

Protective Effects of Curcumin Against Hemorrhagic Stroke Injury

Номер: US20150087705A1
Принадлежит:

Disclosed herein are compounds, compositions and methods for preventing and treating diseases such as intracerebral hemorrhage, cancer, or conditions associated with damaged cells, activated lymphocytes, or microbial products. The disclosed compounds are curcumin analogs. The curcumin analogs possess anti-inflammatory and antioxidant properties, which in part, reduce AP-1 and NF-κB activity. 2. A compound of claim 1 , wherein{'sub': 1', '2', '3', '4', '5', '6', '7', '8', '9', '10, 'R, R, R, R, R, R, R, R, R, and Rare independently selected from the group consisting of hydrogen, alkyl, halogen, alkoxy, carboxyl, alkoxycarbonyl, haloalkyl, haloalkloxy, and haloalkylamino, and'}{'sub': '11', 'Ris independently selected from the group consisting of hydrogen, alkyl, halogen, alkoxy, carboxyl, alkoxycarbonyl, ester, and alkyl ester.'}3. A compound according to claim 1 , wherein{'sub': 1', '2', '3', '4', '5', '6', '7', '8', '9', '10', '1', '4, 'R, R, R, R, R, R, R, R, Rand Rare independently selected from the group consisting of hydrogen, alkyl, halogen, and C-Calkoxy, and'}{'sub': '11', 'Ris selected from the group consisting of hydrogen, alkyl, alkoxy, carboxyl, alkoxycarbonyl, ester, and alkyl ester.'}5. A pharmaceutical composition comprising one or more of the compounds claim 1 , pharmaceutically acceptable salt claim 1 , prodrug claim 1 , clathrate claim 1 , tautomer or solvate thereof according to and a pharmaceutically acceptable excipient.6. The composition of claim 5 , wherein the one or more compounds are present in an effective amount to reduce the expression of proinflammatory mediators claim 5 , tumor necrosis factor-α claim 5 , interleukin-6 claim 5 , or interleukin-1β.7. The composition of claim 5 , wherein the one or more compounds are present in an effective amount to reduce disruption of the blood-brain barrier.8. The composition of claim 5 , wherein the one or more compounds are present in an effective amount to increase neurological outcome scores ...

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31-03-2022 дата публикации

MOISTURE-CURABLE POLYOLEFIN FORMULATION

Номер: US20220098432A1
Принадлежит:

A moisture-curable polyolefin formulation comprising a (hydrolyzable silyl group)-functional polyolefin prepolymer and a condensation-cure catalyst system comprising and/or made from mixture of a compound that is a carboxamidine or a guanidine and a compound that is a cobalt acetylacetonate or a zinc acetylacetonate, wherein each compound independently is unsubstituted or substituted. Also, methods of making and using same, a cured polyolefin made therefrom, and articles containing or made from same. Also, condensation-cure catalyst systems useful therein. 1. A moisture-curable polyolefin formulation comprising:(A) a (hydrolyzable silyl group)-functional polyolefin prepolymer; and{'sub': ['2', '3', '2'], '#text': '(B) a condensation-cure catalyst system comprising a mixture made by contacting a compound that is a carboxamidine or a guanidine and is unsubstituted or substituted (collectively called “(aza)carboxamidine”) with a compound that is a cobalt acetylacetonate coordination complex or a zinc acetylacetonate coordination complex, wherein each acetylacetonate independently is unsubstituted or substituted with from 1 to 5 alkyl groups, wherein each alkyl group is unsubstituted (collectively called “Co,Zn (alkyl)acetylacetonate”); wherein the Co,Zn (alkyl)acetylacetonate is selected from a cobalt(II) ((alkyl)acetylacetonate), a cobalt(III) ((alkyl)acetylacetonate), and a zinc(II) ((alkyl)acetylacetonate);'}wherein the amount of (A) is from 79.0 to 99.99 weight percent (wt %) and the amount of (B) is from 21.0 to 0.01 wt %, respectively, of the moisture-curable polyolefin formulation; andwherein the (B) condensation-cure catalyst system is characterized by an (aza)carboxamidine/Co,Zn (alkyl)acetylacetonate molar ratio of from 15 to 0.15.2. The moisture-curable polyolefin formulation of wherein the (A) (hydrolyzable silyl group)-functional polyolefin prepolymer is characterized by any one of limitations (i) to (iii): (i) each hydrolyzable silyl group is ...

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12-03-2020 дата публикации

Sacubitril intermediate and preparation method thereof

Номер: US20200079721A1

The present invention relates to a sacubitril intermediate and a preparation method thereof. The sacubitril intermediate disclosed herein can be prepared by a deprotection reaction of a compound. In addition, the intermediate can be used as a raw material to synthesize sacubitril.

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25-03-2021 дата публикации

REACTIVE DISTILLATION FOR FORMING SURFACTANTS

Номер: US20210087124A1
Принадлежит: Sironix Renewables, Inc.

Devices, systems, and methods for forming furan based surfactants by reactive distillation are disclosed herein. Various embodiments can provide a consolidated reaction process that uses reactive distillation to synthesize oleo-furan surfactant molecules and intermediates by combining reaction and separation steps into a single reaction unit or a number of connected reaction units. The single reaction unit or a number of connected reaction units can include a catalyst bed and act to separate reaction side products at opposing ends of the unit or units. 1. A method of forming a surfactant , the method comprising:providing a fatty acid at a second fluid medium space within a distillation column device, the distillation column device including a first catalyst bed containing a first catalyst material within the distillation column, the second fluid medium space being above the first catalyst bed and a first fluid medium space being below the first catalyst bed within the distillation column device; andperforming an acylation of the fatty acid with a furan-based structure at the first catalyst bed to form an alkylfuran ketone at the first fluid medium space within the distillation column device.2. The method of claim 1 , wherein the furan-based structure is selected from the group consisting of: furan and methylfuran.3. The method of claim 1 , wherein the first catalyst material is selected from the group consisting of: H-Bea claim 1 , HY claim 1 , Ultrastable-Y claim 1 , MCM-41 claim 1 , SBA-15 claim 1 , tungstated zirconia claim 1 , sulfated zirconia claim 1 , amorphous silica claim 1 , Nafion NR-50 claim 1 , Nafion SAC-13 claim 1 , or Nafion deposited on a support such as silica.4. The method of claim 1 , wherein the fatty acid provided at the second fluid medium space is a fatty acid anhydride claim 1 , and wherein performing the acylation comprises performing the acylation of the fatty acid anhydride with the furan-based structure at the first catalyst bed.5. The ...

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25-03-2021 дата публикации

COMPOUNDS HAVING S1P5 RECEPTOR AGONISTIC ACTIVITY

Номер: US20210087141A1
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

A compound represented by the general formula (V) 3. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein{'sub': 3', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'sup': 6', '6', '6, 'L is (1) —O—(C2-7 alkyl), (2) —O—(C2-7 alkenyl), (3) —O—(C2-7 alkynyl), (4) —O—(C1-5 alkylene)-OCH, (5) —O—(C1-4 alkylene)-OCHCH, (6) —CHO—(C1-6 alkyl), (7) —CHO—(C2-6 alkenyl), (8) —CHO—(C2-6 alkynyl), (9) —CHCHO—(C1-5 alkyl), (10) —CHCHO—(C2-5 alkenyl), (11) —CHCHO—(C2-5 alkynyl), (12) —S—(C2-7 alkyl), (13) —S—(C2-7 alkenyl), (14) —S—(C2-7 alkynyl), (15) —NR—(C2-7 alkyl), (16) —NR—(C2-7 alkenyl), (17) —NR—(C2-7 alkynyl), (18) a C3-8 alkyl group, (19) a C3-8 alkenyl group, or (20) a C3-8 alkynyl group, and'}{'sup': '6', 'Rrepresents a hydrogen atom or a C1-4 alkyl group,'}provided that a carbon atom in each group may be substituted with 1 to 13 halogen atoms.4. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein L is a branched or linear chain group in which the number of atoms in the main chain is 4 to 7.5. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein{'sub': 3', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'sup': 6', '6', '6, 'L is (1) —O—(C3-6 alkyl), (2) —O—(C3-6 alkenyl), (3) —O—(C3-6 alkynyl), (4) —O—(C1-4 alkylene)-OCH, (5) —O—(C1-3 alkylene)-OCHCH, (6) —CHO—(C2-5 alkyl), (7) —CHO—(C2-5 alkenyl), (8) —CHO—(C2-5 alkynyl), (9) —CHCHO—(C1-4 alkyl), (10) —CHCHO—(C2-4 alkenyl), (11) —CHCHO—(C2-4 alkynyl), (12) —S—(C3-6 alkyl), (13) —S—(C3-6 alkenyl), (14) —S—(C3-6 alkynyl), (15) —NR—(C3-6 alkyl), (16) —NR—(C3-6 alkenyl), (17) —NR—(C3-6 alkynyl), (18) a C4-7 alkyl group, (19) a C4-7 alkenyl group, or (20) a C4-7 alkynyl group, and'}{'sup': '6', 'Rrepresents a hydrogen atom or a C1-4 alkyl group,'}provided that a carbon atom in each group may be substituted with 1 to 13 halogen atoms.6. The compound or a pharmaceutically acceptable salt thereof ...

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25-03-2021 дата публикации

NOVEL CURCUMINOID-INSPIRED SYNTHETIC COMPOUNDS AS ANTI-TUMOR AGENTS

Номер: US20210087208A1
Автор: Laali Kenneth K.

Novel CUR- and CUR-BFcompounds as well as novel bis and mono-NSAID/CUR-BFand NSAID/CUR hybrids exhibiting anti-tumor properties are presented. CUR compounds bearing fluorinated moieties with selective fluorine introduction into the α-carbonyl moiety as well as CUR-BFadducts and CURs with diverse substitution patterns in the phenyl rings including fluorinated substituents (SCF, OCF, and F) and/or bulky activating groups (OMe, OAc, and OBz) are presented. Fluorinated aryl-pyrazoles and isoxazoles as well as novel CUR and CUR-BFcompounds with monocyclic aromatic and bicyclic-heteroaromatic lateral rings, bearing fluorine(s), OCF, CF, and SCFgroups, and their alpha-carbonyl-fluorinated analogs, as well as their pyrazole and isoxazole derivatives are presented. The CUR-pyrazoles embody analogs that are fluorinated at the phenyl-pyrazole moiety. The hybrids, compounds, and their derivatives exhibited exceptional cytotoxic and anti-proliferative activity against several cancer cell-lines. The hybrid NSAID/CUR compounds also exhibited exceptional anti-inflammatory activity over NSAID or curcumin alone. 2. The composition of claim 1 , wherein Ris O associated with a difluoroboron adduct.3. The composition of claim 2 , wherein Ris O associated with a difluoroboron adduct.5. The method of claim 4 , wherein Ris O associated with a difluoroboron adduct.6. The method of claim 5 , wherein Ris O associated with a difluoroboron adduct.7. The method of claim 6 , wherein Ris p-OH.8. The method of claim 7 , wherein the at least one cancer cell is a colorectal cancer cell.10. The composition of claim 9 , further comprising at least one deuterated substituent on the aryl.11. The composition of claim 10 , wherein the at least one deuterated substitution is a plurality of deuterated substitutions.12. The composition of claim 11 , wherein the plurality of deuterated substitutions is at the meta positions. This application is a continuation in part of and claims priority to currently pending ...

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02-04-2015 дата публикации

AGRICULTURAL CHEMICALS

Номер: US20150094474A1
Принадлежит:

The present invention relates to derivatives of compounds which are known to be of use in the field of agriculture. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more changes one or more of which may be considered to represent a change of oxidation state relative to the groups in the original compound. We refer to these compounds generally as redox derivatives. The compounds are of use as insecticides, herbicides and insect repellents. 3. A compound according to claim 1 , wherein X is CHor NH.4. A compound according to claim 1 , wherein Yand Ytogether form ═O.612.-. (canceled)19. A compound according to claim 16 , wherein W is COR. The present invention relates to derivatives of compounds which are known to be of use in the field of agriculture. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more changes one or more of which may be considered to represent a change of oxidation state relative to the groups in the original compound. We refer to these compounds generally as redox derivatives.Given the global increase in demand for food, there is an international need for new treatments to reduce food crop losses to disease, insects and weeds. Over 40% of crops are lost before harvest, and 10% post harvest, worldwide. Losses have actually increased since the mid-1990s.A new threat contributing to this is the emergence of chemical-resistant organisms, for example glyphosate-resistant weeds in USA.Many current crop protection products are harmful and may cause acute and chronic health effects in those who are exposed, ranging from irritation of the skin and eyes to ...

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06-04-2017 дата публикации

USE OF VANILLIN DERIVATIVES AS PRESERVING AGENTS, PRESERVING PROCESS, COMPOUNDS AND COMPOSITION

Номер: US20170096381A1
Автор: Dalko Maria
Принадлежит:

The present invention relates to the use, in a cosmetic, dermatological or pharmaceutical composition, of at least one compound of formula (I): 2. The process according to claim 1 , wherein said compound is present in an amount of from 0.01% to 5% by weight claim 1 , relative to the weight of the composition.3. The process according to claim 1 , wherein said compound is present in an amount of from 0.1% to 2.5% by weight claim 1 , relative to the weight of the composition.4. The process according to claim 1 , wherein the composition does not contain any preserving agent in addition to said compound.5. The process according to claim 1 , wherein the composition does not contain a paraben.6. The process according to claim 1 , wherein the composition is in the form of a product for making up the skin of the face claim 1 , body or lips; an aftershave gel or lotion;a hair-removing cream; a body hygiene composition such as a shower gel or a shampoo; a pharmaceutical composition; a solid composition such as a soap or a cleansing bar; an aerosol composition also comprising a pressurized propellant; a hair-setting lotion, a hair-styling cream or gel, a dyeing composition, a hair-restructuring lotion, a permanent-wave composition, a lotion or a gel for combating hair loss; or a composition for oro-dental use.7. The process according to claim 1 , wherein the composition comprises a physiologically acceptable medium which comprises at least one ingredient selected from the group consisting of silicone fatty substances selected from the group consisting of silicone oils claim 1 , gums and waxes; non-silicone fatty substances selected from the group consisting of oils claim 1 , pastes and waxes of plant claim 1 , mineral claim 1 , animal and/or synthetic origin; and wherein the composition optionally further comprises an active cosmetic agent.8. The process according to claim 1 , wherein the composition comprises a physiologically acceptable medium comprising at least one ...

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23-04-2015 дата публикации

ORGANIC COMPOUNDS

Номер: US20150111811A1
Автор: Kraft Philip
Принадлежит:

Branched optionally unsaturated ketones particularly useful in providing typical and characteristic orris facets to perfume compositions. 2. The compound according to wherein the dotted line together with the bond between C-3 and C-4 and the bond between C-5 and C-6 represent double bonds claim 1 , and both double bonds are in (E)-configuration.3. The compound according to selected from the group consisting of 5-tert-butylocta-3 claim 1 ,5-dien-2-one claim 1 , 5-(tert-pentyl)octa-3 claim 1 ,5-dien-2-one claim 1 , 5-(tert-butyl)-7-methylnona-3 claim 1 ,5-dien-2-one claim 1 , 5-tert-butyloctan-2-one claim 1 , 6 claim 1 ,6-dimethyl-5-propyloctan-2-one claim 1 , and 5-tert-butyl-7-methylnonan-2-one.4. The compound according to selected from (3E claim 2 ,5E)-5-tert-butylocta-3 claim 2 ,5-dien-2-one claim 2 , (3E claim 2 ,5E)-5-(tert-pentyl)octa-3 claim 2 ,5-dien-2-one claim 2 , and (3E claim 2 ,5E)-5-(tert-butyl)-7-methylnona-3 claim 2 ,5-dien-2-one.6. The method according to claim 5 , wherein the compound of formula (I) wherein the dotted line together with the bond between C-3 and C-4 and the bond between C-5 and C-6 represent double bonds claim 5 , and both double bonds are in (E)-configuration.8. The perfumed product according to wherein the product is selected from fine perfumery claim 7 , fabric care claim 7 , household products claim 7 , beauty and personal care products claim 7 , and air care products. The present invention relates to novel compounds possessing olfactory properties reminiscent of orris oil. The invention furthermore refers to a method for their production, and to flavour and fragrance compositions containing these.With a price of well above US$75,000, orris absolute constitutes probably the most expensive perfumery raw material still in use. Irones, α-irone (A), β-irone (B), and γ-irone (B) as depicted below, are the major constituents of orris oil and determine its typical odour, albeit there is some controversy about which irone stereoisomers ...

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19-04-2018 дата публикации

A METHOD FOR PREPARING OPTICALLY ACTIVE CARBONYL COMPOUND

Номер: US20180105477A1
Принадлежит:

The present invention discloses a method for preparing optically active carbonyl compound, comprising the following steps: under the catalysis of chiral amine salt and transition metal catalysts, with hydrogen and catalytic amount of dihydropyridine compound as hydrogen source, use α, β-unsaturated aldehydes or α, β-unsaturated troponoid compounds to conduct asymmetric catalytic reaction to obtain the optically active carbonyl compound. This method comes in moderate reaction condition, simple operation, and catalytic amount of dihydropyridine compounds usage, the target product is easy to be separated and purified from the reaction system, and the metal catalyst can be recycled, it is economical. 2. The method for preparing an optically active carbonyl compound according to claim 1 , which is characterized in that: in the R claim 1 , Rand R claim 1 , alkyl is alkyl containing 1 to 30 carbon atoms;heteroaryl is aromatic heterocyclic aryls containing 3 to 9 carbon atoms;alkoxy is cyclo-alkoxy or linear or branched alkoxys containing 1 to 30 carbon atoms, and these alkoxys can be substituted by fluorine, chlorine, bromine, iodine, hydroxy or aryl;acylaminos are acylaminos containing 1 to 20 carbon atoms.3. The method for preparing an optically active carbonyl compound according to claim 2 , which is characterized in that: the heteroaryl is: 2-furyl claim 2 , 2-pyrryl claim 2 , 2-thienyl claim 2 , 2-pyridyl claim 2 , 2-indolyl claim 2 , 3-furyl claim 2 , 3-pyrryl claim 2 , 3-thienyl claim 2 , 3-pyridyl claim 2 , or 3-indolyl;the alkoxies are: methoxyl, ethyoxyl, n-propoxyethyl, isopropoxy, n-butoxy, isobutoxy, 2-butoxy, tert-butoxy, n-pentyloxy, 2-pentyloxy, 2-pentyloxy, tert-pentyloxy, n-hexyloxy, cyclopropoxy, cyclobutoxy, cyclopentyloxy, cyclohexyloxy, heptyloxy, octyloxy, nonyloxy, decyloxy, undecyloxy, dodecyloxy, tridecyloxy, tetradecyloxy, pentadecyloxy, hexadecyloxy, heptadecyloxy, octadecyloxy, nonadecyloxy, eicosyloxy, phenylmethoxy, 1-phenylethoxy, or 2- ...

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02-04-2020 дата публикации

MARMELIN ANALOGS AND METHODS OF USE IN CANCER TREATMENT

Номер: US20200102264A1
Принадлежит: The University of Kansas

A pharmaceutical composition can include: a marmelin analog compound, and a pharmaceutically acceptable carrier having the compound. The compound can be present in a therapeutically effective amount to treat or inhibit a disease state. The disease state can be cancer. The cancer can be selected from brain cancers, head and neck cancers, thyroid cancers, gastrointestinal cancers, esophageal cancers, stomach cancers, pancreatic cancers, liver cancers, colo-rectal cancers, lung cancers, kidney cancers, prostate cancers, bladder cancers, testicular cancers, breast cancers, ovarian cancers, cervical cancers, and melanomas. The carrier includes a cyclodextrin, which may form a complex with the compound. The compounds and compositions can be used to treat or inhibit progression of cancers. Colo-rectal, bladder, and prostate cancers are examples of some of the cancers that can be treated with the marmelin analog compounds. 2. The compound of claim 1 , wherein:{'sup': '2', 'Rincludes one or more of a hydrogen, halogens, hydroxyls, alkoxys, straight aliphatics, branched aliphatics, cyclic aliphatics, substituted aliphatics, unsubstituted aliphatics, saturated aliphatics, unsaturated aliphatics, aromatics, polyaromatics, substituted aromatics, hetero-aromatics, amines, primary amines, secondary amines, tertiary amines, aliphatic amines, thios, sulfhydryls, phosphors, carbonyls, carboxyls, amides, esters, amino acids, peptides, polypeptides, derivatives thereof, substituted or unsubstituted, or combinations thereof.'}3. The compound of claim 1 , wherein Rincludes one or more of hydrogen claim 1 , C-Calkyl claim 1 , C-Calkenyl claim 1 , C-Calkynyl claim 1 , C-Caryl claim 1 , C-Calkaryl claim 1 , C-Caralkyl claim 1 , halo claim 1 , hydroxyl claim 1 , sulfhydryl claim 1 , C-Calkoxy claim 1 , C-Calkenyloxy claim 1 , C-Calkynyloxy claim 1 , C-Caryloxy claim 1 , acyl claim 1 , C-Calkylcarbonyl (—CO-alkyl) claim 1 , C-Carylcarbonyl (—CO-aryl) claim 1 , acyloxy (—O-acyl) claim 1 , C- ...

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11-04-2019 дата публикации

RENEWABLE KETONE WAXES WITH UNIQUE CARBON CHAIN LENGTHS AND POLARITIES

Номер: US20190106371A1
Принадлежит:

The present disclosure provides ketone waxes, methods of forming ketone waxes, and compositions comprising ketone waxes. In at least one embodiment, a ketone wax is provided. The ketone wax includes about 50 wt % or greater C-Cketone content; about 50 wt % or greater of the ketone wax has a boiling point of 961° F. or greater; and a paraffins content of less than about 10 wt %, as determined by 2-dimensional gas chromatography. In at least one embodiment, a method for forming a C-Cketone wax includes exposing a feed stock to a basic catalyst under conditions suitable for coupling unsaturated carbon chains from the feed to form a composition including a ketone wax, oligomerizing the ketone wax to form a ketone wax having C-Cketone wax, and distilling and/or extracting the oligomerized ketone wax to provide a C-Cketone wax of the present disclosure. 2. The ketone wax of claim 1 , wherein the ketone wax has a 1R-naphthene equivalent of from about 0.1 wt % to about 20 wt % claim 1 , as determined by 2-dimensional gas chromatography.3. The ketone wax of claim 1 , wherein the ketone wax has a 1R-naphthene equivalent of from about 1 wt % to about 10 wt % claim 1 , as determined by 2-dimensional gas chromatography.4. The ketone wax of claim 1 , wherein the ketone wax has a paraffins content of from about 0 wt % to about 5 wt % claim 1 , as determined by 2-dimensional gas chromatography.5. The ketone wax of claim 1 , wherein the ketone wax has a 2R-naphthene equivalent of from about 0.1 wt % to about 20 wt % claim 1 , as determined by 2-dimensional gas chromatography.6. The ketone wax of claim 1 , wherein the ketone wax has a 2R-naphthene equivalent of from about 5 wt % to about 10 wt % claim 1 , as determined by 2-dimensional gas chromatography.7. The ketone wax of claim 1 , wherein the ketone wax has a 1R-aromatic equivalent of from about 50 wt % to about 99.9 wt %.8. The ketone wax of claim 1 , wherein the ketone wax has a 1R-aromatic equivalent of from about 80 wt % to ...

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13-05-2021 дата публикации

COMPOUNDS AND MATRICES FOR USE IN BONE GROWTH AND REPAIR

Номер: US20210138117A1
Принадлежит: HUMAN BIOMOLECULAR RESEARCH INSTITUTE

Compositions of small molecules, matrices, and isolated cells including methods of preparation, and methods for differentiation, trans-differentiation, and proliferation of animal cells into the osteoblast cell lineage were described. Examples of osteogenic materials that were administered to cells or co-cultured with cells are represented by compounds of Formula II, IV, and VI independently or preferably in combination with a matrix to afford bone cells. Small molecule-stimulated cells were also combined with a matrix, placed with a cellular adhesive or material carrier and implanted to a site in an animal for bone repair. Matrix pretreated with compounds of Formula II, IV, and VI were also used to cause cells to migrate to the matrix that is of use for therapeutic purposes. 11. The composition of any one of - , wherein the isolated cells capable of differentiating into bone cells are isolated human bone marrow-derived mesenchymal stem cells , human mesenchymal stem cells of adipose tissue , human mesenchymal stem cells of blood , human mesenchymal stem cells of bone allograft or autograft tissues , human mesenchymal stem cells of dental pulp , human pericytes , human myoblasts , and human chondrocytes , human osteoprogenitor cells , urine stem cells , or their respective progenitor cells such as stem cell isolated from amniotic fluid or cord blood , embryonic stem cells , and induced pluripotent stem cells.12. The composition of - wherein the calcium phosphate matrix is a tricalcium phosphate ceramic or is oseoinductive.13. The composition of - wherein the calcium phosphate matrix is a tricalcium phosphate ceramic or is oseoinductive.14. The composition of compound 8-10 wherein the calcium phosphate matrix is a tricalcium phosphate ceramic or is oseoinductive.15. The compositions of any one of - further comprising a calcium phosphate matrix , wherein the compound is covalently associated onto the calcium phosphate matrix.16. The compositions of any one of - ...

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13-05-2021 дата публикации

NOVEL BENZYLIDENEACETONE DERIVATIVE AND USE THEREOF

Номер: US20210139414A1
Принадлежит:

The present invention relates to novel benzylideneacetone derivatives or uses thereof, more specifically, the present invention relates to a pharmaceutical composition for preventing or treating, or food composition for ameliorating a cancer or a bone disease comprising a compound defined by Formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. 2. The compound defined by Formula 1 or a pharmaceutically acceptable salt thereof of claim 1 , wherein R1 is one selected from the group consisting of —OH claim 1 , methyl claim 1 , methoxy claim 1 , —F claim 1 , and —SH;{'sub': 1-4', '1-4, 'R2 is one selected from the group consisting of —OH, —SH, Cstraight or branched alkyl, Cstraight or branched alkoxy, halogen, allyloxy, benzyloxy, aryloxy having one or more selected from the group consisting of hetero atoms and substituents, and heterocycloalkyl of 3 to 7 atoms having one or more hetero atoms, wherein the hetero atoms consist of O, N and S;'}{'sub': '2', 'R3 is methyl or —NH.'}3. The compound defined by Formula 1 or a pharmaceutically acceptable salt thereof of claim 2 , wherein the compound defined by Formula 1 is selected from the group consisting of the following compounds:(1) (E)-4-(3-hydroxy-4-methylphenyl)but-3-en-2-one;(2) (E)-4-(4-fluoro-3-hydroxyphenyl)but-3-en-2-one;(3) (E)-4-(4-hydroxy-3-methoxyphenyl)-3-buten-2-one;(4) (E)-4-(3-hydroxy-4-methoxyphenyl)-3-buten-2-one;(5) (E)-4-(3-fluoro-4-hydroxyphenyl)-3-buten-2-one;(6) (E)-3-(3-hydroxy-4-methylphenyl)acrylamide;(7) (E)-3-(4-fluoro-3-hydroxyphenyl)acrylamide;(8) (E)-4-(4-mercapto-3-hydroxyphenyl)but-3-en-2-one;(9) (E)-4-(4-hydroxy-3-mercaptophenyl)but-3-en-2-one;(10) (E)-4-(3-hydroxy-4-isopropoxyphenyl)but-3-en-2-one;(11) (E)-4-(4-(benzyloxy)-3-hydroxyphenyl)but-3-en-2-one;(12) (E)-4-(4-(allyloxy)-3-hydroxyphenyl)but-3-en-2-one;(13) (E)-4-(3-hydroxy-4-(4-methylpiperazine-1-yl)phenyl)but-3-en-2-one;(14) (E)-4-(3-hydroxy-4-(pyrrolidine-1-yl)phenyl)but-3-en-2-one;{'img': {'@id': 'CUSTOM ...

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03-05-2018 дата публикации

5-substituted-5-hydroxy-5-aryl-3-oxo-pentanoate derivatives and their enantiopure forms

Номер: US20180118648A1

The present invention relates to novel tertiary alcohol derivatives substituted with aryl and trifluoromethyl, and optical isomers thereof. In addition, the present invention also relates to methods for the preparation and use as enantiomer recognition agent thereof. The present invention provides pharmaceutical composition and use as therapeutically active substance thereof.

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25-08-2022 дата публикации

Phospholipase-a2 inhibitors for the prevention of cancer metastasis

Номер: US20220265576A1
Принадлежит: Coegin Pharma AS

A compound of formula (I)R-L-CO—X   (I)wherein R is a C10-24 unsaturated hydrocarbon group optionally interrupted by one or more heteroatoms or groups of heteroatoms selected from S, O, N, SO, SO2, said hydrocarbon group comprising at least 4 non-conjugated double bonds;L is a linking group forming a bridge of 1 to 5 atoms between the R group and the carbonyl CO wherein L comprises at least one heteroatom in the backbone of the linking group; andX is an electron withdrawing group; or a salt thereof;for use in the prevention of metastasis in cancer, especially breast cancer.

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14-05-2015 дата публикации

GGA DERIVATIVES

Номер: US20150133431A1
Автор: LOOK Gary C.
Принадлежит: COYOTE PHARMACEUTICALS, INC.

This invention relates to geranylgeranyl acetone (GGA) derivatives, pharmaceutical compositions comprising GGA derivatives and the use of GGA derivatives. 23. The compound of claim 21 , wherein R claim 21 , Rand Rare methyl.2423. A pharmaceutical composition comprising a compound of any one of - and a pharmaceutically acceptable excipient. This application claims priority under 35 U.S.C. section 119(e)(1) to U.S. provisional application No. 61/845,302, filed Jul. 11, 2013, which is incorporated herein in its entirety by reference.This invention relates generally to GGA derivatives, compositions comprising and methods for using the same.Geranylgeranyl acetone is an acyclic isoprenoid compound with a retinoid skeleton that has been shown to induce expression of heat shock proteins in various tissue types. GGA is a known anti-ulcer drug used commercially and in clinical situations.GGA has also been shown to exert cytoprotective effects on a variety of organs, such as the eye, brain, and heart (See for example Ishii Y., et al., Invest Ophthalmol V is Sci 2003; 44:1982-92; Tanito M, et al., J Neurosci 2005; 25:2396-404; Fujiki M, et al., J Neurotrauma 2006; 23:1164-78; Yasuda H, et al., Brain Res 2005; 1032:176-82; Ooie T, et al., Circulation 2001; 104:1837-43; and Suzuki S, et al., Kidney Int 2005; 67:2210-20). The effects and cytoprotective benefits of GGA in these settings is less understood as is the relationship of isomers of GGA to these cytoprotective benefits. There is a need for GGA derivatives for use in these and other therapies.In various aspects, provided herein are GGA derivatives, such as those of Formulas (I) and (VIII)-(XXII), and sub-formulas thereof, compositions, preferably pharmaceutical formulations, thereof, processes of their syntheses, and their use, wherein Formulas (I) and (VIII)-(XXII) are shown below:or pharmaceutically acceptable salt thereof; wherein Qx is Q, Q, or Q, and all the variables for Formulas (I), (VIII), (IX), and (XI) are as ...

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11-05-2017 дата публикации

Polymorphs and amorphous forms of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoromethyl)sulfinyl]-1h-pyrazole-3-carbonitrile

Номер: US20170129860A1
Автор: Sharona Zamir
Принадлежит: Adama Makhteshim Ltd

The present invention relates to novel crystalline polymorphs, solvate pseudomorphs and amorphous form of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoromethyl)sulfinyl]-1H-pyrazole-3-carbonitrile (fipronil). The present invention also provides methods for preparing the novel polymorphs, pseudomorphs and amorphous form, as well as insecticidal or pesticidal compositions comprising same, and methods of use thereof as pesticidal agents.

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02-05-2019 дата публикации

METHODS FOR PRODUCING CYCLIC AND ACYCLIC KETONES

Номер: US20190127292A1
Принадлежит:

Provided herein are methods for producing cyclic and acyclic ketones from trimerization and dimerization of alkyl ketones, including for example methyl ketones. Such cyclic and acyclic ketones may be suitable for use as fuel and lubricant precursors, and may be hydrodeoxygenated to form their corresponding cycloalkanes and alkanes. Such cycloalkanes and alkanes may be suitable for use as fuels, including jet fuels, and lubricants. 14-. (canceled)8. The method of claim 5 , wherein the catalyst comprises at least one metal and a basic support.9. The method of claim 8 , wherein at least one metal is a transition metal.10. The method of claim 5 , wherein the catalyst has one or more of the following properties:(i) a pKa between 8 to 16;{'sub': 2', '2', '2, '(ii) a COdesorption of at least 50° C., wherein COdesorption is carried out by adsorbing COto the catalyst at room temperature and heating up to 773 K;'}(iii) at least one basic oxygen atom; and(iv) a proton affinity of at least 700 kJ/mol;(v) is solid;(vi) is acidic; and(vii) is amphoteric.11. The method of claim 5 , wherein the catalyst comprises:a metal oxide;a non-metal oxide;a supported alkali metal ion;an ionic liquid supported metal oxide; oran aluminophosphate,or any combinations thereof.12. The method of claim 5 , wherein the catalyst comprises:an apatite;a sepiolite;a chrysotile;a zeolite;a mesoporous silica;a hydrotalcite; ora synthetic talc,or any combinations thereof.13. The method of claim 5 , wherein the catalyst comprises an alkali oxide claim 5 , an alkaline earth oxide claim 5 , a non-metal oxide claim 5 , a transition metal oxide claim 5 , or a rare metal oxide claim 5 , or any combinations thereof.14. The method of claim 5 , wherein the catalyst comprises Mg claim 5 , Ti claim 5 , Sr claim 5 , Ca claim 5 , Si claim 5 , Al claim 5 , La claim 5 , Zr claim 5 , Na claim 5 , K claim 5 , Pd claim 5 , Cu claim 5 , or Pd—Cu alloy claim 5 , or any combinations thereof.15. The method of claim 5 , wherein ...

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02-05-2019 дата публикации

Aryl beta diketones and their use as odorants

Номер: US20190127305A1
Принадлежит: Givaudan SA

The present invention refers to aryl beta diketones of the formula (I) wherein Y, R 1 , R 2 and R 3 have the meaning R 1 is selected from the group consisting of hydrogen, C 1 -C 4 alkyl, hydroxyl, methoxy, CF 3 and F; R 2 is selected from the group consisting of methyl and ethyl; R 3 is selected from the group consisting of methyl and ethyl; and Y is a bivalent residue selected from the group consisting of —C(O)—; —CH 2 ═CH 2 —C(O)—; —CR I R II —C(O)—, wherein R I and R II are independently selected from hydrogen and methyl; and —CHR III —CHR IV —C(O)—, wherein R III and R IV are independently selected from hydrogen and methyl with the proviso, that R III ═R IV are hydrogen or either R III or R IV is methyl. The invention further refers to fragrance compositions and fragranced articles comprising them.

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01-09-2022 дата публикации

Modular Chemical Probe For Detection Of Amino Acid Citrulline In Physiological Samples

Номер: US20220276257A1
Принадлежит:

An improved chemical probe for the detection of the amino acid citrulline combines: 1) a reactive head formed of 1,3-dicarbonyl moiety that reacts with a citrulline side chain in an improved manner compared to currently used 1,2-dicarbonyl moieties; and 2) a modular action of the probe where citrulline side chains are labeled first using reactive heads described above, and attachment of a read-out subunit or tag, be it a fluorophore, a nanoparticle, or an antigen is performed separately. The modular nature of the chemical probe increases the sensitivity of the probes due to their smaller size. Additionally, the chemical probes of the present disclosure allow the same sample to be analyzed using a variety of read-out methods. 1. A chemical probe for the detection of the amino acid citrulline comprising a reactive head , wherein the reactive head is formed of 1 ,3-dicarbonyl moiety.3. The probe of wherein the reactive head includes a triple bond opposite the 1 claim 1 ,3-dicarbonyl moeity.4. The probe of wherein the 1 claim 3 ,3-dicarbonyl moiety includes a ketone-ketone claim 3 , a ketone-aldehyde claim 3 , or an aldehyde-aldehyde structure.11. The probe of further comprising a detection tag bonded to reactive head.12. The probe of wherein the detection tag comprises:a. a probe linker attached to the reactive head; andb. a read-out tag attached to the probe linker.13. The probe of wherein the probe tinker is an azide-modified probe linker.14. The probe of wherein the read-out tag is a fluorescent read-out tag.16. The probe of wherein the read-out tag is a biotinylated read-out tag.18. The probe of wherein the read-out tag is a superparamagnetic nanoparticle read-out tag.20. A method for detecting the presence of the amino acid citrulline in proteins from biological samples claim 12 , the method comprising the steps of:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a) providing the detection probe of ;'}b) reacting the reactive head of the probe with citrulline to ...

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17-05-2018 дата публикации

FUNCTIONALIZED PHOTOINITIATORS

Номер: US20180134645A1
Принадлежит: Schmid Rhyner AG

The present invention provides mixtures of compounds and compounds having the formula: 138-. (canceled)40: The mixture as recited in claim 39 , wherein no single compound of formula (IV) is present in an amount of more than 45 wt.-% with respect to the total weight of the compounds of formula (IV) in the mixture.41: The mixture as recited in claim 39 , wherein the total amount of compounds of formula (IV) present in the mixture comprising the compounds of formula (IV) having at least one of p and q being 5 or larger is 20 wt.-% or less.42: The mixture as recited in claim 39 , wherein the weight of the compounds of formula (IV) with respect to a total weight of the mixture is from 10 to 100 wt.-%.45: The mixture as recited in claim 39 , wherein L is missing.47: The mixture as recited in claim 46 , wherein no single compound of formula (VI) is present in the amount of more than 45 wt.-% with respect to the total weight of compounds of formula (VI).50: The mixtures as recited in claim 46 , wherein the total amount of compounds of formula (VI) present in the mixtures which comprise compounds of formula (IV) having at least one of p and q being 5 or larger is 20 wt.-% or less.52: The photo-curable composition as recited in claim 51 , wherein the at least one ethylenically unsaturated components is selected from mono(meth)acrylates claim 51 , aliphatic or aromatic urethane (meth)acrylates claim 51 , polyether (meth)acrylates claim 51 , polyester (meth)acrylates and epoxy (meth)acrylates.53: The photo-curable composition as recited in claim 52 , wherein the mono(meth)acrylates are selected from the group consisting of methylacrylate claim 52 , methyl methacrylate claim 52 , ethyl acrylate claim 52 , ethyl methacrylate claim 52 , ethylhexyl acrylate claim 52 , ethylhexyl methacrylate claim 52 , hydroxyethyl acrylate claim 52 , hydroxyethyl methacrylate claim 52 , isobornyl acrylate claim 52 , isobornyl methacrylate claim 52 , butyl acrylate claim 52 , and butyl methacrylate ...

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28-05-2015 дата публикации

Low volatile reactive malodor counteractives and methods of use thereof

Номер: US20150147287A1

The present invention relates to compounds for counteracting thiol- and amine-based malodors in consumer, industrial and textile products. Also disclosed are a consumer, industrial or textile product containing one of these compounds and a method for counteracting a thiol- or amine-based malodor using these compounds.

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30-04-2020 дата публикации

NOVEL ORGANOLEPTIC COMPOUNDS

Номер: US20200131451A1
Принадлежит: International Flavors & Fragrances Inc.

The present invention relates to novel compounds and their use as fragrance materials. 2. The compound of selected from the group consisting of:(E)-1-((1R,6R)-4,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-one;(E)-1-((1S,6S)-3,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-one;(E)-1-((1R,6S)-4,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-one;(E)-1-((1S,6R)-3,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-one;(E)-1-((1R,6R)-4,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-ol;(E)-1-((1S,6S)-3,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-ol;(E)-1-((1R,6S)-4,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-ol;(E)-1-((1S,6R)-3,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-ol; anda mixture thereof.3. The compound of claim 2 , wherein the compound is the mixture of (E)-1-((1R claim 2 ,6R)-4 claim 2 ,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-one claim 2 , (E)-1-((1S claim 2 ,6S)-3 claim 2 ,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-one claim 2 , (E)-1-((1R claim 2 ,6S)-4 claim 2 ,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-one and (E)-1-((1S claim 2 ,6R)-3 claim 2 ,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-one.5. The fragrance formulation of claim 4 , wherein the compound is selected from the group consisting of:(E)-1-((1R,6R)-4,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-one;(E)-1-((1S,6S)-3,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-one;(E)-1-((1R,6S)-4,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-one;(E)-1-((1S,6R)-3,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-one;(E)-1-((1R,6R)-4,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-ol;(E)-1-((1S,6S)-3,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-ol;(E)-1-((1R,6S)-4,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-ol;(E)-1-((1S,6R)-3,6-dimethylcyclohex-3-en-1-yl)-2-methylpent-1-en-3-ol; anda mixture thereof.6. The fragrance formulation of claim 5 , wherein the compound is the mixture of (E)-1-((1R claim 5 ,6R)-4 claim 5 ,6- ...

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04-06-2015 дата публикации

Geranyl Geranyl Acetone Analogs and Uses Thereof

Номер: US20150152076A1
Принадлежит:

The invention relates to novel therapeutic compounds, more in particular to biologically active analogs and uses thereof as medicament, for instance for the treatment of atrial fibrillation. Provided is a compound of the general formula (formula I) wherein Ris H or a saturated or unsaturated aliphatic moiety comprising 1 to 8 C-atoms; and X is selected from the group consisting of moieties X, X, X, X, Xand X. Exemplary uses include the prevention or therapeutic treatment of a HSF1-mediated disease. 141-. (canceled)43. The compound or salt according to claim 42 , wherein Ris H.44. The compound or salt according to claim 42 , wherein X is X.45. The compound or salt according to claim 44 , wherein Ris H or C-Calkyl.46. The compound or salt according to claim 44 , wherein at least one of Rand Ris C-Calkyl claim 44 , optionally substituted with one or more of halogen claim 44 , oxo claim 44 , hydroxyl claim 44 , — CN claim 44 , alkoxy claim 44 , amino claim 44 , amido claim 44 , phenyl claim 44 , benzyl claim 44 , hetero-aryl claim 44 , cyclo-alkyl claim 44 , heterocycloalkyl claim 44 , —C(═O)O—R3a claim 44 , wherein R3a is H claim 44 , C-Calkyl or CH-aryl.47. The compound or salt according to claim 44 , wherein the compound is selected from compounds 28 claim 44 , 22 claim 44 , 76 claim 44 , 69 claim 44 , 70 claim 44 , 24 claim 44 , 23 claim 44 , 84 claim 44 , 78 claim 44 , 89 claim 44 , 82 claim 44 , and 125 shown in .48. The compound or salt according to claim 42 , wherein X is X.49. The compound or salt according to claim 48 , wherein Rand/or Ris H or wherein Rand/or Ris a substituted or unsubstituted C-Cstraight chain alkyl.50. The compound or salt according to claim 48 , wherein the compound is selected from compounds 62 claim 48 , 64 claim 48 , and 65 shown in .51. The compound or salt according to claim 42 , wherein X is X.52. The compound or salt of claim 51 , wherein the compound is compound 111 shown in .53. The compound or salt according to claim 42 , wherein ...

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25-05-2017 дата публикации

MARMELIN ANALOGS AND METHODS OF USE IN CANCER TREATMENT

Номер: US20170144965A1
Принадлежит:

A pharmaceutical composition can include: a marmelin analog compound, and a pharmaceutically acceptable carrier having the compound. The compound can be present in a therapeutically effective amount to treat or inhibit a disease state. The disease state can be cancer. The cancer can be selected from brain cancers, head and neck cancers, thyroid cancers, gastrointestinal cancers, esophageal cancers, stomach cancers, pancreatic cancers, liver cancers, colo-rectal cancers, lung cancers, kidney cancers, prostate cancers, bladder cancers, testicular cancers, breast cancers, ovarian cancers, cervical cancers, and melanomas. The carrier includes a cyclodextrin, which may form a complex with the compound. The compounds and compositions can be used to treat or inhibit progression of cancers. Colorectal, bladder, and prostate cancers are examples of some of the cancers that can be treated with the marmelin analog compounds. 2. The compound of claim 1 , wherein:{'sup': 1', '2', '3', '4', '5, 'at least one of R, R, R, or R, or Rindependently includes one or more of a hydrogen, halogens, hydroxyls, alkoxys, straight aliphatics, branched aliphatics, cyclic aliphatics, substituted aliphatics, unsubstituted aliphatics, saturated aliphatics, unsaturated aliphatics, aromatics, polyaromatics, substituted aromatics, hetero-aromatics, amines, primary amines, secondary amines, tertiary amines, aliphatic amines, thios, sulfhydryls, phosphors, carbonyls, carboxyls, amides, esters, amino acids, peptides, polypeptides, derivatives thereof, substituted or unsubstituted, or combinations thereof.'}3. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , R claim 1 , R claim 1 , or Rindependently includes one or more of hydrogen claim 1 , C-Calkyl claim 1 , C-Calkenyl claim 1 , C-Calkynyl claim 1 , C-Caryl claim 1 , C-Calkaryl claim 1 , C-Caralkyl claim 1 , halo claim 1 , hydroxyl claim 1 , sulfhydryl claim 1 , C-Calkoxy claim 1 , C-Calkenyloxy claim 1 , C-Calkynyloxy claim 1 ...

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15-09-2022 дата публикации

COMPOSITION FOR PREVENTING OR TREATING BACTERIAL INFECTIOUS DISEASE COMPRISING 4-GINGEROL DERIVATIVE COMPOUND AS ACTIVE INGREDIENT

Номер: US20220289657A1
Принадлежит:

The present invention relates to a 4-gingerol derivative compound, or a racemate, isomer, or pharmaceutically acceptable salt thereof, the compound being capable of inhibiting biofilm formation and production of virulence factors. The 4-gingerol derivative compound according to the present invention has binding affinity to RhlR and corresponding RhlR antagonism activity that are significantly improved, and therefore can effectively inhibit biofilm formation and production of virulence factors. Furthermore, various bacterial infectious diseases caused by biofilms can be fundamentally prevented or treated by using a pharmaceutical composition comprising the 4-gingerol derivative compound, or a racemate, isomer, or pharmaceutically acceptable salt thereof as an active ingredient. 4. The compound of claim 3 , wherein the gingerol derivative compound represented by Formula 2 is any one selected from combinations of X claim 3 , Y claim 3 , and Z:(1) X═OMe, Y═OH, Z═H(2) X═H, Y═H, Z═H(3) X═OMe, Y═H, Z═H(4) X═H, Y═OH, Z═H(5) X═OH, Y═H, Z═H(6) X═H, Y═OMe, Z═H(7) X═H, Y═F, Z═H(8) X═H, Y═Cl, Z═H(9) X═H, Y=Me, Z═H{'sub': '2', '(10) X═H, Y═NMe, Z═H'}(11) X═OH, Y═OH, Z═H(12) X═OMe, Y═OMe, Z═H(13) X═F, Y═OH, Z═H(14) X═OEt, Y═OH, Z═H(15) X═F, Y═F, Z═H(16) X=Me, Y=Me, Z═H(17) X═OMe, Y═F, Z═H(18) X═F, Y═H, Z═OMe5. The compound of claim 1 , which inhibits biofilm formation and virulence factor production.6Pseudomonas aeruginosa, SalmonellaShigellaVibrio parahaemolyticus, Vibrio choreae, Escherichia coliCampylobacter jejuni, Clostridium difficile, Clostridium perfringens, Yersinia enterocolitica, Helicobacter pylori, Entemoeba histolytica, Bacillusu cereus, Clostridium botulinum, Haemophilus influenzae, Streptococcus pneumoniae, Chlamidia pneumoniae, Legionella pneumoniae, Branhamella catarrhalis, Mycobacterium tuberculosis, Mycoplasma pneumoniaeStreptococcusStreptococcus pyogenesCorynebacterium diphtheriae, Bordetella pertussis, Chramidia psittaciStaphylococcus aureusEscherichia coli, ...

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16-05-2019 дата публикации

Compounds and compositions for biofilm prevention

Номер: US20190144368A1
Принадлежит: Inhibio As

The present invention relates to compounds and compositions for effective biofilm prevention. Particularly, the invention provides compositions comprising certain cyclic ketones found to be efficient in preventing bacterial biofilm formation.

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31-05-2018 дата публикации

PHENOL DERIVATIVES TO TREAT CANCER

Номер: US20180148427A1

The present invention relates to compounds of general formula (I) 115-. (canceled)19. The compound according to claim 16 , wherein Ris hydrogen.20. The compound according to claim 16 , wherein Ris hydrogen or chloro.21. The compound according to claim 16 , wherein Ris hydrogen and Ris CHO.22. The compound according to claim 16 , wherein Ris hydrogen.23. The compound according to claim 16 , wherein hydroxyl protecting groups for R claim 16 , R claim 16 , R claim 16 , R claim 16 , R claim 16 , R claim 16 , R claim 16 , Rand Rare independently selected from the group consisting of:ethers of formula —R′;esters of formula —C(═O)R′; andcarbonates of formula —C(═O)OR′;wherein R′ can be independently selected from the group consisting of substituted or unsubstituted alkyl and substituted or unsubstituted aryl.27. A method for the manufacture of a medicament comprising the step of combining a compound of formula (I) as defined for the pharmaceutical composition of or a pharmaceutically acceptable salt claim 25 , stereoisomer or solvate thereof claim 25 , with a pharmaceutically acceptable excipient.28. A method for the treatment and/or prophylaxis of cancer claim 25 , the method comprising administering to the subject in need of such a treatment or prophylaxis an effective amount of a compound of formula (I) as defined for the pharmaceutical composition of or a pharmaceutically acceptable salt claim 25 , stereoisomer or solvate thereof.31. The method according to claim 29 , wherein the compound of formula (I) meets at least one of the following conditions (a) to (d):{'sup': '3', '(a) Ris hydrogen;'}{'sup': '5', '(b) Ris hydrogen or chloro;'}{'sup': 6', '7, '(c) Ris hydrogen and Ris CHO; and'}{'sup': '8', '(d) Ris hydrogen.'}32. The method according to claim 30 , wherein the compound of formula (I) meets at least one of the following conditions (a) to (d):{'sup': '3', '(a) Ris hydrogen;'}{'sup': '5', '(b) Ris hydrogen or chloro;'}{'sup': 6', '7, '(c) Ris hydrogen and Ris CHO; ...

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31-05-2018 дата публикации

Photopolymerization initiator composition, active energy ray-curable composition, and cured product

Номер: US20180148519A1
Автор: Masako Yamashita
Принадлежит: Fujifilm Corp

An object of the present invention is to provide a photopolymerization initiator composition, which exhibits excellent storage stability at a low temperature and has an excellent effect of inhibiting bleed out occurring on the surface of a cured product after the thermocycling test, an active energy ray-curable composition, and a cured product. The photopolymerization initiator composition of the present invention contains a photopolymerization initiator represented by General Formula (I) and at least one kind of additive selected from the group consisting of compounds represented by General Formulae (II) to (IV).

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01-06-2017 дата публикации

Fungicidal pyrazoles and their mixtures

Номер: US20170150719A1
Принадлежит: EI Du Pont de Nemours and Co

Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, N-oxides, and salts thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the disclosure; and (b) at least one additional fungicidal compound. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of a compound of Formula 1, an N-oxide, or salt thereof (e.g., as a component in the aforesaid composition). Also disclosed is a composition comprising: (a) at least one compound selected from the compounds of Formula 1 described above, N-oxides, and salts thereof; and at least one invertebrate pest control compound or agent.

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18-06-2015 дата публикации

DIHYDROOROTIC ACID DEHYDROGENASE INHIBITOR

Номер: US20150166498A1
Принадлежит: NAI INC.

The present invention provides a novel dihydroorotic acid dehydrogenase inhibitor which is applicable to various diseases. When used as an active ingredient, a compound represented by formula (I): 2. The dihydroorotic acid dehydrogenase inhibitor according to claim 1 , whereinX represents a chlorine atom,{'sup': '2', 'Rrepresents a methyl group, and'}{'sup': 4', '0', '0, 'sub': 2', '3', '3', '3', '3', '2', '3', '2', '3', '3', '2', '3', '3', '3', '3', '3', '3', '3, 'Rrepresents —CH—CH═C(CH)—R(wherein Rrepresents an alkyl group containing 1 to 12 carbon atoms which may have a substituent on the terminal carbon and/or on a non-terminal carbon, or an alkenyl group containing 2 to 12 carbon atoms which may have a substituent on the terminal carbon and/or on a non-terminal carbon), provided that when Ro has a substituent, the substituent is selected from the group consisting of —O—CO—C(CH), —O—CO—CH(CH), —C(CH)—O—CH, —O-(2-furyl), —OH, —CH(OCH)—CH—CO—C(CH), —CHO, —CO—O—CH, —CO—CH, —O—CO—CHand —CO—C(CH).'}4. The dihydroorotic acid dehydrogenase inhibitor according to claim 1 , which comprises glycerol.5. The dihydroorotic acid dehydrogenase inhibitor according to claim 1 , which is used as an immunosuppressive agent.6. The dihydroorotic acid dehydrogenase inhibitor according to claim 1 , which is used as a therapeutic agent for rheumatism.7. The dihydroorotic acid dehydrogenase inhibitor according to claim 1 , which is used as an anticancer agent.8. The dihydroorotic acid dehydrogenase inhibitor according to claim 1 , which is used as a therapeutic agent for graft rejection in organ transplantation.9. The dihydroorotic acid dehydrogenase inhibitor according claim 1 , which is used as a therapeutic agent for diabetes.10. The dihydroorotic acid dehydrogenase inhibitor according to claim 1 , which is used as an antiviral agent.11H. pylori. The dihydroorotic acid dehydrogenase inhibitor according to claim 1 , which is used as an anti-agent.13. The kit according to claim 12 , ...

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23-05-2019 дата публикации

Fluorene Photoinitiator, Preparation Method Therefor, Photocurable Composition Having Same, and Use of Same in Photocuring Field

Номер: US20190155153A1
Автор: Qian Xiaochun
Принадлежит:

A fluorene-based photoinitiator, a preparation method thereof, a photocurable composition having the same, and use thereof in the field of photocuring are disclosed. In some embodiments, the fluorene-based photoinitiator has a structure represented by Formula I, wherein X is -A-(X′), wherein A is selected from a heteroatom which is selected from O, N, or S, X′ is selected from a C-Clinear alkyl group, a C-Cbranched alkyl group, a C-Ccycloalkyl group, a C-Calkyl group substituted with a C-Ccycloalkyl group or one or more of carbon atoms in X′ are substituted with a heteroatom, and n is 1 or 2; and Ris a hydroxy group or a N-morpholinyl group. In some embodiments, the fluorene-based photoinitiator comprises a structure represented by Formula II. 2. The fluorene-based photoinitiator according to claim 1 , wherein in Formula I claim 1 , the Rand the R′ are each independently selected from hydrogen claim 1 , a halogen claim 1 , a C-Clinear alkyl group claim 1 , a C-Cbranched alkyl group claim 1 , a C-Ccycloalkyl group claim 1 , or a C-Calkyl group substituted with a C-Ccycloalkyl group.3. The fluorene-based photoinitiator according to claim 1 , wherein in Formula I claim 1 , the Rand the Rare each independently selected from a C-Clinear alkyl group claim 1 , a C-Cbranched alkyl group claim 1 , a C-Ccycloalkyl group claim 1 , or a C-Calkyl group substituted with a C-Ccycloalkyl group; or the Rand the Rare connected to form a C-Ccycloalkyl group.4. The fluorene-based photoinitiator according to claim 1 , wherein in Formula I claim 1 , the X′ is selected from a methyl group claim 1 , an ethyl group claim 1 , a cyclohexyl group claim 1 , or a cyclopentyl group.7. A paint composition claim 1 , comprising a photoinitiator and a photopolymerizable monomer claim 1 , wherein the photoinitiator is the fluorene-based photoinitiator having the structure represented by Formula I in claim 1 , and the photopolymerizable monomer is an alkenyl-containing compound and/or an epoxy compound ...

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30-05-2019 дата публикации

NOVEL DERIVATIVES OF CURCUMINOIDS AND USE THEREOF AS AN ANTICANCER AGENT

Номер: US20190161430A1
Принадлежит:

A series of novel bis(hydroxymethyl) alkanoate derivatives of curcuminoids were designed, and synthesized, which show anticancer activity, and in particular to breast cancer, colon cancer, and prostate cancer. 2. The compound of claim 1 , wherein Rc is H claim 1 , and at least one of Ra claim 1 , Rb claim 1 , Ra′ and Rb′ is —OC(═O)Rd claim 1 , and Rd is a C3-C9 branched alkylol.3. The compound of claim 2 , wherein Rd is —C(CH)(CHOH) claim 2 , —C(CH)(CHOH) claim 2 , —C(CHOH) claim 2 , or —C(CHOH)(CHOC(═O)C(CHOH)).4. The compound of claim 3 , which one or two of Ra claim 3 , Rb claim 3 , Ra′ and Rb′ are —OC(═O)Rd claim 3 , Rd is —C(CH)(CHOH) claim 3 , and the remaining of Ra claim 3 , Rb claim 3 , Ra′ and Rb′ are H claim 3 , OH claim 3 , CH claim 3 , CH claim 3 , OCH claim 3 , OCH claim 3 , OCF; Re and Re′ are H claim 3 , CH claim 3 , CH claim 3 , OCH claim 3 , or OCH.5. The compound of claim 1 , wherein Rc is methyl claim 1 , ethyl claim 1 , benzyl claim 1 , propagyl claim 1 , allyl claim 1 , CHOH claim 1 , CHOC(═O)CH claim 1 , or CHOC(═O)Rd claim 1 , wherein Rd is —C(CH)(CHOH) claim 1 , —C(CH)(CHOH) claim 1 , —C(CHOH) claim 1 , or —C(CHOH)(CHOC(═O)C(CHOH)); Re and Re′ are H; and Ra claim 1 , Rb claim 1 , Ra′ and Rb′ independently are H claim 1 , OH claim 1 , C1-C6 alkoxy claim 1 , or —OC(═O)Rd claim 1 , wherein Rd is —C(CH)(CHOH) claim 1 , —C(CH)(CHOH) claim 1 , —C(CHOH) claim 1 , or —C(CHOH)(CHOC(═O)C(CHOH)).6. The compound of claim 5 , wherein Rc is methyl claim 5 , ethyl claim 5 , benzyl claim 5 , propagyl claim 5 , allyl claim 5 , CHOH claim 5 , CHOC(═O)CH claim 5 , or CHOC(═O)C(CH)(CHOH); and Ra claim 5 , Rb claim 5 , Ra′ and Rb′ independently are H claim 5 , OH claim 5 , methoxy claim 5 , or —OC(═O)Rd claim 5 , wherein Rd is —C(CH)(CHOH) claim 5 , —C(CHOH) claim 5 , or —C(CHOH)(CHOC(═O)C(CHOH)).9. A method for inhibiting growth of cancer cells comprising administering a compound according to or a pharmaceutically acceptable salt thereof to a subject suffering ...

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11-09-2014 дата публикации

COMPOSITIONS AND METHODS FOR THE TREATMENT OF GLOMERULONEPHRITIS

Номер: US20140256824A1
Принадлежит: Avexxin AS

The invention provides compositions and methods for the treatment of glomerulonephritis. In one embodiment, the invention provides a compound of formula (I)

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21-06-2018 дата публикации

METHODS FOR PRODUCING CYCLIC AND ACYCLIC KETONES

Номер: US20180170824A1
Принадлежит:

Provided herein are methods for producing cyclic and acyclic ketones from trimerization and dimerization of alkyl ketones, including for example methyl ketones. Such cyclic and acyclic ketones may be suitable for use as fuel and lubricant precursors, and may be hydrodeoxygenated to form their corresponding cycloalkanes and alkanes. Such cycloalkanes and alkanes may be suitable for use as fuels, including jet fuels, and lubricants. 2. The method of claim 1 , wherein the contacting of the at least one ketone with the catalyst further produces water as the at least one cyclic ketone is produced claim 1 , and the method further comprises controlling the amount of water present in the reaction mixture.3. The method of claim 2 , wherein:controlling the amount of water present in the reaction mixture comprises removing at least a portion of the water present in the reaction mixture; orthe amount of water present in the reaction mixture is less than 5 wt %;or a combination thereof.4. A method for producing at least one cycloalkane claim 1 , comprising hydrodeoxygenating at least one cyclic ketone having a structure of formula (I) claim 1 , (II) claim 1 , (III) or (IV) claim 1 , or any isomers thereof claim 1 , produced according to the method of to produce at least one cycloalkane.8. The method of claim 5 , wherein the catalyst comprises at least one metal and a basic support.9. The method of claim 8 , wherein at least one metal is a transition metal.10. The method of claim 1 , wherein the catalyst has one or more of the following properties:(i) a pKa between 8 to 16;{'sub': 2', '2', '2, '(ii) a COdesorption of at least 50° C., wherein COdesorption is carried out by adsorbing COto the catalyst at room temperature and heating up to 773 K;'}(iii) at least one basic oxygen atom; and(iv) a proton affinity of at least 700 kJ/mol;(v) is solid;(vi) is acidic; and(vii) is amphoteric.11. The method of claim 1 , wherein the catalyst comprises:a metal oxide;a non-metal oxide;a ...

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18-09-2014 дата публикации

NOVEL HETEROCYCLIC ALKANOL-DERIVATIVES

Номер: US20140274952A1
Принадлежит: BAYER INTELLCTUAL PROPERTY GMBH

The present invention relates to novel heterocyclic alkanol derivatives, to processes for these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators. 2. Heterocyclic alkanol derivative of the formula (I) and/or salt according to claim 1 , in whichX represents O or S,{'sub': 2', '2, 'Y represents O, S, SO, SO, —CH— or a direct bond,'}m represents 0 or 1,n represents 0 or 1,{'sub': 1', '7', '1', '8', '2', '7', '2', '7', '1', '4', '1', '3', '1', '4', '1', '3', '1', '3', '1', '3', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '3', '7', '3', '7', '1', '3', '1', '4, 'R represents in each case optionally branched C-C-alkyl, C-C-haloalkyl, C-C-alkenyl, C-C-haloalkenyl, C-Calkoxy-C-C-alkyl, C-C-haloalkoxy-C-C-alkyl, tri(C-C-alkyl)silyl-C-C-alkyl, in each case optionally halogen-, C-C-alkyl-, C-C-haloalkyl-, C-C-alkoxy-, C-C-haloalkoxy-, C-C-haloalkylthio-, C-C-alkylthio- or phenoxy-substituted (where phenoxy may in turn be substituted by halogen or C-C-alkyl) C-C-cycloalkyl or C-C-cycloalkyl-C-C-alkyl where any substitution is on the cycloalkyl moiety, and in each case optionally mono- to tri-halogen- or —C-C-alkyl-substituted phenyl,'}{'sup': '1', 'sub': 1', '4', '1', '4, 'Rrepresents hydrogen, SH, C-C-alkylthio, C-C-alkoxy or halogen,'}{'sup': '2', 'sub': 1', '4', '1', '4, 'Rrepresents fluorine, chlorine, bromine, iodine, C-C-alkyl or C-C-haloalkyl,'}{'sup': '3', 'sub': 1', '4', '1', '4, 'Rrepresents hydrogen, fluorine, chlorine, bromine, iodine, C-C-alkyl or C-C-haloalkyl,'}{'sup': '4', 'sub': 1', '3', '1', '3', '1', '3', '1', '3, 'Rrepresents hydrogen, (C-C-alkyl)carbonyl, C-C-alkyl, formyl, (C-C-haloalkyl)carbonyl or tri(C-C-alkyl)silyl,'}{'sup': 2', '3, 'sub': 2', '5, 'Rand Rtogether may furthermore represent straight-chain or branched und optionally halogen ...

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05-07-2018 дата публикации

PLANT GROWTH PROMOTERS AND METHODS OF USING THEM

Номер: US20180184651A1
Автор: AL-BABILI Salim
Принадлежит:

New plant growth regulators, including compounds and compositions, and methods of use including for promoting root growth. The compounds are carotenoid oxidation products, and a preferred example is 3-OH-β-apo-13-Carotenone. A method comprising promoting the growth of at least one plant with use of an effective amount of at least one composition comprising an effective amount of at least one compound which is represented by A-B-C, wherein B is a bivalent polyene moiety, A is a monovalent moiety linked to B by a six-membered carbon ring, wherein the ring has at least one substituent linked to the ring by an oxygen atom, and C is a monovalent moiety linked to B by a carbonyl group. Synergistic effects can be used with combinations of compounds. 1. A method comprising promoting the growth of at least one plant with use of an effective amount of at least one composition comprising an effective amount of at least one compound which is represented by A-B-C , wherein B is a bivalent polyene moiety , A is a monovalent moiety linked to B by a six-membered carbon ring , wherein the ring has at least one substituent linked to the ring by an oxygen atom , and C is a monovalent moiety linked to B by a carbonyl group.2. The method of claim 1 , wherein the bivalent polyene moiety B is a C-Chydrocarbon moiety with no heteroatoms.3. The method of claim 1 , wherein the bivalent polyene moiety B has three conjugated double bonds.4. The method of claim 1 , wherein the double bonds of bivalent polyene moiety B are in an all trans configuration.6. The method of claim 1 , wherein the six-membered ring is a phenyl ring claim 1 , a cyclohexane ring claim 1 , a cyclohexadiene ring claim 1 , or a cyclohexene ring.7. The method of claim 1 , wherein the six-membered ring is an unsaturated ring.8. The method of claim 1 , wherein monovalent moiety A consists of only one cyclohexene ring.9. The method of claim 1 , wherein monovalent moiety A comprises a cyclohexene ring claim 1 , and the ...

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18-06-2020 дата публикации

Compounds, compositions, and methods for use in treating autophagy-associated disorders

Номер: US20200190007A1
Автор: Ian Henderson
Принадлежит: Biophagy Inc

The invention provides compounds and methods of treating autophagy mediated diseases and disorders and related pharmaceutical compositions, diagnostics, screening techniques and kits.

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18-06-2020 дата публикации

METHOD FOR PRODUCING 2-ACETYL-4H,9H-NAPHTHO[2,3-B]FURAN-4,9-DIONE

Номер: US20200190049A1
Принадлежит: Sumitomo Dainippon Pharma Co., Ltd.

The invention addresses the problem of providing a method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione that is suited to industrial production. The invention provides a method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione by reacting 3-bromo-3-buten-2-one and 2-hydroxy-1,4-naphthoquinone in the presence of a solvent, then obtaining crystals of 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione by adding an alcohol-based solvent and/or water to the reaction system, and treating the crystals by using a specific adsorbent in the presence of a solvent. 139-. (canceled)40. A production method of 2-acetyl-4H ,9H-naphtho[2 ,3-b]furan-4 ,9-dione comprising the following step (d):(d) dissolving 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione in a non-alcohol-based solvent C, followed by adding an adsorbent to purify the 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione.41. The production method according to claim 40 , further comprising the following step (e) after the step (d):(e) removing the adsorbent used in the step (d) and evaporating the non-alcohol-based solvent C.42. The production method according to claim 41 , further comprising the following step (f) after the step (e):(f) crystallizing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione obtained in the step (e) by adding at least one crystallization solvent D selected from the group consisting of a hydrocarbon-based solvent, an alcohol-based solvent, an acid-based solvent, an ester-based solvent, an ether-based solvent, and water, to obtain 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione.43. The production method according to claim 42 , further comprising the following step (g) after the step (f):(g) slurrying 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione obtained in the step (f) with ethyl acetate to form a crystal of 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione.44. The production method according to claim 40 , wherein the non-alcohol-based solvent C used in the step (d) is at least one selected from the ...

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19-07-2018 дата публикации

METHOD FOR PRODUCING 2-ACETYL-4H,9H-NAPHTHO[2,3-B]FURAN-4,9-DIONE

Номер: US20180201597A1
Принадлежит: Sumitomo Dainippon Pharma Co., Ltd.

The invention addresses the problem of providing a method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione that is suited to industrial production. The invention provides a method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione by reacting 3-bromo-3-buten-2-one and 2-hydroxy-1,4-naphthoquinone in the presence of a solvent, then obtaining crystals of 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione by adding an alcohol-based solvent and/or water to the reaction system, and treating the crystals by using a specific adsorbent in the presence of a solvent. 1. A production method of 2-acetyl-4H ,9H-naphtho[2 ,3-b]furan-4 ,9-dione comprising the following step (c):(c) reacting 3-bromo-3-buten-2-one, 2-hydroxy-1,4-naphthoquinone, and a base in the presence of a non-alcohol, non-ketone-based solvent A, and adding an alcohol-based solvent B and/or water to obtain a crystal of 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione.2. The production method according to claim 1 , wherein in the step (c) claim 1 , an oxidant is added to a reaction solution after the addition of the alcohol-based solvent B and/or water.3. The production method according to claim 2 , wherein the oxidant is at least one selected from the group consisting of oxygen claim 2 , hydrogen peroxide claim 2 , sodium hypochlorite claim 2 , sodium chlorite claim 2 , chlorine claim 2 , iodine claim 2 , nitric acid claim 2 , and potassium nitrate.4. The production method according to claim 3 , wherein the oxidant is oxygen.5. The production method according to claim 1 , wherein in the step (c) claim 1 , a gas having an oxygen concentration of 1-25% is added to the reaction solution after the addition of the alcohol-based solvent B and/or water.68-. (canceled)9. The production method according to claim 1 , further comprising the following step (d) after the step (c):(d) purifying 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione obtained in the step (c), using an adsorbent in the presence of a non-alcohol- ...

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04-07-2019 дата публикации

Spontaneous orientation aid for liquid crystal composition, compound suitable for said spontaneous orientation aid, liquid crystal composition, and liquid crystal display element

Номер: US20190203122A1
Принадлежит: DIC Corp

The present invention provides a spontaneous orientation aid for a liquid crystal composition, containing one kind or two or more kinds of a compound having a partial structure represented by the general formula (i), wherein Z i1 represents a single bond, etc.; A i1 represents a divalent 6-membered aromatic group, etc.; m i1 represents an integer of 1 to 5; and K i1 represents a structure represented by any of the following formulae (K-1) to (K-8), wherein W K1 represents a methine group, etc.; X K1 and Y K1 each represent —CH 2 —, etc.; Z K1 represents an oxygen atom, etc.; and U K1 , V K1 , and S K1 each represent a methine group, etc.:

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09-10-2014 дата публикации

Novel Analogs of Curcumin and Methods of Use

Номер: US20140303109A1
Принадлежит:

Water-soluble fluorinated analogs of natural curcumin, and particularly difluoro Knoevenagel condensates and Schiff bases, along with their corresponding copper (H) complexes have improved bioavailablity over curcumin. The fluorine-substituted analogs of curcumin are useful as chemopreventive and/or therapeutic agents against cancers and/or against the development of drug-resistant cancer. A preferred compound is (IE,6E)-1,7-bis(4-hydroxy-3-methoxyphenyl)hepta-1,6-diene{4(3,4 difluorobenzaldehyde)}-3,5-dione. 2. The compound of wherein the amino is selected from the group consisting of saturated and unsaturated claim 1 , substituted and unsubstituted amines claim 1 , alkylamines claim 1 , arylamines claim 1 , heterocyclic amines claim 1 , phenylamines claim 1 , naphthoylamines claim 1 , isothiocyanates claim 1 , semicarbazides claim 1 , thiosemicarbazides claim 1 , hydrazones claim 1 , hydrazides claim 1 , thioureas claim 1 , hydroxamates claim 1 , arylazos claim 1 , azocylics claim 1 , and carboxyamidrazones.3. The compound of analogs of wherein R═H or —CH—CHF.5. The compound of wherein R is —CH—CHF.6. The compound of wherein X═Xand selected from the group consisting of O and an amino that forms a ligand that will conjugate with a metal ion to form a 1:1 metal ion to ligand complex.7. A formulation comprising a therapeutically effective amount of a compound of Formula I claim 1 , or a salt thereof claim 1 , in a pharmaceutically-acceptable non-toxic carrier.8. The formulation of wherein the compound of Formula I is (1E claim 7 ,6E)-1 claim 7 ,7-bis(4-hydroxy-3-methoxyphenyl)hepta-1 claim 7 ,6-diene{4(3 claim 7 ,4 difluorobenzaldehyde)}-3 claim 7 ,5-dione.9. The formulation of further comprising at least one or more chemotherapeutic or cytotoxic pharmaceutical agents.10. The formulation of wherein the at least one or more chemotherapeutic or cytotoxic pharmaceutical agents are selected from the group consisting of genistein claim 9 , celecoxib claim 9 , gemcitabine ...

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04-08-2016 дата публикации

MTOR-independent activator of TFEB for autophagy enhancement and uses thereof

Номер: US20160221907A1
Принадлежит:

The present invention relates to a composition comprising an autophagy enhancement compound. Small molecules that are able to enhance autophagy and lysosome biogenesis by activating the gene TFEB which can prevent the accumulation of toxic protein aggregates in treating neurodegenerative diseases are disclosed. 6. The method according to claim 5 , wherein the neurodegenerative diseases comprising Alzheimer's disease claim 5 , Parkinson's disease claim 5 , Huntington's disease and Creutzfeldt-Jakob disease.12. A method of enhancing lysosome biogenesis in cells comprising providing the mono-carbonyl analog of .13. The method of claim 12 , wherein the cells are neuronal cells.14. The method of claim 12 , wherein the cells are non-neuronal cells.16. The method according to wherein said mono-carbonyl analog of curcumin is administered to the subject in need thereof via oral administration.17. The method according to wherein said cells are neuronal cells. This application is a continuation-in-part application of the U.S. non-provisional patent application Ser. No. 14/609,438 filed Jan. 30, 2015, which claims the benefit of U.S. Provisional Patent Application Ser. No. 61/949,233 filed on Mar. 6, 2014, the disclosures are hereby incorporated by reference in their entirety.The present invention relates to a composition comprising an autophagy enhancement compound. In particular, the present invention relates to a composition comprising a small molecule being able to enhance autophagy and lysosome biogenesis by activating the gene TFEB which can prevent the accumulation of toxic protein aggregates in treating neurodegenerative diseases such as Parkinson's, Alzheimer's and Huntington's diseases.Macroautophagy, herein referred to as autophagy, is a highly conserved process for cellular degradation and recycling of cytosolic contents to maintain cellular homeostasis. Autophagy substrates are generally cellular organelles, long-lived proteins and aggregate-prone proteins. Due to ...

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11-07-2019 дата публикации

Method for the Selection of Patients and Kit

Номер: US20190212326A1
Принадлежит:

The invention provides a method for selecting a patient who may respond to a compound having at least one (substituted phenyl)-propenal moiety, which comprises contacting the compound with a sample derived from the patient and determining whether the compound decreases the amount of a protein selected from AR, c-MYC, Aurora-A, mutated p53, CDK4, or Her2 or whether the compound increases the amount of reactive oxygen species in the sample, wherein decrease of the protein or increase of the reactive oxygen species indicates that the patient may respond to the compound. The invention also provides a kit, a method for identifying a candidate compound which may treat an androgen receptor associated medical condition, and a candidate compound identified by the method as mentioned above. 2. The method according to claim 1 , wherein the patient is suffering from an androgen receptor associated medical condition.3. The method according to claim 2 , wherein the androgen receptor associated medical condition is selected from inflammation claim 2 , acne claim 2 , alopecia claim 2 , hirsutism claim 2 , wound claim 2 , spinal and bulbar muscular atrophy (SBMA claim 2 , Kennedy's disease) claim 2 , unwanted immune response claim 2 , immune disorder claim 2 , or cancer.4. The method according to claim 3 , wherein the cancer is selected from prostate cancer claim 3 , liver cancer claim 3 , bladder cancer claim 3 , cervical cancer claim 3 , lung cancer and breast cancer claim 3 , skin cancer claim 3 , small cell lung cancer claim 3 , testicular cancer claim 3 , lymphoma claim 3 , leukemia claim 3 , esophageal cancer claim 3 , stomach cancer claim 3 , colon cancer claim 3 , endometrial cancer claim 3 , ovarian cancer claim 3 , central nervous system cancer claim 3 , and the like.5. The method according to claim 1 , which comprises determining whether the compound enhances the degradation of the protein.6. The method according to claim 4 , wherein the sample is derived from a biopsy of ...

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18-07-2019 дата публикации

PROCESS FOR THE MANUFACTURE OF HYDROXY-SUBSTITUTED AROMATIC COMPOUNDS

Номер: US20190218181A1
Принадлежит:

The present invention relates to a process for the manufacture of hydroxy-substituted aromatic styryl or stilbene compounds. 2. The process according to claim 1 , wherein Z is a divalent substituted aromatic group.3. The process according to claim 1 , wherein the compound of formula (III) is formed in situ from a compound of formula (IV){'br': None, 'HOOC—CH═CH—Ar \u2003\u2003(IV),'}wherein Ar is as defined above.4. The process according to claim 1 , wherein the transition metal catalyst is a bimetallic catalyst comprising palladium and at least one further transition metal.5. The process according to claim 1 , wherein the leaving group X is a halogenide.6. The process according to claim 1 , wherein Z is derived from a substituted six-membered aromatic group.7. The process according to claim 1 , wherein Z is derived from a hydroxy-substituted benzene group and/or Ar is derived from a hydroxyl-substituted benzene group.8. The process according to claim 1 , wherein each group Ar is derived from a hydroxy-substituted benzene group.11. The process according to claim 1 , which is carried out in at least one solvent claim 1 , and in the presence of at least one base.12. The process according to comprising adding water to the process.13. The process according to claim 1 , which is carried out in the presence of at least one phase transfer catalyst compound.14. The process according to claim 13 , which is carried out in the absence of triphenylphosphane.15. The process according to claim 1 , which further comprises at least one subsequent derivatization reaction of the compound of formula (I).16. The process according to claim 1 , which further comprises the admixture of a compound of formula (1) with at least one pharmaceutical or cosmetic excipient.17. The process according to claim 4 , wherein the at least one further transition metal comprises copper or silver.18. The process according to claim 5 , wherein the halogenide is chlorine or bromine.19. The process according ...

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19-08-2021 дата публикации

Preparation method of pyrrolo-amino-pyridazinone compound and intermediate thereof

Номер: US20210253585A1

Provided are a preparation method of pyrrolo-amino-pyridazinone compound and an intermediate thereof. The reaction conditions are easy to control, the processing following the reaction is simple, the production rate is high, and the method is advantageous for industrial production.

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16-08-2018 дата публикации

Perfume systems

Номер: US20180230398A1
Принадлежит: Procter and Gamble Co

The present application relates to perfume raw materials, perfume delivery systems and consumer products comprising such perfume raw materials and/or such perfume delivery systems, as well as processes for making and using such perfume raw materials, perfume delivery systems and consumer products. Such perfume raw materials and compositions, including the delivery systems, disclosed herein expand the perfume communities' options as such perfume raw materials can provide variations on character and such compositions can provide desired odor profiles.

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03-09-2015 дата публикации

FLAVOR AND FRAGRANCE FORMULATION (II)

Номер: US20150245985A1
Принадлежит:

The present invention relates to the use of specific organic compounds as flavor and fragrance material. Furthermore the invention relates to a new specific organic compound, as well as to flavor and fragrance formulations comprising at least one of the specific organic compounds. 4. Flavor and fragrance formulation according to comprising 0.0001-10 wt-% claim 3 , related to the total weight of the flavor and fragrance formulation claim 3 , of at least one compound of formula (I) and/or of at least one compound of formula (II).5. Flavor and fragrance formulation according to claim 3 , wherein the flavor and fragrance formulation is solid claim 3 , gel-like or liquid.6. Flavor and fragrance formulation according to claim 3 , wherein the flavor and fragrance formulation is a perfume claim 3 , air care product claim 3 , household product claim 3 , laundry product claim 3 , body care product or cosmetic product. The present invention relates to the use of specific organic compounds as flavor and fragrance material. Furthermore the invention relates to new specific organic compounds, as well as to flavor and fragrance formulations comprising at least one of the specific organic compounds.In the flavor and fragrance industry there is always a need and demand for compounds that enhance, modify, improve or otherwise positively influence an odour note and therefore giving perfumers or other persons the ability to create new fragrances for perfumes, colognes, personal care products, household products or any other products, which comprise flavor and fragrance materials.Surprisingly it was found that the compounds of formula (I) and/or compounds of formula (II) are very useful as flavor and fragrance material.Therefore the present invention is related to the use of a compound of formula (I) and/or a compound of formula (II)whereinas flavor and fragrance material.Preferred is the use of at least one compound selected from the group consisting of the compounds of formulae (Ia)-( ...

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