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序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
161 Novel materials containing nitrogen US327839 1973-01-30 US3965184A 1976-06-22 Ronald Eric Banks; Robert Neville Haszeldine
Compositions of matter including the structural unit ##EQU1## wherein R.sub. F ' is a divalent polyfluoroalkylene group having a chain length of from 1 to 4 carbon atoms which may be substituted at one or more positions with chloro-or polyfluoroalkyl, chlorofluoroalkyl or polyfluorocycloalkyl groups containing up to six carbon atoms; and R.sub.F is a monovalent straight or branched chain, or cyclic, polyfluoroalkyl group or a chlorofluoroalkyl group containing up to ten carbon atoms and the R.sub.F groups are the same or different or is a divalent polyfluoroalkylene group having a chain length of from 1 to 4 carbon atoms which may be substituted at one or more positions with chloro or polyfluoroalkyl, chlorofluoroalkyl or polyfluorocycloalkyl groups containing up to six carbon atoms and the R.sub.F groups are interconnected to form a cyclic structure.
162 Hydroxyguanidine O-carbamates US37314773 1973-06-25 US3867447A 1975-02-18 CHERKOFSKY SAUL CARL
Disclosed herein are particular variously substituted 2hydroxyguanidine O-carbamates, useful as antihypertensive agents, made by reacting an hydroxyguanidine with an isocyanate. Exemplary is 1-methyl-1-n-propylhydroxyguanidine O-(N-methyl carbamate).
163 SAFE AND EFFICIENT PROCESS FOR THE PREPARATION OF CARMUSTINE EP17158359.4 2017-02-28 EP3214075B1 2019-08-21 TOMASI, Attilio; CANDIANI, Ilaria; CORCELLA, Francesco; CALDARELLI, Francesco Saverio
164 SAFE AND EFFICIENT PROCESS FOR THE PREPARATION OF CARMUSTINE EP17158359.4 2017-02-28 EP3214075A3 2017-11-29 TOMASI, Attilio; CANDIANI, Ilaria; CORCELLA, Francesco; CALDARELLI, Francesco Saverio

The present invention relates to a safe and efficient process for the preparation of carmustine (1) and to useful intermediate compounds of such process and their preparation. Such process employs safe and readily available starting materials under mild reaction conditions and allows for recovery of the product in a good yield and a high purity. For these reasons, such new process is also suitable for plant scale production. Starting materials comprise 2-chloroethylamine hydrochloride (5) and 1,1'-carbonyldiimidazole (4) to afford 1,3-bis(2-chloroethyl)-1-urea (2), which then undergoes nitrosation to give the final product.

165 SAFE AND EFFICIENT PROCESS FOR THE PREPARATION OF CARMUSTINE EP17158359.4 2017-02-28 EP3214075A2 2017-09-06 TOMASI, Attilio; CANDIANI, Ilaria; CORCELLA, Francesco; CALDARELLI, Francesco Saverio

The present invention relates to a safe and efficient process for the preparation of carmustine (1) and to useful intermediate compounds of such process and their preparation. Such process employs safe and readily available starting materials under mild reaction conditions and allows for recovery of the product in a good yield and a high purity. For these reasons, such new process is also suitable for plant scale production. Starting materials comprise 2-chloroethylamine hydrochloride (5) and 1,1'-carbonyldiimidazole (4) to afford 1,3-bis(2-chloroethyl)-1-urea (2), which then undergoes nitrosation to give the final product.

166 NITRIC OXIDE DONATING PROSTAMIDES EP09742454.3 2009-05-11 EP2274279A1 2011-01-19 BENEDINI, Francesca; BIONDI, Stefano; CHIROLI, Valerio; CHONG, Wesley, Kwan, Mung; DONG, Liming; KRAUSS, Achim, Hans-Pter; NICOLI, Fabio; PRASANNA, Ganesh; VERNIER, William, Francois; YANG, Yi
Nitroderivatives of prostaglandins having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.
167 ARYL NITRONE THERAPEUTICS FOR THE TREATMENT OF INFLAMMATORY BOWEL DISEASE EP99922983.4 1999-05-18 EP1077694B1 2004-07-21 FLITTER, William, D.; GARLAND, William, A.; GREENWOOD-VAN MEERVELD, Beverly; IRWIN, Ian
168 POLYMERIC ACETOACETANILIDE AZO COLORANTS EP01984933 2001-11-26 EP1337509A4 2004-05-19 XIA JUSONG; MASON MARY G; MILEY JOHN W; STEPHENS ERIC B; STARKS LEONARD J; STEPHENSON KYLE E
This invention related to colorans comprising a chromophore having a single azo acetoacetanilide moiety, wherein said moiety each have at least one poly(oxyalkylene) chain. Such colorants exhibit extremely good base stability and lighfastness, particularly when incorporate within certain media and/or on the surface of certain substrates. These poly(oxyalkylene) chains provide sulubility in different solvents or resins thereby permitting the introduction of such excellent coloring chromophores within diverse media and/or or diverse substrates. Compositions and articles comprising such colorants are provided as are methods for producing such inventive colorants.
169 POLYMERIC ACETOACETANILIDE AZO COLORANTS EP01984933.0 2001-11-26 EP1337509A1 2003-08-27 XIA, Jusong; MASON, Mary, G.; MILEY, John, W.; STEPHENS, Eric, B.; STARKS, Leonard, J.; STEPHENSON, Kyle, E.
This invention related to colorans comprising a chromophore having a single azo acetoacetanilide moiety, wherein said moiety each have at least one poly(oxyalkylene) chain. Such colorants exhibit extremely good base stability and lighfastness, particularly when incorporate within certain media and/or on the surface of certain substrates. These poly(oxyalkylene) chains provide sulubility in different solvents or resins thereby permitting the introduction of such excellent coloring chromophores within diverse media and/or or diverse substrates. Compositions and articles comprising such colorants are provided as are methods for producing such inventive colorants.
170 NOVEL NITRIC OXIDE-RELEASING AMIDINE- AND ENAMINE-DERIVED DIAZENIUMDIOLATES, COMPOSITIONS AND USES THEREOF AND METHOD OF MAKING SAME EP98933062.6 1998-07-01 EP1000023A2 2000-05-17 HRABIE, Joseph, A.; KEEFER, Larry, K.
The present invention relates to nitric oxide-releasing amidine- and enamine-derived diazeniumdiolates, compositions comprising such compounds, methods of using such compounds and compositions, and to a method for the preparation of nitric oxide-releasing amidine- and enamine-derived diazeniumdiolates via the direct reaction of nitric oxide with amidines and enamines, and to a method of converting amines into such compounds.
171 N-hydroxy-alpha-amino acids, amides and other derivatives thereof EP89200193.4 1989-01-31 EP0330247B1 1993-07-07 Kamphuis, Johan; Boesten, Wilhelmus Hubertus Joseph
172 Amine oxide process EP88119882.4 1988-11-29 EP0320694A3 1990-11-28 Bauer, Dennis Paul; Summerford, Teresa Kay

Tert-amine oxides that are substantially free of nitrosamines are made by reacting a tert-amine, e.g., dodecyl dimethylamine, with aqueous hydrogen peroxide in the presence of the synergistic combination of (a) ascorbic acid and (b) a promoter formed from carbon dioxide.

173 Fluoroalkyl ether, surface modifying composition and method for modifying surface EP89117633.1 1989-09-25 EP0361346A2 1990-04-04 Shoji, Mitsuyoshi; Nakakawaji, Takayuki; Ito, Yutaka; Komatsuzaki, Shigeki; Mukoh, Akio

A solid surface modifying composition comprising a film forming material and a fluoroalkyl ether (-(Rf)̵mCONH-X-NHCO-Y)m (m = 1 or 2; Rf: perfluoropolyether chain; provides surfaces with such improvements as durable water and oil repellency, lubricity and lowered surface energy. The lubricating protective coating is applicable for coatings of recording mediums, photoreceptors and wirings.

174 N-hydroxy-alpha-amino acids, amides and other derivatives thereof EP89200193.4 1989-01-31 EP0330247A1 1989-08-30 Kamphuis, Johan; Boesten, Wilhelmus Hubertus Joseph

The invention relates to a process for the preparation of N-­hydroxy-alpha-amino acids and the derivatives thereof by reacting a derivative of an alpha-amino acid with an aromatic aldehyde to form a Schiff base, oxidizing the Schiff base to an oxaziridine and con­verting the oxaziridine into the corresponding N-hydroxy-alpha-amino acid derivative and, if so desired, converting that derivative into the acid or a different derivative, in which an alpha-amino acid amide is used as starting material.

175 Inhibitors of RNA guided nucleases and uses thereof US16346392 2017-10-31 US11787795B2 2023-10-17 Amit Choudhary; Peng Wu; Basudeb Maji; Elisa Franco; Hari K. K. Subramanian
Compositions and methods are provided for the inhibition of the function of RNA guided endonucleases, including the identification and use of such inhibitors.
176 Lipid compound as well as lipid vector, nucleic acid lipid nanoparticle composition, and pharmaceutical preparation comprising the same US17873404 2022-07-26 US11786609B2 2023-10-17 Ke Huang; Chaoxuan Jing; Yingwen Li; Yinjia Gao; Yuping Liu; Zhenhua Sun
The present disclosure belongs to the technical field of gene therapy, and specifically relates to a series of lipid compounds as well as lipid vectors, nucleic acid lipid nanoparticle compositions, and pharmaceutical preparations containing the same. The compound having the structure of formula (I) provided by the present disclosure may be used in combination with other lipid compounds to prepare a lipid vector, which exhibits pH responsiveness, has high encapsulation efficiency for nucleic acid drugs, and greatly enhances the in-vivo delivery efficiency of nucleic acid drugs. Moreover, it is possible to select lipid compounds with different structures as lipid vectors to adjust the enrichment of nucleic acid drugs in different organs, thereby having good market application prospect.
177 Methods for modulating RNA splicing US16463775 2017-11-27 US11702646B2 2023-07-18 Anuradha Bhattacharyya; Amal Dakka; Kerstin Effenberger; Vijayalakshmi Gabbeta; Wencheng Li; Nikolai Naryshkin; Christopher Trotta; Kari Wiedinger
In one aspect, described herein is an intronic recognition element for splicing modifier (iREMS) that can be recognized by a compound provided herein. In another aspect, described herein are methods for modulating the amount of a product of a gene, wherein a precursor RNA transcript transcribed from the gene contains an intronic REMS, and the methods utilizing a compound described herein. More particularly, described herein are methods for modulating the amount of an RNA transcript or protein product encoded by a gene, wherein a precursor RNA transcript transcribed from the gene comprises an intronic REMS, and the methods utilizing a compound described herein. In another aspect, provided herein are artificial gene constructs comprising an intronic REMS, and uses of those artificial gene constructs to modulate protein production. In another aspect, provided herein are methods for altering endogenous genes to comprise an intronic REMS, and the use of a compound described herein to modulate protein produced from such altered endogenous genes.
178 LIPID COMPOUND AS WELL AS LIPID VECTOR, NUCLEIC ACID LIPID NANOPARTICLE COMPOSITION, AND PHARMACEUTICAL PREPARATION COMPRISING THE SAME US17873404 2022-07-26 US20220378938A1 2022-12-01 Ke HUANG; Chaoxuan JING; Yingwen LI; Yinjia GAO; Yuping LIU; Zhenhua SUN
The present disclosure belongs to the technical field of gene therapy, and specifically relates to a series of lipid compounds as well as lipid vectors, nucleic acid lipid nanoparticle compositions, and pharmaceutical preparations containing the same. The compound having the structure of formula (I) provided by the present disclosure may be used in combination with other lipid compounds to prepare a lipid vector, which exhibits pH responsiveness, has high encapsulation efficiency for nucleic acid drugs, and greatly enhances the in-vivo delivery efficiency of nucleic acid drugs. Moreover, it is possible to select lipid compounds with different structures as lipid vectors to adjust the enrichment of nucleic acid drugs in different organs, thereby having good market application prospect.
179 Synthesis of 1:1:1 co-crystal of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(β-D-glucopyranos-1-yl)-benzene, L-proline and water US16771717 2018-12-17 US11225500B2 2022-01-18 Matthias Eckhardt; Monika Brink; Frank Himmelsbach; Stefan Sahli; Chutian Shu; Xiao-Jun Wang; Beat Theodor Weber; Bing-Shiou Yang
The invention relates to a process for the manufacture of the crystalline compound according to formula (I) comprising the steps (a) deacetylating the final intermediate (FI), (b) forming the crystalline compound according to formula (I) by reacting the deacetylated final intermediate of step (a) with L-proline and water and isolating the final reaction product; processes of manufacturing intermediates thereof; process intermediates and their uses in the processes according to the present invention.
180 SYNTHESIS OF 1:1:1 CO-CRYSTAL OF 1-CYANO-2-(4-CYCLOPROPYL-BENZYL)-4-(ß-D-GLUCOPYRANOS-1-YL)-BENZENE, L-PROLINE AND WATER US16771717 2018-12-17 US20210139520A1 2021-05-13 Matthias ECKHARDT; Monika BRINK; Frank HIMMELSBACH; Stefan SAHLI; Chutian SHU; Xiao-Jun WANG; Beat Theodor WEBER; Bing-Shiou YANG
The invention relates to a process for the manufacture of the crystalline compound according to formula (I) comprising the steps (a) deacetylating the final intermediate (FI), (b) forming the crystalline compound according to formula (I) by reacting the deacetylated final intermediate of step (a) with L-proline and water and isolating the final reaction product; processes of manufacturing intermediates thereof; process intermediates and their uses in the processes according to the present invention.
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