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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
281 UNIVERSAL SUPPORTS FOR OLIGONUCLEOTIDE SYNTHESIS PCT/US2001/044326 2001-11-29 WO02044398A2 2002-06-06
Universal supports for oligonucleotide synthesis include a support material represented by the formula (I). In this formula, substituent A is selected from H, alkyl, aryl, or a polymeric or silica base material; substituent B is selected from acyl, aroyl or a polymeric or silica base material; and substituent C is selected from a dimethoxytrityl group or a protecting group removable under acidic or neutral conditions. For the supports, one of substituents A or B constitutes the polymeric or silica base material. In use, an oligonucleotide is attached to the support at substituent C.
282 USE OF 2-PHENYLENE DIAMINE DERIVATIVES FOR THE TREATMENT OF INFECTIONS PCT/EP2001/002016 2001-02-22 WO01062709A2 2001-08-30
The invention relates to the use of compounds of formula (I), wherein n = 0 - 3; R<1>, R<2> = H, alkyl, aryl, heteroaryl, acyl; R<3> = H, halogen, alkyl, aryl, heteroaryl, arylalkyl, acyl, CN, NO2, R<4>-X-; R<4> = H, alkyl, aryl, heteroaryl, aralkyl, acyl; X = NH, O, S, SO2, NHSO2, OSO2, and A, B, C = organic groups. The inventive compounds are used for the prophylaxis and the therapeutic treatment of infectious processes, especially of infectious processes caused by parasites. The invention further relates to medicaments that contain the inventive compounds.
283 HSV PRIMASE INHIBITORS PCT/CA2000/000324 2000-03-23 WO00058270A3 2001-03-01
The invention provides compounds of formula (1) that are active against the HSV primase enzyme: wherein R1 is hydroxy or amino; R2 is hydrogen, halo, (C1-4)alkyl or (C1-4)alkoxy; R3 is hydrogen, halo, (C1-4)alkyl, (C1-4)alkoxy, amino or azido; R4 has the same significance as R2; R5 is hydrogen or (C1-4)alkyl; and R is (C1-7)alkyl, (C3-6)cycloalkyl, {phenyl(C1-7)alkyl}, {phenyl(C1-7)alkoxy}, {{(monocyclic heterocyclo)-{(C1-7)alkoxy}}, CH(W)C(O){O-(C1-4)alkyl} wherein W is hydrogen or (C1-7)alkyl, or (a) wherein Y is hydrogen or (C1-7)alkyl, and Z is (C1-7)alkyl, (C3-6) cycloalkyl, {(C3-6)cycloalkyl}-{(C1-7)alkyl}, phenyl(C1-7)alkyl or {{(monocyclic heterocyclo)-{(C1-7)alkyl}}, or Y and Z together with the nitrogen atom to which they are attached represent, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl or 1-(4-methylpiperazinyl); with the provisos that (1) when R is CH(W)C(O)-{O-(C1-4)alkyl} as defined herein, then R5 is hydrogen; and (2) at least one of R2, R3 and R4 is other than hydrogen.
284 PROCESS FOR PREPARING ACIDS VIA ALPHA-CHLOROEPOXY ESTERS PCT/US2000/021394 2000-08-04 WO01010822A1 2001-02-15
This invention relates to a method for preparing certain acids of formula (I) via a chloroepoxy ester, which are useful as phosphodiesterase 4 inhibitors.
285 MONOMERS AND NETWORK POLYMERS OBTAINED THEREFROM PCT/GB1999/002416 1999-07-26 WO00006533A2 2000-02-10
A compound of formula (I) where R<1> is CH and R<6> is a bond, or R<1> and R<6> together form an electron withdrawing group; R<2> and R<3> are independently selected from (CR<7>R<8>)n, or a group CR<9>R<10>, -(CR<7>R<8>CR<9>R<10>)- or -(CR<9>R<10>CR<7>R<8>)- where n is 0,1 or 2, R<7> and R<8> are independently selected from hydrogen or alkyl, and either one of R<9> or R<10> is hydrogen and the other is an electron withdrawing group, or R<9> and R<10> together form an electron withdrawing group, and R<4> and R<5> are independently selected from CH or CR<11> where R<11> is an electron withdrawing group; the dotted lines indicate the presence or absence of a bond, and X<1> is a group CX<2>X<3> where the dotted line bond to which it is attached is absent and a group CX<2> where the dotted line bond to which it is attached is present, Y<1> is a group CY<2>Y<3> where the dotted line bond to which it is attached is absent and a group CY<2> where the dotted line bond to which it is attached is present, and X<2>, X<3>, Y<2> and Y<3> are independently selected from hydrogen and fluorine; R<16> is a bridging group of valency r and r is an integer of 2 or more, subject to the following provisos: (i) that at least one of (a) R<1> and R<6> or (b) R<2> and R<3> or (c) R<4> and R<5> includes an electron withdrawing group. These compounds are useful in the production of network polymers, for example for coatings or binders.
286 PHARMACEUTICALLY ACTIVE COMPOUNDS AND METHODS OF USE PCT/US1998/022309 1998-10-20 WO99020599A1 1999-04-29
The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.
287 INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE PCT/US1998/017327 1998-08-24 WO99011606A2 1999-03-11
The present invention comprises small molecular weight, non-peptidic inhibitors of formula (I) and (II) of Protein Tyrosine Phosphatase 1 (PTP1) which are useful for the treatment and/or prevention of Non-Insulin Dependent Diabetes Mellitus (NIDDM).
288 Amorphous solid succinylated 3-(fatty acid amido)-2-hydroxy-1- (protected hydroxy)-propane salts and methods of making the same US17987469 2022-11-15 US12122735B2 2024-10-22 Jennifer Elizabeth Albaneze-Walker
Aspects of the disclosure includes methods for preparing an amorphous solid composition of a fatty acid metal salt. In practicing the subject methods according to certain embodiments, a succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane organic salt is contacted with a metal base to produce a succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane metal salt; and the succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane metal salt is precipitated in a solvent to produce an amorphous solid succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane metal salt composition. An amorphous solid succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane lithium salt is also provided.
289 Amorphous Solid Succinylated 3-(Fatty Acid Amido)-2-Hydroxy-1-(Protected Hydroxy)-Propane Salts and Methods of Making the Same US17987469 2022-11-15 US20230192597A1 2023-06-22 Jennifer Elizabeth Albaneze-Walker
Aspects of the disclosure includes methods for preparing an amorphous solid composition of a fatty acid metal salt. In practicing the subject methods according to certain embodiments, a succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane organic salt is contacted with a metal base to produce a succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane metal salt; and the succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane metal salt is precipitated in a solvent to produce an amorphous solid succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane metal salt composition. An amorphous solid succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane lithium salt is also provided.
290 Amorphous solid succinylated 3-(fatty acid amido)-2-hydroxy-1 -(protected hydroxy)-propane salts and methods of making the same US17079129 2020-10-23 US11530179B2 2022-12-20 Jennifer E. Albaneze-Walker
Aspects of the disclosure includes methods for preparing an amorphous solid composition of a fatty acid metal salt. In practicing the subject methods according to certain embodiments, a succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane organic salt is contacted with a metal base to produce a succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane metal salt; and the succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane metal salt is precipitated in a solvent to produce an amorphous solid succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane metal salt composition. An amorphous solid succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane lithium salt is also provided.
291 AMORPHOUS SOLID SUCCINYLATED 3-(FATTY ACID AMIDO)-2-HYDROXY-1-(PROTECTED HYDROXY)-PROPANE SALTS AND METHODS OF MAKING THE SAME US17079129 2020-10-23 US20210147344A1 2021-05-20 Jennifer E. Albaneze-Walker
Aspects of the disclosure includes methods for preparing an amorphous solid composition of a fatty acid metal salt. In practicing the subject methods according to certain embodiments, a succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane organic salt is contacted with a metal base to produce a succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane metal salt; and the succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane metal salt is precipitated in a solvent to produce an amorphous solid succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane metal salt composition. An amorphous solid succinylated 3-(fatty acid amido)-2-hydroxy-1-(protected hydroxy)-propane lithium salt is also provided.
292 N-acylethanolamide derivatives and uses thereof US16349548 2017-10-12 US10933037B2 2021-03-02 Andrew D. Levin
The present disclosure provides certain N-Acylethanolamide derivatives, and uses relating thereto.
293 Curing agents and degradable polymers and composites based thereon US14781242 2014-04-18 US10308594B2 2019-06-04 Bing Qin; Xin Li; Bo Liang
The present invention provides, among others, compounds of Formula (I) or a salt thereof, methods for making these compounds, degradable polymers and reinforced composites made therefrom, and methods for degrading and/or recycling the degradable polymers and reinforced composites.
294 Graphene quantum dots and method of making US14261936 2014-04-25 US09637443B2 2017-05-02 Julia Xiaojun Zhao; Xu Wu
A method for forming a graphene quantum dot product includes adding an organic starting material to a vessel and heating the organic starting material to a temperature within 20° C. of the organic starting material's boiling temperature for a time no longer than ten minutes to form graphene quantum dots. A method for sensing a graphene quantum dot includes forming a graphene quantum dot, exciting the graphene quantum dot with light having a first wavelength, measuring light emitted by the excited graphene quantum dot at a second wavelength different from the first wavelength. A graphene quantum dot includes carbon atoms and nitrogen atoms where the nitrogen atoms are present within the graphene quantum dot at a level between 6.0% and 11.0% of a level of carbon atoms present in the graphene quantum dot.
295 Crystalline forms of (1S,2R)-2-(amino methyl)-N,N-diethyl-1-phenyl cyclopropane carboxamide US14518300 2014-10-20 US09259403B2 2016-02-16 Rahul Surana; Mahendra G. Dedhiya
The present invention relates to novel crystalline forms of (1S,2R)-2-(amino methyl)-N,N-diethyl-1-phenyl cyclopropane carboxamide. Processes for the preparation of this form, compositions containing the form, and methods of use thereof are also described.
296 Use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas US13678802 2012-11-16 US08987262B2 2015-03-24 Christine Leaute-Labreze; Eric Dumas De La Roque; Alain Taieb; Jean-Benoit Thambo
The present technology relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present technology provides an alternative to the known compounds, e.g. corticosteroïds, interferon or vincristine, generally used for the treatment of hemangiomas.
297 Cysteine protease inhibitors US13139962 2009-12-18 US08853281B2 2014-10-07 Susana Ayesa; Anna Karin Belfrage; Bjorn Classon; Urszula Grabowska; Ellen Hewitt; Vladimir Ivanov; Daniel Jönsson; Pia Kahnberg; Peter Lind; Magnus Nilsson; Lourdes Odén; Mikael Pelcman; Horst Wähling
Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain.
298 Concurrent therapy regime/regimen for the treatment of acne related diseases US12992425 2009-05-18 US08853275B2 2014-10-07 Jean-Charles Dhuin; Nabil Kerrouche; Stéphanie Arsonnaud; Pascale Soto
A novel therapy regime/regimen for the treatment of acne related diseases includes administering a topical fixed-dose combination of a retinoid and an anti-bacterial agent, such as BPO, to a course of oral antibiotic therapy.
299 Additive for preserving the fluidity of fluids containing gas hydrates US12293922 2007-03-16 US08821754B2 2014-09-02 Martin Hellsten; Hans Oskarsson
The present invention relates to the use of a specific group of alkoxylated and/or acylated non-quaternary nitrogen-containing compounds as anti-agglomerants for gas hydrates.The invention also relates to a method for inhibiting the agglomeration of gas hydrates in a conduit, and compositions comprising the gas hydrate anti-agglomerant, a corrosion inhibitor and/or a paraffin deposition inhibitor.
300 Method and composition for prolonging analgesic effect of local anesthetic US13340330 2011-12-29 US08779003B2 2014-07-15 Yu-Chun Hung
Disclosed herein is a method for prolonging analgesic effect of a membrane permeable local anesthetic in a subject in need thereof. The method uses cinnamaldehyde as an adjuvant which, when administered prior to or simultaneously with the administration of a local anesthetic, prolongs the analgesic effect of the local anesthetic. Also disclosed herein is a method for providing analgesic effect in a subject in need thereof. The method uses cinnamaldehyde as an analgesic compound which, when administered alone to the subject in an analgesically effective amount, provides the analgesic effect.
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