子分类：
| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 201 | HIGHLY CHEMOSELECTIVE REACTIONS IN PRESENCE OF AROMATIC AMINO GROUPS | PCT/IN2017/050074 | 2017-02-22 | WO2017175238A1 | 2017-10-12 | DALVI, Mahesh Bhagoji; KENNY, Rajesh Shashikant; PATIL, Ajit Aappa; PALKAR, Tushar Tanaji |
: The invention discloses a novel process for highly chemoselective reactions of substituted anilines without any detectable reaction at aromatic amino group. The invention also relates to a novel process for preparation of neostigmine methylsulphate via chemoselective reaction of 3-amionphenol and aryl dimethylcarbamates. |
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| 202 | CARBAMATE COMPOUNDS AND OF MAKING AND USING SAME | PCT/US2013/020551 | 2013-01-07 | WO2013103973A1 | 2013-07-11 | CISAR, Justin, S.; GRICE, Chery, A.; JONES, Todd, K.; NIPHAKIS, Micah, J.; CHANG, Jae, Won; LUM, Kenneth, M.; CRAVATT, Benjamin, F. |
This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compunds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition. |
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| 203 | COMPOUNDS AND METHODS FOR MODULATING PROTEIN DEGRADATION | PCT/US2007/009205 | 2007-04-12 | WO2008048373A3 | 2008-04-24 | GOLDBERG, Alfred, L.; SMITH, David, M. |
Compositions and methods for altering protein degradation by the 20S proteasome are provided. Screening assays for identifying compounds that modulate protein degradation are provided. Methods of treating disorders by modulating protein degradation are also provided. |
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| 204 | RADIOLABELLED CARBAMATES | PCT/EP2007/001624 | 2007-02-26 | WO2007096193A3 | 2007-08-30 | HENRIKSEN, Gjermund |
The present invention provides a process for the preparation of a 11C of 18F- labelled carbamate comprising reacting a primary or secondary amine or an anion thereof with carbon dioxide and a compound of formula RX or R1X, wherein X represents a leaving group; R represents an alkyl or alkylene containing group; R1 represents an alkyl or alkylene containing group which group comprises a 18F-label; and said group R and/or the carbon dixoide has a 11C-labelled carbon atom. |
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| 205 | RADIOLABELLED CARBAMATES | PCT/EP2007001624 | 2007-02-26 | WO2007096193A2 | 2007-08-30 | HENRIKSEN GJERMUND |
| The present invention provides a process for the preparation of a 11C of 18F- labelled carbamate comprising reacting a primary or secondary amine or an anion thereof with carbon dioxide and a compound of formula RX or R1X, wherein X represents a leaving group; R represents an alkyl or alkylene containing group; R1 represents an alkyl or alkylene containing group which group comprises a 18F-label; and said group R and/or the carbon dixoide has a 11C-labelled carbon atom. | ||||||
| 206 | ARYL CARBAMATE OLIGOMERS FOR HYDROLYZABLE PRODRUGS AND PRODRUGS COMPRISING SAME | PCT/US2004015004 | 2004-05-06 | WO2005016240A3 | 2006-09-28 | EKWURIBE NNOCHIRI N; ODENBAUGH AMY L |
| The present invention provides a compound having a formula: (I) where R1 is selected from the group consisting of alkyl, -CH2(OC2H4)OCH3, and -(OC2H4)OCH3; n is 0-4; Olig is an oligomer having a formula (I) where L is a optional linker moiety selected from the group consisting of CH2O , CH2OX , OX , C(O) , C(O)X, NH , NHC(O) , XNHC(O) , NHC(O)X , C(O)NH , C(O)NHX , and (I), where X is alkyl1-6 or is not present, Y is N or O or is not present, and R3 is alkyl1-6; PAG is a linear or branched polyalkylene glycol moiety; R2 is an alkyl1-22 capping moiety if X is present or alkyl2-22 if X is not present; and q is a number from 1 to the maximum number of branches on PAG; and m is 1-5. | ||||||
| 207 | PEPTIDIC COMPOUNDS | PCT/AU2005/001444 | 2005-09-21 | WO2006074501A1 | 2006-07-20 | BOYLE, Timothy, Patrick; BREMNER, John, Barnard; BRKIC, Zinka; COATES, Jonathan, Alan, Victor; DALTON, Neal, Kevin; DEADMAN, John; KELLER, Paul, Anthony; MORGAN, Jody; PYNE, Stephen, Geoffrey; RHODES, David, Ian; ROBERTSON, Mark, James |
The present invention provides a compound of formula (I), (II), (III) and (IV) as defined herein and pharmaceutically acceptable derivatives thereof. The present invention further provides use of the compounds of the present invention in the treatment of bacterial infection and in the treatment of HIV infection. Also provided are pharmaceutical compositions comprising the compounds of the present invention. |
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| 208 | MODULATION OF ANXIETY THROUGH BLOCKADE OF ANANDAMIDE HYDROLYSIS | PCT/US0331844 | 2003-10-07 | WO2004033422A3 | 2004-07-29 | PIOMELLI DANIELE; DURANTI ANDREA; TONTINI ANDREA; MOR MARCO; TARZIA GEORGIO |
| Fatty acid amide hydrolase inhibitors of the Formula (I) are provided, wherein X is NH, CH2, O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R1 and R2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R1 and R2 is absent, and that, if Z is N, optionally R1 and R2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they are each attached. Pharmaceutical compositions comprising the compounds of Formula (I) and methods of using them to inhibit FAAH and/or treat appetite disorders, glaucoma, pain, insomnia, and neurological and psychological disorders including anxiety disorders, epilepsy, and depression are provided. | ||||||
| 209 | NOVEL AMINOBENZOPHENONE COMPOUNDS | PCT/DK0300900 | 2003-12-19 | WO2004056762A2 | 2004-07-08 | OTTOSEN ERIK RYTTER; BJOERKLING FREDRIK; DANNACHER HEINZ WILHELM |
| The invention provides novel compounds according to formula (I) relates to compounds with the general formula (I), said compounds being useful, e.g. in the treatment of inflammatory diseases. | ||||||
| 210 | PRODRUGS VIA ACYLATION WITH CINNAMATE | PCT/US0211330 | 2002-04-12 | WO02083067A9 | 2004-02-26 | GILBERT CARL W; MCGOWAN ELEANOR B; BLACK KIRBY S; HARPER GREGORY T P |
| A prodrug composition containing a cinnamate moiety and a biologically active molecule moiety which can be released by hydrolysis or activated by light is disclosed. The cinnamate moiety can have substituents of various electronically donating or electronically withdrawing groups to modify the cinnamate moiety's electric properties as well as photo reactivities for the purpose of achieving a proper hydrolysis rate of the acyl bond between the biologically active molecule moiety and the cinnamic acid backbone. The biologically active molecule can be any biologically active agent or diagnostic, for example, a chemotherapeutic such as a paclitaxel, campotothecin, doxorubicin, amethopterin, etoposide, or fluconazole. The prodrug composition can be modified to add a carrier moiety on the prodrug composition for targeting or to facilitate uptake of the drug. The prodrug compositions can be activated with an energy source to release the drug at the desired site. Representative energy sources can be in the form of electric force, ultrasound. Light or radiation of a radioactive material which can be administered either externally or internally. | ||||||
| 211 | METHOD FOR PRODUCING ARYL-IMINOMETHYL-CARBAMIC ACID ESTERS | PCT/EP0100262 | 2001-01-11 | WO0151457A3 | 2002-01-17 | BRANDENBURG JOERG; SOYKA RAINER; SCHMID ROLF; ANDERSKEWITZ RALF; BAUER ROLF; HAMM RAINER; KROEBER JUTTA |
| The invention relates to a method for producing compounds of formula (I) wherein the radicals R<1> and R<2> have the meanings given in the description and in the claims, which can be used on a large scale. | ||||||
| 212 | NOVEL HERBICIDES | PCT/EP9802288 | 1998-04-17 | WO9847864A3 | 1999-02-11 | REMPFLER HERMANN; MUEHLEBACH MICHEL; LUTZ WILLIAM; LUETHY CHRISTOPH |
| Compounds of formula (I) wherein R signifies halogen C1-C3-halogenalkyl, C1-C3-halogenalkoxy, cyano or nitro; Z is hydrogen or halogen; or Z and R in 2- and 3-position of the phenyl ring together form a group -O-CF2-O-; R1 signifies C1-C5-alkyl or C3-C6-cycloalkyl; R2 signifies hydrogen or C1-C4-alkyl; Q is a group (Q1) or (Q2); R3 and R4 independently of one another, signify C1-C4-alkyl, C1-C4-halogenalkyl, or benzyl which is optionally substituted on the phenyl ring; or R3 and R¿4? together signify a group (1); R5 signifies hydrogen, C1-C4-alkyl, C1-C4-halogenalkyl or optionally substituted phenyl; n is 2, 3, or 4; R6 and R7, indenpendently of one another, are hydrogen or C1-C4-alkyl; R10 is hydrogen or C1-C3-alkyl; R11 and R12, independently of one another, are hydrogen or C1-C4-alkyl; R13 signifies hydrogen, C1-C4-alkoxy; C1-C6-alkyl optionally substituted by halogen, C1-C3-alkoxy, C1-C3-alkylthio, C1-C3-alkylsulphinyl or C1-C3-alkylsulphonyl; C2-C6-alkenyl or C3-C6-cycloalkyl optionally substituted by halogen or methyl; or phenyl or thienyl optionally substituted by halogen, methyl, trifluoromethyl or methoxy; R14 is hydrogen, C1-C6-alkyl optionally substituted by halogen, C1-C3-alkoxy, C1-C3-alkylthio, C1-C3-alkylsulphinyl; or C1-C3-alkylsulphonyl; or C3-C6-cycloalkyl optionally substituted by halogen or methyl; or R13 and R14 together form a group (2), (3), (4), (5), (6) or (7); R21 and R22, independently of one another, are hydrogen or methyl; R23 signifies hydrogen, halogen or C1-C3-alkyl; m signifies 1, 2, 3 or 4; W signifies -O-, -S-, -S(O)- or -S(O)2-; o signifies 3 or 4; p signifies 1, 2 or 3; q signifies 2 or 3; and r signifies 1 or 2, as well as the diastereoisomers and enantiomers of these compounds, are suitable for use as herbicides. | ||||||
| 213 | NOVEL PENTAERYTHRITE DERIVATIVES, THE PRODUCTION AND USE THEREOF AND INTERMEDIATE PRODUCTS FOR THE SYNTHESIS OF THE SAME | PCT/DE1998/001635 | 1998-06-11 | WO98056759A2 | 1998-12-17 | |
| The invention relates to novel compounds derived from pentaerythrite as defined in the patent claims, i.e. compounds of formula (XII) and (XVI), which can be used as pharmaceutically active substances, specially in the treatment of cardiac and circulatory diseases. | ||||||
| 214 | ALKYD AND ARALKYD DERIVATIVES OF PHENOLIC POLYMERS | PCT/US1998/004121 | 1998-01-05 | WO98030596A2 | 1998-07-16 | |
| Phenolic aralkylation polymers modified by esterification with fatty acids, transesterification with glyceride oils, or other modifications to reactive hydroxyl moieties to improve the characteristics and properties of coating systems in which the modified materials are incorporated. At least a portion of the hydroxyl moieties of the polyol is esterified or otherwise modified. The hydroxyl moieties include those that have been "chain-extended", if desired. | ||||||
| 215 | S-nitrosothiols as smooth muscle relaxants and therapeutic uses thereof | PCT/US9202560 | 1992-03-30 | WO9217445A3 | 1992-12-10 | STAMLER JONATHAN S; LOSCALZO JOSEPH; SLIVKA ADAM; SIMON DANIEL; BROWN ROBERT; DRAZEN JEFFREY |
| S-nitrosothiols exert a potent relaxant effect, mediated by guanylate cyclase, upon non-vascular smooth muscle. Such types of smooth muscle include airway, gastrointestinal, bladder, uterine and corpus cavernosal. Thus, S-nitrosothiols may be used for the treatment or prevention of disorders associated with relaxation of smooth muscle, such as airway obstruction, and other respiratory disorders, bladder dysfunction, premature labor and impotence. Additionally, S-nitrosothiols may be used to alleviate smooth muscle contraction and spasm, and thus facilitate procedures involving diagnostic instrumentation, such as endoscopy, bronchoscopy, laparoscopy and cystoscopy. Figure 2 shows the relaxation effects of various S-nitrosothiols on guinea pig trachea. | ||||||
| 216 | MODIFIED CONJUGATED DIENE-BASED POLYMER | EP20892377.1 | 2020-11-27 | EP3925985A4 | 2022-04-13 | BAEK, Geun Seung; LEE, Ro Mi; LEE, He Seung; MUN, Min Sik; KIM, No Ma |
| The present invention relates to a modified conjugated diene-based polymer, more particularly, a modified conjugated diene-based polymer prepared by continuous polymerization and accordingly, having specific polymer structure, molecular weight distribution and shape, excellent processability and narrow molecular weight distribution, a unimodal shape molecular weight distribution curve by gel permeation chromatography (GPC), and molecular weight distribution (PDI; MWD) of 1.0 to less than 1.7, and including a functional group derived from a modifier represented by Formula 1 at one terminal and a functional group derived from a modification initiator at the other terminal. | ||||||
| 217 | CARBAMATE COMPOUNDS FOR USE IN THERAPY | EP20164236.0 | 2013-01-07 | EP3698782A1 | 2020-08-26 | CISAR, Justin S.; GRICE, Cheryl A.; JONES, Todd K.; NIPHAKIS, Micah J.; CHANG, Jae Won; LUM, Kenneth M.; CRAVATT, Benjamin F. |
This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compunds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition. |
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| 218 | CYCLOPROPENE AMINO ACIDS AND METHODS | EP15711271.5 | 2015-03-10 | EP3116993B1 | 2019-11-13 | ELLIOTT, Thomas |
| 219 | ELECTROLYTE CONTAINING AN AMIDE COMPOUND, AND ELECTROCHEMICAL DEVICE COMPRISING THE SAME | EP11733121.5 | 2011-01-17 | EP2525433B1 | 2016-12-07 | LEE, Byoung-Bae; OH, Jae-Seung; LEE, Sang-Hyun; CHOI, Kwon-Young; KIM, Dong-Su; HONG, Yeon-Suk; LEE, Hyo-Jin |
| 220 | TREATMENT OF CATAPLEXY | EP14778088.6 | 2014-03-12 | EP2968208A4 | 2016-10-12 | KHAYRALLAH, Moise A.; BREAM, Gary; BUTTS, Stephen E. |
| The present invention relates to a method of treating cataplexy in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of certain carbamate compounds. | ||||||
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