Treatment of cancer

The present invention provides compositions of matter, kits and methods for their use in the treatment of cancer. In particular, the invention provides compositions and methods for treating cancer in a subject by inhibiting a poly-ADP-ribose polymerase, as well as providing formulations and modes of administering such compositions.

PYRAZOLECARBOXAMIDE DERIVATIVES AND THEIR USE AS MICROBIOCIDES

Compounds of Formula (I) wherein Ris C-Calkyl or C-Chaloalkyl; Ris C-Calkyl; Ris hydrogen or halogen; Ris hydrogen, C-Calkyl or C-Chalogenalkyl; Ris hydrogen, halogen, C-Calkyl or C-Chalogenalkyl; Ris hydrogen, halogen, C-Calkyl, C-Calkenyl or C-Calkinyl; Ris hydrogen, halogen, C-Calkyl, C-Calkenyl, C-Calkinyl, C-Ccycloalkyl-C-Calkinyl, halophenoxy, halophenyi, C-Chaloalkyl, C-Chaloakoxy, C-Chaloalkenyl, or C-Chaloalkenyloxy; Ris hydrogen, halogen, C-Calkyl, C-Calkenyl or C-Calkinyl; with the provisio that at least one of R, Rand Ris different from hydrogen; n is 0 or 1, are suitable for use as microbriocides. 2. A compound of formula I according to claim 1 , wherein{'sub': '1', 'Ris difluoromethyl, trifluoromethyl or methyl,'}{'sub': '2', 'Ris methyl;'}{'sub': '3', 'Ris hydrogen or fluoro;'}{'sub': '4', 'Ris methyl;'}{'sub': '5', 'Ris hydrogen or methyl;'}n is 0; and{'sub': 6', '7', '8, 'R, Rand Rindependently from each other, are hydrogen or chloro.'}3. A compound of formula I according to claim 2 , wherein{'sub': '5', 'Ris hydrogen.'}4. A compound of formula I according to claim 1 , wherein{'sub': '1', 'Ris difluoromethyl or trifluoromethyl;'}{'sub': '2', 'Ris methyl;'}{'sub': '3', 'Ris hydrogen;'}{'sub': '4', 'Ris methyl;'}{'sub': 6', '7', '8, 'R, Rand Rare, independently from each other, hydrogen or halogen.'}5. A compound of formula I according to claim 4 , wherein R claim 4 , Rand Rare claim 4 , independently from each other claim 4 , hydrogen or chloro claim 4 , with the proviso that at least one of R claim 4 , Rand Ris different from hydrogen.6. A compound of formula I according to claim 1 , wherein{'sub': '5', 'Ris hydrogen.'}7. A compound of formula I according to claim 1 , wherein{'sub': 1', '1', '4, 'Ris C-Chaloalkyl;'}{'sub': 2', '1', '4, 'Ris C-Calkyl;'}{'sub': '3', 'Ris hydrogen;'}{'sub': 4', '1', '4, 'Ris C-Calkyl;'}{'sub': '5', 'Ris hydrogen;'}n is 0 or 1;{'sub': '6', 'Ris hydrogen or halogen;'}{'sub': 7', '8, 'Ris halogen; and Ris hydrogen or ...

C7-Fluoro Substituted Tetracycline Compounds

The present invention is directed to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.

ADAMANTANE DERIVATIVES POSSESSING ANTI-VIRAL AND ANTI-MICROBIAL ACTIVITY

The present invention relates to adamantane derivatives that are active as antiviral and anti-microbial agents; antiviral or antibacterial compositions comprising adamantane derivatives or pharmaceutically acceptable salts thereof; and methods of preventing or treating viral or bacterial infections in mammalian hosts through the administration of adamantine derivatives or their salts or pharmaceutical compositions comprising the same. In particular, viral infections prevented or treated by the methods of the present invention may include, but are not limited to, those caused by arenavirus or one or more pox viruses, such as vaccinia and/or variola. 2. An antiviral composition which comprises:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(a) an effective amount of a compound of ; and'}(b) a pharmaceutically acceptable carrier.3. An antibacterial composition which comprises:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(a) an effective amount of a compound of ; and'}(b) a pharmaceutically acceptable carrier.4. An antiviral and antibacterial composition which comprises:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(a) an effective amount of a compound of ; and'}(b) a pharmaceutically acceptable carrier.5. A method for preventing or treating a bacterial infection in a mammalian host claim 1 , said method comprising administering to a mammal in need thereof an effective amount of a compound of .6. A method for preventing or treating a viral infection in a mammalian host claim 1 , said method comprising administering to mammal in need thereof an effective amount of a compound of .7. A method for preventing or treating a viral infection in a mammalian host claim 1 , wherein said viral infection is caused by vaccinia virus claim 1 , said method comprising administering to a mammal in need thereof an effective amount of a compound of .8. A method for preventing or treating a viral infection in a mammalian host claim 1 , wherein said viral infection is caused ...

Process for Preparing Benzofurans

There is provided a process for the preparation of a compound of formula (I), wherein R, R, R, R, X and Y are as described in the description. Such compounds may, for example, be useful intermediates in the synthesis of drugs such as Dronedarone. 132.-. (canceled)352. The compound of claim wherein Z represents phenyl substituted in the para-position by —OH , —OCHor —O-benzyl. This application is a Divisional of U.S. application Ser. No. 12/681,299, filed Jul. 28, 2010; which is a National Stage of International Application No. PCT/GB08/003,341, filed Oct. 2, 2008; which claims the benefit of priority from GB Application No. 0719180.2, filed Oct. 2, 2007, the entire contents of which are incorporated by reference in their entirety.The present invention relates to a process for the manufacture of various benzofurans by reaction of an arylhydroxylamine and a ketone, and the use of such benzofurans in the synthesis of compounds, e.g. drugs, containing such cores, for instance anti-arrhythmia drugs such as Dronedarone (N-{2-(n-butyl)-3-[4-(3-dibutylamino-propoxy)-benzoyl]-benzofuran-5-yl}methane-sulfonamide).Dronedarone is a Class III anti-arrhythmia drug for the prevention of cardiac arrhythmias such as atrial fibrillation (AF). AF is a condition characterised by an irregular heart beat and occurs when the atria (the upper chambers of the heart) contract very rapidly. This causes the lower chambers of the heart, the ventricles, to contract chaotically so that blood is inefficiently pumped to the body which can lead to tissue damage and even death.Dronedarone is prepared via a stepwise procedure which involves the synthesis of a number of intermediates, including 2-butyl-3-(4-methoxybenzoyl)-5-nitrobenzofuran and 2-butyl-3-(4-hydroxybenzoyl)-5-nitrobenzofuran.2-Butyl-3-aroyl-5-nitrobenzofurans are typically synthesised via Friedel-Craft acylation of 3-unsubstituted 2-butyl-5-nitrobenzofurans. Such reactions are described in U.S. Pat. No. 5,223,510 and U.S. Pat. No. 5,854 ...

Retinoid derivatives with antitumor activity

The present invention relates to compounds of formula (I) and to pharmaceutical compositions containing them: wherein meanings of the substituents are indicated in the description. Such compounds for use in the treatment of cancer and other diseases related to altered angiogenesis, such as arthritic pathology, diabetic retinopathy, psoriasis and chronic inflammatory disease, are also within the scope of the present invention.

COMPOUNDS AND METHODS FOR TREATMENT AND PREVENTION OF FLAVIVIRUS INFECTION

The present invention concerns the use of compounds for the treatment or prevention of Flavivirus infections, such as Zika virus infections. Aspects of the invention include methods for treating or preventing Flavivirus virus infection, such as Zika virus infection, by administering a compound or class of compound disclosed herein, such as a niclosamide compound, an emricasan compound, a cyclin-dependent kinase inhibitor, a proteasome inhibitor, or a combination of two or more of the foregoing, to a subject in need thereof; methods for inhibiting Flavivirus infections such as Zika virus infections in a cell in vitro or in vivo; pharmaceutical compositions; packaged dosage formulations; and kits for treating or preventing Flavivirus infections, such Zika virus infections. 2. The method of claim 1 , wherein the at least one compound comprises a combination of two or more of the compounds.3. The method of claim 1 , wherein the Flavivirus infection is Zika virus infection.4. The method of claim 1 , wherein the at least one compound comprises a compound in Table 7 claim 1 , or a prodrug claim 1 , metabolite claim 1 , or derivative thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing.5. The method of claim 1 , wherein the at least one compound comprises the niclosamide compound claim 1 , and the niclosamide compound comprises:(a) niclosamide,(b) a niclosamide derivative,(c) a prodrug or metabolite of (a) or (b), or(d) a pharmaceutically acceptable salt of (a), (b), or (c).10. The method of claim 1 , wherein the at least one compound comprises an emricasan compound claim 1 , and wherein the emricasan compound comprises:(a) emricasan,(b) an emricasan derivative,(c) a prodrug or metabolite of (a) or (b), or(d) a pharmaceutically acceptable salt of (a), (b), or (c).12. The method of claim 1 , wherein the at least one compound comprises a combination of the niclosamide compound and the emricasan compound claim 1 , and wherein the niclosamide compound ...

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

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

Crystalline salts of (4s,4as,5ar,12as)-4-dimethylamino-3,10,12,12a-tetrahydroxy-7-[(methoxy(methyl)amino)-methyl]-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydro-naphthacene-2-carboxylic acid amide and methods of using the same

A crystalline mono hydrochloride salt of (4S,4aS,5aR,12aS)-4-dimethylamino-3,10,12,12a-tetrahydroxy-7-[(methoxy(methyl)amino)-methyl]-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydro-naphthacene-2-carboxylic acid amide is disclosed having improved stability. In addition, a crystalline mono mesylate salt and crystalline mono sulfate salt of (4S,4aS,5aR,12aS)-4-dimethylamino-3,10,12,12a-tetrahydroxy-7-[(methoxy(methyl)amino)-methyl]-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydro-naphthacene-2-carboxylic acid amide are also disclosed having improved stability. A pharmaceutical composition containing the crystalline salts and methods of treating inflammatory skin disorders and bacterial infections comprising administering the crystalline salts are also disclosed.

Pesticidal compositions and processes related thereto

This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS AND USES THEREOF

β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types. 2. The compound of claim 1 , wherein one of R claim 1 , R claim 1 , R claim 1 , and Rcomprises a chemotherapeutic moiety.4. The compound of claim 1 , wherein the chemotherapeutic moiety is a moiety of Formula (2a):{'br': None, 'sup': 11', '11', '9', '11', '11', '9, 'sub': 2', '2', '2', '2, '-A-NQ(-Z—C(R)—C(R)—R)(—C(R)—C(R)—R)\u2003\u2003(2a)'}wherein,{'sub': 2', '2', '2', '2, 'A is selected from a bond (“—”), methylene (—CH—), oxygen (—O—), methyleneoxy (—CH—O—), carbonyl (—C(═O)—), methylenecarbonyl (—CH—C(═O)—), oxycarbonyl (—O—C(═O)—), and methyleneoxycarbonyl (—CH—O—C(═O)—);'}Z is selected from a bond (“—”) and oxygen (—O—);{'sup': '−', 'Q is selected from —O (a negatively charged oxygen atom that is bound to a positively charged nitrogen atom) and a free electron pair (:);'}{'sup': '11', 'each Ris independently selected from hydrogen and deuterio; and'}{'sup': 9', '40', '40', '40', '40', '40', '40, 'sub': 2', '1-4', '1-4', '2', '1-4', '2', '6-10, 'each Ris independently selected from fluoro (—F), chloro (— ...

CRYSTALLINE SALTS OF (4S,4AS,5AR,12AS)-4-DIMETHYLAMINO-3,10,12,12A-TETRAHYDROXY-7-[(METHOXY(METHYL)AMINO)-METHYL]-1,11-DIOXO-1,4,4A,5,5A,6,11,12A-OCTAHYDRO-NAPHTHACENE-2-CARBOXYLIC ACID AMIDE AND METHODS OF USING THE SAME

A crystalline mono hydrochloride salt of (4S,4aS,5aR, 12aS)-4-dimethylamino-3,10,12,12a-tetrahydroxy-7-[(methoxy(methyl)amino)-methyl]-1, 11-dioxo-1,4,4a,5,5a,6,11,12a-octahydro-naphthacene-2-carboxylic acid amide is disclosed having improved stability. In addition, a crystalline mono mesylate salt and crystalline mono sulfate salt of (4S,4aS,5aR,12aS)-4-dimethylamino-3, 10,12,12a-tetrahydroxy-7-[(methoxy(methyl)amino)-methyl]-1,11-dioxo-1, 4,4a,5,5a,6,11,12a-octahydro-naphthacene-2-carboxylic acid amide are also disclosed having improved stability. A pharmaceutical composition containing the crystalline salts and methods of treating inflammatory skin disorders and bacterial infections comprising administering the crystalline salts are also disclosed. 1. A crystalline salt of (4S ,4aS ,5aR ,12aS)-4-dimethylamino-3 , 10 ,12 ,12a-tetrahydroxy-7- [(methoxy(methyl)amino)-methyl]-1 ,11-dioxo-1 , 4 ,4a ,5 ,5a ,6 ,11 ,12a-octahydro-naphthacene-2-carboxylic acid amide , wherein the salt is selected from a group consisting of mono hydrochloride , mono mesylate and mono sulfate.2. The crystalline salt of claim 1 , wherein the salt is substantially pure.3. The crystalline salt of claim 1 , wherein the salt is mono hydrochloride.4. The crystalline salt of claim 3 , having an XRPD pattern substantially as illustrated in after synthesis of the crystalline salt.5. The crystalline salt of claim 3 , having characteristic peaks at diffraction angle 2-theta degrees appearing at least at about 13.4 claim 3 , about 20.5 and about 23.3 claim 3 , as measured by XRPD.6. The crystalline salt of claim 3 , having a DSC curve substantially as illustrated in after synthesis of the crystalline salt.7. The crystalline salt of claim 3 , having a TGA curve substantially as illustrated in after synthesis of the crystalline salt.8. The crystalline salt of claim 3 , wherein the salt has a β-isomer content at 0 days of about 0.1% peak area to about 7.0% peak area claim 3 , as measured by HPLC.9. The ...

Styrenated Phenol Compound and Method of Preparing the Same

Provided is a styrenated phenol compound represented by Formula 1 in which styrenated phenol and hydroxylamine bind to each other: 2. The compound according to claim 1 , wherein the styrenated phenol includes mono-styrenated phenol claim 1 , di-styrenated phenol claim 1 , and tri-styrenated phenol claim 1 , and a content of the mono-styrenated phenol is 50 wt % or more based on the total weight of the styrenated phenol.3. The compound according to claim 1 , wherein the hydroxylamine is one selected from the group consisting of mono-methylhydroxylamine claim 1 , di-methylhydroxylamine claim 1 , mono-ethylhydroxylamine claim 1 , di-ethylhydroxylamine claim 1 , mono-propylhydroxylamine claim 1 , di-propylhydroxylamine claim 1 , mono-butylhydroxylamine claim 1 , di-butylhydroxylamine claim 1 , isopropylhydroxylamine claim 1 , and di-isopropylhydroxylamine.4. The compound according to claim 1 , wherein a content of the hydroxylamine is 0.1 to 15 wt % based on the total weight of the styrenated phenol compound.6. The composition according to claim 5 , wherein the styrenated phenol includes mono-styrenated phenol claim 5 , di-styrenated phenol claim 5 , and tri-styrenated phenol claim 5 , and a content of the mono-styrenated phenol is 50 wt % or more based on the total weight of the styrenated phenol.7. The composition according to claim 5 , wherein the hydroxylamine is one selected from the group consisting of mono-methylhydroxylamine claim 5 , di-methylhydroxylamine claim 5 , mono-ethylhydroxylamine claim 5 , di-ethylhydroxylamine claim 5 , mono-propylhydroxylamine claim 5 , di-isopropylhydroxylamine claim 5 , and di-isopropylhydroxylamine.8. The composition according to claim 5 , wherein a content of the hydroxylamine is 0.1 to 15 wt % based on the total weight of the styrenated phenol compound.9. The composition according to claim 5 , wherein contents of the main material part of a curing agent and the styrenated phenol compound are 70 to 90 wt % and 10 to 30 wt % ...

C7-fluoro substituted tetracycline compounds

The present invention is directed to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.

COMPOSITIONS FOR THE TREATMENT OF FIBROSIS AND FIBROSIS-RELATED CONDITIONS

The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of fibrosis and fibrosis-related conditions. 2. The compound according to claim 1 , wherein the saturated claim 1 , partly saturated or unsaturated 5- or 6-membered heterocyclyl contains one or more of N claim 1 , S or O claim 1 , optionally substituted with one or more oxo claim 1 , Calkyl claim 1 , amino claim 1 , hydroxyl or halo substituents.3. The compound according to claim 1 , wherein the saturated claim 1 , partly saturated or unsaturated 5- or 6-membered heterocyclyl is selected from pyrrolyl claim 1 , pyrazolyl claim 1 , imidazolyl claim 1 , triazolyl claim 1 , imidazolidinyl claim 1 , pyrrolidinyl claim 1 , pyrrolidinylidene claim 1 , dihydropyrrolyl claim 1 , isoxazolyl dihydrooxazolyl claim 1 , isoxazolidinyl claim 1 , oxazolidinyl and oxazolyl claim 1 , optionally substituted with one or more oxo claim 1 , Calkyl claim 1 , amino claim 1 , hydroxyl or halo substituents.4. The compound according to claim 1 , wherein the Calkoxyl amine is aminooxymethyl.5. The compound according to claim 1 , wherein the Calkyl amine is optionally substituted with one or more of Calkyl claim 1 , Chalo alkyl claim 1 , hydroxyl or halo claim 1 , preferably mono- claim 1 , di- or tri-substituted halo alkyl claim 1 , most preferably tri-fluoro methane.6. The compound according to claim 1 , wherein the Calkyl carboxylic acid is carboxylic acid.7. The compound according to claim 1 , wherein the Calkyl hydroxyl is methyl hydroxyl.8. The compound according to claim 1 , wherein the Calkyl bicyclic heterocyclyl is selected from indolyl claim 1 , isoindolyl claim 1 , insolinyl and isoindolinyl claim 1 , optionally substituted with one or more oxo claim 1 , preferably dioxo.9. The compound according to claim 1 , wherein the Calkoxyl bicyclic heterocyclyl is selected indolyl claim 1 , isoindolyl claim 1 , insolinyl and isoindolinyl claim 1 , optionally substituted with one or ...

BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS

β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types. 1. A method of treating cancer in a patient comprising administering to a patient in need of such treatment a therapeutically effective amount of (3S)-3-amino-4-[5-[bis(2-chloroethyl)amino]-2-methyl-phenyl]butanoic acid (5) , or a pharmaceutically acceptable salt thereof.2. The method of claim 1 , wherein administering comprises administering a pharmaceutical composition claim 1 , wherein the pharmaceutical composition comprises:a therapeutically effective amount of the compound or a pharmaceutically acceptable salt thereof; anda pharmaceutically acceptable vehicle.3. The method of claim 1 , wherein the cancer comprises cancerous tissue that over-expresses the LAT1/4F2hc compared to surrounding non-cancerous tissue.4. The method of claim 1 , wherein the cancer is known to be treated by administering an alkylating agent.5. The method of claim 1 , wherein the cancer is in the brain of the patient.6. The method of claim 1 , wherein the cancer comprises brain cancer.7. The method of claim 6 , wherein the brain ...

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

This document discloses molecules having the following formula (“Formula One”): 2. A molecule according to wherein R1 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.3. A molecule according to wherein R2 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.4. A molecule according to wherein R3 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , ...

PROCESS FOR THE STEREOSELECTIVE PREPARATION OF A PYRAZOLE-CARBOXAMIDE

The present invention relates to a process for the enantioselective preparation of the compound of formula (Ib), which process comprises a) reducing the (E)- or (Z)-form of a compound of formula (II), with an enantioselective reagent to a compound of formula (IIIa), and b) acylating the compound of formula (IIIa) with the compound of formula (IV), or c) coupling the compound of formula (IV) with the compound of formula (II), to give a compound of formula (V) and d) reducing compound of formula (V) in the presence of hydrogen, a catalyst and a chiral ligand, to the compound of formula (Ib). 7. The process of claim 2 , wherein the reduction of the compound of formula (II) is performed via the action of borane in the presence of a single enantiomer of a chiral amino-alcohol.8. The process according to claim 7 , wherein the source of borane is borane diethylaniline. The present invention relates to a process for the stereoselective (enantioselective) preparation of 3-(difluoromethyl)-N-methoxy-1-methyl-N-[1-methyl-2-(2,4,6-trichlorophenyl)ethyl]pyrazole-4-carboxamide.The compound 3-(difluoromethyl)-N-methoxy-1-methyl-N-[1-methyl-2-(2,4,6-trichlorophenyl)ethyl]pyrazole-4-carboxamide is described for example in WO 2010/063700. Said compound shows an excellent fungicidal activity.Said compound can occur in two enantiomeric forms, the form of the formula Iawhich chemical designation is 3-(difluoromethyl)-N-methoxy-1-methyl-N-[(1R)-1-methyl-2-(2,4,6-trichlorophenyl)ethyl]pyrazole-4-carboxamide, and the form of the formula Ibwhich chemical designation is 3-(difluoromethyl)-N-methoxy-1-methyl-N-[(1S)-1-methyl-2-(2,4,6-trichlorophenyl)ethyl]pyrazole-4-carboxamide.The enantiomer of formula Ib shows a more prominent fungicidal activity. A fungicide with an excess of the fungicidally more active enantiomer can be applied in lower concentrations with the same efficiency as the racemate which is economically advantageous. It is therefore highly desired to selectively prepare the Ib- ...

Alkoxyamines for the treatment of cancers

The present invention relates to alkoxyamines of general formula (I), and to compounds of general formula (IIa), (IIb), (IIc), (IId), IIe), (IIf) or (IIg), as such and for the treatment of cancers.

OLIGOMERIC ALKOXYAMINES

A new class of alkoxyamines, exhibiting improved stability on storage, especially in the presence of monomers and/or of solvent is described, particularly where the alkoxylamines are a new class of oligomeric alkoxyamines, which are obtained by addition of one or more monomeric entities to an alkoxyamine. 3. The use of an alkoxyamine as claimed in for synthesizing polymers.4. A polymer obtained in accordance with the use of .5. The use of an alkoxyamine as claimed in for grafting thereof on a surface.6. A composition comprising an alkoxyamine as claimed in claim 1 , a solvent and/or at least one monomer. This is the national phase of International Application No. PCT/FR2019/050918, filed Apr. 17, 2019, which claims priority to French Application No. 1853448, filed Apr. 19, 2018. The disclosure of each of these applications is incorporated herein by reference in its entirety for all purposes.The present invention concerns a new class of alkoxyamines, exhibiting improved stability on storage, especially in the presence of monomers and/or of solvent.The present invention concerns more particularly a new class of oligomeric alkoxyamines, which are obtained by addition of one or more monomeric entities to an alkoxyamine.The present invention also concerns the use of these oligomeric alkoxyamines for synthesizing polymers and copolymers, and also the polymers obtained with this new class of oligomeric alkoxyamines.The present invention also concerns the compositions comprising this new class of oligomeric alkoxyamines in the presence of monomer and/or of solvent.Alkoxyamines are molecules which allow the controlled radical polymerization of monomers exhibiting double bonds (vinylic, styrenic, (meth)acrylic, etc.). This provides access to the synthesis of block copolymers.This technology, though widely described in the literature, retains a low profile in the industrial sphere, since there are obstacles remaining: lack of compatibility with certain monomers, incomplete ...

Compositions and methods for the treatment of inflammatory bowel disease

The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing inflammatory bowel disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of gastrointestinal diseases and inflammation such as inflammatory bowel disease, ulcerative colitis, mild-to-moderate Crohn's disease, rheumatoid arthritis, inflammatory arthritis, psoriatic arthritis, liver cirrhosis and idiopathic urticaria.

Compounds for promoting liposomal and cellular adhesion and compositions and methods of use thereof

The present application describes amphiphatic compounds like compound IIa below, compositions and methods for incorporating chemoselective and bio-orthogonal complementary functional groups into liposomes. Such compounds are incorporated in greater numbers in liposome and fused cell surfaces, leading to greater adhesion and conjugation efficiency. The present application also describes various uses of these modified liposomes including for tethering the chemoselective and bioorthogonal complementary functional groups from cell surfaces by liposome delivery toward the goal of rewiring the cell surface.

NITRATED HYDROCARBONS, DERIVATIVES, AND PROCESSES FOR THEIR MANUFACTURE

Provided is a process for the formation of nitrated compounds by the nitration of hydrocarbon compounds with dilute nitric acid. Also provided are processes for preparing industrially useful downstream derivatives of the nitrated compounds, as well as novel nitrated compounds and derivatives, and methods of using the derivatives in various applications. 2. The compound of selected from formula I-1.3. The compound of claim 2 , wherein Rand Rare unsubstituted.4. The compound of claim 2 , wherein the compound is selected from the group consisting of 3-nitrodecane claim 2 , 4-nitrodecane claim 2 , 5-nitrodecane claim 2 , 4-nitrotridecane claim 2 , 5-nitrotridecane claim 2 , 7-nitrotridecane claim 2 , 2-nitrotetradecane claim 2 , 3-nitrotetradecane claim 2 , 4-nitrotetradecane claim 2 , 5-nitrotetradecane claim 2 , 6-nitrotetradecane claim 2 , 7-nitrotetradecane claim 2 , 2-nitropentadecane claim 2 , 3-nitropentadecane claim 2 , 4-nitropentadecane claim 2 , 5-nitropentadecane claim 2 , 6-nitropentadecane claim 2 , 7-nitropentadecane claim 2 , 8-nitropentadecane claim 2 , 3-nitrohexadecane claim 2 , 4-nitrohexadecane claim 2 , 5-nitrohexadecane claim 2 , 6-nitrohexadecane claim 2 , 7-nitrohexadecane claim 2 , 8-nitrohexadecane claim 2 , 2-nitroheptadecane claim 2 , 3-nitroheptadecane claim 2 , 4-nitroheptadecane claim 2 , 5-nitroheptadecane claim 2 , 6-nitroheptadecane claim 2 , 7-nitroheptadecane claim 2 , 8-nitroheptadecane claim 2 , 9-nitroheptadecane claim 2 , 3-nitrooctadecane claim 2 , 4-nitrooctadecane claim 2 , 5-nitrooctadecane claim 2 , 6-nitrooctadecane claim 2 , 7-nitrooctadecane claim 2 , 8-nitrooctadecane claim 2 , and 9-nitrooctadecane.5. The compound of selected from formula II-1.6. The compound of claim 5 , wherein Ris a linear C-Calkyl; and Ris H claim 5 , linear C-Calkyl claim 5 , or CHOH.7. The compound of claim 5 , wherein Ris H or linear C-Calkyl claim 5 , and the total number of carbons in Rand R claim 5 , together with the carbon to which they are ...

Precatalyst for shibasaki's rare earth metal binolate catalysts

Disclosed herein are schemes for the synthesis of novel hydrogen-bonded rare earth-BINOLate precatalyst complexes, the precatalysts, per se, and their application for the generation of anhydrous REMB catalysts by cation-exchange from metal halides.

Small molecule compound and synthesizing method and uses thereof

Provided is a small molecule compound as represented by structural formula (I). The product of the present invention in various concentrations and dosages can achieve an obvious change in the growth period of hairs, promoting the growth of the hairs, thus exhibiting an obvious effect of promoting hair growth. In addition, changes in the weight of a mouse in each group are slow, indicating that the test compound does not cause weight loss in an animal.

Novel inhibitors of meprin alpha and beta

The present invention relates to novel hydroxamic acid derivatives as inhibitors of meprin β and/or α, pharmaceutical compositions comprising such compounds, methods for treatment or prophylaxis of diseases or conditions, especially such that are related to meprin β and/or α, and compounds and pharmaceutical compositions for use in such methods.

COMPOUNDS AND METHODS FOR TREATMENT AND PREVENTION OF FLAVIVIRUS INFECTION

The present invention concerns the use of compounds for the treatment or prevention of Flavivirus infections, such as Zika virus infections. Aspects of the invention include methods for treating or preventing Flavivirus virus infection, such as Zika virus infection, by administering a compound or class of compound disclosed herein, such as a niclosamide compound, an emricasan compound, a cyclin-dependent kinase inhibitor, a proteasome inhibitor, or a combination of two or more of the foregoing, to a subject in need thereof; methods for inhibiting Flavivirus infections such as Zika virus infections in a cell in vitro or in vivo; pharmaceutical compositions; packaged dosage formulations; and kits for treating or preventing Flavivirus infections, such Zika virus infections. 1. A method for treating or preventing Flavivirus infection in a human or non-human animal subject , said method comprising administering an effective amount of emetine , or a pharmaceutically acceptable salt thereof , to a subject in need thereof.2. The method of claim 1 , wherein the Flavivirus infection is dengue virus infection or Zika virus infection.3. The method of claim 1 , wherein the subject has the Flavivirus infection at the time of said administering claim 1 , and the emetine or pharmaceutically acceptable salt thereof is administered as therapy.4. The method of claim 3 , further comprising claim 3 , prior to said administering claim 3 , identifying the subject as having the Flavivirus infection.5. The method of claim 4 , wherein said identifying comprises assaying a biological sample obtained from the subject for the presence of Flavivirus nucleic acids or Flavivirus proteins.6. The method of claim 5 , wherein said assaying comprises use of reverse transcriptase-polymerase chain reaction (RT-PCR) claim 5 , immunological assay claim 5 , or Plaque-reduction neutralization testing (PRNT).7. The method of claim 1 , wherein the subject does not have the Flavivirus infection at the time of ...

Beta-substituted beta-amino acids and analogs as chemotherapeutic agents

β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS AND USES THEREOF

β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types. 2. The pharmaceutical composition of claim 1 , wherein each of the first chemotherapeutic moiety and the second chemotherapeutic moiety is independently selected from the group consisting of —N(—CH—CH—Cl) claim 1 , —CH—O—N(—CH—CH—Cl) claim 1 , —CH—O—C(═O)—N(—CH—CH—Cl) claim 1 , —O—C(═O)—N(—CH—CH—Cl) claim 1 , —N(—CH—CH—OH)(—CH—CH—Cl) claim 1 , —NH—CH—CH—C claim 1 , and —NH—CH—CH—OH.3. The pharmaceutical composition of claim 1 , wherein each of the first chemotherapeutic moiety and the second chemotherapeutic moiety is —N(—CH—CH—Cl).4. The pharmaceutical composition of claim 1 , wherein Ris hydrogen.5. The pharmaceutical composition of claim 1 , wherein Ris the second chemotherapeutic moiety.6. The pharmaceutical composition of claim 1 , wherein Ris carboxylic acid (—COOH).7. The pharmaceutical composition of claim 1 , wherein claim 1 ,{'sup': '7', 'each Ris hydrogen; and'}{'sup': '8', 'Ris hydrogen.'}8. The pharmaceutical composition of claim 1 , wherein claim 1 ,{'sup': '6', 'Ris carboxylic acid (—COOH);'}{'sup ...

Novel antibiotics

Novel aryl compounds or pharmaceutically acceptable salts thereof, and uses of the same for the treatment of Gram-negative infections.

Lipids for the delivery of active agents

The present invention relates to novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides, to facilitate the cellular uptake and endosomal escape, and to knockdown target mRNA both in vitro and in vivo. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.

ADENYLYL CYCLASE INHIBITORS FOR NEUROPATHIC AND INFLAMMATORY PAIN

The invention generally relates to adenylyl cyclase inhibitor compounds and methods for treating neuropathic or inflammatory pain by using those compounds. 128-. (canceled)301. The method of claim , wherein the adenylyl cyclase is adenylyl cyclase type I (AC1). This application claims the benefit of and priority to U.S. Provisional Application No. 62/116,686, filed Feb. 16, 2015, which is incorporated by reference herein in its entirety.The invention generally relates to adenylyl cyclase inhibitors and methods of use thereof.Adenylyl cyclases are important mediators of signaling through G protein-coupled receptors. Adenylyl cyclase type 1 (AC1) belongs to a family of adenylyl cyclases that are stimulated by calcium in a calmodulin-dependent manner. Notably, AC1 is associated with chronic pain responses in several regions of the central nervous system. Accordingly, inhibition of AC1 has resulted in analgesic effects in both neuroinflammatory and neuropathic pain in rodent models. A dearth of AC1 inhibiting compounds and an inability to efficiently synthesize them means that their analgesic benefits cannot be widely realized and people continue to suffer from neuropathic and inflammatory pain.The invention generally relates to potent adenylyl cyclase inhibitor compounds. The invention further relates to methods for treating neuropathic or inflammatory pain by delivering adenylyl cyclase inhibitor compounds of the invention. Methods of the invention also provide for palladium-catalyzed γ-arylation of tertiary allylic amines and the synthesis of the disclosed AC1 inhibitor compounds as well as drug molecules such as naftifine, cinarizine, flunarizine, and analogs thereof. Heck arylation methods of the invention provide increased regio- and stereo-selectivity and yield over known methods.In certain aspects, the invention provides a compound of formula (I):wherein: X is carbon or nitrogen; n is 0 or 1; Ris selected from aryl, alkenyl, or alkyl optionally substituted by: ...

BETA-SUBSTITUTED GAMMA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS

β-Substituted γ-amino acids, β-substituted γ-amino acid derivatives, and β-substituted γ-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates, capable of passing through the blood-brain barrier, and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an increased efficacy on a variety of tumor types. 2. The compound of claim 1 , wherein claim 1 ,{'sup': '4', 'sub': '1-6', 'Ris Calkyl;'}{'sup': 2', '4', '5, 'each of R, R, and Ris hydrogen; and'}{'sup': '8', 'Ris methyl.'}3. The compound of claim 1 , wherein claim 1 ,{'sup': '4', 'Ris methyl;'}{'sup': 2', '3', '5, 'each of R, R, and Ris hydrogen; and'}{'sup': '8', 'Ris methyl.'}5. The compound of claim 1 , wherein the nitrogen mustard is a moiety having the structure of formula (2a):{'br': None, 'sup': 11', '11', '9', '11', '11', '9, 'sub': 2', '2', '2', '2, '-A-NQ(-Z—C(R)—C(R)—R)(—C(R)—C(R)—R)\u2003\u2003(2a)'}wherein,{'sub': 2', '2', '2', '2, 'A is selected from a bond (“-”), methylene (—CH—), oxygen (—O—), methyleneoxy (—CH—O—), carbonyl (—C(═O)—), methylenecarbonyl (—CH—C(═O)—), oxycarbonyl (—O—C(═O)—), and methyleneoxycarbonyl (—CH—O—C(═O)—);'}Z is selected from a bond (“-”) and oxygen (—O—);{'sup': '−', 'Q is selected from —O (a negatively ...

AMINOOXYLIPIDS FOR THE CONSTRUCTION OF SELF-ASSEMBLING LIPOSOMAL SYSTEMS ENABLING THEIR SUBSEQUENT MODIFICATION BY BIOLOGICALLY FUNCTIONAL MOLECULES

New aminooxylipids of general formula I, wherein n=5-30 and X is polymethylene linker of the general formula II where n=2-10, or X is polyethylene glycol linker of the general formula III, wherein n=1-14 are provided. A method of preparation of the aminooxylipids of general formula I characterized in that the acylation of N-tert-butoxycarbonyl-polymethylenediamine {(CH)C—O—(C═O)—HN—(CH)—NH, n=2-13}, or N-tert-butoxycarbonyl-polyethyleglycoldiamine {(CH)C—O—(C═O)—HN—(CH)—[O—(CH)]—O—(CH)NH, n=1-14} with in position C(2) symmetrically branched fatty acids of general formula IV, wherein n=5-30, in the presence of condensation reagent, or from acid of general formula IV derived acylchloride of general formula V wherein n=5-30, produces N-Boc-aminolipids of general formula VI, wherein n=5-30 a X is polymethylene linker of the general formula II or X is polyethylene glycol linker of the general formula III. 2: Aminooxylipids of general formula I according to characterized in that n=13 and X is polymethylene linker of the general formula II defined in the , wherein n=2 or 3 , or X is polyethylene glycol linker of the general formula III defined in the , wherein n=1.4: Use of the nontoxic aminooxylipids of the general formula I claim 1 , according to claim 1 , for construction and optionally subsequent modification of nontoxic self-assembling liposomal carriers of therapeutics presenting aminooxy groups.5: The use according to claim 4 , wherein the subsequent modification is a modification with biologically functional molecules using oxime ligation technique by reaction of aminooxy group with aldehyde or keto group. The present invention provides novel amino group-containing lipids with suppressed cytotoxicity, a method of their preparation and their use for the construction of self-assembling liposomal drug carriers presenting aminooxy groups. These lipids can be “post-liposomally” covalently modified by biologically functional molecules bearing aldehyde or ketone groups ...

Organic-inorganic hybrid compound, amine hydrogen iodide salt, composition for photoelectric conversion element, and photoelectric conversion element

The present invention provides a novel compound to be used in a solar cell. The compound of the present invention is an organic-inorganic hybrid compound represented by Formula (I). R 1 CH 2 N + H 3 M 1 X 1 3   (I) where, R 1 is a C1-C5 alkyl group or C2-C5 alkenyl group substituted with at least one halogen atom; M 1 is a divalent metal ion; X 1 is a monovalent halogen atom ion; and X 1 3 is formed from one type of halogen atom ion or a combination of two or more types of halogen atom ions.

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

This document discloses molecules having the following formula (“Formula One”):

C7-Fluoro Substituted Tetracycline Compounds

The present invention is directed to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.

DIVERSITY-ORIENTED SYNTHESIS OF N,N,O-TRISUBSTITUTED HYDROXYLAMINES FROM ALCOHOLS AND AMINES BY N-O BOND FORMATION

In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines. 1. A method for producing a trisubstituted hydroxylamine , the method comprising reacting a monoperoxyacetal compound with a secondary amide.2. The method of claim 1 , wherein the monoperoxyacetal compound is a cycloalkyl compound or heterocycloalkyl compound substituted with a peroxyacetal group.3. The method of claim 1 , wherein the peroxyacetal group has the formula —O—O—R claim 1 , wherein Ris a substituted or unsubstituted linear or branched alkyl group claim 1 , a substituted or unsubstituted cycloalkyl group or heterocycloalkyl group claim 1 , a polyether group claim 1 , an alkylpolyether group claim 1 , or a protected monosaccharide claim 1 , disaccharide claim 1 , or polysaccharide.7. The method of claim 5 , wherein Ris methyl or phenyl.10. A trisubstituted hydroxylamine produced by the method in .11. A method for producing a trisubstituted hydroxylamine claim 1 , the method comprising reacting a peroxybenzoate compound with a secondary amide.14. The method of claim 11 , wherein Ris tert-butyl.16. A trisubstituted hydroxylamine produced by the method in .19. The trisubstituted hydroxylamine in claim 17 , wherein Rand Rare claim 17 , independently claim 17 , an unsubstituted alkyl group claim 17 , a substituted or unsubstituted aryl group claim 17 , or a substituted or unsubstituted heteroaryl group.20. The ...

BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS

β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types. 2. The compound of claim 1 , wherein one of R claim 1 , R claim 1 , and Rcomprises a chemotherapeutic moiety.4. The compound of claim 1 , wherein the chemotherapeutic moiety is a moiety of Formula (2a):{'br': None, 'sup': 11', '11', '9', '11', '11', '9, 'sub': 2', '2', '2', '2', '2, '-A-NQ(-Z—C(R)—C(R)—R)(—C(R)—C(R)—R)\u2003\u2003(2a)'}wherein,{'sub': 2', '2', '2', '2, 'A is selected from a bond (“—”), methylene (—CH—), oxygen (—O—), methyleneoxy (—CH—O—), carbonyl (—C(═O)—), methylenecarbonyl (—CH—C(═O)—), oxycarbonyl (—O—C(═O)—), and methyleneoxycarbonyl (—CH—O—C(═O)—);'}Z is selected from a bond (“—”) and oxygen (—O—);{'sup': '−', 'Q is selected from —O(a negatively charged oxygen atom that is bound to a positively charged nitrogen atom) and a free electron pair (:);'}{'sup': '11', 'each Ris independently selected from hydrogen and deuterio; and'}{'sup': 9', '40', '40', '40', '40', '40', '40, 'sub': 2', '1-4', '1-4', '2', '1-4', '2', '6-10, 'each Ris independently selected from fluoro (—F), chloro (—Cl), ...

BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS AND USES THEREOF

β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types. 120-. (canceled)22. The compound of claim 21 , wherein each of the first chemotherapeutic moiety and the second chemotherapeutic moiety is independently selected from —N(—CH—CH—Cl) claim 21 , —CH—O—N(—CH—CH—Cl) claim 21 , —CH—O—C(═O)—N(—CH—CH—Cl) claim 21 , —O—C(═O)—N(—CH—CH—Cl) claim 21 , —N(—CH—CH—OH)(—CH—CH—Cl) claim 21 , —NH—CH—CH—C claim 21 , and —NH—CH—CH—OH.23. The compound of claim 21 , wherein each of the first chemotherapeutic moiety and the second chemotherapeutic moiety is —N(—CH—CH—Cl) claim 21 ,24. The compound of claim 21 , wherein Ris hydrogen.25. The compound of claim 21 , wherein Ris the second chemotherapeutic moiety.26. The compound of claim 21 , wherein Ris carboxylic acid (—COOH).27. The compound of claim 21 , wherein claim 21 ,{'sup': '7', 'each Ris hydrogen; and'}{'sup': '8', 'Ris hydrogen.'}28. The compound of claim 21 , wherein claim 21 ,{'sup': '6', 'Ris carboxylic acid (—COOH);'}{'sup': '7', 'each Ris hydrogen; and'}{'sup': '8', 'Ris hydrogen.'}29. The compound of claim 21 , wherein L ...

MILD AND EFFICIENT PREPARATION METHOD FOR A-ACYLOXYENAMIDE COMPOUNDS AND USE THEREOF IN SYNTHESIS OF AMIDE AND POLYPEPTIDE

Disclosed are a mild and efficient preparation method for an α-acyloxyenamide compound and a use thereof in the synthesis of an amide and a polypeptide. The α-acyloxyenamide compound is obtained by an addition reaction of a ynamide and a carboxylic acid in dichloromethane under conditions where the temperature is 0° C. to 50° C.; the produced α-acyloxyenamide compound can react with an amine compound to produce an amide or a polypeptide; the two reactions can be carried out step by step, and can also be carried out in one pot. According to the invention, the reaction conditions are mild and no metal catalyst is required; when the carboxylic acid, which has chirality on an alpha site of carboxyl, forms an amide bond or a peptide bond, no racemization occurs; and the operation is simple and the application range is wide. 2. The mild and efficient preparation method for an α-acyloxyenamide compound according to claim 1 , wherein the carboxylic acid is selected from carboxylic acids such as an aliphatic acid claim 1 , an aromatic acid claim 1 , a heterocyclic acid claim 1 , an acetylenic acid claim 1 , an olefine acid claim 1 , an α-amino acid claim 1 , and a β-amino acid.3. The mild and efficient preparation method for an α-acyloxyenamide compound according to claim 1 , wherein the molar ratio of the ynamide to the carboxylic acid is 0.1-10.4. The mild and efficient preparation method for an α-acyloxyenamide compound according to claim 1 , wherein the dichloromethane solvent is replaced with a solvent such as chloroform or 1 claim 1 ,2-dichloroethane.5. The mild and efficient preparation method for an α-acyloxyenamide compound according to claim 1 , wherein the temperature is 25° C.7. The method for synthesizing an amide and a polypeptide by directly using a carboxylic acid and an amine compound as raw materials and under the mediation of a ynamide according to claim 6 , wherein the carboxylic acid is selected from carboxylic acids such as an aliphatic acid claim 6 , ...

NITRATED HYDROCARBONS, DERIVATIVES, AND PROCESSES FOR THEIR MANUFACTURE

Provided is a process for the formation of nitrated compounds by the nitration of hydrocarbon compounds with dilute nitric acid. Also provided are processes for preparing industrially useful downstream derivatives of the nitrated compounds, as well as novel nitrated compounds and derivatives, and methods of using the derivatives in various applications. 2. The compound of selected from formula I-1.3. The compound of claim 2 , wherein Rand Rare unsubstituted.4. The compound of claim 2 , wherein the compound is selected from the group consisting of 3-nitrodecane claim 2 , 4-nitrodecane claim 2 , 5-nitrodecane claim 2 , 4-nitrotridecane claim 2 , 5-nitrotridecane claim 2 , 7-nitrotridecane claim 2 , 2-nitrotetradecane claim 2 , 3-nitrotetradecane claim 2 , 4-nitrotetradecane claim 2 , 5-nitrotetradecane claim 2 , 6-nitrotetradecane claim 2 , 7-nitrotetradecane claim 2 , 2-nitropentadecane claim 2 , 3-nitropentadecane claim 2 , 4-nitropentadecane claim 2 , 5-nitropentadecane claim 2 , 6-nitropentadecane claim 2 , 7-nitropentadecane claim 2 , 8-nitropentadecane claim 2 , 3-nitrohexadecane claim 2 , 4-nitrohexadecane claim 2 , 5-nitrohexadecane claim 2 , 6-nitrohexadecane claim 2 , 7-nitrohexadecane claim 2 , 8-nitrohexadecane claim 2 , 2-nitroheptadecane claim 2 , 3-nitroheptadecane claim 2 , 4-nitroheptadecane claim 2 , 5-nitroheptadecane claim 2 , 6-nitroheptadecane claim 2 , 7-nitroheptadecane claim 2 , 8-nitroheptadecane claim 2 , 9-nitroheptadecane claim 2 , 3-nitrooctadecane claim 2 , 4-nitrooctadecane claim 2 , 5-nitrooctadecane claim 2 , 6-nitrooctadecane claim 2 , 7-nitrooctadecane claim 2 , 8-nitrooctadecane claim 2 , and 9-nitrooctadecane.5. The compound of selected from formula IV-1.6. The compound of claim 5 , wherein Ris linear C-Calkyl claim 5 , C-Ccycloalkyl claim 5 , aryl claim 5 , or aryl-alkyl- claim 5 , and Ris H or C-Calkyl.7. The compound of claim 5 , wherein Ris C-Calkyl.8. The compound of claim 5 , wherein Ris linear C-Calkyl.9. The compound of ...

Beta-substituted beta-amino acids and analogs as chemotherapeutic agents and uses thereof

β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

OIL SOLUBLE SULFIDE SCAVENGERS WITH LOW SALT CORROSION AND METHODS OF MAKING AND USING THESE SCAVENGERS

Sulfide scavengers useful to reduce sulfide concentration in fluid streams and methods of using these scavengers. The scavengers comprise oil soluble reaction products of formaldehyde/N-substituted hydroxylamines and can be used to reduce, for example, HS content in viscous hydrocarbon oil streams. 1. A method for reducing sulfides in a fluid comprising contacting said fluid with a reaction product of a N-substituted hydroxylamine and formaldehyde (AHAF).2. A method as recited in wherein said N-substituted hydroxylamine comprises one or more members selected from the group consisting of N claim 1 ,N-dimethylhydroxylamine claim 1 , N claim 1 ,N-diethylhydroxylamine claim 1 , N claim 1 ,N-dibenzylhydroxylamine claim 1 , N-ethylhydroxylamine claim 1 , N-propylhydroxylamine claim 1 , N-isopropylhydroxylamine claim 1 , N-butylhydroxylamine claim 1 , N-phenylhydroxylamine claim 1 , N-cyclohexylhydroxylamine claim 1 , N-tert-butylhydroxylamine claim 1 , N-benzylhydroxylamine.4. The method as recited in wherein said sulfides comprise one or more members selected from the group consisting of organic sulfides claim 1 , mercaptans claim 1 , thiols claim 1 , COS claim 1 , and HS.5. The method of wherein said fluid is (i) a hydrocarbon claim 1 , (ii) natural gas claim 1 , (iii) water claim 1 , or (iv) a multiphase mixture of hydrocarbon.68-. (canceled)9. The method of wherein said hydrocarbon is a hydrocarbon oil selected from the group consisting of crude oil claim 5 , naptha claim 5 , gas oil claim 5 , bunker fuel claim 5 , marine diesel claim 5 , asphalt claim 5 , and bitumen.10. The method of wherein from about 1 to 100 claim 1 ,000 ppm by volume of said reaction product is brought into contact with said fluid based upon one million parts of said fluid.11. (canceled)12. The method as recited in wherein Rand Rare both C-Calkyl.13. The method as recited in wherein both Rand Rare ethyl.14. A method for making a dialkylhydroxylamine/formaldehyde reaction product comprising ...

Hydroxylamine esters as polymerization initiators

The invention relates to novel cyclic and open-chain hydroxylamine esters and polymerizable compositions comprising these hydroxylamine esters and an ethylenically unsaturated monomer or oligomer. The invention also relates to use as polymerization initiators and to the use of known hydroxylamine esters selected from the group consisting of HALS compounds and the novel hydroxylamine esters for the controlled degradation of polypropylene and for achieving a controlled increase in the molecular weight of polyethylene.

Process for the manufacture of nitropropanes

Provided is a process for the formation of 2-nitropropane and/or 2,2-dinitropropane by the nitration of propane with dilute nitric acid.

Aromatic diamide derivatives, chemicals for agricultural or horticultural use and usage thereof

Aromatic diamide derivatives of general formula (I) or salts thereof; chemicals for agricultural or horticultural use; and usage thereof [wherein A1 is optionally substituted C¿1-8? alkylene, C3-8 alkenylene, or the like; B is O- or -N(R?4¿)- (wherein R4 is H, C¿1-6? alkyl, halo C1-6 alkyl, or the like); R?1¿ is H, C¿1-6? alkyl, optionally substituted phenyl, an optionally substituted heterocyclic group, or the like; R?2 and R3¿ are each H, C¿3-6? cycloalkyl, or -A?2-R8¿ (wherein A2 is C(=O)-, -C(=S)-, or -C(=NR9)-; and R?8 and R9¿ are each H, C¿1-6? alkyl, or the like); Q?1 to Q5¿ are each carbon or nitrogen; X and Y are each halogeno, cyano, nitro, C¿3-6? cycloalkyl, optionally substituted phenyl, an optionally substituted heterocyclic group, or the like; n is 0 to 4; m is 1 to 5; and Z?1 and Z2¿ are each O or S]. The above chemicals exhibit remarkable controlling effects against various agricultural, forest and horticultural insect pests and stored grain insect pests which injure paddy rice, fruit trees, vegetables, other crop plants, flowers, ornamental plants, or the like.

Novel compounds

The present invention comprises novel aromatic molecules, which can be used in the treatment of pathological conditions, such as cancer, skin diseases, muscle disorders, and immune system-related disorders such as disorders of the haematopoietic system including the haematologic system in human and veterinary medicine.

N-substituted imides as polymerization initiators

The invention relates to novel N-substituted imides and polymerizable compositions com¬ prising these N-substituted imides. The invention further relates to the use of N-substituted imides as polymerization initiators. The imides are compounds of the formula (I) and (II) wherein n is 1 or 2; m is 1 or 2; R1 and R2 are each, independently of one another, hydrogen, C1-C18alkyl, C1-C-18alkenyl C6-C14aryl, aralkyl, C5-C12cycloalkyl, each of which may be substituted by halogen, C1-C4-alkyl, hydroxy, C1-C6alkoxy, carbonyl, C1-C6alkoxycarbonyl; or R1 and R2 together with the adjacent -CO-N-CO- group may form a monocyclic, bicyclic or polycyclic ring, said ring having up to 50 non hydrogen atoms and wherein said ring may contain the structural element (formula III) more than once; R3 if n is 1, is C1-C18alkyl, C6-C14aryl, aralkyl, C5-C12cycloalkyl, OR10 or SR11, NR12R13; wherein R3 if n is 2, is C2-C12alkylene, C6-C14arylene, xylylene R4 and R5, correspond to R1 and R2; R6 if n is 1, is hydrogen, C1-C18alkyl, C6-C14aryl, aralkyl, C5-C12cycloalkyl, NR14R15; wherein R6 if n is 2, is C2-C12alkylene, C6-C14arylene, xylylene; R7 is hydrogen, C1-C18alkyl, C6-C14aryl, aralkyl, C5-C12cycloalkyl, each of which may be substituted by halogen, C1-C4-alkyl, hydroxy, C1-C6alkoxy, carbonyl, C1-C6alkoxy- carbonyl; or R7 and R14 or R7 and R15 form together with the N-atom attached to R7 a 5- 6 membered ring, optionally interrupted by -NH-, -N(C1-C8alkyl)-, -O- and/or S-atoms.

Processo para preparar hidroxílaminas aromáticas ou heteroaromáticas

Alkylated and polymeric macromolecular antioxidants and methods of making and using the same

Alkylated antioxidant macromolecules are represented by Structural Formula (I), wherein the variables are described herein. Also included are methods of making the molecules and methods of using the molecules as antioxidants.

Processo per la preparazione di composti fluorurati e nuovi prodotti ottenuti.

디아미노카르보네이트 화합물 및 그것을 촉매로서 사용하는 방법(diaminocarbonate compounds and their use as catalysts)

用于治疗纤维化和纤维化相关病症的组合物

本发明涉及新的化合物及其预防性治疗和/或治疗性治疗纤维化及纤维化相关病症的用途。

Process for the controlled increase in the molecular weight of polyethylenes or polyethylene blends

본 발명은 폴리에틸렌 또는 폴리에틸렌 배합물의 분자량을 제어 증가시키는 방법에 관한 것이다. The present invention relates to a method of controlling the molecular weight of a polyethylene or polyethylene blend. 폴리에틸렌, 분자량 제어증가 Polyethylene Increases Molecular Weight Control

Compositions for treating fibrosis and fibrosis-related conditions

FIELD: chemistry.SUBSTANCE: present invention relates to a novel compound of formula:or to its pharmacologically acceptable salt. In said structural formulas A is selected from: partially saturated or unsaturated 5- or 6-member heterocyclyl selected from pyrrolyl, pyrazolyl, imidazolyl, triazolyl, imidazolidinyl, pyrrolidinyl, pyrrolidinylidene, dihydropyrrolyl, isoxazolyl-dihydrooxazolyl, isoxazolidinyl, oxazolidinyl and oxazolyl, where said partially saturated or unsaturated 5- or 6-member heterocyclyl is optionally substituted with one or more oxo, Calkyl, amino, hydroxyl or halogen; Calkoxylamine; Calkylamine, optionally substituted with one or more substitutes, which are Calkyl, Chaloalkyl, hydroxyl or halogen; Calkyl-carboxylic acid; Calkylhydroxyl; saturated or unsaturated Calkyl-bicyclic-heterocyclyl, selected from indolyl, isoindolyl, indolinyl and isoindolinyl, where said saturated or unsaturated Calkyl-bicyclic-heterocyclyl is optionally substituted with one or more oxo; and saturated or unsaturated Calkoxy-bicyclic-heterocyclyl, selected from indolyl, isoindolyl, indolinyl and isoindolinyl, where said Calkoxy-bicyclic-heterocyclyl is optionally substituted with one or more oxo.EFFECT: compound is used for preventive or therapeutic treatment of fibrosis.27 cl, 22 dwg, 15 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07C 39/15 (2006.01) C07C 47/575 (2006.01) C07C 65/03 (2006.01) C07C 211/29 (2006.01) C07C 217/48 (2006.01) C07D 207/267 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА C07D 207/36 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07D 207/408 (2006.01) C07D 207/448 (2006.01) C07D 209/48 (2006.01) (12) (13) 2 712 140 C2 C07D 233/78 (2006.01) C07D 261/14 (2006.01) C07D 263/42 (2006.01) C07D 263/44 (2006.01) A61K 31/165 (2006.01) A61K 31/192 (2006.01) A61K 31/381 (2006.01) A61K 31/42 (2006.01) A61P 1/12 (2006.01) (см. продолжение) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК (21)(22) Заявка: 2017135950, 18.03.2016 18.03.2016 (73) Патентообладатель(и): ВЕКТУС БАЙОСИСТЕМС ...

Process for preparing hydroxamic acids

본 발명은 하이드록시 또는 아미노기와 같은 반응성 치환체를 포함하지 않는 카복실산 중간체로부터 하이드록삼산을 제조하는 방법에 관한 것이다. The present invention relates to a process for preparing hydroxylsamic acid from carboxylic acid intermediates that do not contain reactive substituents such as hydroxy or amino groups.

중합반응 개시제로서 히드록실아민 에스테르

본 발명은 신규 고리상 및 열린사슬 히드록실아민 에스테르, 및 이들 히드록실아민 에스테르와 에틸렌성 불포화 단량체 또는 올리고머를 포함하는 중합성 조성물에 관한 것이다. 본 발명은 중합 개시제로서의 용도 및 폴리프로필렌의 제어분해와 폴리에틸렌 분자량의 제어증가를 위한, HALS 화합물로 구성된 군으로부터 선택된 공지 히드록실아민 에스테르와 신규 히드록실아민 에스테르의 용도에도 관한 것이다.

Method for decreasing polypropylene molecular mass

FIELD: organic chemistry, chemistry of polymers, chemical technology. SUBSTANCE: invention relates to using hydroxylamine esters for decreasing molecular mass of polypropylene, propylene copolymers or polypropylene mixtures. Method involves addition to propylene polymers subjected for destruction at least one hydroxylamine ester chosen from group including compound of the formula (IA): wherein n means 1; R a means aliphatic carboxylic acid acyl radical comprising from 2 to 18 carbon atoms; R' 1 , R' 2 and R' 3 mean independently of one another hydrogen atom or methyl group; G means aliphatic carboxylic acid acyl-acyl radical comprising from 1 to 18 carbon atoms or aromatic carboxylic acid acyl-acyl radical comprising from 7 to 18 carbon atoms of the formula (IB): wherein n means 1; R a means aliphatic carboxylic acid acyl radical comprising from 2 to 18 carbon atoms; each R' 1 , R' 2 and R' 3 means independently of one another hydrogen atom or methyl group; G 1 means hydrogen atom, (C 2 -C 18 )-alkanoyl; G 2 means hydrogen atom, (C 1 -C 8 )-alkyl, aliphatic carboxylic acid acyl-acyl radical comprising from 1 to 18 carbon atoms of the formula (IC): wherein n means 1; R a means aliphatic carboxylic acid acyl radical comprising from 2 to 18 carbon atoms; each R' 1 , R' 2 and R' 3 means independently of one another hydrogen atom or methyl group; G means (C 2 -C 8 )-alkylene, (C 4 -C 22 )-acyloxyalkylene or aliphatic carboxylic acid acyl radical comprising from 1 to 18 carbon atoms and this mixture is heated to temperature below 280°C. Addition of hydroxylamine esters results to increasing the destruction degree of used polypropylene polymer that is reflected by the melt efflux velocity value in comparison with this index of the parent polymer. EFFECT: improved method for molecular mass decreasing. 3 cl, 15 tbl ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (11) 2 298 563 (13) C2 (51) ÌÏÊ C08F 8/50 (2006.01) C07F 9/59 (2006.01) C07D 295/24 (2006.01) ...

抑制鸟氨酸脱羧酶的环状氨基氧基化合物及其用途

本发明描述了式I化合物及其盐，其中基团A为C 3 -C 6 亚环烷基；n为0或1；并且m为0或1；条件是：a)所述氨基氧基H 2 N-O-与氨基-NH 2 之间的距离至少为3个并不大于4个碳原子并且b)H 2 N-(CH 2 ) n -和-(CH 2 ) m -O-NH 2 两基团不键合到A的同一环碳原子上。所述式I化合物及其盐是鸟氨酸脱羧酶抑制剂。 H 2 N-(CH 2 ) n -A-(CH 2 ) m -O-NH 2 (I)

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7 ВУ“” 2017135950"” АЗ Дата публикации: 16.08.2019 Форма № 18 ИЗ,ПМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение 5 «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2017135950/04(06269Т) 18.03.2016 РСТ/АЧ2016/000095 18.03.2016 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 2015900979 18.03.2015 АО Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) Композиции для лечения фиброза и связанных с фиброзом состояний Заявитель: ВЕКТУС БАЙОСИСТЕМС ЛИМИТЕД, АЧ 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. П см. Примечания [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) С07С 39/15 (2006.01) С07О 207/408 (2006.01) Аб1К 31/165 (2006.01) С07С 47/575 (2006.01) С07О 207/448 (2006.01) Аб/1К 31/192 (2006.01) С07С 65/03 (2006.01) С07О 209/48 (2006.01) Аб1К 31/381 (2006.01) С07С 211/29 (2006.01) (070 233/78 (2006.01) Аб/1К 31/42 (2006.01) С07С 217/48 (2006.01) (070 261/14 (2006.01) Аб1Р 1/12 (2006.01) С07О 207/267 (2006.01) (070 263/42 (2006.01) Аб1Р 9/10 (2006.01) С07О 207/36 (2006.01) (070 263/44 (2006.01) Аб1Р 13/12 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) С07С ...

섬유증 및 섬유증 관련 질병 치료용 조성물

본 발명은 섬유증 및 섬유증 관련 질병의 예방 및/또는 치료에서의 신규 화합물 및 이의 용도에 관한 것이다.

Композиции для лечения фиброза и связанных с фиброзом состояний

一种阳离子型线性氯胺抗菌剂及其合成方法

本发明属于氯胺抗菌剂的合成与应用技术领域，提供了一种阳离子型线性氯胺抗菌剂的合成方法，以N‑叔丁基‑氯烷基酰胺Ⅱ和化合物Ⅳ为原料，制得氯胺前体化合物Ⅲ，再与次氯酸叔丁酯在常温条件下反应制得氯胺化合物Ⅰ；其中化合物Ⅳ为携不同烷基链的叔胺化合物Ⅳ 1 、携不同烷基链的吡啶化合物Ⅳ 2 及三丁基膦中的一种。本发明的制备方法，在规避氰化钾使用的同时，向线性氯胺分子中引入不同阳离子结构以改善水溶性并提高抗菌活性；而且向阳离子中心引入的长烷基链的结构与氯胺结构可产生强大的协同抗菌作用，抗菌活性较海因类氯胺有显著的提高；其有望对高效阳离子型氯胺抗菌材料的制备提供理论基础。

살충 조성물 및 그와 관련된 방법

본원은 하기 화학식 ("화학식 1")을 갖는 분자; 및 그와 관련된 방법을 개시한다. <화학식 I>

항미생물 폴리에테르 및 폴리올 화합물

본 출원은 하기 화학식 I 및 화학식 IA 의 화합물 및 본원에 기술한 바와 같이 항균제, 소독제, 항진균제, 살균제 또는 항생제를 포함하는 항미생물제로서 유용한 화합물을 기술한다:

Hydroxylamin derivatives

내용없음 No content

作为聚合引发剂的羟胺酯类

本发明涉及新型环状和开链羟胺酯类和包括这些羟胺酯类和烯属不饱和单体或低聚物的可聚合的组合物。本发明还涉及作为聚合引发剂的用途和涉及选自HALS化合物的已知羟胺酯类和该新型羟胺酯类用于聚丙烯的控制降解和实现聚乙烯的分子量的控制提高的用途。

Ингибиторы гистондеацетилазы и их композиции и способы их применения

Предусмотрены ингибиторы гистондеацетилазы (HDAC) формулы I, их композиции и способы их применения.

Pesticide compositions and related methods

FIELD: chemistry. SUBSTANCE: invention relates to a molecule of formula one, where R1 is H, F, Cl, Br or I; R2 is H, F, Cl, Br or I; R3 is H, F, Cl, Br or I; R4 is H, F, Cl, Br or I; R5 is H, F, Cl, Br or I; R6 is a (C 1 -C 8 )halogenalkyl; R7 is H; R8 is H; R9 is H; R10 is F, Cl, Br, I, (C 1 -C 8 )alkyl or halogen(C 1 -C 8 )alkyl; R11 is C(=O)N(R14)((C 1 -C 8 )alkylC(=O)R15); R12 is H; R13 is H; R14 is H; R15 is N(R16)(R17) or (C 1 -C 8 )alkyl-C(=O)N(R16)(R17); R16 is H; R17 is halogen(C 1 -C 8 )alkyl; X1 is CR12; X2 is CR13; X3 is CR9. Formula one EFFECT: obtaining novel compounds which can be used against pests. 9 cl, 3 tbl, 129 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07C 63/74 (2006.01) C07C 69/78 (2006.01) C07C 211/29 (2006.01) C07C 233/66 (2006.01) C07C 243/38 (2006.01) C07C 275/24 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА C07D 209/08 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07D 209/48 (2006.01) C07D 211/58 (2006.01) C07D 213/40 (2006.01) (12) ФОРМУЛА (21)(22) Заявка: 2013158080, 21.06.2012 21.06.2012 31.03.2017 61/500,685; 61/540,056; 61/601,077; 61/645,267 (43) Дата публикации заявки: 27.07.2015 Бюл. № 21 (45) Опубликовано: 31.03.2017 Бюл. № 10 (73) Патентообладатель(и): ДОУ АГРОСАЕНСИЗ ЛЛК (US) (86) Заявка PCT: US 2012/043418 (21.06.2012) (56) Список документов, цитированных в отчете о поиске: WO 9901422 A1, 14.01.1999. RU (87) Публикация заявки PCT: WO 2012/177813 (27.12.2012) Адрес для переписки: 119019, Москва, Гоголевский бульвар, 11, этаж 3, "Гоулингз Интернэшнл Инк.", Т.Н. Лыу 2144526 C1, 20.01.2000. RU 2416599 C2, 20.04.2011. EP 1428817 A1, 16.06.2004. WO 03016304 A1, 27.02.2003. WO 2010129497 A1, 11.11.2010. (54) ПЕСТИЦИДНЫЕ КОМПОЗИЦИИ И СВЯЗАННЫЕ С НИМИ СПОСОБЫ R U (57) Формула изобретения 1. Молекула формулы один Стр.: 1 C 2 C 2 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 24.01.2014 (72) Автор(ы): ХАНТЕР Джеймс Е. (US), ЛО Ульям С. (US), УОТСОН Джералд Б. (US), ПАТНИ Акшай (US), ГУСТАВСОН Гари Д. (US), ПЕРНИЧ Дэн (US), БРЮСТЕР ...

Ингибиторы вич интегразы

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (11) 2004 119 963 (13) A (51) ÌÏÊ C07C 229/02 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2004119963/04, 06.12.2002 (71) Çà âèòåëü(è): ÁÐÈÑÒÎË-ÌÀÅÐÑ ÑÊÂÈÁÁ ÊÎÌÏÀÍÈ (US) (30) Ïðèîðèòåò: 12.12.2001 US 60/339,674 (43) Äàòà ïóáëèêàöèè çà âêè: 10.01.2006 Áþë. ¹ 01 (86) Çà âêà PCT: US 02/39092 (06.12.2002) (87) Ïóáëèêàöè PCT: WO 03/049690 (19.06.2003) Àäðåñ äë ïåðåïèñêè: 119034, Ìîñêâà, Ïðå÷èñòåíñêèé ïåð., 14, ñòð.1, 4 ýòàæ, "Ãîóëèíãç Èíòåðíýøíë Èíê.", Þ.Â.Äåìåíòüåâîé A (54) ÈÍÃÈÁÈÒÎÐÛ ÂÈ× ÈÍÒÅÃÐÀÇÛ Ôîðìóëà èçîáðåòåíè R U A 2 0 0 4 1 1 9 9 6 3 1. Ñîåäèíåíèå ôîðìóëû I â êîòîðîé R 1 ïðåäñòàâë åò ñîáîé -àðèë, -C1-Ñ6àëêèëàðèë, -C1-Ñ6àëêèë-S(O)n-àðèë, -C1-C5àëêèë-O-àðèë; èëè êîãäà R 1 âë åòñ íåçàìåùåííûì èëè íåçàâèñèìî çàìåùåííûì 1-3 R 3; êàæäûé R 3 íåçàâèñèìî âûáèðàþò èç -Í, -ãàëîãåíà, -CN. -C1-C6àëêèëà, -Ñ3-Ñ6öèêëîàëêèëà, -OR 4, -C1-Ñ10àëêèë-O-R 4, Ñòðàíèöà: 1 RU 2 0 0 4 1 1 9 9 6 3 (74) Ïàòåíòíûé ïîâåðåííûé: Äåìåíòüåâà Þëè Âëàäèìèðîâíà R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 29.06.2004 (72) Àâòîð(û): ÓÎÊÅÐ Ìàéêë À. (US), ÁÀÍÂÈËÜ Æàê (CA), ÐÅÌÈËËÀÐÄ Ðîäæåð (CA), ÏËÀÌÎÍÄÎÍ Ñåðæ (CA) A 2 0 0 4 1 1 9 9 6 3 A R U 2 0 0 4 1 1 9 9 6 3 Ñòðàíèöà: 2 R U -CO2R 5, -Ñ1-Ñ10àëêèë-ÑÎ2R 5, -NC(R 6)(R 7), -Ñ1-Ñ10àëêèë-N(R 6)(R 7), -CON(R 6)(R 7), -C1-Ñ10àëêèë-CON(R 6)(R 7) -S(O)nR 8, -C1-Ñ10àëêèë-S(O)nR 8, -S(O)nN(R 9)(R 10), -C1-Ñ10àëêèë-S(O)nN(R 9)(R 10), -àðèëà, -O-àðèëà, -ãåòåðîàðèëà, -O-ãåòåðîàðèëà, -C1-Ñ6àëêèëàðèëà, -C1-Ñ6àëêèëãåòåðîàðèëà, -Ñ(O)-ãåòåðîöèêëè÷åñêîãî ðàäèêàëà, -C1-Ñ10àëêèë-Ñ(O)-ãåòåðîöèêëè÷åñêîãî ðàäèêàëà èëè -C1-Ñ6ãàëîãåíàëêèëà; R 2 ïðåäñòàâë åò ñîáîé -Í, -Ñ1-Ñ10àëêèë, -Ñ3-Ñ6öèêëîàëêèë, -C1-C10ãàëîãåíàëêèë, -àðèë, -ãåòåðîàðèë, -C1-Ñ6àëêèëàðèë, -C1-C5àëêèë-O-àðèë, -C1-Ñ6àëêèëãåòåðîàðèë, -C1-C5àëêèë-O-ãåòåðîàðèë, -C1-Ñ10àëêèë-OR 4, -C1-Ñ10àëêèë-CO2R 5, -Ñ1-Ñ10àëêèë-N(R 6)(R 7), -C1-Ñ10àëêèë-CON(R 6)(R7), -C1-Ñ10àëêèë-S(O)nR 8, -C1-Ñ10 ...

PROCESS FOR PREPARING A ZEOLITE-CONTAINING SOLIDS

N-замещенные имиды как инициаторы полимеризации

1. Соединения формул I и IIив которых n обозначает 1 или 2;m обозначает 1 или 2;Rи Rкаждый независимо друг от друга обозначает водородный атом, С-Салкил, С-Салкенил, С-Сарил, аралкил, С-Сциклоалкил, каждый из которых может быть замещен атомом галогена, С-Салкилом, гидроксилом, С-Салкокси, карбонилом, С-Салкоксикарбонилом; или Rи Rсовместно со смежной группой -CO-N-CO- могут образовывать моноциклическое, бициклическое или полициклическое кольцо, причем указанное кольцо содержит до 50 неводородных атомов и указанное кольцо может включать больше одного структурного элементаR, если n обозначает 1, обозначает С-Салкил, С-Салкенил, С-Сарил, аралкил, С-Сциклоалкил, каждый из которых может быть замещен атомом галогена, С-Салкилом, гидроксилом, С-Салкокси, карбонилом, C-Салкоксикарбонилом; или Rобозначает ORили SR, NRR, где Rобозначает С-Салкил, С-Сарил, аралкил, С-Сциклоалкил, каждый из которых может быть замещен атомом галогена, С-Салкилом, гидроксилом, С-Салкокси, карбонилом, C-Салкоксикарбонилом; Rобозначает С-Салкил, С-Сарил, аралкил, С-Сциклоалкил, каждый из которых может быть замещен атомом галогена, С-Салкилом, гидроксилом, С-Салкокси, карбонилом, C-Салкоксикарбонилом; a Rи Rнезависимо друг от друга обозначают водородный атом, С-Салкил, С-Сарил, аралкил, С-Сциклоалкил, каждый из которых может быть замещен атомом галогена, С-Салкилом, гидроксилом, C-Салкокси, карбонилом, C-Салкоксикарбонилом; или Rи Rобразуют совместно с атомом N, к которому они присоединяются, 5- или 6-членное кольцо, необязательно прерываемое -NH-, -N(C-Cалкил)-, -О- и/или атомами S, R, если n обозначает 2, обозначает С-Салкилен, С-Салкенилен, С-Сарилен, ксилилен при условии, что исключаются след� ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2007 121 503 (13) A (51) ÌÏÊ C08F 4/00 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2007121503/04, 31.10.2005 (71) Çà âèòåëü(è): ÖÈÁÀ ÑÏÅØÈÀËÒÈ ÊÅÌÈÊÝËÇ ÕÎËÄÈÍà ÈÍÊ. (CH) (30) ...

一种有机胺氧化物的制备方法

本发明公开了一种有机胺氧化物的制备方法，包括以下步骤：将有机胺类化合物、溶剂、碳酸乙烯酯类化合物催化剂混合升温，然后滴加过氧化氢水溶液，滴加完毕后保温反应，气相色谱检测反应液，待有机胺类化合物的含量小于0.5％时，停止反应，即得所述有机胺氧化物。本发明碳酸乙烯酯类化合物催化剂为液体，便于实现工艺连续化；后处理简单，可以省去过滤操作，能有效降低生产成本，提高经济效益。

Process for the controlled increase in the molecular weight of polyethylenes

The invention relates to novel cyclic hydroxylamine esters and to the use of known hydroxylamine esters selected from the group consisting of HALS (sterically hindered amine) compounds and the novel hydroxylamine esters achieving a controlled increase in the molecular weight of polyethylene.

Process for the controlled increase in the molecular weight of polyethylenes

The invention relates to hydroxylamine esters and polymerizable compositions comprising these hydroxylamine esters and an ethylenically unsaturated monomer or oligomer and methods for achieving a controlled increase in the molecular weight of polyethylene.

Open chain alkoxyamine compounds and their use as polymerization regulators

The invention relates to a compound of formula (Ia), (Ib) or (Ic). The open chain alkoxyamine compounds are useful for the polymerization of ethylenically unsaturated monomers. The compounds of the present invention provide polymeric resin products having low polydispersity. The polymerization process proceeds with enhanced monomer to polymer conversion efficiency. In particular, this invention relates to stable free radical-mediated polymerization processes which provide homopolymers, random copolymers, block copolymers, multiblock copolymers, graft copolymers and the like, at enhanced rates of polymerization and enhanced monomer to polymer conversions.

Process for the controlled increase in the molecular weight of polyethylenes

The invention relates to novel cyclic hydroxylamine esters and to the use of known hydroxylamine esters selected from the group consisting of HALS (sterically hindered amine) compounds and the novel hydroxylamine esters achieving a controlled increase in the molecular weight of polyethylene.

Composition for the treatment of pulmonary fibrosis

본 발명은 폐 섬유증 및/또는 관련 질환의 예방 및/또는 치료학적 치료에서의 화합물 및 이의 용도에 관한 것이다. The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related diseases.

Tetracycline compounds have been substituted for C7-fluorine

Stable 1,2-bis-adduct of nitroxide and substituted ethylene, and stabilized composition

(57)【要約】 【課題】 蒸留、加工もしくは貯蔵中のエチレン性不飽 和モノマーの早期重合のない安定な組成物のため抑制剤 の提供 【解決手段】 下式Ｉ及びIIで表される安定な立体障害 性有機ニトロキシル合物とエチレン性不飽和モノマーと の反応により形成される１，２−ビス付加物。例えば１ −オキシル−２，２，６，６−テトラメチル−４−ベン ゾイルオキシピペリジンとスチレンとの１，２−ビス− 付加物。

Process for the controlled increase in the molecular weight of polyethylenes

The invention relates to hydroxylamine esters and polymerizable compositions comprising these hydroxylamine esters and an ethylenically unsaturated monomer or oligomer and methods for achieving a controlled increase in the molecular weight of polyethylene.

Preparation of Optically Pure ß-Amino Acid Type Active Pharmaceutical Ingredients and Intermediates thereof

The present invention relates to the preparation of optically resolved chiral compounds of β-amino acid type active pharmaceutical ingredients (API), more specifically to β-aminobutyryl substituted compounds and especially β-aminobutyryl compounds having γ-bound aryl groups. The present invention more particularly relates to the preparation of enantiomerically enriched chiral compounds useful as intermediates for the preparation of anti-diabetic agents, preferably sitagliptin.

PROCESS FOR REDUCING THE POLYPROPYLENE MOLECULAR WEIGHT USING HYDROXYLAMINE ESTERS.

POLYALCOXYAMINES FROM BETA-SUBSTITUTED NITROXIDES

Polyalcoxyamines obtained from β-substituted nitroxides

The invention relates to polyalcoxyamines obtained from beta-substituted nitroxides of formula (1) wherein A represents a di- or polyvalent structure, R1 represents a molar mass of more than 15 and is a monovalent radical, and n>2. The inventive compounds can be used as initiators for (co)polymerizations of at least one radically polymerizable monomer.

Processing technique

Pyrazino [2,3-d] isoxazole derivatives

1. Производное пиразино[2,3-d]изоксазола, соответствующее следующей формуле (I):[Химическая формула 1]формула (I)где X обозначает собой атом галогена, гидроксильную группу или сульфамоилоксигруппу, и Y обозначает -C(=O)R или -CN; где R обозначает атом водорода, алкоксигруппу, арилоксигруппу, алкильную группу, арильную группу или аминогруппу; где сульфамоилоксигруппа, алкоксигруппа, арилоксигруппа, алкильная группа, арильная группа и аминогруппа могут быть необязательно замещенными.2. Производное пиразино[2,3-d]изоксазола по п.1, где Y обозначает -C(=O)R, где R обозначает алкоксигруппу или аминогруппу, и алкоксигруппа и аминогруппа могут быть необязательно замещенными.3. Производное пиразино[2,3-d]изоксазола по п.1 или 2, где X обозначает гидроксильную группу, атом хлора или атом фтора.4. Производное пиразино[2,3-d]изоксазола по п.1, где X обозначает атом фтора или атом хлора, и Y обозначает -C(=O)R, где R обозначает необязательно замещенную алкоксигруппу.5. Производное пиразино[2,3-d]изоксазола по п.1, где X обозначает атом фтора или атом хлора, и Y обозначает -C(=O)R, где R обозначает метоксигруппу, этоксигруппу, н-пропоксигруппу, изопропоксигруппу или н-бутоксигруппу.6. Способ получения производного пиразино[2,3-d]изоксазола, соответствующего следующей формуле (I-1):[Химическая формула 3]формула (I-1)где Y имеет такое же значение, как описано ниже,который включает обработку кислотой производного изоксазола, соответствующего следующей формуле (II):[Химическая формула 2]формула (II)где Y обозначает -C(=O)R или -CN; где R обозначает атом водорода, алкоксигруппу, арилоксигруппу, алкильную группу, арильную группу или аминогруппу; и Rобозначает атом водорода или алкильну� РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 498/04 (13) 2013 126 415 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2013126415/04, 11.11.2011 (71) Заявитель(и): ФУДЖИФИЛМ КОРПОРЭЙШН (JP), ТОЯМА КЕМИКАЛ КО., ЛТД. (JP) Приоритет(ы): (30) ...

Method of production of solid substance containing zeolite

FIELD: mining. ^ SUBSTANCE: invention refers to methods of zeolite production. The method of production of solid substance containing titanium-silicate-1 consists in stage (I): at least partial crystallisation of solid substance containing at least one zeolite out of synthesis mixture with production of mixture (I) including at least the said solid substance and also at least one template compound presenting tetrapropylammonia hydroxide as an additive; stage (II): concentration of solid substance which is present in mixture (I) by ultra-filtration with obtaining retentate and permeate; notably, that permeate contains the said at least one template compound; stage (III): agglomeration or granulation or agglomeration and granulation of particles of solid substance in retentate from stage (II); also permeate produced at stage (II) containing the said at least one template compound at least partially is returned to stage (I); while ultra-filtration is performed with implementing at least one membrane containing dividing layers with diametre of pores from 50 nm to 200 nm. ^ EFFECT: invention facilitates re-circulating template compounds to stage of re-crystallising. ^ 9 cl, 1 dwg РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 353 580 (13) C2 (51) МПК C01B 39/02 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21), (22) Заявка: 2005103819/15, 17.07.2003 (24) Дата начала отсчета срока действия патента: 17.07.2003 (73) Патентообладатель(и): БАСФ Акциенгезелльшафт (DE) (43) Дата публикации заявки: 10.09.2005 2 3 5 3 5 8 0 (45) Опубликовано: 27.04.2009 Бюл. № 12 (56) Список документов, цитированных в отчете о поиске: SU 1799355 A3 28.02.1993. WO 0226380 A1 04.04.2002. WO 9855229 A1 10.12.1999. US 5919721 A 06.07.1999. 2 3 5 3 5 8 0 R U (86) Заявка PCT: EP 03/07767 (17.07.2003) C 2 C 2 (85) Дата перевода заявки PCT на национальную фазу: 17.02.2005 (87) Публикация PCT: WO 2004/007369 (22.01.2004) Адрес для ...

The tetracycline compound that C7-fluorine replaces

本发明公开了一种C7-氟取代的四环素化合物，所述化合物为由下列结构式表示的化合物：

Chemical liquid for dissolution modification and dissolution modification processesing method

본 발명은 유기막 패턴에 대해 균일한 용해 변형 처리를 실시할 수 있는 용해 변형용 약액을 제공하는 것을 목적으로 한다. 본 발명은 유기막 패턴의 용해 변형 처리에 사용하는 약액으로서, 아미드류 및 니트릴류 중 적어도 어느 1 종을 함유하는 용해 변형용 약액이다. 또, 본 발명은 유기막 패턴의 용해 변형 처리에 사용하는 약액으로서, 적어도 질소 함유 알칼리 성분과 용해 변형용 용제를 함유하는 용해 변형용 약액이다. An object of the present invention is to provide a solution for dissolution deformation that can be subjected to a uniform solution for dissolution deformation of an organic film pattern. The present invention is a chemical liquid for use in the dissolution deformation treatment of an organic film pattern, and is a chemical solution for dissolution deformation containing at least one of amides and nitriles. Moreover, this invention is a chemical | medical solution for dissolution deformation containing at least a nitrogen containing alkali component and a solvent for dissolution deformation | transformation as a chemical liquid used for the dissolution deformation process of an organic film pattern. 용해 변형 처리, 용해 변형용 약액, 유기막 패턴, 리플로우 처리, 리플로우 용제 Melt strain treatment, melt strain chemicals, organic film pattern, reflow treatment, reflow solvent

Triazolopyrimidines

本发明涉及新的式(I)三唑并嘧啶化合物，其中R 1 、R 2 、R 3 、R 4 和X具有说明书中给出的含义。本发明还涉及制备所述新化合物的多种方法，和所述化合物在抗不需要的微生物中的应用，新的式(II)、(V)中间体产物及其制备方法，以及具有说明书所示的式的新的胺和氨基甲酸酯化合物及其制备方法。

Ornithine decarboxylase inhibiting cyclic aminooxidants

Описаны соединения формулы IHN-(CH)-A-(CH)-O-NH(I)и их соли, в которых радикал А представляет собой С-Сциклоалкилен; n = 0 или 1 и, независимо от n, m = 0 или 1; при условии , что а) расстояние между аминооксирадикаломN-O- и аминогруппой -NHравно по меньшей мере 3, но не более 4 атомов углерода и что б) два радикала HN-(CH)- и - (CH)-O-NHне присоединены к одному и тому же атому углерода цикла А. Соединения формулы I и их соли являются ингибиторами орнитиндекарбоксилазы

Method of preparing n,n-dichloramide of terephthalic or isophthalic acid

Naphthalene-containing cyclic hydrocarbon compounds for the treatment of disturbances of calcium sensor receptor activity

PROCESS FOR THE PREPARATION OF POLYPEPTIDES SUITABLE AS ANTAGONISTS OF EXCITATORY AMINO ACID NEUROTRANSMITTERS AND / OR BLOCKS OF THE CALCIUM CHANNELS

Die Erfindung betrifft Verfahren zur Herstellung bestimmter Polypeptide, die in dem Gift der Agelenopsis aperta Spinne gefunden wurden. Die Polypeptide der Erfindung und eines der Polyamine und deren Salze blockieren Calciumkanaele in Zellen verschiedener Organismen und sind geeignet zum Blockieren der Calciumkanaele in Zellen an sich, in der Behandlung von mit Calciumkanaelen in Verbindung stehenden Krankheiten und Zustaende und zur Kontrolle von wirbellosen Schaedlingen. Die Erfindung betrifft auch Zusammensetzungen, enthaltend die Polyamine, Polypeptide und deren Salze.{Polyamine; Polypeptide; Agelenopsis; Spinne; Neurotransmitter, exzitatorisch; Calciumkanaele; Schaedlinge; Gift} The invention relates to methods of producing certain polypeptides found in the venom of the Agelenopsis aperta spider. The polypeptides of the invention and one of the polyamines and their salts block calcium channels in cells of various organisms and are useful for blocking the calcium channels in cells themselves, in the treatment of calcium channel-related diseases and conditions, and for the control of invertebrate pests. The invention also relates to compositions containing the polyamines, polypeptides and their salts. {Polyamines; polypeptides; Agelenopsis; Spider; Neurotransmitter, excitatory; Calciumkanaele; Pest; Gift}

Use of polyamines as ionic-channel regulating agents

Polyamine compounds are used as agents regulating ionic conductances in cellular membranes. These polyamines are used in blocking, modulating or activating calcium and other cationic channels in neuronal cell membranes and in blocking, modulating or activating calcium channels of a specific type in any cell membrane when such channels are present.

Pesticide compositions and related methods

FIELD: agriculture. SUBSTANCE: composition includes a molecule according to Formula One: , where: (a) R1 is selected from: (1) H, F, Cl, Br, I, CN, NO 2 , (C 1 -C 8 )alkyl, halo (C 1 -C 8 )alkyl, (C 1 -C 8 )alkoxy, halo(C 1 -C 8 )alkoxy, S(C 1 -C 8 )alkyl, S(halo(C 1 -C 8 )alkyl), S(O)(C 1 -C 8 )alkyl, S(O)(halo(C 1 -C 8 ) alkyl), S(O) 2 (C 1 -C 8 )alkyl, S(O) 2 (halo(C 1 -C 8 )alkyl), N(R14)(R15), (2) substituted (C 1 -C 8 )alkyl, where the substituted (C 1 -C 8 )alkyl has one or more substituents selected from CN and NO 2 , (3) substituted halo(C 1 -C 8 ) alkyl, where the said substituted halo(C 1 -C 8 )alkyl has one or more substituents selected from CN and NO 2 , (4) substituted (C 1 -C 8 )alkoxy, where the substituted (C 1 -C 8 )alkoxy has one or more substituents selected from CN and NO 2 , and (5) substituted halo (C 1 -C 8 )alkoxy, where the substituted halo(C 1 -C 8 )alkoxy has one or more substituents selected from CN and NO 2 ; (b) R2 is selected from: (1) H, F, Cl, Br, I, CN, NO 2 , (C 1 -C 8 )alkyl, halo(C 1 -C 8 )alkyl, (C 1 -C 8 ) alkoxy, halo(C 1 -C 8 )alkoxy, S(C 1 -C 8 )alkyl, S(halo(C 1 -C 8 )alkyl), S(O)(C 1 -C 8 )alkyl, S(O)(halo(C 1 -C 8 )alkyl), S(O) 2 (C 1 -C 8 )alkyl, S(O) 2 (halo(C 1 -C 8 )alkyl), N(R14)(R15), (2) substituted (C 1 -C 8 )alkyl, where the substituted (C 1 -C 8 )alkyl has one or more substituents selected from CN and NO 2 , (3) substituted halo(C 1 -C 8 )alkyl, where the substituted halo(C 1 -C 8 )alkyl has one or more substituents selected from CN and NO 2 ,(4) substituted (C 1 -C 8 )alkoxy, where the substituted (C 1 -C 8 )alkoxy has one or more substituents selected from CN and NO 2 , and (5) substituted halo(C 1 -C 8 )alkoxy, where the substituted halo(C 1 -C 8 )alkoxy has one or more substituents selected from CN and NO 2 ; (c) R3 is selected from: (1) H, F, Cl, Br, I, CN, NO 2 , (C 1 -C 8 )alkyl, halo(C 1 -C 8 )alkyl, (C 1 -C 8 )alkoxy, halo(C 1 -C 8 )alkoxy, S(C 1 -C 8 )alkyl, S(halo(C 1 -C 8 )alkyl), S(O)(C 1 -C 8 ) ...

Process for producing acylhydrazones of formylacetic acid ester

A process is provided for production of acylhydrazones of formyl-acetic acid ester of the general formula <IMAGE> wherein R1 is an alkyl group with from 1 to 6 carbon atoms and R2 is an alkoxy group or an amino group. A propiolic acid ester of the general formula H-C 3BOND C-COOR1 is contacted with hydrazine derivatives of the general formula H2N-NH-CO-R2 in the presence of a solvent such as water or a lower alcohol. The resulting products are technically valuable starting materials for the production of biocides, for example of 1,2,3-thiadiazole derivatives.

Substituted tetracycline compounds

本发明至少部分涉及新的取代四环素化合物。这些四环素化合物能够用于治疗很多四环素化合物敏感性疾病，例如细菌感染和肿瘤，以及其它已知的通常应用二甲胺四环素和四环素化合物的疾病，例如阻断四环素流出和调节基因表达。