- Preparing method for hydroxyurea
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The invention discloses a preparing method for hydroxyurea. The preparing method comprises the steps that methyl carbamate is added into a sodium hydroxide solution, then a hydroxylamine aqueous solution is dripped, and a condensation reaction is carried out after dripping is completed; pH is regulated to range from 7 to 8 through hydrochloric acid after the reaction is completed; then 70-80% of water is distilled off through decompression at the temperature of 58-62 DEG C, and then suction filtration is carried out immediately; filter liquor is added into cationic resin to be decolored and then subjected to suction filtration; filter liquor is cooled to 0-5 DEG C for heat-preservation crystallization, then suction filtration is carried out, a filter cake is washed twice through 0-5 DEG C cold water and then dried, and the hydroxyurea product is obtained. The method is easy to implement and practical, treatment steps are shortened, the yield of the hydroxyurea product is increased, solid waste and waste liquid are reduced, pollution to the environment is reduced, and environment friendliness is achieved.
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Paragraph 0036-0039
(2017/01/12)
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- Analyte detection utilizing polynucleotide sequences, composition, process and kit
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A method of detecting in a sample an analyte (A) having a molecularly recognizable portion thereon, which comprises: providing (B) a molecular bridging entity having thereon: (i) a portion capable of recognizing the molecularly recognizable portion on the analyte; and (ii) a portion comprising a polynucleotide sequence; and (C) a signalling entity having thereon: (i) a polynucleotide portion capable of annealing to the polynucleotide portion of the bridging entity, thereby to form a stable polynucleotide hybrid, and (ii) a signal generating portion; forming a complex comprising: (1) the analyte (A) complexed through its molecularly recognizable portion to (2) the recognizing portion of the entity (B); the entity (B) being complexed through the polynucleotide portion thereon to (3) the polynucleotide portion of the signalling entity; and detecting a signal by means of the signal generating portion present in the complex.
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- THERAPEUTIC FOR HEPATIC CANCER
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A novel pharmaceutical composition for treating or preventing hepatocellular carcinoma and a method of treatment are provided. A pharmaceutical composition for treating or preventing liver cancer is obtained by combining a chemotherapeutic agent with an anti-glypican 3 antibody. Also disclosed is a pharmaceutical composition for treating or preventing liver cancer which comprises as an active ingredient an anti-glypican 3 antibody for use in combination with a chemotherapeutic agent, or which comprises as an active ingredient a chemotherapeutic agent for use in combination with an anti-glypican 3 antibody. Using the chemotherapeutic agent and the anti-glypican 3 antibody in combination yields better therapeutic effects than using the chemotherapeutic agent alone, and mitigates side effects that arise from liver cancer treatment with the chemotherapeutic agent.
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- Anti-Claudin 3 Monoclonal Antibody and Treatment and Diagnosis of Cancer Using the Same
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Monoclonal antibodies that bind specifically to Claudin 3 expressed on cell surface are provided. The antibodies of the present invention are useful for diagnosis of cancers that have enhanced expression of Claudin 3, such as ovarian cancer, prostate cancer, breast cancer, uterine cancer, liver cancer, lung cancer, pancreatic cancer, stomach cancer, bladder cancer, and colon cancer. The present invention provides monoclonal antibodies showing cytotoxic effects against cells of these cancers. Methods for inducing cell injury in Claudin 3-expressing cells and methods for suppressing proliferation of Claudin 3-expressing cells by contacting Claudin 3-expressing cells with a Claudin 3-binding antibody are disclosed. The present application also discloses methods for diagnosis or treatment of cancers.
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- ISOXAZOLE-ISOXAZOLES AND ISOXAZOLE-ISOTHIAZOLES
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The present invention is concerned with isoxazole-isoxazoles and isoxazole-isothiazoles of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
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Page/Page column 16
(2010/08/22)
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- Heterocyclic compounds as inhibitors of beta-lactamases
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This invention discloses and claims methods for inhibiting bacterial β-lactamases and treating bacterial infections by inhibiting bacterial β-lactamases in man or an animal comprising administering a therapeutically effective amount to said man or said animal of a compound, or pharmaceutically acceptable salt thereof, of formula (I) either alone or in combination with a β-lactamine antibiotic wherein said combination can be administered separately, together or spaced out over time. Pharmaceutical compositions comprising a compound of formula (I), or a combination of a compound of formula (I) and a therapeutically effective amount of a β-lactamine antibiotic, and a pharmaceutically acceptable carrier are also disclosed and claimed. 1
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- Inhibitors for the soluble epoxide hydrolase
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Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
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- Agents for corneal or intrastromal administration to treat or prevent disorders of the eye
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Methods and preparations for treating disorders of the eye and/or causing dissolution of corneal proteoglycans and organized healing of corneal stroma, softening of the cornea for non-surgical refractive correction of eyesight, removing corneal haze and opacification, inhibiting fibroblasts and preventing corneal fibrosis and scar formation, treating pterigiums and treating corneal neovascularization as well as iris neovascularization. Preparations containing a) urea, b) urea derivatives (e.g., hydroxyurea, thiourea), c) antimetabolites, e) urea, urea derivatives, non-enzymatic proteins, nucleosides, nucleotides and their derivatives (e.g., adenine, adenosine, cytosine, cytadine, guanine, guanitadine, guanidinium, guanidinium chloride, guanidinium salts, thymidine, thymitadine, uradine, uracil, cysteine), reduced thioctic acid, uric acid, calcium acetyl salicylate, ammonium sulfate, isopropyl alcohol, ethanol, polyethylene glycol, polypropylene glycol or other compound capable of causing nonenzymatic dissolution of the corneal protoeglycans or f) any of the possible combinations thereof, are administered to the eye in therapeutically effective amounts.
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- Medicines for treating tumoral pathologies containing the ro5-4864 compound and an apoptosis-inducing agent
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The invention concerns the use of Ro5-4864, and compounds derived therefrom, for preparing medicines for treating tumoral pathologies. The invention also concerns said compounds combined with an apoptosis-inducing agent, as combination products for simultaneous, separate or prolonged use, in cancer therapy.
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- Method and compositions for the treatment of pruritus
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A composition for treating pruritus, comprising a compound selected from the group consisting of opioid receptor antagonists, opioid receptor agonists/antagonists, and pharmaceutically acceptable salts thereof, and a compound useful in treating the cause of the pruritus. This invention also relates to a method of treating pruritus using such compositions, and a method for preparing these compositions.
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- Thrombin inhibitors
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This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of defined compounds of formula I as thrombin inhibitors.
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- Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders
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2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.
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- Agents for intravitreal administration to treat or prevent disorders of the eye
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Methods and preparations for treating disorders of the eye and/or causing posterior vitreous disconnection or disinsertion. Preparations containing a) urea, b) urea derivatives (e.g., hydroxyurea, thiourea), c) a non-steroidal anti-inflamatory agents, d) antmetabolites, e) urea, urea derivatives, non-enzymatic proteins, nucleosides, nucleotides and their derivatives (e.g., adenine, adenosine, cytosine, cytadine, guanine, guanitadine, guanidinium, thymidine, thimitadine, uradine, uracil, cystine), uric acid, calcium acetal salicylate, ammonium sulfate or other compound capable of causing non-enzymatic dissolution of the hyaloid membrane or e) any of the possible combinations thereof, are administered to the eye in therapeutically effective amounts.
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- Substituted oximes and hydrazones as neurokinin antagonists
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Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein: a is 0-3; b, d and e are 0-2; R is H, alkyl, F or —OR6; A is an optionally substituted oxime or hydrazone; d is not 0 and X is a bond, —C(O)—, —O—, —NR9—, —S(O)e—, —N(R6)C(O)—, —C(O)N(R6)—, —OC(O)NR6—, —OC(═S)NR6—, —N(R6)C(═S)O—, —S(O)2N(R6)—, —N(R6)S(O)2—, —N(R6)C(O)O—, —OC(O)— or —N(R6)C(O)NR7—; or d is 0 and X is a bond or —NR6—; T is H, aryl, heterocycloalkyl or heteroaryl; Q is phenyl, naphthyl or heteroaryl; R6is H, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, and benzyl; R9is R6or —OR6 R6a, R7a, R8aand R9aare H or alkyl; Z is a nitrogen-containing heterocyclo group, e.g., piperidinyl, substituted by a heterocyclo- or heterocycloalkyl group; wherein phenyl, benzyl, aryl, heterocycloalkyl, heteroaryl and cycloalkyl groups are optionally substituted; methods of treating diseases such as asthma, cough, bronchospasm, depression, emesis, imflammatory diseases, and gastrointestinal disorders with said compounds, and pharmaceutical compositions comprising said compounds are disclosed.
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- Synthesis of acid addition salts of hydroxylamines
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This invention relates to novel diastereomeric acid addition salts of homochiral hydroxylamines, to processes for obtaining such, to processes for the conversion thereof to the corresponding homochiral hydroxylamines, to certain novel homochiral hydroxylamines and the processes for using these as intermediates.
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- COMPOUNDS AND METHODS FOR THE TREATMENT OF CARDIOVASCULAR, INFLAMMATORY AND IMMUNE DISORDERS
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2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i,e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.
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- ACETYLENE DERIVATIVES HAVING LIPOXYGENASE INHIBITORY ACTIVITY
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Compounds of the structure where p and q are zero or one, but cannot both be the same, M is a pharmaceutically acceptable cation or a metabolically cleavable group, B is a valence bond or a straight or branched alkylene group, R is alkyl, cycloalkyl or --NR1 R2, where R1 and R2 are hydrogen, alkyl, cycloalkyl or alkanoyl, and A is optionally substituted carbocyclic aryl, furyl, benzo[b]furyl, thienyl, or benzo[b]thienyl are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
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- N-hydroxyurea derivatives as antiallergy and antiinflammatory agents
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Compounds of formula I STR1 or salts thereof, where R is alkyl, phenyl, phenoxy or substituted phenyl and phenoxy; X is S or O; n is an integer of 1 or 2; A is --CH2 -- or --CH(CH3)--; and B is hydrogen or methyl, useful as antiallergy and antiinflammatory agents.
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- COMPOUNDS AND METHODS FOR THE TREATMENT OF DISORDERS MEDIATED BY PLATELET ACTIVATING FACTOR OR PRODUCTS OF 5-LIPOXYGENASE
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2,5-Diaryl tetrahydrofurans, 2,5-diaryl terahydrothiophenes, 2, 4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiphenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
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- ARYLALKYLETHER AND ARYLALKYLTHIOETHER INHIBITORS OF LIPOXYGENASE ENZYME ACTIVITY
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The present invention provides compounds having the structure Y-Het-[Q1]-X-[Q2 ]-Z which inhibit the catalytic action of lipoxygenase enzymes, particularly 5-lipoxygenase, and thereby reduce the biosynthesis of leukotrienes B4, C4, D4, and E4. In the generic formula given above, X is oxygen or sulfur and Het is a heteroaryl group selected from the group consisting of furyl, thienyl, 2-, 3-, and 4-pyridyl, 2- and 3-benzo[b]furyl, 2- and 3-benzo[b]thienyl and thienothienyl. Y is one or two substituents independently selected from hydrogen, hydroxy, halogen, cyano, alkyl, haloalkyl, alkoxy, alkylthio, alkoxyaryl), alkylthioaryl, ary-lalkoxy, arylalkylthio, aryloxy, arylthio, alkylamido, cycloalkyl, alkanoyl, alkoxycarbonyl, amino, alkyl-amino, dialkylamino, and the following groups wherein R, at each occurrence, is independently selected from hydrogen and alkyl of from one to six carbon atoms: -CRROR, -NRC(O)R, -NRC(O)OR, and -C-(O)NRR. The group Q1 is absent or is divalent alkylene of from one to six carbon atoms, and Q2 is divalent alkylene from two to ten carbon atoms. The group Z is N(ORi)COR2 where Ri is selected from hydrogen or a pharmaceutically suitable salt. R2 is selected from hydrogen; alkyl; cycloalkyl; amino; alkyl-amino, optionally substituted by hydroxyl, halogen, alkoxy or carboxyl; dialkylamino in which the alkyl groups are independently are optionally substituted by hydroxyl, halogen, alkoxy or carboxyl; cycloalkylamino; 2-hydroxyethylamino; N-morpholino; N-thiomorpholino; N-piperazine; N'-alkyl-N-piperazine and cyclopropylmethylamino.
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- UREA BASED LIPOXYGENASE INHIBITING COMPOUNDS
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Substituted phenyl, naphthyl, and thienyl N-hydroxy urea compounds form a class of potent inhibitors of 5-and 12-lipoxygenase and are thus useful compounds in the treatment of inflammatory disease states where leukotrienes and other products of lipoxygenase enzyme activity are implicated.
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- Aryl derivatives
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Novel compounds of formula (I) wherein: k, p and q are independently 0 or 1; Ar represents either: (i) naphthyl, tetrahydronaphthyl, pyridyl or (ii) phenyl, optionally substituted, L is selected from --(CH2)r -- (where r is 1-4), --O--, --CH2 O--, --CH2 S--, --OCH2 --, --CONH--, --NHCO--, --CO-- and --CH2 NH--, and, Ar' represents phenylene, thienylene or pyridylene optionally substituted, X represents oxygen, sulphur or carbonyl, Y is C1-10 alkylene or C1-10 alkenylene; Q represents a non-cyclic moiety selected from groups of formula STR1 in which one of m and n is 0 and the other is 1, R1 and R2 is selected from hydrogen, C1-4 alkyl, amino, C1-4 alkylamino, di-C1-4 alkylamino, C5-7 cycloalkylamino, C5-7 cycloalkyl (C1-4 alkyl) amino, anilino, N-C1-4 alkylanilino or Q represents a cyclic moiety selected from 1-hydroxy-1,3-dihydroimidazol-2-one and groups of formula STR2 in which Z represents a C2-5 alkylene chain in which one of the carbon atoms may be replaced by a hetero atom; and salts thereof.
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- HETEROARYL N-HYDROXY AMIDES AND UREAS WITH POLAR SUBSTITUENTS AS 5-LIPOXYGENASE INHIBITORS
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Compounds, compositions a method of inhibiting lipoxygenase and treating related disorders are disclosed.
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- LIPOXYGENASE INHIBITING COMPOUNDS
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Compounds having 5- and 12-lipoxygenase inhibitory activity have the structure where A is straight or branched divalent alkylene of from one to four carbon atoms, R1 is methyl, amino, or alkylamino of from one to six carbon atoms and the substituent group R2 is C1-C2 alkyl. The group R3 is one or more substituents selected from hydrogen, alkyl of from one to six carbon atoms, alkoxy of from one to six carbon atoms, thioalkoxy of from one to six carbon atoms, halogen, cyano, and trihalomethyl, and R4 is one or more substituents selected from hydrogen, alkyl of from one to six carbon atoms, alkoxy of from one to six carbon atoms, thioalkoxy of from one to six carbon atoms, hydroxy, halogen, cyano, and trihalo-methyl, with the proviso that when R1 is amino and A is >CHCH3, R3 and R4 may not both be hydrogen. The group designated M is hydrogen, a pharmaceutically acceptable cation, or a metabolically cleavable group. Pharmaceutical compositions and a method of inhibiting 5- and 12-lipoxygenase activity are also disclosed
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- Benzazole lipoxygenase inhibiting compounds
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Compounds of the formula: STR1 wherein R1 is (1) hydrogen, (2) C1 to C4 alkyl, (3) C2 to C4 alkenyl, or (4) NR2 R3, wherein R2 and R3 are independently selected from (1) hydrogen, (2) C1 to C4 alkyl and (3) hydroxyl, but R2 and R3 are not simultaneously hydroxyl; X is (1) oxygen, (2) sulfur, (3) SO2, or (4) NR4, wherein R4 is (1) hydrogen, (2) C1 to C6 alkyl, (3) C1 to C6 alkyl or (4) aroyl; A is selected from C1 to C6 alkylene and C2 to C6 alkenylene; n is 0-4; Y is selected independently at each occurrence from (1) hydrogen, (2) halogen, (3) hydroxy, (4) cyano, (5) halosubstituted alkyl, (6) C1 to C12 alkyl, (7) C2 to C12 alkenyl, (8) C1 to C12 alkoxy, (9) C3 to C8 cycloalkyl, (10) aryl, (11) aryloxy, (12) aroyl, (13) C1 to C12 arylalkyl, (14) C2 to C12 arylalkenyl, (15) C1 to C12 arylalkoxy, (16) C1 to C12 arylthioalkoxy, and substituted derivatives of (17) aryl, (18) aryloxy, (19) aroyl, (20) C1 to C12 arylalkyl, (21) C2 to C12 arylalkenyl, (22) C1 to C12 arylalkoxy, or (23) C1 to C12 arylthioalkoxy, wherein substituents are selected from halo, nitro, cyano, C1 to C12 alkyl, alkoxy, and halosubstituted alkyl; and M is hydrogen, a pharmaceutically acceptable cation, aroyl, or C1 to C12 alkoyl, are potent inhibitors of 5- and/or 12-lipoxygenase enzymes. Also disclosed are lipoxygenase inhibiting compositions and a method for inhibiting lipoxygenase.
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- Method of treating nausea and vomiting with certain substituted-phenylalkylamino (and aminoacid) derivatives and other serotonin depleting agents
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A method for the treatment of emesis in a mammal, which method comprises administering to said mammal an emesis inhibiting amount of a compound which depletes serotonin in the brain of mammals; among which are compounds having the formula: STR1 wherein, R is selected from hydrogen, loweralkyl, trifluoromethyl, carboxyl, or loweralkoxycarbonyl; R1 and R2 are hydrogen or loweralkyl; Z is trifluoromethyl or halogen; the optical isomers and pharmaceutically acceptable salts thereof; two of the preferred compounds of the invention are fenfluramine and norfenfluramine.
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- N-(3-phenoxycinnamyl)acetohydroxamic acid
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Novel compounds of formula (I) wherein: k, p and q are independently 0 or 1; Ar represents either: (i) naphthyl, tetrahydronaphthyl, pyridyl or (ii) phenyl, optionally substituted, L is selected from --(CH2)r -- (where r is 1-4), --O--, --CH2 O--, --CH2 S--, --OCH2 --, --CONH--, --NHCO--, --CO-- and --CH2 NH--, and, Ar' represents phenylene, thienylene or pyridylene optionally substituted, X represents oxygen, sulphur or carbonyl, Y is C1-10 alkylene or C1-10 alkenylene; Q represents a non-cyclic moiety selected from groups of formula STR1 in which one of m and n is 0 and the other is 1, R1 and R2 is selected from hydrogen, C1-4 alkyl, amino, C1-4 alkylamino, di-C1-4 alkylamino, C5-7 cycloalkylamino, C5-7 cycloalkyl (C1-4 alkyl) amino, anilino, N-C1-4 alkylanilino or Q represents a cyclic moiety selected from 1-hydroxy-1,3-dihydroimidazol-2-one and groups of formula STR2 in which Z represents a C2-5 alkylene chain in which one of the carbon atoms may be replaced by a hetero atom; and salts thereof.
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- N'-phenyl-N-methylurea derivatives
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A compound of the formula: STR1 wherein A is a hydrogen atom, a methyl group or a methoxy group, Rs are same or different and each a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a trifluoromethyl group, a cyano group or a methylenedioxy group, X is a hydrogen atom or a halogen atom, Y is an oxygen atom or a sulfur atom, Z is a lower alkylene group and n is an integer of 0 to 3, provided that the substituted ureido group being present at the m- or p-position to the substituent represented by the symbol X and at the same time at the m- or p-position to the substituent represented by the symbol Z, which shows herbicidal and/or fungicidal activities and can be prepared, for instance, by reacting the corresponding phenyl isocyanate with a reagent of the formula: STR2 wherein A is as defined above.
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