2561 results about "Formamides" patented technology

A novel crystalline form of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.

A pharmaceutical composition comprising Compound 1, (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide, and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering the pharmaceutical composition of Compound 1 are also disclosed.

The sulfonamide or carboamide derivatives of the formula (I) and a pharmaceutical composition which comprise them as an active ingredient:(wherein A ring, B ring is carbocyclic ring, heterocyclic ring; Z1 is -COR1, -CH=CH-COR1 etc.; Z2 is H, alkyl etc.; Z3 is single bond, alkylene; Z4 is SO2, CO; Z5 is alkyl, phenyl, heterocyclic ring etc.; R2 is CONR8, O, S, NZ6, Z7-alkylene, alkylene etc.; R3 is H, alkyl, halogen, CF3 etc.; R4 is H, (substituted) alkyl etc.; n, t is 1-4).The compounds of the formula (I) can bind to receptors of PGE2 and show antagonistic activity against the action thereof or agonistic activity. Therefore, they are considered to be useful as medicine for inhibition of uterine contraction, analgesics, antidiarrheals, sleep inducers, medicine for increase of vesical capacity or medicine for uterine contraction, cathartic, suppression of gastric acid secretion, antihypertensive or diuretic agents.

In one aspect, the invention relates to compounds, including phenylethynylbenzamide derivatives, cycloalkylethynylbenzamide derivatives, styrylbenzamide derivatives, 4-(3-phenyl-1,2,4-oxadiazol-5-yl)benzamide derivatives, 4-(pyridinylethynyl)benzamide derivatives, and N1-phenylterephthalamide derivatives, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

The present invention provides one kind of 1, 2, 3-thiobiazole-5-formamide compounds and their synthesis process and pesticide bioactivity screening. The screening system includes the determination of tobacco mosaic disease resisting activity, tobacco mosaic disease virus resistance inducing activity, and pesticidal and fungus-inhibiting activity. The related compounds are 1, 2, 3-thiobiazole-5-formamide derivatives with the general expression as shown, and include 7 hetero cycle containing 1, 2, 3-thiobiazole-5-formamide derivatives, 2 benzene ring containing 1, 2, 3-thiobiazole-5-formamide derivatives, and 2 aliphatic radical containing 1, 2, 3-thiobiazole-5-formamide derivatives.

A therapeutic composition is provided including a polysaccharide or a cationic peptide dissolved in an organic substance. The polysaccharide can be heparin or a derivative of heparin. The cationic peptide can be L-arginine, oligo-L-arginine or poly-L-arginine. The organic substance can be formamide. A method of coating an implantable medical device is also provided, comprising applying the therapeutic composition to the device and allowing the organic substance to evaporate. The device can be a stent.

There is provided a compound having a capsaicin receptor VR1 inhibitory activity and useful as a therapeutic agent for various pains including inflammatory pain and neurogenic pain, migraine, cluster headache, bladder diseases including overactive bladder, and the like. A benzamide derivative or a salt thereof wherein a benzene ring is attached to a D ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring) through an amide bond, the benzene ring is directly bonded to an E ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring), and the benzene ring is further bonded to A (an amino moiety, a monocyclic or bicyclic heterocycle) through L (a lower alkylene).

Salts and crystalline forms of 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}-sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.

The present invention provides a compound represented by the formula (I):whereinring A is a ring which is optionally further substituted;R1 is a hydrogen atom or a substituent;R2 is a hydrogen atom or a substituent;R3 is a hydrogen atom or a substituent;R4 is a hydrogen atom or a substituent;R5 is a hydrogen atom or a substituent;R6 is a hydrogen atom or a substituent;X is ═N— or ═C(Z)- (Z is a hydrogen atom or a substituent);when X is ═C(Z)-, Z and R6 are optionally bonded to each other to form, together with the carbon atom bonded thereto, an optionally substituted ring,provided that when X is ═CH—, then R6 is not optionally substituted 2-piperidinyl, excluding N-imidazo[1,2-a]pyridin-2-yl-4-methyl-benzamide, N-imidazo[1,2-a]pyridin-2-yl-benzamide and N-(7-methylimidazo[1,2-a]pyridin-2-yl)-benzamide, or a salt thereof, and a pharmaceutical agent containing same.The compound of the present invention has an ASK1 inhibitory action, and is useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, inflammatory diseases and the like, and the like.

The invention provides a method for preparing synthetic leather and the synthetic leather prepared by the method. The method comprises the following steps: (1) coating slurry containing surface waterborne polyurethane resin on the surface of release paper, and drying to form a finishing coat; (2) mixing and foaming the slurry containing the foaming waterborne polyurethane resin with air by using a foaming machine, and coating the foamed slurry on the surface of the finishing layer, and drying to form a medium foaming layer; and (3) adhering the surface of the foaming layer and a basic fabric by using an adhesive containing waterborne polyurethane resin, and drying. The method uses the waterborne resin foaming layer to replace the Base leather manufacturing process, avoids using toxic and harmful organic solvents, such as dimetbyl formamide (DMF), toluene and the like, solves the pollution problem in the synthetic leather industry, and realizes clean manufacture of the synthetic leather.

A pharmaceutical composition comprising Compound 1, (R)-1-(2,2-difluorobenzo[d][1,3]dioxo-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide, and at least one excipient selected from: a filler, a disintegrant, a surfactant, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering the pharmaceutical composition of Compound 1 are also disclosed.

The present invention relates to compounds of the formula I:wherein R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and / or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.

Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

The invention discloses a preparation method and application of pseudomonas chlororaphis for resisting disease and promoting growth. A strain is pseudomonas chlororaphis HT66CCTCC No:M2013467. A main metabolite of the strain comprises phenazine-1-phenazine and phenazine-1 formamide. The strain is inoculated into a microorganism culture medium and is fermented to obtain a thallus with high concentration and the metabolite, and can be mixed with materials like powder active carbon, bentonite, swell soil, kaolin, diatomite, zeolite, calcium carbonate and the like to prepare a microbial agent; the quantity of viable organisms in a finished product is 1-8.5*10<9>cfu / mL. The tablet laboratory verifies that the pseudomonas chlororaphis has good control effect of pathogenic bacteria of rice sheath blight diseases, cotton fusarium wilt, gaeumannomyces graminis and watermelon fusarium wilt, and also has a good promotion function in the growth of a part of plants.

A fruit juice-containing food product containing following components (a) and (b) in addition to a fruit component and a base having sweetness; and a method for reinforcing a flavor of a fruit juice-containing food product. (a) one or more refreshing feeling substances selected from the group consisting of menthol, menthone, camphor, pulegol, isopulegol, pulegone, cineol, mint oil, peppermint oil, spearmint oil, eucalyptus oil, and fractions there of. (b) one or more cool feeling substances selected from the group consisting of 3-1-menthoxypropane-1,2-diol, N-ethyl-p-menthane-3-carboxamide, 3-1-menthoxy-2-methylpropane-1,2-diol, p-menthane-3,8-diol, 2-1-menthoxyethane-1-ol, 3-1-menthoxypropane-1-ol, 4-1-menthoxybutane-1-ol, cyclic carboxamides, acyclic carboxamides,N,2,3-trimethyl-2-isopropyl butanamide, a menthoxy alkanol (alkyl group having 2 to 6 carbons), a menthoxy alkyl ether (alkyl group having 1 to 6 carbons), and a menthoxy alkanediol (alkyl group having 3 to 6 carbons).

Polymeric compounds of formula I comprising boronic acid are provided. These polymeric compounds are prepared either by grafting boronic acid containing compounds (e.g. 4-carboxyphenylboronic acid) to hydrolysed poly(N-vinylformamide) or hydrolysing copolymer(s) obtained by copolymerizing vinyl group containing boronic acid monomers (e.g. -vinylphenyl boronic acid) and N-vinylformamide. These polymeric compounds are used in increasing the wet strength of paper in paper-making processes. Formula (I).

The invention searches the novel micromolecule inhibitor pyrazolo (1, 5-a) miazines compounds of cyclin-dependent kinase CDK9 (cyclin-dependent kinase) through the virtual screening of a computer, biometrically measures activity thereof, and validates interaction mechanism. The invention specifically comprises the following steps: the three-dimensional crystal conformation of the cyclin-dependent kinase family member CDK9 is obtained in a way of homology modeling; and micromolecule three-dimensional database is screened with DOCK (molecular docking). The invention uses a MTT tumor cell growth inhibition test to biometrically measures the activity of the selected compounds, researches the selected compounds pyrazolo (1, 5-a) miazines with high activety in a way of molecular mechanism, validates the inhibiting effect of the compounds to the activity of CDK9 kinase, and clarifies the interaction mechanism of the compounds for inhibiting the external activity and the molecule of various malignancies such as lung cancer, osteosarcoma, oophoroma, cervical carcinoma, breast cancer, etc.

This invention provides novel substituted tricyclic pyridyl carboxamides which act as oxytocin receptor competitive antagonists, as well as methods of their manufacture, pharmaceutical compositions and methods of their use in treatment, inhibition, suppression or prevention of preterm labor, dysmenorrhea, endometritis, suppression of labor at term prior to caesarean delivery, and to facilitate antinatal transport to a medical facility. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.

The present disclosure provides substituted pyridyl-, pyrimidinyl-, pyrazinyl-, pyridazinyl-, and triazinyl-based carboxamides of Formula I-A: R10 Z-HET-E I-A and the pharmaceutically acceptable salts and solvates thereof, wherein Z, HET, R10 and E are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I-A to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.

The present invention includes peptidomimetic compound compositions and methods of making and using peptidomimetic compounds to modulate the activity of a peptide receptor for the treatment of one or more of hyperglycemia, insulin resistance, hyperinsulinemia, obesity, hyperlipidemia, hyperlipoproteinemia or other symptoms that relate to the function of the targeted receptor. The peptidomimetic includes an oligo-benzamide compound having at least three optionally substituted benzamides.

The present invention is related to the preparation and pharmaceutical use of novel benzamide derivatives as defined in the specification of formula (I) as histone deacetylase inhibitors (HDACI), their preparations and the methods of using these compounds or their pharmaceutically acceptable salt in the treatment of cell proliferative diseases, e.g. cancer and psoriasis

The invention relates to a preparation process of a metal-organic framework porous adsorption material for C4-C8 normal paraffin and isoparaffin adsorption separation. According to the preparation method of the synthesized metal-organic framework porous adsorption material, metal ion nitrate and an organic ligand are dissolved according to the mass ratio of 1:1-15 in a mixed solution of N,N-dimethylformamide and N,N-diethyl formamide; stirring is carried out for 0.5-12 h; reaction temperature is controlled to 80-250 DEG C, and reaction time is 12-120 h; and by a hydrothermal synthesis method, the metal-organic framework porous adsorption material is prepared. The material has characteristics as follows: specific surface area is large; pore structure height is ordered; pore size is controllable; surface potential energy is controllable; and adsorption capacity of normal paraffin is large. The material can selectively adsorb normal paraffin from mixed materials of normal paraffin and isoparaffin, has high selectivity and has a wide practical application prospect in normal paraffin and isoparaffin separation.

Novel solvates and crystal polymorphs of Ritonavir are disclosed, as well as methods of making them. Specific solvates of the compound include a formamide solvate and a partially desolvated solvate. Also disclosed are methods of making previously known forms of Ritonavir. Methods of using the novel forms of Ritonavir for the treatment of diseases, such as HIV-infection, are disclosed, as are pharmaceutical compositions and unit dosage forms comprising the novel forms of Ritonavir.

The problems of the present invention are to find a pharmaceutical composition and a method for treating cancer that exhibit excellent anti-tumor effect. Excellent anti-tumor effect is achieved when 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide, an analogous compound thereof, a pharmacologically acceptable salt thereof or a solvate thereof is used in combination with taxane.

Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.