- Continuous preparation method of metal fatty acid salt
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The invention relates to a continuous preparation method of metal fatty acid salt. The continuous preparation method of the metal fatty acid salt comprises the step of continuously enabling fatty acidand metal hydroxides to react in a solvent and prepare the metal fatty acid salt in a microchannel reactor or pipeline reactor. The preparation method disclosed by the invention can control the particle diameter of a product material to be within 70nm and 1000nm, and the particle diameter of the product material can be adjusted as needed; the metal fatty acid salt is simple in preparation method,short in technological process, few in three wastes (waste water, waste residues and waste gas), beneficial to environmental protection and suitable for industrial production; the reactor used in theinvention has short reaction time, high safety, high efficiency and large productivity, and can realize continuous production, furthermore, the space utilization rate of workshops is high, and mass production can be realized; by adopting the preparation method disclosed by the invention, the solvent can be recycled to lower the production cost; and the preparation method has high conversion rateof raw materials, stable quality and high purity.
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Paragraph 0088; 0089; 0090; 0091
(2019/04/04)
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- Magnesium stearate and preparation process thereof
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The invention belongs to the technical field of chemical engineering, and particularly relates to magnesium stearate and a preparation process thereof. The preparation process includes the following steps: (1) subjecting tristearin and water to hydrolysis under the action of catalyst and antioxidant; (2) adding magnesium oxide and catalyst step by step, and performing condensation, dehydration and salifying to synthesize magnesium stearate. The magnesium stearate provided is industrial-grade magnesium stearate, and is low in raw material cost, high in production yield, good in color, low in free acid content and stable in quality. In the preparation process of magnesium stearate, discharge of wastewater containing chlorine and sulfate ions is avoided, the production process is safe and environment friendly, and overall production cost is low. The provided magnesium stearate is high in quality, and is more practical and comparable than similar products on the market in practical application.
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Paragraph 0033-0037
(2018/02/04)
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- Dissolution of soap scum by surfactant part I: Effects of chelant and type of soap scum
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The equilibrium solubilities of two model soap scums [calcium stearate and magnesium stearate: Ca(C18)2 and Mg(C18) 2] were measured in aqueous solutions containing three different types of surfactants: methyl ester sulfonate (MES) as an anionic; alcohol ethoxylate (EO9) as a nonionic; and dimethyldodecylamine oxide (DDAO) as an amphoteric with and without a chelating agent [disodium ethylenediaminetetraacetate (Na2EDTA)]. The solubility of calcium soap scum was generally higher than that of magnesium soap scum, the exception being some DDAO systems. The use of the DDAO surfactant with the Na 2EDTA chelating agent at high pH gives the highest solubilities of both studied soap scums. The soap scum solubility is on the order of 2,000 times that in water at high pH. The DDAO is the most effective surfactant under all conditions. The MES is more effective than the EO9 at low pH with the opposite trend observed at high pH. The synergism from added chelant is generally greater at higher pH and is greatest for DDAO followed by EO9.
- Itsadanont, Sawwalak,Scamehorn, John F.,Soontravanich, Sukhwan,Sabatini, David A.,Chavadej, Sumaeth
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p. 849 - 857
(2014/11/08)
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- Use of selectively moisture-adjusted tabletting material in the production of mechanically stable tablets which contain at least one hydrate-forming active substance and/or adjuvant relevant to the mechanical stability of the tablets, particularly arginine-containing tablets
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The present invention relates inter alia to the use of selectively moisture-adjusted tabletting material in the preparation of mechanically stable oral tablets which contain at least one hydrate-forming active substance and/or adjuvant relevant to the mechanical stability of the tablets, particularly arginine-containing oral tablets.
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Page/Page column
(2014/04/18)
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- Glutathione and Acetaminophen Composition and Preparation Method Thereof
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A pharmaceutical composition of glutathione and acetaminophen and preparation method thereof. The active ingredients of the composition include glutathione with composition ration of 0.1%?99.9% and acetaminophen with composition ratio of 99.9%?0.1%. The further purpose of the invention is to prepare glutathione and acetaminophen composition (raw materials) into various pharmaceutically acceptable dosage forms, such as tablets, sustained/controlled release preparations, capsules, pills, syrups, films, granules, oral solutions, oral suspensions, oral emulsions and oral powders. The beneficial effects of the invention is reflected in that glutathione and acetaminophen combination can effectively prevent the liver cell damage and necrosis caused by acetaminophen overdose and is strongly in favor of cancer pain relief and chemotherapy.
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Page/Page column
(2014/07/08)
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- METHODS AND COMPOSITIONS USING ERGOTHIONEINE TO TREAT A VARIETY OF HEALTH RELATED FACTORS
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In one embodiment, a composition containing ergothioneine and/or synthesized l-ergothioneine and one or more compounds selected from the group consisting of vitamin B-12, glucosamine sulfate, calcium ascorbate, turmeric extract, black pepper extract, hyaluronic acid, collagen, glycosaminoglycans, cat's claw extract, acai berry; and white willow bark extract is provided to a mammal to improve a variety of health related factors, including but not limited to brain health, joint health, eye health, mitondchorial optimization/improvement and reduction of inflammation and pain in a mammal.
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- Pharmaceutical composition for the prevention and treatment of liver disease comprising a lonicera caerulea L. Var. Edulis extract
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Disclosed herein is a pharmaceutical composition having preventative and therapeutic effects on liver diseases, comprising an extract from Lonicera caerulea L. var. edulis. The composition has preventative and therapeutic effects on hepatitis, liver cirrhosis, fatty liver, and the like.
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- COMPOSITION CONTAINING PEPTIDE AS THE ACTIVE INGREDIENT
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The invention provides a composition used for promoting glucose uptake, which comprises a peptide having an effect of promoting glucose uptake as the active ingredient, as well as a composition comprising a dipeptide containing leucine and/or isoleucine as the active ingredient. The composition is effective in preventing or treating diabetes mellitus or an elevation of blood glucose level, in promoting glycogen storage, or in enhancing physical strength, enhancing athletic ability, improving endurance performance or relieving fatigue.
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- Formulations comprising selective androgen receptor modulators
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The present invention relates to pharmaceutical compositions and formulations comprising a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia,osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; and/or e) decreasing the incidence of, halting or causing a regression of prostate cancer. The present invention provides pharmaceutical compositions comprising the selective androgen receptor modulator compounds, together with pharmaceutically acceptable excipients.
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- Preventives/remedies for alzheimer's disease
-
The present invention provides an agent for the prophylaxis or treatment of Alzheimer's disease. The agent for the prophylaxis or treatment of Alzheimer's disease of the present invention containing a compound having a GnRH antagonistic action shows low toxicity and has a superior preventive and therapeutic effect on Alzheimer's disease.
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- Naphthalene derivatives, their production and use
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A composition containing a compound of the formula: wherein A is a nitrogen-containing heterocyclic group which may be substituted, R1 is a hydrogen atom, hydrocarbon group which may be substituted, or monocyclic aromatic heterocyclic group which may be substituted, R2 is a hydrogen atom or a lower alkyl group which may be substituted, R3, R4, R5, R6, R7, R8 and R9 are independently a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxy group which may be substituted, a thiol group which may be substituted, an amino group which may be substituted, an acyl group or a halogen atom, a salt thereof or a prodrug thereof has steroid C17,20-lyase inhibitory activity, and is useful for preventing and treating for example, primary cancer of malignant tumor, its metastasis and recurrence thereof.
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- Formulations comprising selective androgen receptor modulators
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The present invention relates to pharmaceutical compositions and formulations comprising a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia,osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; and/or e) decreasing the incidence of, halting or causing a regression of prostate cancer. The present invention provides pharmaceutical compositions comprising the selective androgen receptor modulator compounds, together with pharmaceutically acceptable excipients.
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- DRUGS
-
The present invention relates to a medicine which comprises a compound (I) of the formula:[wherein the ring M is a heterocylic ring having -N=Ca and Rb are bound to each other to form the ring A, or they are the same or different each representing a hydrogen atom or a substituent on the ring M;the rings A and B each is an optionally substituted homocycle or heterocycle, and at least one of them is an optionally substituted heterocycle;the ring C is an optionally substituted homocycle or heterocycle;the ring Z is an optionally substituted nitrogen-containing heterocycle; andn is an integer of 1 to 6] or a salt thereof in combination with a drug having an emetic action. The compounds (I) or their salts are useful as anti-emetic drugs. Particularly, vomiting caused by drugs having an emetic action can be inhibited by these compounds rapidly and safely at a low dose.
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- Gastroprotective pharmaceutical preparations containing N-benzyl-N-((1S,5S)-6,6-dimethylbicyclo(3,1,1)-hept-2-ylethoxy-ethyl)-morpholinium salts
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A method of inhibiting peripheral blood circulation disorders or damage such as hemorrhagic lesions induced by gastrotoxic doses of substances such as alcohol or non-steroid, antiinflammatory medicaments in the gastrointestinal tract of a mammal comprising administering to said mammal an effective peripheral circulation disorder or gastrointestinal damage inhibiting amount of a quaternary N-benzyl-N-{2-[2-((1S,5S)-6,6-dimethylbicyclo[3,1,1]hept-2-yl)-ethoxy]-ethyl}-morpholinium salt, and pharmaceutical compositions comprising a substance having a tendency to induce a peripheral blood circulation disorder or damage such as a hemorrhagic lesion in the stomach and/or intestinal wall of a mammal and an effective peripheral circulation disorder or gastrointestinal damage inhibiting amount of a quaternary N-benzyl-N-{2-[2-((1S,5S)-6,6-dimethylbicyclo[3,1,1]hept-2-yl)-ethoxy]-ethyl}-morpholinium salt.
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- Pharmaceutical composition
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A pharmaceutical product preferably in the form of a capsule comprises in one case Atenolol and aspirin. A barrier film coating including a dihydric alcohol is provided around a tablet of Atenolol which in turn is surrounded by Aspirin inside a capsule. Aspirin is preferentially and maximally absorbed in the first hour after ingestion before significant release and absorbtion of Atenolol.
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- Arylalkylamine derivatives
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Disclosed is a novel arylalkylamine derivative represented by the formula (I) STR1 wherein X represents --O--, --CH2 -- or --NR3 -- in which R3 represents hydrogen or lower alkyl; Y represents --NH-- or STR2 Z represents STR3 in which R4 represents hydrogen or lower alkyl or STR4 Q represents an optionally substituted aryl or optionally substituted aromatic heterocyclic group; each of R1 and R2 independently represents hydrogen or lower alkyl; each of m and n independently represents an integer of 0 or 1; and a pharmaceutically acceptable salt thereof. The compound (I) and a pharmaceutically acceptable salt thereof show bronchodilatory and antiallergic activities, and are useful for treating respiratory disorders such as bronchial asthma.
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- Synergistic compositions for the treatment of coronary insufficiency and methods of use thereof
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There are disclosed pharmaceutical preparations and methods for the use thereof which have a cardioprotective action useful in coronary insufficiency, in the prevention of the constitution of an infarction or of sudden death. It consists in the utilization of amiodarone, a nitrate derivative and a beta-blocker.
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- ANTIPSYCHOTIC BENZOTHIOPYRANYLAMINES
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Disclosed are 3,4-dihydro-2H-1-benzothiopyran-3-yl-methyl-and ethylamines useful as antipsychotics, processes for the preparation of said compounds, pharmaceutical compositions containing same, and a method of treating psychotic disorders by administering said compounds.
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- Novel alpha-cyano-beta-oxopropionamides
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α-(Substituted carbamoyl)-β-aryl- and heteroaryl-β-oxo-propionitriles of formula, , A-CO- enol ethers thereof and salts thereof, as well as pharmaceutical preparations containing same and methods of preparing and using these compounds are disclosed. Said compounds represent novel antiinflammatory and antirheumatic agents. Their property to interfere with both the cyclooxygenase and lipoxygenase pathway of the arachidonic fatty acid bioconversion to inflammatory mediators make them valuable therapeutics. These properties render the mentioned substituted carbamoyl-β-oxopropionitriles useful for the treatment of arthritic and rheumatic diseases and other inflammatory conditions in mammals.
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- Site specific alkylating agents
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The invention relates to distamycin A analogs of the following formula STR1 wherein n is 2, 3 or 4; A is an optionally substituted divalent radical chosen from STR2 and -Het- wherein Het is a pentatomic or hexatomic heteromonocyclic ring, except pyrrole; and wherein either one of R1 and R2 is hydrogen and the other is an acylating moiety or R1 and R2 are both hydrogen or both alkyl groups optionally substituted, including the pharmaceutically acceptable salts of the said compounds. The compounds of the invention can be useful antitumor and antiviral agents.
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- Lipases and lipase extracts, their preparation process and their therapeutic use
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Process for the preparation of a gastric lipase. The stomachs of rabbits or horses undergo extraction by an acid aqueous medium, the lipase extract is salted out by the addition of hydrosoluble salts then, by filtration on a molecular sieve, followed by separation using ion exchange chromatography, an elution fraction containing the lipase is collected. Medicament for fighting against malabsorptions of fatty substances.
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- Preventives and remedies for medicinal and alcoholic poisoning
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Preventives or remedies for medicinal and alcoholic poisoning contain as a pharmaceutically effective component phytic acid or its salt which may be an innoxious metal salt, or an innoxious salt with an organic base, a basic amino acid or an organic ester residue.
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- Anti-hypertensive substituted 2-azabicyclooctane-3-carboxylic acids
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Compounds of formula (I): STR1 in which E denotes a lower alkyl group, or preferably a hydrogen atom, and their addition salts with a pharmaceutically acceptable acid or base, the preparation thereof and pharmaceutical compositions containing them.
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- PYRIDINE DERIVATIVES
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A pyridine derivative represented by formula (I): wherein the symbols are as defined in the specification, which exhibits selective, potential, and long-lasting inhibitory activity on biosynthesis of thromboxane A2 and is useful in the treatment and prevention of a broad range of diseases.
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- Tricyclic compounds
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Novel tricyclic compounds having a TXA2 -antagonizing activity represented by formula (I): STR1 which strongly antagonize an action of thromboxane A2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.
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- Androst-4-ene-3,17-diones and process for their preparation
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The present invention relates to new 6-substituted 1.2βmethylenandrost-4-ene-3,17-diones of the following general formula: STR1 wherein one of R1 and R2 is hydrogen and the other is halogen, amino or azido, or R1 and R2, taken together, form a =CH2 or =O group, and, when one of R1 and R2 is amino, the pharmaceutically acceptable salts thereof. The compounds of the invention are useful in therapy, in particular as anti-cancer agents.
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- 4-substituted-6-aryl-pyrimidine compounds
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This invention describes the synthesis and anti-neoplastic use of 4-aziridyl-5-substituted/unsubstituted 6-aryl-pyrimidine compounds of Formula IA STR1 as well as N'-[2-(1-aziridyl)ethyl]-6-aryl-2,4-pyrimidinediamines of Formula IB STR2 and 4-chloro or bromo-5-substituted/unstubstituted-6-aryl-pyrimidines.
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- Methylthioquinolyl guanidine derivative, process of preparation thereof and pharmaceutical compositions therefrom
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The compound of formula (I): STR1 N-cyclohexyl-N"-4-(2-methylthioquinolyl)-N'-2-thiazolyl-guanidine and pharmaceutically acceptable salts thereof is a valuable antiinflammatory, analgesic and antipyretic agent. The compound of the invention may be formulated with conventional pharmaceutically acceptable carriers or diluents to provide a pharmaceutical composition.
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- Complexes of flavanolignans with phospholipids, preparation thereof and associated pharmaceutical compositions
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The invention relates to novel compounds comprising lipophilic complexes of silybin, silidianin, and silicristin with phospholipids, and the preparation of these complexes by non-conventional methods. Absorption of the novel compounds in the gastrointestinal tract is appreciably greater, resulting in higher plasma levels than for the individual flavanolignans. The resulting improvement in the pharmacokinetic and pharmacological parameters is such that the substances can advantageously be used in the treatment of acute and chronic liver disease of toxic, metabolic or infective origin or of degenerative nature.
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- Process for inhibiting blood platelet aggregation and promoting vasodilation
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A method for inhibiting blood platelet aggregation in humans, and promoting vasodilation in humans, by administering to a human in need of the same an effective amount of 2-hydroxy-3-isopropyl-5,6-dimethylpyrazine or a hydrate or a pharmaceutically acceptable non-toxic salt thereof. Administration can be orally in an amount of about 0.02-12 mg/kg body weight per day, or parenterally in an amount of about 0.01-6 mg/kg of body weight per day.
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- Composition for gastrointestinal ulcers
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Fab or Fc fragment of human IgG which is obtainable by enzymatic digestion of the human IgG is reduced by a reducing agent to sever an interchain of disulfide bonds therein and then blocked the SH radicals formed with alkyl group which may contain other group. The resulting alkylated Fab and Fc fragments display therapeutic and prophylactic action for gastrointestinal ulcers by the oral or parenteral administration.
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- Process for the preparation of a stable modification of torasemide
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The present invention provides a process for the preparation of crystalline torasemide in the pure modification I (monoclinic, space group P21 /c, melting point 162° C.) from torasemide of modification II (monoclinic, space group P2/n, melting point 169° C.), wherein a suspension of torasemide of modification II is stirred in water with the addition of a catalytic amount of modification I until the rearrangement is complete. The present invention also provides a pharmaceutical compositions containing torasemide of modification I.
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- Pyridyl ester containing 1,4-dihydropyridine derivatives and salts thereof and pharmaceutical composition containing the same
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This invention relates to a novel 1,4-dihydropyridine derivative of the formula STR1 wherein R2 is pyridyl, or a salt thereof. These compounds have a vasodilating activity and a platelet aggregation inhibiting activity. Also disclosed are pharmaceutical compositions containing the same.
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- Delivery device for zero-order release of an active principle into a dissolution fluid and process for its preparation
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A delivery device for zero-order release of an active principle into a dissolution fluid includes a reservoir consisting of a solid matrix of a homogeneous mixture of a polymer material, at least a portion of the active principle and an additive soluble in the dissolution fluid with negative heat of solution, a coating on the solid matrix-type reservoir of a first, release rate-controlling insoluble membrane which modulates the active principle release according to the desired kinetics; and a second, protective membrane on the release rate-controlling membrane of a soluble polymer material.
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- Certain β-oxo-α-carbamoylpyrrolepropionitriles
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1-Unsubstituted β-oxo-α-(phenylcarbamoyl)-β-pyrrolylpropionitriles, e.g. those of the formula STR1 wherein R1 and R2 =H or alkyl, and R3 and R4 =H, alkyl, alkoxy, OH, halogen or CF3, are analgesic, and antiarthritic agents. Their synthesis, pharmaceutical compositions thereof, and methods of treatment utilizing such compounds are included.
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- Formulation with special 1,2-diacylglycero-3-phosphocholines for the treatment of gastrointestinal disorders
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Pharmaceutical formulations for the treatment of gastrointestinal disorders, which contain as the active component an effective gastrointestinal disorder alleviating amount of a 1,2-diacylglycero-3-phosphocholine in which 75-86% by weight of the acyl radicals are unsaturated fatty acid radicals having a chain length of 16, 18 or 20 carbon atoms. The mixtures of fatty acid radicals in the acyl groups in the 1- and 2-positions preferably have different compositions. The formulations can also contain other active compounds, in particular those which display injurious gastrointestinal side effects.
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- Phenylethanolaminotetralines, a process for their preparation and pharmaceutical compositions containing them
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A novel phenylethanolaminotetraline having lipolytic activity of formula STR1 wherin X represents hydrogen, halogen, a trifluoromethyl or a lower alkyl group and R represents hydrogen, a lower alkyl group not substituted or substituted by a cycloalkyl group containing 3 to 7 carbon atoms, a hydroxy group, a lower alkoxy, carboxy or lower carbalkoxy group; a cycloalkyl group containing 3 to 7 carbon atoms; or a lower alcanoyl group; or a pharmaceutically acceptable salt thereof; a process for its preparation; and pharmaceutical compositions containing it as active ingredient, useful for the treatment of obesity.
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- Novel fluorinated resorcinol ethers
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4-Acylresorcinol ethers of the formula STR1 in which R1 is lower alkyl, R2 is fluorinated lower alkyl, R3 is hydrogen, lower alkoxy, trifluoromethyl or halogen, alk is an alkylene or hydroxyalkylene radical which is uninterrupted or interrupted by oxygen, one of the radicals R4, R5 and R7 is a group of the formula --NH--C(=O)--R8, a radical R4 or R5 which differs from this is a radical R9 and a radical R7 which differs from this is a radical R10, R6 is hydrogen, lower alkyl, trifluoromethyl, halogen, carboxyl which is free, esterified or amidated, cyano or lower alkanoyl, R8 is carboxyl which is free, esterified or amidated or 5-tetrazolyl, R9 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl and R10 is hydrogen, lower alkyl, lower alkoxy, halogen, trifluoromethyl, cyano or carboxyl which is free, esterified or amidated, and their salts have antiallergic and antiinflammatory properties. They are prepared, for example, by reacting compounds of the formulae STR2 in which one of the radicals X5 and X6 is hydroxyl which is free or in salt form and the other is an alkoxy radical substituted by reactive esterified hydroxyl or epoxy. The invention also relates to intermediates of the formula STR3 in which R2 is fluorinated lower alkyl, R3 is hydrogen, lower alkoxy, trifluoromethyl or halogen and R11 is hydrogen or a group of the formula R1 --O(=O)--, in which R1 is lower alkyl, and their salts.
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- Pharmaceutical preparation for the therapeutic treatment of rheumatic diseases
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Pharmaceutical preparation containing phospholipids for the therapeutic treatment of rheumatic diseases which contain in addition to the antiphlogistically acting oxicam derivatives of the general formula STR1 special 1,2-diacyl-glycero-3-phosphocholines wherein 75-86% by weight of the acyl radicals are unsaturated fatty acid radicals, and the preparation thereof.
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- Ethene derivatives
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Ethene derivatives of the formula: wherein R5 represents optionally substituted heterocyclyl or a group --CR4 =CR2 R3, or optionally substituted aryl, heterocyclylalkyl or arylalkyl and R1 represents --NR6 -- wherein R6 represents hydrogen or optionally substituted alkyl or aryl, or R5 represents a quinonoidal group, and R1 represents =N--, R4 represents hydrogen, alkoxy, alkylthio, trifluoromethyl or optionally substituted alkyl or aryl, R2 represents cyano, formyl, alkoxycarbonyl, alkylsulphonyl, dialkylcarbamoyl, dialkylthiocarbamoyl, aryloxycarbonyl, arylsulphinyl or arylsulphonyl, R3 represents a group R2 or hydrogen, nitro or optionally substituted aryl or aroyl or alkanoyl, and m and n are 1 or 2, and pharmaceutically acceptable salts thereof, with the exclusion of certain compounds in which R5 represents pyridyl, 5-halogenopyrid-2-yl or 1,2,4-triazolo[4,3-a]-quinoline possess useful pharmacological properties.
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- Azolylmethylcycloalkanes, their preparation and their use as drugs
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Azolylmethylcycloalkanes of the formula I STR1 where A and B are identical or different and are each hydrogen, unsubstituted or halogen-substituted alkyl of 1 to 4 carbon atoms, naphthyl, hetaryl, biphenyl or phenyl, where the phenyl radical can be substituted by halogen, nitro, alkyl, alkoxy or haloalkyl, each of 1 to 4 carbon atoms, phenoxy or phenylsulfenyl, D and E are identical or different and are each hydrogen or halogen, Z is CH or N, m can be 1, 2, 3 or 4 and n can be 0, 1 or 2, their addition salts with acids and their metal complexes, and the preparation of these compounds, are described. The compounds are useful for treating disorders and for crop, wood and material protection.
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- 5-azolylacetoxymilbemycins as ecto- and endoparasites
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The present invention relates to milbemycin derivatives of the formula I STR1 wherein X is hydrogen or β-halogen, R is methyl, ethyl, isopropyl or sec-butyl and Az is a 5 membered heterocyclic aromatic ring which contains 2-4 nitrogen atoms and is attached in the 1-position and which is unsubstituted or substituted by one or two C1 -C6 alkyl groups. These compounds, and the acid addition salts and metal complexes thereof, are effective pesticides for controlling endo-and ectoparasites, especially for controlling neamatodes which are parasites of animals. The may be obtained by appropriate esterification in 5-position of milbemycin derivatives. The selective β-halogenation of 14,15-epoxymilbemycin derivatives can be effected via the intermediate Δ13,14 -15-hydroxymilbemycins with appropriate halogenating agents.
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- Galenical formulation of toloxatone
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A new formulation for the oral administration of Toloxatone, an anti-depressant, contains 400 to 600 mg of Toloxatone per unit dose. Such a high Toloxatone content is possible due to the discovery that Toloxatone is competitive with Tyramine towards the A form of a monomine oxidase, and thus does not cause hypertensive crisis. The anti-depressant composition of this invention can therefore be administered to the patient even when Tyramine is present in the patient's system.
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- 2H-benzofuran-3-one-derivatives and process for their preparation
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2H-Benzofuran-3-one derivatives, process for their preparation and pharmaceutical compositions containing them. The compounds and compositions are useful in the treatment of allergies.
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- 3-Amino-[1]-benzazepin-2-one-1-alkanoic acids
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Variously substituted 1-carboxymethyl-3-(carboxymethylamino)-2,3,4,5-tetrahydro-1H-[1]benzazepin-2-ones and functional derivatives are angiotensin converting enzyme inhibitors and are useful as antihypertensive agents. Synthesis of, compositions and methods of treatment utilizing such compounds are included.
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- Antihypotensive tetrahydro-1H-pyrazolo[5,1-a]isoindoles
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New substituted tetrahydro-1H-pyrazolo[5,1-a]isoindoles of the formula I STR1 in which R1 denotes a hydrogen or halogen atom or an alkoxy group having 1 to 4 carbon atoms, R2, R3 and R4, which can be identical or different, denote a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, or R2 and R3 together denote the ethylene group, and X denotes a nitrogen atom or a methine group, and their acid addition salts have a long-lasting hypertensive effect and can be used as anti-hypotensives.
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- Dibenz[b,e]oxepin compounds
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A dibenz[b,e]oxepin compound having an antiallergic activity is represented by the following general formula: STR1 wherein R1 represents a cyano group, a 5-tetrazolyl group, a carbamoyl group or --CO2 R3 wherein R3 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms or a 1-(ethoxycarbonyloxy)ethyl group, and R2 represents a 4-alkylpiperazino group wherein the alkyl group has 1 to 5 carbon atoms, a 3-quinuclidinylamino group or --X--(CH2)n --NR4 R5 wherein X represents --NH--, --S -- or --O--, R4 and R5 are same or different and each represents an alkyl group having 1 to 5 carbon atoms and n represents 2 or 3; and the pharmaceutically acceptable acid addition salts or metal salts thereof.
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- Methylflavone-8-carboxylates
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3-methylflavone derivatives which are useful in the treatment of allergies, asthma and inflammation.
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- Condensed benzopyrone derivatives
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The present invention relates to new condensed benzopyrone derivatives, to a process for their preparation and to pharmaceutical compositions containing them.
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- CERTAIN BENZO-(PYRANO AND THIOPYRANO)-PYRIDINES, USEFUL AS CNS AGENTS
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Disclosed are the compounds of formula I STR1 wherein X represents oxygen or sulfur; ring A is unsubstituted or substituted by one to three identical or different substituents selected from hydroxy, hydroxy-lower alkyl, etherified hydroxy, etherified hydroxy-lower alkyl, acyloxy, acyloxy-lower alkyl, halogen, lower alkyl, trifluoromethyl, amino, mono-and di-lower alkylamino and acylamino; or ring A is substituted by one lower alkylenedioxy; R represents hydrogen, lower alkyl or aryl-lower alkyl; R 1 represents hydrogen, lower alkyl, lower alkylthio-lower alkyl, amino, acylamino, (amino, mono-or di-lower alkylamino)-lower alkyl, carboxy, lower alkoxycarbonyl, carbamoyl or mono-or di-lower alkylcarbamoyl; R 2 to R 5 represent hydrogen or lower alkyl; the dehydro derivatives thereof with a double bond at the 1, 2-position, or at the 1,10b-position in which case R 5 is absent; or a pharmaceutically acceptable salt thereof; methods for their synthesis; pharmaceutical compositions thereof; and use thereof as psychactive agents for the treatment of central nervous system disorders.
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