Patents Assigned to Spofa spojene podniky pro
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Patent number: 4898930Abstract: Peptide ester and amide derivatives of the general formula I: ##STR1## in which X is H or an acyl, A and B are structurally defined amino acid residues, n is an integer of from 1 to 3, R.sup.1 is H or a lower alkyl and either R.sup.2 or C is a defined optionally modified amino acid residue and the other is a lower alkoxyl, an amino group or a direct chemical bond, are converted under physiologic conditions, by enzymic hydrolysis in pathologically altered tissues and subsequent spontaneous cyclization, into pharmacodynamically active spirocyclic peptide derivatives of the general formula III: ##STR2## in which R.sup.3 and R.sup.4 are H atoms, optionally substituted alkyl groups or jointly an aliphatic chain forming preferably a 2,5- piperazinedione ring, and hence can act as pro-farmaca (drug precursors) of prolonged biological effect.Type: GrantFiled: June 12, 1987Date of Patent: February 6, 1990Assignee: Spofa, spojene podniky proInventors: Evzen Kasafirek, Miroslav Rybak, Ivan Krejci, Antonin Sturc, Alena Roubalova, Jiri Vanzura, Evzen Krepela, Michal Bartik
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Patent number: 4847403Abstract: 2-Isopropyl-2-(2-methylphenyl)-5-(N-methylhomoveratrylamino)-valeronitrile ("mepamil") of the Formula I: ##STR1## preferably administered in the form of water-soluble acid addition salts such as e.g. hydrochloride. The claimed compound is advantageously prepared by alkylation of 2-(2-methylphenyl)-3-methylbutyronitrile with 3,3-diethoxypropylchloride. Subsequently, the obtained 5,5-diethoxy-2-isopropyl-2-(2-Methylphenyl)-valeronitrile is mildly, acidically hydrolisized to yield the appropriate aldehye, i.e. 2-isopropyl-2-(2-methylphenyl)-5-oxovaleronitrile. This aldehyde is then reacted with N-methylhomoveratrylamine under conditions of reductive alkylation, suitably by catalytic hydrogenation over a platinum or palladium catalyst or by chemical reduction with the use of formic acid as a reducing agent. The resulting base is optionally converted by neutralization with a pharmaceutically acceptable organic or inorganic acid, i.e. hydrochloric or fumaric acid, into the corresponding acid addition salt.Type: GrantFiled: July 17, 1987Date of Patent: July 11, 1989Assignee: Spofa, spojene podniky pro zdravotnickouInventors: Luedvik Blaha, Miroslav Rajsner, Ivan Helfert, Vaclav Trcka
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Patent number: 4833072Abstract: The present invention relates to antigenic peptides of the formulaH--Val--X--Y FORMULA Iwherein X is a polypeptide residue selected from the group consisting of:Val-Pro-Arg-Arg-Lys-Ala-Lys-Ile;Ser-Gly-Lys-Ala-Arg-Gly-Trp-Phe;Tyr-Tyr-Arg-Asp-Ser-Arg-Ash-Pro-Leu;Phe-Ile-His-Asn-Phe-Lys-Arg-Lys-Gly;Ser-Ile-Glu-Trp-Arg-Lys-Lys-Arg-Tyr-Ser; andLeu-His-Thr-Gly-Glu-Arg-Asp-Trp-His-Leu-Gly,and Y is a hydroxyl group or an amino group. The invention also relates to a method of preparing these peptides.These novel peptides exhibit useful antigenic properties, with respect to Human Immunodeficiency Virus (HIV), formerly known as Human T-cell Lymphotropic Type-III Virus (HTLV-III). Human Immunodeficiency Virus is associated with the diseases known as Acquired Immune Deficiency Syndrome (AIDS) and Aids Related Complex (ARC). The present antigenic peptides are useful for the detection of antibodies active against HIV and are suitable for use as diagnostic agents.Type: GrantFiled: November 13, 1986Date of Patent: May 23, 1989Assignee: Spofa spojene podniky proInventors: Viktor Krchnak, Milan Krojidlo, Otakar Mach
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Patent number: 4775673Abstract: Substituted acylpiperazinoquinazolines of formula I ##STR1## wherein n is 0 or 1, R represents an alkyl group with 1 to 4 carbon atoms or a benzyl group, and R.sub.1 is a hydrogen atom, a methyl group or a phenyl group. Addition salts of these compounds with inorganic and organic acids are also disclosed. The compounds possess a significant antihypertensive activity. They can be prepared by the reaction of 2-halogeno quinazoline derivatives with the corresponding acylpiperazines, followed (if required) by neutralization of the respective base with a suitable acid to form its pharmaceutically convenient addition salt.The acid addition salts, especially hydrochlorides, are readily soluble in water and give stable, almost neutral aqueous solutions which can be used in parenteral (injectable) and peroral medicinal dosage forms.Type: GrantFiled: April 14, 1986Date of Patent: October 4, 1988Assignee: SPOFA, spojene podniky pro zdravotnickou vyrobuInventors: Jan Koenig, Miroslav Rajsner, Vaclav Trcka, Sverluse Macova
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Patent number: 4720497Abstract: 6-purinyl N-(2-chloroethyl) carbamate and thiocarbamate are disclosed of the general formula I, ##STR1## in which X stands for an oxygen or sulfur atom, and also a process for their preparation by reacting a purine derivative of the general formula II (hypoxanthine or 6-mercaptopurine, respectively) with 2-chloroethylisocyanate. The subject compounds of formula I show a remarkable antineoplastic effect in vitro and in vivo, and consequently have great potential for the treatment of malignant neoplastic diseases in mammals.Type: GrantFiled: December 23, 1985Date of Patent: January 19, 1988Assignee: SPOFA, Spojene Podniky pro Zdravotnickou VyrobuInventors: Antonin Cerny, Jiri Krepelka, Milan Melka, Milan Miko, Stanislava Pokorna, Ruzena Reichlova, Irena Kejhova, Marta Beitova, Jaroslava Grimova
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Patent number: 4711952Abstract: Novel peptide analogs of the serum thymic factor are disclosed, structurally modified, in comparison with the natural substance, both in their N-terminal and C-terminal parts and inside the amino-acid sequence, corresponding to the general formula IA-Gly-Gly-Ser-Asn-B-C-NH-R (I),in which A is pGlu, Gln, Ala-Lys-Ser-Gln, pGlu-Ala-Lys-Ser-Gln or Gln-Ala-Lys-Ser-Gln, B and C are Gly, Phe, Leu, Ala or a direct bond, and R is H, an alkyl with 1 to 6 carbon atoms or a 2-phenylethyl. Depending upon their chemical structure, the subject thymic factor analogs possess either agonistic (immunostimulative) or antagonistic (immunosuppressory) properties.Type: GrantFiled: June 17, 1986Date of Patent: December 8, 1987Assignee: SPOFA, spojene podniky pro zdravotnickouvyrobuInventors: Evzen Kasafirek, Martin Cerny, Petr Kocis, Jiri Krepelka, Jozef Rovensky
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Patent number: 4692452Abstract: This invention relates to a method for the treatment of endometritis (chronic and/or acute puerperal inflammations) in mammalian females comprising the administration of 1-(8-alpha-ergolinyl)-3,3-diethylurea derivatives of Formula I ##STR1## in which R.sup.1 represents an alkyl group containing 1 to 3 carbon atoms, R.sup.2 represents a hydrogen atom or an alkyl group containing 1 to 3 carbon atoms, and X represents a hydrogen atom or a double bond between the carbon atoms at positions 9 and 10. The compound according to Formula I, or a pharmaceutically acceptable acid addition salt thereof, is the physiologically active component of the therapeutic composition and method. The compound may be combined with a pharmaceutically acceptable diluent, vehicle, excipient, auxiliary, or carrier. The invention is particularly advantageous in veterinary medicine, when applied to the treatment of farm animals, such a cows.Type: GrantFiled: June 12, 1986Date of Patent: September 8, 1987Assignee: SPOFA, spojene podniky pro zdravotnickou vyrobuInventors: Antonin Cerny, Jiri Krepelka, Karel Rezabek, Maria Fruhaufova, Milan Pesak, Bohumil Sevcik, Josef Kral, Antonin Borovicka, Petr Bilek, Dagmar Picmausova, Josef Stuchlik, Josef Picha, Jana Strakova
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Patent number: 4683331Abstract: The invention relates to omega-(2',4'-dihalobiphenylyl)oxo alkanoic acids of Formula: ##STR1## wherein X.sup.1 and X.sup.2 each represent a fluorine or chlorine atom and Y represents a bivalent hydrocarbon chain selected from the group consisting of --CH.sub.2 --CH--CH.sub.3 and (CH.sub.2).sub.3, and to a process for their preparation.The compounds of the invention are highly active and longlasting anti-inflammatory agents.Type: GrantFiled: July 29, 1985Date of Patent: July 28, 1987Assignee: Spofa spojene podniky pro zdravotnickouInventors: Miroslav Kuchar, Bohumila Brunova, Jaroslava Grimova, Eva Maturova
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Patent number: 4678788Abstract: N-substituted 2-chloro-7-fluoro-10-piperazino-10,11-dihydrodibenzo(b,f)thiepins are disclosed of the general formula I, ##STR1## in which R represents an aminocarbonyl, amino-oximinomethyl, 1,3-dioxolan-2-yl or 1,3-dioxan-2-yl, group and their addition salts with convenient organic and inorganic acids. These compounds are highly potent antidopaminergic, non-cataleptic neuroleptics of use in the treatment of schizophrenia. According to recent pharmacological assay results, the subject compounds are expected to be substantially free of the usual undesired extrapyramidal side effects. They can be obtained by common preparative methods from the respective starting compounds of formula III, IV or V, or also by appropriate interconversion reactions of other compounds of formula I.Type: GrantFiled: January 24, 1986Date of Patent: July 7, 1987Assignee: SPOFA, Spojene Podniky Pro Zdravotnickou VyrobuInventors: Miroslav Protiva, Jiri Jilek, Irena Cervena, Antonin Dlabac, Martin Valchar, Josef Pomykacek
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Patent number: 4661297Abstract: Basic ethers of 7-oxo-7H-benzo(c) fluorene have been shown to evidence a pronounced antineoplastic and immunosuppressive effect in mammals suffering from leukemia. The technique for preparing the described ethers and the addition salts thereof with pharmaceutically acceptable organic and inorganic acids involves the aminoalkylation of 5-hydroxy-7-oxo-7H-benzo(c) fluorene and its corresponding nuclear substituted derivatives on the hydroxylic oxygen atom.Type: GrantFiled: September 14, 1982Date of Patent: April 28, 1987Assignee: SPOFA, spojene podniky pro zdravotnickou vyrobuInventors: Jiri Krepelka, Iva Vancurova, Karel Rezabek, Milan Melka, Vojtech Pujman, Stanislava Pokorna, Ruzena Reichlova, Slavjanka Cernochova
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Patent number: 4599415Abstract: This invention relates to the compound 3-[2-(2-Benzimidazolyl) Benzoyloxyethyl]-4(3H)-Quinazolinone of Formula I, and a process for the preparation thereof. The compound exhibits strong analgesic activity and almost zero toxicity in laboratory mice. ##STR1## The compound of Formula I is prepared by acylation of the compound 3-(2-hydroxyethyl)-4(3H)-quinazolinone with a reactive derivative of 2-(2-benzimidazolyl)benzoic acid, preferably its imidazolide, formed by treatment of the acid of Formula III with 1,1'-carbonyldiimidazole. The compounds of Formula II and Formula III are reacted in situ, at room temperature, and in the presence of an inert organic solvent. The product compound is isolated and purified by common techniques.Type: GrantFiled: April 8, 1985Date of Patent: July 8, 1986Assignee: SPOFA, spojene podniky pro zdravotnickou vyrobuInventors: Ludmila Fisnerova, Jaroslava Grimova, Zdenek Roubal, Oldrich Nemecek
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Patent number: 4554100Abstract: A method is described for the preparation of novel alkylamides of carboxyalkanoyl peptides of the formula ##STR1## wherein R is an aralky or an alkyl group of 1-5 carbon atoms, A is a residue of peptidically bound proline or alanine, B is a straight bond or a residue of peptidically bound proline or alanine and X is a CH.dbd.CH group or a methylene group of 1-3 carbon atoms.The described compounds are capable of inhibiting elastase.Type: GrantFiled: August 9, 1982Date of Patent: November 19, 1985Assignee: Spofa, Spojene podniky pro zdravotnickou vyrobuInventors: Evzen Kasafirek, Premysl Fric, Jan Slaby, Alena Roubalova
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Patent number: 4528133Abstract: This invention relates to biologically active tripeptide and tetrapeptide alkylamides of the general formula ##STR1## wherein R.sup.1 is an alkyl with 1 to 5 carbon atoms,A is a peptidically bound alanine or proline residue,B is a peptidically bound glycine, alanine or proline residue,n is an integer of 1 or 2, andR.sup.2 is an alkylcarbonylamino group with 2 to 12 carbon atoms, an alkenyl with 6 to 12 carbon atoms or a benzyloxycarbonylamino group.The compounds effectively inhibit the enzymatic activity of pancreatic and leucocytal elastase and are expected to find use in the treatment of acute pancreatitis, chronic obstructive pulmonary disease, pulmonary emphysema, and certain forms of arthritis. The invention also relates to processes for the preparation of the title compounds and to pharmaceutical compositions containing them.Type: GrantFiled: October 3, 1983Date of Patent: July 9, 1985Assignee: SPOFA, spojene podniky pro zdravotnickou vyrobuInventors: Evzen Kasafirek, Premysl Fric, Jan Slaby, Alena Robalova
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Patent number: 4515715Abstract: The invention relates to L-Alanyl-D-isoglutamine adamantylamide of the formula ##STR1## wherein AD represents a residue of adamantane bound in the number 1 position. The described compound evidences an immunostimulatory and immunoadjuvant activity of unusual degree without any relevant side effects such as pyrogenity.Type: GrantFiled: June 29, 1983Date of Patent: May 7, 1985Assignee: SPOFA, spojene podniky pro zdratvonickou vyrobuInventors: Martin Flegel, Milan Krojidlo, Jiri Kolinsky, Karel Masek, Jaroslav Seifert
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Patent number: 4512461Abstract: A spherical swollen hydrophillic toric contact lens is converted into a planarized xerogel and stored and transported on a planar or moderately curved base provided with an angle scale in the range of 0 to 180 degrees. The base is formed to locate the lens above the center of the scale with the cylindric axis lying on the lines converting the 0 or 180 degrees with the center of the angle scale. A permeable cover capable of compressing the lens is placed over the lens causing the lens to assume the surface shape of the base in the xerogel state.Type: GrantFiled: December 11, 1981Date of Patent: April 23, 1985Assignee: SPOFA, spojene podniky pro zdravotnickou vyrobuInventor: Otto Wichterle
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Patent number: 4512923Abstract: A luteinizing and follicle stimulating hormone of the formula ##STR1## wherein X represents a hydrogen atom or a protective group is described. The described hormones evidence high gonadotropic activity and are useful in human and veterinary medicine.Type: GrantFiled: August 8, 1983Date of Patent: April 23, 1985Assignee: SPOFA, spojene podniky pro zdravotnickou vyrobuInventors: Martin Flegel, Jan Pospisek, Josef Picha, Drahomira Pichova, Milan Krojidlo, Jiri Kolinsky
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Patent number: 4431808Abstract: A technique is described for the preparation of a wide variety of basic derivatives of linearly condensed tricyclic systems formed by two external benzene nuclei and a 7-membered central ring having 2 chalcogen atoms as hetero atoms.Derivatives of 11H-dibenzo(b,e)-1,4-dioxepin are obtained when the chalcogens are both oxygen atoms; derivatives of 11H-dibenzo(b,f)-1,4-dithiepin are obtained when the chalcogens are both sulfur atoms; derivatives of 6H-dibenz(b,e)-1,4-oxathiepin and 11H-dibenz(b,f)-1,4-oxathiepin are obtained with combinations of sulfur and oxygen atoms as chalcogens.Type: GrantFiled: March 9, 1982Date of Patent: February 14, 1984Assignee: SPOFA, spojene podniky pro zdravotnickou vyrobuInventors: Miroslav Protiva, Karel Sindelar, Antonin Dlabac, Jirina Metysova
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Patent number: 4384118Abstract: 4-(3-Iodopropargyloxy) pyrimidine derivatives of the general formula ##STR1## wherein R.sub.1 is selected from among a halogen atom, an amino group, a C.sub.1 -C.sub.4 alkylamino or a C.sub.1 -C.sub.4 alkylthio group, and R.sub.2 is selected from among a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or a C.sub.1 -C.sub.4 alkoxy group, are disclosed. The described compounds are prepared by reacting a 4-halopyrimidine with propargyl alcohol and iodinating the resultant product in the 3 position of the propargyl chain.Type: GrantFiled: June 15, 1981Date of Patent: May 17, 1983Assignee: SPOFA, spojene podniky pro zdravotnickou vyrobuInventors: Dusan Hesoun, Bohumir Vondracek, Jana Turinova
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Patent number: 4322139Abstract: The invention pertains to a method of temporary planarization of hydrogel contact lenses by drying of a lens swollen in a volatile hydrophilic swelling agent and clamped in the planarized state between two surfaces, at least one of which is formed by a thin foil permeable for the hydrophilic volatile swelling agent, as long as the swelling agent diffuses through the foil and the lens is transfered into a xerogel state. According to this invention, the planarized lens may have an enlarged surface and reduced thickness in comparison with the relaxed lens and may be provided with temporary marking comprising signs or lines showing the direction of cylindric axis with toric lenses, a marginal angle scale to enable easier truncation of toric lenses, and additional specifications of the lens. The temporary marking is achieved by pressing the planarized lens during drying against a base with embosed drawing or against projections at the compression foil. According to the invention, water, C.sub.1 -C.sub.Type: GrantFiled: June 15, 1979Date of Patent: March 30, 1982Assignee: SPOFA, spojene podniky pro zdravotnickou vyrobuInventor: Otto Wichterle
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Patent number: 4256369Abstract: A toric hydrogel contact lens having an inner concave surface of the meniscus shape of a rotating liquid and the outer convex plane formed by a rotation-symmetric peripheric ring which passes to a central toric surface by means of two longitudinal strips having a toric component parallel with this component of the central surface, but of the opposite sign. These strips are linked up with the central surface in two parallel bands of mutual distance of at least 4 mm. Continuous transitions are formed between the rotation-symmetric peripheric ring, the central toric surface, and the longitudinal strips.Type: GrantFiled: April 25, 1979Date of Patent: March 17, 1981Assignee: SPOFA, spojene podniky pro zdravotnichouInventor: Otto Wichterle