Patents by Inventor Jaroslav Kalvoda
Jaroslav Kalvoda has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 5317100Abstract: Compounds of the formula ##STR1## in which R.sub.1 is hydrogen or lower alkyl, R.sub.2 is hydrogen or a hydroxyl protective group R.sub.2 ' and R.sub.3 is substituted or unsubstituted phenyl or lower alkyl can be prepared in a three-stage process from readily accessible .beta.-lactam starting materials.Type: GrantFiled: October 22, 1992Date of Patent: May 31, 1994Assignee: Ciba-Geigy Corp.Inventors: Jaroslav Kalvoda, Martin Kessler, Rene Lattmann, Gerardo Ramos
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Patent number: 5215997Abstract: The invention relates to an improved process for the preparation of compounds of formula ##STR1## or salts thereof, starting from compounds of formulae ##STR2## via compounds of formulae ##STR3## in which compounds R.sub.1 is hydrogen or lower alkyl, R.sub.2 is an organic radical which may carry a functional group which may be protected by a customary protective group R.sub.2.sup.o, R.sub.3 is hydrogen or a customary carboxyl protective group R.sub.3.sup.o, W is a group which can be replaced by a thiocarboxylic acid radical of formula III, and Z is oxygen or sulfur.Type: GrantFiled: July 1, 1992Date of Patent: June 1, 1993Assignee: Ciba-Geigy CorporationInventors: Ernst Hungerbuhler, Jaroslav Kalvoda
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Patent number: 5153315Abstract: The invention relates to an improved process for the preparation of compounds of formula ##STR1## or salts thereof, starting from compounds of formulae ##STR2## via compounds of formulae ##STR3## in which compounds R.sub.1 is hydrogen or lower alkyl, R.sub.2 is an organic radical which may carry a functional group which may be protected by a customary protective group R.sub.2 .degree., R.sub.3 is hydrogen or a customary carboxyl protective group R.sub.3 .degree., W is a group which can be replaced by a thiocarboxylic acid radical of formula III, and Z is oxygen or sulfur.Type: GrantFiled: May 18, 1990Date of Patent: October 6, 1992Assignee: Ciba-Geigy CorporationInventors: Ernst Hungerbuhler, Jaroslav Kalvoda
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Patent number: 4962196Abstract: The invention relates to an improved process for the preparation of compounds of formula ##STR1## or salts thereof, starting from compounds of formulae ##STR2## via compounds of formulae ##STR3## in which compounds R.sub.1 is hydrogen or lower alkyl, R.sub.2 is an organic radical which may carry a functional group which may be protected by a customary protective group R.sub.2.sup.o, R.sub.3 is hydrogen or a customary carboxyl protective group R.sub.3.sup.o, W is a group which can be replaced by a thiocarboxylic acid radical of formula III, and Z is oxygen or sulfur.Type: GrantFiled: March 24, 1989Date of Patent: October 9, 1990Assignee: Ciba-Geigy CorporationInventors: Ernst Hungerbuhler, Jaroslav Kalvoda
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Patent number: 4619921Abstract: Novel 6.alpha.,9.alpha.,21-trihalogeno-11.beta.-hydroxy-16.alpha. or 16.beta.-methyl-17.alpha.-propionyloxy-pregn-4-ene-3,20-dione compounds of the formula ##STR1## in which X represents chlorine or flourine, R represents the group --CH.sub.2 CH--, --CH.dbd.CH-- or --CH.dbd.CCl--, the chlorine atom being in the positon 2 of the steroid numbering, and in which the 16-methyl radical is .alpha.- or .beta.-oriented, are useful pharmaceuticals, especially anti-inflammatory agents for topical administration.Type: GrantFiled: April 20, 1984Date of Patent: October 28, 1986Assignee: Ciba-Geigy CorporationInventors: Jaroslav Kalvoda, Georg Anner
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Patent number: 4614614Abstract: The present invention relates to an improved process for the manufacture of (3S)-3,4-trans-disubstituted azetidinones of the formula ##STR1## in which R.sub.1 represents hydrogen or lower alkyl,R.sub.2 represents hydrogen or a hydroxy-protecting group,Y represents the group --S(.dbd.O)--R.sub.3 or --S(.dbd.O).sub.2 --R.sub.3 wherein R.sub.3 represents an organic radical bonded to the sulphur atom by a carbon atom that is not bonded to hydrogen, or the group --C(.dbd.O)--O--R.sub.3 ' wherein R.sub.3 ' represents an organic radical bonded to the oxygen atom of the carboxy group by a carbon atom that is not bonded to hydrogen, or a carboxy-protecting group, andR.sub.4 represents hydrogen or an amino-protecting group R.sub.4 '.The process according to the invention is carried out under particularly favorable reaction conditions and yields compounds (I) in particularly high yields.Type: GrantFiled: March 22, 1984Date of Patent: September 30, 1986Assignee: Ciba-Geigy CorporationInventors: Ivan Ernest, Jaroslav Kalvoda, Wolfgang Frostl
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Patent number: 4559332Abstract: Steroid compounds of the 20-spiroxane series and their analogues having an open ring E of the formula, ##STR1## in which --A--A-- represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,R.sup.1 represents hydrogen, andR.sup.2 represents an .alpha.-oriented lower alkoxycarbonyl radical, orR.sup.1 and R.sup.2 together represent an .alpha.- or a .beta.-oriented methylene radical,--B--B-- represents the group --CH.sub.2 --CH.sub.2 -- or an .alpha.- or .beta.-oriented group ##STR2## X represents two hydrogen atoms or oxo, Y.sup.1 and Y.sup.2 together represent the oxygen bridge --O--, orY.sup.1 represents hydroxy, andY.sup.2 represents hydroxy, lower alkoxy or, if X represents H.sub.2, also lower alkanoyloxy,and salts of compounds in which X represents oxo and Y.sup.2 represents hydroxy, are distinguished as effective aldosterone-antagonists with minimal side-effects and, for that reason, are especially suitable for the treatment of all forms of hyperaldosteronism.Type: GrantFiled: April 9, 1984Date of Patent: December 17, 1985Assignee: Ciba Geigy CorporationInventors: Jurgen Grob, Jaroslav Kalvoda
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Patent number: 4552871Abstract: (5.alpha.)-20-spirox-1-en-3-ones (I) and 17-hydroxy-5.alpha.,17.alpha.-pregn-1-en-3-ones (II) of the formulae ##STR1## in which X represents O or H.sub.2, R.sub.2 represents O and R.sub.1 represents OH, OMe, OAlk, NH.sub.2, NHR.sub.3, NR.sub.3 R.sub.4, or R.sub.2 represents H.sub.2 and R.sub.1 represents OH, OAlk, OAr, OAralk or OAc,in which R.sub.3, R.sub.4 and Alk represent lower alkyl, Me represents a metal atom or metal equivalent or the cation of an organic base, Ar represents monocyclic aryl, Aralk represents monocyclic aryl-lower alkyl, and Ac represents lower alkanoyl, monocyclic aroyl, lower alkylsulphonyl or monocyclic arylsulphonyl, it being possible for R.sub.3 together with R.sub.4 also to represent a lower alkylene group optionally interrupted by a hetero atom,are manufactured by known analogy processes.Type: GrantFiled: April 9, 1984Date of Patent: November 12, 1985Assignee: Ciba Geigy CorporationInventors: Jurgen Grob, Jaroslav Kalvoda
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Patent number: 4285937Abstract: The invention provides novel esters of androstadiene 17-carboxyclic acids of the formula ##STR1## wherein R' represents a hydroxyl group which is esterified with a carboxyclic acid having not more than 7 carbon atoms, R" represents a methyl group in the .alpha.- or .beta.-position or the methylene group, wherein R is H or Cl, each of X and Y represents a hydrogen, chlorine or fluorine atom, with the proviso that at least one of these substituents is one of these halogens, when R is Cl, and that Y is only Cl or F and X only Cl, when R is H and that the androstadiene-17-carboxylic acid ester group does not contain more than 11 carbon atoms.The new esters have pronounced antiinflammatory action coupled with remarkably low systemic side effects on thymus, adrenals and body weight. They are especially suitable to be used in dermatology.Type: GrantFiled: October 30, 1979Date of Patent: August 25, 1981Assignee: Ciba-Geigy CorporationInventor: Jaroslav Kalvoda
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Patent number: 4221786Abstract: The invention relates to the preparation of polyhalogenated pregnane derivatives of the formula ##STR1## wherein X represents fluorine or chlorine and R a free or esterified hydroxyl group or chlorine. The new compounds display a high antiinflammatory activity. No side action on the thymus, the body weight or the adrenals can be detected at the therapeutic dose when the compounds are administered topically. The new compounds are therefore particularly suitable for use as medicaments in dermatology.The new compounds can be prepared according to methods known in the art, e.g. by introducing the chlorine atom in 2-position of corresponding compounds which are non chlorinated in this position, or by the introduction of the halogen atom in 9-position starting from the 9,11.beta.-epoxide or the 9,11-dehydro-compound or by acetonization of the 16,17-dihydroxy group or by replacing a 21-hydroxy group by chlorine.Type: GrantFiled: June 20, 1978Date of Patent: September 9, 1980Assignee: Ciba-Geigy CorporationInventor: Jaroslav Kalvoda
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Patent number: 4172075Abstract: 11,12-Unsaturated 9.alpha.-fluorosteroids comprising a new class of steroid compounds are obtained by a novel process, wherein a corresponding 9.alpha.-fluoro-11.beta.-hydroxysteroid is dehydrated with a reagent of the formula F.sub.3 SX in which X denotes an amino group derived from a secondary amine. Of a particular interest among the products of the invention are compounds of the general formula IB ##STR1## in which the symbols R.sub.5 -R.sub.10 have the meanings given hereinafter; such compounds are especially useful as analogues of cortical hormones possessing antiinflammatory activity.Type: GrantFiled: February 21, 1978Date of Patent: October 23, 1979Assignee: Ciba-Geigy CorporationInventors: Michel Biollaz, Jaroslav Kalvoda
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Patent number: 4092310Abstract: A novel group of 18,18-difluorosteroids of the general formula ##STR1## wherein St, R.sub.1 and R.sub.2 have the meanings given hereinafter is produced by a chemically novel process characterized in that a corresponding 18-oxo compound is treated with a compound of the formula F.sub.3 SX, wherein X denotes a fluorine atom or an amino group derived from a secondary amine. The compounds of the invention are useful as pharmaceutical intermediates. A number of them are physiologically active and possess hormone-like properties, e.g. those of sexual and/or adrenocortical hormones, such as the gonadotropin-blocking, ovulation-blocking, androgenic, oestrogenic, progestagenic, anabolic, antioestrogenic, antiandrogenic, mineralocorticoid, glucocorticoid and antiinflammatory activity, and can be used in lieu of known hormones or agents possessing corresponding hormone-like properties.Type: GrantFiled: July 23, 1975Date of Patent: May 30, 1978Assignee: Ciba-Geigy CorporationInventors: Michel Biollaz, Jaroslav Kalvoda
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Patent number: 4052421Abstract: A new class of 13-ethinyl-steroids is prepared by a novel process comprising Wittig reaction of a 13-formyl steroid with a chloro- or bromomethylenephosphorane and dehydrohalogenation of the intermediate 13-(2-halogenovinyl)steroid with an extremely strong base. Preferred products are those of the formula ##STR1## wherein R denotes a hydrogen atom or the methyl group, R.sub.3 denotes a hydrogen atom or a lower alkyl or lower alkanoyl group, R.sub.4 denotes a hydrogen atom or a lower aliphatic hydrocarbon radical, or R.sub.3 and R.sub.4 together denote a C--O linkage, R.sub.5 denotes the oxo group, a hydrogen atom together with an esterified or free hydroxyl group, or two hydrogen atoms, R.sub.6 denotes a hydrogen atom or a lower alkyl group, and R.sub.7 denotes a hydrogen atom or the methyl group, it also being possible for an additional 1,2-double bond to be present in compounds in which R is the methyl group.Type: GrantFiled: January 20, 1976Date of Patent: October 4, 1977Assignee: Ciba-Geigy CorporationInventors: Michel Biollaz, Jaroslav Kalvoda