Patents by Inventor Jorge Casals

Jorge Casals 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).

  • Patent number: 4450107
    Abstract: 7.alpha.-Alkoxycarbonyl-15.beta.,16.beta.-methylene-4-androstene compounds of Formula I ##STR1## wherein R.sup.1 is hydrogen or methyl,R.sup.2 is alkyl of 1-4 carbon atoms,X is ##STR2## and Y is carbonyl, andthe bond between the C-1 and C-2 carbon atoms is a single or double bond, orwhen the bond between the C-1 and C-2 carbon atoms is a single bond,X can also be ##STR3## when Y is ##STR4## possess valuable pharmacological properties, e.g., as aldosterone antagonists, i.e. they reverse the effect of deoxycorticosterone on the excretion of sodium and potassium.
    Type: Grant
    Filed: March 23, 1982
    Date of Patent: May 22, 1984
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Nickisch, Henry Laurent, Rudolf Wiechert, Jorge Casals-Stenzel
  • Patent number: 4446147
    Abstract: Azaprostacyclins of Formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic residue, or a phenacyl residue optionally substituted on the phenyl ring by bromine, phenyl, alkoxy, or dialkoxy,W is a free or functionally modified carbonyl group or a ##STR2## wherein R.sub.8 is hydrogen or alkyl of 1-5 carbon atoms and R.sub.9 is hydrogen or a readily cleavable ether or acyl residue and wherein the OR.sub.9 -group can be in the .alpha.- or .beta.-position,R.sub.2 is a free or functionally modified hydroxy group.
    Type: Grant
    Filed: February 22, 1982
    Date of Patent: May 1, 1984
    Assignee: Schering Aktiengesellschaft
    Inventors: Norbert Schwarz, Werner Skuballa, Helmut Vorbrueggen, Jorge Casals-Stenzel, Ekkehard Schillinger, Michael H. Town
  • Patent number: 4423067
    Abstract: Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic residue, or NHR.sub.3, wherein R.sub.3 is an acid residue or hydrogen;X is oxygen;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--;W is free or functionally modified hydroxymethylene or free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position; D is a straight-chain or branched, saturated or unsaturated aliphatic group of 1-10 carbon atoms, which can optionally be substituted by fluorine atoms, 1,2-methylene, 1,1-trimethylene;E is --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 are hydrogen or alkyl of 1-5 carbon atoms;R.sub.4 is an aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group;R.sub.5 is free or functionally modified hydroxy and,when R.sub.
    Type: Grant
    Filed: December 21, 1981
    Date of Patent: December 27, 1983
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Raduchel, Norbert Schwarz, Helmut Vorbruggen, Jorge Casals-Stenzel, Ekkehard Schillinger, Michael H. Town
  • Patent number: 4378370
    Abstract: Prostacyclin derivatives of the formula ##STR1## wherein R.sub.1 is OR.sub.3 wherein R.sub.3 is hydrogen or alkyl of 1-10 carbon atoms, or R.sub.1 is NHR.sub.4 wherein R.sub.4 is alkanoyl or alkanesulfonyl,B is alkylene of 1-5 carbon atoms,A is --CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH--, or trans--CH.dbd.CH--,W is hydroxymethylene or ##STR2## wherein the OH-group is optionally substituted by alkanoyl of 1-4 carbon atoms and the free or substituted OH-group can be in the .alpha.- or .beta.- position,R.sub.2 is alkyl of 1-6 carbon atoms optionally substituted by phenyl, or R.sub.2 is phenyl,R.sub.5 is hydroxy optionally substituted by alkanoyl of 1-4 carbon atoms,R.sub.6 is hydrogen, fluorine, or alkyl of 1-4 carbon atomsor when R.sub.3 is hydrogen, a salt thereof with a physiologically compatible base,have pharmacological activity e.g., blood pressure-lowering and bronchodilatory effects.
    Type: Grant
    Filed: October 6, 1981
    Date of Patent: March 29, 1983
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Vorbrueggen, Bernd Raduechel, Werner Skuballa, Gerda Mannesmann, Jorge Casals-Stenzel, Ekkehard Schillinger
  • Patent number: 4364950
    Abstract: 5-cyano-prostacyclins of the formula ##STR1## wherein R.sub.1 is OR.sub.2 or NHR.sub.3 ; R.sub.2 and R.sub.3 each independently is (a) H, (b) C.sub.1-10 -alkyl, (c) C.sub.1-10 -alkyl substituted by halo, C.sub.1-4 -alkoxy or phenyl, 1-naphthyl or 2-naphthyl, each optionally substituted as defined below, (d) C.sub.4-10 -cycloalkyl, (e) C.sub.4-10 -cycloalkyl substituted by C.sub.1-4 -alkyl, (f) phenyl, 1-naphthyl or 2-naphthyl, (g) phenyl, 1-naphthyl or 2-naphthyl substituted by 1-3 halogen atoms, phenyl, 1-3 alkyl groups of 1-4 C atoms each, or a chloromethyl-, fluoromethyl-, trifluoromethyl-, carboxyl-, hydroxy- or alkoxy-group of 1-4 C atoms, or (h) an aromatic, 5- or 6-membered heterocyclic ring containing one hetero atom which is O, N or S, the remaining atoms being carbon; R.sub.3 also possibly being an acyl group of a C.sub.
    Type: Grant
    Filed: November 2, 1981
    Date of Patent: December 21, 1982
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Helmut Vorbruggen, Bernd Raduchel, Jorge Casals-Stenzel, Ekkehard Schillinger, Michael H. Town
  • Patent number: 4315013
    Abstract: Prostane derivatives of the formula ##STR1## wherein R.sub.1 is (a) hydrogen, (b) C.sub.1-10 alkyl, (c) C.sub.1-10 alkyl substituted by halogen; C.sub.1-4 alkoxy; C.sub.6-10 aryl; C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group; di-C.sub.1-4 -alkylamino; or tri-C.sub.1-4 alkylammonium; (d) C.sub.4-10 cycloalkyl, (e) C.sub.4-10 cycloalkyl substituted by C.sub.1-4 alkyl, (f) C.sub.6-10 aryl, (g) C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group, or (h) an aromatic heterocycle of 5 or 6 ring atoms one of which is O, N or S;W is hydroxymethylene or RO-methylene; or ##STR2## wherein OH or OR is in the .alpha.
    Type: Grant
    Filed: February 19, 1980
    Date of Patent: February 9, 1982
    Assignee: Schering, Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Raduechel, Helmut Vorbrueggen, Gerda Mannesmann, Wolfgang Losert, Jorge Casals
  • Patent number: 4291029
    Abstract: Compounds of the formula ##STR1## wherein the 15,16-methylene group is in the .alpha.- or .beta.-position, andE is ##STR2## are useful as diuretics.
    Type: Grant
    Filed: May 29, 1980
    Date of Patent: September 22, 1981
    Assignee: Schering, Aktiengesellschaft
    Inventors: Rudolf Wiechert, Dieter Bittler, Ulrich Kerb, Klaus Prezewowsky, Jorge Casals-Stenzel, Wolfgang Losert
  • Patent number: 4191694
    Abstract: Prostane derivatives of the formula ##STR1## wherein R.sub.1 is OR.sub.2 or NHR.sub.3 ;R.sub.2 is hydrogen, C.sub.1-10 alkyl, C.sub.4-10 cycloalkyl, C.sub.6-10 aryl, or a 5 or 6 membered heterocyclic ring having 1-3 hetero atoms selected from O, N and S;R.sub.3 is the residue of a hydrocarbon carboxylic or sulfonic acid of 1-15 carbon atoms;W is (a) an OH-substituted methylene group, (b) a ##STR2## wherein the OH-groups in (a) or (b) can be in the .alpha.- or .beta.-position, or (c) such a group wherein the H atom of the OH group is replaced by the residue of a hydrocarbon carboxylic or sulfonic acid of 1-15 carbon atoms or by a conventional etherifying OH-blocking group;R.sub.4 is OH or hydroxy whose H atom is replaced as defined for W; andR.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11 each independently is hydrogen or alkyl of 1-5 carbon atoms; or R.sub.9 and R.sub.10 together represent a direct bond; and, when R.sub.11 is alkyl, R.sub.
    Type: Grant
    Filed: July 26, 1978
    Date of Patent: March 4, 1980
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Raduchel, Norbert Schwarz, Helmut Vorbruggen, Bernd Muller, Gerda Mannesmann, Olaf Loge, Ekkehardt Schillinger, Jorge Casals-Stenzel
  • Patent number: 4180570
    Abstract: Compounds of the formula I ##STR1## wherein R.sub.2 is hydrogen or an organic acid residue;R.sub.3 is methyl or ethyl;R.sub.4 is hydrogen or methyl; ##STR2## wherein R.sub.1 is lower alkyl; and ##STR3## and when R.sub.2 is a dibasic acid residue, the physiologically acceptable salts thereof with the free acid moiety of the R.sub.2 group, are physiologically active, e.g., are diuretics having aldosterone antagonist effects.
    Type: Grant
    Filed: May 10, 1978
    Date of Patent: December 25, 1979
    Assignee: Schering Aktiengesellschaft
    Inventors: Rudolf Wiechert, Dieter Bittler, Ulrich Kerb, Jorge Casals-Stenzel, Wolfgang Losert
  • Patent number: 4129564
    Abstract: New spirolactones of the formula ##STR1## R is a lower alkyl of up to 5 carbon atoms, and ##STR2##
    Type: Grant
    Filed: November 11, 1977
    Date of Patent: December 12, 1978
    Assignee: Schering, A.G. Patentabteilung
    Inventors: Rudolf Wiechert, Dieter Bittler, Ulrich Kerb, Jorge Casals-Stenzel, Wolfgang Losert
  • Patent number: 4118488
    Abstract: 4-Androsten-3-ones of the formula ##STR1## wherein R.sub.1 is hydrogen or the acyl radical of an organic or inorganic acid, R.sub.2 is hydrogen, alkyl, or the acyl radical of an organic or inorganic acid, R.sub.3 is methyl or ethyl, R.sub.4 is hydrogen or methyl, ##STR2## and R.sub.5 is lower alkyl, have diuretic activity.
    Type: Grant
    Filed: March 3, 1977
    Date of Patent: October 3, 1978
    Assignee: Schering Aktiengesellschaft
    Inventors: Rainer Philippson, Bernhard Krieger, Jorge Casals-Stenzel, Ulrich Kerb, Wolfgang Losert, Klaus Prezewowsky, Rudolf Wiechert, Dieter Bittler