Patents by Inventor Helmut Hofmeister

Helmut Hofmeister 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: 4885117
    Abstract: (Z)-17.alpha.-halovinyl steroids of general Formula I ##STR1## wherein . . . . is a single bond or a double bond,V is a carbon-to-carbon bond or a methylene group,R.sub.1 is a hydrogen atom or a methyl group,X is a chlorine atom, a bromine atom or an iodine atom, andA symbolizes the remainder of the steroid molecule,are prepared by hydrogenating a 17.alpha.-haloethynyl steroid of formula II with diimide. ##STR2## wherein . . . , V, R.sub.1, X and A have the meanings given above. The compounds of Formula I include both known and novel compounds, all of which are pharmacologically active.
    Type: Grant
    Filed: August 11, 1987
    Date of Patent: December 5, 1989
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Hofmeister, Henry Laurent, Rudolf Wiechert
  • Patent number: 4777165
    Abstract: 6.alpha.,16.beta.-Dimethyl corticoids of general Formula I ##STR1## wherein the bond .sub.-------- is a single bond or a double bond, andX is a hydrogen atom, a fluorine atom, a chlorine atom, or a bromine atom,Z is a hydrogen atom or, jointly with X, is a carbon-carbon bond,R.sub.1 is a formyl group, an alkanoyl group or alkoxyalkyl group of 2-8 carbon atoms, or a benzoyl group, andY is a hydrogen atom or a methyl group,are pharmacologically active compounds.
    Type: Grant
    Filed: June 17, 1987
    Date of Patent: October 11, 1988
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Annen, Henry Laurent, Helmut Hofmeister, Rudolf Wiechert, Michael Topert
  • Patent number: 4725426
    Abstract: 17.alpha.-bromo-.alpha. and 17.alpha.-iodo-vinyl-estrane derivatives of general formula I ##STR1## wherein X is a bromine or iodine atom in Z or E position,R.sup.1 is hydrogen, hydroxy or acyloxy with up to 3 C atoms,R.sup.2 is hydrogen, alkyl with up to 3 C atoms and alkanoyl and aroyl with up to 7 C atoms,R.sup.3 is hydrogen or methyl,R.sup.4 is a hydrogen atom in the .alpha. or .beta. position,R.sup.5 is hydrogen, methyl or methoxy andR.sup.6 is hydrogen or methyl,are pharmacologically effective with a profile of action like ethinylestradiol and in the form of their radioactively labeled compounds are also valuable diagnostic media.The Z-isomers can be prepared by a new process by reaction of the corresponding 17.alpha.-ethinyl steroids with trialkyl (or phenyl) tin hydride with addition of a free radical former.
    Type: Grant
    Filed: July 25, 1985
    Date of Patent: February 16, 1988
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Hofmeister, Henry Laurent, Paul E. Schulze, Rudolf Wiechert, Walter Elger, Kunhard Pollow, Hans J. Grill
  • Patent number: 4719054
    Abstract: A process and novel starting materials for the production of 17.alpha.-ethynyl-17.beta.-hydroxy-18-methyl-4,15-estradien-3-one of Formula I ##STR1## are disclosed. Novel 17-ketone starting materials have the Formula II ##STR2## wherein R is an alkyl residue of 1-3 carbon atoms and ##STR3## is the grouping ##STR4## wherein R' is an acyl group of up to 10 carbon atoms.
    Type: Grant
    Filed: May 9, 1986
    Date of Patent: January 12, 1988
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Hofmeister, Henry Laurent, Hans-Peter Lorenz, Rudolf Wiechert
  • Patent number: 4708823
    Abstract: Known pregnane derivatives are prepared by esterificiation of known androstane derivatives to give new ester of Formula III ##STR1## wherein in each case symbolizes a single bond or a double bond,n is 1 or 2,R.sub.1 is hydrogen or methyl,R.sub.2 is hydrogen or formyl, andR.sub.3 is chlorine, hydroxy or an alkanoyloxy group of up to 6 carbon atoms,and reaction of the latter with Ag(I) and formic acid.
    Type: Grant
    Filed: September 17, 1985
    Date of Patent: November 24, 1987
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Hofmeister, Klaus Annen, Henry Laurent, Rudolf Wiechert
  • Patent number: 4701451
    Abstract: Compounds of Formula I ##STR1## wherein the bond is a single bond or a double bond,X is hydrogen, fluorine, chlorine, or bromine,R.sub.1 is formyl, alkanoyl or alkoxyalkyl each of which contains 2-8 carbon atoms, or benzoyl, andY is chlorine, hydroxy, formyl, alkanoyloxy of 2-8 carbon atoms, or benzoyloxy,have valuable anti-inflammatory properties.
    Type: Grant
    Filed: October 29, 1985
    Date of Patent: October 20, 1987
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Annen, Henry Laurent, Helmut Hofmeister, Rudolf Wiechert, Michael Toepert, Hans Wendt
  • Patent number: 4670427
    Abstract: 1.alpha.,2.alpha.-methylene-6-methylene- and 6.alpha.-methylpregnenes of Formula I ##STR1## wherein A is ##STR2## and R is a hydrogen atom, an acyl group, or an alkoxymethyl groupare strong antiandrogens, and suitable for the topical treatment of seborrhea, acne, alopecia, and hirsutism.
    Type: Grant
    Filed: January 18, 1985
    Date of Patent: June 2, 1987
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Annen, Henry Laurent, Walter Elger, Rudolf Wiechert, Helmut Hofmeister, Michael Topert
  • Patent number: 4645763
    Abstract: 6.alpha.-Methyl corticoids of formula I ##STR1## wherein is a single bond or a double bond, R is acyloxy of up to 8 carbon atoms, and X is chlorine, hydroxy, or acyloxy of up to 8 carbon atoms, are pharamacologically effective substances.
    Type: Grant
    Filed: November 22, 1983
    Date of Patent: February 24, 1987
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Annen, Henry Laurent, Helmut Hofmeister, Rudolf Wiechert, Hans Wendt
  • Patent number: 4619922
    Abstract: 6.alpha.,16.alpha.-Dimethyl corticoids of general Formula I ##STR1## wherein the bond is a single bond or a double bond,X is a hydrogen atom, a fluorine atom, a chlorine atom, or a bromine atom,R.sub.1 is a formyl group, an alkanoyl group or alkoxyalkyl group of 2-8 carbon atoms, or a benzoyl group, andY is a hydrogen atom, a chlorine atom, a hydroxy group, a formyl group, an alkanoyloxy group of 2-8 carbon atoms, or a benzoyloxy group,are pharmacologically effective compounds.
    Type: Grant
    Filed: January 2, 1985
    Date of Patent: October 28, 1986
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Annen, Henry Laurent, Helmut Hofmeister, Michael Topert
  • Patent number: 4603013
    Abstract: Estrane derivatives of the general formula I ##STR1## wherein one of the substituents X or Z signifies a hydrogen atom and the other together with Y represents a carbon-carbon bond, or wherein the substituents X and Z represent hydrogen atoms and Y represents an .alpha.-position hydroxy group or a .beta.-position alkyl group with up to 6 carbon atoms, are valuable intermediates for preparation of pharmacologically effective substances.
    Type: Grant
    Filed: August 27, 1984
    Date of Patent: July 29, 1986
    Assignee: Schering Aktiengesellschaft
    Inventors: Gunter Neef, Karl Petzoldt, Gerhard Sauer, Helmut Hofmeister
  • Patent number: 4587236
    Abstract: 6.alpha.-Methylprednisolone derivatives of Formula I ##STR1## wherein R.sub.1 is 1-oxoalkyl of 2-6 carbon atoms or benzoyl andR.sub.2 is 1-oxoalkyl of 2-6 carbon atoms, are pharmacologically efficacious compounds, e.g., as antiinflammatories.
    Type: Grant
    Filed: October 27, 1983
    Date of Patent: May 6, 1986
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Annen, Karl Petzoldt, Henry Laurent, Rudolf Wiechert, Helmut Hofmeister
  • Patent number: 4567002
    Abstract: 17-haloethynyl steroids of the partial formula ##STR1## wherein R.sub.1 is hydrogen or methyl,R.sub.2 is alkyl of 1-4 carbon atoms, acyl of 1-7 carbon atoms, trimethylsilyl, 2-tetrahydropyranyl, or nitrate,X is bromine or iodine, andV is methylene, ethylene, vinylene, ethylidene, vinylidene or cyclopropylene,can be prepared by treating an ethynyl steroid of the partial formula ##STR2## wherein R.sub.1, R.sub.2, and V are as defined above, in an inert solvent with a brominating agent or an iodinating agent in the presence of a silver salt. Certain new compounds are also provided.
    Type: Grant
    Filed: April 25, 1984
    Date of Patent: January 28, 1986
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Hofmeister, Henry Laurent, Klaus Annen, Rudolf Wiechert
  • Patent number: 4555507
    Abstract: Compounds of Formula I ##STR1## wherein the bond is a single bond or a double bond,X is hydrogen, flourine, chlorine, or bromine,R.sub.1 is formyl, alkanoyl or alkoxyalkyl each of which contains 2-8 carbon atoms, or benzoyl, andY is chlorine, hydroxy, formyl, alkanoyloxy of 2-8 carbon atoms, or benzoyloxy,have valuable anti-inflammatory properties.
    Type: Grant
    Filed: July 19, 1983
    Date of Patent: November 26, 1985
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Annen, Henry Laurent, Helmut Hofmeister, Rudolf Wiechert, Michael Toepert, Hans Wendt
  • Patent number: 4550100
    Abstract: A process for preparing bromine- or iodine-unlabeled or radioactively labeled 17.alpha.-bromoethynyl- and 17.alpha.-iodoethynyl-17.beta.-hydroxy steroids of the androstane and estrane series of the partial formula ##STR1## wherein is a single bond or a double bond,V is a carbon-carbon bond or a methylene group,R is hydrogen or methyl, andX is bromine or iodine,from corresponding 17.alpha.-ethynyl-17.beta.-hydroxy steroids, comprises treating the starting steroid in an inert solvent with a brominating agent or an iodinating agent in the presence of a silver salt.The process enables production of old and new compounds having value as pharmacologically active compounds and also as diagnostic agents when the iodine or bromine is radioactive.
    Type: Grant
    Filed: November 16, 1983
    Date of Patent: October 29, 1985
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Hofmeister, Paul E. Schulze, Klaus Annen, Henry Laurent, Rudolf Wiechert
  • Patent number: 4536401
    Abstract: Compounds of the formula I ##STR1## wherein R.sub.1 is ##STR2## wherein R.sup.I and R.sup.II each independently is alkyl of 1-4 carbon atoms, or R.sup.I and R.sup.II together with the connecting N-atom form a 5- or 6-membered heterocyclic ring whose remaining atoms are all C-atoms, or which also includes and additional N-atom, an additional O or S atom or a combination thereof; ##STR3## wherein R.sup.I and R.sup.II are as defined above; --SR.sup.III, wherein R.sup.III is methyl, ethyl or phenyl; or--OR.sup.IV, wherein R.sup.IV is methyl, ethyl, propyl, methoxymethyl, allyl, or .beta.-dimethylaminoethyl;R.sub.2 is hydrogen, methyl, or ethyl; ##STR4## wherein the wavy lines mean that the substituent is in the .alpha.- or .beta.-position, and ##STR5## M is Na, K or Li; and R.sup.V, R.sup.VI, R.sup.VII and R.sup.VIII each independently is alkyl of 1-4 carbon atoms, have valuable pharmacological properties, e.g., a combination of antiprogestational and antimineralocorticordal effects.
    Type: Grant
    Filed: February 21, 1984
    Date of Patent: August 20, 1985
    Assignee: Schering Aktiengesellschaft
    Inventors: Guenter Neef, Gerhard Sauer, Rudolf Wiechert, Helmut Hofmeister, Ralph Rohde, Klaus Annen, Henry Laurent, Sybille Beier, Wolfgang Losert, Walter Elger, David Henderson
  • Patent number: 4464365
    Abstract: 11.beta.-Chloro-.DELTA..sup.15 -steroids of Formula I ##STR1## wherein R.sup.1 is hydrogen or acyl andR.sup.2 is ethynyl, chloroethynyl, or propynyl have strong progestational activity.
    Type: Grant
    Filed: April 18, 1983
    Date of Patent: August 7, 1984
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Hofmeister, Karl Petzoldt, Klaus Annen, Henry Laurent, Rudolf Wiechert, Yukeshige Nishino
  • Patent number: 4440684
    Abstract: A process for preparing 6-methyl-.DELTA..sup.4,6 -3-keto steroids of the formula ##STR1## comprises reacting a corresponding .DELTA..sup.4 -3-keto steroid with methoxymethyl acetate (CH.sub.3 --O--CH.sub.2 --OAc) in an inert solvent at temperatures above room temperature in the presence of an alkali metal acetate.
    Type: Grant
    Filed: February 4, 1983
    Date of Patent: April 3, 1984
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Annen, Henry Laurent, Helmut Hofmeister, Rudolf Wiechert
  • Patent number: 4435390
    Abstract: Hydrocortisone derivatives of Formula I ##STR1## wherein is a single bond or a double bond,n is 1 or 2,R.sub.1 is hydrogen or methyl,R.sub.2 is alkyl of 1-6 carbon atoms, andR.sub.3 is hydrogen or 1-oxoalkyl (alkanoyl) of 2-6 carbon atoms,are pharmacologically active compounds, e.g., as antiinflammatories.
    Type: Grant
    Filed: August 18, 1982
    Date of Patent: March 6, 1984
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Annen, Henry Laurent, Helmut Hofmeister, Rudolf Wiechert
  • Patent number: 4432976
    Abstract: Corticoids of Formula I ##STR1## wherein is a single bond or a double bond,X is hydrogen, fluorine, or chlorine,Y represents two hydrogen atoms or an oxygen atom, andZ is hydrogen or acyloxy of 2-6 carbon atoms, are pharmacologically active compounds, e.g., as anti-inflammatories.
    Type: Grant
    Filed: August 23, 1982
    Date of Patent: February 21, 1984
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Annen, Henry Laurent, Helmut Hofmeister
  • Patent number: 4404141
    Abstract: .DELTA..sup.16 - and .DELTA..sup.17 -21-chloro-20-keto steroids of the formula ##STR1## wherein n is 1 or 2,C.sub.1 C.sub.2 and C.sub.9 C.sub.11 represent a CC-single or CC-double bond,R.sub.1 is H or OH,R.sub.2 is H or CH.sub.3,R.sub.3 is H or F wherein, when R.sub.3 =F, C.sub.9 C.sub.11 is a CC-single bond, andR.sub.4 is H, CH.sub.3, or F,are valuable intermediates for preparation of highly effective, known steroids.A process for preparing these compounds involves heating the corresponding 11.beta.- and/or 17.alpha.- or 17a.alpha.-nitrooxy-21-mesyloxy-20-keto steroids with lithium chloride in a dipolar aprotic solvent at temperatures above room temperature.
    Type: Grant
    Filed: March 9, 1982
    Date of Patent: September 13, 1983
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Annen, Henry Laurent, Helmut Hofmeister