Patents by Inventor Jens K. Perregaard
Jens K. Perregaard 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: 5807889Abstract: Compounds of formula I ##STR1## wherein R1=(cyclo)alk(en)yl, aralkyl, alkyl(oxy)carbonyl, CONH2, etc.; R2=H, (cyclo)alk(en)yl, aralkyl, etc.; R3-R5=H, halo, alkyl, alkoxy, etc.; R6,R7=H, alkyl; R6R7=atoms to complete a ring; R8,R9=groups cited for R2, 2-oxoimidazolidinoalkyl, etc.; NR8R9=heterocyclyl; 1 of X,Y=CH2 and the other=CH2, O, S were prepd. Thus, 1-indancarboxylic acid was converted in 5 steps to 1-(N,N-dipropylaminomethyl)-6-formylaminoindane oxalate which had ED50 of 0.0055.mu.M/kg s.c. in the 8-OH DPAT cue agonism test in rats.Type: GrantFiled: June 6, 1995Date of Patent: September 15, 1998Assignee: H. Lundbeck A/SInventor: Jens K. Perregaard
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Patent number: 5462948Abstract: 1-Aryl-3-(4-1piperidyl)-indole derivatives having general formula (I), ##STR1## wherein R.sup.1 is hydrogen, halogen, alkyl, alkoxy, hydroxy, cyano, nitro, alkylthio, trifluoromethyl, trifluoromethylthio, alkylsulfonyl, amino, alkylamino or dialkylaminio; R is optionally substituted phenyl or a heteroaromatic group; and R.sup.2 is hydrogen, cycloalkyl, alkyl or alkenyl, optionally substituted with one or two hydroxy groups, or R.sup.2 is a group of formula (IV), ##STR2## wherein n is an integer of from 2-6; W is O, S or N--R.sup.3, wherein R.sup.3 is H alkyl or cycloalkyl; U is N or CH, Z is --(CH.sub.2).sub.m --, m being 2 or 3, or Z is --CH.dbd.CH--, 1,2-phenylene, or --COCH.sub.2 -- or --CSCH.sub.2 --; V is O,S,CH.sub.2, or NR.sup.4, wherein R.sup.4 is hydrogen, optionally hydroxy substituted alkyl, alkenyl or cycloalkylmethyl; are useful in alleviating, relieving or suppressing withdrawal or abstinence symptons or suppressing the dependency of a drug or a substance of abuse.Type: GrantFiled: September 1, 1993Date of Patent: October 31, 1995Assignee: H. Lundbeck A/SInventors: Jens K. Perregaard, Brenda Costall
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Patent number: 5457115Abstract: A substituted indole compound having the formula I: ##STR1## where Ar is one of a phenyl group, a phenyl group substituted with at least one substituent selected from halogen, lower alkyl, lower alkoxy, hydroxy, trifluoromethyl, and cyano, and a hetero aromatic group selected from 2-thienyl, 3-thienyl, 2-furanyl, 3-furanyl, 2-oxazolyl, 2-imidazolyl, 2-pyridyl, 3-pyridyl, and 4-pyridyl; each dotted line is an optional double bond; X and X' are independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy, lower alkylthio, lower alkylsulfonyl, lower alkylamino, lower dialkylamino, cyano, trifluoromethyl, and trifluoromethylthio; or X and X' are taken together to form a 5 to 7 membered carbocyclic ring; R.sup.1 is selected from the group consisting of hydrogen, lower alkyl and lower alkyl substituted with one or two hydroxy groups; with the proviso that when X is hydrogen or fluoro then R.sup.Type: GrantFiled: March 9, 1994Date of Patent: October 10, 1995Assignee: H. Lundbeck A/SInventors: Jens K. Perregaard, Kim Andersen, Klaus P. Boegesoe, Henrik Pedersen
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Patent number: 5444073Abstract: A method for treating memory impairment is disclosed. The method comprises administering a therapeutically effective amount of a compound having the formula: ##STR1## or a pharmaceutically acceptable acid addition salt or prodrug therefor to a patient.Type: GrantFiled: September 1, 1993Date of Patent: August 22, 1995Assignee: H. Lundbeck A/SInventors: Jens K. Perregaard, Brenda Costall
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Patent number: 5439922Abstract: A method for treating anxiety in mammals comprising administering in an effective amount to said mammal an 1-aryl-3-(4-piperidyl)-indole derivative having the general formula: ##STR1## wherein R.sup.1 is H, F, Cl, Br, methyl, methoxy or cyano; and R.sup.3 is H or methyl; or a pharmaceutical acceptable acid addition salt thereof.Type: GrantFiled: December 17, 1992Date of Patent: August 8, 1995Assignee: H. Lundbeck A/SInventors: Jens K. Perregaard, Brenda Costall
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Patent number: 5428036Abstract: Reaction products of sertindole with an acid or an activated acid, with formaldehyde alone, formaldehyde in the presence of an alcohol or an amine, or with an acyloxymethylene halide, and having general formula (1) wherein X is CO, CS, or CH.sub.2, and if X is CO or CS, R is (i) hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl or cycloalk(en)ylalk(en)yl optionally substituted with hydroxy, or optionally substituted phenyl; or (ii) YR.sup.1, wherein Y is O or S and R.sup.1 is one of the substituents defined for R under (i) above; or (iii) NR.sup.2 R.sup.3, wherein R.sup.2 and R.sup.3 independently are selected from the substituents defined for R under (i) above or R.sup.2 and R.sup.3 are combined to form a heterocyclic ring; or if X is CH.sub.2, R is: (iv) a group YR.sup.1 as defined in (ii); (v) a group NR.sup.2 R.sup.3 as defined in (iii); or (vi) a group OC(O)R.sup.4, wherein R.sup.4 is as defined for R.sup.Type: GrantFiled: March 30, 1993Date of Patent: June 27, 1995Assignee: H. Lundbeck A/SInventors: Jens K. Perregaard, Henrik Pederson
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Patent number: 5393761Abstract: 3-Arylindole or 3-arylindazole derivatives having formula: ##STR1## wherein Ar is optionally substituted phenyl or a heteroaromatic group; R.sup.1 -R.sup.4 are independently selected from hydrogen, halogen, alkyl, alkoxy, hydroxy, nitro, alkylthio, alkylsulphonyl, alkyl- or dialkylamino, cyano, trifluoromethyl, or trifluoromethylthio;the dotted lines designate optional bonds;X is N or a group CR.sup.6 wherein R.sup.6 is hydrogen, halogen, trifluoromethyl or alkyl, or X is CH.sub.2 ; Y is N or CH, or Y is C;R.sup.5 is hydrogen, cycloalkyl, cycloalkylmethyl, alkyl or alkenyl, optionally substituted with one or two hydroxy groups, or R.sup.5 is a group taken from structures 1a and 1b: ##STR2## wherein n is an integer from 2-6; W is O or S; U is N or CH; Z is --(CH.sub.2).sub.m --, m being 2 or 3, --CH.dbd.CH--, 1,2-phenylene or --COCH.sub.2 --or --CSCH.sub.2 --; V is O, S, CH.sub.2, or NR.sup.7 ; U.sup.1 is O, S, CH.sub.2 or NR.sup.8 ; and V.sup.1 is NR.sup.9 R.sup.10, OR.sup.11, SR.sup.12 or CR.sup.13 R.sup.Type: GrantFiled: October 4, 1993Date of Patent: February 28, 1995Assignee: H. Lundbeck A/SInventors: Jens K. Perregaard, Kim Andersen
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Patent number: 5322851Abstract: Specific 2- and 2,5-substituted indoles or 2,3-dihydroindole compounds of the following formula ##STR1## wherein, R is formula 1a ##STR2## and X, X', Ar, R.sup.1, n, U, Z, V and W are defined in the specification are provided, having long lasting serotonin activity with specific binding to 5-HT.sub.2 receptors of the central nervous system. These compounds are suitable for therapeutic treatment of CNS disorders, such as anxiety, depression, sleep disturbances, migraine, negative symptoms of schizophrenia, and Parkinson's disease.Type: GrantFiled: February 25, 1993Date of Patent: June 21, 1994Assignee: H. Lundbeck A/SInventors: Jens K. Perregaard, Kim Andersen, Klaus P. Boegesoe, Henrik Pedersen
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Patent number: 5216001Abstract: Specific 6-substituted or 2-alkyl substituted indole or 2,3-dihydroindole compounds are provided, having long lasting serotonin activity with specific binding to 5-HT.sub.2 receptors of the central nervous system. These compounds are suitable for therapeutic treatment of CNS disorders, such as anxiety, depression, sleep disturbances, migraine, negative symptoms of schizophrenia, and Parkinson's disease.Type: GrantFiled: June 27, 1991Date of Patent: June 1, 1993Assignee: H. Lunbeck A/SInventors: Jens K. Perregaard, Kim Andersen, Klaus P. Boegesoe, Henrik Pedersen
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Patent number: 4946863Abstract: The present invention relates to 3-aminomethyl derivatives of indane, dihydrobenzofurane, dihydrobenzothiophene, and indoline, acid addition salts thereof, isomers thereof, methods of preparation, pharmaceutical compositions and method of treating CNS-disorders such as schizophrenia, Parkinson's disease, depression, anxiety, migraine and senile dementia, or in the cure of cardiovascular diseases, by administering such a derivative.Type: GrantFiled: January 18, 1989Date of Patent: August 7, 1990Assignee: H. Lundbeck A/SInventors: Klaus P. Boegesoe, Jens K. Perregaard
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Patent number: 4855307Abstract: The present invention relates to the novel acetic acid ester of 4-(4-(4-chlorophenyl)-4-hydroxy-1-piperidinyl)-1-(4-fluorophenyl)-1-butano ne, as well as pharmaceutically acceptable acid addition salts thereof, a method of preparation, pharmaceutical compositions and a method of treating psychoses by administering said ester to an animal or human body.Type: GrantFiled: September 4, 1987Date of Patent: August 8, 1989Assignee: H. Lundbeck A/SInventor: Jens K. Perregaard
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Patent number: 4847254Abstract: The present invention relates to 3-aminomethyl derivatives of indane, dihydrobenzofurane, dihydrobenzothiophene, and indoline, acid addition salts thereof, isomers thereof, methods of preparation, pharmaceutical compositions and method of treating CNS-disorders such as schizophrenia, Parkinson's disease, depression, anxiety, migraine and senile dementia, or in the cure of cardiovascular diseases, by administering such a derivative.Type: GrantFiled: February 12, 1988Date of Patent: July 11, 1989Assignee: H. Lundbeck A/SInventors: Klaus P. Boegesoe, Jens K. Perregaard
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Patent number: 4710500Abstract: The present invention relates to novel indole derivatives which have interesting pharmacodynamic effects indicating pronounced activity in the treatment of psychic disorders, especially psychoses and, at the same time, a low degree of undesired side effects.Moreover, the invention relates to methods for the preparation of said indole derivatives, pharmaceutical compositions containing same, and methods for the treatment of psychic disorders, especially psychoses, by administering a therapeutically active amount of one of said derivatives to a living animal body, including human beings.The novel indole derivatives of the present invention are represented by the following formula: ##STR1## wherein R is phenyl, optionally substituted with halogen, lower alkyl or trifluoromethyl, or a hetero aromatic group, such as 2-thienyl, 3-thienyl, 2-furoyl, 3-furoyl, 2-thiazol, 2-oxazol, 2-imidazole, 2-pyridyl, 3-pyridyl or 4-pyridyl; R.sup.Type: GrantFiled: April 1, 1986Date of Patent: December 1, 1987Assignee: H. Lundbeck A/SInventor: Jens K. Perregaard
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Patent number: 4525360Abstract: The present invention relates to novel phenylindene derivatives having interesting pharmacodynamic properties which make them useful as psychopharmacologicals in the treatment especially of psychoses such as schizophrenia, having a low degree of undesired side effects such as cataleptic effects, methods for the preparation of said phenylindene derivatives, pharmaceutical compositions containing same, and methods for the treatment of psychic disorders, such as psychoses and depressions and pain, by administering a therapeutically active amount of one of said derivatives to a living animal body, including human beings.Type: GrantFiled: October 5, 1983Date of Patent: June 25, 1985Assignee: Kefalas A/SInventor: Jens K. Perregaard
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Patent number: 4353910Abstract: Carbamoyl derivatives of 4,5,6,7-Tetrahydroisoxazolo[5,4-c] Pyridine-3-one, and method of preparation, pharmaceutical compositions thereof, and methods of treatment of GABA-system malfunctions therewith, are all disclosed.Type: GrantFiled: November 27, 1981Date of Patent: October 12, 1982Assignee: Kefalas A/SInventor: Jens K. Perregaard
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Patent number: RE34299Abstract: The present invention relates to novel indole derivatives which have interesting pharmacodynamic effects indicating pronounced activity in the treatment of psychic disorders, especially psychoses and, at the same time, a low degree of undesired side effects.Moreover, the invention relates to methods for the preparation of said indole derivatives, pharmaceutical compositions containing same, and methods for the treatment of psychic disorders, especially psychoses, by administering a therapeutically active amount of one of said derivatives to a living animal body, including human beings.The novel indole derivatives of the present invention are represented by the following formula; ##STR1## wherein R is phenyl, optionally substituted with halogen.[., lower alkyl or trifluoromethyl,.]. or a hetero aromatic group, such as 2-thienyl, 3-thienyl, .[.2-furoyl, 3-furoyl, 2-thiazol, 2-oxazol, 2-imidazole, 2-pyridyl, 3-pyridyl.]. .Iadd.2-oxazolyl, 2-imidazolyl, 2-pyridyl 3-pyridyl.Iaddend.or 4-pyridyl; R.sup.Type: GrantFiled: September 13, 1991Date of Patent: June 29, 1993Assignee: H. Lundbeck A/SInventor: Jens K. Perregaard
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Patent number: RE34712Abstract: The two enantiomers of the anti-depressant drug of the formula I ##STR1## are disclosed. Methods for resolving intermediates and their .[.steroselective.]. .Iadd.stereoselective .Iaddend.conversion to a corresponding .[.enatiomer.]. .Iadd.enantiomer .Iaddend.of I are also disclosed.Type: GrantFiled: September 14, 1993Date of Patent: August 30, 1994Assignee: H. Lundbeck A/SInventors: Klaus P. Boegesoe, Jens K. Perregaard