Patents Represented by Attorney, Agent or Law Firm Mary Appollina
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Patent number: 6103725Abstract: The present invention concerns the compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is O or S; n is 2, 3, 4 or 5; R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy or halo; R.sup.2 is hydrogen, C.sub.1-6 alkyl, phenyl, phenylC.sub.1-6 alkyl or phenylcarbonyl; R.sup.3 and R.sup.4 each independently are selected from hydrogen, halo, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, haloC.sub.1-6 alkyl, aminosulfonyl, mono- or di(C.sub.1-4 alkyl)aminosulfonyl; or R.sup.3 and R.sup.4 may also be taken together to form a bivalent radical of formula --CH.dbd.CH--CH.dbd.CH--; it further relates to processes for their preparation, compositions comprising them as well as their use as a medicine; compounds of formula (I) containing a radioactive isotope; a process of marking dopamine D.sub.4 receptor sites; and a process for imaging an organ are disclosed.Type: GrantFiled: November 9, 1998Date of Patent: August 15, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Serge Maria Aloysius Pieters
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Patent number: 6100268Abstract: The present invention is concerned with compounds of formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is hydrogen or C.sub.1-6 -alkyl; R.sup.4 is hydrogen, halo, C.sub.1-6 alkyl, hydroxy, C.sub.1-6 alkyloxy, aryloxy or arylmethoxy; R.sup.5 and R.sup.6 designate R.sup.5a and R.sup.6a wherein R.sup.5a and R.sup.6a taken together form a bivalent radical; or R.sup.5 and R.sup.6 can designate R.sup.5b and R.sup.6b wherein R.sup.5b is hydrogen and R.sup.6b is a heterocycle or an optionally substituted alkenyl or alkynyl group; or R.sup.5 and R.sup.6 designate R.sup.5c and R.sup.6c, wherein R.sup.5c and R.sup.6c are hydrogen, halo, C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, hydroxy, C.sub.1-6 alkyloxy, cyano, aminoC.sub.1-6 alkyl, carboxyl, C.sub.1-6 alkyloxycarbonyl, nitro, amino, aminocarbonyl, C.sub.Type: GrantFiled: July 28, 1998Date of Patent: August 8, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Guy Rosalia Eugene Van Lommen, Piet Tom Bert Paul Wigerinck, Marcel Frans Leopold De Bruyn, Wim Gaston Verschueren, Marc Francis Josephine Schroven
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Patent number: 6099863Abstract: The present invention is concerned with a fast-dissolving tablet for oral administration comprising as an active ingredient a therapeutically effective amount of galanthamine hydrobromide (1:1) and a pharmaceutically acceptable carrier, characterized in that said carrier comprises a spray-dried mixture of lactose monohydrate and microcrystalline cellulose (75:25) as a diluent, and a disintegrant; and with a direct compression process of preparing such fast-dissolving tablets.Type: GrantFiled: December 9, 1998Date of Patent: August 8, 2000Assignee: Janssen Pharmaceutica N.V.Inventors: Paul Marie Victor Gilis, Valentin Florent Victor De Conde
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Patent number: 6077843Abstract: The present invention is concerned with a pharmaceutical composition suitable as a depot formulation for administration via intramuscular or subcutaneous injection, comprising:(1) as an active ingredient a therapeutically effective amount of a 9-hydroxyrisperidone fatty acid ester or a salt, or a stereoisomer or a stereoisomeric mixture thereof and(2) a pharmaceutically acceptable carrier;wherein the pharmaceutically acceptable carrier is water and the active ingredient is suspended therein; and with a process of preparing such a composition. The invention further concerns such a pharmaceutical composition for use as a medicament in the treatment of schizophrenia, non-schizophrenic psychoses, behavioural disturbances associated with neurodegenerative disorders, e.g. in dementia, behavioural disturbances in mental retardation and autism, bipolar mania, depression, anxiety.Type: GrantFiled: November 12, 1998Date of Patent: June 20, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Marc Karel Jozef Fran.cedilla.ois, Roger Carolus Augusta Embrechts, Herman Karel Borghijs, Johan Monbaliu
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Patent number: 6077841Abstract: The invention is directed to novel substituted 5-heterocyclyl pyrazolopyrimidinones and derivatives thereof, their synthesis and their use in treating sexual dysfunction in mammals, especially male erectile dysfunction. Pharmaceutical compositions containing the compounds and methods of using them to treat sexual dysfunction are also described.Type: GrantFiled: September 2, 1999Date of Patent: June 20, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Zhihua Sui, Jihua Guan, Mark J. Macielag
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Patent number: 6075046Abstract: This invention relates to the use of an .alpha.,.alpha.'-iminobis(methylene)bis[2-chromanmethanol] derivative for the manufacture of a medicament for the therapeutic or prophylactic treatment of humans suffering from or prone to degenerative diseases and conditions of the vascular and nervous system which are associated with oxidative stress.Type: GrantFiled: December 21, 1998Date of Patent: June 13, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Didier Robert Guy Gabriel de Chaffoy de Courcelles, Anne Simone Josephine Lesage, Josepha Eduarda Maria Francisca Leysen
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Patent number: 6066651Abstract: Orally-active nipecotamide glycolamide ester derivatives of formula (I): ##STR1## are disclosed as useful in treating platelet-mediated thrombotic disorders.Type: GrantFiled: October 20, 1998Date of Patent: May 23, 2000Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventor: William J. Hoekstra
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Patent number: 6057441Abstract: This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; halomethylcarbonyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R.sup.3 and R.sup.4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or halomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.Type: GrantFiled: October 6, 1998Date of Patent: May 2, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Pilar Gil-Lopetegui, Francisco Javier Fernandez-Gadea, Theo Frans Meert
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Patent number: 6057325Abstract: This invention concerns the compounds of formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C.sub.1-6 alkanediyl; R.sup.1 is hydrogen, C.sub.1-6 alkyl, aryl or aryl C.sub.1-6 alkyl; R.sup.2, R.sup.3 and R.sup.4 are each independently selected from hydrogen, halo, hydroxy, nitro, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, trifluoromethyl, C.sub.1-6 alkylthio, mercapto, amino, mono- and di(C.sub.1-6 alkyl)amino, carboxyl, C.sub.1-6 alkyloxycarbonyl or C.sub.1-6 alkylcarbonyl; R.sup.5 is hydrogen, C.sub.1-6 alkyl, phenyl or phenylC.sub.1-6 alkyl; R.sup.6 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, or a radical of formula --NR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 are each independently selected from hydrogen, C.sub.1-6 alkyl, phenyl or phenylC.sub.1-6 alkyl; R.sup.7 is hydrogen or C.sub.1-6 alkyl; or R.sup.6 and R.sup.7 taken together may form a bivalent radical of formula --R.sup.6 --R.sup.Type: GrantFiled: November 9, 1998Date of Patent: May 2, 2000Assignee: Janssen Pharmaceutia, N.V.Inventors: Ludo Edmond Josephine Kennis, Josephus Carolus Mertens
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Patent number: 6054468Abstract: The present invention is concerned with the compound 1-(1H-pyrrol-2-ylmethyl)-2-piperidone for use as a medicine, in particular for use as an agent for reducing excessive directional cell migration (as in metastasis); and with pharmaceutical compositions comprising a pharmaceutically acceptable carrier and the title compound as an active ingredient.Type: GrantFiled: November 24, 1998Date of Patent: April 25, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Hugo Alfons Gabriel Geerts, Michael Joseph Kukla, Johan Jozef Gustave Hendrik Geysen
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Patent number: 6051718Abstract: The present invention concerns 2-cyanoiminoimidazole derivatives having the formula ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; difluoromethyl; trifluoromethyl; C.sub.3-6 cycloalkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; 6,7-dihydro-5H-cyclopentapyridinyl; bicyclo[2.2.1]-2-heptenyl; bicyclo[2.2.1]heptanyl; C.sub.1-6 alkylsulfonyl; arylsulfonyl; or substituted C.sub.1-10 alkyl; R.sup.3 is hydrogen, halo or C.sub.1-6 alkyloxy; R.sup.4 is hydrogen; halo; C.sub.1-6 alkyl; trifluoromethyl; C.sub.3-6 cycloalkyl; carboxyl; C.sub.1-4 alkyloxycarbonyl; C.sub.3-6 cycloalkylaminocarbonyl; aryl; Het.sup.1 ; or substituted C.sub.1-6 alkyl; or R.sup.4 is --O--R.sup.7 or --NH--R.sup.8 ; R.sup.5 is hydrogen, halo, hydroxy, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; R.sup.Type: GrantFiled: March 19, 1999Date of Patent: April 18, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Eddy Jean Edgard Freyne, Francisco Javier Fernandez-Gadea, Jose Ignacio Andres-Gil
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Patent number: 6037350Abstract: This invention comprises the novel compounds of formula (I) ##STR1## wherein the dotted line represents an optional bond; X is oxygen or sulfur; R.sup.1 is hydrogen, C.sub.1-12 alkyl, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, quinolinylC.sub.1-6 alkyl, pyridylC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxyC.sub.1-6 alkyl, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyl, aminoC.sub.1-6 alkyl, or a radical of formula -Alk.sup.1 -C(.dbd.O)--R.sup.9, -Alk.sup.1 -S(O)--R.sup.9 or -Alk.sup.1 -S(O).sub.2 --R.sup.9 ; R.sup.2, R.sup.3 and R.sup.16 each independently are hydrogen, hydroxy, halo, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, hydroxyC.sub.1-6 alkyloxy, C.sub.1-6 alkyloxyC.sub.1-6 alkyloxy, aminoC.sub.1-6 alkyloxy, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyloxy, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, Ar.sup.2 oxy, Ar.sup.2 C.sub.1-6 alkyloxy, hydroxycarbonyl, C.sub.1-6 alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C.sub.2-6 alkenyl; R.sup.4 and R.sup.5 each independently are hydrogen, halo, Ar.Type: GrantFiled: May 26, 1998Date of Patent: March 14, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Marc Gaston Venet, Patrick Rene Angibaud, Philippe Muller, Gerard Charles Sanz
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Patent number: 6022532Abstract: The use of a compound having the formula ##STR1## wherein R represents methyl or ethyl, for regulating the greasiness of the skin, particular novel physical forms of said compound, cosmetic compositions comprising said agent, processes for preparing said agent and compositions, and a method of reducing the greasiness of the skin.Type: GrantFiled: August 25, 1998Date of Patent: February 8, 2000Assignee: Janssen Pharmaceutica, N.V.Inventor: Gerard Frans Maria Jan Cauwenbergh
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Patent number: 5994376Abstract: The present invention describes 1,3-dihydro-1-(phenylalkyl)-2H-imidazol-2-one compounds and their use for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases.Type: GrantFiled: September 29, 1997Date of Patent: November 30, 1999Assignee: Janssen Pharmaceutica, N.V.Inventors: Eddy Jean Edgard Freyne, Gaston Stanislas Marcella Diels, Jose Ignacio Andres-Gil, Francisco Javier Fernandez-Gadea
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Patent number: 5990123Abstract: The present invention is concerned with compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein .dbd.a.sub.1 --a.sub.2 .dbd.a.sub.3 --a.sub.4 .dbd. is a bivalent radical of formula .dbd.N--CH.dbd.CH--CH.dbd. (a), .dbd.CH--N.dbd.CH--CH.dbd. (b), .dbd.CH--CH.dbd.N--CH.dbd. (c), .dbd.CH--CH.dbd.CH--N.dbd. (d), wherein one or two hydrogen atoms can be substituted by halo, hydroxy, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is C.sub.1-5 alkanediyl; Alk.sup.2 is C.sub.2-15 alkanediyl; Q is a five- or six-membered heterocyclic ring containing at least one nitrogen atom or a radical of formula --C(NR.sup.5 R.sup.6).dbd.C--R.sup.4 wherein R.sup.4 is hydrogen, cyano, aminocarbonyl or C.sub.1-6 alkyl; R.sup.5 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.Type: GrantFiled: August 6, 1997Date of Patent: November 23, 1999Assignee: Janssen Pharmaceutica, N.V.Inventors: Guy Rosalia Eugene Van Lommen, Jose Ignacio Andres-Gil, Francisco Javier Fernandez-Gadea, Maria Encarnacion Matesanz-Ballesteros
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Patent number: 5968952Abstract: The present invention is concerned with compounds of formula (I), ##STR1## the stereoisomeric forms thereof and the pharmaceutically acceptable acid or base addition salts thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; R.sup.1 is hydrogen, C.sub.1-12 alkyl, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, quinolinylC.sub.1-6 alkyl, pyridylC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxyC.sub.1-6 alkyl, mono- or di(C.sub.1-6 alkyl)-aminoC.sub.1-6 alkyl, aminoC.sub.1-6 alkyl, or a radical of formula --Alk.sup.1 --C(.dbd.O)--R.sup.9, --Alk.sup.1 --S(O)--R.sup.9 or --Alk.sup.1 --S(O).sub.2 --R.sup.9 ; R.sup.2 and R.sup.3 each independently are hydrogen, hydroxy, halo, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, hydroxyC.sub.1-6 alkyloxy, C.sub.1-6 alkyloxy-C.sub.1-6 alkyloxy, aminoC.sub.1-6 alkyloxy, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyloxy, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, Ar.sup.2 oxy, Ar.sup.2 C.sub.1-6 alkyloxy, hydroxycarbonyl, C.sub.Type: GrantFiled: April 29, 1998Date of Patent: October 19, 1999Assignee: Janssen Pharmaceutica, N.V.Inventors: Marc Gaston Venet, Patrick Rene Angibaud, Gerard Charles Sanz, David William End
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Patent number: 5952510Abstract: The present invention concerns the compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; difluoromethyl; trifluoromethyl; C.sub.3-6 cycloalkyl; a saturated 5-, 6 or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; bicyclo?2.2.1!-2-heptenyl; bicyclo?2.2.1!heptanyl; C.sub.1-6 alkylsulfonyl; arylsulfonyl; or substituted C.sub.1-10 alkyl; R.sup.3 is hydrogen, halo or C.sub.1-6 alkyloxy; R.sup.4 is hydrogen; cyano; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkyloxycarbonyl or aryl; R.sup.5 is hydrogen; cyano; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkyloxycarbonyl or aryl; Y is a direct bond or C.sub.1-3 alkanediyl; --A--B-- is a bivalent radical of formula --CR.sup.6 .dbd.CR.sup.7 -- or --CHR.sup.6 --CHR.sup.7 --; L is hydrogen; optionally substituted C.sub.Type: GrantFiled: September 30, 1997Date of Patent: September 14, 1999Assignee: Janssen Pharmaceutica, N.V.Inventors: Eddy Jean Edgard Freyne, Gaston Stanislas Marcella Diels, Jose Ignacio Andres-Gil, Francisco Javier Fernandez-Gadea
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Patent number: 5922734Abstract: This invention is concerned with the compounds of formula ##STR1## the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof,wherein: R.sup.1 is hydrogen, amino or C.sub.1-4 alkyl; R.sup.2 is hydrogen, halo or C.sub.1-4 alkyl; R.sup.3 is hydrogen, halo or C.sub.1-4 alkyl; Y is 0 or S, and --X.sup.1 .dbd.X.sup.2 --is a bivalent radical having the formula --N.dbd.CH--(a-1) or --CH.dbd.N--(a-2);compositions containing the same, and processes of preparing these compounds. It further relates to their use as a medicine, in particular their use as a medicine to treat keratinization disorders.Type: GrantFiled: June 16, 1997Date of Patent: July 13, 1999Assignee: Janssen Pharmaceutica, N.V.Inventors: Marc Gaston Venet, Dominique Jean-Pierre Mabire, Gerard Charles Sanz
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Patent number: 5919788Abstract: The present invention concerns the compounds of formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dashed line designates an optional bond; R.sup.1 and R.sup.2 are each independently hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; R.sup.3 and R.sup.4 are each independently hydrogen, C.sub.1-6 alkyl, phenyl or phenyl substituted with one, two or three substituents selected from halo, hydroxy, nitro, cyano, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, mercapto, amino, mono- and di(C.sub.1-6 alkyl)-amino, carboxyl, C.sub.1-6 alkyloxycarbonyl and C.sub.1-6 alkylcarbonyl; Alk is C.sub.1-4 alkanediyl; D is a pyrimidinone, piperidone or a benzimidozolidinone; having antipsychotic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: June 27, 1997Date of Patent: July 6, 1999Assignee: Janssen Pharmaceutica, N.V.Inventors: Jan Vandenberk, Ludo Edmond Josephine Kennis, Josephus Carolus Mertens
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Patent number: 5904929Abstract: A pharmaceutical composition for trans-mucosal or transdermal administration wherein a per-C.sub.2-18 acylated cyclodextrin is used as a drug reservoir or carrier. The composition can be used safely and exhibits excellent drug release behavior.Type: GrantFiled: July 2, 1997Date of Patent: May 18, 1999Assignee: Janssen Pharmaceutica, N.V.Inventors: Kaneto Uekama, Fumitoshi Hirayama, Akira Kondo, Masaaki Ohta, Yasuhiro Okamoto, Haruo Kunihiro