Patents by Inventor Alfons H. M. Raeymaekers
Alfons H. M. Raeymaekers 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: 6201119Abstract: The compounds are of the class 1,4-benzodiazepines of the formula: An illustrative compound is (S)-6-chloro-2,3,4,5-tetrahydro-3-methyl-4-(3-methyl-2-butenyl)-1H-1,4-benzodiazepin-9-amine. The compounds are useful as intermediates in the preparation of tetrahydroimidazo[1,4]benzodiazepin-2-(thi)ones.Type: GrantFiled: October 17, 1994Date of Patent: March 13, 2001Assignee: Janssen Pharmaceutica N.V.Inventors: Michael Joseph Kukla, Henry Joseph Breslin, Alfons H. M. Raeymaekers, Josephus L. H. Van Gelder, Paul Adriaan Jan Janssen
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Patent number: 5612354Abstract: (1H-azol-1-ylmethyl)substituted quinoline derivatives, compositions containing the same, and methods of treating mammals suffering from disorders which are characterized by an increased proliferation and/or abnormal differentiation of epithelial tissues.Type: GrantFiled: March 23, 1995Date of Patent: March 18, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Gerard C. Sanz, Marc G. Venet, Eddy J. E. Freyne, Alfons H. M. Raeymaekers
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Patent number: 5602134Abstract: The present invention relates to novel positive inotropic and lusitropic compounds of formula ##STR1## the pharmaceutical acceptable acid addition salts thereof and the stereochemically isomeric forms thereof wherein L is a radical of formula --O-Alk-(NH).sub.p -C(.dbd.O)-R.sup.1, pharmaceutical compositions thereof, methods of preparing said compounds and intermediates in the preparation thereof.Type: GrantFiled: November 29, 1995Date of Patent: February 11, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers
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Patent number: 5541325Abstract: The present invention relates to compounds of the formula ##STR1## wherein R represents hydrogen; C.sub.1-6 alkyl; C.sub.3-6 cycloalkyl; phenyl optionally substituted with from 1 to 3 substituents each independently selected from halo, hydroxy, C.sub.1-6 alkyloxy, C.sub.5-6 cycloalkyloxy, C.sub.1-6 alkyl or trifluoromethyl; pyridinyl; or thienyl optionally substituted with halo or C.sub.1-6 alkyl; and.dbd.C.dbd.X is a radical of the formula:.dbd.C.dbd.O (a),.dbd.C.dbd.N--O--R.sup.1 (b), or.dbd.C.dbd.CH--R.sup.2 (c);the addition salts thereof and stereochemically isomeric forms thereof, said compounds being useful as intermediate to potent inhibitors of both phosphodiesterase III and IV, which are useful in the treatment of warm-blooded animals suffering from allergic disorders, atopic diseases and related afflications.Type: GrantFiled: April 18, 1995Date of Patent: July 30, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers, Didier R. G. G. de Chaffoy de Courcelles
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Patent number: 5527915Abstract: The present invention relates to novel 6-aryl-5,6-dihydroimidazo[2,1-b]thiazole derivatives having immunostimulating properties, which are useful for treating humans and warm-blooded animals suffering from disorders and/or diseases wherein the immune system is impaired or suppressed. Processes of preparing said novel compounds and compositions containing the same as active ingredient.Type: GrantFiled: May 13, 1994Date of Patent: June 18, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Alfons H. M. Raeymaekers, Leopold F. C. Roevens, Willy J. C. Van Laerhoven, Jean Pierre F. Van Wauwe
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Patent number: 5521187Abstract: Novel 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives of formula ##STR1## wherein R is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, phenyl optionally substituted with from 1 to 3 substituents each independently selected from halo, hydroxy, C.sub.1-6 alkyloxy, C.sub.5-6 cycloalkyloxy, C.sub.1-6 alkyl or trifluoromethyl; pyridinyl; thienyl optionally substituted with halo or C.sub.1-6 alkyl; and>C.dbd.X is a radical of formula>C.dbd.O (a),>C.dbd.N--O--R.sup.1 (b),or>C.dbd.CH--R.sup.2 (c);the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, said compounds being potent inhibitors of both phosphodiesterase III and IV, which are useful in the treatment of allergic disorders, atopic diseases and related afflictions. Intermediates in the preparation thereof. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.Type: GrantFiled: March 15, 1994Date of Patent: May 28, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers, Didier R. G. G. de Chaffoy de Courcelles
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Patent number: 5516908Abstract: The present invention relates to novel 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives of formula ##STR1## wherein R is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, phenyl optionally substituted with from 1 to 3 substituents each independently selected from halo, hydroxy, C.sub.1-6 alkyloxy, C.sub.5-6 cycloalkyloxy, C.sub.1-6 alkyl or trifiuoromethyl; pyridinyl; thienyl optionally substituted with halo or C.sub.1-6 alkyl; and>C.dbd.X is a radical of formula>C.dbd.O (a),>C.dbd.N--O--R.sup.1 (b),or>C.dbd.CH--R.sup.2 (c);the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, said compounds being potent inhibitors of both phosphodiesterase III and IV, which are useful in the treatment of warm-blooded animals suffering from allergic disorders, atopic diseases and related afflictions. Intermediates in the preparation thereof. Pharmaceutical compositions containing said compounds as an active ingredient.Type: GrantFiled: April 18, 1995Date of Patent: May 14, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers, Didier R. G. G. de Chaffoy de Courcelles
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Patent number: 5500435Abstract: A method for treating skin disorders in warm-blooded animals, said method comprising administering to said warm-blooded animals an effective amount of an appropriately substituted benzimidazole or benzotriazole which suppresses the metabolism of retinoids. Compositions comprising said compounds and an effective amount of a retinoid.Type: GrantFiled: March 23, 1995Date of Patent: March 19, 1996Assignee: Janssen Pharmaceutica, N.V.Inventors: Jean P. F. Van Wauwe, Alfons H. M. Raeymaekers
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Patent number: 5491161Abstract: Pyrroloimidazolyl and imidazopyridinyl substituted 1H-benzimidazole derivatives having the formula ##STR1## wherein n is 0 or 1;R.sup.1 is hydrogen, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, halo, C.sub.1-6 alkyl, hydroxy or C.sub.1-6 alkyloxy;R.sup.2 is hydrogen; C.sub.1-10 alkyl; C.sub.3-6 alkenyl; C.sub.3-6 alkynyl; C.sub.3-7 cycloalkyl; phenyl; substituted phenyl; C.sub.1-4 alkyl substituted with phenyl, substituted phenyl, naphthalenyl, thienyl, furanyl, C.sub.1-4 alkylfuranyl, C.sub.3-7 cycloalkyl; andR.sup.3 is hydrogen; C.sub.1-8 alkyl; C.sub.3-7 cycloalkyl; hydroxy; amino; C.sub.1-6 alkyloxy; C.sub.1-6 alkyloxycarbonylamino; phenyl; C.sub.1-4 alkyl substituted with phenyl, piperazinyl, 4-(C.sub.1-4 alkyl)piperazinyl or morpholinyl;each substituted phenyl independently is phenyl substituted with a substituent independently selected from halo, hydroxy, hydroxymethyl, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.Type: GrantFiled: May 25, 1995Date of Patent: February 13, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Marcel A. C. Janssen, Alfons H. M. Raeymaekers, Eddy J. E. Freyne, Michael N. Greco
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Patent number: 5457102Abstract: Pyrroloimidazolyl and imidazopyridinyl substituted 1H-benzimidazole derivatives having the formula ##STR1## wherein n is 0 or 1;R.sup.1 is hydrogen, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, halo, C.sub.1-6 alkyl, hydroxy or C.sub.1-6 alkyloxy;R.sup.2 is hydrogen; C.sub.1-10 alkyl; C.sub.3-6 alkenyl; C.sub.3-6 alkynyl; C.sub.3-7 cycloalkyl; phenyl; substituted phenyl; C.sub.1-4 alkyl substituted with phenyl, substituted phenyl, naphthalenyl, thienyl, furanyl, C.sub.1-4 alkylfuranyl, C.sub.3-7 cycloalkyl; andR.sup.3 is hydrogen; C.sub.1-8 alkyl; C.sub.3-7 cycloalkyl; hydroxy; amino; C.sub.1-6 alkyloxy; C.sub.1-6 alkyloxycarbonylamino; phenyl; C.sub.1-4 alkyl substituted with phenyl, piperazinyl, 4-(C.sub.1-4 alkyl)piperazinyl or morpholinyl;each substituted phenyl independently is phenyl substituted with a substituent independently selected from halo, hydroxy, hydroxymethyl, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.Type: GrantFiled: July 7, 1994Date of Patent: October 10, 1995Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel A. C. Janssen, Alfons H. M. Raeymaekers, Eddy J. E. Freyne, Michael N. Greco
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Patent number: 5441954Abstract: (1H-azol-1-ylmethyl)substituted quinoline derivatives, compositions containing the same, and methods of treating mammals suffering from disorders which are characterized by an increased proliferation and/or abnormal differentiation of epithelial tissues.Type: GrantFiled: October 5, 1993Date of Patent: August 15, 1995Assignee: Janssen Pharmaceutica N. V.Inventors: Gerard C. Sanz, Marc G. Venet, Eddy J. E. Freyne, Alfons H. M. Raeymaekers
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Patent number: 5420147Abstract: A method for treating skin disorders in warm-blooded animals, said method comprising administering to said warm-blooded animals an effective amount of an appropriately substituted benzimidazole or benzotriazole which suppresses the metabolism of retinoids. Compositions comprising said compounds and an effective amount of a retinoid.Type: GrantFiled: April 26, 1994Date of Patent: May 30, 1995Assignee: Janssen Pharmaceutica N.V.Inventors: Jean P. F. Van Wauwe, Alfons H. M. Raeymaekers
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Patent number: 5371079Abstract: The compounds are of the class of tetrahydroimidazo[1,4]benzodiazepin-2-(thi)ones possessing antiretroviral, especially anti-HIV-1, activity. An illustrative compound is (+)-S-4,5,6,7-tetrahydro-9-chloro-5-methyl-6-(3-methyl-2-butenyl)imidazo[4 ,5,1-jk][1,4]benzodiazepine-2(1H)-thione. These compounds are represented by the formula: ##STR1## The application also discloses compositions containing these compounds as active ingredients and methods of treating subjects suffering from retroviral infections by administering said compounds.Type: GrantFiled: October 5, 1993Date of Patent: December 6, 1994Assignee: Janssen Pharmaceutica N.V.Inventors: Michael J. Kukla, Henry J. Breslin, Alfons H. M. Raeymaekers, Josephus L. H. Van Gelder, Paul A. J. Janssen
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Patent number: 5342957Abstract: A method for treating skin disorders in warm-blooded animals, said method comprising administering to said warm-blooded animals an effective mount of an appropriately substituted benzimidazole or benzotriazole which suppresses the metabolism of retinoids. Compositions comprising said compounds and an effective amount of a retinoid.Type: GrantFiled: August 10, 1992Date of Patent: August 30, 1994Assignee: Janssen Pharmaceutica N.V.Inventors: Jean P. F. Van Wauwe, Alfons H. M. Raeymaekers
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Patent number: 5270464Abstract: Novel tetrahydroimidazo[1,4]benzodiazepin-2-(thi)ones possessing anti-HIV-1 activity, compositions containing these compounds as active ingredients, and methods of treating subjects suffering from HIV-1 infection by administering these compounds.Type: GrantFiled: April 5, 1993Date of Patent: December 14, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Michael J. Kukla, Henry J. Breslin, Alfons H. M. Raeymaekers, Josephus L. H. Van Gelder, Paul A. J. Janssen
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Patent number: 5256681Abstract: [5(6)-(benzisoxa-, benzisothia- or indazol-3-yl)-1H-benzimidazol-2-yl]carbamates of formula (I) wherein R.sup.1 is hydrogen, C.sub.1-4 alkyl, halo, hydroxy or C.sub.1-4 alkyloxy; R.sup.2 is C.sub.1-4 alkyl; and X is O, S, SO, SO.sub.2 or NR.sup.3, said R.sup.3 being hydrogen, C.sub.1-4 alkyl, aryl or arylC.sub.1-4 alkyl. The compounds of formula (I) have anthelminthic properties. Compositions containing said compounds as active ingredient, a method of combating helminths, and a process for preparing said compounds and compositions.Type: GrantFiled: August 27, 1991Date of Patent: October 26, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Alfons H. M. Raeymaekers, Eddy J. E. Freyne, Gustaaf M. Boeckx
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Patent number: 5220023Abstract: The present invention relates to novel positive inotropic and lusitropic 3,5-dihydroimidazo[2,1-b]quinazolin-2(1H)-one derivatives having positive inotropic and lusitropic properties which are useful in the treatment of warm-blooded animals suffering from Congestive Heart Failure. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.Type: GrantFiled: April 10, 1992Date of Patent: June 15, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers
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Patent number: 5212192Abstract: The present invention relates to novel 6-aryl-5,6-dihydroimidazo[2,1-b]thiazole derivatives having immunostimulating properties, which are useful for treating humans and warm-blooded animals suffering from disorders and/or diseases wherein the immune system is impaired or suppressed. Processes of preparing said novel compounds and compositions containing the same as active ingredient.Type: GrantFiled: December 19, 1991Date of Patent: May 18, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Alfons H. M. Raeymaekers, Leopold F. C. Roevens, Willy J. C. Van Laerhoven, Jean P. F. Van Wauwe
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Patent number: 5185346Abstract: (1H-azol-1-ylmethyl)substituted quinoline derivatives, compositions containing the same, and methods of treating mammals suffering from disorders which are characterized by an increase proliferation and/or abnormal differentation of epithelial tissues.Type: GrantFiled: May 23, 1991Date of Patent: February 9, 1993Assignee: Hanssen PharmaceuticaInventors: Gerard C. Sanz, Marc G. Venet, Eddy J. E. Freyne, Alfons H. M. Raeymaekers
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Patent number: 5180832Abstract: Novel [[[(3-pyridinyl)methylen]amino]oxy]alkanoic acids and esters, compositions containing the same, and methods of treating clinical conditions related with the production of thromboxane A.sub.2, prostacyclin and/or prostaglandin s D.sub.2, E.sub.3 and F.sub.2.alpha..Type: GrantFiled: September 17, 1990Date of Patent: January 19, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers, Victor Sipido, Marc G. Venet