Five-membered Hetero Ring Consisting Of One Nitrogen And Four Carbons Patents (Class 544/372)
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Publication number: 20020065308Abstract: This invention is directed to EP4 receptor selective prostaglandin agonists of the Formula I, 1Type: ApplicationFiled: November 21, 2001Publication date: May 30, 2002Inventors: Kimberly O. Cameron, Bruce A. Lefker
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Patent number: 6384035Abstract: This invention relates a to a series of heterocyclic substituted piperazines of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &agr;-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this disease.Type: GrantFiled: October 9, 1998Date of Patent: May 7, 2002Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Richard H. Hutchings, Haripada Khatuya, Gee-Hong Kuo, Xiaobing Li, William V. Murray, Catherine Prouty, Frank Villani, Nelson C. F. Yim, Cynthia Maryanoff
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Patent number: 6372764Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.Type: GrantFiled: March 1, 2000Date of Patent: April 16, 2002Assignee: Merck & Co., Inc.Inventors: Jianming Bao, Robert K. Baker, William H. Parsons, Kathleen Rupprecht
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Patent number: 6369063Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: April 13, 1998Date of Patent: April 9, 2002Assignee: Cor Therapeutics, Inc.Inventors: Ting Su, Bing-Yan Zhu, Robert M. Scarborough
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Patent number: 6355644Abstract: Disclosed are benzylpiperazinyl-indolinylethanone compounds which are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.Type: GrantFiled: June 14, 2000Date of Patent: March 12, 2002Assignee: Neurogen CorporationInventors: He Zhao, Andrew Thurkauf
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Patent number: 6355642Abstract: A compound of formula (I) for use in the treatment or prevention of mental diseases A is N, CH, C having a double bond or CR5; each of B and Z is independently N, CH or CR1, with the proviso that A is N when B and/or Z is N; R1, R2, R3, R4 and R5 and n are as defined in the specification.Type: GrantFiled: December 28, 1998Date of Patent: March 12, 2002Assignee: Meiji Seika Kaisha, Ltd.Inventors: Masao Koyama, Chika Kikuchi, Osamu Ushiroda, Takashi Ando, Hiroshi Nagaso, Kazuyuki Fuji, Masayo Okuno, Toyokazu Hiranuma
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Publication number: 20020028821Abstract: A compound of formula (I) wherein R1 is a group of formula G1, G2, G3, G4 or G5; R2 is hydrogen, (C1 C4 )alkyl, phenyl or naphthyl, wherein said phenyl or naphthyl may optionally be substituted with one or more substituents, preferably from zero to three substituents, independently selected from chloro, fluoro, bromo, iodo, (C1 C6 )alkyl, (C1 C6 )alkoxy, trifluoromethyl, cyano and SO g (C1 C6 )alkyl wherein g is zero, one or two; R3 is (CH2)m B, wherein m is zero, one, two or three and B is hydrogen, phenyl, naphthyl or a 5 or 6membered heteroaryl group containing from one to four hetero atoms in the ring (e.g., furyl, thienyl, pyridyl, pyrimidyl, thiazolyl, pyrazolyl, isothiazolyl, oxazolyl, isoxazolyl, pyrrolyl, triazolyl, tetrazolyl, imidazolyl, etc.), and wherein each of the foregoing aryl and heteroaryl groups may optionally be substituted with one or more substituents, preferably from zero to three substituents, independently selected from chloro.Type: ApplicationFiled: September 24, 1998Publication date: March 7, 2002Inventor: HARRY R. HOWARD
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Publication number: 20020025956Abstract: Disclosed are 1-Azatricyclic-4-benzylpiperazine compounds which are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.Type: ApplicationFiled: June 28, 2001Publication date: February 28, 2002Inventors: Kevin Hodgetts, Stanislaw Rachwal, Daniel Rosewater, Andrew Thurkauf, Xiaoyan Zhang
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Patent number: 6348602Abstract: Novel compounds that are potent and selective inhibitors of PIDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.Type: GrantFiled: November 17, 2000Date of Patent: February 19, 2002Assignee: ICOS CorporationInventors: Kerry W. Fowler, Amy Oliver, Joshua Odingo
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Publication number: 20020002168Abstract: A compound of the formula 1Type: ApplicationFiled: May 22, 2001Publication date: January 3, 2002Inventor: Harry R. Howard
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Patent number: 6331545Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: December 17, 1999Date of Patent: December 18, 2001Inventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
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Patent number: 6323207Abstract: Novel benzoylguanidine derivatives of general formula I useful for the treatment or reduction of tissue damage due to ischaemia.Type: GrantFiled: September 15, 1999Date of Patent: November 27, 2001Assignee: Boehringer Ingelheim Pharma KGInventors: Christian Eickmeier, Erich Buerger, Stefan Matthias Blech, Otto Roos
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Publication number: 20010041705Abstract: A compound of the formula 1Type: ApplicationFiled: May 22, 2001Publication date: November 15, 2001Inventor: Harry R. Howard
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Patent number: 6316617Abstract: This invention encompasses compounds of the formula where X1, X2, and X3, independently represent substituents of formula and the pharmaceutically acceptable salts thereof wherein the remaining variables are as defined herein and wherein said compounds are useful in the diagnosis and treatment of feeding disorders such as obesity and bulimia and cardiovascular diseases such as essential hypertension and congestive heart failure due to the binding of these compounds to human Neuropeptide Y1 receptors.Type: GrantFiled: August 8, 2000Date of Patent: November 13, 2001Assignee: Neurogen CorporationInventors: Charles A. Blum, Robert DeSimone, Alan Hutchison, John M. Peterson
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Patent number: 6316623Abstract: Libraries of ethylenediamine compounds having the general formula (I): wherein R1 to R6, m, n, o and p are as defined herein, are prepared using solid phase combinatorial chemistry techniques. A heterocyclic alcohol is reacted with an ethylenediamine bound to a solid support to give a scaffold having sites of diversity. Libraries of the invention are useful for screening in biological assays in order to identify pharmaceutically useful compounds.Type: GrantFiled: August 21, 1998Date of Patent: November 13, 2001Assignee: ISIS Pharmaceuticals, Inc.Inventors: Eric Edward Swayze, Elizabeth Anne Campbell Jefferson
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Publication number: 20010039280Abstract: The present invention relates to optically active 3-[(2-piperazinylphenyl)methyl]-1-[4-(trifluoromethyl)phenyl]-2-pyrrolidinones and pharmaceutically acceptable salts thereof, to processes for their preparation, to isotopically-labeled analogs thereof, to pharmaceutical compositions comprising them and to their medicinal use as selective antagonists of the 5-HT1D receptor. The compounds of the invention are useful in treating depression, obsessive-compulsive disorder (OCD) and diseases, disorders or conditions for which a 5-HT1D receptor selective antagonist is therapeutically indicated.Type: ApplicationFiled: December 19, 2000Publication date: November 8, 2001Inventors: Harry Ralph Howard, Stephane Caron, Mavis Diane Adam
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Patent number: 6310080Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically inhibiting retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: December 1, 1999Date of Patent: October 30, 2001Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
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Patent number: 6303593Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.Type: GrantFiled: March 1, 2000Date of Patent: October 16, 2001Assignee: Merck & Co., Inc.Inventors: Jianming Bao, Christopher Forbes, Shouwu Miao, William H. Parsons, Kathleen Rupprecht, Frank Kayser
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Patent number: 6303594Abstract: This invention relates to a series of arylsubstituted piperazines, of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &agr;-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.Type: GrantFiled: March 15, 2000Date of Patent: October 16, 2001Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Linda Jolliffe, William Murray, Virginia Pulito, Allan Reitz, Xiaobing Li, Linda Mulcahy, Cynthia Maryanoff, Frank Villani
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Patent number: 6303611Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formula having the structure: wherein R1, R2, and X Y, Z, Ar and n are as described in the specification.Type: GrantFiled: September 9, 1998Date of Patent: October 16, 2001Assignee: Adolor CorporationInventors: Wei Yuan Zhang, Alan L. Maycock, Michael Anthony Marella, Virendra Kumar, Forrest Gaul, An-Chih Chang, Deqi Guo
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Patent number: 6281214Abstract: A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: wherein R1, R2, R3, R4, and R5 are defined in the specification, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis. The compounds exhibit dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism.Type: GrantFiled: October 5, 1998Date of Patent: August 28, 2001Assignee: Eisai Co., LtdInventors: Kozo Akasaka, Masahiro Yonaga, Akiharu Kajiwara, Kunizo Higurashi, Kohshi Ueno, Satoshi Nagato, Makoto Komatsu, Noritaka Kitazawa, Masataka Ueno, Yoshiharu Yamanishi, Yoshimasa Machida, Yuki Komatsu, Naoyuki Shimomura, Norio Minami, Toshikazu Shimizu, Atsushi Nagaoka
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Patent number: 6277852Abstract: A compound of the formula or the pharmaceutically acceptable salt thereof, wherein Z is oxygen, S(O)m wherein m is 0, 1 or 2; or NQ wherein Q is hydrogen, (C1-C6)alkyl or phenyl; X is hydrogen, chloro, fluoro, bromo, iodo, hydroxy, nitro, cyano, (C1-C6)alkyl, trifluoromethyl, (C1-C6)alkoxy, (C1-C6)alkyl S(O)a wherein a is 0, 1 or 2; or phenyl wherein the phenyl group is optionally substituted; Y is wherein M is oxygen or sulfur; X2 is hydrogen, fluoro, chloro, trifluoromethyl, (C1-C6)alkyl, (C1-C6)alkoxy or (C1-C6)alkyl S(O)c wherein c is 0, 1 or 2; R1 is selected from wherein R6 is selected from the group consisting of hydrogen, optionally substituted (C1-C6)alkyl; and wherein R6 in G5 together with R7 form a 2 carbon chain; and R9 and R10 are independently hydrogen or (C1-C6)alkyl; R2 is hydrogen, (C1-C4)alkyl, phenyl or naphthyl, wherein said phenyl or naphthyl may optionally substituted; and R3 is —(CH2)tB, wherein t is 0-3 and B is hydrogType: GrantFiled: April 14, 1999Date of Patent: August 21, 2001Assignee: Pfizer INCInventor: Harry R. Howard
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Publication number: 20010014680Abstract: Compounds of the formula 1Type: ApplicationFiled: March 30, 2001Publication date: August 16, 2001Inventors: Michael G. Kelly, Yvette L. Palmer
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Patent number: 6265380Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.Type: GrantFiled: April 16, 1999Date of Patent: July 24, 2001Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roger D. Tung, Scott L. Harbeson, David D. Deininger, Mark A. Murcko, Govinda R. Bhisetti, Luc J. Farmer
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Patent number: 6265408Abstract: Sulphonamide compounds according to formula (I) or pharmaceutically acceptable salts thereof: wherein: Ar is naphthyl, phenyl or thienyl optionally substituted by one or more substituents selected from the group consisting of C1-6 alkyl optionally substituted by NR7R8, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkylthio, cyano, nitro, halogen, CF3, C2F5, NR7R8, CONR7R8, NR7COR8, S(O)pNR7R8, CHO, OCF3, SCF3, COR9, CH2OR9, CO2R9 or OR9 where p is 1 or 2 and R7, R8 and R9 are independently hydrogen or C1-6 alkyl. R1 and R2 are independently hydrogen or C1-6alkyl or together with the nitrogen atom to which they are attached form a 5- to 7-membered heterocyclic ring optionally substituted by Cl-6alkyl and optionally containing a further heteroatom selected from nitrogen, sulphur or oxygen, the nitrogen atom being substituted by hydrogen, C1-6 alkyl or cycloC3-7alkyl; R3 is hydrogen or C1-6 alkyl; X is oxygen, sulphur or a bond; n is 2 or 3; and m is 1 or 2; are provided.Type: GrantFiled: March 5, 1999Date of Patent: July 24, 2001Assignee: SmithKline Beecham plcInventors: Ian Thomson Forbes, Francis David King, Shirley Katherine Rahman
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Patent number: 6255302Abstract: Compounds of the formula are useful for the treatment of disorder of the central nervous system including anxiety, depression, panic, alcohol and drug addiction, sexual dysfunction, sleep disorders, cognitive disorders, Alzheimer's disease and Parkinson's disease.Type: GrantFiled: December 13, 1999Date of Patent: July 3, 2001Assignee: American Home Products CorporationInventors: Michael G. Kelly, Yvette L. Palmer
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Patent number: 6242438Abstract: The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof. Such compounds and salts are tachykinin antagonists.Type: GrantFiled: June 1, 1998Date of Patent: June 5, 2001Assignee: Pfizer Inc.Inventors: Alexander Roderick MacKenzie, Allan Patrick Marchington, Donald Stuart Middleton, Sandra Dora Meadows
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Patent number: 6232468Abstract: Disclosed are compounds which are neurokinin (tachykinin)-antagonists, useful for the treatment or prevention of inflammatory and allergic disease.Type: GrantFiled: December 1, 1999Date of Patent: May 15, 2001Assignee: Boehringer Ingelheim KGInventors: Franz Esser, Gerd Schnorrenberg, Hans-Peter Ignatow, Günther Giesler, Birgit Jung, Georg Speck
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Patent number: 6218394Abstract: 4-Aryl-1-(indanmethyl, dihydrobenzofuramethyl or dihydrobenzothiophenemethyl) piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I) wherein one of X and Y is CH2, and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9 is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10 and R11 are hydrogen, alkyl or aryl, or R10 and R11 are linked to form a ring; R2 is hydrogen, alkyl, cycloalkyl or cycloalkylalkyl; or R1 and R2 are linked to form a ring; R3-R5 are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6 and R7 are hydrogen or alkyl or they are linked to constitute a 3-7-membered ring; R8 is hydrogen or alkylType: GrantFiled: December 9, 1996Date of Patent: April 17, 2001Assignee: H. Lundbeck A/SInventors: Jens Kristian Perregaard, John Willie Stenberg, Bitten Hansen
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Patent number: 6207665Abstract: This invention is directed to acyl piperazine derivatives of formula (Ia): wherein R1a, R2, R3, R4, R5 and R6 are defined herein, which are useful as anti-inflammatory agents. This invention is also directed to other acyl piperazine derivatives, pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.Type: GrantFiled: June 9, 1998Date of Patent: March 27, 2001Assignee: Schering AktiengesellschaftInventors: John G. Bauman, Brad O. Buckman, Ameen F. Ghannam, Joseph E. Hesselgesser, Richard Horuk, Imadul Islam, Meina Liang, Karen B. May, Sean D. Monahan, Michael M. Morrissey, Howard P. Ng, Guo Ping Wei, Wei Xu, Wei Zheng
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Patent number: 6207825Abstract: A compound represented by the following formula (12) useful as an intermediate for production of drug or agricultural chemical: (wherein R21 to R25 are each independently a hydrogen atom, a hydroxyl group, a halogen atom, an alkyl group of 1 to 4 carbon atoms, an alkoxy group of 1 to 4 carbon atoms, a perfluoroalkyl group of 1 to 4 carbon atoms, a cyano group, a nitro group, an amino group, a carboxyl group, a thiol group, an alkylthio group of 1 to 4 carbon atoms or a carbamoyl group) can be produced by reacting a compound represented by the formula (13): (wherein R21 to R25 have the same definitions as given above) with 1,1-cyclopropanedicarboxylic acid. The compound of the formula (12) is useful as a raw material for production of a pyrrolidinone compound useful as an active ingredient of drug.Type: GrantFiled: November 13, 1998Date of Patent: March 27, 2001Assignee: Mitsui Chemicals, Inc.Inventors: Hajime Iizuka, Hiroshi Nagase, Naruyoshi Mita
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Patent number: 6200986Abstract: The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.Type: GrantFiled: May 12, 1998Date of Patent: March 13, 2001Assignee: SmithKline Beecham CorporationInventors: Pradip Kumar Bhatnagar, Dirk Andries Heerding
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Patent number: 6197750Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.Type: GrantFiled: October 22, 1998Date of Patent: March 6, 2001Assignee: Idun Pharmaceuticals, Inc.Inventors: Donald S. Karanewsky, Robert J. Ternansky
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Patent number: 6194413Abstract: The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.Type: GrantFiled: May 12, 1998Date of Patent: February 27, 2001Assignee: SmithKline Beecham CorporationInventors: Pradip Kumar Bhatnagar, Dirk Andries Heerding
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Patent number: 6169186Abstract: The invention relates to bismaleimides comprising mesogenic groups which consist, corresponding to (I), of two reactive terminal maleimide groups which are linked via linear or singly alkyl-substituted alkylene chains A, which are linked to an aromatic mesogen M via ester, amide or ether groups, wherein A, X, M and R are as defined in the specification. The invention, moreover, relates to oligomeric liquid crystalline bismaleimides of general formula (II) wherein A, X, M and R are as defined above, n represents and integer from 1 to 100 and B represents piperazinyl or a divalent radical which is derived from a primary or secondary para-substituted cyclic diamine, wherein B is bonded via the amino groups of the diamine. The invention also relates to methods of producing said bismaleimides.Type: GrantFiled: December 27, 1999Date of Patent: January 2, 2001Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Masaru Imai, Rainer B. Frings, Gerwald F. Grahe, Joji Kawamura, Naoki Obi
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Patent number: 6166037Abstract: The present invention is directed to pyrrolidine and piperidine compounds of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.4d, R.sup.4e, R.sup.4f, R.sup.4g, R.sup.4h, m, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.Type: GrantFiled: August 27, 1998Date of Patent: December 26, 2000Assignee: Merck & Co., Inc.Inventors: Richard J. Budhu, Edward Holson, Jeffrey J. Hale, Christopher Lynch, Malcolm Maccoss, Scott C. Berk, Sander G. Mills, Christopher A. Willoughby
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Patent number: 6159995Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: December 12, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
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Patent number: 6153611Abstract: Novel non-dopaminergic antiischemic compounds have Formula I: ##STR1## wherein R=R.sub.1 and is independently H, C.sub.1-4 alky C.sub.1-4 alkoxy, C.sub.1-4 trihaloalkyl or halogen, or R and R.sub.1 may be taken together to form an --O(CH.sub.2).sub.m O-- (m=1 or 2);X=a 3-indolyl, phenyl, naphthalenyl or 2-benzothiazolyl residue;n=0, 1, 2 or 3; ##STR2## R.sub.2 =R.sub.3 and is independently H or C.sub.1-4 alkyl; and R.sub.4 =phenyl, 2-thienyl, 2-quinolinyl, 4-pyridinyl or substituted phenyl.Type: GrantFiled: June 25, 1993Date of Patent: November 28, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Ronald J. Mattson, John D. Catt
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Patent number: 6150367Abstract: A chemical compound and composition of Formula 1: ##STR1## wherein Ar represents a phenyl ring substituted by the groups like halo, alkoxy, alkyl or heteroaryl, n=1 or n=2; said compounds and compositions as being useful therapeutic agents for hypertension, ischemic, cardiovascular and other adrenergic receptor related disorders.Type: GrantFiled: October 20, 1997Date of Patent: November 21, 2000Assignee: Council of Scientific & Industrial ResearchInventors: Neelima Sinha, Sanjay Jain, Anil Kumar Saxena, Nitya Anand, Ram Mohan Saxena, Mangal Prasad Dubey, Madhur Ray, Gyanendra K. Patnaik, deceased
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Patent number: 6150527Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains.Type: GrantFiled: February 28, 1997Date of Patent: November 21, 2000Assignee: Ariad Pharmaceuticals, Inc.Inventors: Dennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
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Patent number: 6147212Abstract: The invention relates to new amino acid derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein group B is --A.sup.2 --NR.sup.2 R.sup.3 or R.sup.5, wherein group R.sup.5 is ##STR1## and R.sup.1, A.sup.1, A.sup.2, R.sup.2, R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.9, X, Y, Z, t and u have the meanings described in the specification, as well as the preparation and use thereof. The novel compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: July 8, 1998Date of Patent: November 14, 2000Assignee: Boehringer Ingelheim KGInventors: Franz Esser, Gerd Schnorrenberg, Horst Dollinger, Birgit Jung, Erich Burger
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Patent number: 6133456Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formulaM.sup.1 --L--M.sup.2where M.sup.1 and M.sup.2 are independently moieties of the formula: ##STR1## in which B.sup.1, B.sup.2, B.sup.3, R.sup.1, R.sup.2, n, W, X and Y are as defined.Type: GrantFiled: February 28, 1997Date of Patent: October 17, 2000Assignee: ARIAD Gene Therapeutics, Inc.Inventors: Dennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
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Patent number: 6133268Abstract: The present invention relates to 1,4-disubstituted piperazines of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for the treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.Type: GrantFiled: March 18, 1999Date of Patent: October 17, 2000Assignee: Novo Nordisk A/SInventors: Rolf Hohlweg, Peter Madsen, Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Brett Watson, Zdenek Polivka, Otylie Konigova, Martina Kovandova, Alexandra Silhankova, Vladimir Valenta
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Patent number: 6130101Abstract: The present invention describes xanthene dyes, including rhodamines, rhodols and fluoresceins that are substituted one or more times by a sulfonic acid or a salt of a sulfonic acid. The dyes of the invention, including chemically reactive dyes and dye-conjugates are useful as fluorescent probes, particularly in biological samples.Type: GrantFiled: September 23, 1997Date of Patent: October 10, 2000Assignee: Molecular Probes, Inc.Inventors: Fei Mao, Wai-Yee Leung, Richard P. Haugland
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Patent number: 6130222Abstract: Compounds of the formula (I) ##STR1## as well as their pharmaceutically acceptable salts, and pharmaceutical compositions comprising the novel compounds. The novel compounds of the formula (I) are useful in the management of pain.Type: GrantFiled: April 24, 1997Date of Patent: October 10, 2000Assignee: Astra Pharma Inc.Inventors: Edward Roberts, Niklas Plobeck, Claes Wahlestedt
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Patent number: 6124283Abstract: New piperidinyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula ##STR1## wherein X is N or CH;Y is NR.sub.2 CH.sub.2, CH.sub.2 --NR.sub.2, NR.sub.2 --CO, CO--NR.sub.2 or NR.sub.2 SO.sub.2 ;R.sub.1 is H, C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl;R.sub.3 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or (CH.sub.2).sub.n -aryl,where aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted;n is 0-4;as (R)-enantiomer, (S)-enantiomer or a racemate in the form of the free base or a pharmaceutically acceptable salt or hydrate thereof; a pharmaceutical formulation containing the compounds, use of the compounds in the treatment of 5-hydroxytryptamine mediated disorders, processes for the preparation of the compounds and intermediates for the preparation of the compounds.Type: GrantFiled: April 25, 1997Date of Patent: September 26, 2000Assignee: Astra AktiebolagInventors: Stefan Berg, Lennart Florvall, Svante Ross, Seth-Olov Thorberg
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Patent number: 6124330Abstract: The present invention is concerned with compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen, hydroxy, C.sub.1-6 alkyl or aryl; R.sup.2 is hydrogen; optionally substituted C.sub.1-12 alkyl; C.sub.3-7 cycloalkyl; C.sub.2-8 alkenyl, optionally substituted pyrrolidinyl or aryl; R.sup.3 is hydrogen, optionally substituted C.sub.1-6 alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; ##STR2## is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.Type: GrantFiled: April 29, 1999Date of Patent: September 26, 2000Assignee: Janssen-Cilag S.A.Inventors: Marc Gaston Venet, Dominique Jean-Pierre Mabire, Jean Fernand Armand Lacrampe, Gerard Charles Sanz
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Patent number: 6114335Abstract: The present invention relates to novel benzoylguanidine derivatives, processes for preparing them and their use in the preparation of pharmaceutical compositions.The novel benzoylguanidine derivatives correspond to general formula (I) ##STR1## which benzoylguanidine derivatives are useful in the treatment of ischemia.Type: GrantFiled: September 25, 1998Date of Patent: September 5, 2000Assignee: Boehringer Ingelheim KGInventors: Erich Buerger, Christian Eickmeier, Otto Roos
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Patent number: 6090809Abstract: Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found to exhibit selective .alpha..sub.1A adrenergic activity. The compounds are useful for treatment of disease conditions, such as peripheral vascular disease, congestive heart failure, hypertension and especially benign prostatic hypertrophy.Type: GrantFiled: December 2, 1998Date of Patent: July 18, 2000Assignee: Ranbaxy Laboratories LimitedInventors: Nitya Anand, Neelima Sinha, Sanjay Jain, Anita Mehta, Anil Kumar Saxena
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Patent number: H2007Abstract: Compounds of the following structure are disclosed as effective insecticides: in which: A and B are independently lower alkyl; U is lower alkylidene, lower alkenylidene, or CH—Z, where Z is hydrogen, lower alkyl, lower cycloalkyl, or phenyl; R is phenyl or a dibenzocyclo(C5-8)alkyl, each optionally substituted, or where R3 and R4 are independently selected from phenyl, optionally substituted with, halogen, lower alkyl, lower haloalkyl, lower alkoxy, lower haloalkoxy, lower alkenyl, or phenyl; R1 is selected from a variety of substituents, including 3-R2, where R2 is where D, E, and G are hydrogen, hydroxy, halogen, cyano, hydroxy, lower alkyl, lower haloalkyl, lower alkoxy, nitro, lower haloalkylsuffonyloxy, lower alkylcarboxylato, lower alkylcarbonylamino, lower alkylcarbonyl, lower alkoxycarbonyl, arylcarbonylamino; D and E taken together may form the group —O(CH2)O—; J is hydrogen or lower alkyl; m is 2 or 3, n is 1, 2, or 3; and halogType: GrantFiled: January 9, 1997Date of Patent: December 4, 2001Assignee: FMC CorporationInventors: Ian R. Silverman, Syed F. Ali, Daniel H. Cohen, John W. Lyga, Kirk A. Simmons, Thomas G. Cullen