Five-membered Hetero Ring Having Two Or More Ring Hetero Atoms Of Which At Least One Is Nitrogen Patents (Class 544/366)
  • Patent number: 6271235
    Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 7, 2001
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Bruce A. Dressman, James E. Fritz, Stephen W. Kaldor, Vincent J. Kalish, Siegfried Heinz Reich, Michael J. Rodriguez, Timothy A. Shepherd, John H. Tatlock, Louis Nickolaus Jungheim
  • Patent number: 6262052
    Abstract: The present invention concerns novel compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts thereof and stereochemically isomeric forms thereof, wherein —A—B— forms a bivalent radical of formula —N═CH— (a), —CH═N— (b), —CH═CH— (c), L represents the acyl moiety of an amino acid; D is an azole containing 1,3- or 1,4-dioxolane derivative as broad-spectrum antifungals; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: July 26, 1999
    Date of Patent: July 17, 2001
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Lieven Meerpoel, Jan Heeres, Robert Jozef Maria Hendrickx
  • Patent number: 6251907
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 17, 1999
    Date of Patent: June 26, 2001
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 6245915
    Abstract: Asymmetrical bis benzotriazoles of the formula I where G2′ is perfluoroalkyl of 1 to 12 carbon atoms, preferably CF3, and where G2 does not contain said group are red-shifted and due to the asymmetry are particularly soluble and useful in a host of applications including automotive coatings, thermoplastics and especially in adhesive compositions, themselves useful in solar panels and other laminate structures.
    Type: Grant
    Filed: April 17, 2000
    Date of Patent: June 12, 2001
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Mervin Wood, Jacqueline Lau, Ramanathan Ravichandran
  • Patent number: 6207829
    Abstract: A process is provided for the preparation of a compound of formulae (IA) (sidenafil) and (IB) comprising reacting a compound of formula (IIA) and (IIB) respectively in the presence of —OR, wherein R in the case of formation of compound (IA) is CH2CH3 and R in the case of formation of compound (IB) is CH2CH2CH3, where X is a leaving group:
    Type: Grant
    Filed: October 8, 1999
    Date of Patent: March 27, 2001
    Assignee: Pfizer Inc.
    Inventors: Peter James Dunn, Philip Charles Levett
  • Patent number: 6207665
    Abstract: 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: Grant
    Filed: June 9, 1998
    Date of Patent: March 27, 2001
    Assignee: Schering Aktiengesellschaft
    Inventors: 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
  • Patent number: 6200977
    Abstract: Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.
    Type: Grant
    Filed: February 12, 1999
    Date of Patent: March 13, 2001
    Assignee: Tularik Inc.
    Inventors: Timothy D. Cushing, Heather L. Mellon, Juan C. Jaen, John A. Flygare, Shi-Chang Miao, Xiaoqi Chen, Jay P. Powers
  • Patent number: 6200986
    Abstract: 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: Grant
    Filed: May 12, 1998
    Date of Patent: March 13, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Pradip Kumar Bhatnagar, Dirk Andries Heerding
  • Patent number: 6200978
    Abstract: Compounds of the formula (I)—shown below—are described. The compounds are useful in the manufacture of a pharmaceutical composition for preventing or treating inflammatory diseases such as arthritis, psoriasis, asthma, or inflammatory bowel disease, disorders of respiratory function, gastrointestinal disorders such as functional bowel disease, functional GI disorders such as irritable bowel syndrome, functional diarrhoea, functional distension, functional pain, non-ulcerogenic dyspepsia or others associated with disorders of motility or secretion, urogenital tract disorders such as incontinence, as analgesics for treating pain including non-somatic pain, or as immunosuppressants to prevent rejection in organ transplant and skin graft.
    Type: Grant
    Filed: March 3, 1999
    Date of Patent: March 13, 2001
    Assignee: Pfizer Inc.
    Inventors: Graham Nigel Maw, Donald Stuart Middleton
  • Patent number: 6194413
    Abstract: 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: Grant
    Filed: May 12, 1998
    Date of Patent: February 27, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Pradip Kumar Bhatnagar, Dirk Andries Heerding
  • Patent number: 6187774
    Abstract: The present invention relates to a fused heterocyclic compound of the formula (I) wherein each symbol is as defined in the specification, an optical isomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing a compound of the formula (I), an optical isomer thereof or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable additive, and a medicament containing a compound of the formula (I), an optical isomer thereof or a pharmaceutically acceptable salt thereof. The compound of the present invention is a useful antipsychotic agent effective not only for positive symptoms centering on hallucination and delusion characteristic of the acute stage of schizophrenia, but also negative symptoms of apathy, abulia and autism.
    Type: Grant
    Filed: September 3, 1998
    Date of Patent: February 13, 2001
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Hiroshi Tanaka, Takanobu Kuroita, Yoshifumi Togo, Seigo Ishibuchi, Masakazu Fujio, Takashi Futamura
  • Patent number: 6174883
    Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives of the formula and the phamaceutically-accepted salts thereof which are inhibitors of prostaglandin H2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 16, 2001
    Assignee: Pfizer Inc.
    Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
  • Patent number: 6172222
    Abstract: This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula wherein: R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R1 and R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl; R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2; n is 0 or 1; R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons; and all crystalline forms and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: June 7, 1999
    Date of Patent: January 9, 2001
    Assignee: American Home Products Corporation
    Inventors: Adam Matthew Gilbert, Zhen-jia Chen
  • Patent number: 6166020
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.4, R.sup.23, R.sup.24, R.sup.25 and R.sup.26 are defined as in the specification.These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and antagonists.
    Type: Grant
    Filed: April 20, 1999
    Date of Patent: December 26, 2000
    Assignee: Pfizer Inc.
    Inventors: Harry R. Howard, Jr., Bertrand L. Chenard, John E. Macor, Kevin D. Shenk, Kishor A. Desai
  • Patent number: 6166218
    Abstract: Benzotriazole UV absorbers which are substituted at the 5-position of the benzo ring by an electron withdrawing group exhibit enhanced durability and very low loss rates when incorporated into automotive coatings. This is particularly the case when the 3-position of the phenyl ring is also substituted by phenyl or phenylalkyl such as .alpha.-cumyl. Compounds where the 5-position of the benzo ring are substituted by perfluoroalkyl such as trifluoromethyl are particularly of interest for both their enhanced durability and for their excellent solubility and excellent color properties in some thermoplastic compositions when the phenyl ring is substituted at the 3-position by hydrogen or tert-alkyl.
    Type: Grant
    Filed: January 21, 1999
    Date of Patent: December 26, 2000
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Ramanathan Ravichandran, Joseph Suhadolnik, Mervin G. Wood, Anthony Debellis, Robert E. Detlefsen, Revathi Iyengar, Jean-Pierre Wolf
  • Patent number: 6153616
    Abstract: A compound of formula I, or an optical isomer or pharmaceutically acceptable salt thereof, ##STR1## is disclosed as well as a pharmaceutical composition and a method of treating or preventing a fungal infection using the compound.
    Type: Grant
    Filed: January 16, 1998
    Date of Patent: November 28, 2000
    Assignees: Synphar Laboratories, Inc., Taiho Pharmaceuticals Co., Ltd.
    Inventors: Mohsen Daneshtalab, Yadagiri Bathini, Dai Nguyen, Inderjit Sidhu, Mark Abel, Chan Ha, Sameeh Salama, Jehangir Khan, Ronald Micetich, Tetsuo Furukawa, Norio Unemi
  • Patent number: 6130217
    Abstract: This invention relates to certain heterocyclic compounds and their pharmaceutically acceptable salts, which are useful for sensitizing multidrug-resistant tumor cells to anticancer agents and multidrug resistant forms of malaria, tuberculosis, leishmania and amoebic dysentery to chemotherapeutants. The compounds and their pharmaceutically acceptable salts are also inhibitors of the active drug transport capability of P-glycoprotein which is encoded by the human MDR1 gene, as well as of certain other related ATP-binding-cassette transporters from eukaryotic and prokaryotic organisms (e.g., pfmdr from Plasmodium falciprum, and murine mdr1 and mdr3 gene products).
    Type: Grant
    Filed: September 20, 1995
    Date of Patent: October 10, 2000
    Assignee: Pfizer Inc
    Inventors: Lee Daniel Arnold, Jotham Wadsworth Coe, Takushi Kaneko, Mikel Paul Moyer
  • Patent number: 6071928
    Abstract: The present invention relates to compounds of formula (I), wherein R is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, which groups are optionally substituted by hydroxy, C.sub.1-4 alkoxy or NR.sup.a R.sup.b, where R.sup.a and R.sup.b each independently repesent hydrogen or C.sub.1-4 alkyl; or R is C.sub.1-4 alkyl substituted by Ar, and optionally further substituted by one or both of R.sup.4 and R.sup.5 ; R.sup.1, R.sup.2 and R.sup.3 represent a variety of substituents; R.sup.9 and R.sup.10 are each hydrogen, halogen, C.sub.1-6 alkyl, CH.sub.2 OR.sup.c, oxo, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b where R.sup.c represents hydrogen, C.sub.1-6 alkyl or phenyl; X is --CH.sub.2, or --CH.sub.2 CH.sub.2 --; Y is --CH--, --CH.sub.2 --, --CH.sub.2 CH-- or --CH.sub.2 CH.sub.2 --, with the proviso that the sum total of carbon atoms in X+Y is 2 or 3; and when Y is --CH-- or --CH.sub.
    Type: Grant
    Filed: December 16, 1998
    Date of Patent: June 6, 2000
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventors: Neil Roy Curtis, Ian Thomas Huscroft, Janusz Jozef Kulagowski, Christopher John Swain
  • Patent number: 6054456
    Abstract: The present invention provides a compound of formula I, or a pharmaceutically acceptable salt thereof: ##STR1## wherein Z, E, Q, T, U, V and L are as defined herein; processes for its preparation and its use in the treatment of conditions for which the administration of an agonist selective for the 5-HT.sub.1D.alpha. receptor subtype is indicated, such as migraine.
    Type: Grant
    Filed: May 26, 1998
    Date of Patent: April 25, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Tamara Ladduwahetty, Angus Murray MacLeod, Michael Rowley
  • Patent number: 6043245
    Abstract: A compound of the formula I ##STR1## wherein G is H or PO.sub.3 H.sub.2 or a pharmaceutical acceptable salt thereof, pharmaceutical compositions containing such compounds and method of using such compounds or pharmaceutical compositions containing them to treat or prevent fungal infection are disclosed.
    Type: Grant
    Filed: September 25, 1998
    Date of Patent: March 28, 2000
    Assignee: Schering Corporation
    Inventors: Frank Bennett, Viyyoor M. Girijavallabhan, Naginbhai M. Patel, Anil K. Saksena, Ashit Ganguly
  • Patent number: 6040455
    Abstract: 5-Sulfonyl substituted benzotriazole UV absorbers are prepared from the corresponding 5-chlorobenzotriazole in a two step, but one-pot process where the second step involves the oxidation of the non-isolated 5-thio substituted benzotriazole using sodium tungstate, hydrogen peroxide and formic acid. The 5-sulfonyl substituted benzotriazoles exhibit enhanced absorption in the near-visible range (over 350 nm) thus providing effective protection to substrates in this critical area of the spectrum.
    Type: Grant
    Filed: January 21, 1999
    Date of Patent: March 21, 2000
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Mervin G. Wood, William Wiggins, Catherine Blake, Albert Carpenter, Wha Chen
  • Patent number: 6034085
    Abstract: The crystalline, stable methanesulfonate salt of nefazodone showed significantly higher intrinsic dissolution in water and THAM buffer (pH 7.5) compared to other salts of nefazodone. The faster dissolution rate of this salt at neutral pH suggests better dissolution and absorption in the intestine, allowing controlled release of nefazodone for oral formulations.
    Type: Grant
    Filed: September 29, 1998
    Date of Patent: March 7, 2000
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Hemant N. Joshi, Terry D. Wilson, Jatin M. Patel
  • Patent number: 6020336
    Abstract: Compound of formula (I): ##STR1## wherein: n is 0 or 1,A represents a .sigma. bond or alkylene or alkenylene,X represents nitrogen or C--R.sub.2,R.sub.1 represents hydrogen or alkyl, andG.sub.1 represents any one of the groups defined in the description and medicaments containing the same.
    Type: Grant
    Filed: September 2, 1998
    Date of Patent: February 1, 2000
    Inventors: Gilbert Lavielle, Olivier Muller, Christine Vayssettes-Courchay, Jean-Jacques Descombes, Tony Verbeuren
  • Patent number: 6004963
    Abstract: A substituted 2,4-imidazolidinedione compound corresponding to the formula I ##STR1## a process for production thereof and the use of these compounds in a pharmaceutical preparation are described. Substituents R1, R2, R3 and R4 have the same meaning as defined in the specification.
    Type: Grant
    Filed: October 25, 1996
    Date of Patent: December 21, 1999
    Assignee: Gruenenthal GmbH
    Inventors: Oswald Zimmer, Hoerst Boehlke, Stephan Wnendt, Cornelia Geist, Kai Zwingenberger
  • Patent number: 6001834
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: December 14, 1999
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau
  • Patent number: 6002005
    Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof;useful for treating disorders of the central nervous system.
    Type: Grant
    Filed: May 4, 1998
    Date of Patent: December 14, 1999
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Jan W.F. Wasley
  • Patent number: 5998415
    Abstract: A class of piperazinones, homopiperazinones and thione analogues thereof, substituted at the 1-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, and linked at the 4-position via an alkylene spacer to a fused bicyclic heteroaromatic moiety, typically indolyl, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
    Type: Grant
    Filed: April 17, 1998
    Date of Patent: December 7, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Mark Stuart Chambers, Sarah Christine Hobbs, Leslie Joseph Street
  • Patent number: 5981529
    Abstract: A class of 1-[3-(1H-indol-3-yl)propyl]-4-(2-phenylethyl)piperazine derivatives, substituted at the 5-position of the indole nucleus by a five-membered heteroaromatic moiety, on one or other of the ethylene carbon atoms of the phenethyl moiety by halogen, trifluoromethyl, alkyl, hydroxyalkyl or alkoxyalkyl, and optionally on the phenyl ring of the phenethyl moiety by halogen, trifluoromethyl, alkoxy or an oxazolidinone group and optionally by one or two further substituents, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D .alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D .alpha. receptor subtype relative to the 5-HT.sub.1D .beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.
    Type: Grant
    Filed: March 18, 1998
    Date of Patent: November 9, 1999
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Raymond Baker, Mark Stuart Chambers, Sarah Christine Hobbs, Angus Murray MacLeod, Austin John Reeve, Francine Sternfeld, Leslie Joseph Street
  • Patent number: 5981520
    Abstract: The invention relates to compounds of the formula ##STR1## These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
    Type: Grant
    Filed: June 17, 1998
    Date of Patent: November 9, 1999
    Assignee: Schering Corporation
    Inventors: Ho-Jane Shue, Neng-Yang Shih, David J. Blythin, Xiao Chen, Wing C. Tom, John J. Piwinski, Kevin D. McCormick
  • Patent number: 5977113
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 2, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: 5977154
    Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity.
    Type: Grant
    Filed: June 26, 1997
    Date of Patent: November 2, 1999
    Assignee: Eli Lilly and Company
    Inventors: Michael Gregory Bell, Christine Ann Droste, Cynthia Darshini Jesudason, Christopher John Rito, Anthony John Shuker, Mark Alan Winter
  • Patent number: 5977116
    Abstract: A class of N-substituted piperazine, piperidine and tetrahydropyridine derivatives, linked by a fluoro-substituted alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 4-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D recptor agonists.
    Type: Grant
    Filed: May 12, 1998
    Date of Patent: November 2, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Angus Murray MacLeod, Michael Rowley, Monique Bodil Van Niel
  • Patent number: 5977112
    Abstract: Benzofurans of the formula I ##STR1## and their salts in which R.sup.1, R.sup.2 and X have the meanings indicated in claim 1, are suitable as intermediates in the synthesis of medicaments and show effects on the central nervous system.
    Type: Grant
    Filed: October 29, 1997
    Date of Patent: November 2, 1999
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Andreas Bathe, Bernd Helfert, Henning Bottcher, Kurt Schuster
  • Patent number: 5977115
    Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
    Type: Grant
    Filed: December 4, 1997
    Date of Patent: November 2, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Michael A. Patane, Mark G. Bock, Roger M. Freidinger, Rose Ann Ponticello, Randall C. Newton
  • Patent number: 5977359
    Abstract: The invention relates to compounds of the formula ##STR1## in which: A is a divalent radical selected from:A.sub.1) --O--CO--A.sub.2) --CH.sub.2 --O--CO--A.sub.3) --O--CH.sub.2 --CO--A.sub.4) --O--CH.sub.2 --CH.sub.2 --A.sub.5) --N(R.sub.1)--CO--A.sub.6) --N(R.sub.1)--CO--CO--A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 --A.sub.8) --O--CH.sub.2 --in which:R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; andAm is a nitrogen-containing heterocycle.
    Type: Grant
    Filed: October 20, 1998
    Date of Patent: November 2, 1999
    Assignee: Sanofi
    Inventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
  • Patent number: 5968933
    Abstract: The invention relates to novel bis-benzimidazole compounds which have the ability to bind to the minor groove of DNA and to alkylate DNA, to methods of preparing the compounds, and the use of the compounds in the treatement of neoplastic disease.
    Type: Grant
    Filed: February 19, 1997
    Date of Patent: October 19, 1999
    Assignees: Auckland Division Cancer Society of New Zealand Inc., Circadian Pharmaceuticals (Australia) Pty. Ltd.
    Inventors: William A. Denny, Jeffrey B. Smaill
  • Patent number: 5968938
    Abstract: This invention relates to certain novel piperazine compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor in mammals, especially humans. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery.
    Type: Grant
    Filed: May 29, 1998
    Date of Patent: October 19, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Peter D. Williams, Michelle A. Sparks, Ian Bell, James P. Guare, Jr., Roger M. Freidinger
  • Patent number: 5962686
    Abstract: N-Benzylazolium derivatives of the general formula (I), ##STR1## wherein Q is the remainder of an azole compound of the formula II ##STR2## possessing antifungal activity; Z is nitrogen or methine;R.sup.1 and R.sup.2 are each independently a hydrogen atom or a group --OY ?in which Y is a group easily hydrolyzable under physiological condition!;R.sup.3 and R.sup.4 are each independently a hydrogen or halogen atom, lower alkyl, lower alkoxy, lower alkylthio, (lower alkylcarbonyl)thiomethyl, carboxy or methoxycarbonyl; andX.sup.- is a pharmaceutically acceptable anion,as well as salts, hydrates or solvates of the compounds of the general formula (I) have antiftngal properties.
    Type: Grant
    Filed: January 8, 1999
    Date of Patent: October 5, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Shigeyasu Ichihara, Chikako Murasaki, Noriko Ohga, Jun Ohwada, Daisuke Sawada, Nobuo Shimma, Michio Shirai, Isao Umeda
  • Patent number: 5959113
    Abstract: This invention relates to novel imidazole derivatives of formula a ##STR1## and pharmaceutically acceptable salts of these compounds, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.5, R.sup.7 and R.sup.8 are as disclosed herein. These compounds are protein kinase inhibitors useful in the treatment of atherosclerosis, psoriasis, alopecia, and tumors.
    Type: Grant
    Filed: June 12, 1997
    Date of Patent: September 28, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Charles Stanford Harmon, Markus Kamber, Anna Krasso, Wolfgang Pirson, Pierre-Charles Wyss
  • Patent number: 5942532
    Abstract: The invention relates to benzimidazole antibacterial compounds of the Formula I: ##STR1## as described herein, pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.
    Type: Grant
    Filed: September 5, 1997
    Date of Patent: August 24, 1999
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Kwasi Adomako Ohemeng, Van Nhatton Nguyen
  • Patent number: 5925638
    Abstract: A class of 1-?3-(1H-indol-3-yl)propyl!-4-benzylpiperazine derivatives of formula I, substituted at the 5-position of the indole nucleus by a 1,2,4-triazol-4-yl moiety, and on the methylene linkage of the benzyl moiety by a range of substituted alkyl groups, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
    Type: Grant
    Filed: April 28, 1998
    Date of Patent: July 20, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Mark Stuart Chambers, Sarah Christine Hobbs, Leslie Joseph Street
  • Patent number: 5922718
    Abstract: The present invention concerns novel compounds of formula (I). ##STR1## wherein R.sup.1 is C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl or C.sub.1-6 alkyl substituted with C.sub.3-7 cycloalkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; Alk represents C.sub.1-3 alkanediyl; --A-- represents a bivalent radical of formula --CH.dbd.CH--N.dbd.CH-- (a), --N.dbd.CH--N.dbd.CH-- (b), --CH.dbd.N--N.dbd.CH-- (c), --CH.dbd.CH--CH.dbd.N-- (d); in said bivalent radicals a hydrogen atom may be replaced by C.sub.1-6 alkyl; and Ar is unsubstituted phenyl; phenyl substituted with up to two substituents selected from halo, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; unsubstituted naphthyl; or naphthyl substituted with up to two substituents selected from halo, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: October 7, 1997
    Date of Patent: July 13, 1999
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jan Heeres, Leo Jacobus Josef Backx, Paul August Clement Luyts, Didier Robert Guy Gabriel de Chaffoy de Courcelles
  • Patent number: 5919783
    Abstract: Compounds of formula (I), or a salt or prodrug thereof, wherein Z represents an optionally substituted five-membered heteroaromatic ring selected from furan, thiophene, pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole, and tetrazole; E represents a chemical bond or a straight or branched alkylene chain containing from 1-4 carbon atoms; Q represents a straight or branched alkylene chain containing from 1-6 carbon atoms; T represents nitrogen or CH; R.sup.1 represents aryl(C.sub.1-6)alkyl or heteroaryl(C.sub.1-6)alkyl, either of which groups may be optionally substituted; and R.sup.2 represents hydrogen or C.sub.1-6 alkyl are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta.
    Type: Grant
    Filed: January 21, 1997
    Date of Patent: July 6, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Mark Stuart Chambers, Victor Giulio Matassa, Leslie Joseph Street
  • Patent number: 5919785
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: March 25, 1997
    Date of Patent: July 6, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, Theresa M. Williams, Jeffrey Bergman
  • Patent number: 5916889
    Abstract: 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 antagonizing peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.
    Type: Grant
    Filed: October 3, 1997
    Date of Patent: June 29, 1999
    Assignee: Novo Nordisk A/S
    Inventors: 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
  • Patent number: 5900486
    Abstract: N-Benzylazolium derivatives of the general formula (I), ##STR1## wherein Q is the remainder of an azole compound of the formula II ##STR2## possessing antifungal activity; Z is nitrogen or methine;R.sup.1 and R.sup.2 are each independently a hydrogen atom or a group --OY ?in which Y is a group easily hydrolyzable under physiological condition!;R.sup.3 and R.sup.4 are each independently a hydrogen or halogen atom, lower alkyl, lower alkoxy, lower alkylthio, (lower alkylcarbonyl)thiomethyl, carboxy or methoxycarbonyl; andX.sup.- is a pharmaceutically acceptable anion,as well as salts, hydrates or solvates of the compounds of the general formula (I) have antifungal properties.
    Type: Grant
    Filed: September 9, 1997
    Date of Patent: May 4, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Shigeyasu Ichihara, Chikako Murasaki, Noriko Ohga, Jun Ohwada, Daisuke Sawada, Nobuo Shimma, Michio Shirai, Isao Umeda
  • Patent number: 5900485
    Abstract: Process for the manufacture of triazolone compounds and in particular nefazodone and intermediates useful in the manufacture thereof.
    Type: Grant
    Filed: October 15, 1997
    Date of Patent: May 4, 1999
    Assignee: Apotex, Inc.
    Inventors: Bo Lei, Tim Fat Tam, Khashayar Karimian, Rudolf Kubela
  • Patent number: 5889008
    Abstract: A class of 1-?3-(1H-indol-3-yl)propyl!-4-(2-phenylethyl) piperazine derivatives, substituted at the 5-position of the indole nucleus by a five-membered heteroaromatic moiety, and on the phenyl ring of the phenethyl moiety by fluoro, chloro, trifluoromethyl, alkoxy or an oxazolidinone group and optionally by one or two further substituents, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D .alpha. receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT.sub.1D .alpha. receptor subtype relative to the 5-HT.sub.1D .alpha. subtype; they are therefore usefull in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
    Type: Grant
    Filed: February 5, 1998
    Date of Patent: March 30, 1999
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventors: Richard Alexander Jelley, Angus Murray MacLeod, Austin John Reeve, Francine Sternfeld, Leslie Joseph Street
  • Patent number: 5889004
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: March 30, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Patent number: RE37029
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: November 5, 1998
    Date of Patent: January 23, 2001
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegler