Polycyclo Ring System Having A 1,2-diazine Ring As One Of The Cyclos Patents (Class 544/233)
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Patent number: 6559306Abstract: This invention relates to new fluorescent or non-fluorescent dye compounds having a terminal hydroxy, carboxylic acid/ester or amino group and a process for their preparation. The new fluorescent or non-fluorescent dye compounds are useful as colorants for preparing colored synthetic polymer resins with pigmentary properties, for dyeing or printing homo- or mixed synthetic, semi-synthetic or natural polymers or substrates or for preparing inks. The dye compounds provide excellent properties, especially high temperature stability and easy applicability.Type: GrantFiled: July 13, 2001Date of Patent: May 6, 2003Assignee: Clariant Finance (BVI) LimitedInventors: Bansi Lal Kaul, Jean-Christophe Graciet
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Patent number: 6552021Abstract: A compound which is a heteroaromatic[a]phenazine carboxamide derivative of formula (I) wherein X is a five- or six-membered heteroaromatic ring which contains one or two nitrogen atoms and which is unsubstituted or substituted by C1-C6 alkyl, hydroxyl or C1-C6 alkoxy; Q is C1-C6 alkylene which is unsubstituted or substituted by C1-C6 alkyl which is unsubstituted or substituted by a hydroxy group; and R1 and R2 which are the same or different are each C1-C6 alkyl; or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of topoisomerase I and II and can be used to treat tumours, including tumours which express MDR.Type: GrantFiled: March 5, 2001Date of Patent: April 22, 2003Assignee: Xenova LimitedInventors: John Milton, Nigel Vicker, William Alexander Denny, Swarnalatha Akuratiya Gamage, Julie Ann Spicer
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Publication number: 20030073691Abstract: Novel polycyclic compounds of the formula [I], 1Type: ApplicationFiled: September 25, 2002Publication date: April 17, 2003Inventors: Tsunehisa Aoyama, Kenichi Kawasaki, Miyako Masubuchi, Tatsuo Ohtsuka, Kiyoaki Sakata
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Publication number: 20030054198Abstract: An organic EL device includes a luminescence layer containing, as a luminescent material allowing a high-luminescence and high-efficiency luminescence for a long period of time, a metal coordination compound represented by the following formula (1): LmML′n, wherein M denotes Ir, Pt, Ph or Pd; L denotes a bidentate ligand; L′ denotes a bidentate ligand different from L; m is an integer of 1, 2 or 3; and n is an integer of 0, 1 or 2 with the proviso that the sum of m and n is 2 or 3.Type: ApplicationFiled: November 29, 2001Publication date: March 20, 2003Inventors: Akira Tsuboyama, Hidemasa Mizutani, Shinjiro Okada, Takao Takiguchi, Seishi Miura, Koji Noguchi, Takashi Moriyama, Satoshi Igawa, Jun Kamatani, Manabu Furugori
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Publication number: 20030023085Abstract: Compounds, compositions and methods are provided that are useful in the treatment and/or prevention of a condition or disorder mediated by a G-protein coupled receptor. In particular, the compounds of the invention are useful in the treatment and/or prevention of eating disorders, obesity, anxiety disorders and mood disorders.Type: ApplicationFiled: May 3, 2002Publication date: January 30, 2003Applicant: Tularik Inc.Inventors: Xiaoqi Chen, Kang Dai, Pingchen Fan, Shugui Huang, Leping Li, Jeffrey Thomas Mihalic
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Patent number: 6491749Abstract: The present inventions relates to nucleus-extended perylenebisimides of formula (I) intermediates in the preparation of compounds (I) and processes for the preparation of those intermediates and also processes for the preparation of compounds, (I), and the use thereof as colorants.Type: GrantFiled: March 20, 2001Date of Patent: December 10, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: Heinz Langhals, Susanne Kirner, Patrick Blanke, Markus Speckbacher
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Patent number: 6486167Abstract: The present invention provides compounds of formula I: wherein the R substituents and atoms X and Y are as defined in specification. The present invention also provides pharmaceutical compositions and methods of inhibiting cancer cell growth.Type: GrantFiled: September 29, 2000Date of Patent: November 26, 2002Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. La Voie, Darshan B. Makhey, Baoping Zhao, Leroy Fong Liu
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Patent number: 6469021Abstract: Non-peptide compounds that act as antagonists of the intestinal hormone glucagons-like peptide 1 (GLP-1) have a 9H-b-carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding to the GLP-1 receptor and/or prevent activation of the receptor by bound GLP-1. The invention further relates to a method of inhibiting the binding of GLP-1 to the GLP-1 receptor and a method of inhibiting the activation of the GLP-1 receptor. Intermediate compounds useful for making non-peptide GLP-1 receptor antagonists are also described.Type: GrantFiled: October 26, 2001Date of Patent: October 22, 2002Assignee: Agouron Pharmaceuticals, Inc.Inventors: Larry Kenneth Truesdale, Richard A. Bychowski, Javier Gonzalez, Atsuo Kuki, Ranjan Jagath Rajapakse, Min Teng, Dan Kiel, Daljit S. Dhanoa, Yufeng Hong, Tso-sheng Chou, Anthony L. Ling, Michael David Johnson, Vlad Edward Gregor
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Patent number: 6440968Abstract: The maduraphthalazine derivatives of the formula (4) are able to inhibit the effect of the cytokines interleukin-2, interleukin-4 and interleukin-5 and are suitable for the production of pharmaceuticals.Type: GrantFiled: April 13, 2000Date of Patent: August 27, 2002Assignee: Elbion G.m.b.H.Inventors: Regina Draheim, Thomas Kronbach, Lothar Heinisch, Ernst Roemer, Norbert Höfgen, Hildegard Poppe, Peter Jütten, Wolfgang Haas, Walter Werner, Udo Gräfe
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Patent number: 6429311Abstract: The present invention is directed to certain N-amino- and N-hydroxy-quinazolinone compounds and synthetic methods for synthesis thereof, which compounds may find use in combinatorial libraries. More specifically, the invention is directed to the synthesis of 3-hydroxy- and 3-amino-4 (1H)-quinazolinones via the reaction of an appropriate 2-aminobenzamide compound with a carboxylic acid or acyl halide at ambient temperature performed on a solid support or in solution.Type: GrantFiled: February 1, 2001Date of Patent: August 6, 2002Assignee: Sepracor Inc.Inventor: Yun Gao
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Patent number: 6426346Abstract: The present application describes 6-membered aromatics of formula I: or pharmaceutically acceptable salt forms thereof, wherein D may be CH2NH2 or C(═NH)NH2, which are useful as inhibitors of factor Xa.Type: GrantFiled: February 15, 2000Date of Patent: July 30, 2002Assignee: Bristol - Myers Squibb Pharma CompanyInventors: James Russell Pruitt, Donald Joseph Phillip Pinto, Mimi Lifen Ouan, Ruth Richmond Wexler
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Patent number: 6380193Abstract: A compound of formula I: or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof.Type: GrantFiled: September 1, 1998Date of Patent: April 30, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Jia-He Li, Jie Zhang
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Patent number: 6376428Abstract: The dihalopropene compounds of the general formula [I] have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.Type: GrantFiled: May 25, 2001Date of Patent: April 23, 2002Assignee: Sumitomo Chemical Company, LimitedInventors: Noriyasu Sakamoto, Sanshiro Matsuo, Masaya Suzuki, Taro Hirose, Kazunori Tsushima, Kimitoshi Umeda
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Patent number: 6359111Abstract: A compound comprising a ligand portion which has binding affinity for an opioid receptor, and a therapeutically or diagnostically effective group selected from radionuclide chelating agents, fluorochromes, toxins, drugs, polyboron moieties, proteins, biological response modifiers, chemical moieties capable of binding to other molecules of interest, and radioisotopes selected from therapeutically effective alpha and beta emitters, and diagnostically effective gamma emitters. The compound may be used in a method of treating cancer, and in a method of imaging opioid receptors either inside or outside of the central nervous system.Type: GrantFiled: May 27, 1999Date of Patent: March 19, 2002Assignee: NeoRx CorporationInventors: Damon L. Meyer, Sudhakar Kasina
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Patent number: 6339092Abstract: A compound selected from those of the formula (I): wherein: R1 represents hydrogen or halogen, or alkyl or alkoxy, R2 represents hydroxy, alkoxy or —NHOH, Ar1 represents phenylene or biphenylene, X represents oxygen or sulphur, NR, —C≡C— or a bond, R represents hydrogen or alkyl, n is an integer from 0 to 6 inclusive, Ar2 represents any one of the groups as defined in the description, its isomers and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful as metalloprotease inhibitors.Type: GrantFiled: June 30, 2000Date of Patent: January 15, 2002Assignee: Adir et CompagnieInventors: Guillaume de Nanteuil, Alain Benoist, Jacqueline Bonnet, Massimo Sabatini, Ghanem Atassi, Alain Pierre
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Patent number: 6331541Abstract: 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, Daniel S. Gardner
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Patent number: 6316214Abstract: The purification and structure elucidation of several products of the metabolism of Et 743 by human cytochrome CYP3A4 have been accomplished. These compounds are abbreviated herein as “ETM” followed by a numeric value, which represents the approximate molecular weight. Three compounds have been identified to date, namely ETM 305, ETM 775 and ETM 204.Type: GrantFiled: May 11, 1999Date of Patent: November 13, 2001Assignee: The Board of Trustees of the University of IllinoisInventors: Kenneth L. Rinehart, Jose J. Morales, Joel Reid, Isabel Reymundo, Pablo Floriano, Lola Garcia Gravalos
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Patent number: 6291425Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.Type: GrantFiled: September 1, 1999Date of Patent: September 18, 2001Assignee: Guilford Pharmaceuticals Inc.Inventors: Jia-He Li, Jie Zhang
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Patent number: 6255305Abstract: Substituted triazolo-pyridazine derivative compounds represented by wherein the variables are disclosed herein are selective ligands for GABA-A receptors, particularly for the &agr;2 and/or &agr;3 subunits.Type: GrantFiled: November 10, 1998Date of Patent: July 3, 2001Assignee: Merck Sharp & Dohme LimitedInventors: Howard Barff Broughton, William Robert Carling, Jose Luis Castro Pineiro, Alexander Richard Guiblin, Andrew Madin, Kevin William Moore, Michael Geoffrey Russell, Leslie Joseph Street
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Patent number: 6184377Abstract: The present invention is directed to certain N-amino- and N-hydroxy-quinazolinone compounds and synthetic methods for synthesis thereof, which compounds may find use in combinatorial libraries. More specifically, the invention is directed to the synthesis of 3-hydroxy- and 3-amino-4(1H)-quinazolinones via the reaction of an appropriate 2-aminobenzamide compound with a carboxylic acid or acyl halide at ambient temperature performed on a solid support or in solution.Type: GrantFiled: December 15, 1997Date of Patent: February 6, 2001Assignee: Sepracor Inc.Inventor: Yun Gao
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Patent number: 6174900Abstract: Disclosed herein is a substituted piperidine derivative represented by the following general formula (1): wherein R1 means an aryl or heteroaryl group which may have at least one substituent, R2 denotes an alkyl, alkenyl or aralkyl group, R3 stands for a hydrogen atom or an alkyl group, and R4 is a hydrogen atom, an alkyl group, or an aryl, heteroaryl, aralkyl, aralkenyl or heteroaralkyl group which may have at least one substituent, or a salt thereof. A medicine including this compound is also disclosed. The compound has excellent anticholinergic effect and calcium antagonism and inhibits reflex bladder contraction and is hence useful for prophylaxis of and treatment for a urinary disturbance such as pollakiuria.Type: GrantFiled: June 14, 1999Date of Patent: January 16, 2001Assignee: SS Pharmaceutical Co., Ltd.Inventors: Tomomi Okada, Fujiko Konno, Terumitsu Kaihoh, Masago Ishikawa, Yoshinori Takahashi, Hiroyuki Mizuno, Haruyoshi Honda, Susumu Sato, Hideaki Matsuda
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Patent number: 6143890Abstract: Hydrazam imides of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are each independently of the other (a) hydrogen or nitro, at least one of which radicals being nitro, or R.sup.1 and R.sup.2 together are (b) one of the following radicals ##STR2## wherein B is ##STR3## and R.sup.5 is C.sub.1 -C.sub.18 alkyl or R.sup.3 or R.sup.4, in which case R.sup.1 and R.sup.2 are bound to the compound of formula I in the positions a and b,R.sup.3 and R.sup.4 are each independently of the other unbranched C.sub.1 -C.sub.10 alkyl, and processes for their preparation and their use.Type: GrantFiled: December 16, 1999Date of Patent: November 7, 2000Assignee: Ciba Specialty Chemicals CorporationInventors: Heinz Langhals, Rami Ismael
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Patent number: 6140328Abstract: The invention provides compounds of formula I: whereinR.sub.1 -R.sub.8 and X and Y have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.Type: GrantFiled: December 12, 1997Date of Patent: October 31, 2000Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Darshan B. Makhey, Baoping Zhao, Leroy Fong Liu
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Patent number: 6124277Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.Type: GrantFiled: March 11, 1999Date of Patent: September 26, 2000Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 6124290Abstract: Polycyclic phthalazines, in particular 2-substituted maduraphthalazines (10,12,15,16-tetrahydroxy-8-methoxy-11-methyl-1,9,14-trioxo-1,2,6,7,9,14-h exahydronaphthaceno-1,2-g-phthalazines), of formula I and their use against gram-positive bacterial strains, particularly against multi-resistant staphylococci (MRSA) and against glycopeptide-resistant, for example vancomycin-resistant, enterococci. The polycyclic phthalazines are thus suitable for preparing anti-bacterially effective pharmaceutical compositions. In formula I, R.sup.1 is carboxyalkyl or carboxyaryl, and R.sup.2 and R.sup.3 represent H or acyl (for example CO-alkyl or COO-alkyl), with R.sup.1 being different from optionally substituted carboxyphenyl when R.sup.3 represents C.sub.1-8 alkanoyl. The invention also relates to salts, amides and esters of compounds of formula I.Type: GrantFiled: January 28, 2000Date of Patent: September 26, 2000Assignee: Gruenenthal GmbHInventors: Lothar Heinisch, Ute Moellmann, Wolfgang Witte, Christiane Cuny, Ernst Roemer, Walter Werner, Udo Graefe
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Patent number: 6110931Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: March 25, 1999Date of Patent: August 29, 2000Assignee: Merck & Co., Inc.Inventors: Thomas F. Walsh, Mark T. Goulet, Feroze Ujjainwalla, Jonathan R. Young
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Patent number: 6107304Abstract: Invented are substituted thieno (2,3-b)pyrazolo(3,4-d)pyridin-3-ones, pharmaceutical compositions containing these compounds, and methods of using these compounds to enhance erythropoiesis. Also invented are intermediates and processess used in preparing these compounds.Type: GrantFiled: June 7, 1999Date of Patent: August 22, 2000Assignee: SmithKline Beecham CorporationInventor: Juan Ignacio Luengo
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Patent number: 6093821Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: October 8, 1997Date of Patent: July 25, 2000Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Mark E. Goldman, Charlotte L. F. Pooley, David T. Winn, James P. Edwards, Sarah J. West, Christopher M. Tegley, Lin Zhi
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Patent number: 6022870Abstract: Cyclic amides of Formula I which are useful as fungicides: ##STR1## wherein A is N; G is N and the floating double bond is attached to A; W is O or S; X is OR.sup.1, S(O).sub.m R.sup.1 or halogen; R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z are defined in the disclosure, are disclosed. Also, disclosed are fungicidal compositions containing these compounds and the use of these cyclic amide compounds for controlling plant diseases caused by fungal plant pathogens.Type: GrantFiled: May 13, 1999Date of Patent: February 8, 2000Assignee: E. I. du Pont de Nemours and CompanyInventors: Richard James Brown, King-Mo Sun, Deborah Ann Frasier
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Patent number: 6005105Abstract: The present invention is directed to a process for preparing the following compound ##STR1## which is prepared starting from ##STR2## which is reacted succesively with 4-iodobenzyl or 4-bromobenzyl bromide, hydrazine and 1,4-dimethyl-1,3-cyclohexadiene, reduced and reacted with phenyltetrazole or suitably protected phenyltetrazole followed by removalType: GrantFiled: December 6, 1995Date of Patent: December 21, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Hiroyoshi Yamada, Kiyotaka Munesada, Keiko Koh, Kazuo Tsuzuki, Mikio Taniguchi, Yoshiji Fujita
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Patent number: 5994544Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors and the method of preparing these compounds are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: October 8, 1997Date of Patent: November 30, 1999Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Christopher M. Tegley, Lin Zhi, James P. Edwards
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Patent number: 5985876Abstract: Five new nucleophile substituted ecteinascidin (Et) compounds have been isolated from extracts of Ecteinascidia turbinata. These compounds have been purified by chromatographic techniques and their structures and bioactivities have been determined. The five nucleophile substituted Et compounds have been designated herein as Et 802 (1), Et 788 (2), Et 760 (3), Et 858 (4) and Et 815 (5). Also obtained were three new N-oxide ecteinascidin compounds, which have been designated herein as Et 717 (6), Et 775 (7) and Et 789 (8). Some of these newly discovered Et compounds show exceedingly potent cytotoxicity against L1210.Type: GrantFiled: April 10, 1998Date of Patent: November 16, 1999Inventors: Kenneth L. Rinehart, Tong Zhou
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Patent number: 5952335Abstract: Novel fused polycyclic heterocycle derivatives having excellent antitumor effects and a process for producing the same. A compound represented by the following general formula (I) or pharmacologically acceptable salts thereof: ##STR1## wherein the ring A represents an optionally substituted monocyclic aromatic ring or a dicyclic fused ring in which at least one of the rings is an aromatic ring; the ring B represents pyrrole, 4H-1,4-oxazine, 4H-1,4-thiazine or 4(1H)-pyridone; the ring C represents an optionally substituted, monocyclic or dicyclic fused aromatic ring; and Y represents a group represented by the formula --e--f (wherein e represents a lower alkylene; and f represents amidino, guanidino or amino optionally substituted by optionally hydroxylated or optionally lower-alkylaminated lower alkyl;provided that the cases where the rings A and B are both optionally substituted monocyclic aromatic rings are excluded. Which has an excellent antitumor activity.Type: GrantFiled: November 26, 1997Date of Patent: September 14, 1999Assignee: Eisai Co., Ltd.Inventors: Hiroyuki Sugumi, Jun Niijima, Yoshihiko Kotake, Toshimi Okada, Jun-ichi Kamata, Kentaro Yoshimatsu, Takeshi Nagasu, Katsuji Nakamura, Toshimitsu Uenaka, Atsumi Yamaguchi, Hiroshi Yoshino, Nozomu Koyanagi, Kyosuke Kito
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Patent number: 5948792Abstract: Novel fluorine-containing 1,4-disubstituted piperidine derivatives, represented by general formula ?I! ##STR1## such as, for example, (2R)-N-?1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl!-2-?(1R)-3,3-difluoroc yclopentyl!-2-hydroxy-2-phenylacetamide or pharmaceutically acceptable salt thereof, are potent and selective antagonists for muscarinic M.sub.3 receptors with little side effects. The compounds of formula ?I! exhibit excellent oral activity, duration of activity and pharmacolkinetics. They are useful for treatment and prophylaxis of respiratory diseases, such as chronic obstructive pulmonary diseases; urinary diseases, such as urinary incontinence; and digestive diseases, such as irritable bowel syndrome, and motion sickness.Type: GrantFiled: July 31, 1997Date of Patent: September 7, 1999Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshimi Tsuchiya, Takashi Nomoto, Hirokazu Ohsawa, Kumiko Kawakami, Kenji Ohwaki, Masaru Nishikibe
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Patent number: 5886177Abstract: Novel ethylene glycol compounds bearing various functional groups are used to prepare oligomeric structures. The ethylene glycol monomers can be joined via standard phosphate linkages including phosphorothioate, phosphodiester, and phosphoramidate linkages. Useful functional groups include nucleobases as well as polar groups, hydrophobic groups, ionic groups, aromatic groups and/or groups that participate in hydrogen-bonding.Type: GrantFiled: August 8, 1996Date of Patent: March 23, 1999Assignee: ISIS Pharmaceuticals, Inc.Inventors: Phillip Dan Cook, Oscar L. Acevedo, Peter W. Davis, David J. Ecker, Normand Hebert
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Patent number: 5852030Abstract: A novel compound which is a .delta.-opioid antagonist having high selectivity and activity, that exhibits immunosuppressive action, antiallergic action, anti-inflammatory action and brain cell-protecting action is disclosed. The compound according to the present invention is an indole derivative represented by the formula (I): ##STR1## and pharmaceutically acceptable acid addition salts thereof. The present invention also provides an immunosuppressive agent, antiallergic agent, anti-inflammatory agent and brain cell-protecting agent comprising the derivative or the salt as an effective ingredient.Type: GrantFiled: September 10, 1996Date of Patent: December 22, 1998Assignee: Toray Industries, Inc.Inventors: Hiroshi Nagase, Akira Mizusuna, Koji Kawai, Izumi Nakatani
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Patent number: 5808060Abstract: Disclosed are biologically active, non-indole-containing compounds referred to as fused isoindolones, which are represented by the following general formula: ##STR1## The fused indolones can be obtained by complete chemical synthesis. Methods for making and using the fused isoindolones are disclosed.Type: GrantFiled: December 9, 1996Date of Patent: September 15, 1998Assignee: Cephalon, Inc.Inventors: Robert L. Hudkins, Neil W. Johnson
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Patent number: 5786361Abstract: Compounds of the formula (I): ##STR1## are prepared by reaction of the phenylacetic acid derivatives substituted by the appropriate heterocycles, optionally in an activated form, with phenylglycinols. The compounds are suitable as active compounds in medicaments, in particular in medicaments having antiatherosclerotic activity.Type: GrantFiled: April 11, 1997Date of Patent: July 28, 1998Assignee: Bayer AktiengesellschaftInventors: Ulrich Muller, Peter Eckenberg, Rudi Grutzmann, Hilmar Bischoff, Dirk Denzer, Ulrich Nielsch
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Patent number: 5753664Abstract: A novel compound of the formula:A--Z--Ar.sup.1 1'CO--Ar.sup.2wherein A is a condensed pyrimidinone or condensed pyridazinone ring; Ar.sup.1 and Ar.sup.2 are independently a ring; Z is a divalent group, or a salt thereof which have an excellent antitumor activity.Type: GrantFiled: March 13, 1996Date of Patent: May 19, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Tetsuya Aono, Shogo Marui, Fumio Itoh, Masuo Yamaoka, Masafumi Nakao
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Patent number: 5750540Abstract: This invention provides novel 1,4-di-substituted piperidine derivatives of the general formula ?I! ##STR1## and the pharmaceutically acceptable salts thereof, wherein: Ar represents a phenyl group or a five- or six-membered heteroaromatic group having one or two hetero atoms selected from the group consisting of an oxygen atom, a sulfur atom and a nitrogen atom in which one or two optional hydrogen atoms on the ring may be replaced by substituent groups selected from the group consisting of a halogen atom and a lower alkyl group;R.sup.1 represents a cycloalkyl group of 3 to 6 carbon atoms or a cycloalkenyl group of 3 to 6 carbon atoms;R.sup.2 represents a saturated or unsaturated aliphatic hydrocarbon radical of 5 to 15 carbon atoms; andX represents O or NH.These compounds have selective antagonistic activity against the muscarinic M.sub.3 receptors and can hence be used safely with a minimum of side effects.Type: GrantFiled: July 31, 1996Date of Patent: May 12, 1998Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshimi Tsuchiya, Takashi Nomoto, Hirokazu Ohsawa, Kumiko Kawakami, Kenji Ohwaki, Masaru Nishikibe
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Patent number: 5696130Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: December 9, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, David T. Winn, Mark E. Goldman, Lawrence G. Hamann, Lin Zhi, Luc J. Farmer, Robert L. Davis
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Patent number: 5696127Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: December 9, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Lin Zhi, James P. Edwards, Christopher M. Tegley, Sarah J. West
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Patent number: 5693647Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: December 2, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Lin Zhi, Christopher M. Tegley, David T. Winn, Lawrence G. Hamann, James P. Edwards, Sarah J. West
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Patent number: 5693646Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: December 2, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Christopher M. Tegley, Lin Zhi, James P. Edwards, Sarah J. West
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Patent number: 5693640Abstract: A class of pyridazino?4,5-b!indole-1,4-dione derivatives, substituted in the 2-position by an optionally substituted phenyl moiety, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment and/or prevention of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA antagonist.Type: GrantFiled: June 6, 1995Date of Patent: December 2, 1997Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Tamara Ladduwahetty, Angus Murray MacLeod
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Patent number: 5688793Abstract: The invention relates to new pyridazino?4',5':3,4!-pyrrolo?2,1-a!isoquinolines of the formula ##STR1## and the physiologically acceptable salts thereof with acids and complex-forming agents, wherein X is O, S or NHO and R.sub.1, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are defined as in the specification, and pharmaceutical preparations containing these compounds.Type: GrantFiled: August 19, 1996Date of Patent: November 18, 1997Assignee: Boehringer Ingelheim GmbHInventors: Walter Losel, Otto Roos, Dietrich Arndts
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Patent number: 5688808Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: November 18, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, David T. Winn, Lin Zhi, Lawrence G. Hamann, Christopher M. Tegley, Charlotte L. F. Pooley
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Patent number: 5688810Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: June 5, 1995Date of Patent: November 18, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Mark E. Goldman, Charlotte L.F. Pooley, David T. Winn, James P. Edwards, Sarah J. West, Christopher M. Tegley, Lin Zhi
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Patent number: 5677304Abstract: The invention relates to the use of 9-amino-pyridazino-?4',5':3,4!pyrrolo?2,1-a!isoquinolines of the formula ##STR1## and the physiologically acceptable salts thereof with acids, bases and complexing agents for preparing agents for treating chronic inflammatory processes, ulcerative colitis and Crohn's disease, and for producing agents having an antiproliferative activity. The definitions of substituents R.sub.1 to R.sub.9 are given in the specification. The invention also relates to new compounds of general formula I which are also defined in the specification and their use as cerebroprotective agents.Type: GrantFiled: May 17, 1996Date of Patent: October 14, 1997Assignee: Boehringer Ingelheim KGInventors: Dietrich Arndts, Walter Losel, Otto Roos
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Patent number: 5658917Abstract: The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C--R.sup.11 (wherein R.Type: GrantFiled: April 28, 1995Date of Patent: August 19, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Shigeki Fujiwara, Daisuke Machii, Haruki Takai, Hiromi Nonaka, Hiroshi Kase, Kozo Yao, Michiyo Kawakage, Hideaki Kusaka, Akira Karasawa