Plural Chalcogens Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/155)
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Patent number: 6608083Abstract: NK3 receptor antagonists of formula (I): in which: Ar is an optionally substituted phenyl group, or a naphthyl or C5-7 cycloalkdienyl group, or an optionally substituted single or fused ring heterocyclic group, having aromatic character, containing from 5 to 12 ring atoms and comprising up to four hetero-atoms in the or each ring selected from S, O, N; R is linear or branched C1-8 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, an optionally substituted phenyl group or a phenyl C1-6 alkyl group, an optionally substituted five-membered heteroaromatic ring comprising up to four heteroatoms selected from O and N, hydroxy C1-6 alkyl, amino C1-6 alkyl, C1-6 alkylaminoalkyl, di C1-6 alkylaminoalkyl, C1-6 acylaminoalkyl, C1-6 alkoxyalkyl, C1-6 alkylcarbonyl, carboxy, C1-6 alkoxyxcarbonyl, C1-6 alkoxycarbonyl C1-6 alkyl, aminocarbonyl, C1-6 alkylaminocarbonyl, di C1-6 alkylaminocarbonyl, halogeno C1-6 alkyl; or is a group —(CH2)p— when cyclized onto Ar, where p is 2 or 3; R1 and R2, whiType: GrantFiled: May 25, 1995Date of Patent: August 19, 2003Assignee: SmithKline Beecham Farmaceutici S.p.AInventors: Carlo Farina, Giuseppe Arnaldo Maria Giardina, Mario Grugni, Luca Francesco Raveglia
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Patent number: 6605616Abstract: The invention is related to compounds of general formula (I) wherein R is methyl, ethyl, n-propyl, iso-propyl, n-butyl or allyl; R′ is methyl, methoxy, fluoro, chloro, bromo, azido, trifluorometlhyl, or OCHxFy, wherein x=0−2, y=1−3 with the. proviso that x+y=3; R″ is hydrogen, fluoro or chloro; with the proviso that R″ is fluoro or chloro only when R′ is fluoro or chloro; R4 is hydrogen or pharmaceutically acceptable inorganic or organic cations; R5 is dimethylamino or nitro; R6 is hydrogen; and when R′ is azido R5 is also ethyl, n-propyl, iso-propyl, methoxy, ethoxy, chloro, bromo, trifluoromethyl, OCHxFy, wherein x=0−2, y=1−3 with the proviso that x+y=3, or R5 and R6 taken together are methylenedioxy; and any tautomer thereof. The invention also relates to pharmaceutical compositions containing a compound of the general formula (I) together with a pharmaceutically acceptable carrier.Type: GrantFiled: July 21, 2000Date of Patent: August 12, 2003Assignee: Active Biotech ABInventors: Anders Björk, Stig Jönsson, Tomas Fex, Gunnar Hedlund
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Patent number: 6593343Abstract: Compounds of formula (I) and tautomers thereof are effective for the treatment of mammals suffering from diseases resulting from autoimmunity and pathological inflammation.Type: GrantFiled: April 25, 2002Date of Patent: July 15, 2003Assignee: Active Biotech ABInventors: Anders Björk, Stig Jönsson, Tomas Fex, Gunnar Hedlund
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Publication number: 20030120075Abstract: The present invention describes methods for the stereoselective synthesis of heterocyclic enantiomers. The methods of the present invention incorporate the stereo-preferred oxidation of quinolone thiomethyl intermediates by optically active camphor based oxaziridines to provide R(+) or S(−) quinolone methylsulfinyl derivatives.Type: ApplicationFiled: October 25, 2001Publication date: June 26, 2003Applicant: R.T. Alamo Adventures I, LLCInventors: Stefan Kwiatkowski, Miroslaw Golinski, Joseph Kupper
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Patent number: 6583179Abstract: The present invention is directed to a series of novel substituted aminoalkylamide derivatives, pharmaceutical compositions containing them and their use in the treatment of reproductive disorders and affective conditions. Further, the compounds of the invention are antagonists of follicle stimulating hormone, a hormone associated with the human reproductive system.Type: GrantFiled: December 21, 2000Date of Patent: June 24, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Steven J. Coats, Louis J. Fitzpatrick, Dennis J. Hlasta, Carolina L. Lanter, Mark J. Macielag, Ke Pan, Ralph A. Rivero, Stephen S. Palmer
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Patent number: 6579986Abstract: The invention relates to a process for preparing quinoline-substituted carbonate and carbamate compounds, which are important intermediates in the synthesis of 6-O-substituted macrolide antibiotics. The process employs metal-catalyzed coupling reactions to provide a carbonate or carbamate of formula (I) or (II) or a substrate that can be reduced to obtain the same.Type: GrantFiled: April 29, 2002Date of Patent: June 17, 2003Assignee: Abbott LaboratoriesInventors: Michael S. Allen, Ramiya H. Premchandran, Sou-Jen Chang, Stephen Condon, John A. DeMattei, Steven A. King, Lawrence Kolaczkowski, Sukumar Manna, Paul J. Nichols, Hemant H. Patel, Subhash R. Patel, Daniel J. Plata, Eric J. Stoner, Jien-Heh J. Tien, Steven J. Wittenberger
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Patent number: 6579881Abstract: A 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: wherein A, B, C, D, T, Y, and Z each represent a methine or a nitrogen linkage; R1, R2, R3, R4, and R5 each represent a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3. The compounds have serotonin antagonism. They are therefore clinically useful as medicaments, in particular, for treating, ameliorating, and preventing spastic paralysis. They are also useful as central muscle relaxants for ameliorating myotonia.Type: GrantFiled: May 18, 2001Date of Patent: June 17, 2003Assignee: Eisai Co., Ltd.Inventors: Noritaka Kitazawa, Kohshi Ueno, Keiko Takahashi, Teiji Kimura, Atsushi Sasaki, Koki Kawano, Tadashi Okabe, Makoto Komatsu, Manabu Matsunaga, Atsuhiko Kubota
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Patent number: 6569870Abstract: The present invention provides fluorinated quinolones which are fluorinated on the phenyl group thereof, along with pharmaceutical formulations containing the same, methods of treating tumors or cancer by the administration of such compounds, and methods of inhibiting cellular mitosis by the administration of such compounds.Type: GrantFiled: September 25, 2000Date of Patent: May 27, 2003Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Yi Xia, Zheng-Yu Yang, Sheno-Chu Kuo
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Publication number: 20030087929Abstract: The problem to be solved by the present invention is to provide a quinolinone derivative formulation, and its production method, having for its active ingredient the &bgr; crystal form and/or &ggr; crystal form of the quinolinone derivative represented with chemical formula (I), which is useful as a pharmaceutical, and particularly as an antiallergic, which has superior bioabsorption and stability.Type: ApplicationFiled: June 24, 2002Publication date: May 8, 2003Applicant: DAINIPPON INK AND CHEMICALS, INC.Inventors: Nobuyuki Kimura, Hiroyuki Fukui, Hidetsugu Takagaki, Nahoko Muratake
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Publication number: 20030069271Abstract: The present invention relates to quinolone compounds and their use in the treatment of viral infections.Type: ApplicationFiled: June 17, 2002Publication date: April 10, 2003Inventors: Clarence Webster Andrews,III, George Andrew Freeman, Andrew Lee Hopkins
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Patent number: 6515127Abstract: The invention concerns a method for preparing quinoline-5,8-diones of formula (I) wherein R1, R2 and R3 are as defined in claim 1, by light-induced oxygenation of a 8-hydroxyquinoline.Type: GrantFiled: February 12, 2002Date of Patent: February 4, 2003Assignee: Laboratoire L. LafonInventors: Janine Cossy, Damien Belotti
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Patent number: 6509352Abstract: A 2-oxoquinoline compound or its pharmaceutically acceptable salt of general formula [I]: (wherein each symbol in the formula is as determined in the description), and its pharmaceutical use. The compound [I] of the present invention and its pharmaceutically acceptable salts selectively act on cannabinoid receptors, particularly on peripheral type cannabinoid receptors, and have fewer side effects on the central nervous system, having great immunosuppressive action, anti-inflammatory action or antiallergic action. Therefore, these compounds are useful as cannabinoid receptors (particularly peripheral type cannabinoid receptors) modulator, immunosuppressants, anti-inflammatory agents, and antiallergic agents.Type: GrantFiled: August 29, 2001Date of Patent: January 21, 2003Assignee: Japan Tobacco Inc.Inventors: Takashi Inaba, Tetsudo Kaya, Hiroyuki Iwamura
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Publication number: 20020173519Abstract: Compounds of formula (I) 1Type: ApplicationFiled: April 25, 2002Publication date: November 21, 2002Applicant: Active Biotech ABInventors: Anders Bjork, Stig Jonsson, Tomas Fex, Gunnar Hedlund
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Publication number: 20020173520Abstract: The invention is related to compounds of general formula (I) 1Type: ApplicationFiled: April 25, 2002Publication date: November 21, 2002Applicant: Active Biotech ABInventors: Anders Bjork, Stig Jonsson, Tomas Fex, Gunnar Hedlund
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Patent number: 6448243Abstract: A novel 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: (wherein A, B, C, D, T, Y and Z represent each methine or nitrogen; R1, R2, R3, R4 and R5 represent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3.) The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.Type: GrantFiled: August 11, 1999Date of Patent: September 10, 2002Assignee: Eisai Co., Ltd.Inventors: Noritaka Kitazawa, Kohshi Ueno, Keiko Takahashi, Teiji Kimura, Atsushi Sasaki, Koki Kawano, Tadashi Okabe, Makoto Komatsu, Manabu Matsunaga, Atsuhiko Kubota
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Patent number: 6432978Abstract: As novel compounds which possess a chymase-inhibiting activity and are useful as medicines for a variety of applications, there are provided SF2809-I substance, SF2809-II substance, SF2809-III substance, SF2809-IV substance, SF2809-V substance and SF2809-VI substance which are represented by the following general formula (VII) wherein R1 is a hydrogen atom, phenyl group or p-hydroxyphenyl group, and R2 is acetylamino group —NHCOCH3 or hydroxyl group, or pharmaceutically acceptable salts thereof, and which possess the chymase-inhibiting activity. Also provided is a process for the preparation of the above SF2809 substances, as well as a pharmaceutical composition comprising one of those substances.Type: GrantFiled: May 31, 2001Date of Patent: August 13, 2002Assignee: Meiji Seika Kaisha, Ltd.Inventors: Masato Tani, Yasuhiro Gyobu, Chieko Moriyama, Toru Sasaki, Osami Takenouchi, Takashi Kawamura, Takashi Kamimura, Toshiaki Harada
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Publication number: 20020107392Abstract: Organic compounds having the formulas I and II are provided where the variables have the values described herein.Type: ApplicationFiled: September 11, 2001Publication date: August 8, 2002Inventors: Paul A. Renhowe, Sabina Pecchi, Timothy D. Machajewski, Cynthia M. Shafer, Clarke Taylor, William R. McCrea, Christopher McBride, Elisa Jazan
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Patent number: 6407242Abstract: Quinoline compound, zinc halogenide complex and zinc complex suited for use in an electro-luminescence (EL) element, a fluorescent material and an ultraviolet absorption material, and a preparation process for these compounds are described. These compounds and a tautomer of the same has a strong luminescent intensity and is used for an EL material, the compound of zinc halogenide complex and zinc complex and a tautomer of the same has absorption at a wave length of 400 nm or less and is used for an ultraviolet absorption material, and further the quinoline compound and a tautomer has a strong luminescent intensity and is used for a fluorescent material. The zinc halogenide complex and zinc complex can be prepared by related preparation processes directly from a quinoline derivative and a phthalimide derivative, or by way of the quinoline compound which is obtained from these derivatives.Type: GrantFiled: August 22, 2000Date of Patent: June 18, 2002Assignee: Mitsui Chemicals, Inc.Inventors: Tadashi Okuma, Hideki Ikuta, Tatsuya Nagayoshi, Akira Ogiso, Hisato Ito
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Patent number: 6395750Abstract: The invention relates to a method for the treatment of tumors in mammals by the administration of compounds of the general formula (I) wherein A is O41 or NR42 R43 wherein R41 is hydrogen or a pharmaceutically acceptable inorganic or organic cation, or CORA wherein RA is alkyl and aryl; R42 and R43 are hydrogen, C1-C4-alkyl, cyclopropyl, cyclopentyl or cyclohexyl; or R42 is benzyl or phenethyl, optionally mono- or disubstituted by methyl, iso-propyl methoxy, fluoro, chloro, bromo, dimethylamino, trifluoromethyl or nitro and R43 is hydrogen; or R42 and R43 form a 5- or 6-membered ring; or R42 is CORB wherein RB is alkyl or aryl, —CH2N(CH3)2 or —CH2CH2COOH or CORB is a 2-acyloxymethylbenzoyl group wherein RC is methyl, ethyl, phenyl or benzyl; R42 is COORD wherein RD is C1-C4-alkyl, phenyl or benzyl; or R42 is —CH2OCO-tert.Type: GrantFiled: October 24, 2000Date of Patent: May 28, 2002Assignee: Active Biotech ABInventors: Gunnar Hedlund, Karl Jansson, Stig Jönsson, Anders Björk
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Patent number: 6387926Abstract: Disclosed are quinoline and benzazepine derivatives that inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogenic protein Ras. Thus, the compounds are useful as anti-cancer agents. The compounds are also useful in the treatment of diseases other than cancer.Type: GrantFiled: May 29, 1998Date of Patent: May 14, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Rajeev S. Bhide, Charles Z. Ding, John T. Hunt, Soong-Hoon Kim, Katerina Leftheris
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Patent number: 6388080Abstract: Polymorphs Form B, Form C, and amorphous of 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-2(1H)-quinolinone, commonly known as cilostazol, have been identified. These polymorphs may be formed in pure form, in combination with each other, in combination with other polymorphs of cilostazol, or together with other pharmaceutical agents. Processes for preparing these polymorphs, and combinations of these polymorphs, as well as methods of use and unit dosages of these polymorphic forms, and their combinations, are described.Type: GrantFiled: June 29, 2001Date of Patent: May 14, 2002Inventors: Grayson Walker Stowell, Robert R. Whittle
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Patent number: 6362193Abstract: Novel pyridyl or pyrimidinyl substituted cycloalkenyl compounds and compositions for use in therapy.Type: GrantFiled: April 7, 2000Date of Patent: March 26, 2002Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Ravi Garigipati
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Patent number: 6335447Abstract: Novel quinolonecarboxylic acid derivatives of general formula (1) or salts thereof which have potent antibacterial effects on gram-positive bacteria in particular Propionibacterium acnes (wherein R1 represents a hydrogen atom or a carboxyl-protective group; R2 represents an optionally substituted cycloalkyl group; R3 represents a hydrogen atom, a halogen atom, an optionally substituted alkyl, alkoxy or alkylthio group, an optionally protected hydroxyl or amino group, or a nitro group; R4 represents an optionally substituted alkyl or alkoxy group; and Z represents a pyridin-4-yl or pyridin-3-yl group which is optionally substituted with at least one group selected from a halogen atom, an optionally substituted alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio or amino group and an optionally protected hydroxyl or amino group).Type: GrantFiled: October 5, 2000Date of Patent: January 1, 2002Assignee: Toyama Chemical Co., Ltd.Inventors: Kazuya Hayashi, Tokunori Kito, Junichi Mitsuyama, Tetsumi Yamakawa, Hiroshi Kuroda, Hiroyo Kawafuchi
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Patent number: 6329389Abstract: The present invention provides a compound of the formula: wherein Ar represents an aromatic group which may be substituted; X represents methylene, S, SO, SO2 or CO; Y represents a spacer having a main chain of 2 to 5 atoms; n represents an integer of 1 to 5; i) R1 and R2 each represents a hydrogen atom or a lower alkyl which may be substituted, ii) R1 and R2 form, taken together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic ring which may be substituted, or iii) R1 or R2 together with —(CH2)n—N═ form, bonded to a component atom of Ring B, a spiro-ring which may be substituted; Ring A represents an aromatic ring which may be substituted; Ring B represents a 4- to 7-membered nitrogen-containing non-aromatic ring which may be further substituted by alkyl or acyl, with a proviso that X represents S, SO, SO2 or CO when Ring A has as a substituent a group represented by the formula: —NHCOR11 where R11 represents alkyl, alkoxyalkyl, alkylthioType: GrantFiled: November 19, 1999Date of Patent: December 11, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Nobuhiro Suzuki, Kaneyoshi Kato, Shiro Takekawa, Jun Terauchi, Satoshi Endo
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Patent number: 6320051Abstract: Compounds of formula (I) are inhibitors of the bacterial enzyme S aureus methionyl tRNA synthetase and are of use in treating bacterial infections.Type: GrantFiled: October 26, 2000Date of Patent: November 20, 2001Assignee: SmithKline Beecham plcInventors: John Michael Berge, Pamela Brown, John Stephen Elder, Andrew Keith Forrest, Dieter Wolfgang Hamprecht, Richard Lewis Jarvest, David Jonathan McNair, Robert John Sheppard
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Patent number: 6307050Abstract: A high-yield, 4-step synthesis for flosequinan starting with 4-fluoroanthranilic acid comprising cyclization with phosgene to create an intermediate -A, followed by methylation to create an intermediate -B, then by reaction with dimsyl sodium to create an intermediate -C, then by reaction with triethyl orthoformate in the presence of piperdine and acetic acid to give flosequinan. The overall yield of the disclosed process is greater than about 16%.Type: GrantFiled: February 7, 2001Date of Patent: October 23, 2001Assignee: R. T. Alamo Venture I LLCInventors: Stephan Kwiatkowski, Maya Siddidqui, Rodney Eisenberg, Sudarsan Mukhopadhyay, Lowell Jeffry Lawrence, Steven G. Mobley
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Patent number: 6258824Abstract: The present invention relates to compounds of formula 1 and pharmaceutically acceptable salts and solvates thereof wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and Z are as defined herein. The invention also relates to pharmaceutical compositions comprising compounds of formula 1 and to methods of inhibiting abnormal cell growth, including cancer, in a mammal by administering compounds of formula 1 to the mammal. The invention also relates to intermediates and methods useful in synthesizing compounds of formula 1.Type: GrantFiled: February 9, 2000Date of Patent: July 10, 2001Assignee: Pfizer Inc.Inventor: Bingwei V. Yang
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Patent number: 6255479Abstract: A method for preparing an &agr;-oxolactam comprising, reacting a corresponding &agr;-diazolactam with an oxygen donor, in the presence of a transition metal catalyst, to yield the corresponding &agr;-oxolactam.Type: GrantFiled: December 29, 1998Date of Patent: July 3, 2001Assignee: Research Corporation Technologies, Inc.Inventors: John D. Buynak, Akireddy Srinivasa Rao
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Patent number: 6252080Abstract: The present invention provides for 8-hydroxy-7-substituted quinoline compounds such as formula IA These compounds are useful as anti-viral agents. Specifically, these compounds have anti-viral activity against the herpes virus, cytomegalovirus (CMV). Many of these compounds are also active against other herpes viruses, such as the varicella zoster virus, the Epstein-Barr virus, the herpes simplex virus and the human herpes virus type 8 (HHV-8).Type: GrantFiled: October 22, 1999Date of Patent: June 26, 2001Assignee: Pharmacia & UpJohn CompanyInventors: Suvit Thaisrivongs, Oliver Bezencon
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Patent number: 6221881Abstract: Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NOn-PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides a composition comprising a therapeutically effective amount of an phosphodiesterase inhibitor (PDE inhibitor), which can optionally be substituted with at least one NO or NO2 moiety, and one to ten fold molar excess of a compound that donates, transfers or releases nitrogen monoxide as a charged species, i. e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or which stimulates endogenous EDRF production. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides methods for treating sexual dysfunctions in males and females.Type: GrantFiled: February 10, 1999Date of Patent: April 24, 2001Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada
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Patent number: 6211374Abstract: The present invention provides water-soluble, pyran-based photochromic compounds characterized by improved stability when in an open, excited configuration. The advantages of the present invention are provided, at least in part, by functionalizing a pyran-based photochromic compound with carboxylate functionality in such a way that the carboxylate and/or its counter ion have sufficient mobility to engage in intermolecular and intramolecular interactions. In preferred embodiments, such a mobile carboxylate and/or counter ion provided on one side of an open pyran ring is preferably capable of complexing with functionality on the other side of the open pyran ring, greatly stabilizing the open configuration.Type: GrantFiled: April 22, 1998Date of Patent: April 3, 2001Inventor: Joseph Thomas Ippoliti
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Patent number: 6211196Abstract: Benzyloxy-substituted, fused N-heterocycles, because of their ability to act as bradykinin receptor antagonists, have been found to be useful as therapeutics for the treatment and prevention of liver cirrhosis or Alzheimer's disease. This application describes such compounds, as well as processes for their preparation and use. The compounds according to this invention include compounds of formula (I) in which B, D, R1, and R2 have the meanings indicated herein.Type: GrantFiled: March 26, 1998Date of Patent: April 3, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Holger Heitsch, Adalbert Wagner, Klaus Wirth, Bernward Schölkens
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Patent number: 6200971Abstract: The bicyclic heterocyclic compounds are prepared by reaction of correspondingly substituted carboxylic acids with amines, in particular with phenylglycinolamine. The bicyclic heterocyclic compounds according to the invention are suitable as active compounds in medicaments, in particular in medicaments having an antiatherosclerotic action.Type: GrantFiled: October 18, 1999Date of Patent: March 13, 2001Assignee: Bayer AktiengesellschaftInventors: Richard Connell, Siegfried Goldmann, Ulrich Müller, Stefan Lohmer, Hilmar Bischoff, Dirk Denzer, Rudi Gr{umlaut over (u )}tzmann, Stefan Wohlfeil
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Patent number: 6174901Abstract: Selected novel substituted pyridine and pyridazine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: December 18, 1998Date of Patent: January 16, 2001Assignee: Amgen Inc.Inventors: Nathan B. Mantlo, Chan-Kou Hwang, Ulrike D. Spohr
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Patent number: 6172232Abstract: The present invention relates to novel compounds of the formula (I) in which the substituents have the meaning defined in the description. These novel compounds are excellent stabilizers for organic material against the damaging effects of light, heat and oxygen.Type: GrantFiled: September 3, 1998Date of Patent: January 9, 2001Assignee: Clariant GmbHInventor: Thomas St{umlaut over (a)}hrfeldt
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Patent number: 6166219Abstract: Novel benzimidazole derivatives represented by the formula (I): ##STR1## wherein R.sub.3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl group, or their pharmaceutically acceptable salts. Because of their blood sugar-depressing effect or PDE5 inhibitory effect, these compounds or salts thereof are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin resistance, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, or hypertension; or stenocardia, hypertension, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, atherosclerosis, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, diabetic complications, nephritis, cancerous cachexia, or restenosis after PTCA.Type: GrantFiled: November 2, 1998Date of Patent: December 26, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Noritsugu Yamasaki, Takafumi Imoto, Yoshiyuki Murai, Takahiro Hiramura, Teruo Oku, Kouzou Sawada
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Patent number: 6162813Abstract: There are disclosed compounds of formula (I) 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 conditions in both men and women.Type: GrantFiled: November 12, 1998Date of Patent: December 19, 2000Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Robert J. Devita, Matthew J. Wyvratt, Jr., Jonathan R. Young
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Patent number: 6150352Abstract: 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 conditions in both men and women.Type: GrantFiled: November 12, 1998Date of Patent: November 21, 2000Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Eric E Allen, Matthew J. Wyvratt, Jr., Jinlong Jiang, Richard B. Toupence, Thomas F Walsh, Feroze Ujjainwalla, Jonathan R Young, Robert J. Devita
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Patent number: 6150522Abstract: There are disclosed compounds of formula (I) 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 conditions in both men and women.Type: GrantFiled: November 12, 1998Date of Patent: November 21, 2000Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Robert J. DeVita, Matthew J. Wyvratt, Jr., Jonathan R. Young
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Patent number: 6147088Abstract: There are disclosed compounds of formula (I) and pharmaceutical 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 conditions.Type: GrantFiled: November 12, 1998Date of Patent: November 14, 2000Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Eric E Allen, Matthew J. Wyvratt, Jr., Jinlong Jiang, Roy G. Smith, Thomas F Walsh, Yi Tien Yang, Jonathan R Young, Robert J. Devita
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Patent number: 6133285Abstract: The invention is related to compounds of general formula (I) wherein R is methyl, ethyl, n-propyl, iso-propyl, n-butyl or allyl; R' is methyl, methoxy, fluoro, chloro, bromo, trifluoromethyl, or OCH.sub.x F.sub.y, whereinx=0-2, y=1-3 with the proviso that x+y=3, R" is hydrogen, fluoro or chloro; with the proviso that R" is fluoro or chloro only when R' is fluoro or chloro; R.sub.4 is hydrogen or pharmaceutically acceptable inorganic or organic cations;R.sub.5 is ethyl, n-propyl, iso-propyl, methoxy, ethoxy, chloro, bromo, trifluoromethyl, OCH.sub.x F.sub.y, or OCH.sub.2 CH.sub.x F.sub.y wherein x=0-2, y=1-3 with the proviso that x+y=3;R.sub.6 is hydrogen; or R.sub.5 and R.sub.6 taken together are methylenedioxy; and any tautomer thereof.The invention also relates to pharmaceutical compositions containing a compound of the general formula (I) together with a pharmaceutically acceptable carrier.Type: GrantFiled: July 14, 1999Date of Patent: October 17, 2000Assignee: Active Biotech ABInventors: Anders Bjork, Stig Jonsson, Tomas Fex, Gunnar Hedlund
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Patent number: 6133286Abstract: This invention relates to novel benzopyran and other benzo-fused leukotriene B.sub.4 (LTB.sub.4) antagonists and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds or a pharmaceutically acceptable salt thereof, and to methods of using such compounds as LTB.sub.4 antagonists. The compounds and the pharmaceutically acceptable salts of this invention inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders including rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, psoriasis and other skin disorders such as eczema, erythema, pruritus and acne, stroke and other forms of reperfusion injury, graft rejection, autoimmune diseases, asthma, and other conditions where marked neutrophil infiltration occurs.Type: GrantFiled: January 28, 2000Date of Patent: October 17, 2000Assignee: Pfizer Inc.Inventors: Mark A. Dombroski, Kevin Koch, Anthony D. Piscopio
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Patent number: 6127383Abstract: The 2-aryl-substituted pyridines are prepared by reacting pyridylaldehydes with organometallic compounds and then selectively reducing the products. The 2-aryl-substituted pyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of arteriosclerosis.Type: GrantFiled: December 21, 1998Date of Patent: October 3, 2000Assignee: Bayer AktiengesellschaftInventors: Gunter Schmidt, Rolf Angerbauer, Arndt Brandes, Michael Logers, Matthias Muller-Gliemann, Hilmar Bischoff, Delf Schmidt, Stefan Wohlfeil
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Patent number: 6121287Abstract: The invention is related to compounds of general formula (I) ##STR1## wherein R is Me, Et, n-Pr, iso-Pr, n-Bu, iso-Bu, sec.-Bu or allyl; R' is hydrogen, Me, MeO, fluoro, chloro, brorno, CF.sub.3, or OCH.sub.x F.sub.y ; R" is hydrogen or fluoro, with the proviso that R" is fluoro when R' is fluoro; and further when R' and R" are both hydrogen, R is not Me; R.sub.4 is selected from hydrogen and pharmaceutically acceptable inorganic and organic cations; R.sub.5 is selected from MeS, EtS, n-PrS, iso-PrS, MeSO, EtSO, MeSO.sub.2 and EtSO.sub.2 ; wherein x=0-2, y=1-3 with the proviso that x+y=3; and Me is methyl, Et is ethyl, Pr is propsy and Bu is butyl; and any tautomer, optical isomer and racemate thereof. The invention also relates to pharmaceutical compositions containing a compound of the general formula (I) together with a pharmaceutically acceptable carrier.Type: GrantFiled: July 14, 1999Date of Patent: September 19, 2000Assignee: Active Biotech ABInventors: Anders Bjork, Stig Jonsson, Tomas Fex, Gunnar Hedlund
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Patent number: 6114352Abstract: The present invention offers 7-aminoquinolinone derivatives, physiologically acceptable salts thereof, anti-allergic agents having as an active ingredient a 7-aminoquinolinone derivative or physiologically acceptable salt thereof, and 7-nitroquinolinone derivatives, wherein the 7-aminoquinolinone derivative is expressed by the following general formula (I): ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl group;R.sub.2 and R.sub.3 are mutually different groups, each of which is selected from among hydrogen atoms, acyl groups, alkyl groups or alkenyl groups; andR.sub.4 and R.sub.5 are mutually different or identical groups, each of which is selected from among hydrogen atoms, acyl groups, alkyl groups, alkenyl groups or aralkyl groups;and physiologically acceptable salts thereof.Type: GrantFiled: December 30, 1998Date of Patent: September 5, 2000Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Hidetsugu Takagaki, Masayoshi Abe, Mitsuru Sakai, Yasuo Aoki, Shigenori Nakanishi, Nobuyuki Kimura, Akihide Koda
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Patent number: 6093727Abstract: This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human a, adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the .alpha..sub.2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: October 20, 1998Date of Patent: July 25, 2000Assignee: Synaptic Pharmaceutical CorporationInventors: Wai C. Wong, Yoon T. Jeon, Charles Gluchowski
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Patent number: 6083943Abstract: A compound of the chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein Y is C.sub.2 -C.sub.4 alkylene; Z is a valence bond or C.sub.1 -C.sub.6 alkylene; R.sup.1 is substituted or unsubstituted aryl (e.g., phenyl and naphthyl) or heteroaryl (e.g., thienyl and furyl); R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.3 is hydrogen, hydroxy or the like; R.sup.4 is substituted or unsubstituted benzyl or the like. Typical examples are (2S*,3S*,4R*,5R*)-4-Carboxy-3-[N-(5-Isopropyl-2-methoxy-benzyl)amino]-5-me thyl-2-phenylpyrrolidine and (2S*,3S*,5S*)-5-Carboxy-3-[N-(2-methoxy-5-trifluoromethoxybenzyl)amino]-2- phenylpiperidine. The novel substituted azaheterocyclecarboxylic acids in this invention have excellent substance P antagonistic activity and are thus useful for the treatment of gastrointestinal disorders, central nervous system disorders, allergy, inflammatory diseases, asthma, pain, emesis or migraine in mammals, especially humans.Type: GrantFiled: March 19, 1999Date of Patent: July 4, 2000Assignee: Pfizer IncInventors: Masaya Ikunaka, Yuji Shishido, Masami Nakane
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Patent number: 6077851Abstract: The invention relates to compounds of general formula (I) ##STR1## wherein R is selected from ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl, sec.-butyl and allyl; R.sub.4 is selected from hydrogen and pharmaceutically acceptable inorganic and organic cations; R.sub.5 is selected from methyl, ethyl, n-propyl, iso-propyl, methoxy, ethoxy, chloro, bromo, CF.sub.3, and OCH.sub.x F.sub.y ; wherein x=0-2, y=1-3 with the proviso that x+y=3; R.sub.6 is hydrogen; or R.sub.5 and R.sub.6 taken together are methylenedioxy; and any tautomer hereof. The invention also relates to pharmaceutical compositions containing a compound of the general formula (I) together with a pharmaceutically acceptable carrier. Included are also processes for the preparation of the compounds of formula (I), as well as methods of treating mammals suffering from diseases resulting from autoimmunity and pathological inflammation by administering a compound having the formula (I) to said mammal.Type: GrantFiled: April 22, 1999Date of Patent: June 20, 2000Assignee: Active Biotech ABInventors: Anders Bjork, Stig Jonsson, Tomas Fex, Gunnar Hedlund
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Patent number: 6051583Abstract: The present invention relates to new substituted 2,3,3a,4,9,9a-hexahydro-8-hydroxy-1H-benz[f]indole derivatives, processes for preparing them and their use as pharmaceutical compositions.Type: GrantFiled: July 30, 1999Date of Patent: April 18, 2000Assignee: Boehringer Ingelheim Pharma KGInventors: Matthias Grauert, Christoph Hoenke, Adrian Carter, Wolf-Dietrich Bechtel, Thomas Weiser, Rainer Palluk, Uwe Pschorn
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Patent number: RE37729Abstract: 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: GrantFiled: February 3, 1999Date of Patent: June 4, 2002Assignee: Aventis Pharmaceuticals Inc.Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler