Plural Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 546/197)
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Patent number: 6433179Abstract: A process for producing a paroxetine represented by the following formula (4), which comprises reacting an N-alkylpiperidine represented by the following general formula (1) with a haloformic acid ester represented by the general formula (2) to prepare an alkoxycarbonylpiperidine represented by the general formula (3), and hydrolyzing the alkoxycarbonylpiperidine under alkaline conditions: wherein each of R1 and R2 is a lower alkyl group, a lower cycloalkyl group, an aralkyl group or CmF2m+1 (wherein m is an integer of from 1 to 6), and X is a halogen atom.Type: GrantFiled: May 21, 1997Date of Patent: August 13, 2002Assignee: Asahi Glass Company Ltd.Inventors: Shu-zhong Wang, Yasushi Matsumura
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Publication number: 20020103208Abstract: Compound of formula (I) 1Type: ApplicationFiled: August 21, 2001Publication date: August 1, 2002Inventors: Enzo Cereda, Luciano Maiocchi, Alessandro Brambilla, Ettore Giraldo, Giovanni Battista Schiavi
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Publication number: 20020099208Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.Type: ApplicationFiled: November 16, 2001Publication date: July 25, 2002Inventors: Kuo-Long Yu, Rita L. Civiello, Keith D. Combrink, Hatice Belgin Gulgeze, Ny Sin, Xiangdong Wang, Nicholas Meanwell, Brian Lee Venables, Yi Zhang, Bradley C. Pearce, Zhiwei Yin, Jan Willem Thuring
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Patent number: 6420415Abstract: Compounds represented by general formula (1) or salts thereof which have a matrix metalloprotease inhibitory activity and are useful as drugs, wherein the rings A and B represent each an optionally substituted homocycle or heterocycle, etc.; R1s are the same or different and each represents hydrogen, optionally substituted hydrocarbyl, acyl, etc.; X1 represents a bond, optionally substituted divalent aliphatic hydrocarbyl, etc.; X2 represents a bond, optionally substituted divalent aliphatic hydrocarbyl, —O—, etc.; Ys are the same or different represents hydrogen, optionally substituted hydrocarbyl, oxo, etc.; m is 0 or 1; n is an integer of 1 to 3; q1 is an integer of 1 to 2n+4; and q2 is an integer of 0 to 2n+3, provided that q1+q2 is 2n+4.Type: GrantFiled: March 20, 2001Date of Patent: July 16, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Toshiro Yamashita, Hiroshi Nara, Masayuki Takizawa, Koji Yoshimura
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Publication number: 20020072611Abstract: Compounds of Formula I are useful antipsychotic and antidepressant agents demonstrating potent inhibition of 5-HT reuptake and dopamine D2 receptor antagonism.Type: ApplicationFiled: December 12, 2000Publication date: June 13, 2002Inventors: Ronald J. Mattson, Joseph P. Yevich, Jun Yuan, Arlene S. Eison, Derek Denhart
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Publication number: 20020065419Abstract: Compound of formula (I): 1Type: ApplicationFiled: October 12, 2001Publication date: May 30, 2002Inventors: Jean-Louis Peglion, Jean-Paul Vilaine, Nicole Villeneuve, Catherine Thollon, Marie-Pierre Bourguignon, Christophe Poitevin
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Patent number: 6391882Abstract: A substituted 4-, 5-, 6-, and 7-indole derivative of Formula (I) wherein A is a group having formula (IIA), (IIB), (IIC) wherein X, U, Y, R3 to R12, Z, W, n and m are as defined above. The compounds are potent serotonin reuptake inhibitors and have 5-HT1A receptor antagonistic activity.Type: GrantFiled: February 2, 2001Date of Patent: May 21, 2002Assignee: H. Lundbeck A/SInventors: Ejner Knud Moltzen, Ivan Mikkelsen, Christian Korg-Jensen
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Publication number: 20020058679Abstract: A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor.Type: ApplicationFiled: August 27, 2001Publication date: May 16, 2002Inventors: Shin-Ichi Yokota, Kozo Yamamoto, Souichi Morikawa, Yoshihide Fuse, Mikio Kitahara
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Patent number: 6387931Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diType: GrantFiled: October 12, 2001Date of Patent: May 14, 2002Assignee: Pfizer INCInventors: Kevin Neil Dack, Gavin Alistair Whitlock
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Patent number: 6372762Abstract: The present invention relates to compounds of the formula and the pharmaceutically acceptable salts and solvates thereof wherein X1, X2, X3, R1, R2, R3 and R4 are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods of treating shizophrenic and shizo-affective disorders, and related disorders which may be treated by administering compounds having dopaminergic activity such as the above compounds of formula 1.Type: GrantFiled: April 27, 1999Date of Patent: April 16, 2002Assignee: Pfizer Inc.Inventors: Anton Franz Joseph Fliri, Todd William Butler
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Publication number: 20020042430Abstract: This invention concerns the compounds of formula 1Type: ApplicationFiled: August 20, 2001Publication date: April 11, 2002Inventors: Jean-Paul Rene Marie Bosmans, Christopher John Love, Marc Gustaaf Celine Verdonck, Joannes Adrianus Jacobus Schuurkes
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Patent number: 6369074Abstract: The present invention relates to novel aminomethylene substituted non-aromatic heterocycles and, specifically, to compounds of the formula wherein W, R1, R2, R3, A, X′, Y′ and Z′ are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formulae Ia and Ib are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.Type: GrantFiled: October 1, 1999Date of Patent: April 9, 2002Assignee: Pfizer Inc.Inventors: Harry R. Howard, Brian T O'Neill
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Publication number: 20020035130Abstract: Piperidine compounds, processes for preparing them, pharmaceutical compositions comprising them and their use in therapy are disclosed.Type: ApplicationFiled: September 21, 2001Publication date: March 21, 2002Applicant: SmithKline Beecham p.l.c.Inventors: Andrew Simon Craig, Victor Witold Jacewicz, Michael Urquhart
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Patent number: 6358979Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R3, R4, R5, R6, R7, R8, X, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.Type: GrantFiled: June 8, 2000Date of Patent: March 19, 2002Assignee: Merck & Co., Inc.Inventors: Paul E. Finke, Kerry A. Hilfiker, Malcolm MacCoss, Kevin T. Chapman, Jennifer L. Loebach, Sander G. Mills, Ravi N. Guthikonda, Shrenik K. Shah, Dooseop Kim, Dong-Ming Shen, Bryan Oates
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Patent number: 6358980Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.Type: GrantFiled: January 27, 2000Date of Patent: March 19, 2002Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, Aranapakam M. Venkatesan, James M. Chen, Arie Zask, Vincent P. Sandanayaka, Mila T. Du, Jannie L. Baker
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Publication number: 20020028832Abstract: This invention provides compounds of Formula I having the structure 1Type: ApplicationFiled: July 12, 2001Publication date: March 7, 2002Applicant: American Home Products CorporationInventors: Mark A. Ashwell, William R. Solvibile, Dominick A. Quagliato, Albert J. Molinari
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Publication number: 20020028942Abstract: Paroxetine hydrochloride is obtained in an easily soluble form suitable for preparing stable aqueous solutions, suitable for parenteral use, by freeze-drying solutions prepared by dissolving paroxetine free base in aqueous hydrochloric acid, or of paroxetine hydrochloride hemihydrate or other hydrate/solvate/amorphous forms of paroxetine hydrochloride.Type: ApplicationFiled: August 8, 2001Publication date: March 7, 2002Inventors: Victor Witold Jacewicz, Neal Ward
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Patent number: 6353010Abstract: Compounds of the formula (i) have therapeutic utility via inhibition of TNF or phosphodiesterase.Type: GrantFiled: October 21, 1999Date of Patent: March 5, 2002Assignee: Darwin Discovery, Ltd.Inventors: Hazel Joan Dyke, John Gary Montana
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Patent number: 6353099Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.Type: GrantFiled: August 17, 2000Date of Patent: March 5, 2002Assignee: Merck & Co., Inc.Inventors: Stephen E. DeLaszlo, William K. Hagmann, Theodore M. Kamenecka
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Publication number: 20020019386Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof:Type: ApplicationFiled: August 27, 2001Publication date: February 14, 2002Applicant: SmithKline Beecham p.l.c.Inventors: Francis David King, Laramie Mary Gaster, Keith Raymond Mulholland
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Publication number: 20020019401Abstract: The present invention relates to compounds of the formula 1Type: ApplicationFiled: September 27, 2001Publication date: February 14, 2002Inventors: Anton Franz Joseph Fliri, Todd William Butler
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Patent number: 6340704Abstract: The present invention provides a compound represented by the formula: wherein R1 is an amino group which may be substituted; R2 is a hydrogen atom or a lower alkyl group which may be substituted; X is a methyne group which may be substituted or N(O)m (m is 0 or 1); a ring A is a homo- or hetero-cycle which is substituted by a halogen atom, lower alkyl, lower alkoxy or lower alkylenedioxy; and a ring B is a homo- or hetero-cycle which may be substituted; or a salt thereof, which exhibits excellent cell differentiation-inducing action and cell differentiation-inducing factor action-enhancing action, and is useful in the treatment and prevention of various nerve diseases or bone/joint diseases.Type: GrantFiled: July 19, 1999Date of Patent: January 22, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Shogo Marui, Masatoshi Hazama, Kohei Notoya, Koki Kato
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Publication number: 20020002184Abstract: Paroxetine hydrochloride is obtained in a free-flowing and easily soluble form (suitable for preparing solid formulations or aqueous solutions, suitable for parenteral use) by spry-drying solutions of paroxetine hydrochloride hemihydrate or other anhydrate/hydrate/solvate/amorphous forms.Type: ApplicationFiled: August 9, 2001Publication date: January 3, 2002Applicant: SmithKline Beecham plcInventors: Victor Witold Jacewicz, Neal Ward
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Patent number: 6331544Abstract: The present invention relates to substituted indane or dihydroindole compounds of Formula (I), wherein A and B are independently O or S; D is an optionally substituted methylene group; X is N or optionally substituted C; and W is a spacer group. The compounds are either selective dopamine D4 ligands or they have combined effects at dopamine D4 and serotonergic receptors and/or the serotonergic transporter. These compounds are therefore useful in the treatment of certain psychiatric and neurologic disorders, including psychosis, depression and anxiety.Type: GrantFiled: August 3, 1999Date of Patent: December 18, 2001Assignee: H. Lundbeck A/SInventors: Jens Kristian Perregaard, Ivan Mikkelsen, Henrik Pedersen
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Publication number: 20010049442Abstract: Paroxetine hydrochloride is obtained in a free-flowing and easily soluble form (suitable for preparing solid formulations or aqueous solutions, suitable for parenteral use) by spray-drying solutions of paroxetine hydrochloride hemihydrate or other anhydrate/hydrate/solvate/amorphous forms.Type: ApplicationFiled: August 3, 2001Publication date: December 6, 2001Applicant: SmithKline Beecham p.l.c.Inventors: Victor Witold Jacewicz, Neal Ward
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Patent number: 6326496Abstract: A process for the preparation of a compound of formula I in which R1 represents an amine protecting group wherein a compound of formula II in which R1 is as defined above is reduced by a metal hydride in the presence of an inorganic salt in the presence of a diluent.Type: GrantFiled: November 15, 1999Date of Patent: December 4, 2001Assignee: Knoll AktiengesellschaftInventor: James Patrick Brennan
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Patent number: 6323206Abstract: Disclosed is a method of treating a subject with a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to the subject a therapeutically effective amount of a compound represented by the following structural formula: and physiologically acceptable salts thereof.Type: GrantFiled: January 21, 1998Date of Patent: November 27, 2001Assignee: Millennium Pharmaceuticals, Inc.Inventors: Charles F. Schwender, Charles R. Mackay, Julia C. Pinto, Walter Newman
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Patent number: 6316468Abstract: 3-(Piperidin-4-yl)-1H-indole derivatives bearing an optionally substituted phenyl moiety at the 2-position of the indole ring system and an alkyl or aryl-alkyl substituent on the nitrogen atom of the piperndine ring are selective antagonists of the human 5-HT2A receptor. They are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including psychotic disorders such as schizophrenia.Type: GrantFiled: March 1, 2000Date of Patent: November 13, 2001Assignee: Merck Sharp & Dohme Ltd.Inventors: Robert James Maxey, Michael Rowley, Monique Bodil Van Niel
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Patent number: 6310246Abstract: Herbicidal fluorovinyloxyacetamide compounds of formula (I) are useful for protecting crops from weeds: wherein: R1 is a phenyl group optionally having one or more substituents selected from the group consisting of C1-6 alkyl, halogen-substituted C1-6 alkyl, C1-6 alkoxy and halogen; R2 is a C1-6 alkyl; or R1 and R2 together with the nitrogen atom to which they are bound form a 5-, 6- or 7-membered nitrogen heterocycle optionally having one or more ring oxygen atoms, double bonds and C1-6 alkyl substituents; R3 is a phenyl or thiophen-2-yl group optionally having one or more substituents selected from the group consisting of C1-6 alkyl, halogen-substituted C1-6 alkyl, C1-6 alkoxy, methylenedioxy and halogen; and R4is a perfluoro C1-6 alkyl group.Type: GrantFiled: August 14, 2000Date of Patent: October 30, 2001Assignee: Korea Research Institute of Chemical TechnologyInventors: Bum-Tae Kim, No-Kyun Park, Kyung-Sik Hong, Jae-Eup Park, Yong-Woong Kwon
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Patent number: 6306859Abstract: Compounds of the Formula (I) wherein R2, Y, X and n are as defined in the specification which compounds are useful in the treatment of disorders associated with serotonergic neuron-related diseases.Type: GrantFiled: March 1, 2000Date of Patent: October 23, 2001Assignee: American Home Products CorporationInventors: Wayne E. Childers, Michael G. Kelly, Gan Zhang, Yvette L. Palmer, Edward J. Podlesny
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Patent number: 6307051Abstract: New compounds of formula I wherein: R and R1 are independently selected from hydrogen, (C1-C6)alkyl, styryl and (C3-C6)cycloalkyl or, taken together with the carbon to which they are linked, form a (C3-C6)cycloalkyl group; A is selected from the following groups: —CH2C≡CCH2—, or —(CH2)q—NH—(CH2)q—, wherein q is an integer from 2 to 3 B is selected from T is selected from —CH2—C≡CH, —C≡CH, —(CH2)p—R3, —CH═CH—R3, —CH2—NHCO—R3, —(CH2)p—O—R3, —CH(NH2)—CH2R3, in which p is 0 or an integer from 1 to 4, R3 is a carbocyclic or heterocyclic ring as medicaments having antitumor and/or antimetastatic activities.Type: GrantFiled: January 31, 2000Date of Patent: October 23, 2001Assignee: Roche Diagnostics GmbHInventors: Walter-Gunar Friebe, Bernhard Koenig, Hans-Willi Krell, Sabine Woelle
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Patent number: 6303627Abstract: This invention provides compounds and a method for the inhibition of serotonin reuptake in mammals.Type: GrantFiled: June 3, 1999Date of Patent: October 16, 2001Assignee: Eli Lilly and CompanyInventors: Daniel James Koch, Vincent Patrick Rocco
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Patent number: 6303620Abstract: Disclosed are 4,4-disubstituted and 3,3-disubstituted piperidine compounds of formula I wherein D, E, G, J, R1, a, b, c, and d are defined in the specification, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.Type: GrantFiled: May 6, 1999Date of Patent: October 16, 2001Assignee: Novo Nordisk A/SInventors: Thomas Kruse Hansen, Michael Ankersen
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Publication number: 20010023253Abstract: Piperidine compounds, processes for preparing them, pharmaceutical compositions comprising them and their use in therapy are disclosed.Type: ApplicationFiled: March 14, 2001Publication date: September 20, 2001Applicant: SmithKline Beecham p.l.c.Inventors: Andrew Simon Craig, Victor Witold Jacewicz, Michael Urquhart
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Patent number: 6291481Abstract: Compounds of formula I the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the substituents are as described in the specification, and process for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.Type: GrantFiled: August 27, 1998Date of Patent: September 18, 2001Assignee: Janssen Pharmaceutica, N.V.Inventors: Jean-Paul René Marie Bosmans, Christopher John Love, Marc Gustaaf Celine Verdonck, Joannes Adrianus Jacobus Schuurkes
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Publication number: 20010021776Abstract: A method of producing amorphous paroxetine hydrochloride, which comprises converting paroxetine or its lower alkanoic acid salt into paroxetine hydrochloride and then spray drying a solution of the hydrochloride.Type: ApplicationFiled: May 4, 2001Publication date: September 13, 2001Applicant: Asahi Glass Company, Ltd.Inventors: Shu-Zhong Wang, Takashi Okazoe, Yasushi Matsumura
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Patent number: 6288234Abstract: Disclosed are multibinding compounds which inhibit microsomal triglyceride transferase protein (MTP), a protein which mediates the transfer of lipids during the assembly of lipoproteins and related biomolecules. The multibinding compounds contain from 2 to 10 ligands covalently attached to one or more linkers. The multibinding compounds of this invention are useful for lowering serum lipid, cholesterol and/or triglyceride levels, and for preventing and treating disorders associated with hyperlipemia, hyperlipidemia, hyperlipoproteinemia, hypercholestrolemia, hypertriglyceridemia and the like, such atherosclerosis.Type: GrantFiled: June 4, 1999Date of Patent: September 11, 2001Assignee: Advanced Medicine, Inc.Inventor: John H. Griffin
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Patent number: 6284774Abstract: Novel 4-Benzyl piperidine alkylsulfoxide heterocycles are disclosed and their use as subtype selective NMDA receptor antagonists, particularly for the treatment of Parkinson's disease, most preferably in combination with L-DOPA.Type: GrantFiled: October 31, 2000Date of Patent: September 4, 2001Assignee: Warner-Lambert CompanyInventors: Jonathan L. Wright, Suzanne Ross Kesten, Ravindra B. Upasani, Nancy C. Lan
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Patent number: 6281229Abstract: A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor. The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an inhibitor of inducing the production of a protein regulated by HSF, which inhibits the activity of a heat shock factor, a transcriptional regulatory factor, thereby in turn inhibiting transcription of a structural gene having a heat shock element sequence in the gene region for transcriptional regulation into RNA, and thus inhibiting translation of the gene into a protein, and resulting in inhibition of inducing production of RNA or protein encoded by the gene. It also provides a drug for treating or preventing cancer through thermotherapy and a drug for treating or preventing stress diseases such as depression.Type: GrantFiled: March 27, 2000Date of Patent: August 28, 2001Assignee: Kaneka CorporationInventors: Shin-ichi Yokota, Kozo Yamamoto, Souichi Morikawa, Yoshihide Fuse, Mikio Kitahara
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Publication number: 20010008940Abstract: Non-crystalline paroxetine hydrochloride is prepared by precipitation of the same as a solid from a solution of paroxetine hydrochloride, or by drying an oil containing paroxetine hydrochloride, or by removing water/solvent from a hydrate/solvate. The oil may also be obtained by precipitation from a solution of paroxetine hydrochloride.Type: ApplicationFiled: January 12, 2001Publication date: July 19, 2001Applicant: SmithKline Beecham plcInventors: Andrew Simon Craig, Victor Witold Jacewicz
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Patent number: 6239168Abstract: Radicicol derivatives represented by the following formula (I) having tyrosine kinase inhibition activity or pharmacologically acceptable salts thereof: wherein R1 and R2 are the same or different, and each represents hydrogen, alkanoyl, alkenoyl, tert-butyldiphenylsilyl or tert-butyldimethylsilyl; R3 represents Y—R5 {wherein Y represents substituted or unsubstituted alkylene; and R5 represents CONR6R7 (wherein R6 represents hydrogen, hydroxyl, substituted or unsubstituted lower alkyl, substituted or unsubstituted higher alkyl; R7 represents hydroxyl, substituted lower alkyl), CO2R12 (wherein R12 represents substituted lower alkyl, substituted or unsubstituted higher alkyl, X represents halogen.Type: GrantFiled: February 25, 2000Date of Patent: May 29, 2001Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yoji Ino, Nobuyoshi Amishiro, Mayumi Miyata, Chikara Murakata, Harumi Ogawa, Tadakazu Akiyama, Shiro Akinaga, Shiro Soga, Yukimasa Shiotsu
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Patent number: 6225324Abstract: Compounds of formula I are useful antidepressant agents demonstrating potent inhibition of 5-HT reuptake. Z is selected from among various phenyl and hetaryl moieties while Y is benzyl or indolyl.Type: GrantFiled: December 21, 1999Date of Patent: May 1, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Michael A. Poss, David R. Tortolani, Ronald J. Mattson, Joseph P. Yevich
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Patent number: 6218405Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof in which A is methylene or —O—; B is methylene or —O—; G1—G2—G3 form a heteroaromatic or heteroaliphatic chain; g is 0, 1 or 2; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T is an optionally substituted aryl or heteroaryl group, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendrocrine syType: GrantFiled: June 16, 1999Date of Patent: April 17, 2001Assignee: KNOLL AktiengesellschaftInventors: Alan Martin Birch, Paul Anthony Bradley
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Patent number: 6201004Abstract: Compounds of formula I and pharmaceutically acceptable salts thereof in which A is methylene or —O—; B is methylene or —O—; G1—G2—G3 form a heteroaromatic or heteroaliphatic chain; g is 0, 1 or 2; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T is an optionally substituted aryl or heteroaryl group, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neType: GrantFiled: September 1, 1999Date of Patent: March 13, 2001Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, Paul Anthony Bradley
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Patent number: 6194448Abstract: A method for the inhibition of the binding of &agr;4&bgr;1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of diseases states in which &agr;4&bgr;1 is involved.Type: GrantFiled: October 14, 1999Date of Patent: February 27, 2001Assignee: Texas Biotechnology CorporationInventors: Ronald J. Biediger, Vanessa O. Grabbe, George W. Holland, Jamal M. Kassir, Timothy P. Kogan, Shuqun Lin, Robert V. Market, Bore G. Raju, Ian L. Scott, Chengde Wu
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Patent number: 6187792Abstract: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.Type: GrantFiled: March 5, 1998Date of Patent: February 13, 2001Assignee: Astra Pharma Inc.Inventors: Daniel Delorme, Edward Roberts, Zhongyong Wei
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Patent number: 6184234Abstract: Compounds of the following structure, the corresponding N-oxides and agriculturally acceptable salts thereof, are disclosed as effective insecticides: wherein U is —(CH2)n—; Q is hydroxy; and R is: and wherein V, W, Y, and Z are each hydrogen; X is a five- or six-membered heterocycle; optionally substituted with bromine, chlorine, fluorine, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkoxyalkyl, haloalkoxyalkyl, or aminocarbonyl; and the heterocycle is optionally connected to the phenyl ring through a —O—, —S—, —(CH2)p, —C(O)—, or —O—(CR3R4)q linkage; R1 and R2 are independently selected from phenyl or pyridyl substituted with pentahalothio, haloalkylthio, haloalkylsulfinyl, or haloalkylsulfonyl; phenyl substituted with —OC(M)2O—, where M is bromine, chorine or fluorine, to provide a dihalobenzodioxolyl fused ring; or pyridyl substituted with —OC(M)2O— to provide a dihalodioxolType: GrantFiled: October 7, 1999Date of Patent: February 6, 2001Assignee: FMC CorporationInventors: Ian R. Silverman, Daniel H. Cohen, John W. Lyga, Steven W. Szczepanski, Syed F. Ali, Thomas G. Cullen, Robert N. Henrie, II, Clinton J. Peake
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Patent number: 6166011Abstract: Compounds of formula (I), their salts and solvates, wherein the substituents are as described herein, are FKBP inhibitors.Type: GrantFiled: July 15, 1999Date of Patent: December 26, 2000Assignee: Pfizer IncInventors: Martin J. Wythes, Michael J. Palmer, Mark I. Kemp, Malcolm C. MacKenny, Robert J. Maguire, James F. Blake, Jr.
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Patent number: 6166036Abstract: Described is an Lp(a) lowering agent or an apo(a) formation suppressing agent, which comprises as an effective ingredient a phenylcarboxylic acid derivative represented by the following formula (1): (wherein, R.sup.1 represents a phenyl group which may have a substituent, A represents a lower alkylene or lower alkyleneoxy group, B represents a methylene or carbonyl group, D represents a lower alkylene group, E represents a lower alkylene or lower alkenylene group, R.sup.2 represents a hydrogen atom or a lower alkyl group and 1, m and n each stands for 0 or 1), or salt thereof. The agent is capable of lowering the blood level of Lp(a) significantly while hardly causing side effects.Type: GrantFiled: October 22, 1999Date of Patent: December 26, 2000Assignee: Taiho Pharmaceutical Co., Ltd.Inventor: Akira Yamamoto
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Patent number: 6159995Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: December 12, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen