Nitrogen Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 514/426)
-
Publication number: 20020037915Abstract: Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I 1Type: ApplicationFiled: September 26, 2001Publication date: March 28, 2002Applicant: 3-Dimensional Pharmaceuticals, Inc.Inventors: Carl R. Illig, Nalin L. Subasinghe, James B. Hoffman, Kenneth J. Wilson, M. Jonathan Rudolph, Roger F. Bone, Scott L. Klein, Troy L. Randle
-
Patent number: 6358945Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: GrantFiled: February 16, 2000Date of Patent: March 19, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Steffen Breitfelder, Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, John R. Proudfoot, John R. Regan, Alan D. Swinamer, Hidenori Takahashi
-
Publication number: 20020028797Abstract: This invention provides compounds of Formula I having the structure 1Type: ApplicationFiled: July 12, 2001Publication date: March 7, 2002Applicant: American Home Products CorporationInventors: Fuk-Wah Sum, Michael S. Malamas
-
Patent number: 6353016Abstract: The invention is directed to a pharmaceutical composition comprising a pyrrole derivative of the following formula [1] or its pharmaceutically acceptable salt as an active ingredient. (wherein R1 represents hydrogen or alkoxycarbonylamino; R2 represents alkyl, aryl which may be substituted, a aromatic heterocyclyl which may be substituted, unsubstituted amino, monoalkyl-substituted amino, dialkyl-substituted amino, or cyclic amino which may be substituted; R3 represents cyano or carbamoyl; R4 represents hydrogen or alkyl; E represents alkylene; q represents 0 or 1; A represents methyl, aryl which may be substituted, or a aromatic heterocyclyl which may be substituted). This pharmaceutical composition is useful as a potassium channel activator.Type: GrantFiled: June 29, 2000Date of Patent: March 5, 2002Assignee: Nippon Shinyaku Co., Ltd.Inventors: Mitsushi Tanaka, Masami Tsuda, Ayatsugu Nakamura
-
Patent number: 6350761Abstract: This invention is directed to benzenamine derivatives of formula (I): wherein A, W, m, n, R1, R2, R3, R4, R5 and R6 are defined herein. These compounds are useful as anti-coagulants.Type: GrantFiled: July 24, 2000Date of Patent: February 26, 2002Assignee: Berlex Laboratories, Inc.Inventors: William J. Guilford, Steven T. Sakata, Kenneth J. Shaw, Shung Wu, Wei Xu, Zuchun Zhao
-
Patent number: 6348465Abstract: The present invention relates to methods of treating an individual with diabetes mellitus by administering to said individual an effective amount of copper chelators, hydrazine compounds, and/or substrate analogues. The invention also relates to methods of treating an individual with diabetes mellitus by lessening frictosamine odixase activity in said individual. Provided within is disclosure pertaining to treatment, pharmaceutical compositions, dosage ranges, and uses of frictosaminc oxidase enzyme inhibitors to lessen fructosamine oxidase activity.Type: GrantFiled: September 27, 2000Date of Patent: February 19, 2002Assignee: Protemix Corporation LimitedInventor: John Richard Baker
-
Publication number: 20020016326Abstract: The present application describes nitrogen containing heteroaromatics with ortho-substituted P1's and derivatives thereof of formula I: 1Type: ApplicationFiled: April 12, 2001Publication date: February 7, 2002Inventors: Robert A. Galemmo, Lori L. Bostrom, Donald J.P. Pinto, Karen A. Rossi
-
Publication number: 20020013310Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.Type: ApplicationFiled: July 30, 2001Publication date: January 31, 2002Inventors: Yong Mi Choi-Sledeski, Heinz W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong, Julian Levell
-
Patent number: 6342518Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist and an arylpyrrole insecticide. Also provided are methods for synergistic insect control and crop protection.Type: GrantFiled: March 9, 2000Date of Patent: January 29, 2002Assignee: BASF AktiengesellschaftInventors: Michael Frank Treacy, Raymond Frank Borysewicz, Paul E. Rensner
-
Publication number: 20020010199Abstract: 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: ApplicationFiled: May 21, 2001Publication date: January 24, 2002Inventors: William K. Hagmann, George A. Doherty, Shrenik Shah
-
Patent number: 6329373Abstract: A compound of formula (I) wherein X is a —CONHOH group and the R groups are defined in the claims. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation and inhibitors of the release of tumour necrosis factor from cells.Type: GrantFiled: January 7, 2000Date of Patent: December 11, 2001Assignee: British Biotech Pharmaceuticals, Ltd.Inventors: Fionna Mitchell Martin, Christopher Norman Lewis, Mark Whittaker
-
Publication number: 20010046975Abstract: A method of controlling Take-all disease of plants by applying, preferably to the seed prior to planting, a fungicide of the formula 1Type: ApplicationFiled: May 9, 2001Publication date: November 29, 2001Applicant: Monsanto CompanyInventors: Dennis Paul Phillion, Diane Susan Braccolino, Matthew James Graneto, Wendell Gary Phillips, Karey Alan Van Sant, Daniel Mark Walker, Sai Chi Wong
-
Patent number: 6316467Abstract: Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the “good” cholesterol and as such may be useful for treating diseases such as atherosclerosis.Type: GrantFiled: November 16, 1998Date of Patent: November 13, 2001Assignee: American Home Products CorporationInventor: Thomas J. Commons
-
Patent number: 6312709Abstract: Seaweed supplement is included in diet of mammals and poultry to enhance immune response. In one embodiment, pasture forage is treated with seaweed supplement. When cattle or lambs are grazed on seaweed supplement treated endophyte-infected forage, immune function is preserved or depressed immune function is reversed. The enhanced immune function continues to the feedlot finishing phase even though no seaweed supplement is fed in that phase. In an independently inventive embodiment, seaweed supplement is administered to pigs exposed to PRRS disease to impart resistance to said disease and improve performance. In still another independently inventive embodiment, seaweed supplement is administered to lactating mares prior to weaning to mitigate the stress of weaning.Type: GrantFiled: May 18, 2000Date of Patent: November 6, 2001Assignees: Texas Tech University, Virginia Tech Intellectual Properties, Inc.Inventors: Vivien Gore Allen, Kevin R. Pond, Korinn E. Saker, Joseph P. Fontenot
-
Patent number: 6310083Abstract: Derivatives of o-nitromandelyoxycarbonyl (Nmoc) which are capable of releasing an amino acid (or derivative thereof), upon irradiation with ultraviolet (UV) light are disclosed, as well as a method for producing a free amino acid (or derivative thereof) employing the same, e.g., to study neurophysiology.Type: GrantFiled: December 21, 1998Date of Patent: October 30, 2001Assignee: University of Maryland Boitechnology InstituteInventors: Joseph P.Y. Kao, Francis M. Rossi
-
Publication number: 20010031781Abstract: The present invention is directed to compounds of Formula I: wherein X is O, S or NR7 and R1-R7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain of the compounds exhibit direct, selective inhibition of urokinase, or are intermediates useful for forming compounds having such activity.Type: ApplicationFiled: April 10, 2001Publication date: October 18, 2001Inventors: Carl R. Illig, Nalin L. Subasinghe, James B. Hoffman, Kenneth J. Wilson, M. Jonathan Rudolph, Juan J. Marugan
-
Patent number: 6300366Abstract: Compound of formula (I): in which: n is 1 or 2, X represents alkylene, alkenylene, alkynylene or optionally substituted arylene or heteroarylene, R10 represents hydrogen or alkyl and R11 and R12 together form a bond, or alternatively R12 represents hydrogen or alkyl and R10 and R11 together form a bond, R2, R3 and R4 each independently of the others represents hydrogen, alkyl, hydroxyalkyl, alkoxy, alkoxycarbonyl, aryl, arylalkyl or aryloxyalkyl, or two of R2, R3 and R4 form a cycloalkyl radical. Medicinal products containing the same are useful in the treatment of cardiovascular diseases.Type: GrantFiled: November 16, 2000Date of Patent: October 9, 2001Assignee: Adir et CompagnieInventors: Pascal Bousquet, Jean-Daniel Ehrhardt, VĂ©ronique Bruban, Josiane Feldman, Stephan Schann, Elisabeth Scalbert, Bruno Pfeiffer, Pierre Renard
-
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
-
Patent number: 6262090Abstract: Compounds of the formula wherein A is heteroaryl; R9-R12 are independently hydrogen, alkyl of 1 to 4 carbon atoms, perhaloalkyl of 1 to 4 carbon atoms, halogen, alkoxy of 1 to 4 carbon atoms, or cyano, or R9 and R10 or R11 and R12 may be taken together to form aryl of 5 to 7 carbon atoms; W is O, NR6, or is absent; G is aryl or heteroaryl; and X is a bond X is a bond, —NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 carbon atoms, or (CH)J; and J is alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or benzyl; and n is an integer from 1 to 6; or a pharmaceutical acceptable salt thereof, useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.Type: GrantFiled: November 22, 1999Date of Patent: July 17, 2001Assignee: American Home Products CorporationInventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
-
Patent number: 6262101Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor &agr;, nuclear factor &kgr;B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovis replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.Type: GrantFiled: August 16, 2000Date of Patent: July 17, 2001Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
-
Patent number: 6258822Abstract: Compounds having the formula are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions and a method of inhibiting urokinase in a mammal.Type: GrantFiled: August 6, 1998Date of Patent: July 10, 2001Assignee: Abbott LaboratoriesInventors: Andrew G. Geyer, William J. McClellan, Todd W. Rockway, Kent D. Stewart, Moshe Weitzberg, Michael D. Wendt
-
Patent number: 6251919Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, epilepsy, asthma, amyotrophic lateral sclerosis, or pain and to pharmaceutical compositions that contain the compounds of Formula I.Type: GrantFiled: June 14, 1999Date of Patent: June 26, 2001Assignee: Warner-LambertInventors: Lain-Yen Hu, Michael Francis Rafferty, Todd Robert Ryder
-
Patent number: 6235778Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R114 R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and mare set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: November 26, 1997Date of Patent: May 22, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
-
Patent number: 6180095Abstract: The present invention is directed to double prodrugs containing polymeric-based transport forms.Type: GrantFiled: October 30, 1998Date of Patent: January 30, 2001Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Annapurna Pendri, Yun H. Choe
-
Patent number: 6177408Abstract: A compound which is a distamycin derivative of formula (I), wherein n is 2, 3 or 4; R0is C1-C4 alkyl or C1-C3 haloalkyl; R1 and R2, which may be the same or different, are each hydrogen, C1-C4 alkyl optionally substituted by one or more fluorine atoms, or C1-C4 alkoxy; X is a halogen atom; B is selected from (A, B, C, D, E, F, G, H, I, J and K); wherein R3, R4, R5, R6, R7, R8, and R9, which may be the same or different, are each hydrogen or C1-C4 alkyl, and m is 0, 1, or 2; or a pharmaceutically acceptable salt thereof. Such compounds are useful as antineoplastic and antiviral agents.Type: GrantFiled: November 13, 1998Date of Patent: January 23, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Paolo Cozzi, Italo Beria, Marina Caldarelli, Maria Cristina Geroni, Enrico Pesenti
-
Patent number: 6162815Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds having the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## which are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders are provided. In particular, based on their RXR-agonist activity, these compounds may be used to treat noninsulin-dependent diabetes mellitus (NIDDM) and obesity.Type: GrantFiled: September 10, 1998Date of Patent: December 19, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
-
Patent number: 6162927Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.Type: GrantFiled: August 4, 1997Date of Patent: December 19, 2000Assignee: Abbott LaboratoriesInventors: Martin Winn, Steven A. Boyd, Charles W. Hutchins, Hwan-Soo Jae, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Bryan K. Sorensen, Bruce G. Szczepankiewicz, Kenneth J. Henry, Gang Liu, Steven J. Wittenberger, Steven A. King
-
Patent number: 6156784Abstract: Disclosed are compositions containing compounds of the formula (I) below wherein A,B,C,G,Q and R are defined herein. The compounds are useful as phosphotyrosine mimics that, when incorporated into an appropriate molecular structure, inhibit the binding of tyrosine kinase-dependent regulatory proteins to their native phosphotyrosine-containing ligands or receptors. Also disclosed are methods for preparing the compounds of the formula (I).Type: GrantFiled: December 7, 1999Date of Patent: December 5, 2000Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rajashekhar Betageri, Jean-Marie Ferland, Montse Llinas-Brunet, Neil Moss, John R. Proudfoot
-
Patent number: 6153626Abstract: Compounds of general formula (I) ##STR1## wherein m is 0 or 1, and n is 1 or 2; 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 3, 1998Date of Patent: November 28, 2000Assignee: Astra Pharma Inc.Inventors: Benjamin Pelcman, Edward Roberts
-
Patent number: 6140350Abstract: A method for controlling ectoparasites systemically through host animal blood which comprises administering at least one neonocotinoid compound among those defined in the specification to the host animal.Type: GrantFiled: April 23, 1999Date of Patent: October 31, 2000Assignee: Sumitomo Chemical Company, LimitedInventor: Satoshi Sembo
-
Patent number: 6140321Abstract: Donepezil hydrochloride, 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride, is provided here in the form of four polymorphs which are stable against heat and humidity in the pharmaceutical use. They can be industrially produced. They are specified by peaks in X-ray powder diffraction pattern and absorption peaks in infrared absorption spectra in potassium bromide.Type: GrantFiled: December 30, 1996Date of Patent: October 31, 2000Assignee: Eisai Co., Ltd.Inventors: Akio Imai, Hideaki Watanabe, Takashi Kajima, Yasushi Ishihama, Akiyo Ohtsuka, Tomohide Tanaka
-
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
-
Patent number: 6110958Abstract: Compounds of formula (I) ##STR1## wherein the substituents are as defined herein, are antiparasitic agents.Type: GrantFiled: December 1, 1999Date of Patent: August 29, 2000Assignee: Pfizer Inc.Inventors: Bernard Joseph Banks, Nathan Anthony Logan Chubb
-
Patent number: 6075023Abstract: Fish mycoses and single-cell ectoparasites on fish are controlled using an active compound suitable for inhibiting the mitochondrial respiratory chain at the stage of the b/c.sub.1 complex.Type: GrantFiled: February 17, 1998Date of Patent: June 13, 2000Assignee: BASF AktiengesellschaftInventors: Gerhard Peter Dohmen, Christoph Kunast, Reinhart Munk, Gerhard Rothhaas
-
Patent number: 6057342Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: July 7, 1997Date of Patent: May 2, 2000Assignee: Dupont Pharmaceutical Co.Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
-
Patent number: 6051593Abstract: The present invention relates to novel 3-(cycloalkanoheteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.Type: GrantFiled: June 19, 1998Date of Patent: April 18, 2000Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
-
Patent number: 6051243Abstract: Novel pharmaceutically/cosmetically-active polyaromatic amides have the structural formula (I): ##STR1## wherein Z is a radical --CO--NH-- or --NH--CO--,and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: November 13, 1997Date of Patent: April 18, 2000Assignee: Centre International de Recherches DermatologiquesInventor: Jean-Michel Bernardon
-
Patent number: 6034093Abstract: The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.Type: GrantFiled: August 6, 1998Date of Patent: March 7, 2000Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: William R. Ewing, Michael R. Becker, Yong Mi Choi-Sledeski, Heinz W. Pauls, Daniel G. McGarry, Roderick S. Davis, Alfred P. Spada
-
Patent number: 6015569Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: November 17, 1997Date of Patent: January 18, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
-
Patent number: 5998459Abstract: The invention relates to a pharmaceutical composition comprising a pyrrole derivative of the following formula [1] or a pharmaceutically acceptable salt thereof, or a solvate of either of them, as an active ingredient. ##STR1## (wherein R.sup.1 represents hydrogen or alkoxycar91 bonylamino, R.sup.2 represents alkyl, aryl which may be substituted, aromatic heterocyclyl which may be substituted, unsubstituted amino, monoalkylamino, dialkylamino, or cyclic amino which may be substituted; R.sup.3 represents cyano or carbamoyl; R.sup.4 represents hydrogen or alkyl; E represents alkylene; q is equal to 0 or 1, A represents methyl, aryl which may be substituted, or aromatic heterocyclyl which may be substituted). The pharmaceutical composition of the invention is effective for the treatment of pollakiuria or urinary incontinence.Type: GrantFiled: December 8, 1997Date of Patent: December 7, 1999Inventors: Masami Tsuda, Mitsushi Tanaka, Ayatsugu Nakamura
-
Patent number: 5972892Abstract: The invention relates to a therapeutic composition for topical application containing at least one product with an irritant side effect and a substance P antagonist for reducing or even eliminating the irritant effect of this product.It also relates to the use of a substance P antagonist for the preparation of a pharmaceutical composition for topical application containing at least one product with an irritant side effect for reducing or even eliminating the irritant effect of this product.The substance P antagonist may be a peptide compound or a nitrogen-containing compound or a nitrogen-, sulphur- or oxygen-containing heterocyclic compound.Type: GrantFiled: June 15, 1998Date of Patent: October 26, 1999Assignee: L'orealInventors: Olivier De Lacharriere, Lionel Breton
-
Patent number: 5973000Abstract: The invention relates to a hair revitalizing tonic composition containing, as an active ingredient, at least one lipid derivative of the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Y are as defined in the specification, and a and b are 0 or 1, as well as its use. Thus, there is provided a hair revitalizing tonic composition having an excellent hair loss prevention and hair revitalizing effect and, moreover, an excellent dandruff and itchy scalp prevention effect.Type: GrantFiled: June 3, 1997Date of Patent: October 26, 1999Assignees: Shiseido Company, Ltd., Takeda Chemical Industries, Ltd.Inventors: Tsunao Magara, Yoshiharu Tsuji, Chika Hamada, Yosuke Nakazawa, Eriko Takeoka, Masahiro Tajima, Masazumi Watanabe
-
Patent number: 5962506Abstract: Compounds of Formula I ##STR1## are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is an dialkoxyphosphonate, or .alpha.-hydroxyamide group and Z is an acyl or .alpha.-ketocarbamate functionality. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid support, are also disclosed.Type: GrantFiled: July 7, 1997Date of Patent: October 5, 1999Assignee: Pharmacopeia, Inc.Inventors: Carolyn DiIanni Carroll, Roland Ellwood Dolle, III, Yvonne Class Shimshock, Timothee Felix Herpin
-
Patent number: 5958918Abstract: The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.Type: GrantFiled: November 21, 1997Date of Patent: September 28, 1999Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: William R. Ewing, Michael R. Becker, Henry W. Pauls, Daniel L. Cheney, Jonathan Stephen Mason, Alfred P. Spada, Yong Mi Choi-Sledeski
-
Patent number: 5952363Abstract: The present invention relates to novel pyrrolidine compounds having the general formula I ##STR1## and pharmaceutically acceptable acid addition salts or hydrates or prodrugs thereof, wherein R.sup.1 is straight or branched C.sub.1-14 -alkyl optionally substituted with C.sub.3-7 -cycloalkyl, C.sub.1-6 -alkoxy, phenoxy, perhalomethyl, halogen, optionally substituted phenyl;CR.sup.2 is optionally C.dbd.R.sup.2 or C--R.sup.2R.sup.2 is oxygen, hydroxy, halogen, amino or mercapto,R.sup.3 and R.sup.4 independently are hydroxy, halogen, amino or mercapto, the use of these compounds as medicament, the use of these medicaments in the treatment of diabetes, pharmaceutical compositions containing these compounds and methods of preparing the compounds.Type: GrantFiled: March 5, 1998Date of Patent: September 14, 1999Assignee: Novo Nordisk A/SInventors: Marit Kristiansen, Palle Jakobsen, Jane Marie Lundbeck
-
Patent number: 5932196Abstract: The present invention are for emulsion compositions and the process for making such compositions containing biological and cosmetic actives subject to hydrolysis of actives during processing and storage of the emulsion composition. Buffers are incorporated into emulsion at a point wherein the acidic and basic conditions created during processing have little effect on compositions.Type: GrantFiled: November 4, 1994Date of Patent: August 3, 1999Assignee: The Procter & Gamble CompanyInventors: Curtis Bobby Motley, Patricia Sue Raleigh
-
Patent number: 5932520Abstract: There is provided a method for controlling or combatting the attachment of a fouling organism to an underwater surface which comprises contacting said organism with an antifouling-effective amount of a 2-arylpyrrole compound. A method for protecting aquatic structures against fouling by a marine or freshwater fouling organism and antifoulant compositions therefor are also provided.Type: GrantFiled: May 23, 1995Date of Patent: August 3, 1999Assignee: American Cyanamid CompanyInventors: Mark Arthur Josepha Van der Flass, Lantz Stephen Crawley
-
Patent number: 5929114Abstract: Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O, S, and N,R.sup.1 and R.sup.2 are substituent groups, X is ##STR2## or SO.sub.2 NR.sup.4 Z, Y is H or SZ when n is 1, a single bond when n is 2; R.sup.4 and Z can be hydrogen or alkyl.Type: GrantFiled: May 15, 1997Date of Patent: July 27, 1999Assignee: Warner-Lambert CompanyInventors: John Michael Domagala, Edward Faith Elslager, Rocco Dean Gogliotti
-
Patent number: 5914351Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.Type: GrantFiled: December 12, 1997Date of Patent: June 22, 1999Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
-
Patent number: 5885990Abstract: Substituted amidinonaphthyl ester compounds effective for treatment of thrombosis are represented by the following formula (I) and pharmaceutically acceptable acid addition salts thereof: ##STR1## wherein R.sub.1 represents (4,5-dihydro-1H-imidazol-2-yl)amino group, (4,5-dihydro-1,3-thiazol-2-yl)amino group, amidino group, morpholinomethyl group, nitro group, amino group, dimethylamino group, ##STR2## R.sub.3 represents hydrogen, methoxy group, hydroxyl group, acetylamino group, morpholino group, piperidino group, 1-pyrrolidinyl group or dimethylamino group,m represents 0-4,R.sub.4 represents hydrogen or methyl group,R.sub.2 represents NH.sub.2 CO(CH.sub.2).sub.n --, 2-(carbamoyl)vinyl group or R.sub.5 OOC(CH.sub.2).sub.n --,R.sub.5 represents dimethylcarbamoylmethyl group, hydrogen or lower alkyl group, andn represents 0-2.Type: GrantFiled: June 12, 1997Date of Patent: March 23, 1999Assignee: Torii Pharmaceutical Co., Ltd.Inventors: Toyoo Nakayama, Hiroyuki Kawamura, Hiroyuki Uchiyama