Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Five Membered Hetero Ring (e.g., Pyrrole Carbonyl Halides, Pyrrole Carboxaldehyde, Etc.) Patents (Class 548/530)
  • Patent number: 6268511
    Abstract: An itaconic acid derivative having the following formulas (1) or (2): wherein R1 represents a hydrogen atom, a lower alkyl group or a phenyl lower alkyl group, wherein the phenyl ring of the phenyl lower alkyl group is unsubstituted or substituted by at least one lower alkyl group, R2 represents a hydrogen atom or a lower alkyl group and A represents a lower alkylene group, or salts thereof. Copolymers can be made from the itaconic acid derivatives.
    Type: Grant
    Filed: December 3, 1999
    Date of Patent: July 31, 2001
    Assignees: Santen Pharmaceutical Co., Ltd.
    Inventor: Fumian Li
  • Patent number: 6265228
    Abstract: Combinatorial chemical libraries of the Formula [S]—C(O)—L′—Z containing dihyroxy amides and hydroxyphosphonate amides are disclosed, in which [S] represents a solid support and —L′—Z is a linker/ligand residue. In these libraries, Z is and Y is —P(O)(OR6)(OR7), —CH(OH)—COR8, —CH,CH═CH2—CH2CH(OH)CH2OH, —CH2CHO, —CH2CH2OH, —CH2CH2OC(O)NHR26, —CH2CH2NR27R28, or The combinatorial libraries are optionally encoded with tags. The use of these libraries in assays to discover biologically active compounds is also disclosed.
    Type: Grant
    Filed: June 18, 1999
    Date of Patent: July 24, 2001
    Assignee: Pharmacopeia, Inc.
    Inventors: Roland Ellwood Dolle, III, Timothee Felix Herpin, Yvonne Class Shimshock, Cullen Lee Cavallaro
  • Patent number: 6251892
    Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-oxides of heterocyclic esters, amides, thioesters, and ketones having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.
    Type: Grant
    Filed: April 21, 2000
    Date of Patent: June 26, 2001
    Assignee: GPI NIL Holdings, Inc.
    Inventors: Gregory S. Hamilton, Joseph P. Steiner, Eric S. Burak
  • Patent number: 6251931
    Abstract: Oleamide is an endogenous fatty acid primary amide that possesses sleep-inducing properties in animals and has been shown to effect seratonergic systems and block gap junction communication in a structurally specific manner. Certain agents can serve both as an oleamide agonist and as an inhibitor of fatty acid amide hydrolase. Fatty acid amide hydrolase is responsible for the rapid inactivation of oleamide in vivo. The structural features of oleamide required for inhibition of gap junction-mediated chemical and electrical transmission in rat glial cells are defined. Effective inhibitors fall into two classes of fatty acid primary amides of which oleamide and arachidonamide are the prototypical members. Of these two, oleamide constitutes the most effective and its structural requirements for inhibition of the gap junction are well defined.
    Type: Grant
    Filed: April 19, 2000
    Date of Patent: June 26, 2001
    Assignee: The Scripps Research Institute
    Inventors: Dale L. Boger, Norton B. Gilula, Richard A. Lerner, Benjamin F. Cravatt
  • Patent number: 6242609
    Abstract: A method for manufacturing a color coupler used in a silver halide photographic light-sensitive material using an ammonium trihalide. Said method for manufacturing the color coupler comprising the following step: a step for halogenating a coupling position of a four equivalent coupler using a halogenating agent, wherein said halogenating agent is said ammonium trihalide.
    Type: Grant
    Filed: April 7, 1999
    Date of Patent: June 5, 2001
    Assignee: Konica Corporation
    Inventor: Fumio Ishii
  • Patent number: 6242476
    Abstract: The present invention relates to leukotriene A4 hydrolase inhibitors containing compounds represented by the formula [I] or salts thereof as active ingredients, wherein R1 represents hydrogen, alkyl, phenylalkyl, alkanoyl or benzoyl; R2 and R3 each represent hydrogen or alkyl; R4 represents hydroxyl, alkoxy, phenylalkoxy, amino, alkylamino or phenylalkylamino; R5 represents phenylalkyl or naphthylalkyl; “Z” represents sulfur or oxygen; “A” represents alkylene; and “n” represents 0, 1 or 2; providing that the phenyl ring in R1 can be substituted by alkyl, alkoxy or halogen, and that the phenyl ring or the naphthyl ring in R5 can be substituted by alkyl, cycloalkyl, alkoxy, alkylthio or halogen.
    Type: Grant
    Filed: September 17, 1999
    Date of Patent: June 5, 2001
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Shiro Mita, Masato Horiuchi, Masakazu Ban, Ken-ichi Fujimura, Hiroshi Suhara
  • Patent number: 6228872
    Abstract: The present invention relates to the design, synthesis, and the peptidyl-prolyl isomerase (PPIase or rotamase) inhibitory activity of novel pyrrolidinemethyl diamide and carbamate compounds that are neurotrophic agents (i.e. compounds capable of stimulating growth or proliferation of nervous tissue) and that bind to immunophilins such as FKBP12 and inhibit their rotamase activity. This invention also relates to pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: November 8, 1999
    Date of Patent: May 8, 2001
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gene M. Dubowchik, Jonathan L. Ditta, David P. Provencal, Derek J. Denhart
  • Patent number: 6218424
    Abstract: This invention relates to neurotrophic, low molecular weight, small molecule heterocyclic ketone and thioester compounds, compositions containing the same, and the use of such compounds for treating neurological disorders, including physically damaged nerves and neurodegenerative diseases.
    Type: Grant
    Filed: November 22, 1999
    Date of Patent: April 17, 2001
    Assignee: GPI NIL Holdings, Inc.
    Inventors: Gregory S. Hamilton, Jia-He Li
  • Patent number: 6184388
    Abstract: An antimicrobial drug having excellent antimicrobial activity and high safety is disclosed, which comprises as an active ingredient, a quinolone derivative having a substituted aminocycloalkylpyrrolidine as a substituent and which is further substituted with various substituents, represented by formula (I), its salts and hydrates thereof: wherein Q is represented by formula (II) or (IV).
    Type: Grant
    Filed: September 17, 1999
    Date of Patent: February 6, 2001
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Makoto Takemura, Youichi Kimura, Hisashi Takahashi, Kenichi Kimura, Satoru Miyauchi, Hitoshi Ohki, Kazuyuki Sugita, Rie Miyauchi
  • Patent number: 6180818
    Abstract: A silver halide photographic material is disclosed, comprising a support having thereon at least one light-sensitive silver halide emulsion layer, wherein said silver halide photographic material contains a compound by formula (IA), or which contains at least one hydroxamic acid compound having a bicyclo ring as a partial structure and represented by formula (IB).
    Type: Grant
    Filed: November 3, 1999
    Date of Patent: January 30, 2001
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hisashi Mikoshiba, Hiroo Takizawa, Junichiro Hosokawa, Yoshio Ishii, Keiji Mihayashi, Masakazu Morigaki, Mamoru Sakurazawa
  • Patent number: 6177408
    Abstract: 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: Grant
    Filed: November 13, 1998
    Date of Patent: January 23, 2001
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Paolo Cozzi, Italo Beria, Marina Caldarelli, Maria Cristina Geroni, Enrico Pesenti
  • Patent number: 6172060
    Abstract: 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: Grant
    Filed: February 10, 1999
    Date of Patent: January 9, 2001
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, Inigo Saenz de Tejada
  • Patent number: 6169206
    Abstract: 4-(N,N-Dialkylamino)aniline compounds of the following general formula (I): wherein R1 represents an alkyl group, an aryl group or a heterocyclic group, R2 to R5 each represent a hydrogen atom or a substituent, and R2 and R3, R1 and R2, or R4 and R5 may form a ring together; a processing composition for color photography, which contains at least one of these compounds; and a color image-forming method wherein at least one of these aniline compounds is used.
    Type: Grant
    Filed: January 24, 2000
    Date of Patent: January 2, 2001
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Keizo Kimura, Shigeo Hirano, Hiroshi Kawamoto
  • Patent number: 6166222
    Abstract: The invention relates to a process for preparing chiral 3,4-dehydroproline compounds of formula (I), in which R, R' and R" have the meanings given in the description. The invention is characterized by a pyrrolecarboxylic acid derivative compound of formula (II) reacted first with an alkali or alkaline earth metal in ammonia and then with an aqueous salt solution or a compound of formula (III) in which X is a leaving group to form the final chiral product compound.
    Type: Grant
    Filed: December 1, 1999
    Date of Patent: December 26, 2000
    Assignee: BASF Aktiengesellschaft
    Inventor: Bernd Schafer
  • Patent number: 6166063
    Abstract: The present invention relates to a compound of formula (I) ##STR1## wherein R is substituted adamantyl; and n is 0 to 3; in free form or in acid addition salt form. Compounds of formula I inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.
    Type: Grant
    Filed: December 9, 1999
    Date of Patent: December 26, 2000
    Assignee: Novartis AG
    Inventor: Edwin Bernard Villhauer
  • Patent number: 6166082
    Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula(T).sub.x A--B--D--E--Gwherein A and B are aryl or heteroaryl rings; each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR1## the group E represents a three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and the group G represents --M, ##STR2## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; andR.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids, and include pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 9, 1998
    Date of Patent: December 26, 2000
    Assignee: Bayer Corporation
    Inventors: Harold Clinton Eugene Kluender, Guenter Hans Heinz Herbert Benz, David Ross Brittelli, William Harrison Bullock, Kerry Jeanne Combs, Brian Richard Dixon, Stephan Schneider, Jill Elizabeth Wood, Michael Christopher VanZandt, Donald John Wolanin, Scott M. Wilhelm
  • Patent number: 6160126
    Abstract: Novel Intermediates ##STR1## wherein R is a substituted or unsubstituted hydrocarbon residue or acyl group; X is an electron withdrawing group; Y.sup.1 and Y.sup.2, which are the same or different, are each independently oxygen or sulfur; and A is a substituted or unsubstituted, divalent hydrocarbon residue have potent reactivity, this being useful in preparing guanidine derivatives.
    Type: Grant
    Filed: April 9, 1991
    Date of Patent: December 12, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yasuyuki Kando, Hideki Uneme, Isao Minamida
  • Patent number: 6159989
    Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
    Type: Grant
    Filed: December 15, 1999
    Date of Patent: December 12, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Lin Chu, Mark Goulet, Thomas F. Walsh, Matthew J. Wyvratt, Stephanie L. Witkin
  • Patent number: 6124472
    Abstract: 3-Pyrroline-2-carboxylic acid derivatives of the formula I ##STR1## are prepared by eliminating the sulfonic acid residue, with the aid of a base, from a compound of the formula II ##STR2##
    Type: Grant
    Filed: January 22, 1999
    Date of Patent: September 26, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Helmut Mack, Thomas Pfeiffer, Werner Seitz, Thomas Zierke, Friedhelm Balkenhohl, Udo Lange
  • Patent number: 6121461
    Abstract: A novel crystalline form of [(R-(R*,R*)]-2-(4-fluorophenyl)-.beta.,.delta.-dihydroxy-5-(1-methylethyl) -3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt designated Form III is characterized by its X-ray powder diffraction and/or solid state NMR is described, as well as methods for the preparation and pharmaceutical composition of the same, which is useful as an agent for treating hyperlipidemia and hypercholesterolemia.
    Type: Grant
    Filed: July 26, 1999
    Date of Patent: September 19, 2000
    Assignee: Warner-Lambert Company
    Inventor: Ann T. McKenzie
  • Patent number: 6114570
    Abstract: A silver halide photographic material is disclosed, comprising a support having thereon at least one light-sensitive silver halide emulsion layer, wherein said silver halide photographic material contains a compound by formula (IA), or which contains at least one hydroxamic acid compound having a bicyclo ring as a partial structure and represented by formula (IB).
    Type: Grant
    Filed: September 2, 1998
    Date of Patent: September 5, 2000
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hisashi Mikoshiba, Hiroo Takizawa, Junichiro Hosokawa, Yoshio Ishii, Keiji Mihayashi, Masakazu Morigaki, Mamoru Sakurazawa
  • Patent number: 6114364
    Abstract: The present invention relates to a compound represented by the following general formula (1) ##STR1## (wherein X represents O, S, SO, SO.sub.2, or NH, Y is a substituted or unsubstituted hydrocarbon residue containing 1 through 6 carbon atoms and having an overall molecular weight of not less than 15 and not more than 400, and the hydrocarbon residue, when the residue is ring, may contain one or two hetero-atoms in the ring, and Z is a carboxyl group, a group derived therefrom or an aliphatic hydrocarbon residue having from 1 to 4 carbon atoms which may be substituted or unsabstituted) or a pharmacologically acceptable salt thereof (excluding (1R,2S)-2-[(2R)-(2-acetyl-amino-2-carboxyethyl)thiomethyl]-3-oxo-1-cyclope ntane-carboxylic acid (cystacyclin)), a method for production thereof and a medicinal use thereof. The compound of the present invention is useful as a neuron differentiation accelerator.
    Type: Grant
    Filed: October 5, 1998
    Date of Patent: September 5, 2000
    Assignee: Nippon Kayaku Co., Ltd.
    Inventors: Seiichi Saito, Tomio Morino, Kuniko Masuda
  • Patent number: 6077955
    Abstract: A process for the preparation of five-membered or six-membered ring lactams from aliphatic .alpha.,.omega.-dinitriles has been developed. In the process an aliphatic .alpha.,.omega.-dinitrile is first converted to an ammonium salt of an .omega.-nitrilecarboxylic acid in aqueous solution using a catalyst having an aliphatic nitrilase (EC 3.5.5.7) activity, or a combination of nitrile hydratase (EC 4.2.1.84) and amidase (EC 3.5.1.4) activities. The ammonium salt of the .omega.-nitrilecarboxylic acid is then converted directly to the corresponding lactam by hydrogenation in aqueous solution, without isolation of the intermediate .omega.-nitrilecarboxylic acid or .omega.-aminocarboxylic acid. When the aliphatic .alpha.,.omega.-dinitrile is also unsymmetrically substituted at the .alpha.-carbon atom, the nitrilase produces the .omega.-nitrilecarboxylic acid ammonium salt resulting from hydrolysis of the .omega.
    Type: Grant
    Filed: July 1, 1998
    Date of Patent: June 20, 2000
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Robert Di Cosimo, Robert Donald Fallon, John Edward Gavagan, Frank Edward Herkes
  • Patent number: 6069247
    Abstract: The present invention relates to a process for preparing acrylamides; wherein, a propiolamide is reacted with an activated aromatic ring to yield a wide variety of acrylamides.
    Type: Grant
    Filed: October 5, 1998
    Date of Patent: May 30, 2000
    Assignee: Eli Lilly and Company
    Inventors: Lynne Ann Hay, David Mitchell
  • Patent number: 6066662
    Abstract: The invention provides hydroxylamine derivatives of formula (I) wherein A, R.sup.1, R.sup.2 and R.sup.3 have the significance given in the description, which are matrix metalloproteinase inhibitors and which also prevent TNF release. They are therefore useful for the control or prevention of degenerative joints diseases such as rheumatoid arthritis and osteoarthritis or for the treatment of invasive tumours, atherosclerosis or multiple sclerosis. They can be manufactured according to generally known methods.
    Type: Grant
    Filed: November 20, 1996
    Date of Patent: May 23, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael John Broadhurst, Paul Anthony Brown, William Henry Johnson
  • Patent number: 6057342
    Abstract: 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: Grant
    Filed: July 7, 1997
    Date of Patent: May 2, 2000
    Assignee: Dupont Pharmaceutical Co.
    Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
  • Patent number: 6054452
    Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-oxides of heterocyclic esters, amides, thioesters, and ketones having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.
    Type: Grant
    Filed: July 9, 1998
    Date of Patent: April 25, 2000
    Assignee: GPI NIL Holdings, Inc.
    Inventors: Gregory S. Hamilton, Joseph P. Steiner, Eric S. Burak
  • Patent number: 6048877
    Abstract: Tetralone derivatives of the formula ##STR1## where R.sup.1 is halo, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, (aryl)alkenyl, (aryl)alkynyl, alkoxy, O-alkenyl, O-aryl, O-alkyl(heterocyclo), COO-alkyl,alkanoyl, CO-amino, CO-substituted amino, alkyl-CO-amino, alkyl-CO-substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-alkyl(heterocyclo), N(alkyl)CO-alkyl, N(alkyl)CO-aryl, N(alkyl)CO-heterocyclo, N(alkyl)CO-alkyl(heterocyclo);R.sup.2 is hydrogen, alkyl, halo, aryl, alkoxy, amino, substituted amino;R.sup.3 is oxo, hydroxy, alkoxy, O--COalkyl, --O--COaryl, --O--COheterocyclo, NOH, NO-alkyl, N-amino, N-substituted amino, N-NHCONHalkyl, N-NHSO.sub.2 alkyl, N-NHSO.sub.2 aryl, amino, substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-heterocyclo, spiroheterocyclo;R.sup.4 is hydrogen, alkyl, alkyl(COalkyl), alkyl(COOalkyl); orR.sup.3 and R.sup.4 taken together with the atoms to which they are attached form a five- to seven-membered ring which can contain up to three heteroatoms selected from oxygen, nitrogen and sulfur;R.sup.
    Type: Grant
    Filed: January 20, 1998
    Date of Patent: April 11, 2000
    Assignee: Bristol-Myers Squibb Company
    Inventors: Saleem Ahmad, Philip D. Stein, Francis N. Ferrara, Karnail S. Atwal
  • Patent number: 6034136
    Abstract: Disclosed are compound of formula I whereinR represents hydrogen, lower alkyl, cycloalkyl, bicycloalkyl, adamantyl, aryl, biaryl, or mono- or di-(cycloalkyl, aryl or biaryl)-lower alkyl, di-(lower alkyl or aryl-lower alkyl)amino-lower alkyl, or (piperidino, morpholino, pyrrolidino)-lower alkyl;R.sub.1 represents hydrogen, lower alkyl, cycloalkyl, aryl, biaryl, or (cycloalkyl, aryl or biaryl)-lower alkyl;R.sub.2 represents hydrogen, lower alkyl, lower alkoxy, aryl-lower alkyl, aryl-lower alkoxy, amino, mono- or di-(lower alkyl or aryl-lower alkyl)-amino, acylamino, or (lower alkyl or aryl-lower alkyl)-(thio, sulfinyl or sulfonyl);R.sub.3 represents hydrogen, lower alkyl, cycloalkyl, aryl-lower alkyl, cycloalkyl-lower alkyl, or C.sub.2 -C.sub.7 -alkyl interrupted by S, SO, SO.sub.2, O or N--R.sub.5 ;R.sub.4 represents hydrogen or acyl;R.sub.
    Type: Grant
    Filed: March 17, 1998
    Date of Patent: March 7, 2000
    Assignee: Novartis AG
    Inventor: Cynthia A. Fink
  • Patent number: 6028192
    Abstract: The present invention relates to a process for the preparation of compounds of the formula 1 ##STR1## by reacting a secondary acid amide of the formula 2 ##STR2## with an acid chloride of the formula 3 ##STR3## in the presence of N,N-diisopropyl-N-ethylamine. R.sup.1, R.sup.2 and R.sup.3 are alkyl or alkenyl radicals, if required also aryl radicals. The compounds of the formula 1 are suitable for use as insecticides or bleach activators.
    Type: Grant
    Filed: January 27, 1998
    Date of Patent: February 22, 2000
    Assignee: Clariant GmbH
    Inventors: Johannes Becherer, Klaus Delpy, Karl-Heinz Keil, Bernhard Mees
  • Patent number: 6022873
    Abstract: Compounds of formula (I) ##STR1## wherein n, V, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification are matrix metalloproteinase inhibitors.
    Type: Grant
    Filed: July 23, 1998
    Date of Patent: February 8, 2000
    Assignee: British Biotech Pharmaceuticals Limited
    Inventors: Raymond Paul Beckett, Fionna Mitchell Martin, Andrew Miller, Richard Simon Todd, Mark Whittaker
  • Patent number: 6011155
    Abstract: N-(N'-substituted glycyl)-2-cyanopyrrolidines of formula I ##STR1## Compounds of formula I inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.
    Type: Grant
    Filed: October 31, 1997
    Date of Patent: January 4, 2000
    Assignee: Novartis AG
    Inventor: Edwin Bernard Villhauer
  • Patent number: 6004992
    Abstract: The present invention relates to novel fluorobutenyl aminocarboxylates of the formula (I)R--CO--O--CH.sub.2 --CH.sub.2 --CX.dbd.CF.sub.2 (I)in whichX represents hydrogen or halogen andR represents one of the groups ##STR1## (b) R.sup.3 --A--CO--NR.sup.4 --CR.sup.5 R.sup.6 -- or ##STR2## in which A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each as defined in the description, to processes for their preparation and to their use for controlling animal pests.
    Type: Grant
    Filed: May 22, 1998
    Date of Patent: December 21, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Udo Kraatz, Wolfram Andersch, Andreas Turberg, Norbert Mencke
  • Patent number: 5942538
    Abstract: The present invention relates to benzamidoxime derivatives represented by the formula ?I!; ##STR1## wherein R.sup.1 is unsubstituted or substituted C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted C.sub.2 -C.sub.4 alkenyl or unsubstituted or substituted C.sub.2 -C.sub.4 alkynyl, R.sup.2 is phenyl optionally having substituents or heterocycle optionally having substituents X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are each independently hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 alkylthio or the like, and r.sub.1 and r.sub.2 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl or the like, having excellent fungicidal activity and being useful as a fungicide for agricultural and horticultural use, and methods for preparation thereof.
    Type: Grant
    Filed: June 26, 1998
    Date of Patent: August 24, 1999
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Isamu Kasahara, Hirohito Ooka, Shinsuke Sano, Hiroyasu Hosokawa, Homare Yamanaka
  • Patent number: 5925772
    Abstract: A class of cysteine protease inhibitors which inactivate a cysteine protease by covalently bonding to the protease and releasing a heterocyclic leaving group is presented. The cysteine protease inhibitors of the present invention comprise a first portion which targets a desired cysteine protease and positions the inhibitor near the thiolate anion portion of the active site of the protease, and a second portion which covalently bonds to the cysteine protease and irreversibly deactivates that protease by providing a carbonyl or carbonyl-equivalent which is attacked by the thiolate anion of the active site of the cysteine protease to sequentially cleave a heterocyclic leaving group. The heterocyclic leaving group of the protease inhibitor is of the formula: --O--Het, where Het is a heterocycle having 4-7 atoms in the ring, with at least one of the heterocycle atoms being N, O or S.
    Type: Grant
    Filed: September 2, 1997
    Date of Patent: July 20, 1999
    Assignee: Prototek, Inc.
    Inventors: Mary P. Zimmerman, Robert E. Smith
  • Patent number: 5919790
    Abstract: The present invention relates to compounds that are inhibitors of interleukin-1.beta. converting enzyme that have the Formula II ##STR1## This invention also relates to a method of treatment of stroke, inflammatory diseases, septic shock, reperfusion injury, Alzheimer's disease, shigellosis, and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1.beta. converting enzyme.
    Type: Grant
    Filed: October 2, 1997
    Date of Patent: July 6, 1999
    Assignees: Warner-Lambert Company, BASF Aktiengesellsschaft
    Inventors: Hamish John Allen, Kenneth Dale Brady, Bradley William Caprathe, Paul Galatsis, John Lodge Gilmore, Sheryl Jeanne Hays, Robert Vincent Talanian, Nigel Walker, Joseph Scott Warmus
  • Patent number: 5919774
    Abstract: A class of novel pyrroles is disclosed together with the use of such compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.
    Type: Grant
    Filed: December 5, 1997
    Date of Patent: July 6, 1999
    Assignee: Eli Lilly and Company
    Inventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim
  • Patent number: 5917038
    Abstract: The present invention relates to a process for preparing acrylamides; wherein, a propiolamide is reacted with an activated aromatic ring to yield a wide variety of acrylamides.
    Type: Grant
    Filed: April 11, 1997
    Date of Patent: June 29, 1999
    Assignee: Eli Lilly and Company
    Inventors: Lynne Ann Hay, David Mitchell
  • Patent number: 5891901
    Abstract: Compounds of the formula ##STR1## wherein R is alkyl, alkylthio or hydroxy, as well as, pharmaceutically acceptable salts of compounds of formula I are antiproliferative agents useful in the treatment of cancer.
    Type: Grant
    Filed: July 24, 1997
    Date of Patent: April 6, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Urvashi Hooda Dhingra, Donna Mary Huryn, Dennis Dalton Keith, Giuseppe Federico Weber
  • Patent number: 5874449
    Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.
    Type: Grant
    Filed: December 31, 1996
    Date of Patent: February 23, 1999
    Assignee: GPI NIL Holdings, Inc.
    Inventors: Gregory S. Hamilton, Jia-He Li, Wei Huang
  • Patent number: 5872262
    Abstract: Compounds of Formula I ##STR1## are disclosed as inhibitors of plasmepsin and cathepsin D. The compounds are therefore useful to treat diseases such as malaria. In preferred compounds of formula I, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or a substituted piperazinealkanoic acid. Intermediates in the solid phase synthesis of compounds of formula I, in which the compounds are attached to a solid support, are also disclosed.
    Type: Grant
    Filed: December 8, 1997
    Date of Patent: February 16, 1999
    Assignee: Pharmacopeia, Inc.
    Inventors: Roland Ellwood Dolle, III, Hitesh K. Patel, Theodore O. Johnson, Jr., Carolyn DiIanni Carroll, Shiwei Tao
  • Patent number: 5869675
    Abstract: Novel lactacystin derivatives other than lactacystin per se, with superior activity for the genesis of neurites and highly selective toxicity and low cytotoxicity as compared with known lactacystin have been prepared, of the formula ##STR1## wherein R is lower alkoxy, --S--(CH.sub.2).sub.n R.sup.1 or --S--(CH.sub.2) .sub.n --CH(R.sup.2)-(R.sup.3), in which R.sup.1 is branched or straight-chain lower alkyl, hydroxy, carboxyl, lower alkoxycarbonyl, optionally substituted phenyl, substituted or unsubstituted amino or pyridyl, R.sup.2 is substituted or unsubstituted amino, lower alkyl or amino acid residue, R.sup.3 is carboxyl, lower alkoxycarbonyl, lower alkenyloxycarbonyl or amino acid residue, and n is 0-4, or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: November 28, 1997
    Date of Patent: February 9, 1999
    Assignee: The Kitasato Institute
    Inventors: Satoshi Omura, Toshiaki Sunazuka, Haruo Tanaka
  • Patent number: 5859047
    Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituted group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.
    Type: Grant
    Filed: May 30, 1997
    Date of Patent: January 12, 1999
    Assignee: Bayer Corporation
    Inventors: Harold Clinton Eugene Kluender, David Ross Brittelli, William Harrison Bullock, Kerry Jeanne Combs, Brian Richard Dixon, Michael Christopher VanZandt, Scott McClelland Wilhelm, Donald John Wolanin
  • Patent number: 5856517
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.1' are independently alkyl, aryl, alkenyl or alkynyl;R.sup.2 and R.sup.2' are independently hydrogen or alkyl;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently are ##STR2## CH.sub.2 OR.sup.10, CHO, CH.sub.2 NR.sup.11 R.sup.12, hydrogen, halogen, cyano, alkyl, hydroxy, alkoxy, aryloxy, haloalkyl, nitro, amino, acylamino, aralkyloxy, monoalkylamino, dialkylamino, alkylthio, alkylsulphinyl or alkylsulphonyl, provided that at least one of R.sup.4, R.sup.5, R.sup.6 or R.sup.7 is cyano, ##STR3## CH.sub.2 OR.sup.10, CH.sub.2 NR.sup.11 R.sup.12, or CHO ; R.sup.8 is alkyl, aralkyl or aryl;R.sup.10 is hydrogen, alkyl, aralkyl or aryl;R.sup.11 and R.sup.
    Type: Grant
    Filed: July 24, 1997
    Date of Patent: January 5, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Donna Mary Huryn, Dennis Dalton Keith
  • Patent number: 5792776
    Abstract: Disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF and/or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 27, 1994
    Date of Patent: August 11, 1998
    Assignee: Cytomed, Inc.,
    Inventors: Tesfaye Biftu, Ralph Scannell, Xiong Cai, Sajjat Hussoin
  • Patent number: 5792778
    Abstract: The present invention addresses 2-substituted aryl pyrroles, as well as compositions containing such compounds and methods of treatment. Cytokine mediated diseases refers to diseases or conditions in which excessive or unregulated production or activity of one or more cytokines occurs. Interleukin-1 (IL-1), Interleukin-6 (IL-6), Interleukin-8 (IL-8) and Tumor Necrosis Factor (TNF) are cytokines which are involved.
    Type: Grant
    Filed: August 8, 1996
    Date of Patent: August 11, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Stephen E. de Laszlo, Nigel J. Liverton, Gerald S. Ponticello, Harold G. Selnick, Nathan B. Mantlo
  • Patent number: 5786515
    Abstract: A simple, high yielding synthesis of a-chloro ketones is described, involving acylation of Grignard and organolithium reagents with N-methoxy-N-methylchloroacetamide. The efficiency of the process is further enhanced by recycling N,O-dimethylhydroxylamine.
    Type: Grant
    Filed: August 30, 1996
    Date of Patent: July 28, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen
  • Patent number: 5780645
    Abstract: A process for the alkylation of imides wherein the imides are reacted with a dialkyl carbonate, in the liquid state, at a temperature of between 100.degree. C. and 250.degree. C. and at a pressure of between 0 and 60 atmospheres in the presence of a basic catalyst. The dialkyl carbonate reagents are not very toxic and are thermally stable and their use as alkylation agents makes it possible to produce waste products with a negligible saline content.
    Type: Grant
    Filed: December 31, 1996
    Date of Patent: July 14, 1998
    Assignee: Enichem S.p.A.
    Inventors: Marcello Notari, Franco Mizia, Franco Rivetti
  • Patent number: 5773239
    Abstract: The invention relates to novel mannosidase inhibitors, processes for their preparation and their use as therapeutic agents. The invention also relates to the use of compounds of the formula II as described herein as prodrugs.
    Type: Grant
    Filed: December 6, 1995
    Date of Patent: June 30, 1998
    Assignees: Mount Sinai Hospital Corporation., GlycoDesign, Inc.
    Inventors: Jeremy Carver, James Wilson Dennis, Rajan Shah
  • Patent number: 5756762
    Abstract: The present invention relates to a novel enantiospecific processes for preparing (S)-4-amino-hepta-5,6-dienoic acid and pharmaceutically acceptable salts thereof, which is useful as an irreversible inhibitor of GABA-T, to novel intermediates thereof, and a process for preparing an intermediate thereof.
    Type: Grant
    Filed: January 9, 1997
    Date of Patent: May 26, 1998
    Assignee: Merrell Pharmaceuticals Inc.
    Inventor: H. Michael Kolb