The Five-membered Hetero Ring Consists Of One Nitrogen And Four Carbons Patents (Class 514/408)

Spiro ring system (Class 514/409)

Polycyclo ring system having the five-membered hetero ring as one of the cyclos (Class 514/410)

Tricyclo ring system having the five-membered hetero ring as one of the cyclos (Class 514/411)
Bicyclo ring system having the five-membered hetero ring as one of the cyclos (Class 514/412)

Ring nitrogen is shared by the cyclos of the bicyclo ring system (Class 514/413)
Additional hetero ring which is not part of the bicyclo ring system (Class 514/414)
The bicyclo ring system consists of the five-membered hetero ring and a benzene ring (e.g., indole, etc.) (Class 514/415)

The ring nitrogen is bonded directly to nonshared ring carbons of the five-membered hetero ring (e.g., isoindole, etc.) (Class 514/416)

Plural chalcogens bonded directly to ring carbons of the five-membered hetero ring (e.g., phthalimide, etc.) (Class 514/417)

Indomethacine per se or ester thereof (Class 514/420)

Chalcogen bonded directly to ring carbon of the five-membered hetero ring (e.g., adrenochrome, etc.) (Class 514/421)

Additional hetero ring (Class 514/422)

C=x bonded directly to the five-membered hetero ring by nonionic bonding (x is chalcogen) (Class 514/423)

Chalcogen bonded directly to the five-membered hetero ring by nonionic bonding (Class 514/424)

Plural chalcogens bonded directly to the five-membered hetero ring by nonionic bonding (Class 514/425)

Nitrogen bonded directly to the five-membered hetero ring by nonionic bonding (Class 514/426)

Two double bonds between ring members of the five-membered hetero ring (e.g., pyrrole, etc.) (Class 514/427)

Chalcogen bonded indirectly to the five-membered hetero ring by acyclic nonionic bonding (Class 514/428)

Carbocyclic ring bonded directly to the five-membered hetero ring (Class 514/429)

Polyamine analogs that activate antizyme framshifting

Publication number: 20040058954

Abstract: Novel polyamines, their synthesis and use in pharmacological, cosmetic or agricultural applications are provided. The polyamines induce antizyme production which in turn down regulates both the production of polyamines by ornithine decarboxylase (ODC) and the transport of polyamines by its corresponding polyamine transporter. These compounds will preferably enter the cell independent of the polyamine transporter. As drugs, these compounds are used to treat any disease associated with cellular proliferation including but not limited to cancer.

Type: Application

Filed: September 23, 2002

Publication date: March 25, 2004

Applicant: MediQuest Therapeutics, Inc.

Inventors: Mark R. Burns, Gerard F. Graminski
N-ureidoheterocycloalkyl-piperidines as modulators of chemokine receptor activity

Publication number: 20040058961

Abstract: The present application describes modulators of CCR3 of formula (I): 1

Type: Application

Filed: July 10, 2003

Publication date: March 25, 2004

Inventors: Soo S. Ko, James R. Pruitt, Dean A, Wacker, Douglas G. Batt
Terminally-branched polymeric linkers and polymeric conjugates containing the same

Publication number: 20040053976

Abstract: The present invention is directed to polymeric-prodrug transport forms of the formula: 1

Type: Application

Filed: August 8, 2003

Publication date: March 18, 2004

Inventors: Anthony J. Martinez, Annapurna Pendri, Richard B. Greenwald, Yun H. Choe
Nitrogen-containing aromatic derivatives

Publication number: 20040053908

Abstract: Compounds represented by the following general formula: 1

Type: Application

Filed: April 18, 2003

Publication date: March 18, 2004

Inventors: Yasuhiro Funahashi, Akihiko Tsuruoka, Masayuki Matsukura, Toru Haneda, Yoshio Fukuda, Junichi Kamata, Keiko Takahashi, Tomohiro Matsushima, Kazuki Miyazaki, Ken-ichi Nomoto, Tatsuo Watanabe, Hiroshi Obaishi, Atsumi Yamaguchi, Sachi Suzuki, Katsuji Nakamura, Fusayo Mimura, Yuji Yamamoto, Junji Matsui, Kenji Matsui, Takako Yoshiba, Yasuyuki Suzuki, Itaru Arimoto
Consumable product including consumable component and alpha-keto enamine derivatives

Publication number: 20040052828

Abstract: The present invention relates to a consumable product that includes a consumable component and a cooling component present in an amount sufficient to provide a cooling sensation to a consumer, which cooling component includes one or more compounds each having the general formula: 1

Type: Application

Filed: May 30, 2003

Publication date: March 18, 2004

Inventors: Thomas Hofmann, Harald Ottinger, Oliver Frank, Tomislav Soldo, Christoph Cerny, Fabien Robert, Imre Blank
Biphenylamidine derivatives

Patent number: 6706745

Abstract: The present invention relates to a biphenylamidine derivative of the general formula (1): or a pharmaceutically acceptable salt thereof, which is a novel compound functioning as a clinically applicable FXa inhibitor.

Type: Grant

Filed: May 18, 2000

Date of Patent: March 16, 2004

Assignee: Teijin Limited

Inventors: Takayuki Hara, Tomohisa Nakada, Yasunobu Takano, Satoshi Sugiura, Takaharu Tsutsumi, Yoshiharu Takazawa, Reiko Takarada
2-substituted-4-nitrogen heterocycles as modulators of chemokine receptor activity

Patent number: 6706735

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.

Type: Grant

Filed: June 26, 2002

Date of Patent: March 16, 2004

Assignee: Bristol-Myers Squibb Pharma Company

Inventors: Paul S. Watson, Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
Caspase-1 inhibitors and methods for their use

Publication number: 20040048895

Abstract: The invention provides compounds of Formula I and derivatives thereof, pharmaceutical compositions comprising a compound of Formula I, and methods of treatment utilizing such compounds and compositions: 1

Type: Application

Filed: June 5, 2003

Publication date: March 11, 2004

Inventors: Darin Allen, Bruce Fahr, Johan Oslob, Brian C. Raimundo, Michael J. Romanowski
Substituted biaryl amides as C5a receptor modulators

Publication number: 20040048913

Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Type: Application

Filed: March 27, 2003

Publication date: March 11, 2004

Inventors: Yang Gao, Alan J. Hutchison, John M. Peterson, Wallace C. Pringle, Andrew Thurkauf, Taeyoung Yoon, He Zhao
Treatment of diseases with adamantane derivatives

Publication number: 20040048892

Abstract: The invention relates to the use of substances for the manufacturing of a pharmaceutical composition or medicament for the treatment of disturbances or illnesses which are linked to malfunction of an ionotropic acetylcholine receptor and/or a calcium-activated potassium channel functionally associated with said acetylcholine receptor, wherein said substance is at least one adamantane derivative.

Type: Application

Filed: July 30, 2003

Publication date: March 11, 2004

Inventors: J. Peter Ruppersberg, Bernd Fakler
Amines that inhibit a mammalian anandamide transporter, and methods of use thereof

Publication number: 20040048907

Abstract: One aspect of the present invention relates to amines. A second aspect of the present invention relates to the use of the amines as inhibitors of a mammalian anandamide transporter. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to asthma, neuropathic pain, persistent pain, inflammatory pain, hyperactivity, hypertension, brain ischemia, Parkinson's disease, spasticity, Tourette's syndrome, schizophrenia, hemorrhagic shock, septic shock, cardiac shock, migrane, Horton's headache, multiple sclerosis, anorexia, AIDS wasting syndrome, organ rejection, autoimmune diseases, allergy, arthritis, Crohn's disease, malignant gliomas, neurodegenerative diseases, Huntington's chorea, glaucoma, nausea, anxiety, psychosis, attention deficit hyperactivity disorder, premature ejaculation, and stroke.

Type: Application

Filed: May 15, 2003

Publication date: March 11, 2004

Inventors: Brian M. Aquila, Seth C. Hopkins, Curtis A. Lockshin, Fengjiang Wang
Aromatic sulfone hydroxamic acid metalloprotease inhibitor

Publication number: 20040048852

Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9, and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. The administered enzyme inhibitor corresponds in structure to formula (I), below, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are both hydrido or R1 and R2 together with the atoms to which they are bonded form a 5- to 8-membered ring containing one, two, or three heteroatoms in the ring that are oxygen, sulfur, or nitrogen. R3 in formula (I) is an optionally substituted aryl or optionally substituted heteroaryl radical.

Type: Application

Filed: January 7, 2003

Publication date: March 11, 2004

Inventors: Thomas E. Barta, Daniel P. Becker, Terri L. Boehm, Gary A. DeCrezcenzo, John N. Freskos, Daniel P. Getman, Joseph J. McDonald, Clara I. Villamil, Louis John Bedell, Jeffery N. Carroll, Theresa R. Fletcher, Susan Landis Hockerman, Stephen A. Kolodziej, Madeleine H. Li, Deborah A. Mischke, Patrick B. Mullins, Carol Pearcy Howard, Joseph Gerace Rico, Nathan W. Stehle
Biphenyl compounds and their use as oestrogenic agents

Publication number: 20040043993

Abstract: Compounds of formula (I), wherein R 5 is an [A]—CH 3 , —[A]—C(OH)ZZ′ or —[A]—C(O) Z″ grouping where —[A]— is an alkylene, alkenylene or alkynylene radical or a single bond, and Z, Z′ and Z″ are a hydrogen atom or an optionally substituted alkyl, alkenyl, alkynyl or aryl radical; and R 1, R 2, R 3, R 4, R 6, R 7 and R 8 are as defined in the description; the use thereof as a drug, pharmaceutical compositions containing same, a preparation method therefor, and intermediates of said method, are disclosed.

Type: Application

Filed: July 8, 2002

Publication date: March 4, 2004

Applicant: Aventis Pharma S.A.

Inventors: Dominique Lesuisse, Jean-Georges Teutsch
Substituted 1 and 2 naphthol mannich bases

Publication number: 20040044061

Abstract: The invention relates to substituted 1 and 2 naphthol Mannich bases, a method for the production thereof, medicaments containing said compounds and the use of said compounds in the production of medicaments.

Type: Application

Filed: June 27, 2002

Publication date: March 4, 2004

Inventors: Matthias Gerlach, Corina Maul
Cannabinoid receptor agonists

Publication number: 20040044051

Abstract: A compound of the formula 1

Type: Application

Filed: June 17, 2003

Publication date: March 4, 2004

Applicant: Schering Corporation

Inventors: Joseph A. Kozlowski, Bandarpalle B. Shankar, Neng-Yang Shih, Ling Tong
Method of treatment of viral infection including HIV using water soluble fullerenes - III

Publication number: 20040044062

Abstract: A water soluble derivative of buckministerfullerene (C50) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.

Type: Application

Filed: February 1, 2003

Publication date: March 4, 2004

Inventors: Simon H. Friedman, Raymond F. Schinazi, Fred Wudl, Craig L. Hill, Diane L. DeCamp, Rintje P. Sijbesma, George L. Kenyon
Compounds for inhibiting insulin secretion and methods related thereto

Publication number: 20040044049

Abstract: Compounds, compositions and methods for altering insulin secretion, particularly in the context of treatment of subjects having, or suspected of being at risk for having, diabetes mellitus.

Type: Application

Filed: February 10, 2003

Publication date: March 4, 2004

Applicant: MitoKor

Inventors: Yazhong Pei, Soumitra S. Ghosh, Ian William James
Multifunctional polyamines for delivery of biologically-active polynucleotides

Publication number: 20040043952

Abstract: The present invention relates, inter alia, to pentaerythritol lipid derivatives that are useful for the intracellular delivery of nucleic acids. Such pentaerythritol lipid derivatives are useful for the preparation of transfection complexes (such as liposomes, lipoplexes, and other lipid vesicles) that can be used to deliver nucleic acids into mammalian cells.

Type: Application

Filed: May 30, 2003

Publication date: March 4, 2004

Applicant: Genteric, Inc.

Inventors: Edmund J. Niedzinski, Michael Bennett
Analogues of lipid mediators derived from omega-3 PUFAs and methods of use

Publication number: 20040044050

Abstract: The present invention is directed to compounds that are analogues of lipid mediators derived from a fish oil-derived fatty acid, eicosapentaenoic acid [C20:5 &ohgr;-3; EPA], but with a longer tissue half-life and enhanced bioactivity. These analogues may be used to treat inflammatory, angioproliferative, cardiovascular, thrombophlebotic, vascular, ocular, dermatologic, neurodegenerative, pulmonary, endocrine, reproductive, rheumatologic and gastrointestinal diseases.

Type: Application

Filed: June 13, 2003

Publication date: March 4, 2004

Inventors: Daniel W. Goodman, Michael R. Hanley, Stuart L. Bursten
Glucocorticoid receptor modulators

Patent number: 6699893

Abstract: The present invention provides non-steroidal compounds of formula I which are selective modulators (i.e., agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides intermediates and processes for preparing these compounds.

Type: Grant

Filed: February 19, 2002

Date of Patent: March 2, 2004

Assignee: Pfizer Inc

Inventors: Robert L. Dow, Kevin K. Liu, Bradley P. Morgan, Andrew G. Swick
Fluoro-substituted benzenesulfonyl compounds for the treatment of inflammation

Patent number: 6699884

Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more fluoro-substituted benzenesulfonyl compounds corresponding to Formula I: wherein A, X, n, R1, R2, and R3 are as described in the specification, and novel fluoro-substituted benzenesulfonyl compounds within Formula I.

Type: Grant

Filed: December 13, 2002

Date of Patent: March 2, 2004

Assignee: Pharmacia Corporation

Inventors: David L. Brown, Matthew J. Graneto, Cindy L. Ludwig, John M. Molyneaux, John J. Talley
Aminoalkylpyrrolidine serotonin receptor ligands and compositions, their pharmaceutical uses, and methods for their synthesis

Publication number: 20040039044

Abstract: Novel aminoalkylpyrrolidine 5-HT7 receptor ligands, methods of preparing such ligands, intermediate compounds useful in the preparation of the receptor ligands, pharmaceutical compositions comprising the receptor ligands, and methods of treating sleep disorders, pain, depression, and schizophrenia employing the receptor ligands are disclosed. The receptor ligands have formula (1): wherein the formula variables are as defined herein, and pharmaceutically acceptable salts, solvates, active metabolites, or prodrugs thereof.

Type: Application

Filed: April 29, 2003

Publication date: February 26, 2004

Inventors: Yuanjin Rui, Atsuo Kuki, Yufeng Hong, Zhengwei Peng, David Robert Luthin
Cyclic amine derivatives and use thereof

Publication number: 20040038966

Abstract: A composition for use as an antiobestic agent and preventive or therapeutic agent for diabetes, containing a compound of the formula (I): 1

Type: Application

Filed: November 25, 2002

Publication date: February 26, 2004

Inventors: Toshisada Yano, Isako Sakaguchi, Goro Katsuura, Naoki Yoshikawa
(1-phenyl-2-heteroaryl)ethyl-guanidine compounds as inhibitors of mitochondrial F1F0 ATP hydrolase

Publication number: 20040039033

Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts thereof, 1

Type: Application

Filed: December 10, 2002

Publication date: February 26, 2004

Inventors: Karnail S. Atwal, Gary J. Grover, Charles Z. Ding, Philip D. Stein, John Lloyd, Saleem Ahmad, Lawrence G. Hamann, David Green, Francis N. Ferrara
Substituted hydrazine derivatives

Publication number: 20040039025

Abstract: A method for the inhibition of high affinity glycine transporters, compounds that inhibit these transporters; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of disease states in which glycine is involved are disclosed.

Type: Application

Filed: August 28, 2003

Publication date: February 26, 2004

Inventors: Syed M. Ali, Kurt R. Brunden, Dario Doller, Brian Herbert, Jack B. Jiang, Amy Jordan
Hydroxypropyl amides for the treatment of Alzheimer's disease

Publication number: 20040039034

Abstract: The present invention relates to compounds of formula (I): 1

Type: Application

Filed: April 30, 2003

Publication date: February 26, 2004

Inventors: John A. Tucker, Brian A. Sherer, Ying Zi Xu, Louis Brogley, Shon R. Pulley, Jon S. Jacobs, James P. Beck, Varghese John
Treatment of asthma with MEK inhibitors

Patent number: 6696440

Abstract: This invention provides a method of preventing or treating asthma by administering to a patient in need of treatment an effective amount of a selective MEK inhibitor, especially a phenyl amine of Formula I and II:

Type: Grant

Filed: July 11, 2001

Date of Patent: February 24, 2004

Assignee: Warner-Lambert Company

Inventors: Alexander James Bridges, David Thomas Dudley, James Leslie Mobley, Alan Robert Saltiel
N-ureidoalkyl-piperidines as modulators of chemokine receptor activity

Publication number: 20040034063

Abstract: The present application describes modulators of CCR3 of formula (I): 1

Type: Application

Filed: February 6, 2003

Publication date: February 19, 2004

Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Ui Tae Kim, Dean A. Wacker, Changsheng Zheng
Novel carbamates and carbamides, production and use thereof as endothelin receptor antagonists

Publication number: 20040034076

Abstract: The present invention relates to carbamates and urea derivatives of the formula I 1

Type: Application

Filed: June 16, 2003

Publication date: February 19, 2004

Inventors: Wilhelm Amberg, Georg Kettschau
Thioaryl sulfonamide hydroxamic acid compounds

Publication number: 20040034071

Abstract: A thioaryl sulfonamide hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a contemplated thioaryl sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Type: Application

Filed: January 21, 2003

Publication date: February 19, 2004

Inventors: Daniel P. Getman, Daniel P. Becker, Thomas E. Barta, Clara I. Villamil, Susan L. Hockerman, Louis J. Bedell, Madeleine Hui Li, John N. Freskos, Robert M. Heintz, Joseph J. Mc.Donald, Gary A. DeCrescenzo
Propanolaminotetralines, preparation thereof and compositions containing same

Publication number: 20040034070

Abstract: The invention relates to phenoxypropanolamines, to pharmaceutical compositions containing them, to processes for preparing them, and to the method of use thereof in the treatment of diseases that are improved by beta-3 agonist action.

Type: Application

Filed: August 8, 2003

Publication date: February 19, 2004

Inventors: Laura Barzaghi, Philippe R. Bovy, Roberto Cecchi, Tiziano Croci, Stefano Romagnano
Synergistic combination

Publication number: 20040034087

Abstract: The invention relates to the combined administration of PDE inhibitors and &bgr;2 adrenoceptor agonists for the treatment of respiratory tract disorders.

Type: Application

Filed: May 14, 2003

Publication date: February 19, 2004

Applicant: ALTANA PHARMA AG

Inventors: Ulrich Kilian, Christian Schudt
Potentiation of the immune response

Patent number: 6692753

Abstract: A method for stimulating proliferation of T-cells containing cytoplasmic post-prolyl dipeptidase activity; the method, in one aspect, involves contacting the T-cells with an organic compound at a concentration below 10−8M, wherein the compound is characterized in that: (a) it is capable of crossing the membrane of T-cells to enter the cytoplasm, (b) it binds to the dipeptidase activity at a concentration of below 10−8M, and thus (c) stimulates proliferation of the T-cells at that concentration.

Type: Grant

Filed: January 26, 2000

Date of Patent: February 17, 2004

Assignee: Trustees of Tufts College

Inventors: Brigitte T. Huber, Tracy Schmitz, Robert Underwood
Composition having insect repellent characteristics

Publication number: 20040028714

Abstract: The present invention relates to a composition having effective insect repellent characteristics comprising as an active ingredient an N-substituted p-menthane carboxamide, which has little or no odor and which is substantially non-toxic for human, pet and livestock.

Type: Application

Filed: June 4, 2003

Publication date: February 12, 2004

Inventors: Philippe Blondeau, Markus Gautschi
Aromatic amides

Publication number: 20040029874

Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

Type: Application

Filed: July 29, 2003

Publication date: February 12, 2004

Inventors: Douglas Wade Beight, Trelia Joyce Craft, Carl Penman Denny, Jeffry Bernard Franciskovich, Theodore Goodson, Steven Edward Hall, David Kent Herron, Sajan Joseph, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milet, Marta Maria Pinelro-Nunez, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
Histone deacetylase inhibitors based on trihalomethylcarbonyl compounds

Publication number: 20040029903

Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, a trihalomethylcarbonyl group, such as a trifluoromethylcarbonyl group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.

Type: Application

Filed: May 21, 2003

Publication date: February 12, 2004

Applicant: Beacon Laboratories, Inc.

Inventors: Hsuan-Yin Lan-Hargest, Robert J. Kaufman
Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Publication number: 20040029932

Abstract: Compounds of Formula (IA) and Formula (IB) 1

Type: Application

Filed: March 21, 2003

Publication date: February 12, 2004

Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.

Inventors: Younes Bekkali, Mario G. Cardozo, Christian Hanke Justus Joachim Harcken, Thomas M. Kirrane, Daniel Kuzmich, John Robert Proudfoot, Hossein Razavi, Hidenori Takahashi, David S. Thomson, Ji Wang, Renee Zindell
Substituted phenylacetic acids

Publication number: 20040029933

Abstract: Substituted phenylacetic acids, phenylethanols and related compounds are provided that are useful in treating or controlling a number of diseases associated with glucose metabolism, lipid metabolism and insulin secretion.

Type: Application

Filed: March 19, 2003

Publication date: February 12, 2004

Applicant: Metabolex, Inc.

Inventors: Zuchun Zhao, Xin Chen, Jianchao Wang, Hongbin Sun, Jack Shih-Chieh Liang
Uracil substituted phenyl sulfamoyl carboxamides

Patent number: 6689773

Abstract: Novel uracil substituted phenyl sulfamoyl carboxamides I and salts thereof, where A=oxygen or sulfur; X1=H, halogen, C1-C4-alkyl; X2=H, CN, CS—NH2, halogen, C1-C4-alkyl, C1-C4-haloalkyl; X3=H, CN, C1-C6-alkyl, C1-C6-alkoxyalkyl, C3-C7-cycloalkyl, C3-C6-alkenyl, C3-C6-alkynyl, optionally substituted benzyl; R1, R2=H, halogen, optionally substituted hydroxy, C1-C10-alkyl, C2-C10-alkenyl, C3-C10-alkynyl, C3-C7-cycloalkyl, phenyl, benzyl or C5-C7-cycloalkenyl, or R1+R2 together with the atom to which they are attached form a 3- to 7-membered heterocyclic ring; Q is selected from Q1 to Q40 as defined in the description. Use: As herbicides; for the desiccation/defoliation of plants.

Type: Grant

Filed: January 22, 2003

Date of Patent: February 10, 2004

Assignee: BASF Aktiengesellschaft

Inventors: Marianne Carlsen, Michael Anthony Guaciaro, James Jan Takasugi
Method and composition for treatment of inflammatory bowel disease

Patent number: 6689788

Abstract: A composition in unit dosage form for the inhibition, prevention or treatment of inflammatory bowel disease comprising an effective amount of a compound having the formula: and a pharmaceutically acceptable carrier therefor.

Type: Grant

Filed: August 25, 2000

Date of Patent: February 10, 2004

Assignee: University of Florida

Inventor: Raymond J. Bergeron, Jr.
Biocidal agents and methods of use

Publication number: 20040024020

Abstract: The present invention provides antimicrobial compositions and methods for treating medical conditions in mammals. The compositions provided herein are based on the surprising discovery that the metapleural gland extract from ants has biocidal activity that is useful against a variety of microorganisms, including bacteria, fungi and viruses. Accordingly, it has been discovered that the components of the metapleural gland extract are useful for the treatment and prevention of disease in mammals. The present invention provides a number of antimicrobial compounds which kill bacteria, fungi and viruses upon contact. In addition, the present invention provides methods for treating microorganism growths in mammals, including application of the antimicrobial compositions provided herein.

Type: Application

Filed: July 24, 2002

Publication date: February 5, 2004

Applicant: MYRMECOL

Inventors: James G. Holwerda, Bruce D. Levine
Histone deacetylase inhibitors based on alpha-chalcogenmethylcarbonyl compounds

Publication number: 20040023944

Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, an alpha-chalcogenmethylcarbonyl group, such as an alpha-ketothio group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.

Type: Application

Filed: May 21, 2003

Publication date: February 5, 2004

Applicant: Beacon Laboratories, Inc.

Inventors: Hsuan-Yin Lan-Hargest, Robert J. Kaufman
Methods of use and compositions for the diagnosis and treatment of infectious disease

Publication number: 20040024022

Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.

Type: Application

Filed: May 19, 2003

Publication date: February 5, 2004

Inventors: Marina Nikolaevna Protopopova, Elena Bogatcheva
CYCLIC AMP-SPECIFIC PHOSPHODIESTERASE INHIBITORS

Publication number: 20040023945

Abstract: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.

Type: Application

Filed: May 17, 2002

Publication date: February 5, 2004

Applicant: ICOS Corporation

Inventors: Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Edward A. Kesicki, Amy Oliver, Laurence E. Burgess, John J. Gaudino, Zachary S. Jones, Bradley J. Newhouse, Stephen T. Schlachter
Aromatic sulfone hydroxamates and their use as protease inhibitors

Publication number: 20040024024

Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.

Type: Application

Filed: November 12, 2002

Publication date: February 5, 2004

Inventors: John N. Freskos, Y vette M. Fobian, Alok K. Awasthi, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Nizal S. Chandrakumar, Gary A. DeCrescenzo, Bipin N. Desai, Marcia I. Heron, Susan L. Hockerman, Sara M. Jull, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Patrick B. Mullins, Monica B. Norton, Joseph G. Rico, John J. Talley, Mahima Trivedi, Clara I. Villamil, Lijuan Jane Wang
Anti tubercular drug: compostions and methods

Publication number: 20040019117

Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.

Type: Application

Filed: May 19, 2003

Publication date: January 29, 2004

Inventors: Marina Nikolaevna Protopopova, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, Elena Bogatcheva, Leo Einck
Thiomolybdate analogues and uses thereof

Publication number: 20040019087

Abstract: The current invention provides novel thiomolybdate derivatives, methods of making novel thiomolybdate derivatives, pharmaceutical compositions of novel thiomolybdate derivatives, methods of using novel thiomolybdate derivatives to treat diseases associated with aberrant vascularization, copper metabolism disorders, neurodegenerative disorders, obesity or NF-&kgr;B dysregulation and methods of using pharmaceutical compositions of thiomolybdate derivatives to treat diseases associated with aberrant vascularization, copper metabolism disorders, neurodegenerative disorders, obesity or NF-&kgr;B dysregulation.

Type: Application

Filed: May 28, 2003

Publication date: January 29, 2004

Inventors: Robert J. Ternansky, Andrew Mazar, Patricia L. Gladstone, Dimitri Coucouvanis, Amy L. Allan, Sean M. O'Hare, Melissa L.P. Price, Steven Robert Pirie-Shepherd, Fernando Donate
Compounds acting as melanocortin receptor ligands

Publication number: 20040019094

Abstract: The present invention provides novel compounds and use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: Wherein X and Y are independently chosen from O, N, S and (CH2)n, where n is 0, 1, 2, 3, 4, or 5, or a combination of these and may contain carbon-carbon multiple bonds and branched chains as well as alicyclic and heterocyclic groups; Q is H or OH; R1 and R2 can be either the same or different and are chosen from hydrogen or the residue of an aromatic group as listed in Scheme 1 and the pharmacologically active salts thereof.

Type: Application

Filed: July 21, 2003

Publication date: January 29, 2004

Inventors: Torbjorn Lundstedt, Anna Skottner, Arne Boman, Per Andersson, Victor Andrianov, Ivars Kalvins
Remedies for retinal nerve diseases containing 1,2-ethanediol derivatives or salts thereof

Publication number: 20040014777

Abstract: 1,2-Ethanediol derivatives represented by the following general formula [1]: 1

Type: Application

Filed: April 9, 2003

Publication date: January 22, 2004

Applicant: Toyama Chemical Co., LTD.

Inventor: Satoshi Ono
Substituted propargylamines

Publication number: 20040014784

Abstract: The present invention relates to the use of substituted aryl- and heteroarylpropargylamines of the formula (I) 1

Type: Application

Filed: August 22, 2002

Publication date: January 22, 2004

Inventors: Harald Jakobi, Susan Mary Cramp, Joachim Dickhaut, Stephen Lindell, Jorg Tiebes, Maria Asuncion Canales, Daniela Jans, Waltraud Hempel, Reed Nathan Royalty, Susan Marie McComb, Maria-Theresia Thonessen, Jutta Maria Waibel, Vincent Lee Salgado

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