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)

The -c(=x)- is part of a -c(=x)x- group, wherein the x's are the same or diverse chalcogens (e.g., pyrrole-3-carboxylic acid, etc.) (Class 548/531)

And is bonded directly to a ring carbon which is adjacent to the ring nitrogen of the five-membered hetero ring (e.g., 4-hydroxy proline, etc.) (Class 548/532)

Additional -C(=X) bonded directly to the five-membered hetero ring (e.g., N n-butyryl-L-proline, etc.) (Class 548/533)
Chalcogen bonded directly to the other ring carbon which is adjacent to the ring nitrogen of the five-membered hetero ring (e.g., 2-pyrrolidone-5 carboxylic acid, etc.) (Class 548/534)
The five-membered hetero ring is further unsubstituted or alkyl substituted only (e.g., proline, etc.) (Class 548/535)

Additional -C(=X)- bonded directly to the five-membered hetero ring (e.g., pyrrole-3,4-dicarboxylic acid esters, etc.) (Class 548/536)

Acyclic nitrogen bonded directly to the -c(=x)- (e.g., 4,5-dihalopyrrole -2 carboxamides, etc.) (Class 548/537)

The -C(=X)- is bonded directly to the ring nitrogen of the five-membered hetero ring (e.g., 1-pyrrolidine carboxanilides, etc.) (Class 548/538)

Carbocyclic ring bonded directly to the -c(=x)- (e.g., 3-benzoyl pyrrolidine, etc.) (Class 548/539)

Acyclic carbon bonded directly to the -c(=x)- (e.g., n-oleoylpyrrolidine, etc.) (Class 548/540)

Tubulin binding agents and corresponding prodrug constructs

Publication number: 20040043969

Abstract: A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, phosphoramidates, and other prodrugs capable of demonstrating selective targeting and destruction of tumor cell vasculature.

Type: Application

Filed: April 1, 2003

Publication date: March 4, 2004

Inventors: Kevin G. Pinney, Vani P. Mocharla, Zhi Chen, Charles M. Garner, Anjan Ghatak, Mallinath Hadimani, Jimmy Kessler, James M. Dorsey, Klaus Edvardsen, David J. Chaplin, Joseph Prezioso, Usha R. Ghatak
Acyl-CoA dehydrogenase allenic inhibitors

Publication number: 20040039032

Abstract: Compounds of formula I 1

Type: Application

Filed: August 20, 2002

Publication date: February 26, 2004

Inventors: Colin Thorpe, Wenzhong Wang
Antitumor agents

Publication number: 20040034202

Abstract: The present invention provides compounds of general formula I or II: 1

Type: Application

Filed: April 14, 2003

Publication date: February 19, 2004

Applicant: The Regents of the University of California

Inventors: Trevor C. McMorris, Michael J. Kelner
Method for producing 3,3-diarylpropylamines

Publication number: 20040034080

Abstract: The invention relates to a novel method for producing 3,3-diarylpropylamines of formula (I), wherein A represents a substituted or unsubstituted aryl radical, X represents H, OH or OR3 and Y, R1, R2 and R3 have the meanings given in the description, by hydroformylation/hydrocarbonylation and subsequent reductive amination using a transition metal catalyst.

Type: Application

Filed: July 14, 2003

Publication date: February 19, 2004

Inventors: Martin Donsbach, Peter Eilbracht, Christian Buss, Andreas Schmidt
Process for the manufacture of 3-amino-pyrrolidine derivatives

Publication number: 20040034236

Abstract: The invention is concerned with a process for the manufacture of 3-amino-pyrrolidine derivatives of the formula 1

Type: Application

Filed: July 29, 2003

Publication date: February 19, 2004

Inventors: Marc Muller, Milan Soukup
Derivative of dicarboxylic acids having six to twelve carbon atoms and use of these derivatives and dicarboxylic acids alone in the preparation of pharmaceutical compositions for enteral and parenteral nutrition

Publication number: 20040034091

Abstract: Linear chain dicarboxylic acids having 6 to 12 carbon atoms and novel derivatives thereof, such as amides with natural amino acids and esters with biliary acids, are useful in the formulation of pharmaceutical compositions suitable for enteral and parenteral administration.

Type: Application

Filed: April 18, 2003

Publication date: February 19, 2004

Applicant: Sigma Tau Industrie Farmaceutiche Riunite S.p.A.

Inventor: Marco Castagneto
Muscarinic receptor antagonists

Patent number: 6693202

Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.

Type: Grant

Filed: August 25, 2000

Date of Patent: February 17, 2004

Assignee: Theravance, Inc.

Inventors: James Aggen, John H. Griffin, Mathai Mammen, Daniel Marquess, Edmund J. Moran, David Oare
Method for producing n-alkoxy-n-alkylamides

Publication number: 20040030142

Abstract: The invention relates to a method for producing N-alkoxy-N-alkylamides of general formula (I), wherein R1 represents C1-10 alkyl, cyclo-C5-7 alkyl, cyclo-C5-7 alkenyl, C2-10 alkenyl, aryl, aryl C1-3 alkyl, heteroaryl, heteroaryl C1-3 alkyl or heterocyclyl; and R2 represents C1-6 alkyl. The inventive compounds are characterized in that an ester of general formula (II): R1COOR3, wherein R1 has the above-mentioned meaning, and R3 represents C1-6 alkyl, 4-nitrophenyl, 2,4-dinitrophenyl, succinimido or benzotriazole-1-yl, is reacted with hydroxylamine, a hydroxylamine derivative or with a hydroxylammonium salt, and the reaction product is alkylated in the presence of a phase transfer catalyst.

Type: Application

Filed: July 24, 2002

Publication date: February 12, 2004

Inventors: Paul Hanselman, Stefan Hildbrand, Etienne Sterren
Methods of asymmetrically synthesizing enantiomers of casodex, its derivatives and intermediates thereof

Publication number: 20040030130

Abstract: A method of synthesizing pure enantiomers of acylanalides such as Casodex® (bicalutamide) and its derivatives includes contacting a compound having a ring structure that, when opened, provides a substituent having the structure of Formula I: 1

Type: Application

Filed: May 23, 2003

Publication date: February 12, 2004

Inventor: Nnochiri Nkem Ekwuribe
Process for producing crystalline atorvastatin calcium

Publication number: 20040024226

Abstract: A factory scale process for producing crystalline atorvastatin calcium includes the step of drying the isolated product in a vacuum pan dryer. The vacuum pan dryer has an agitator which is continuously rotated at a speed of approximately 1 rpm. High quality material is routinely and consistently produced with reduced cycle time.

Type: Application

Filed: August 8, 2003

Publication date: February 5, 2004

Inventors: John O'Connell, William Tully, Evelyn Madigan
Process for the preparation of amorphous atorvastatin

Publication number: 20040024046

Abstract: Atorvastatin, the substance known by the chemical name [R-(R*,R*)]-2-(4-fluorophenyl)-&bgr;,&dgr;dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt, is readily available in one of its crystalline forms as it is known from the prior art. The present invention relates to a novel process for preparing atorvastatin in an amorphous form by precipitating the atorvastatin using a solvent of a second type from a solution of atorvastatin which is provided with a solvent of a first type. This process is useful for the conversion of atorvastatin in a crystalline form into atorvastatin in an amorphous form.

Type: Application

Filed: July 7, 2003

Publication date: February 5, 2004

Inventor: Zlatko Pflaum
HMG CoA-reductase inhibitors

Publication number: 20040019100

Abstract: The invention relates to particular hydroxyl and protected hydroxyl derivatives of compounds known to be useful as HMG CoA-reductase inhibitors.

Type: Application

Filed: May 5, 2003

Publication date: January 29, 2004

Inventors: Yatendra Kumar, Ram Chander Aryan, Jitendra Sattigeri, Mohammad Salman, Gowri Shankar, Kumar Hari Bhushan, Bhargav R. Pandya, Ramnik Sharma
Substituted biphenyl derivatives, method for preparing same and pharmaceutical compositions containing same

Publication number: 20040014969

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

Type: Application

Filed: March 14, 2003

Publication date: January 22, 2004

Inventors: Carole Descamps-Francois, Said Yous, Daniel Lesieur, Gerald Guillaumet, Marie-Claude Viaud, Herve Da Costa, Caroline Bennejean, Philippe Delagranes, Pierre Renard
Antithrombotic agents

Publication number: 20040010017

Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug 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: January 17, 2003

Publication date: January 15, 2004

Inventors: Douglas Wade Beight, John Joseph Masters, Jason Scott Sawyer, Robert Theodore Shuman, Michael Robert Wiley, Ying Kwong Yee
Process for the synthesis of 1,3-diols

Publication number: 20040006231

Abstract: An improved process for the preparation of cis-1,3-diols is described where a beta hydroxy ketone is treated with a trialkylborane or dialkylalkoxyborane or a mixture of a trialkylborane and a dialkylalkoxyborane followed by recovery and reuse of the alkylborane species to convert additional beta hydroxy ketone to the cis-1,3-diol.

Type: Application

Filed: April 11, 2003

Publication date: January 8, 2004

Inventors: Robert Lee Bosch, Richard Joseph McCabe, Thomas Norman Nanninga, Robert Joseph Stahl
Electrophilic ketones for the treatment of herpesvirus infections

Patent number: 6673784

Abstract: A class of compounds is described which can be used for the treatment of viral infections. Compounds of particular interest are defined by Formula II wherein each of R1, R2, and R3 is independently selected from hydrido, halo, and nitro; wherein R8 is selected from haloalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted arylalkoxy and optionally substituted aryloxyalkyl; where Y is selected from fluoroalkyl, and wherein R9 alkylamino; or a pharmaceutically-acceptable salt or tautomer thereof.

Type: Grant

Filed: November 14, 2000

Date of Patent: January 6, 2004

Assignee: G. D. Searle & Co.

Inventors: Daniel L. Flynn, Jeffery Zablocki, Kenneth Williams, Susan L. Hockerman
Succinoylamino heterocycles as inhibitors of a beta protein production

Publication number: 20030232985

Abstract: This invention relates to novel succinoylamino heterocycles having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.

Type: Application

Filed: April 9, 2003

Publication date: December 18, 2003

Inventors: Lorin A. Thompson, Padmaja Kasireddy
Novel compounds and therapeutic uses thereof

Publication number: 20030225102

Abstract: The invention discloses a novel series of compound represented by general formula (I), 1

Type: Application

Filed: April 8, 2003

Publication date: December 4, 2003

Applicant: TORRENT PHARMACEUTICALS LTD.

Inventor: Alangudi Sankaranarayanan
Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors

Publication number: 20030216435

Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Type: Application

Filed: July 23, 2002

Publication date: November 20, 2003

Applicant: G. D. Searle & Co.

Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
Carboxylic acid derivatives, process for producing the same and drugs containing the same as the active ingredient

Publication number: 20030216381

Abstract: A carboxylic acid derivative of formula (1) 1

Type: Application

Filed: February 20, 2003

Publication date: November 20, 2003

Inventors: Kousuke Tani, Masaki Asada, Kaoru Kobayashi, Masami Narita, Mikio Ogawa
Inhibitors of dipeptidyl peptidase IV

Publication number: 20030216450

Abstract: Compounds according to general formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is O, S or CH2, X3 is NR5 or a carbonyl or thiocarbonyl group and R4 is R6R7N, R8(CH2)qOC(═O), R8(CH2)qOC(═S), R6R7NC(═O), R6R7NC(═S); R8(CH2)qC(═O), R8(CH2)qC(═S) or R8(CH2)qSO2, m is 1-3 and n is 0-4 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV. Pharmaceutical compositions of the compounds of the invention, or pharmaceutically acceptable salts thereof, are useful in the treatment of,inter alia, type 2 diabetes.

Type: Application

Filed: January 9, 2003

Publication date: November 20, 2003

Inventors: David Michael Evans, Gary Robert William Pitt
Method of making HIV protease inhibitors

Publication number: 20030216569

Abstract: A method of making HIV protease inhibitors of general formula (1): 1

Type: Application

Filed: November 21, 2002

Publication date: November 20, 2003

Inventors: Bruce A. Dressman, James E. Fritz, Marlys Hammond, William J. Hornback, Stephen W. Kaldor, Vincent J. Kalish, John E. Munroe, Siegfried Heinz Reich, John H. Tatlock, Timothy A. Shepherd, Michael J. Rodriguez
Cyclylamine sulfonamides as &bgr;3-adrenergic receptor agonists

Patent number: 6649603

Abstract: This invention provides compounds of Formula I having the structure wherein R1, R2, R3, W, X, and Z are as defined hereinbefore or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

Type: Grant

Filed: September 5, 2002

Date of Patent: November 18, 2003

Assignee: Wyeth

Inventor: Fuk-Wah Sum
Novel aromatic compounds and poly(oxyalkylene) containing aromatic compounds possessing antibacterial, antifungal or antitumor activity

Publication number: 20030212113

Abstract: The present invention provides novel compounds possessing one or more of the following activities: antibacterial, antifungal and antitumor activity.

Type: Application

Filed: December 24, 2002

Publication date: November 13, 2003

Inventors: Natalia B. Dyatkina, Dong-Fang Shi, Christopher Don Roberts, Mark Douglas Velligan, Sebastian Johannes Reinhard Liehr, Janos Botyanszki, Wentao Zhang, Alexander Khorlin, Peter Harold Nelson, Joseph Martin Muchowski
Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV

Patent number: 6645995

Abstract: Described are compounds of formula I wherein at least one of the bonds in the five-membered ring is a double bond; B is any alpha or beta amino acid connected to the ring with an amide or peptide bond; or a salt thereof with a pharmaceutically acceptable acid or base. Pharmaceutical compositions containing these compounds are also described. These compounds are useful for treating type II diabetes.

Type: Grant

Filed: February 8, 2002

Date of Patent: November 11, 2003

Assignee: Novo Nordisk A/S

Inventors: Anders Kanstrup, Jane Marie Lundbeck, Lise Brown Christiansen
Alpha-hydroxyarylbutanamine inhibitors of aspartyl protease

Publication number: 20030207934

Abstract: Acylated &agr;-hydroxyarylbutanamines and related sulfonamides, ureas and carbamates that inhibit aspartyl protease are disclosed, as are methods of treating diseases, particularly HIV, using these compounds.

Type: Application

Filed: October 22, 2001

Publication date: November 6, 2003

Inventors: Yat Sun Or, Guoqiang Wang, John Rougas, Jude Elizabeth Mathews, Kate Ryan Muldoon, Vincent Alfred Boyd, Jens Werner Eckstein, Steven Wayne Riesinger
Arylsulfonanilide ureas

Publication number: 20030207864

Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

Type: Application

Filed: March 11, 2003

Publication date: November 6, 2003

Applicant: Tulark Inc.

Inventor: Jonathan B. Houze
Convergent synthesis of alpha-aryl-beta-ketonitriles

Publication number: 20030208068

Abstract: The present invention relates to processes for the production of &agr;-aryl-&bgr;-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.

Type: Application

Filed: March 13, 2003

Publication date: November 6, 2003

Inventors: Jiacheng Zhou, Lynette May Oh, Philip Ma
Aminopyrrolidine sulfonamides as serine protease inhibitors

Publication number: 20030203936

Abstract: The present invention is directed to compounds useful as selective serine protease or dual-serine protease inhibitors, compositions thereof and methods for treating serine protease or dual-serine protease mediated disorders.

Type: Application

Filed: May 16, 2003

Publication date: October 30, 2003

Inventors: Michael N. Greco, Bruce E. Maryanoff, Michael J. Hawkins, Robert E. Boyd
Novel compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents

Publication number: 20030203951

Abstract: The present invention relates to novel compounds that can be used as antiinflammatory, immunomodulatory and antiproliferatory agents. In particular the invention refers to new compounds which inhibit dihydroorotate dehydrogenase (DHODH), a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of diseases, in particular their use in diseases where there is an advantage in inhibiting dihydroorotate dehydrogenase (DHODH).

Type: Application

Filed: July 9, 2002

Publication date: October 30, 2003

Applicant: 4SC AG

Inventors: Johan Leban, Bernd Kramer, Wael Saeb, Gabriel Garcia
Pyrrolylalkylidene-hydrazinecarboximidamide derivatives as 5-hydroxytryptamine-6 ligands

Publication number: 20030203895

Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.

Type: Application

Filed: February 13, 2003

Publication date: October 30, 2003

Applicant: Wyeth

Inventors: Michael Gerard Kelly, Ping Zhou
Propanolamine derivatives

Patent number: 6635634

Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.

Type: Grant

Filed: February 14, 2002

Date of Patent: October 21, 2003

Assignee: Fujisawa Pharmaceutical Co., Ltd.

Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
Substituted dimeric compounds

Patent number: 6635650

Abstract: The invention relates to compounds of formula (I): A-G1-Cy-G2-Cy-G3-B (I) wherein: A represents NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents NR1C(Q)R2, C(Q)NR2R3, NR1C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy represents a ring structure G2 represents a chain and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.

Type: Grant

Filed: August 8, 2001

Date of Patent: October 21, 2003

Assignee: Les Laboratoires Servier

Inventors: Daniel Lesieur, Said Yous, Carole Descamps-Francois, François Lefoulon, Gérald Guillaumet, Marie-Claude Viaud, Caroline Bennejean, Philippe Delagrange, Pierre Renard
Amide compounds and use thereof

Publication number: 20030195354

Abstract: An amide compound given by formula [I]: 1

Type: Application

Filed: December 12, 2002

Publication date: October 16, 2003

Inventor: Hiroshi Sakaguchi
Amides of aminoalkyl-substituted azetidines, pyrrolidines, piperidines and azepanes

Publication number: 20030195190

Abstract: Novel amides of aminoalkyl-substituted azetidines, pyrrolidines, piperidines and azepanes, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.

Type: Application

Filed: January 30, 2003

Publication date: October 16, 2003

Inventors: Bernd Peschke, Ingrid Pettersson
Hypoglycemic agent

Publication number: 20030191323

Abstract: The present invention provides a hypoglycemic agent containing an acylsulfonamide derivative such as a compound of the following formula or an analog thereof, which agent is usable for preventing and curing diabetes: 1

Type: Application

Filed: January 2, 2003

Publication date: October 9, 2003

Applicant: Ajinomoto Co., Inc.

Inventors: Hiroshi Ikawa, Masato Nishimura, Keiji Okada, Takashi Nakamura, Niro Inaba, Kazuhiro Kojima, Hideki Kosono
Chemical compounds

Publication number: 20030187020

Abstract: Provided herein are novel and useful compounds having a tryptase inhibition activity, pharmaceutical compositions comprising such compounds, and methods treating subjects suffering from a condition, disease, or disorder that can be ameliorated by the administration of an inhibitor of tryptase, e.g., asthma and inflammatory diseases, to name only a few.

Type: Application

Filed: April 26, 2001

Publication date: October 2, 2003

Inventors: Peter C. Astles, Paul R. Eastwood, Olivier Houille, Julian Levell, Heinz Pauls, Mark Czekaj, Guyan Liang, Yong Gong, James Pribish, Kent Neuenschwander
Selective preventives/remedies for progressive lesions after organ damage

Publication number: 20030181506

Abstract: An object of the present invention is to provide a pharmaceutical agents for preventing and/or treating the progressive lesion after the organic damage without inhibiting organic function or regeneration function thereof, by selectively suppressing the induction of cytotoxic effector macrophages which are induced into the damaged organs in response to chemokines and cytokines which are expressed depending on the type of damaged organic tissues.

Type: Application

Filed: December 12, 2002

Publication date: September 25, 2003

Inventors: Michio Ishibashi, Alain Wagner, Charles Mioskowski, Catherine Sylvain
Sulfonylaminocarboxylic acid N-arylamides as guanylate cyclase activators

Publication number: 20030171352

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

Type: Application

Filed: January 24, 2003

Publication date: September 11, 2003

Applicant: Aventis Pharma Deutschland GmbH

Inventors: Ursula Schindler, Karl Schoenafinger, Hartmut Strobel
Aminoacid-iodine complex

Publication number: 20030171598

Abstract: An amino-acid iodine complex, viz. amino-acid amino-carboxyl iodine complex, was provided wherein its coordinate center is iodine molecule, complex reagent is amino-acid, sites of complexing reaction are amino and carboxyl groups of amino-acid. The complex can be used for the production of feedstuff, food additive, disinfectant, antiseptic and medicament. Also provided is a method for the production of said complex comprising opening the inner-complex ring of amino-acid by acid catalysis and allowing the amino-acid to combine with iodine molecule to form an amino-acid amino-carboxyl iodine complex; because amino-acid is a nutriment and amino-carboxyl complex is achieved, their introduction not only increases the nutritional function of the complex and improves the stability of iodine, but also is beneficial to the environment protection and enhances the disinfecting activity against viruses and bacteria.

Type: Application

Filed: February 10, 2003

Publication date: September 11, 2003

Inventors: Xiongfei Zeng, Jiang Zeng, Yan Zeng
TRH-like peptide derivatives as inhibitors of the TRH-degrading ectoenzyme

Publication number: 20030166944

Abstract: Peptide derivatives useful as inhibitors of activity of thyrotropin-releasing hormone-degrading ectoenzyme (TRH-DE) disclosed.

Type: Application

Filed: August 19, 2002

Publication date: September 4, 2003

Applicant: The Provost, Fellows and Scholars of the College of th Holy

Inventor: Julie A. Kelly
Anticancer activity of imino acid conjugates or methylglyoxal

Patent number: 6613793

Abstract: The invention relates to the use of imino acid conjugates of methylglyoxal for the inhibition and/or treatment of cancer. The invention relates more specifically to the use imino acid conjugates of methylglyoxal for inhibition and/or treatment of cancer of the Colon, Prostate, Larynx, Kidney, Pancreas, Lung, Breast, Intestine, Oral cavity, Ovary, Glioblastoma, and Leukemia. The invention also relates to compositions and methods of inhibiting cancer using imino acid conjugates of methylglyoxal.

Type: Grant

Filed: July 1, 2002

Date of Patent: September 2, 2003

Assignee: Dabur Research Foundation

Inventors: Anand C. Burman, Rama Mukherjee, Manu Jaggi, Anu T. Singh, Kamal K. Kapoor, Sudhanand Prasad, Manju Ray
Glutaminyl based DPIV inhibitors

Publication number: 20030162820

Abstract: The present invention provides compounds of the formula: 1

Type: Application

Filed: September 16, 2002

Publication date: August 28, 2003

Inventors: Hans-Ulrich Demuth, Torsten Hoffmann, Ulrich Heiser
Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis

Patent number: 6610730

Abstract: Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.

Type: Grant

Filed: April 12, 2001

Date of Patent: August 26, 2003

Assignee: Agouron Pharmaceuticals, Inc.

Inventors: Theodore O. Johnson Jr., Ye Hua, Hiep T. Luu, Peter S. Dragovich
Alkyl urea retinoid agonists

Publication number: 20030158226

Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.

Type: Application

Filed: September 17, 2002

Publication date: August 21, 2003

Applicant: Roche Bioscience, a division of Syntex (U.S.A.) LLC

Inventors: Paula Nanette Belloni, Denis John Kertesz, Michael Klaus, Jean-Marc Lapierre
Naphthamide neurokinin antagonists for use as medicaments

Publication number: 20030158180

Abstract: A compound having the general formula (Ia) and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.

Type: Application

Filed: October 3, 2002

Publication date: August 21, 2003

Inventor: Peter Bernstein
Short-acting sedative hypnotic agents for anesthesia and sedation

Publication number: 20030153554

Abstract: The invention provides compounds compositions and methods useful for inducing or maintaining general anesthesia or sedation in mammals.

Type: Application

Filed: January 24, 2003

Publication date: August 14, 2003

Inventors: Thomas E. Jenkins, Sabine Axt, Jennifer Bolton
Pyrrolidinone derivatives

Publication number: 20030149081

Abstract: The present invention provides pharmaceutical compositions and novel compounds useful in the treatment of conditions mediated by CCR2, MCP-1 or the interaction thereof. The compounds of the present invention are pyrrolidinones and pyrrolidine-thiones.

Type: Application

Filed: September 26, 2002

Publication date: August 7, 2003

Inventors: Dong Zou, Olivier Dasse, Janelle Evans, Paul Higgins, Jeremy Kintigh, Rama Kondru, Eric Schwartz, Laurent Knerr, Hai-Xiao Zhai
Process for the production of amorphous atorvastatin calcium

Publication number: 20030149279

Abstract: A process for the preparation of amorphous atorvastatin calcium and hydrates thereof which comprises: (a) dissolving crystalline atorvastatin calcium in a non-hydroxylic solvent; (b) adding a non-polar hydrocarbon anti-solvent or adding the dissolved atorvastatin to the non-polar anti-solvent to precipitate out atorvastatin calcium; and (c) removing the solvent by filtration to afford amorphous atorvastatin calcium.

Type: Application

Filed: March 3, 2003

Publication date: August 7, 2003

Inventors: Yatendra Kumar, Rajesh Kumar Thaper, S. M. Dileep Kumar
Method for the production of acyloxy acetaldehydes

Publication number: 20030149271

Abstract: The invention relates to a method for the production of acyloxy acetaldehydes of formula (I), wherein R can represent an alkyl, aryl, heteroaryl, alkalyl, aklylheteroaryl or aralkyl radical which has been optionally substituted once or several times or a heterocycle or alkyl heterocycle which has been substituted once or several times, by reacting a compound of formula (II), wherein R has the meaning previously defined and M can be an alkali or alkaline earth atom, in an appropriate solvent with a compound of formula (III), wherein R1 and R2 independently represent a C1-C6-alkyl radical or together represent a C2-C6-alkyl radical and X represents a halogen atom, whereupon the correspondingly formed dialkylacetal of formula (IV), wherein R, R1 and R2 have the previously described meaning, undergoes acetal cleavage to obtain the desired acyloxy acetaldehyde of formula (I).

Type: Application

Filed: November 25, 2002

Publication date: August 7, 2003

Inventors: Wilhelmus Hubertus Boesten, Peter Riebel, Gerhard Niederhumer

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