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)

Cyclylamine sulfonamides as beta-3 adrenergic receptor agonists

Publication number: 20030027797

Abstract: This invention provides compounds of Formula I having the structure 1

Type: Application

Filed: September 5, 2002

Publication date: February 6, 2003

Applicant: Wyeth

Inventors: Fuk-Wah Sum, Baihua Hu
Method for producing n-alkenyl amides

Publication number: 20030028035

Abstract: A process for preparing N-alkenyl-amides by reacting the corresponding NH-amides with acetylenes in the liquid phase in the presence of basic alkali metal compounds and of a cocatalyst comprises using as the cocatalyst compounds of the general formulae (Ia) and/or (Ib)

Type: Application

Filed: June 19, 2002

Publication date: February 6, 2003

Inventors: Arnd Boettcher, Rolf Pinkos, Thomas Preiss, Rudolf Erich Lorenz
Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use

Publication number: 20030023087

Abstract: The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.

Type: Application

Filed: August 13, 2002

Publication date: January 30, 2003

Inventors: David S. Garvey, Inigo Saenz De Tejada, Richard A. Earl, Subhash P. Khanapure
Substituted pyrrole mannich bases to combat pain and allergic reactions

Publication number: 20030023100

Abstract: The invention relates to substituted pyrrole Mannich bases of general formula (I), wherein R1=H, a C1-10-alkyl-, aryl, a heteroaryl- or an aryl, heteroaryl-, CN, Br—, Cl or OH radical bound by a C1-6 alkylene group, R2=CH(R4)N(R5)(R6), R3, R3′, R3″ identically or individually represent H, F, Cl, Br, CF3, CN, NO2, SO2NH2, NHR′, SR8, OR9, CO(OR10), CH2CO(OR11), COR15, a C1-10-alkyl-, aryl-, heteroaryl- aryl radical or a heteroalkyl radical bound by a C1-6 alkylene group, R4=an unsubstituted phenyl radical or a phenyl radical substituted at least with C1-4 alkyl, C1-3-alkoxy-, halogen-, a method for the production of the above-mentioned compounds, medicaments containing said compounds, and the use of said compounds in the production of medicaments.

Type: Application

Filed: June 25, 2002

Publication date: January 30, 2003

Inventors: Matthias Gerlach, Corinna Maul
Alpha-aminoacetic acid derivatives- alpha4beta7 receptor antagonists

Publication number: 20030018195

Abstract: Disclosed are compounds which bind &agr;4&bgr;7 integrin. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by &agr;4&bgr;7 integrin. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Type: Application

Filed: May 20, 2002

Publication date: January 23, 2003

Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett
Pyruvate derivatives

Publication number: 20030013846

Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.

Type: Application

Filed: May 3, 2002

Publication date: January 16, 2003

Inventors: Bing Wang, Guy Miller, Satyanarayana Janagani, Wei Zhang
Pyruvate derivatives

Publication number: 20030013657

Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.

Type: Application

Filed: May 3, 2002

Publication date: January 16, 2003

Inventors: Bing Wang, Guy Miller, Satyanarayana Janagani
Cyclic AMP-specific phosphodiesterase inhibitors

Publication number: 20030013754

Abstract: Pyrrole 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: January 22, 2002

Publication date: January 16, 2003

Applicant: ICOS Corporation

Inventors: Timothy J. Martins, Kerry W. Fowler, Amy Oliver, Carmen C. Hertel
PROCESS FOR THE REMOVAL OF NITROBENZENESULFONYL

Publication number: 20030009056

Abstract: A 2- or 4-nitrobenzenesulfonamide is allowed to react with an alkali metal alkoxide to remove a nitrobenzenesulfonyl group to thereby obtain an amine corresponding to the amide. Furthermore, a method for producing an amine derivative by allowing the resulting amine without isolation to react with an activated, substituted oxycarbonyl compound or an activated acyl compound is provided. According to this method, a corresponding free amine and its substituted derivative can be produced easily and industrially advantageously from the 2- or 4-nitrobenzenesulfonamide without using a thiol compound.

Type: Application

Filed: June 11, 2002

Publication date: January 9, 2003

Inventor: Nobuo Nagashima
Cyclic a-amino-y hydroxyamide compounds

Publication number: 20030004138

Abstract: Compound of formula (I): 1

Type: Application

Filed: June 18, 2002

Publication date: January 2, 2003

Inventors: Michel Wierzbicki, Jean-Marie Fourquez, Nigel Levens, Bernadette Hussson-Robert, Olivier Nosjean, Michelle Boulanger
Cyclic derivatives as modulators of chemokine receptor activity

Publication number: 20030004151

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

Type: Application

Filed: December 20, 2001

Publication date: January 2, 2003

Inventor: Robert Cherney
Amino ceramide - like compounds and therapeutic methods of use

Publication number: 20020198240

Abstract: Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.

Type: Application

Filed: April 29, 2002

Publication date: December 26, 2002

Inventors: James A. Shayman, Norman S. Radin
2,4-substituted pyrrolidine derivatives-CCR-3 receptor antagonists

Publication number: 20020198255

Abstract: This invention relates to certain 2,4-substituted pyrrolidine derivatives that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Type: Application

Filed: December 19, 2001

Publication date: December 26, 2002

Inventors: Denis John Kertesz, Michael Garret Roepel
Propanolamine derivatives

Patent number: 6495546

Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.

Type: Grant

Filed: November 22, 2000

Date of Patent: December 17, 2002

Assignee: Fujisawa Pharmaceutical Co., Ltd.

Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
Novel olefination process to itaconate and succinate derivatives

Publication number: 20020188121

Abstract: An efficient and selective process, capable of scale-up, to make itaconate derivatives of formula (IV), and/or succinate derivatives of formula (V) and/or (VI) by asymmetric hydrogenation of the itaconate derivatives.

Type: Application

Filed: July 18, 2002

Publication date: December 12, 2002

Inventors: Andrew Michael Derrick, Nicholas Murray Thomson
3.4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents

Patent number: 6492413

Abstract: A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: wherein Y is selected from O, S and NR1; wherein R1 is selected from hydrido and lower alkyl; wherein X is one or two substituent selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R2 and R3 are independently aryl or heteroaryl; and wherein R2 and R3 are optionally substituted at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.

Type: Grant

Filed: March 20, 2000

Date of Patent: December 10, 2002

Assignee: G.D. Searle & Co.

Inventors: John J. Talley, Stephen R Bertenshaw, Paul W Collins, Thomas D. Penning, David B. Reitz, Roland S Rogers
Process for the preparation of amorphous atorvastatin

Publication number: 20020183527

Abstract: Atorvastatin, the substance known by the chemical name [R-(R*,R*)]-2-(4-fluorophenyl)-&bgr;,&dgr;-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(penylamino)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: June 6, 2002

Publication date: December 5, 2002

Inventor: Zlatko Pflaum
Novel crystal forms of atorvastatin hemi-calcium and processes for their preparation as well as novel processes for preparing other forms

Publication number: 20020183378

Abstract: The present invention provides novel forms of atorvastatin designated Forms VI, VIII, IX, X, XI and XII and novel processes for their preparation as well as processes for preparing atorvastatin Forms I, II, IV, V and amorphous atorvastatin.

Type: Application

Filed: November 29, 2001

Publication date: December 5, 2002

Inventors: Judith Aronhime, Ramy Lidor-Hadas, Valerie Niddam, Revital Lifshitz, Eti Ishai, Guy Sambursky
Dipeptide derivatives

Publication number: 20020183260

Abstract: Compounds of the formula 1

Type: Application

Filed: May 9, 2002

Publication date: December 5, 2002

Inventor: Cynthia Anne Fink
Modulators of proteins with phosphotyrosine recognition units

Publication number: 20020183518

Abstract: Y—X—C(R′)═C(R″)COOR″′ (A1)

Type: Application

Filed: November 27, 2001

Publication date: December 5, 2002

Applicant: ONTOGEN CORPORATION

Inventors: Adnan M. M. Mjalli, Xiaodong Cao, Edmund J. Moran
Methods for the stereoselective synthesis of substituted piperidines

Publication number: 20020177721

Abstract: One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.

Type: Application

Filed: December 4, 2001

Publication date: November 28, 2002

Inventors: Brian M. Aquila, Thomas D. Bannister, Gregory C. Cuny, James R. Hauske, Michele L.R. Heffernan, Michael Z. Hoemann, Donald W. Kessler, Liming Shao, Xinhe Wu, Roger L. Xie
Botanical drug for treatment and prevention of alzhimer's disease

Patent number: 6486169

Abstract: The present invention related to safe botanical drug for treatment and prevention of Alzheimer's disease. Specifically, this invention proves a safe botanical drug, Huperzine (HUE) and Clausenamide (CLE) and their preparation. HUE has the following pharmaceutical functions: inhibiting acetylcholinesterase (CAT), increasing memory, decreasing Alzheimer amyloid protein, increasing RNA and protein synthesis of brain, increasing calcium in brain, decreasing superoxide anion. CLE has the following pharmaceutical functions: increasing memory, decreasing Alzheimer amyloid protein, increasing RNA and protein synthesis of brain, increasing calcium in brain, decreasing superoxide anion, increasing long-term potentiation and increasing dopanmine (DA). It is important that HUE combined with CLE have stronger function as mentioned above.

Type: Grant

Filed: February 19, 2002

Date of Patent: November 26, 2002

Inventor: Yaguang Liu
N-oxides of heterocyclic esters, amides, thioesters, and ketones

Patent number: 6486151

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 26, 2001

Date of Patent: November 26, 2002

Assignee: GPI NIL Holdings Inc.

Inventors: Gregory S. Hamilton, Joseph P. Steiner, Eric S. Burak
Substituted aryl and heteroaryl derivatives, their production and their use as medicines

Patent number: 6479524

Abstract: Compounds that prolong thrombin time. Exemplary are: (a) rac-4-{3-[5-ethoxycarbonylmethyl-2-methyl-4-(2-methyl-pyrrolidinocarbonyl)-phenyl]-propargylamino}benzamidine, (b) rac-4-{3-[2,5-dimethyl-4-(2-methyl-pyrrolidinocarbonyl)-phenyl]-propargylamino}benzamidine, and (c) 4-[3-(2,5-dimethyl-4-isopropylcarbonyl-phenyl)propargyl-amino]benzamidine.

Type: Grant

Filed: October 18, 2001

Date of Patent: November 12, 2002

Assignee: Boehringer Ingelheim Pharma KG

Inventors: Henning Priepke, Iris Kauffmann-Hefner, Norbert Hauel, Uwe Ries, Herbert Nar, Jean Marie Stassen, Wolfgang Wienen
Fungicides containing pyrrolidones as their active agents

Patent number: 6476061

Abstract: The invention relates to fungicides containing compounds of formula (I) as their active agents, the radicals in said formula (I) having the following meanings: R1 is hydrogen, C1-C6-alkyl, C1-C6-alkylcarbonyl, formyl or C1-C6-halogenalkylcarbonyl; R2 is hydrogen, C1-C6-alkyl or C1-C6-halogenalkyl; R3-R12 are hydrogen, halogen, C1-C8-cycloalkyl, C1-C6-alkyl, C1-C6-halogenalkyl, C1-C6-alkoxy, C1-C6-halogenalkoxy, C1-C6-alkylsulfonyl, C1-C6-halogenalkylsulfonyl, formyl, cyano, C1-C6-alkylthio or phenyl which can optionally be substituted by halogen atoms, C1-C6-alkyl or C1-C6-halogenalkyl groups, and to their agriculturally usable salts. The invention also relates to methods for combating fungi in plants using these fungicides.

Type: Grant

Filed: May 9, 2001

Date of Patent: November 5, 2002

Assignee: BASF Aktiengesellschaft

Inventors: Joachim Rheinheimer, Karl Eicken, Ingo Rose, Thomas Grote, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Gerhard Hamprecht
Novel peptides as NS3-serine protease inhibitors of hepatitis C virus

Publication number: 20020160962

Abstract: The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Type: Application

Filed: July 19, 2001

Publication date: October 31, 2002

Inventors: Anil K. Saksena, Viyyoor Moopil Girijavallabhan, Stephane L. Bogen, Raymond G. Lovey, Edwin E. Jao, Frank Bennett, Jinping L. Mc Cormick, Haiyan Wang, Russell E. Pike, Yi-Tsung Liu, Tin-Yau Chan, Zhaoning Zhu, Ashok Arasappan, Kevin X. Chen, Srikanth Venkatraman, Tejal Parekh, Patrick A. Pinto, Bama Santhanam, F. George Njoroge, Ashit K. Ganguly, Henry A. Vaccaro, Scott Jeffrey Kemp, Odile Esther Levy, Marguerita Lim-Wilby, Susan Y. Tamura
Illudin analogs useful as antitumor agents

Publication number: 20020161206

Abstract: The present invention provides illudin analogs of the general formula (I): 1

Type: Application

Filed: April 29, 2002

Publication date: October 31, 2002

Applicant: The Regents of the University of California

Inventors: Trevor C. McMorris, Michael J. Kelner
Process for producing crystalline atorvastatin calcium

Publication number: 20020161239

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: June 14, 2002

Publication date: October 31, 2002

Inventors: John O'Connell, William Tully, Evelyn Madigan
Arylacetamido-ketobenzoxazole as cysteine protease inhibitors

Publication number: 20020156063

Abstract: The present invention thus provides compounds of Formula I: 1

Type: Application

Filed: April 8, 2002

Publication date: October 24, 2002

Inventors: Eduardo L. Setti, Shankar Venkatraman
Process for the preparation of zofenopril calcium salt

Publication number: 20020156293

Abstract: A process for the preparation of polymorph A of zofenopril calcium salt in substantially pure form, which comprises: 1) reaction of S(-)-3-benzoylthio-2-methylpropanoic acid chloride with cis-4-phenylthio-L-proline in water at pH ranging from 9.0 to 9.5 and recovery of zofenopril in the acidic form; b) salification of acid zofenopril with a potassium salt in alcoholic solution, and recovery of the resulting potassium salt; c) conversion of the potassium salt to the calcium salt by addition of zofenopril potassium salt aqueous solution to a CaCl2 aqueous solution at a temperature of 70-90° C. with simultaneous seeding to promote the precipitation of polymorph A.

Type: Application

Filed: May 28, 2002

Publication date: October 24, 2002

Applicant: MENARI RICERCHE S.P.A.

Inventors: Raffaello Giorgi, Antonio Giachetti, Carlo Mannucci, Anita Falezza, Rosaria Pirari, Alberta Giorgi
Factory scale process for producing crystalline atorvastatin trihydrate hemi calcium salt

Publication number: 20020156294

Abstract: A factory scale process for producing crystalline atorvastatine trihydrate hemi calcium salt includes the addition of extra methyl tert-butyl ether to the reaction mixture to supersaturate the crystallization matrix. A seed slurry is made up in a make-up/delivery vessel and delivered, under pressure, to the reaction mixture. The process produces crystalline atorvastatin calcium within a consistent size range on a factory scale.

Type: Application

Filed: June 14, 2002

Publication date: October 24, 2002

Inventor: William Tully
Carboxylic acid amides having antithrombotic activity

Publication number: 20020151595

Abstract: Compounds with antithrombotic activity and factor Xa-inhibiting activity of the general formula: 1

Type: Application

Filed: January 17, 2002

Publication date: October 17, 2002

Inventors: Uwe Joerg Ries, Henning Priepke, Herbert Nar, Jean-Marie Stassen, Wolfgang Wienen
Substituted arylamine derivatives and methods of use

Publication number: 20020147198

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Type: Application

Filed: January 10, 2002

Publication date: October 10, 2002

Inventors: Guoqing Chen, Guolin Cai, Celia Dominguez, Julie Germain, Joseph L. Kim, Tae-Seong Kim, Leon M. Smith, Andrew Tasker, Chester Chenguang Yuan, Shon Booker, Michael Croghan, Lucian DiPietro, Daniel Elbaum, Qi Huang, Ning Xi, Shimin Xu, Vinod F. Patel
Glucagon antagonists/inverse agonists

Publication number: 20020143186

Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism, such as dyslipidemia, and obesity.

Type: Application

Filed: June 22, 2001

Publication date: October 3, 2002

Inventors: Anker Steen Jorgensen, Inge Thoger Christensen, Janos Tibor Kodra, Christian Sams, Carsten Behrens, Peter Madsen, Jesper Lau
Cyclic AMP-specific phosphodiesterase inhibitors

Patent number: 6458787

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: Grant

Filed: May 2, 2001

Date of Patent: October 1, 2002

Assignee: 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. Schlacter
Methods for crystallization of n-(1(s)-ethoxycarbonyl-3-phenylpropyl)-l-alanine n-carboxyanhydride

Publication number: 20020137944

Abstract: A crystallization is carried out by adding a solution of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine N-carboxylic anhydride in a good solvent to an aliphatic hydrocarbon solvent while inhibiting the oil formation and scaling of said N-carboxylic anhydride.

Type: Application

Filed: April 24, 2002

Publication date: September 26, 2002

Inventor: Masafumi Fukae
Synthesis of compounds useful in the manufacture of ketorolac

Publication number: 20020137945

Abstract: A multi-step method of synthesizing ketorolac, an analgesic compound, is shown. Several of the reactions and intermediate compounds are novel. The reaction sequence begins with the known compound N-2-bromoethylpyrrole.

Type: Application

Filed: February 5, 2002

Publication date: September 26, 2002

Inventors: Douglas C. Caskey, John R. Duchek, Henry J. Buehler
Novel heterocyclic amide derivatives

Publication number: 20020132810

Abstract: A compound of the formula 1

Type: Application

Filed: January 31, 2001

Publication date: September 19, 2002

Inventors: Matthew F. Brown, Christopher S. Poss
Phosgene-free process for preparing carbamates

Publication number: 20020120140

Abstract: A phosgene-free method for preparing a carbamate from a compound containing an amine group involves reacting the compound with an alkylating agent in the presence of carbon dioxide and cesium carbonate. A reaction can take place under standard pressure and temperature conditions and produces carbamates in a high yield with low by-product formation.

Type: Application

Filed: October 24, 2001

Publication date: August 29, 2002

Inventor: Byung H. Lee
Synthesis of 4-substituted pyrrole-2-carbaldehyde compounds

Patent number: 6441194

Abstract: The invention relates to an a process for making a 4-substituted pyrrole-2-carbaldehyde compound comprising reacting: a. a pyrrole-2-carbaldehyde compound; and b. an alkylating agent; c. in the presence of at least one catalyst; to form a 4-alkyl substituted pyrrole-2-carbaldehyde compound.

Type: Grant

Filed: October 23, 2000

Date of Patent: August 27, 2002

Assignee: Emory University

Inventors: Lanny S. Liebeskind, Wansheng Liu
Thrombin or factor Xa inhibitors

Publication number: 20020115854

Abstract: This invention relates generally to inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.

Type: Application

Filed: December 4, 2001

Publication date: August 22, 2002

Inventors: Patrick Y.S. Lam, Charles G. Clark, John M. Fevig, Robert A. Galemmo, Qi Han, Irina C. Jacobson, Renhau Li, Donald J.P. Pinto, Ruth R. Wexler
Multi-functional reagent for erythrocytes

Publication number: 20020115118

Abstract: A multifunctional reagent for erythrocytes containing an amount sufficient to produce the lysis of erythrocytes or the sphering of erythrocytes in such a way that they can be detected by a cytometer or an automatic counting device, of a carbamate or of an agent inducing the formation by the erythrocytes, from carbonate and from a nitrogenated heterocycle or ammonium ions, of a carbamate combined with the absorption of CO2 by said erythrocytes, process for lysing or sphering erythrocytes and preparation process for leucocytes.

Type: Application

Filed: September 14, 2001

Publication date: August 22, 2002

Applicant: IMMUNOTECH

Inventors: Andre van Agthoven, Jean-Pierre Daziano, John Allen Maples
Atorvastatin hemi-calcium form VII

Publication number: 20020115709

Abstract: The present invention provides a novel form of atorvastatin hemi-calcium designated Form VII and novel processes for its preparation whereby another crystalline form of atorvastatin hemi-calcium is suspended in ethanol, preferably absolute ethanol, and is converted to the new form, which is then isolated. The present invention further provides a method of reducing the plasma low density lipoprotein level in patients suffering from or susceptible to hypercholesterolemia and compositions and dosage forms for practicing the invention.

Type: Application

Filed: November 5, 2001

Publication date: August 22, 2002

Inventors: Judith Aronhime, Ramy Lidor-Hadas, Valerie Niddam, Revital Lifshitz
Novel succinate compounds, compositions and methods of use and preparation

Publication number: 20020115863

Abstract: Novel hydroxamic acid compounds are disclosed. These hydroxamates inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes. The hydroxymates are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as matrix metalloproteinases (MMPs). Methods of synthesis and of use of the compounds are also disclosed.

Type: Application

Filed: December 13, 2000

Publication date: August 22, 2002

Inventors: Dinesh Patel, Jeffrey W. Jacobs, Rakesh Jain, Zhi-Jie Ni, Zhengyu Yuan
Pesticidal 1-polyarylpyrroles

Patent number: 6433002

Abstract: A compound of formula (I): compositions containing them and methods of use to control pests.

Type: Grant

Filed: April 12, 2001

Date of Patent: August 13, 2002

Assignee: Rhone-Poulenc Inc.

Inventors: Jamin Huang, Scot Kevin Huber
Thyromimetic organic compounds

Publication number: 20020107390

Abstract: Compounds of the formula 1

Type: Application

Filed: August 16, 2001

Publication date: August 8, 2002

Inventor: Paivi J. Kukkola
Process for preparing pyrrolidone derivative

Patent number: 6429316

Abstract: Disclosed is a process for preparing a pyrrolidone derivative, which comprises allowing at least one of &ggr;-butyrolactone, 4-hydroxybutyric acid, and a low-molecular polymer of 4-hydroxybutyric acid to react with an alkylamine, wherein (i) the content of a primary amine in said alkylamine is 85% by weight or lower, and (ii) the molar ratio of the total amount of the charged primary and secondary amines to the total amount of the charged &ggr;-butyrolactone, 4-hydroxybutyric acid, and low-molecular 4-hydroxybutyric acid polymers satisfies formula: 1.0≦(A1+A2/2.5)/(B1+B2+B3) wherein A1, A2, B1, B2, and B3 represent the molar amounts of a primary amine, a secondary amine, &ggr;-butyrolactone, 4-hydroxybutyric acid, and low-molecular 4-hydroxybutyric acid polymers, respectively.

Type: Grant

Filed: November 23, 1999

Date of Patent: August 6, 2002

Assignee: Mitsubishi Chemical Corporation

Inventors: Kazunari Takahashi, Yoko Seto, Masaru Utsunomiya, Souichi Orita, Kazutaka Maruyama, Tomonori Okubi
Cyclic hydroxamic acids as metalloproteinase inhibitors

Patent number: 6429213

Abstract: The present application de gibes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease inhibitors.

Type: Grant

Filed: June 17, 1999

Date of Patent: August 6, 2002

Inventors: Chu-Biao Xue, Carl P. Decicco, Xiaohua He
Benzene tricarboxylic acid derivatives as insulin receptor activators

Publication number: 20020103183

Abstract: Compounds of Formula I, and pharmaceutical compositions containing these compounds, activate the insulin receptor kinase, which leads to an increased sensitivity to insulin and an increase in glucose uptake, and are therefore useful for the treatment of animals, especially humans, with hyperglycemia, especially for the treatment of type 2 diabetes. Processes for preparation of the compounds, and their use in assays, are also disclosed.

Type: Application

Filed: September 6, 2001

Publication date: August 1, 2002

Inventors: Louise Robinson, Prasad V.V.S.V. Manchem, Nicolas Cairns, Steven R. Schow
Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV

Publication number: 20020103384

Abstract: Described are compounds of formula I 1

Type: Application

Filed: February 8, 2002

Publication date: August 1, 2002

Inventors: Anders Kanstrup, Jane Marie Lundbeck, Lise Brown Christiansen

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