Chalcogen Attached Indirectly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 549/58)
-
Patent number: 6586463Abstract: Compounds having the general structure: which are useful for the treatment of a variety of diseases and conditions, such as bone disorders.Type: GrantFiled: September 4, 2001Date of Patent: July 1, 2003Assignee: The Procter & Gamble CompanyInventors: Mitchell Anthony deLong, David Lindsey Soper, John August Wos, Biswanath De
-
Publication number: 20030109570Abstract: A benzothiophene derivative represented by formula (1): 1Type: ApplicationFiled: September 20, 2002Publication date: June 12, 2003Inventors: Hidetoshi Tsunoda, Nobuyuki Fukuzawa, Kyoko Chiba, Toshifumi Nakao, Noriaki Asada, Nozomi Takebayashi, Kenji Kibayashi, Hideyuki Migita, Maki Morikawa
-
Patent number: 6562807Abstract: 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: GrantFiled: June 22, 2001Date of Patent: May 13, 2003Assignee: Novo Nordisk A/SInventors: Anker Steen Jorgensen, Inge Thoger Christensen, Janos Tibor Kodra, Christian Sams, Carsten Behrens, Peter Madsen, Jesper Lau
-
Patent number: 6555028Abstract: Described are polymeric matrix compatibilized naphthopyran compounds, examples of which are certain 2H-naphtho[1,2-b]pyrans, 3H-naphtho[2,1-b]pyrans and indeno[2,1-f]naphtho[1,2-b]pyrans each having at least one substituent containing terminal and/or pendant groups selected from hydroxyl, carboxyl, sulfo, sulfono, (meth)acryloxy, 2-(methacryloxy)ethylcarbamyl, epoxy or a mixture thereof. Specific substituents are also present on the naphtho, indeno and/or pyrano portions of the compounds. These compounds may be represented by the following graphic formulae: Also described are various substrates that contain or that are coated with such compounds. Optically clear articles such as contact lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, are also described.Type: GrantFiled: April 6, 2001Date of Patent: April 29, 2003Assignee: Transitions Optical, Inc.Inventors: Robert W. Walters, Barry Van Gemert
-
Patent number: 6555697Abstract: The invention concerns a novel method for preparing a benzofuran or benzothiophene compound by cyclizing an aromatic compound bearing a side-chain comprising at least two carbon atoms, one of the carbon atoms being bound to the benzene cycle by an oxygen or sulphur atom, the other carbon atom is in carboxylic form and a formyl radical in ortho position relative to said chain. The inventive method is characterised in that it consists in cyclizing the latter in the presence of an efficient amount of a carbonate base in a medium comprising a carboxylic acid anhydride and optionally an organic solvent.Type: GrantFiled: April 11, 2002Date of Patent: April 29, 2003Assignee: Rhodia ChimieInventor: Thierry Schlama
-
Patent number: 6518264Abstract: Disclosed are azetidine derivatives of formula: their optical isomers, their salts, their preparation and medicaments containing them.Type: GrantFiled: March 9, 2001Date of Patent: February 11, 2003Assignee: Aventis Pharma S.A.Inventors: Daniel Achard, Hervé Bouchard, Jean Bouquerel, Marc Capet, Serg Grisoni, Jean-Luc Malleron, Serge Mignani, Augustin Hittinger
-
Patent number: 6515124Abstract: Aromatic dehydroamino acids are disclosed that are active as LFA-1 arnagonists This activity enables these compounds to prevent inflammation which is a consequence of T cell activation and accordingly reduce or eliminate inflammatory skin disease psoriasis.Type: GrantFiled: January 5, 2001Date of Patent: February 4, 2003Assignee: Hoffman-La Roche Inc.Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
-
Patent number: 6495546Abstract: 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: GrantFiled: November 22, 2000Date of Patent: December 17, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
-
Patent number: 6492416Abstract: The present invention provides a novel class of 4,5-diaryl-3(2H)-furanone derivatives, which inhibit strongly and selectively COX-2 over COX-1. They are useful to treat inflammation, inflammation-associated disorders, and COX-2 mediated diseases.Type: GrantFiled: November 27, 2001Date of Patent: December 10, 2002Assignee: Pacific CorporationInventors: Song Seok Shin, Min-Soo Noh, Young Joo Byun, Jin Kyu Choi, Jin Kwan Kim, Kyung Min Lim, Ji Young Kim, Young Hoon Choi, Jun-Yong Ha, Ki-Wha Lee, Joo Hyun Moh, Yeon Su Jeong, Shin Chung, Yung Hyup Joo, Chang Hoon Lee, Seon Hwa Kang, Young-Ho Park, Jung Bum Yi
-
Patent number: 6482859Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or by C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl: or a group NR11R12 wherein R11 and R12 are each independently of the other hydrogen or C1-C8alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eaType: GrantFiled: February 4, 2000Date of Patent: November 19, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: Martin Zeller, André Jeanguenat
-
Patent number: 6465508Abstract: Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.Type: GrantFiled: February 23, 2001Date of Patent: October 15, 2002Assignee: WyethInventors: Frances Christy Nelson, Arie Zask, James Ming Chen, Dominick Mobilio, Ramaswamy Nilakantan
-
Patent number: 6441196Abstract: Novel processes and intermediates useful in the preparation of 11-oxa prostaglandin analogs are disclosed.Type: GrantFiled: May 18, 2001Date of Patent: August 27, 2002Assignee: Alcon, Inc.Inventors: Pete Delgado, Raymond E. Conrow, William D. Dean, Michael S. Gaines
-
Patent number: 6432983Abstract: The instant invention provides compound of formula I wherein: R1 is —H, —OH, —O(C1-C4 alkyl), —O—CO—(C1-C6 alkyl), —O—CO—O(C1-C6 alkyl), —O—CO—Ar in which Ar is optionally substituted phenyl, or —O—SO2—(C4-C6 alkyl); R2 is —H, —OH, —O(C1-C4 alkyl), —O—CO—(C1-C6 alkyl), —O—CO—O(C1-C6 alkyl), —O—CO—Ar in which Ar is optionally substituted phenyl, —O—SO2—(C4-C6 alkyl), —F, —Cl, or —Br; n is an integer from 5 to 8; R3 and R4 each are independently C1-C4 alkyl, or combine to form, with the nitrogen to which they are attached, piperidinyl, pyrrolidinyl, methylpyrrolidinyl, dimethylpyrrolidinyl, or hexamethyleneimino; or a pharmaceutically acceptable salt or solvate thereof, intermediates, pharmaceutical formulations, processes, and methods of use.Type: GrantFiled: June 30, 1997Date of Patent: August 13, 2002Assignee: Eli Lilly and CompanyInventors: George Joseph Cullinan, Kennan Joseph Fahey
-
Patent number: 6433004Abstract: The present invention relates to novel substituted &bgr;,&ggr;-fused lactones, to processes for their preparation and to their use for the prevention and/or treatment of disorders caused by hyper- or hypofunction of the glutamatergic system, in particular of cerebral ischaemias, craniocerebral trauma, states of pain or CNS-mediated spasms.Type: GrantFiled: July 14, 2000Date of Patent: August 13, 2002Assignee: Bayer AktiengesellschaftInventors: Andreas Stolle, Horst-Peter Antonicek, Stephen Lensky, Arnd Voerste, Thomas Müller, Jörg Baumgarten, Karsten von dem Bruch, Gerhard Müller, Udo Stropp, Ervin Horváth, Jean-Marie-Viktor de Vry, Rudy Schreiber
-
Publication number: 20020086891Abstract: The present invention relates to heteroaromate OSC inhibitors. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.Type: ApplicationFiled: October 31, 2001Publication date: July 4, 2002Inventors: Johannes Aebi, Jean Ackermann, Henrietta Dehmlow, Hans-Peter Maerki, Olivier Morand
-
Patent number: 6407100Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.Type: GrantFiled: September 1, 1993Date of Patent: June 18, 2002Assignee: Bayer AktiengesellschaftInventors: Hans Peter Isenring, Bettina Weiss
-
Patent number: 6391916Abstract: Novel C3-substituted cyclodeca-1,5-diynes can be prepared through novel synthetic procedures using starting (E)-C3-substituted-4-(aryl- or heteroarylmethylidene)cyclodeca-1,5-diynes reagents. Both the C3-substituted cyclodeca-1,5-diyn-3-enes and the starting reagents have improved thermal stability compared to unsubstituted counterparts.Type: GrantFiled: July 21, 2000Date of Patent: May 21, 2002Assignee: The Hong Kong University of Science and TechnologyInventors: Wei-Min Dai, Anxin Wu, Yuk Ha Lee, Wataru Hamaguchi, Sei-ichi Nishimoto, Ling Zhou, Atsushi Ishii
-
Patent number: 6388105Abstract: Compounds of the formula Where the variables are defined as in the specification, are selective agonists of RXR retinoid receptors.Type: GrantFiled: September 27, 2001Date of Patent: May 14, 2002Assignee: Allergan Sales, Inc.Inventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
-
Patent number: 6384281Abstract: A pharmaceutical compound of formula (I) in which R1 and R2 are each hydrogen or C1-4 alkyl, or R1 and R2 together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, or morpholino group, said group being optionally substituted with 1 to 3 C1-4alkyl substituents, R3 is a naphythyl, indolyl, benzothienyl, benzofuranyl, benzothiazolyl, quinolinyl or isoquinolinyl group, said group being optionally substituted, and n is 1 or 2; or a salt or ester thereof.Type: GrantFiled: October 3, 2001Date of Patent: May 7, 2002Assignee: Eli Lilly and CompanyInventors: Martine Keenan, Sandra Ginette Milutinovic, David Edward Tupper
-
Patent number: 6380221Abstract: This invention is directed to compounds of formula (III): wherein B, C, D, E, R1, R2 and R3 are disclosed herein. These components are disclosed as being useful as anti-coagulants.Type: GrantFiled: August 3, 2000Date of Patent: April 30, 2002Assignee: Berlex Laboratories, Inc.Inventors: Damian O. Arnaiz, Yuo-Ling Chou, Brian D. Griedel, Rushad E. Karanjawala, Monica J. Kochanny, Wheeseong Lee, Amy Mei Liang, Michael M. Morrissey, Gary B. Phillips, Karna Lyn Sacchi, Steven T. Sakata, Kenneth J. Shaw, R. Michael Snider, Shung C. Wu, Bin Ye, Zuchun Zhao
-
Patent number: 6376534Abstract: Compounds of general formula I are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain. Intermediates to the compounds of the formula I are also claimed.Type: GrantFiled: June 1, 2000Date of Patent: April 23, 2002Assignee: Astrazeneca Canada Inc.Inventors: Daniel Delorme, Vlad Gregor, Edward Roberts, Eric Sun
-
Patent number: 6362216Abstract: The present invention is directed to compounds which are capable of inhibiting the activity of tryptase. Such compounds are useful in the treatment or prevention of inflammatory disease, particularly those disease states which are mediated by mast cell activation. Also encompassed by the invention are formulations comprising the noted compounds, processes for preparing such compounds and methods for treating or preventing an inflammatory disease.Type: GrantFiled: May 3, 2000Date of Patent: March 26, 2002Assignee: Array Biopharma Inc.Inventors: Laurence E. Burgess, James P. Rizzi
-
Patent number: 6359148Abstract: The invention described novel compounds of formula wherein the general symbols are as defined in claim 1, as stabilisers for protecting organic materials, in particular polymers and lubricants, against thermal, oxidative or light-induced degradation.Type: GrantFiled: July 23, 1998Date of Patent: March 19, 2002Inventors: Peter Nesvadba, Samuel Evans, Christoph Kröhnke, Jürg Zingg
-
Patent number: 6350754Abstract: The present invention relates to novel 3-(cycloalkano-heteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.Type: GrantFiled: January 12, 2000Date of Patent: February 26, 2002Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
-
Patent number: 6346628Abstract: Processes for producing compounds of the formula (VI) are disclosed. Benzothiophenecarboxylic acid derivatives of the formula (I), which are useful as starting materials for producing drugs, are disclosed. Particularly, disclosed is a process for preparing 5-dydroxybenzo[b]-thiophene-3-carboxylic acid derivatives of the formula (VI), which are specific PGD2 antagonists are also disclosed.Type: GrantFiled: September 26, 2001Date of Patent: February 12, 2002Assignee: Shionogi & Co., Ltd.Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu
-
Patent number: 6340691Abstract: Compounds of the formula are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.Type: GrantFiled: January 27, 2000Date of Patent: January 22, 2002Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, Aranapakam M. Venkatesan, Derek C. Cole, James M. Chen, Jamie M. Davis, George T. Grosu
-
Patent number: 6340694Abstract: The diarylbenzopyran derivatives represented by formula I, and the pharmaceutically acceptable salts thereof, are disclosed. The composition comprising the compound of formula I, or a pharmaceutically acceptable salt thereof, shows an excellent selective inhibition of cyclooxygenase-2.Type: GrantFiled: February 20, 2001Date of Patent: January 22, 2002Assignee: Pacific CorporationInventors: Yung Hyup Joo, Chang Hoon Lee, Min-Soo Noh, Jun-Yong Ha, Jin Kyu Choi, Kyung Min Lim, Jin Kwan Kim, Seon-Hwa Kang
-
Patent number: 6329421Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: February 25, 1997Date of Patent: December 11, 2001Assignee: Merck Frosst Canada & Co.Inventors: Petpiboon Prasit, Daniel Guay, Zhaoyin Wang, Serge Leger, Michel Therien
-
Patent number: 6319930Abstract: 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 and G2 represents a chain and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: March 24, 2000Date of Patent: November 20, 2001Assignee: Adir et CompagnieInventors: Daniel Lesieur, Said Yous, Carole Descamps-Francois, François Lefoulon, Gérald Guillaumet, Marie-Claude Viaud, Caroline Bennejean, Philippe Delagrange, Pierre Renard
-
Patent number: 6316487Abstract: The subject invention pertains to novel compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. The new compounds can have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The product can also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.Type: GrantFiled: October 6, 2000Date of Patent: November 13, 2001Assignee: Aryx TherapeuticsInventors: Pascal Druzgala, Peter G. Milner
-
Patent number: 6313122Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a 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: GrantFiled: March 20, 2000Date of Patent: November 6, 2001Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, 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
-
Patent number: 6310074Abstract: The invention relates to compound of formula (I): A—G1—Cy—G2—Cy′—G3—B (I) wherein: A represents a grouping NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents a grouping NR1C(Q)R2, NR1C(Q)NR2R3, C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy and Cy′, which are different, represent a ring structure or G2 represents a chain and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: May 18, 2000Date of Patent: October 30, 2001Assignee: Adir et CompagnieInventors: Patrick Depreux, Said Yous, Gwenael Cheve, Gérald Guillaumet, Marie-Claude Viaud, Carlos Larraya, Caroline Bennejean, Philippe Delagrange, Pierre Renard, Carole Descamps-Francois
-
Patent number: 6310088Abstract: Compounds of formula (I) are useful therapeutic agents, by virtue of having MMP and TNF inhibitory activity.Type: GrantFiled: May 4, 2000Date of Patent: October 30, 2001Assignee: Darwin Discovery, Ltd.Inventors: Andrew Douglas Baxter, David Alan Owen, John Gary Montana, Elizabeth Jane Reed Nicholson
-
Patent number: 6306911Abstract: This invention relates to a series of substituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules that bind to neutral sphingomyelinase and inhibit its activity.Type: GrantFiled: February 7, 2000Date of Patent: October 23, 2001Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Michael P. Wachter, Praful Lalan
-
Patent number: 6288105Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.Type: GrantFiled: February 3, 2000Date of Patent: September 11, 2001Assignee: Eli Lilly and CompanyInventors: Nickolay Y Chirgadze, Matthew J Fisher, Richard W Harper, Ho-Shen Lin, Jefferson R McCowan, Alan D Palkowitz, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Minsheng Zhang
-
Patent number: 6277849Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and isomeric mixtures thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8acycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C8alkenyloxycarbonyl, C1-C5alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl: C2-C12alknyl; C1-C12haloalkyl or a group NR11R12; wherein R11, and R12 are each independently of the other hydrogen, C1-C6alkyl or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8acycloalkyl-C1-C4alkyl or wherein the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eacType: GrantFiled: August 24, 1999Date of Patent: August 21, 2001Assignee: Syngenta Crop Protection, Inc.Inventor: Martin Zeller
-
Patent number: 6265575Abstract: This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.Type: GrantFiled: August 5, 1999Date of Patent: July 24, 2001Assignee: Eli Lilly and CompanyInventors: Kenneth Jeff Thrasher, Kenneth Lee Hauser, Alan David Palkowitz
-
Patent number: 6251921Abstract: This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.Type: GrantFiled: May 14, 1999Date of Patent: June 26, 2001Assignee: Eli Lilly and CompanyInventors: Jolie Anne Bastian, Nickolay Yuri Chirgadze, Michael Lyle Denney, Matthew Joseph Fisher, Robert James Foglesong, Richard Waltz Harper, Mary George Johnson, Valentine Joseph Klimkowski, Todd Jonathan Kohn, Ho-Shen Lin, Michael Patrick Lynch, Jefferson Ray McCowan, Alan David Palkowitz, Michael Enrico Richett, Daniel Jon Sall, Gerald Floyd Smith, Kumiko Takeuchi, Jennifer Marie Tinsley, Minsheng Zhang
-
Patent number: 6248264Abstract: Compositions comprising a naphtho [1,2-b]pyran of formula (I): wherein R7 and/or R9 is hydrogen or an amino group provided that R7 and R9 are not both hydrogen, and the other substituents are as defined in the specifcation.Type: GrantFiled: November 1, 1999Date of Patent: June 19, 2001Assignee: James Robinson LimitedInventors: David A. Clarke, Bernard Mark Heron, Christopher David Gabbutt, John David Hepworth, Steven Michael Partington, Stephen Nigel Corns
-
Patent number: 6242637Abstract: The invention relates to compounds of the formula in which: A is a divalent radical selected from: A1) —O—CO— A2) —CH2—O—CO— A3) —O—CH2—CO— A4) —O—CH2—CH2— A5) —N(R1)—CO— A6) —N(R1)—CO—CO— A7) —N(R1)—CH2—CH2— A8) —O—CH2— in which: R1 is a hydrogen or a (C1-C4)-alkyl; and Am is a nitrogen-containing heterocycle.Type: GrantFiled: October 20, 1998Date of Patent: June 5, 2001Assignee: Sanofi-SynthelaboInventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
-
Patent number: 6235753Abstract: Inhibitors of the Production of s-CD23 and the secretion of TNF are provided.Type: GrantFiled: January 21, 1999Date of Patent: May 22, 2001Assignee: SmithKline Beecham p.l.c.Inventors: Stuart Bailey, Andrew Faller, David Glynn Smith, Derek Richard Buckle
-
Patent number: 6232467Abstract: Amines and amino acids are prepared by reacting an amine, a carbonyl derivative, and an organoboron compound under mild conditions.Type: GrantFiled: June 27, 1997Date of Patent: May 15, 2001Assignee: University of Southern CaliforniaInventors: Nicos A. Petasis, Ilia A. Zavialov
-
Patent number: 6232322Abstract: This invention provides compounds of Formula I having the structure wherein A, R3, R4, and R5 are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: May 10, 1999Date of Patent: May 15, 2001Assignee: American Home Products CorporationInventors: Michael S. Malamas, Robert E. McDevitt, Folake O. Adebayo
-
Patent number: 6225288Abstract: Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters and hydrates thereof are disclosed along with pharmaceutical compositions and methods of treatment. The compounds are useful as inhibitors of caspase-3, which is implicated in modulating apoptosis.Type: GrantFiled: March 16, 2000Date of Patent: May 1, 2001Assignee: Merk Frosst Canada & Co.Inventors: Yongxin Han, Andre Giroux, Erich Grimm, Renee Aspiotis, Sebastien Francoeur, Robert Zamboni, Petpiboon Prasit, Christopher Bayly, Dan McKay, Cameron Black
-
Patent number: 6221902Abstract: This invention provides compounds of Formula I having the structure wherein A, Q, R3, and R4 are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: May 10, 1999Date of Patent: April 24, 2001Assignee: American Home Products CorporationInventors: Michael S. Malamas, Folake O. Adebayo, Paul J. Dollings
-
Patent number: 6218135Abstract: The present invention has its objects to provide a compound not only which is easy to handle, thermally stable, and high in emission efficiency, but also which can show high emission efficiency without coexisting enhancer in the system even in a protic solvent. The present invention is related to a 1,2-dioxetane derivative of general formula (I). [wherein R1, R2, R3, R4 and R5 each independently represents hydrogen, alkyl or aryl; a pair of R2 and R3 and a pair of R4 and R5 may respectively be joined to each other to form a cycloalkyl group.Type: GrantFiled: March 15, 1999Date of Patent: April 17, 2001Inventors: Masakatsu Matsumoto, Nobuko Watanabe
-
Patent number: 6210608Abstract: The invention relates to novel naphthopyran- and phenanthropyran-type compounds having a carbobicycle annelated in 5,6-position. These compounds have formula (I) given below: These compounds (I) have interesting photochromic properties. The invention also relates to their preparation, to their applications as photochromes, as well as to the compositions and (co)polymer matrices containing them.Type: GrantFiled: February 16, 2000Date of Patent: April 3, 2001Assignee: Corning S.A.Inventors: You-Ping Chan, Patrick Jean
-
Patent number: 6207686Abstract: A compound of formula (I), in which: R1 is lower alkyl, cyclo(lower)alkyl, optionally substituted aryl, optionally substituted heterocyclic group, cyclo(lower)alkyl(lower)alkyl, or ar(lower)alkyl; R2 is hydrogen, hydroxy or protected hydroxy; R3 is lower alkyl, aryl, ar(lower)alkyl or optionally substituted heterocyclic(lower)alkyl; R4 is carboxy, protected carboxy or lower alkylsufonylcarbamoyl; R5 is hydrogen or lower alkyl; R6 is hydrogen or heterocyclic group; A is a single bond or lower alkylene, and Ar is optionally substituted aryl, or pharmaceutically acceptable salts thereof, having endothelin antagonistic activity.Type: GrantFiled: June 20, 1997Date of Patent: March 27, 2001Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masahiro Neya, Tatsuya Zenkoh, Hitoshi Sawada, Chiyoshi Kasahara, Masayoshi Murata, Keiji Hemmi
-
Patent number: 6197225Abstract: A photochromic compound featuring a large fading rate to prevent a change in the color tone at the time of fading, exhibiting little color after aged, and exhibiting good durability in the photochromic property. The photochromic compound is a novel chromene compound having a substituted phenyl group at the second position of the naphthopyrane ring and an alkyl group at the fifth position thereof, and is represented by, for example, the following formula, wherein R1 is an alkyl group, R2 and R3 are substituted phenyl groups, and R4 and R5 are substituents.Type: GrantFiled: February 19, 1999Date of Patent: March 6, 2001Assignee: Tokuyama CorporationInventors: Tsuneyoshi Tanizawa, Tadashi Hara, Yuichiro Kawabata, Junji Momoda, Hironobu Nagoh
-
Patent number: RE37087Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.Type: GrantFiled: June 20, 1991Date of Patent: March 6, 2001Assignee: Schering AktiengesellschaftInventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles