Chalcogen Or Nitrogen Attached Directly To The Hetero Ring By Nonionic Bonding Patents (Class 549/28)
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Patent number: 7253940Abstract: A nanoporous, nanocrystalline film and electrochromic device. The nanoporous, nanocrystalline film has a conducting metal oxide having an electroactive compound, which is either a p-type or n-type redox promoter or p-type or n-type redox chromophore, absorbed thereto. The electrochromic device has at least one electrode, the at least one electrode having a transparent or translucent substrate bearing an electrically conducting coating, which in turn bears a conducting nanostructured metal oxide film.Type: GrantFiled: February 1, 2005Date of Patent: August 7, 2007Inventors: Donald Fitzmaurice, David Cummins, David Corr, S. Nagaraja Rao, Gerrit Boschloo
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Patent number: 7250522Abstract: The present invention provides a method for preparing an aryl 5-thio-?-D-aldohexopyranoside derivative of Formula (III), which comprises reacting a 5-thio-D-aldohexopyranose derivative of Formula (I) with Ar-OH of Formula (II) in the presence of a phosphine represented by PR11R12R13 and an azo reagent represented by R21—N?N—R22 in accordance with the following schemeType: GrantFiled: August 8, 2003Date of Patent: July 31, 2007Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Hiroyuki Kakinuma, Hajime Asanuma
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Patent number: 7241810Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: March 21, 2005Date of Patent: July 10, 2007Assignee: Pfizer IncInventors: Alan Daniel Brown, Mark Edward Bunnage, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Paul Alan Glossop, Kim James, David Anthony Price
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Patent number: 7112683Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.Type: GrantFiled: September 2, 2004Date of Patent: September 26, 2006Assignees: G.D. Searle & Co., Monsanto CompanyInventors: Deborah E. Bertenshaw, Daniel P. Getman, Robert M. Heintz, John J. Talley, Kathryn L. Reed, Robert A. Chrusciel, Michael Clare
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Patent number: 7105518Abstract: The present invention provides compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein R1 and R2 are independently hydrogen, an option ally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and R3 is an optionally substituted C3-20 heterocyclyl or C5-20 aryl group, and their use as pharmaceuticals, particularly in treating diseases which are retroviral mediated or ameliorated by the inhibition of DNA-PK,Type: GrantFiled: August 14, 2002Date of Patent: September 12, 2006Assignee: Cancer Research Technology LimitedInventors: Niall Morrison Barr Martin, Graeme Cameron Murray Smith, Roger John Griffin, Bernard Thomas Golding, Ian Robert Hardcastle, Laurent Jean Martin Rigoreau, David Richard Newell, Hilary Alan Calvert, Nicola Jane Curtin, Paul Workman, Florence Irene Raynaud, Bernard Paul Nutley
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Patent number: 7053115Abstract: The present invention relates to a novel crystalline form of dorzolamide hydrochloride, to processes for its preparation and a pharmaceutical composition containing it.Type: GrantFiled: April 7, 2003Date of Patent: May 30, 2006Assignee: Hetero Drugs LimitedInventors: Reddy Bandi Parthasaradhi, Reddy Kura Rathnakar, Reddy Rapolu Raji, Reddy Dasari Muralidhara, Reddy Itiyata Srinivas
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Patent number: 6905786Abstract: A compound represented by the following formula (I): wherein R1, R2 and R3each represents an aryl group, a heterocyclic group or an aliphatic hydrocarbon group, provided that at least one of R1, R2 and R3 represents an aryl group or a heterocyclic group and at least one of the aryl group and heterocyclic group contains a group represented by formula (II), R1, R2 and R3 may be linked to each other to form a ring, wherein R4, R5 and R6, each represents a hydrogen atom or a substituent; X1 represents an oxygen atom, a sulfur atom, N—RX1 or CRX2RX3; RX1, RX2,RX3 each represents a hydrogen atom or a substituent; R4, R5, R6 and X1 may be linked to each other to form a ring; Y represents an oxygen atom, a sulfur atom, or N—RY1; and RY1 represents a hydrogen atom or a substituent.Type: GrantFiled: December 3, 2002Date of Patent: June 14, 2005Assignee: Fuji Photo Film., Ltd.Inventor: Kazumi Nii
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Patent number: 6875790Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.Type: GrantFiled: February 20, 2003Date of Patent: April 5, 2005Assignees: G. D. Searle & Co., Pharmacia Corporation (Monsanto Corporation)Inventors: Deborah E. Bertenshaw, Daniel Getman, Robert M. Heintz, John J. Talley, Kathryn L. Reed, Robert Alan Chrusciel, Michael Clare
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Patent number: 6849203Abstract: The invention relates to photoisomerizable compounds of formula I wherein A, Z, L, R, R1, k, m and r are defined herein.Type: GrantFiled: April 5, 2002Date of Patent: February 1, 2005Assignee: Merck Patent Gesellschaft Mit Beschraenkter HaftungInventors: Louise Diane Farrand, Christopher Worrall, Owain Llyr Parri
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Patent number: 6849660Abstract: Provided are antibacterial compounds having Formula I: In such compositions, X is O or S; Y is CH2; n is 0 or 1. One of R1 and R1? is —C(O)NR5R5?, —C(O)—Q—NR5R5?, —CH2NR5R5? or —S(O)2NR5R5? and the other is H or R3. One of R2 and R2? is —NHC(O)R6 or —NHS(O)2R6 and the other is H or R4. Q is an amino acid or peptide. R3 is H, halogen, —NR5R5? or —NHC(O)R6; and R4 is selected from the group consisting of H, halogen, hydroxyl, amino, carboxyl, alkyl, alkenyl and alkynyl. R5 is selected from the group consisting of H, alkyl, alkenyl or alkynyl optionally substituted with halogen, OH, amino, amidinyl, guanidinyl, urea, alkyl, carboxyl, oxo, carboxamide; R5? is H or R5 and R5? together form a 5-16 member heterocycle optionally substituted with halogen, OH, amino, alkyl, carboxyl, carbonyl or carboxamide.Type: GrantFiled: August 1, 2000Date of Patent: February 1, 2005Assignee: ISIS Pharmaceuticals, Inc.Inventors: Elizabeth Jefferson, Eric Swayze
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Patent number: 6846843Abstract: Thio-alpha-amino acids of general formula (I), wherein R1, R2 and R3 have the meanings given in the description, methods for producing them, and medicaments containing these compounds. The invention also provides methods for treating pain and other diseases using the pharmaceutical compositions comprising the thioamino acids.Type: GrantFiled: March 14, 2003Date of Patent: January 25, 2005Assignee: Gruenenthal GmbHInventors: Boris Chizh, Matthias Gerlach, Michael Haurand, Claudia Puetz, Gero Gaube, D. Enders
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Patent number: 6828276Abstract: There are described benzoylcyclohexanediones of the formula I, their preparation, and their use as herbicides and plant growth regulators. In this formula (I), C1, C2, C3 are cyclic radicals, X1 is a hetero atom, X2 is a chain of carbon atoms, L is a chain-like element, R1, R2, R3, R4, R5 are various radicals, and Y and Z are monoatomic bridge elements.Type: GrantFiled: August 30, 2001Date of Patent: December 7, 2004Assignee: Aventis CropScience GmbHInventors: Thomas Seitz, Andreas van Almsick, Lothar Willms, Hermann Bieringer, Thomas Auler, Hubert Menne
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Patent number: 6809207Abstract: The present invention provides certain alpha-amino acids and derivatives thereof, such as, but not limited to, esters, amides and salts. These derivatives may comprise such representative side groups as a phenyl, pyridyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, or thienyl group. The present invention further provides a method for synthesizing alpha-amino acids and derivatives thereof via a modified Ugi type reaction using an aldehyde, ammonium formate and a C1-C5 alkyl isocyanide. The compounds provided by this method are useful in the development of new pharmaceuticals for the treatment of human diseases.Type: GrantFiled: July 24, 2002Date of Patent: October 26, 2004Assignee: PharmaCore, Inc.Inventors: Sekar Alla, Seung-Yong Choi, Dale Dhanoa, Elso DiFranco, Galina Krokhina, Keqiang Li, Balasubramanian Thiagarajan, Wen-Chun Zhang
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Publication number: 20040204452Abstract: The invention relates to the use of aromatics sulfonamides of the general formula I as peroxynitrite rearrangement catalysts, to the preparation thereof and to the use thereof as medicament for the treatment of various disorders.Type: ApplicationFiled: April 10, 2003Publication date: October 14, 2004Applicant: Schering AGInventors: Thorsten Blume, Roland Neuhaus, Detlev Suelzle, Iris Pribilla, Gisbert Depke, Joseph S. Beckman
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Patent number: 6803129Abstract: The present invention relates to an organic light emitting diode (OLED) device, comprising an anode disposed on a substrate, an organic EL layer disposed on the anode and a cathode disposed on the organic EL layer.Type: GrantFiled: April 25, 2003Date of Patent: October 12, 2004Assignee: RiTdisplay CorporationInventors: Hsien-Chang Lin, Chih-Hao Kung, Chung-Cheng Pai, Shwu-Ju Shieh, Tzu-Chin Tang
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Publication number: 20040176309Abstract: The invention relates to Siglec inhibitors that have an increased affinity for the receptor molecule. The Siglec inhibitors provided by the invention are preferably selective of a given Siglec molecule. The invention further relates to a method for producing Siglec inhibitors and to a method for increasing the binding selectivity for a given Siglec molecule. The invention also relates to pharmaceutical compositions that contain the Siglec inhibitors and to medical indications for the Siglec inhibitors.Type: ApplicationFiled: February 13, 2004Publication date: September 9, 2004Inventors: Sorge Kelm, Reinhard Brossmer
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Patent number: 6750233Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.Type: GrantFiled: September 17, 2001Date of Patent: June 15, 2004Assignee: Pharmacia CorporationInventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Yvette M. Fobian, John N. Freskos, Daniel P. Getman, Joseph J. McDonald, Susan L. Hockerman, Susan C. Howard, Steve A. Kolodziej, Hui Li, Deborah A. Mischke, Joseph G. Rico, Nathan W. Stehle, Michael B. Tollefson, William F. Vernier, Clara I. Villamil
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Publication number: 20040010143Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.Type: ApplicationFiled: February 20, 2003Publication date: January 15, 2004Applicants: G.D. Searle & Co., Pharmacia Corporation (Monsanto Company)Inventors: Deborah E. Bertenshaw, Daniel P. Getman, Robert M. Heintz, John J. Talley, Kathryn L. Reed, Robert Alan Chrusciel, Michael Clare
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Patent number: 6677355Abstract: Compounds of the formula; are useful for inhibiting matrix metalloproteinase enzymes in animals, and as such, prevent and treat diseases resulting from the breakdown of connective tissues. Also disclosed are methods for the preparation of such compounds, pharmaceutical compositions including the same, and methods of treating diseases in which matrix metalloproteinases are involved including multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurysm, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, osteoporosis, rheumatoid or osteoarthritis, renal disease, left ventricular dilation, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.Type: GrantFiled: February 13, 2002Date of Patent: January 13, 2004Assignee: Warner-Lambert CompanyInventors: Christopher Alan Conrad, Patrick Michael O'Brien, Daniel Fred Ortwine, Joseph Armand Picard, Drago Robert Sliskovic
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Publication number: 20030232812Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: January 21, 2003Publication date: December 18, 2003Inventors: Mikhail F. Gordeev, Adam Renslo, Gary W. Luehr, Stuart Lam, Neil E. Westlund, Dinesh V. Patel
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Patent number: 6664272Abstract: The present invention is directed to curcumin analogs exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds.Type: GrantFiled: December 4, 2000Date of Patent: December 16, 2003Assignee: Emory UniversityInventors: James P. Snyder, Matthew C. Davis, Brian Adams, Mamoru Shoji, Dennis C. Liotta, Eva M. Ferstl, Ustun B. Sunay
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Publication number: 20030191027Abstract: There are described derivatives of benzoylcyclohexanediones of the formula (I) and their use as herbicides.Type: ApplicationFiled: September 10, 2002Publication date: October 9, 2003Inventors: Thomas Seitz, Lothar Willms, Andreas van Almsick, Hermann Bieringer, Thomas Auler, Hubert Menne
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Patent number: 6602899Type: GrantFiled: May 9, 2002Date of Patent: August 5, 2003Assignee: Fournier Industrie & SanteInventors: Véronique Barberousse, Benaïssa Boubia, Soth Samreth
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Publication number: 20030138664Abstract: A light emitting device material comprising a compound represented by the following formula (I): 1Type: ApplicationFiled: December 3, 2002Publication date: July 24, 2003Applicant: FUJI PHOTO FILM CO., LTD.Inventor: Kazumi Nii
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Patent number: 6552203Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.Type: GrantFiled: October 11, 2001Date of Patent: April 22, 2003Assignee: Monsanto CompanyInventors: Deborah E. Bertenshaw, Daniel Getman, Robert M. Heintz, John J. Talley, Kathryn L. Reed, Robert Alan Chrusciel, Michael Clare
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Patent number: 6514633Abstract: A light emitting device material comprising a compound represented by the following formula (I): wherein R1, R2 and R3, which may be the same or different, each represents an aryl group, a heterocyclic group or an aliphatic hydrocarbon group, provided that at least one of R1, R2 and R3 represents an aryl group or a heterocyclic group, containing a group represented by the following formula (II): wherein R4, R5 and R6, which may be the same or different, each represents a hydrogen atom or a substituent; X1 represents an oxygen atom, a sulfur atom, N—RX1 or CRX2RX3; RX1, RX2, RX3, which may be the same or different, each represents a hydrogen atom or a substituent; R4, R5, R6 and X1 may be linked to each other to form a ring; Y represents an oxygen atom, a sulfur atom, or N—RY1; and RY1 represents a hydrogen atom or a substituent.Type: GrantFiled: September 18, 2000Date of Patent: February 4, 2003Assignee: Fuji Photo Film Co., Ltd.Inventor: Kazumi Nii
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Patent number: 6479671Abstract: A process for producing a compound of the formula (II): (wherein R1, R2, R3 and R4 are each independently hydrogen, alkyl, alkoxy or the like, R5 is alkyl or alkoxyalkyl, A is O or S, Ar is aryl or the like, * represents the position of an asymmetric carbon atom and that the compound is the (R) or (S) isomer and Q is an optical resolution reagent) comprising isolating the compound as crystals from a solution or suspension containing the compound of the formula (II) (wherein * represents that the compound is the (R) or (S) isomer or a mixture thereof and the other symbols are the same as the above).Type: GrantFiled: August 15, 2000Date of Patent: November 12, 2002Assignee: Shionogi & Co., Ltd.Inventors: Toshiro Konoike, Tadahiko Yorifuji, Shoji Shinomoto, Yutaka Ide, Takashi Ohya, Ken-ichi Matsumura
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Patent number: 6455573Abstract: A method for synthesizing Salacinol, its stereoisomers, and non-naturally occurring selenium and nitrogen analogues thereof having the general formula (I): The compounds are potentially useful as glycosidase inhibitors. The synthetic schemes comprise reacting a cyclic sulfate with a 5-membered ring sugar containing a heteroatom (X). The heteroatom preferably comprises sulfur, selenium, or nitrogen. The cyclic sulfate and ring sugar reagents may be readily prepared from carbohydrate precursors, such as D-glucose, L-glucose, D-xylose and L-xylose. The target compounds are prepared by opening of the cyclic sulfates by nucleophilic attack of the heteroatoms on the 5-membered ring sugars. The resulting heterocyclic compounds have a stable, inner salt structure comprising a heteroatom cation and a sulfate anion. The synthetic schemes yield various stereoisomers of the target compounds in moderate to good yields with limited side-reactions.Type: GrantFiled: July 28, 2000Date of Patent: September 24, 2002Assignee: Simon Fraser UniversityInventors: B. Mario Pinto, Blair D. Johnston, Ahmad Ghavami
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Patent number: 6451766Abstract: Compounds of formula (I) or their salts or esters: [wherein R1 is alkyl or haloalkyl; R2 and R3 each represents hydrogen or aliphatic acyl; X is hydroxy, halogen, alkoxy, or a group of formula RaO—, where Ra is aliphatic acyl; Y is a group of formula RbRcN— or RbRcN—O—, where Rb and Rc each is hydrogen or alkyl; and Z is oxygen or sulfur] have excellent sialidase inhibitory activity and are therefore useful for the treatment and prevention of influenza and other viral diseases where the replication of the virus is susceptible to sialidase inhibitors.Type: GrantFiled: October 3, 2001Date of Patent: September 17, 2002Assignee: Sankyo Company, LimitedInventors: Takeshi Honda, Yoshiyuki Kobayashi, Makoto Yamashita
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Patent number: 6441023Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflmatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.Type: GrantFiled: July 3, 2001Date of Patent: August 27, 2002Assignee: American Home Products CorporationInventors: Aranapakam Mudumbai Venkatesan, Jannie Lea Baker, Jeremy Ian Levin
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Publication number: 20020107264Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.Type: ApplicationFiled: October 11, 2001Publication date: August 8, 2002Inventors: Deborah E. Bertenshaw, Daniel Getman, Robert M. Heintz, John J. Talley, Kathryn L. Reed, Robert Alan Chrusciel, Michael Clare
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Patent number: 6417221Abstract: New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7- substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.Type: GrantFiled: September 27, 2000Date of Patent: July 9, 2002Assignees: Organix, Inc., President and Fellows of Harvard CollegeInventors: Peter C. Meltzer, Bertha K. Madras, Paul Blundell, Zhengming Chen
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Patent number: 6410748Abstract: A monomer represented by the following general formula (m-1): wherein R is a group having an alicyclic skeleton, R2s may be the same or different and are individually hydrogen atom, halogen atom or monovalent organic group, X1 is a bivalent organic group containing a heteroatom, j is an integer of 0 to 3, and R1 is a group selected from the following groups, a monovalent organic group having Si (R1-1), and —(X2)k—R4—(X3)m—C(R6)3 (R1-2), wherein X2 and X3 are a bivalent organic group containing a heteroatom, k and m are an integer of 0 to 3, R4 is a bivalent alkyl group, R6s may be the same or different and are individually hydrogen atom, halogen atom or monovalent organic group.Type: GrantFiled: May 3, 2001Date of Patent: June 25, 2002Assignee: Kabushiki Kaisha ToshibaInventors: Naomi Shida, Toru Ushirogouchi, Koji Asakawa, Takeshi Okino, Shuji Hayase, Yoshihiko Nakano, Makoto Nakase
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Patent number: 6380258Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 24, 1999Date of Patent: April 30, 2002Assignee: G. D. Searle, L.L.C.Inventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo
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Publication number: 20020049317Abstract: The method of this invention prepares acylated cyclic compounds by contacting phenyl esters as acylating agents with cyclic compounds in the presence of a cyanide or fluoride catalyst.Type: ApplicationFiled: April 12, 2001Publication date: April 25, 2002Inventor: Paul Walter Wojtkowski
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Publication number: 20020045199Abstract: Novel methods for the treatment and/or prophylaxis of diseases caused by tissue-adhering bacteria are disclosed. By interacting with periplasmic molecular chaperones it is achieved that the assembly of pili is prevented or inhibited and thereby the infectivity of the bacteria is diminished. Also disclosed are methods for screening for drugs as well as methods for the de novo design of such drugs, methods which rely on novel computer drug modelling methods involving an approximative calculation of binding free energy between macromolecules. Finally, novel pyranosides which are believed to be capable of interacting with periplasmic molecular chaperones are also disclosed.Type: ApplicationFiled: March 7, 2001Publication date: April 18, 2002Inventors: Scott Hultgren, Meta Kuehn, Zheng Xu, Derek Ogg, Mark Harris, Matti Lepisto, Charles Hal Jones, Jan Kihlberg
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Patent number: 6369225Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: April 9, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
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Patent number: 6350761Abstract: This invention is directed to benzenamine derivatives of formula (I): wherein A, W, m, n, R1, R2, R3, R4, R5 and R6 are defined herein. These compounds are useful as anti-coagulants.Type: GrantFiled: July 24, 2000Date of Patent: February 26, 2002Assignee: Berlex Laboratories, Inc.Inventors: William J. Guilford, Steven T. Sakata, Kenneth J. Shaw, Shung Wu, Wei Xu, Zuchun Zhao
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Publication number: 20020019534Abstract: A compound of the formula 1Type: ApplicationFiled: March 27, 2001Publication date: February 14, 2002Inventor: Mark C. Noe
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Publication number: 20020013360Abstract: The invention relates to 3-hydroxy-and 3-keto-cyclohetero-substituted leucine compounds that are inhibitors of cysteine proteases, particularly cathepsin K, and are useful in the treatment of diseases in which inhibition of bone loss is a factor. The 3-hydroxy-or 3-keto-moiety is bonded to a tetrahydrothiophene, tetrahydrothiopyran, tetrahydrofuran or tetrahydropyran ring.Type: ApplicationFiled: July 30, 2001Publication date: January 31, 2002Applicant: SmithKline Beecham CorporationInventors: Andrew D. Gribble, Ashley Edward Fenwick, Robert W. Marquis, Daniel F. Veber, Jason Witherington
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Patent number: 6342511Abstract: The invention concerns novel phenylcyclidine derivatives with selective affinity for low affinity receptors, methods for preparing them, pharmaceutical compositions containing them and their use as protective agents for central or peripheral nervous system cells against acute or chronic degeneration, or as an anticonvulsant.Type: GrantFiled: November 30, 1999Date of Patent: January 29, 2002Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Jean-Marc Kamenka, Jacques Hamon, Jacques Vignon
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Publication number: 20020006920Abstract: A compound of the formula 1Type: ApplicationFiled: July 18, 2001Publication date: January 17, 2002Inventors: Ralph Pelton Robinson, Kim Francis McClure
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Publication number: 20010039287Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.Type: ApplicationFiled: February 24, 1999Publication date: November 8, 2001Inventors: THOMAS E BARTA, DANIEL P BECKER, TERRI L BOEHM, GARY A DECRESCENZO, CLARA I WILLAMI1, JOSEPH J MCDONALD, JOHN N FRESKOS, DANIEL P GETMAN, GUNNAR J HANSON
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Patent number: 6313162Abstract: The invention relates to novel propynyl or dienyl biaromatic compounds which have the general formula (I) as well as to the use of these compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmological complaints in particular), or alternatively in cosmetic compositions.Type: GrantFiled: December 17, 1999Date of Patent: November 6, 2001Assignee: Centre International de Recherche Dermatologiques Galderma (C.I.R.D.) GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6310245Abstract: The invention relates to 2-benzoylcyclohexane-1,3-diones of the formula I where R1, R2 are hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, alkoxyalkyl, alkenyl, alkynyl, —OR5, —OCOR6, —OSO2R6, —SH, —S(O)nR7, —SO2OR5, —SO2NR5R8, —NR8SO2R6 or —NR8COR6; R3 is hydrogen, alkyl, haloalkyl, alkenyl or alkynyl; R4 is hydrogen, unsubstituted or substituted alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, —COR9, —CO2R9, —COSR9 or —CONR8R9; X is oxygen or sulfur; Z is oxygen or NR8; m is 0 or 1; n is 0, 1 or 2; R5 is hydrogen, alkyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl; R6 is alkyl or haloalkyl; R7 is alkyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl; R8 is hydrogen or alkyl; R9 is alkyl, alkenyl, alkynyl, phenyl or benzyl; R10 is alkyl, haloalkyl, alkenyl or alkynyl; Q is an unsubstituted or substituted cyclohexane-1,3-dione ring which is linked in the 2-position; where m is 1 if R3 isType: GrantFiled: June 23, 1999Date of Patent: October 30, 2001Assignee: BASF AktiengesellschaftInventors: Uwe Kardorff, Regina Luise Hill, Michael Rack, Wolfgang von Deyn, Stefan Engel, Martina Otten, Matthias Witschel, Ernst Baumann, Joachim Rheinheimer, Guido Mayer, Ulf Misslitz, Karl-Otto Westphalen, Helmut Walter
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Patent number: 6291512Abstract: New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7- substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.Type: GrantFiled: September 27, 2000Date of Patent: September 18, 2001Assignees: Organix, Inc., President and Fellows of Harvard CollegeInventors: Peter C. Meltzer, Bertha K. Madras, Paul Blundell, Zhengming Chen
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Patent number: 6281365Abstract: Organic platinum complexes active as anti-tumor agents in warm-blooded animals, and methods for synthesis of same, are described.Type: GrantFiled: May 26, 1989Date of Patent: August 28, 2001Assignee: American Cyanamid CompanyInventors: Ralph Grassing Child, Panayota Bitha, Joseph John Hlavka, Yang-I Lin
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Patent number: 6274745Abstract: A binaphthol monophosphoric acid derivative of the following formula (1), (2), (3) or (4): wherein each of R1, R2, R3 and R4 which are independent of one another, is hydrogen, a C2-20 linear or branched alkenyl group, a C2-20 linear or branched alkynyl group, a phenyl group, a phenyl group having its nucleus substituted at the 1- to 4-carbon atom by a C1-10 linear or branched alkyl group, a phenyl group having its nucleus substituted at the 1- to 4-carbon atom by a C2-10 linear or branched alkenyl group, a phenyl group having its nucleus substituted at the 1- to 4-carbon atom by a C2-10 linear or branched alkynyl group, a naphthyl group or a C3-8 cycloalkyl group, provided that R1 to R4 are not simultaneously hydrogen, wherein each of R5, R6, R7 and R8 which are independent of one another, essentially the same as R1, R2, R3 and R4.Type: GrantFiled: March 22, 2000Date of Patent: August 14, 2001Assignee: Tosoh CorporationInventors: Junji Inanaga, Hiroshi Furuno
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Patent number: 6265583Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.Type: GrantFiled: October 22, 1998Date of Patent: July 24, 2001Assignees: G. D. Searle & Co., Monsanto CompanyInventors: Deborah E. Bertenshaw, Daniel Getman, Robert M. Heintz, John J. Talley, Kathryn L. Reed, Robert Alan Chrusciel, Michael Clare
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Patent number: 6239283Abstract: The invention is a process for the preparation of cyclic-sulfur fluorine containing oxazolidinone antibacterial agents which utilizes the important tetrahydrothiopyran-o-fluorinated carbamate of formula (IV)Type: GrantFiled: January 31, 2000Date of Patent: May 29, 2001Assignee: Pharmacia & Upjohn CompanyInventor: James R. Gage