Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/349)
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Publication number: 20020091122Abstract: Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided.Type: ApplicationFiled: December 6, 2001Publication date: July 11, 2002Applicant: Icagen, Inc.Inventors: Grant A. McNaughton-Smith, Michael F. Gross, Alan D. Wickenden
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Publication number: 20020091144Abstract: New methods are provided for treating against apoptotic cell death, including apoptotic cardiac and neuronal cells. Therapies of the invention include administration of a mitochondrial oxidizer compound to a subject in need thereof, such as a subject suffering from or susceptible to stroke, heart attack, brain or spinal cord trauma, or chronic conditions that can resulting apoptotic cell death such as a neurodegenerative disease.Type: ApplicationFiled: October 15, 2001Publication date: July 11, 2002Applicant: Johns Hopkins UniversityInventors: Eduardo Marban, Brian O'Rourke, Masaharu Akao
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Patent number: 6417161Abstract: The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: wherein X is O or NR19 and A1, A2, R7-R10, R18, Ra, Rb, Rc, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing the compounds of Formula I. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal.Type: GrantFiled: April 22, 1999Date of Patent: July 9, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Richard M. Soll
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Publication number: 20020072531Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: ApplicationFiled: September 28, 2001Publication date: June 13, 2002Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, 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 Louis Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Publication number: 20020065284Abstract: This invention is directed to compounds of the formula 1Type: ApplicationFiled: March 30, 2001Publication date: May 30, 2002Inventors: Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
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Publication number: 20020058646Abstract: The present invention is directed to a series of substituted pyridine compounds, a method for selectively controlling neurotransmitter release in mammals using these compounds, and pharmaceutical compositions containing these compounds. Preferred compounds are 3′-(5′- and/or 6′-substituted) pyridyl ethers.Type: ApplicationFiled: February 1, 2001Publication date: May 16, 2002Inventors: Nan-Horng Lin, Liming Dong
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Publication number: 20020055507Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: ApplicationFiled: September 25, 2001Publication date: May 9, 2002Inventors: Rajashehar Betageri, Steffen Breitfelder, Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, Thomas M. Kirrane, Monica H. Moriak, Neil Moss, Usha R. Patel, John R. Proudfoot, John R. Regan, Rajiv Sharma, Sanxing Sun, Alan D. Swinamer, Hidenori Takahashi
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Publication number: 20020052349Abstract: This invention relates to anti-inflammatory and analgesic compounds, especially to certain p-(sulfonyl)phenyl amino derivatives, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: ApplicationFiled: April 26, 2001Publication date: May 2, 2002Inventors: Nancy Elisabeth Krauss, Taraneh Mirzadegan, David Bernard Smith, Keith Adrian Walker
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Publication number: 20020049234Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: ApplicationFiled: September 28, 2001Publication date: April 25, 2002Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, 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
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Patent number: 6369080Abstract: Novel compounds of formula I: including its pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.Type: GrantFiled: October 10, 1997Date of Patent: April 9, 2002Assignee: COR Therapeutics, Inc.Inventors: Bing-Yan Zhu, Robert M. Scarborough
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Publication number: 20020035109Abstract: This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-,states characterized by thrombotic activity.Type: ApplicationFiled: August 7, 2001Publication date: March 21, 2002Applicant: Berlex Laboratories, Inc.Inventors: Brad O. Buckman, David D. Davey, William J. Guilford, Michael M. Morrissey, Howard P. Ng, Gary B. Phillips, Shung C. Wu, Wei Xu
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Publication number: 20020032223Abstract: This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: ApplicationFiled: August 8, 2001Publication date: March 14, 2002Applicant: Berlex Laboratories, Inc.Inventors: Brad O. Buckman, David D. Davey, William J. Guilford, Michael M. Morrissey, Howard P. Ng, Gary B. Phillips, Shung C. Wu, Wei Xu
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Patent number: 6355634Abstract: 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: June 7, 1995Date of Patent: March 12, 2002Assignee: Bayer AktiengesellschaftInventors: Hans Peter Isenring, Bettina Weiss
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Publication number: 20020028820Abstract: This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: ApplicationFiled: August 7, 2001Publication date: March 7, 2002Applicant: Berlex Laboratories, Inc.Inventors: Brad O. Buckman, David D. Davey, William J. Guilford, Michael M. Morrissey, Howard P. Ng, Gary B. Phillips, Shung C. Wu, Wei Xu
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Patent number: 6350764Abstract: Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: wherein X is O or NR9 and Het, R1, R7, R8, R12-R15, Ra, Rb, Rc, Z, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier.Type: GrantFiled: April 6, 2001Date of Patent: February 26, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
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Patent number: 6348478Abstract: The present invention is a biphenylamidine derivative represented by the formula (1) or a pharmaceutically acceptable derivative thereof: and the biphenylamidine derivative or the pharmaceutically acceptable derivative thereof is a novel compound which can be used as a clinically applicable FXa inhibitor.Type: GrantFiled: May 15, 2000Date of Patent: February 19, 2002Assignee: Teijin LimitedInventors: Takayuki Hara, Tomohisa Nakada, Yasunobu Takano, Satoshi Sugiura, Takaharu Tsutsumi, Yoshiharu Takazawa, Reiko Takarada
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Publication number: 20020016328Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae 1Type: ApplicationFiled: January 17, 2001Publication date: February 7, 2002Inventor: Yuhpyng L. Chen
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Publication number: 20020015735Abstract: There is provided an orally deliverable pharmaceutical composition comprising a selective cyclooxygenase-2 inhibitory drug of low water solubility such as celecoxib and a release-extending polymer. The composition is useful in treatment of cyclooxygenase-2 mediated conditions and disorders by once-a-day administration.Type: ApplicationFiled: December 20, 2000Publication date: February 7, 2002Inventors: David B. Hedden, Sreekant Nadkarni
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Patent number: 6342504Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: December 21, 1999Date of Patent: January 29, 2002Assignee: Corvas International, Inc.Inventors: Terence Kevin Brunck, Susan Y. Tamura, Joseph Edward Semple, Robert John Ardecky, Yu Ge, William Charles Ripka
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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
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Publication number: 20020002190Abstract: Para-aryl or heteroaryl substituted phenyl amides which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.Type: ApplicationFiled: May 1, 2001Publication date: January 3, 2002Inventors: Wendy L. Corbett, Nancy-Ellen Haynes, Ramakanth Sarabu
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Publication number: 20010044440Abstract: Compounds of formula I are effective modulators of p38 MAP kinase.Type: ApplicationFiled: February 23, 2001Publication date: November 22, 2001Inventors: David J. Morgans, Silke Thode, Dongxu Sun
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Publication number: 20010044428Abstract: This invention relates to aminopyridines of Formula I: 1Type: ApplicationFiled: March 29, 2001Publication date: November 22, 2001Applicant: CoCensys, Inc.Inventor: Derk J. Hogenkamp
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Patent number: 6306884Abstract: This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: November 8, 1999Date of Patent: October 23, 2001Assignee: Berlex Laboratories, Inc.Inventors: Brad O. Buckman, David D. Davey, William J. Guilford, Michael M. Morrissey, Howard P. Ng, Gary B. Phillips, Shung C. Wu, Wei Xu
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Publication number: 20010020033Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: ApplicationFiled: October 10, 1997Publication date: September 6, 2001Inventors: BING-YAN ZHU, ROBERT M. SCARBOROUGH
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Publication number: 20010018438Abstract: Compounds according to Formula (I) or a salt thereof are selective ligands for GABAA receptors useful for treatment of disorders of the central nervous system: 1Type: ApplicationFiled: January 4, 2001Publication date: August 30, 2001Applicant: MERCK SHARP & DOHME LIMITEDInventors: Ian James Collins, Stephen Robert Fletcher, Timothy Harrison, Paul David Leeson, Christopher Richard Moyes, Alan John Nadin, Michael Rowley, Timothy Jason Sparey, Martin Richard Teall
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Publication number: 20010014689Abstract: The present invention relates to 2-aminopyridine derivatives of the formula I: 1Type: ApplicationFiled: February 8, 2001Publication date: August 16, 2001Inventor: John A. Lowe
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Patent number: 6262302Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: September 17, 1999Date of Patent: July 17, 2001Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Jeffrey S. Nissen, Thomas E. Mabry, Lee H. Latimer, Clark N. Eid, James E. Audia
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Patent number: 6235736Abstract: A 3-anilino-2-cycloalkenone derivative of the formula (I): wherein, R1 represents a C1 to C8 alkyl group, which may have a substituent, except for a methyl group, a C3 to C7 cycloalkyl group, a 3-tetrahydrofuryl group, an 2-indanyl group, etc., R2 represents a C1 to C4 alkyl group, R3 represents a hydrogen atom, a C3 to C7 alkyl group, which may have a substituent, a C3 to C7 cycloalkyl group, etc., R4 represents a hydrogen atom, a C1 to C5 alkyl group, which may have a substituent, a halogen atom, etc., R5, R6, R7, and R8 independently represent a hydrogen atom, a C1 to C5 alkyl group, which may have a substituent, etc., X represents —(CR11R12)n—, wherein n is 0 to 2, R11 and R12 independently represent a hydrogen atom, a C1 to C5 alkyl group, which may have a substituent, etc.Type: GrantFiled: March 20, 2000Date of Patent: May 22, 2001Assignee: Nikken Chemicals Co., Ltd.Inventors: Shinji Ina, Kenjirou Yamana, Kyoji Noda, Akane Takahama, Toshihiko Akiyama
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Patent number: 6221886Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: January 11, 2000Date of Patent: April 24, 2001Assignee: Berlex Laboratories, Inc.Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
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Patent number: 6201024Abstract: The invention provides adamantane derivatives, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.Type: GrantFiled: January 26, 1999Date of Patent: March 13, 2001Assignee: AstraZeneca UK LimitedInventors: Andrew Baxter, Thomas McInally, Michael Mortimore, David Cladingboel
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Patent number: 6200996Abstract: 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: March 13, 2001Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, James M. Chen, Frances C. Nelson
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Patent number: 6191167Abstract: Preventive as well as therapeutic treatment to alleviate cosmetic conditions and symptoms of dermatologic disorders with amphoteric compositions containing alpha hydroxyacids, alpha ketoacids, related compounds or polymeric forms of hydroxyacids is disclosed. The cosmetic conditions and the dermatologic disorders in which the amphoteric compositions and the polymeric compounds may be useful include dry skin, dandruff, acne, keratoses, psoriasis, eczema, pruritus, age spots, lentigines, melasmas, wrinkles, warts, blemished skin, hyperpigmented skin, kyperkeratotic skin, inflammatory dermatoses, skin changes associated with aging, and skin requiring cleansers.Type: GrantFiled: February 23, 1999Date of Patent: February 20, 2001Assignee: Tristrata Technology, Inc.Inventors: Ruey J. Yu, Eugene J. Van Scott
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Patent number: 6172115Abstract: A method is provided for preventing or reducing the risk of restenosis following angioplasty by administering a retinoid, such as an RXR-selective retinoid, e.g. the compound of the formula: and pharmaceutically acceptable salts and esters and amides thereof.Type: GrantFiled: January 12, 1998Date of Patent: January 9, 2001Assignee: Allergan Sales, Inc.Inventor: Roshantha A. Chandraratna
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Patent number: 6162815Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds having the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## which are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders are provided. In particular, based on their RXR-agonist activity, these compounds may be used to treat noninsulin-dependent diabetes mellitus (NIDDM) and obesity.Type: GrantFiled: September 10, 1998Date of Patent: December 19, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6153652Abstract: Disclosed are compounds which inhibit .beta.-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits .beta.-amyloid peptide release and/or its synthesis as well as methods for treating Alheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: November 21, 1997Date of Patent: November 28, 2000Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Jeffrey S. Nissen, Thomas E. Mabry, Lee H. Latimer, Clark N. Eid, James E. Audia
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Patent number: 6130226Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor .alpha., nuclear factor .kappa.B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.Type: GrantFiled: March 18, 1999Date of Patent: October 10, 2000Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
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Patent number: 6103732Abstract: Carboxylic acid derivatives of the formula I ##STR1## where the radicals have the meanings stated in the description, and the preparation of these agreements [sic] and their use as drugs are described.Type: GrantFiled: October 8, 1998Date of Patent: August 15, 2000Assignee: BASF AktiengesellschaftInventors: Wilhelm Amberg, Andreas Kling, Dagmar Klinge, Hartmut Riechers, Ernst Baumann, Liliane Unger, Manfred Raschack, Stefan Hergenroder, Sabine Schult
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Patent number: 6075023Abstract: Fish mycoses and single-cell ectoparasites on fish are controlled using an active compound suitable for inhibiting the mitochondrial respiratory chain at the stage of the b/c.sub.1 complex.Type: GrantFiled: February 17, 1998Date of Patent: June 13, 2000Assignee: BASF AktiengesellschaftInventors: Gerhard Peter Dohmen, Christoph Kunast, Reinhart Munk, Gerhard Rothhaas
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Patent number: 6071911Abstract: Antiepileptic compounds of the formula ##STR1## wherein X is hydrogen, a C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, trifluoromethoxy or halogen residue, A is an amino, C.sub.1-4 alkylamino, C.sub.1-4 dialkylamino, morpholino, piperidino or pyrrolidino residue, and n is a cardinal number from 0 to 5, and process for preparing the foregoing compounds and for their use as anticonvulsives.Type: GrantFiled: August 6, 1999Date of Patent: June 6, 2000Assignee: Arzneimittelwerk Dresden GmbHInventors: Hans-Joachim Lankau, Klaus Unverferth, Thomas Arnold, Reni Bartsch, Abgelika Rostock, Vladimir Granik, Sofia Grizik
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Patent number: 6060512Abstract: Preventive as well as therapeutic treatment to alleviate cosmetic conditions and symptoms of dermatologic disorders with amphoteric compositions containing alpha hydroxyacids, alpha ketoacids, related compounds or polymeric forms of hydroxyacids is disclosed. The cosmetic conditions and the dermatologic disorders in which the amphoteric compositions and the polymeric compounds may be useful include dry skin, dandruff, acne, keratoses, psoriasis, eczema, pruritus, age spots, lentigines, melasmas, wrinkles, warts, blemished skin, hyperpigmented skin, kyperkeratotic skin, inflammatory dermatoses, skin changes associated with aging, and skin requiring cleansers.Type: GrantFiled: November 4, 1998Date of Patent: May 9, 2000Assignee: Tristrata Technology, Inc.Inventors: Ruey J. Yu, Eugene J. Van Scott
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Patent number: 6057342Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: July 7, 1997Date of Patent: May 2, 2000Assignee: Dupont Pharmaceutical Co.Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
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Patent number: 6054470Abstract: This invention relates to compounds of formula (1): ##STR1## wherein Ring a, A, B, C, D, E, R and Q are defined herein. These compounds possess the ability to disrupt the interaction between regulatory proteins possessing one or more SH2 domains and their native ligands.Type: GrantFiled: December 9, 1998Date of Patent: April 25, 2000Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rajashekhar Betageri, Pierre L. Beaulieu, Jean-Marie Ferland, Montse Llinas-Brunet, Neil Moss, Usha Patel, John R. Proudfoot, Mario Cardozo
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Patent number: 6046221Abstract: Novel aryl amides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is N-benzoyl-3-amino-3-(3',4'-dimethoxyphenyl)propanamide.Type: GrantFiled: August 25, 1998Date of Patent: April 4, 2000Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire, David I. Stirling
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Patent number: 6046239Abstract: Compounds of the formula: ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are, independently, hydrogen, COOR.sub.15, halogen, nitro, cyano, C.sub.1-10 alkoxy, C.sub.1-10 haloalkoxy, sulfonic acid, C.sub.1-10 alkylsulfonyl, C.sub.6-12 arylsulfonyl, C.sub.6-12 aralkylsulfonyl, C.sub.1-10 alkylsulfinyl, C.sub.6-12 alkylsulfinyl, C.sub.6-12 aralkylsulfinyl, sulfamoyl, C.sub.1-10 alkylsulfamido, C.sub.6-12 alkylsulfamido, C.sub.1-10 alkanoyl, C.sub.6-12 aryloyl, C.sub.6-12 aralkanoyl, amino, C.sub.1-10 alkylamino, C.sub.2-10 dialkylamino, C.sub.6-12 aralkylamino, C.sub.6-12 arylamino, carboxamido, C.sub.1-10 alkylcarboxamido, C.sub.6-12 arylcarboxamido, C.sub.1-10 haloalkyl, C.sub.1-10 alkyl, C.sub.2-12 alkenyl, C.sub.6-12 aryl, C.sub.6-12 aralkyl; with the proviso that at least one of R.sub.4 and R.sub.5 is COOR.sub.15 ;R.sub.9 is hydrogen, C.sub.1-10 alkyl and C.sub.1-10 haloalkyl;R.sub.10 is hydrogen, C.sub.1-10 alkyl, C.sub.1-10 haloalkyl, or C.sub.2-12 alkylidene;R.Type: GrantFiled: August 3, 1998Date of Patent: April 4, 2000Assignee: American Home Products CorporationInventors: Joseph Richard Lennox, Schuyler Adam Antane, John Anthony Butera
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Patent number: 6046216Abstract: Derivatives of phenyl pyridinone are useful for the treatment of patients having precancerous lesions. These compounds are also useful to inhibit the growth of neoplastic cells.Type: GrantFiled: April 1, 1997Date of Patent: April 4, 2000Assignee: Cell Pathways, Inc.Inventors: Gary Piazza, Rifat Pamukcu
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Patent number: 6037356Abstract: Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: ##STR1## wherein X is O or NR.sup.9 and Het, R.sup.1, R.sup.7, R.sup.8, R.sup.12 -R.sup.15, R.sup.a, R.sup.b, R.sup.c, Z, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin.Type: GrantFiled: November 25, 1998Date of Patent: March 14, 2000Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
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Patent number: 6034067Abstract: The invention relates to a compound having formula (I), wherein A, B, X, N, Z and Q are defined as described in the description. The compounds of the invention have anticoagulant activity and can be used in treating or preventing thrombin-related diseases.Type: GrantFiled: August 12, 1998Date of Patent: March 7, 2000Assignee: Akzo Nobel, N.V.Inventors: Peter Diederik Jan Grootenhuis, Adrianus Petrus Antonius de Man, Anton Egbert Peter Adang
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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
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Patent number: RE37355Abstract: 6-dimethylaminomethyl-1-phenyl-cyclohexane compounds, methods of preparing them and the use of these compounds in drugs are described.Type: GrantFiled: March 30, 2000Date of Patent: September 4, 2001Assignee: Gruenenthal GmbHInventors: Helmut Heinrich Buschmann, Wolfgang Werner Alfred Strassburger, Norma Selve, Elmar Josef Friderichs