Chalcogen Bonded Directly To Ring Carbon Of The Five-membered Hetero Ring (e.g., Indigoid Dyes, Etc.) Patents (Class 548/450)
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Patent number: 9131688Abstract: The present invention relates to novel strigolactam derivatives of formula (I), to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.Type: GrantFiled: December 14, 2012Date of Patent: September 15, 2015Assignee: Syngenta Participations AGInventors: Mathilde Denise Lachia, Alain De Mesmaeker, Emmanuelle Villedieu-Percheron, Hanno Christian Wolf, Pierre Joseph Marcel Jung, Frank Lanfermeijer, Paul Van Den Wijngard, Claudio Screpanti
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Publication number: 20150065498Abstract: The present invention is directed to N-linked lactam compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: May 11, 2012Publication date: March 5, 2015Inventors: Scott D. Kuduk, Douglas C. Beshore, Zhi-Qiang Yang, Youheng Shu, Daniel Pitts
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Patent number: 8946280Abstract: The present invention relates to novel strigolactam derivatives of formula (I) to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.Type: GrantFiled: December 9, 2011Date of Patent: February 3, 2015Assignee: Syngenta Participations AGInventors: Mathilde Denise Lachia, Alain De Mesmaeker, Hanno Christian Wolf, Pierre Joseph Marcel Jung
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Publication number: 20140336052Abstract: The present invention relates to novel strigolactam derivatives of formula (I), to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.Type: ApplicationFiled: December 14, 2012Publication date: November 13, 2014Inventors: Mathilde Denise Lachia, Alain De Mesmaeker, Emmanuelle Villedieu-Percheron, Hanno Christian Wolf, Pierre Joseph Marcel Jung, Frank Lanfermeijer, Paul Van Den Wijngard, Claudio Screpanti
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Publication number: 20140302993Abstract: The present invention relates to novel strigolactam derivatives of formula (I), to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.Type: ApplicationFiled: December 14, 2012Publication date: October 9, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Mathilde Denise Lachia, Alain De Mesmaeker, Emmanuelle Villedieu-Percheron, Hanno Christian Wolf, Pierre Joseph Marcel Jung, Franciscus Cornelis Lanfermeijer, Paul Willem Jan Van Den Wijngaard, Claudio Screpanti
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Publication number: 20140179732Abstract: Compounds of the formula (I) useful as 11-Beta Hydroxysteroid Dehydrogenase InhibitorsType: ApplicationFiled: October 9, 2013Publication date: June 26, 2014Applicant: Janssen Pharmaceutica NVInventors: Libuse Jaroskova, Joannes Theodorus Maria Linders, Louis Jozef Elisabeth Van Der Veken, Gustaaf Henri Maria Willemsens
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Patent number: 8710241Abstract: The present invention relates to a novel anhydrous crystalline form of zofenopril calcium of formula (I), chemically known as (4S)-1-[(2S)-3-(benzoylthio)-2-methylpropionyl]-4-(phenylthio)-L-proline calcium salt or hemi-calcium salt. The present invention further relates to a process for the preparation of the new crystalline form of zofenopril calcium, its use in pharmaceutical compositions and the use of the new crystalline form and compositions in the treatment of hypertension and various other diseases.Type: GrantFiled: August 8, 2008Date of Patent: April 29, 2014Assignee: Generics [UK]LimitedInventor: Axel Becker
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Publication number: 20130303375Abstract: The present invention relates to novel strigolactam derivatives of formula (I) to processes and intermediates for pre-paring them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.Type: ApplicationFiled: December 9, 2011Publication date: November 14, 2013Applicant: SYNGENTA PARTICIPATIONS AGInventors: Mathilde Denise Lachia, Alain De Mesmaeker, Hanno Christian Wolf, Pierre Joseph Marcel Jung
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Publication number: 20130178612Abstract: Chiral auxiliaries useful for efficiently producing a phosphorus atom-modified nucleic acid derivative with high stereoregularity, and compounds represented by the following the general formula (I) or the general formula (XI) for introducing the chiral auxiliaries.Type: ApplicationFiled: September 22, 2011Publication date: July 11, 2013Applicant: CHIRALGEN, LTD.Inventors: Takeshi Wada, Mamoru Shimizu
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Patent number: 8329377Abstract: An imide compound represented by the formula (I): wherein R1 represents a C1-C20 aliphatic hydrocarbon group etc., W1 represents —CO—O— etc., Q1 and Q2 each independently represent a fluorine atom etc., and A represents a group represented by the formula (I-1): wherein A1 represents —CH2—CH2— etc., and a chemically amplified resist composition containing the same.Type: GrantFiled: July 21, 2009Date of Patent: December 11, 2012Assignee: Sumitomo Chemical Company, LimitedInventors: Ichiki Takemoto, Tatsuro Masuyama, Takashi Hiraoka
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Publication number: 20120287524Abstract: Disclosed are a novel compound, a pigment dispersion composition including the same, a photosensitive resin composition including the same, and a color filter using the same.Type: ApplicationFiled: June 22, 2010Publication date: November 15, 2012Applicant: CHEIL INDUSTRIES INC.Inventors: Seong-Yong Uhm, Seong-Ryong Nam, Taek-Jin Baek, Tae-Gyu Chun, Kyung-Hee Hyung
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Patent number: 8207213Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R1, R2, R3, X and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.Type: GrantFiled: February 1, 2007Date of Patent: June 26, 2012Assignee: Glaxo Group LimitedInventors: Mark Patrick Healy, Gerard Martin Paul Giblin, Helen Susanne Price
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Patent number: 8110681Abstract: Compounds of Formula (I) or (II) useful for the treatment of spinal muscular atrophy or other uses, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced by mutation or frameshift.Type: GrantFiled: March 13, 2007Date of Patent: February 7, 2012Assignees: The United States of America as represented by the Secretary, Department of Health and Human Services, Albany Molecular Research, Inc., Science Applications International Inc. (SAIC)Inventors: Jill Heemskerk, Keith D. Barnes, John M. McCall, Graham Johnson, David Fairfax, Matthew Robert Johnson
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Patent number: 8026270Abstract: The present invention relates to naphthalene derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine.Type: GrantFiled: July 26, 2007Date of Patent: September 27, 2011Assignee: Glaxo Group LimitedInventors: Gerard Martin Paul Giblin, Mark Patrick Healy, Helen Susanne Price
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Patent number: 8003661Abstract: The invention is directed to naphthalene and quinoline sulfonylurea derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: March 25, 2008Date of Patent: August 23, 2011Assignee: Merck Canada Inc.Inventors: Jason Burch, Julie Farand, Yongxin Han, Claudio Sturino
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Publication number: 20110201663Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R1 R2 R3, R4, R5, R6, X and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.Type: ApplicationFiled: February 1, 2007Publication date: August 18, 2011Inventors: Andrew Billinton, Nicholas Maughan Clayton, Gerard Martin Paul Giblin, Mark Patrick Healy
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Publication number: 20110092561Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R1, R2, R3, X and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.Type: ApplicationFiled: February 1, 2007Publication date: April 21, 2011Inventors: Mark Patrick Healy, Gerard Martin Paul Giblin, Helen Susanne Price
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Patent number: 7714131Abstract: The present invention provides a compounds the formula (IV): and methods for producing an ?-(phenoxy)phenylacetic acid compound of the formula: wherein R1 is a member selected from the group consisting of: each R2 is a member independently selected from the group consisting of (C1-C4)alkyl, halo, (C1-C4)haloalkyl, amino, (C1-C4)aminoalkyl, amido, (C1-C4)amidoalkyl, (C1-C4)sulfonylalkyl, (C1-C4)sulfamylalkyl, (C1-C4)alkoxy, (C1-C4)heteroalkyl, carboxy and nitro; the subscript n is 1 when R1 has the formula (a) or (b) and 2 when R1 has the formula (c) or (d); the subscript m is an integer of from 0 to 3; * indicates a carbon which is enriched in one stereoisomeric configuration; and the wavy line indicates the point of attachment of R1; and compounds.Type: GrantFiled: September 20, 2006Date of Patent: May 11, 2010Assignee: Metabolex, Inc.Inventors: Yan Zhu, Peng Cheng, Xin Chen, Jingyuan Ma, Zuchun Zhao
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Publication number: 20100105718Abstract: The invention is directed to naphthalene and quinoline sulfonylurea derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: March 25, 2008Publication date: April 29, 2010Applicant: MERCK FROSST CANADA LTD.Inventors: Jason Burch, Julie Farand, Yongxin Han, Claudio Sturino
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Publication number: 20100092496Abstract: The present disclosure provides drug-ligand conjugates that are potent cytotoxins, wherein the drug is linked to the ligand through either a peptidyl, hydrazine, or disulfide linker. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.Type: ApplicationFiled: November 2, 2009Publication date: April 15, 2010Applicant: Medarex, Inc.Inventors: Sharon E. Boyd, Liang Chen, Sanjeev Gangwar, Vincent Guerlavais, Killian Horgan, Zhi-Hong Li, Bilal Sufi
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Patent number: 7671214Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.Type: GrantFiled: February 14, 2007Date of Patent: March 2, 2010Assignee: Molecular Probes, Inc.Inventors: Wai-Yee Leung, Ching-Ying Cheung, Stephen Yue
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Publication number: 20090318523Abstract: The present invention relates to benzoisoindole phenylacetic acid derivatives, corresponding pharmaceutical compositions, preparation processes and uses in medicine as EP4 receptor angonists.Type: ApplicationFiled: November 19, 2007Publication date: December 24, 2009Inventors: Gerald Martin Paul Giblin, Mark Patrick Healy, Helen Susanne Price
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Publication number: 20090312388Abstract: The present invention relates to naphthalene derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine.Type: ApplicationFiled: July 26, 2007Publication date: December 17, 2009Inventors: Gerard Martin Paul Giblin, Mark Patrick Healy, Helen Susanne Price
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Publication number: 20090030061Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein R1 to R8, X, and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.Type: ApplicationFiled: February 12, 2007Publication date: January 29, 2009Inventors: Mark Patrick Healy, Gerard Martin Paul Giblin, Neil Derek Miller
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Publication number: 20080289541Abstract: A pigment composition contains a specified benzoisoindole derivative, and a pigment. A colored composition contains such a pigment composition and a pigment carrier.Type: ApplicationFiled: August 15, 2007Publication date: November 27, 2008Applicant: TOYO INK MFG. CO., LTD.Inventors: Shoko Goto, Shuuichi Kimura, Masakazu Takayama, Hiroyuki Yanai
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Publication number: 20080214597Abstract: the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents C or N; Y represents C or N; L represents a methyl or a direct bond; Z1 represents a direct bond, C1-2alkyl- or a divalent radical of formula —CH2—CH? (a) or —CH? (b); Z2 represents a direct bond, C1-2alkyl- or a divalent radical of formula —CH2—CH? (a) or —CH? (b); R1 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, hydroxycarbonyl, NR3R4 or C1-4alkyl optionally substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR5R6 or R1 represents C1-4alkyloxy- optionally substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR7R8; R2 represents hydrogen, halo, C1-4alkyl or C1-4alkyloxy-; R3 and R4 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R5 and R6 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R7 and R8 each inType: ApplicationFiled: August 26, 2005Publication date: September 4, 2008Applicant: JANSSEN PHARMACEUTICAL N.V.Inventors: Libuse Jaraskova, Joannes Theodorus Maria Linders, Louis Jozef Elisabeth Van Der Veken, Gustaaf Henri Maria Willemsens
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Patent number: 7173047Abstract: Compounds of formula (I) and pharmaceutically acceptable derivatives thereof bind with high affinity to the EP4 receptor and are of use in the treatment or prevention of conditions such as a pain, inflammatory, immunological, bone, neurodegenerative or renal disorder.Type: GrantFiled: December 20, 2001Date of Patent: February 6, 2007Assignee: Glaxo Group LimitedInventors: Gerard Martin Paul Giblin, Stephen Vernon Frye, Susan Roomans
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Patent number: 7166631Abstract: The present invention relates to a compound of formula (I): corresponding pharmaceutical compositions, preparation processes, and/or methods of using the aforementioned compounds and/or compositions.Type: GrantFiled: February 7, 2002Date of Patent: January 23, 2007Assignee: Glaxo Group LimitedInventors: Miles Stuart Congreve, Gerard Martin Paul Giblin, Ann Louise Walker
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Patent number: 6977305Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.Type: GrantFiled: September 29, 2001Date of Patent: December 20, 2005Assignee: Molecular Probes, Inc.Inventors: Wai-Yee Leung, Ching-Ying Cheung, Stephen Yue
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Patent number: 6924297Abstract: Compounds of formula (I) and pharmaceutically acceptable derivatives thereof bind with high affinity to the EP4 receptor and are of use in the treatment or prevention of conditions such as a pain, inflammatory, immunological, bone, neurodegenerative or renal disorder.Type: GrantFiled: December 20, 2001Date of Patent: August 2, 2005Assignee: SmithKline Beecham CorporationInventors: Gerard Martin Paul Giblin, Haydn Terence Jones, Andrew McMurtrie Mason, Neil Derek Miller, Susan Roomans, Stephen Edward Shanahan, Ann Louise Walker
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Patent number: 6909006Abstract: Compounds of formula (III) or (V), wherein is a solid support; L is a linking group or a single bond; T is a combinatorial unit; n is a positive integer, where if n is greater than 1, each T may be different: X is an electrophilic leaving group; Y is selected from NH-Prot, O-Prot, S-Prot, NO2, —NHOH. N3, NHR, NRR, N?NR, N(O)RR, NHSO2R, N?N?PhR, SR or SSR, where Prot represents a protecting group; A and B collectively represent a fused benzene or pyrrole ring (in either orientation), which is optionally substituted by up to respectively 4 or 2 groups independently selected from R, OH, OR, halo, nitro, amino, Me3Sn, CO2H, CO2R, R1 is a nitrogen protecting group, where if Y includes a protecting group, these protecting groups are orthogonal and R2 and R7 are independently selected from H, R, OH, OR, halo, nitro, amino, Me3Sn, and other related compounds and collections of compounds.Type: GrantFiled: February 22, 2000Date of Patent: June 21, 2005Assignee: Spirogen LimitedInventors: David Edwin Thurston, Philip Wilson Howard
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Patent number: 6784167Abstract: 17-beta-hydroxysteroid dehydrogenase-II inhibitors having the structural formula wherein the phenyl group labeled A and the group —C(R4)(R6)Y are oriented cis to each other; W represents O or S; R1 represents —H or optionally substituted —(C1-C4)alkyl; n represents 0 or an integer of 1-3; and R2 represents any of a variety of substituents on ring A. R4 generally represents —H but may be a bond terminating at the ortho position of ring A. Y represents fluorine, —OR5, or —SR5, and R5 represents —H, optionally substituted —(C1-C4)alkyl, optionally substituted -phenyl, optionally substituted —(C1-C4)alkyl-phenyl, or optionally substituted —(C1-C4)acyl. R6 represents any of a variety of groups as defined in the specification and claims, including heteroaryl, arylalkyl, heteroarylalkyl, arylalkenyl, heteroarylalkenyl, alkynyl, arylalkynyl, heteroarylalkynyl, aryl, and indolyl.Type: GrantFiled: September 28, 2001Date of Patent: August 31, 2004Assignee: Bayer Pharmaceuticals CorporationInventors: Jill E. Wood, Jeremy L. Baryza, Catherine R. Brennan, Soongyu Choi, James H. Cook, Brian R. Dixon, Paul P. Ehrlich, David E. Gunn, Ian McAlexander, Peiying Liu, Derek B. Lowe, Anikó M. Redman, William J. Scott, Yamin Wang
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Patent number: 6699899Abstract: Imido and amido substituted acylhydroxamic acids which reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)propanoate.Type: GrantFiled: December 21, 1999Date of Patent: March 2, 2004Assignee: Celgene CorporationInventors: Hon-Wah Man, George W Muller, Shaei Y Huang
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Patent number: 6605626Abstract: 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: GrantFiled: September 21, 2001Date of Patent: August 12, 2003Assignee: 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
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Patent number: 6534660Abstract: Improved synthesis of seco(−)CBI (5-hydroxy-3-amino-1-[S]-(chloromethyl)-1,2 -dihydro-3H-benz(e)indole): and improved syntheses therefrom of a wide variety of CC-1065 analogs that comprise a cyclopropabenzidole (CBI) alkylating moiety, and which are collectively DC1 and its derivatives, for the synthesis of cell-targeted therapeutic agents.Type: GrantFiled: April 5, 2002Date of Patent: March 18, 2003Assignee: Immunogen, Inc.Inventors: Robert Yongxin, Ravi V. J. Chari
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Patent number: 6498182Abstract: The present invention is directed to compounds of formula I, formula Ia, and formula Ib. wherein each of R1, R2, R3, R4, Ra, and Rb has been defined herein. The invention is also directed to a process for the preparation, the use and pharmaceutical compositions comprising the compounds described above. These novel compounds are useful in therapy, particularly for the treatment of type 2 diabetes.Type: GrantFiled: September 26, 2001Date of Patent: December 24, 2002Assignee: Biovitrum ABInventors: Styrbjörn Byström, Stephen James, Charlotta Liljebris
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Patent number: 6469042Abstract: There is provided novel 3-fluoro-3-phenyl oxindole derivatives of Formula I wherein R1, R2, R3 and R4 each are independently hydrogen, C1-4 alkyl, halogen, fluoromethyl, trifluoromethyl, phenyl, 4-methylphenyl or 4-trifluoromethylphenyl; R5 is C1-6 alkyl optionally substituted with one to three same or different groups selected from fluoro and chloro, provided R5 is not C1-6 alkyl when Y is O; Y is O or S; and R6 and R7 each are independently hydrogen, chloro, bromo or trifluoromethy; which are openers of the KCNQ potassium channels and are useful in the treatment of disorders which are responsive to the opening of the KCNQ potassium channels.Type: GrantFiled: February 14, 2002Date of Patent: October 22, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Piyasena Hewawasam, Pierre Dextraze, Valentin K. Gribkoff, Gene G. Kinney, Steven I. Dworetzky
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Patent number: 6395766Abstract: Compounds according to Formula (I) or a pharmaceutically acceptable salt thereof are GABA-A Alpha 5 ligands useful for enhancing cognition: where A is C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, arylC1-6alkyl, or aryl wherein the aryl group is optionally substituted by halogen, C1-6alkyl, CF3, CN, NO2 or NH2, NR1R10, S(O)pR1, heteroarylC1-6alkyl or heteroaryl where heteroaryl is a 5- or 6-membered heteroaromatic ring as defined for B; and B is phenyl or a 5-membered ring having one or two unsaturations containing 1, 2, 3, or 4 heteroatoms chosen from O, N and S provided that not more than one heteroatom is other than N, a 6-membered heteroaromatic ring containing 1, 2, 3 or 4 nitrogen atoms, each of which rings is optionally substituted by one or more substituents.Type: GrantFiled: November 6, 2000Date of Patent: May 28, 2002Assignee: Merck Sharp & Dohme LimitedInventors: Howard Barff Broughton, Helen Jane Bryant, Mark Stuart Chambers, Neil Roy Curtis
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Patent number: 6323216Abstract: Novel basic derivatives of benz[e]isoindol-1-ones and pyrrolo[3,4-c]quinolin-1-ones which can be represented by the general formula (I) indicated below are described: in which X is CH or N, R is H, Cl or OR1 in which R1 is H or an alkyl group having from 1 to 3 carbon atoms, Het is the 3-endotropyl group (that is, the 8-methyl-8-azadicyclo[3.2.1]oct-3-yl group) or the 3-quinuclidyl group (that is, the 1-azadicyclo[2.2.2]oct-3-yl group); these compounds have been found to be potent and selective antagonists of the 5-HT3 serotonin-like receptor and can therefore be used, for example, as anti-emetics as well as in various pathological conditions of the central nervous system, and as antitussives.Type: GrantFiled: October 13, 1999Date of Patent: November 27, 2001Assignee: Rotta Research Laboratorium S.p.AInventors: Francesco Makovec, Andrea Cappelli, Maurizio Anzini, Salvatore Vomero, Lucio Claudio Rovati
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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
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Patent number: 6130237Abstract: The invention provides compounds of general formula (I), wherein: X is halogen or OSO.sub.2 R, where R represents H or is unsubstituted or hydroxy-or amino-substituted lower alkyl; Y is a nitro or amine group or a substituted derivative thereof; W is selected from the structures of formulae (Ia, Ib or Ic), where E is --N.dbd. or --CH.dbd., G is O, S, or NH, and Q is either up to three of R, OR, NRR, NO.sub.2, CONHR, NHCOR or NHCONHR, or is an additional group of formulae (Ia, Ib or Ic) and HET represents a 5- or 6-membered carbocycle or heterocycle; and A and B collectively represent a fused benzene or 2-CO.sub.2 R pyrrole ring. In one embodiment, the group Y is an amine derivative substituted by a group which is a substrate for a nitroreductase or carboxypeptidase enzyme such that one of said enzymes is able to bring about removal of that group.Type: GrantFiled: March 12, 1999Date of Patent: October 10, 2000Assignee: Cancer Research Campaign Technology LimitedInventors: William A. Denny, Moana Tercel, Graham J. Atwell
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Patent number: 6077840Abstract: Compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof and a process for producing the same are disclosed. The compounds have progesterone receptor binding inhibitory activity and, hence, can be used as therapeutic and prophylactic agents for progesterone-related diseases. Specifically, they are useful as carcinostatic agents for breast cancer and ovarian cancer, therapeutic agents for hysteromyoma, endometriosis, meningioma, and myeloma, abortifacients, oral contraceptive pills, and therapeutic and prophylactic agents for osteoporosis and climacteric disturbance. ##STR1## wherein R.sup.1 represents alkyl or aralkyl; R.sup.Type: GrantFiled: June 18, 1999Date of Patent: June 20, 2000Assignee: Meiji Seika Kaisha, Ltd.Inventors: Kenichi Kurihara, Rie Shinei, Yasushi Kurata, Yuji Tabata, Kiyoshi Tanabe, Tsuneo Okonogi
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Patent number: 6037361Abstract: Fluorinated butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1, and also collagenase, matrilysin, and MMP-13, and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.Type: GrantFiled: March 9, 1998Date of Patent: March 14, 2000Assignee: Warner-Lambert CompanyInventors: Bruce David Roth, Patrick Michael O'Brien, Drago Robert Sliskovic
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Patent number: 6030967Abstract: A compound of the formula: whereinQ is an optionally substituted carbon atom or N(O)p wherein p is 0 or 1;Y is an optionally substituted methylene group, S(O)q wherein q is an integer of 0 to 2, or an optionally substituted imino group;Z.sup.1 is a C.sub.1-3 alkylene group which may have an oxo group or a thioxo group and may contain etherified oxygen or sulfur within the carbon chain;Z.sup.2 is an optionally substituted C.sub.1-3 alkylene group;Ar is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group;one of R.sup.1 and R.sup.2 is a hydrogen atom, a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group;the other is a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group; orR.sup.1 and R.sup.2 taken together with adjacent --c.dbd.c-- form a ring; andring A is a benzene ring which may be substituted in addition to R.sup.1 and R.Type: GrantFiled: October 30, 1997Date of Patent: February 29, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Shogo Marui, Masatoshi Hazama, Kohei Notoya, Masaki Ogino
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Patent number: 5968945Abstract: Novel amides and imides are inhibitors of tumor necrosis factor.alpha. and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. Typical embodiments include 3-(1,3-dioxobenzo[f]isoindol-2-yl)-3-(3-cyclopentyloxy-4-methoxyphenyl)pro pionamide and 3-(1,3-dioxo-4-azaisoindol-2-yl)-3-(3,4-dimethoxyphenyl)-propionarnide.Type: GrantFiled: January 14, 1998Date of Patent: October 19, 1999Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
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Patent number: 5877200Abstract: Cyclic amides are inhibitors of tumor necrosis factor and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is 3-phenyl-3-(1-oxoisoindolin-2-yl)propionamide.Type: GrantFiled: August 29, 1997Date of Patent: March 2, 1999Assignee: Celgene CorporationInventor: George W. Muller
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Patent number: 5854276Abstract: 1. WF16616 substance represented by the following structural formula (1) or its pharmaceutically acceptable salt. ##STR1## WF16616 substance exhibits an antimicrobial activity, especially an excellent antifungal activity.Type: GrantFiled: January 26, 1998Date of Patent: December 29, 1998Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Terumi Okudaira, Yasuhisa Tsurumi, Hiroshi Hatanaka, Toru Kino, Seiji Hashimoto
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Patent number: 5767141Abstract: Substituted propane derivatives, a process for their preparation and the use of the compounds for treating diseasesPropane derivatives of the formula I ##STR1## in which the radicals have the meanings stated in the description, a process for the preparation of these compounds, their use as pharmaceuticals, and pharmaceutical products are described. Also described are novel intermediates for preparing the compounds of the formula I.Type: GrantFiled: March 8, 1995Date of Patent: June 16, 1998Assignee: Hoechst AktiengesellschaftInventors: Gerrit Schubert, Horst Hemmerle, Peter Below, Andreas Herling, Hans-Jorg Burger
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Patent number: 5574039Abstract: The invention relates to TS-inhibiting compounds of the formula ##STR1## where W is an alkylene group; D is a structure having two rings that are unsubstituted or substituted, where (i) one ring is a phenyl ring and (ii) the other ring is a phenyl ring or a 6-membered heterocyclic ring; R is a hydrogen atom or an alkyl group; and X and Y together form ##STR2## and to salts of these compounds. The moiety W can be CH.sub.2, and D can be a phenyl ring bridged through a sulfonyl group to another ring.Type: GrantFiled: September 22, 1994Date of Patent: November 12, 1996Assignee: Agouron Pharmaceuticals, Inc.Inventors: Michael D. Varney, Gifford P. Marzoni, Cynthia L. Palmer, Judith P. Deal, Terence R. Jones
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Patent number: 5565483Abstract: There is provided novel substituted 3-phenyl oxindole derivatives of the formula ##STR1## wherein R is hydrogen, hydroxy or fluoro; R.sup.1, R.sup.2, R.sup.3and R.sup.4 each are independently hydrogen, C.sub.1-4 alkyl, halogen, trifluoromethyl, phenyl, p-methylphenyl or p-trifluoromethylphenyl; or R.sup.1 and R.sup.2, R.sup.2 and R.sup.3 or R.sup.3 and R.sup.4 are joined together to form a benzo fused ring;R.sup.5 is hydrogen or C.sub.1-4 alkyl; andR.sup.6 is chlorine or trifluoromethyl;or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof, which are openers of the large-conductance calcium-activated potassium channels and are useful in the treatment of disorders which are responsive to the opening of the potassium channels.Type: GrantFiled: June 7, 1995Date of Patent: October 15, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Piyasena Hewawasam, Nicholas A. Meanwell, Valentin K. Gribkoff