Chalcogen Bonded Directly At 2- And 4-positions Patents (Class 544/285)
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Publication number: 20110301208Abstract: Novel classes of viral and fungal inhibitors are disclosed. These compounds are useful in treating, preventing, and/or ameliorating viral infections such as, for example, Hepatitis C Virus, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus, and fungal infections such as, for example, candidiasis.Type: ApplicationFiled: September 23, 2009Publication date: December 8, 2011Applicants: WICHITA STATE UNIVERSITY, GEORGETOWN UNIVERSITYInventors: Radhakrishnan Padmanabhan, William C. Groutas, Brent E. Korba
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Publication number: 20110294818Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.Type: ApplicationFiled: July 28, 2011Publication date: December 1, 2011Inventors: Hans Allgeier, Yves Auberson, David Carcache, Philipp Floersheim, Christel Guibourdenche, Wolfgang Froestl, Jörg Kallen, Manuel Koller, Henri Mattes, Joachim Nozulak, David Orain, Johanne Renaud
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Patent number: 8058284Abstract: The present invention provides novel sulfonylurea compounds of formula (I) and pharmaceutically acceptable derivatives and polymorph and amorphous forms thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also provides a method for preparing such compounds and forms and for preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt or forms thereof.Type: GrantFiled: November 3, 2006Date of Patent: November 15, 2011Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert Scarborough, Carroll Anna Scarborough, legal representative, Wolin Huang, Mukund Mehrotra, Xiaoming Zhang, Hilary Cannon, Craig M. Grant
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Patent number: 8058432Abstract: The present invention releates to a method for preparing a phenylalanine compound having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof: where R1-R4 are defined herein. The method involves reacting a specified acyl phenylalanine compound with a carbonyl group-introducing reagent and a specified anthranilic acid compound to form a carboxy-asymmetric urea compound which is converted to a quinazoline-dione compound in the presence of a carboxyl group-activating agent.Type: GrantFiled: May 22, 2009Date of Patent: November 15, 2011Assignee: Ajinomoto Co., Inc.Inventors: Noriyasu Kataoka, Kotaro Okado, Tatsuhiro Yamada, Koichi Fujita, Tamotsu Suzuki, Tatsuya Okuzumi, Masayuki Sugiki, Akinori Tatara
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Publication number: 20110196149Abstract: A method for the fluoridation of an iodonium salt with a fluoride ion source which can be carried out in an aqueous reaction solvent.Type: ApplicationFiled: April 18, 2011Publication date: August 11, 2011Applicant: GE HEALTHCARE LIMITEDInventors: HARRY JOHN WADSWORTH, PETER ANTHONY DEVENISH
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Patent number: 7994182Abstract: The subject of the present invention are quinazoline derivatives and their pharmaceutically acceptable salts of general formula (I), that inhibit a DNA-repairing enzyme, poly(ADP-ribose) polymerase (PARP), enabling them to be used for the preparation of pharmaceutical compositions for preventing or treating illnesses where PARP-inhibition yields a beneficial effect. In general formula (I) R1 stands for either hydrogen or a group of general formula (a); R2 stands for a) hydrogen or C1-6 alkyl group, if R1 is other than hydrogen, and b) if R1 is hydrogen, then R2 may be a group of general formula (b), (c) or (d). The subject of the present invention also embraces the preparation processes of the compounds described above.Type: GrantFiled: April 30, 2004Date of Patent: August 9, 2011Assignee: Pecsi TudomanyegyetemInventors: Balázs Sümegi, Kálmán Hideg, Tamás Kálai
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Patent number: 7951814Abstract: The present invention provides Quinazolinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.Type: GrantFiled: June 16, 2009Date of Patent: May 31, 2011Assignee: Glenmark Pharmaceuticals, S.A.Inventors: Meyyappan Muthuppalniappan, Abraham Thomas, Sukeerthi Kumar, Sanjay Margal, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay, Srinivas Gullapalli
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Publication number: 20110065918Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.Type: ApplicationFiled: November 22, 2010Publication date: March 17, 2011Applicant: Ajinomoto Co., Inc.Inventors: Shingo MAKINO, Tatsuya Okuzumi, Toshihiko Yoshimura, Yuko Satake, Nobuyasu Suzuki, Hiroyuki Izawa, Kazuyuki Sagi, Akira Chiba, Eiji Nakanishi, Masahiro Murata, Takashi Tsuji
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Patent number: 7906521Abstract: The present invention relates to compounds useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: September 17, 2004Date of Patent: March 15, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: B. Wesley Trotter, Richard Isaacs
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Patent number: 7893071Abstract: The present invention is directed to novel thalidomide derivative compounds that have activity as anti-angiogenic compounds. More particularly the compounds have the general structure: where R1 is selected from the group consisting of H, halo, alkyl, haloalkyl, —NH2, hydroxy and alkoxy; R2 is selected from the group consisting of optionally substituted bicyclic, optionally substituted aryl, and R6 is H, or C1-C8 alkyl; R19 is optionally substituted aryl; and m is 0-6.Type: GrantFiled: April 22, 2002Date of Patent: February 22, 2011Assignee: University of Virginia Patent FoundationInventor: Milton L. Brown
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Patent number: 7872125Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.Type: GrantFiled: May 30, 2006Date of Patent: January 18, 2011Assignee: Ajinomoto Co., Inc.Inventors: Shingo Makino, Tatsuya Okuzumi, Toshihiko Yoshimura, Yuko Satake, Nobuyasu Suzuki, Hiroyuki Izawa, Kazuyuki Sagi, Akira Chiba, Eiji Nakanishi, Masahiro Murata, Takashi Tsuji
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Publication number: 20110009434Abstract: Crystals of isopropyl ester of N-(2,6-dichlorobenzoyl)-4-[6-(methylamino)methyl-1-methyl-2,4-dioxo-1,4-dihydroquinazoline-3(2H)-yl]-L-phenylalanine hydrochloride are useful as ?4 integrin inhibitors.Type: ApplicationFiled: September 20, 2010Publication date: January 13, 2011Applicant: AJINOMOTO CO., INC.Inventors: Koichi FUJITA, Shinichiro Takahashi, Tatsuya Okuzumi, Tatsuhiro Yamada, Kotaro Okado, Noriyasu Kataoka, Haruko Hirashima, Hideyuki Yamaguchi
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Publication number: 20100311769Abstract: The present invention relates to a novel quinazoline-2,4-dione derivative of formula (I), a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising a compound of formula (I) as an active ingredient for preventing or treating neurological brain disease.Type: ApplicationFiled: January 8, 2009Publication date: December 9, 2010Applicant: SHIN POONG PHARMACEUTICAL CO., LTD.Inventors: Hwan Cho, II, Eun Bang Lee, Sin Cheol Kang, Won Seok Kim, Chul Kyu Lee
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Patent number: 7842700Abstract: Crystals of isopropyl ester of N-(2,6-dichlorobenzoyl)-4-[6-(methylamino)methyl-1-methyl-2,4-dioxo-1,4-dihydroquinazoline-3(2H)-yl]-L-phenylalanine hydrochloride are useful as ?4 integrin inhibitors.Type: GrantFiled: December 21, 2007Date of Patent: November 30, 2010Assignee: Ajinomoto Co., Inc.Inventors: Koichi Fujita, Shinichiro Takahashi, Tatsuya Okuzumi, Tatsuhiro Yamada, Kotaro Okado, Noriyasu Kataoka, Haruko Hirashima, Hideyuki Yamaguchi
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Publication number: 20100298298Abstract: The invention relates to quinazolinedione derivatives, processes for the preparation thereof and their therapeutic applications.Type: ApplicationFiled: April 5, 2010Publication date: November 25, 2010Applicant: SANOFI-AVENTISInventors: Annie CLAUSS, Christophe GLAESS, Gilbert MARCINIAK, Nicolas MUZET, Jean-Francois NAVE, André SEYER, Bertrand VIVET
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Patent number: 7834023Abstract: Compounds of formula I are provided: wherein Ar1 and Ar2 are substituted aromatic rings and L1 and L2 are independent divalent linking groups. The compounds are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.Type: GrantFiled: September 17, 2007Date of Patent: November 16, 2010Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Carroll Anna Crew, legal representative, Shawn M. Bauer, Anjali Pandey
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Publication number: 20100234350Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 14, 2009Publication date: September 16, 2010Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-McGuire, Hans-Michael Jantzen, David M. Sedlock
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Publication number: 20100222359Abstract: The present invention provides quinazolinedione derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, depression and dementia.Type: ApplicationFiled: February 26, 2010Publication date: September 2, 2010Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Sureshbabu Dadiboyena, Kouacou Adiey
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Publication number: 20100190746Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides quinazolinone, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.Type: ApplicationFiled: November 20, 2009Publication date: July 29, 2010Applicant: ICAGEN, INC.Inventors: Grant A. McNaughton-Smith, James B. Thomas, JR., George S. Amato
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Patent number: 7737274Abstract: The present invention provides a method for producing a phenylalanine derivative(s) having a quinazolinedione ring of formula (5), including steps comprising of reacting an acylphenylalanine derivative(s) of formula (1) with a carbonyl group-introducing reagent(s) and a derivative(s) of anthranilic acid to form an asymmetric urea intermediate(s); making the asymmetric urea intermediate(s) into a quinazolinedione compound(s) of formula (4) in the presence of a base(s); and N-alkylating quinazolinedione ring amide of the obtained quinazolinedione compounds with N-alkylation agents. This production method is an industrially applicable method for producing phenylalanine derivatives having a quinazolinedione skeleton, which are compounds highly useful as drugs having ? 4 integrin inhibiting activity.Type: GrantFiled: August 22, 2005Date of Patent: June 15, 2010Assignee: Ajinomoto Co., Inc.Inventors: Noriyasu Kataoka, Akinori Tatara, Masanobu Yatagai, Junko Yamanaka
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Publication number: 20100144747Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.Type: ApplicationFiled: September 29, 2009Publication date: June 10, 2010Inventors: Hans ALLGEIER, Yves AUBERSON, David CARCACHE, Philipp FLOERSHEIM, Christel GUIBOURDENCHE, Wolfgang FROESTL, Jörg KALLEN, Manuel KOLLER, Henri MATTES, Joachim NOZULAK, David ORAIN, Johanne RENAUD
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Publication number: 20100137593Abstract: The present invention provides crystals of phenylalanine derivatives of the formula (I): and particularly ?-type, ?-type, ?-type, ?-type, and ?-type crystals thereof. These crystals are excellent in preservation stability or moisture resistance. They can also be produced on an industrial scale.Type: ApplicationFiled: February 1, 2010Publication date: June 3, 2010Applicant: AJINOMOTO CO., INCInventors: Shinichiro Takahashi, Noriyasu Kataoka, Akinori Tatara, Toshihiro Matsuzawa
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Publication number: 20100113774Abstract: A compound of formula (I): in free or salt form, wherein A, R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.Type: ApplicationFiled: March 4, 2008Publication date: May 6, 2010Inventor: Roger John Taylor
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Publication number: 20100113391Abstract: [Problem] Provided is a compound, which exhibits a P2Y12 inhibitory action and is useful as a medical drug, particularly, as a platelet aggregation inhibitor. [Means for Solution] The inventors have eagerly investigated P2Y12 inhibitors. As a result, the inventors have found that a bicyclic heterocyclic compound such as quinazolinedione, isoquinolone, and the like having an amino group substituted with lower alkyl, cycloalkyl, or lower alkylene-cycloalkyl at the specific position exhibits an excellent platelet aggregation inhibitory action, thereby completing the present invention. Since the compound of the invention exhibits excellent P2Y12 inhibitory action and platelet aggregation inhibitory action, it is useful as a platelet aggregation inhibitor.Type: ApplicationFiled: April 17, 2008Publication date: May 6, 2010Applicant: Astellas Pharma Inc.Inventors: Yuji Koga, Takao Okuda, Takashi Kamikubo, Michihito Kageyama, Hiroyuki Moritomo
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Patent number: 7696214Abstract: The invention concerns quinazoline derivatives of Formula (I) wherein each of Q1, Z, m, R1, R2, R3 and Q2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumor disease.Type: GrantFiled: November 21, 2005Date of Patent: April 13, 2010Assignee: AstraZeneca ABInventors: Laurent François André Hennequin, Patrick Ple
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Patent number: 7678790Abstract: Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 23, 2005Date of Patent: March 16, 2010Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles Marlowe
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Publication number: 20090326225Abstract: This invention relates to novel processes for the preparation of compounds of the formula [1], wherein R1, R2, R3 and R4 are as defined in the claims and description as well as pharmaceutically acceptable salts thereof. The compounds of the formula [1] are hexacyclic compounds having potent anti-tumor activity.Type: ApplicationFiled: August 25, 2009Publication date: December 31, 2009Applicant: Chugai Seiyaku Kabushiki KaishaInventors: Hiroshi Fukuda, Takeshi Murata, Satoshi Niizuma, Hitomi Suda, Masao Tsukazaki
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Publication number: 20090325987Abstract: The present invention provides Quinazolinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.Type: ApplicationFiled: June 16, 2009Publication date: December 31, 2009Applicant: Glenmark Pharmaceuticals, S.A.Inventors: Meyyappan Muthuppalniappan, Abraham Thomas, Sukeerthi Kumar, Sanjay Margal, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay, Srinivas Gullapalli
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Patent number: 7638520Abstract: Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atheroscelerosis.Type: GrantFiled: November 21, 2006Date of Patent: December 29, 2009Assignee: SmithKline Beecham, plcInventors: Deirdre Mary Bernadette Hickey, Robert John Ife, Colin Andrew Leach, Ivan Leo Pinto, Stephen Allan Smith, Steven James Stanway
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Publication number: 20090318688Abstract: A method for preparing a phenylalanine derivative having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c): (a) reacting an acyl phenylalanine derivative represented by the following formula (2): with a carbonyl group-introducing reagent and a specific anthranilic acid derivative to thus form the corresponding carboxy-asymmetric urea derivative; (b) converting the carboxy-asymmetric urea derivative into the corresponding quinazoline-dione derivative in the presence of a carboxyl group-activating agent: (c) if desired, substituting an N-alkyl group for the hydrogen atom bonded to the nitrogen atom present in the quinazoline-dione ring of the quinazoline-dione derivative using an N-alkylation agent and then deprotecting the resulting product, when the substituent R3? which is a group corresponding to R3 is protected.Type: ApplicationFiled: May 22, 2009Publication date: December 24, 2009Applicant: AJINOMOTO CO., INC.Inventors: Noriyasu KATAOKA, Kotaro OKADO, Tatsuhiro YAMADA, Koichi FUJITA, Tamotsu SUZUKI, Tatsuya OKUZUMI, Masayuki SUGIKI, Akinori TATARA
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Patent number: 7629340Abstract: Disclosed are compounds having Formula (I) and the compositions and methods relating to these compounds, for treating or preventing a viral infection mediated at least in part by a virus in the Flaviviridae family of viruses, wherein A, R2, m, R, V, W, T, Z, R1, Y, and p are disclosed herein.Type: GrantFiled: December 12, 2006Date of Patent: December 8, 2009Assignee: SmithKline Beecham CorporationInventors: Franz Ulrich Schmitz, Christopher Don Roberts, Ali Dehghani Mohammad Abadi, Ronald Conrad Griffith, Martin Robert Leivers
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Patent number: 7625889Abstract: The present invention relates to a series of substituted bis aryl and heteroaryl compounds of formula (I): Wherein X, Y, Z, A, B, D, Ar, R1 and R2 are as defined herein. The compounds of this invention are selective 5HT2A antagonists, and are therefore, useful in treating a variety of diseases including but not limited to a wide variety of sleep disorders as disclosed and claimed herein.Type: GrantFiled: July 25, 2007Date of Patent: December 1, 2009Assignee: Aventis Pharmaceuticals Inc.Inventors: Paul Robert Eastwood, Hazel Hunt, David Mark Fink, Helen Katherine Smith, Richard Simon Todd
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Publication number: 20090274632Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.Type: ApplicationFiled: August 19, 2008Publication date: November 5, 2009Applicant: Senomyx, Inc.Inventors: Xiaodong Li, Andrew Patron, Catherine Tachdjian, Hong Xu, Qing Li, Alexey Pronin, Guy Servant, Lan Zhang, Thomas Brady, Vincent Darmohusodo, Melissa Arellano, Victor Selchau, Brett Weylan Ching, Donald S. Karanewsky, Paul Brust, Jing Ling, Wen Zhao, Chad Priest
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Patent number: 7605165Abstract: The present invention relates to the following phenylalanine derivatives or analogues thereof having an antagonistic activity to ?4 integrin and therapeutic agents for various diseases concerning ?4 integrin.Type: GrantFiled: August 20, 2004Date of Patent: October 20, 2009Assignee: Ajinomoto Co., Inc.Inventors: Kazuyuki Sagi, Hiroyuki Izawa, Akira Chiba, Tatsuya Okuzumi, Toshihiko Yoshimura, Yuji Tanaka, Miho Ono, Masahiro Murata
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Patent number: 7601713Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.Type: GrantFiled: December 15, 2006Date of Patent: October 13, 2009Assignee: Rigel Pharmaceuticals, Inc.Inventors: Pingyu Ding, Ankush Argade, Dane Goff, Rajinder Singh, Esteban Masuda, Vanessa Taylor, Sacha Holland
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Publication number: 20090203708Abstract: Disclosed herein are novel substituted-1H-quinazoline-2,4-dione derivatives, a preparation method thereof, and a pharmaceutical composition containing the same. The novel substituted-1H-quinazoline-2,4-dione derivatives are excellent in binding affinity and selectivity for 5-HT6 receptors over other receptors, inhibit serotonin(5-HT)-stimulated cAMP accumulation, and disrupt apomorphine(2 mg/kg, i.p.)-induced hyperactivity in rats. Thanks to these effects, the derivatives are useful in the treatment of 5-HT6 receptor-related central nervous system diseases.Type: ApplicationFiled: July 5, 2006Publication date: August 13, 2009Applicant: Korea Research Institute of Chemical TechnologyInventors: Churlmin Seong, Nosang Park, Jinil Choi, Chul Min Park, Wookyu Park, Jaeyang Kong
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Publication number: 20090156620Abstract: The present invention provides novel sulfonylurea salts of a salt of formula (I) and polymorph forms thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also provides a method for preparing such compounds and forms and for preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a salt of formula (I) or a pharmaceutically acceptable form thereof.Type: ApplicationFiled: November 5, 2008Publication date: June 18, 2009Applicant: Portola Pharmaceuticals, Inc.Inventors: Emma Sharp, Louisa Jane Quegan, Anjali Pandey, Juan Wang, Matthew Nieder, Wolin Huang
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Patent number: 7498325Abstract: The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.Type: GrantFiled: April 29, 2004Date of Patent: March 3, 2009Assignee: Karl Thomas GmbHInventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Helmut Pieper, Henri Doods, Gerhard Hallermayer, Michael Entzeroth, Wolfgang Wienen
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Publication number: 20090042916Abstract: The present invention provides novel sulfonylurea salts of a salt of formula (I) and polymorph forms thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also provides a method for preparing such compounds and forms and for preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a salt of formula (I) or a pharmaceutically acceptable form thereof.Type: ApplicationFiled: May 2, 2008Publication date: February 12, 2009Applicant: Portola Pharmaceuticals, Inc.Inventors: Emma Sharp, Louisa Jane Quegan, Anjali Pandey, Juan Wang, Matthew Nieder, Wolin Huang
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Publication number: 20090029979Abstract: This invention relates to compounds which bind to serotonin receptors inside or outside the central nervous system, in particular compounds which bind to the 5-HT2 or 5-HT7 receptors, their preparation and use, compositions containing them, and methods of treatment using them.Type: ApplicationFiled: July 7, 2006Publication date: January 29, 2009Applicant: BIO-MEDISINSK INNOVASJON ASInventors: Jo Klaveness, Bjarne Brudeli, Finn Olav Levy
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Publication number: 20080293749Abstract: Pyrrolidine(thi)one compounds substituted by heterocyclic substituents in the 3-position, their preparation and use in pharmaceutical compositions, in particular as immunomodulators for treatment and/or inhibition of inflammatory and autoimmune diseases and haematological-oncological diseases.Type: ApplicationFiled: June 2, 2008Publication date: November 27, 2008Applicant: Gruenenthal GmbHInventors: Sven FRORMANN, Stefanie FROSCH, Carsten GRIEBEL, Derek SAUNDERS, Fritz THEIL, Heinz GRAUBAUM
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Publication number: 20080287473Abstract: The present invention provides compounds capable of regulating apoptosis, e.g., via regulating mitochondrial fission or fusion. The present invention also provides methods of screening for compounds capable of regulating apoptosis and methods of treating conditions association with apoptosis.Type: ApplicationFiled: February 8, 2008Publication date: November 20, 2008Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Jodi Nunnari, Ann Cassidy-Stone, Mark Kurth
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Patent number: 7439249Abstract: The present invention relates to compounds that inhibit phosphatases, compositions thereof, and methods of using those compounds and compositions for treating diseases.Type: GrantFiled: December 31, 2003Date of Patent: October 21, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeffrey O. Saunders, Gregory F. Miknis, Alexandre J. Buckmelter, Kevin W. Hunt, James F. Blake, Guy P. A. Vigers, Xicheng Sun
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Patent number: 7407963Abstract: A compound of general formula (I) wherein R and R1 are as defined herein, or a tautomer, diastereomer, enantiomer, or salt thereof, particularly the physiologically acceptable salts thereof, which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing the compound, their use, and processes for preparing them.Type: GrantFiled: June 27, 2005Date of Patent: August 5, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Wolfgang Eberlein, Wolfhard Engel, Klaus Rudolf, Henri Doods, Gerhard Hallermayer, Eckhart Bauer
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Publication number: 20080153836Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.Type: ApplicationFiled: April 10, 2006Publication date: June 26, 2008Inventors: Hans Allgeier, Yves Auberson, David Carcache, Philipp Floersheim, Christel Guibourdenche, Wolfgang Froestl, Jorg Kallen, Manuel Koller, Henri Mattes, Joachim Nozulak, David Orain, Johanne Renaud
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Patent number: 7358239Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q isType: GrantFiled: March 14, 2005Date of Patent: April 15, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Patent number: 7358257Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 1, 2005Date of Patent: April 15, 2008Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-McGuire
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Publication number: 20080076914Abstract: The invention provides a method for the synthesis of an 18F-labelled product comprising deprotected of a protected 18F-labelled compound using a deprotection agent comprising a weak acid and wherein neutralisation and buffering of the deprotected product are carried out by the addition of a neutralisation agent. The deprotected product is buffered in a pH range suitable for subsequent autoclaving and formulation into an injectable radiopharmaceutical.Type: ApplicationFiled: September 23, 2005Publication date: March 27, 2008Inventors: Julian Grigg, Nigel Osborn
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Patent number: 7345049Abstract: Specific phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.Type: GrantFiled: December 22, 2004Date of Patent: March 18, 2008Assignee: Ajinomoto Co., Inc.Inventors: Kazuyuki Sagi, Tatsuya Okuzumi, Tatsuhiro Yamada, Shunsuke Kageyama, Yoichiro Shima, Tadakiyo Nakagawa, Munetaka Tokumasu, Masayuki Sugiki, Hajime Ito, Itsuya Tanabe, Tamotsu Suzuki, Akira Nakayama, Kazuyuki Ubukata, Kenji Shinkai, Yasuhiro Tanaka, Misato Noguchi, Ayatoshi Andou, Yoriko Yamamoto, Noriyasu Kataoka, Koichi Fujita
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Publication number: 20070191603Abstract: The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, V, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: ApplicationFiled: February 7, 2007Publication date: August 16, 2007Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander