Having Chalcogen, Carbonyl, Or Thiocarbonyl Bonded Directly To The 4-position Substituent Nitrogen Patents (Class 536/28.51)
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Patent number: 7601702Abstract: Deoxyuridine derivatives of Formula (I?); where A is O, S or CH2; B is O, S or CHR3; R1 is H, or various substituents; R2 is H, F; R3 is H, F, OH, NH2; or R2 and R3 together form a chemical bond; D is —NHCO—, —CONH—, —O—, —C(?O)—, —CH?CH, —C?C—, —NR5—; R4 is hydrogen or various substituents; R5 is H, C1-C4 alkyl, C1-C4 alkanoyl; E is Si or C; R6, R7 and R8 are independently selected from C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, or a stable monocyclic, bicyclic or tricyclic ring system have utility in the prophylaxis of treatment of parasitic diseases such as malaria.Type: GrantFiled: January 6, 2005Date of Patent: October 13, 2009Assignee: Medivir ABInventors: Ian Gilbert, Corinne Nguyen, Gian Filippo Ruda, Alessandro Schipani, Ganasan Kasinathan, Nils-Gunnar Johansson, Dolores Gonzalez Pacanowska
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Patent number: 7598230Abstract: The present invention relates to nucleoside diphosphate mimics and nucleoside triphosphate mimics, which contain diphosphate or triphosphate moiety mimics and optionally sugar-modifications and/or base-modifications. The nucleotide mimics of the present invention, in a form of a pharmaceutically acceptable salt, a pharmaceutically acceptable prodrug, or a pharmaceutical formulation, are useful as antiviral, antimicrobial, and anticancer agents. The present invention provides a method for the treatment of viral infections, microbial infections, and proliferative disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of the present invention optionally in combination with other pharmaceutically active agents.Type: GrantFiled: June 14, 2007Date of Patent: October 6, 2009Assignee: Biota Scientific Management Pty LtdInventors: Phillip D. Cook, Guangyi Wang, Thomas W. Bruice, Nicholas A. Boyle, Janet M. Leeds, Jennifer L. Brooks, Marija Prhavc, Maria Eugenia Ariza, Patrick C. Fagan, Yi Jin, Vivek K. Rajwanshi, Kathleen D. Tucker
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Patent number: 7585851Abstract: The present invention relates to compounds, compositions and methods for the treatment of a host infected with a hepatitis B virus. Specifically, compound and compositions of 3?-esters of 2?-deoxy-?-L-pyrimidine nucleosides are disclosed, which can be administered either alone or in combination with other anti-hepatitis B agents. Compound and compositions of 3?,5?-diesters of 2?-deoxy-?-L-pyrimidine nucleosides are also disclosed, which can be administered either alone or in combination with other anti-hepatitis B agents.Type: GrantFiled: October 25, 2004Date of Patent: September 8, 2009Assignees: Idenix Pharmaceuticals, Inc., Centre National de la Recherche Scientifique, L'Universite Montpellier IIInventors: Martin L. Bryant, Gilles Gosselin, Jean-Louis Imbach
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Publication number: 20090209754Abstract: The present application relates to an improved process for the preparation of capecitabine.Type: ApplicationFiled: January 5, 2009Publication date: August 20, 2009Inventors: Peter Lindsay MacDonald, Pierluigi Rossetto, Maurizio Gallina
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Publication number: 20090156547Abstract: The present invention relates to novel amide prodrugs of gemcitabine, compositions thereof and methods for using.Type: ApplicationFiled: November 30, 2005Publication date: June 18, 2009Inventors: David Michael Bender, David Michael Remick
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Publication number: 20090069557Abstract: A process for preparation of gemcitabine hydrochloride and purification thereof.Type: ApplicationFiled: February 6, 2007Publication date: March 12, 2009Applicants: Dr. Reddy's Laboratories Ltd., Dr. Reddy's Laboratories, Inc.Inventors: Venkata Raghavendra Acharyulu Palle, Sekhar Munaswamy Nariyam, Veerender Murki, Anirudha Arvind Waghmare, Vishnu Nandkishore Mundhada
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Publication number: 20090062521Abstract: To provide an excellent amidite for synthesizing modified nucleic acid, which enables a protective group therein to be removed under a moderate condition, thereby stably producing a hydroxyl group-containing modified nucleic acid, and a method for synthesizing modified nucleic acid using the amidite. Specifically, an amidite for synthesizing modified nucleic acid, expressed by General Formula (I): where X represents a base, Y represents a substituent, Z represents a protective group for protecting a hydroxyl group in the substituent, and Q represents one of a hydrogen atom, a hydroxyl group and a hydroxyl group protected by a protective group, wherein the protective group can be removed in an aprotic solvent, and when the protective group is removed, the hydroxyl group emerges in the substituent, and a method for synthesizing modified nucleic acid using the amidite.Type: ApplicationFiled: July 29, 2008Publication date: March 5, 2009Applicant: FUJITSU LIMITEDInventor: Tsuyoshi FUJIHARA
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Patent number: 7485717Abstract: Orthogonally protected 3?-amino nucleoside monomers and efficient methods for their synthesis are described. The methods employ selective protection of the 3?-amino group in the presence of the unprotected nucleoside base.Type: GrantFiled: June 30, 2005Date of Patent: February 3, 2009Assignee: Geron CorporationInventors: Sergei M. Gryaznov, Krisztina Pongracz, Daria Zielinska
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Publication number: 20080300399Abstract: An intermediate (2) useful in making capecitabine can be formed without the use, or presence, of a silylation agent.Type: ApplicationFiled: June 2, 2008Publication date: December 4, 2008Inventor: Gerrit J. B. Ettema
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Publication number: 20080145372Abstract: The present invention relates to a compound of formula (1), or a pharmaceutically acceptable salt thereof, Formula: (1); wherein: R1 is a substituted aryl or heteroaryl group bearing at least one nitro or azido group or is an optionally substituted benzoquinone, optionally substituted naphthoquinone or optionally substituted fused heterocycloquinone: R2 is H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, aryl or heteroaryl; and R3 is selected such that R3NH2 represents a cytotoxic nucleoside analogue or an ester or phosphate ester prodrug of a cytotoxic nucleoside analogue, with the proviso that if R1 is an aryl group then R2 is not H.Type: ApplicationFiled: September 26, 2005Publication date: June 19, 2008Applicants: ANGIOGENE, PHARMACEUTICALS LIMITED, THE GRAY LABORATORY CANCER RESEARCH TRUSTInventors: Peter David Davis, Matthew Alexander Naylor, Peter Thomson, Steven Albert Everett, Michael Richard Lacey Stratford, Peter Wardman
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Patent number: 7378402Abstract: 4-Amino-1-((2R,3S,4S,5R)-5-azido-3,4-dihydroxy-5-hydroxymethyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (I:R1=R2=R3=R4=H) and prodrugs thereof are hepatitis C(HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting HCV and treating HCV-mediated diseases, processes for making the compounds and synthetic intermediates employed in the process.Type: GrantFiled: August 22, 2005Date of Patent: May 27, 2008Assignee: Roche Palo Alto LLCInventors: Joseph Armstrong Martin, Keshab Sarma, David Bernard Smith, Mark Smith
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Patent number: 7365188Abstract: The present invention provides a process for producing a N4-acyl-5?-deoxy-5-fluorocytidine compound of the formula: where R2 is alkyl, cycloalkyl, aralkyl, aryl, or alkoxy.Type: GrantFiled: December 22, 2004Date of Patent: April 29, 2008Assignee: Roche Colorado CorporationInventors: Christopher R. Roberts, Jim-wah Wong
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Patent number: 7276228Abstract: Methods are provided for treating hematological disorders by inhibition of DNA hypomethylation and histone deacetylase. Such disorders include, for example, acute promyelocytic leukemia, acute lymphoblastic leukemia, chronic myelogenous leukemia, myelodysplastic syndromes, and sickle cell anemia. The methods comprise: administering to a patient suffering from the disease a therapeutically effective amount of a DNA methylation inhibitor such as a cysteine analog such as decitabine, in combination with an effective amount of histone deacetylase inhibitor such as hydroxamic acid, cyclic peptide, benzamide, butyrate, and depudecin.Type: GrantFiled: March 15, 2005Date of Patent: October 2, 2007Assignee: SuperGen, Inc.Inventor: Jorge F. DiMartino
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Patent number: 6936709Abstract: A protected 2?-deoxycytidine is purified by precipitating the protected 2?-deoxycytidine represented by general formula (3) in the form of a hydrated crystal from a solution containing the protected 2?-deoxycytidine and water, and by recovering the protected 2?-deoxycytidine: wherein R1 represents a 4-methoxytrityl, 4, 4?-dimethoxytrityl, or triphenylmethyl group; and B1 represents a cytosine group having a protected amino group. The compound represented by general formula (3) is, in particular, a protected 2?-deoxycytidine represented by formula (4): The 2?-deoxycytidine is used as a raw material for antisense DNA.Type: GrantFiled: June 4, 2003Date of Patent: August 30, 2005Assignee: Mitsui Chemicals, Inc.Inventors: Hiroki Ishibashi, Kiyoteru Nagahara, Yasushi Fukuiri, Yasuko Matsuba
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Patent number: 6930097Abstract: A compound of formula 1-[3,4-dihydroxy-5-(2-hydroxyethyl)tetrahydrofuran-2-yl]pryimidine-2,4(1H,3H)-dione has inhibitory effects of matrix metalloproteinase-2 (gelatinase A) enzyme and binding of TNF? to TNF?-RI.Type: GrantFiled: April 21, 2003Date of Patent: August 16, 2005Assignee: Advanced Gene Technology Corp.Inventors: Li-Wei Hsu, Su-Chen Chang, Jeng-Woei Lee, Pang-Hsi Liu, Hui-Ping Lee, Yi-Ching Chen, Chun-Tsun Chen
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Patent number: 6924271Abstract: The invention is directed to 3-?-D-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.Type: GrantFiled: November 27, 2002Date of Patent: August 2, 2005Assignee: Anadys Pharmaceuticals, Inc.Inventors: Devron R. Averett, Stephen E. Webber, Joseph R. Lennox, Erik J. Rueden
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Patent number: 6908906Abstract: The present invention provides crystalline forms and compositions thereof, of a pyrimidine nucleoside derivative of formula (I) having anti-tumour activity, wherein formula (I) is:Type: GrantFiled: August 7, 2003Date of Patent: June 21, 2005Assignee: Sankyo Company, LimitedInventors: Takashi Takita, Keiichi Ohtsuka, Eiji Numagami, Susumu Harashima
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Patent number: 6905669Abstract: Compositions and methods are provided for treating diseases associated with aberrant silencing of gene expression such as cancer by reestablishing the gene expression through inhibition of DNA hypomethylation and histone deacetylase. The method comprises: administering to a patient suffering from the disease a therapeutically effective amount of a DNA methylation inhibitor such as a cysteine analog such as decitabine, in combination with an effective amount of histone deacetylase inhibitor such as hydroxamic acid, cyclic peptide, benzamide, butyrate, and depudecin.Type: GrantFiled: April 24, 2001Date of Patent: June 14, 2005Assignee: SuperGen, Inc.Inventor: Jorge F. DiMartino
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Patent number: 6894159Abstract: The present invention relates to a novel and improved process for preparing 2?-fluoro-5-methyl-?-L-arabinofuranosyluridine represented by formula (1) which shows anti-viral activity, especially potent anti-viral activity against hepatitis B-virus and Epstein-Barr virus:Type: GrantFiled: January 24, 2003Date of Patent: May 17, 2005Assignee: The University of Georgia Research FoundationInventors: Chung K. Chu, Jinfa Du, Yongseok Choi
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Patent number: 6870048Abstract: The present invention is directed to the process for the preparation of 2?-deoxy-2?-halo-?-L-arabinofuranosyl nucleosides, and in particular, 2?-deoxy-2?-fluoro-?-L-arabinofuranosyl thymine (L-FMAU), from L-arabinose, which is commercially available and less expensive than L-ribose or L-xylose, in ten steps. All of the reagents and starting materials are inexpensive and no special equipment is required to carry out the reactions.Type: GrantFiled: March 29, 2002Date of Patent: March 22, 2005Assignee: Triangle PharmaceuticalsInventor: Marcos Sznaidman
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Patent number: 6864244Abstract: The present invention relates to the hemisulfate salt of 1-[4(S)-azido-2(S),3(R)-dihydroxy-4-(hydroxymethyl)-1(R)-cyclopentyl]cytosine (Ia) with improved stability and physical properties which facilitate manufacturing, handling and formulating I and polymorphic crystalline forms thereof.Type: GrantFiled: December 9, 2003Date of Patent: March 8, 2005Assignee: Roche Palo Alto LLCInventors: Terrence Joseph Connolly, Joseph Armstrong Martin, Anthony Prince, Keshab Sarma
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Patent number: 6846810Abstract: The present invention relates to nucleoside derivatives for the treatment of Hepatitis C viral infections including compounds of formula I, pharmaceutical compositions comprising these compounds and methods for treatment or prophylaxis of Hepatitis C Virus mediated diseases employing said compounds in monotherapy or in combination therapy.Type: GrantFiled: November 19, 2003Date of Patent: January 25, 2005Assignee: Roche Palo Alto LLCInventors: Joseph Armstrong Martin, Keshab Sarma, David Bernard Smith, Mark Smith
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Publication number: 20040121980Abstract: The present invention relates to nucleoside derivatives for the treatment of Hepatitis C viral infections including compounds of formula I, pharmaceutical compositions comprising these compounds and methods for treatment or prophylaxis of Hepatitis C Virus mediated diseases employing said compounds in monotherapy or in combination therapy.Type: ApplicationFiled: November 19, 2003Publication date: June 24, 2004Applicant: Roche Palo Alto LLCInventors: Joseph Armstrong Martin, Keshab Sarma, David Bernard Smith, Mark Smith
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Publication number: 20040077588Abstract: This invention provides novel substrate compounds that selectively inhibit the proliferation f path logical cells, for example, pathological cells that endogenously overexpress a target enzyme that confers resistance to biologic and chemotherapeutic agents. The enzyme acts on a substrate compound to 1) convert it to a cellular toxin and/or 2) release a toxic byproduct. In one embodiment, the activity of the target enzyme has been greatly enhanced in a target cell as a result of loss f tum r suppressor function and/or selection resulting from previous exposure to chemotherapy. In another embodiment, the pathological cell contains a target enzyme that is an expression product of an infectious agent in the cell. Further provided by this invention is a method for treating a subject by delivering to the subject a prodrug as described herein. The prodrugs f this invention may be used alone or in combination with ther chemotherapeutics or alternative anti-cancer therapies such as radiation.Type: ApplicationFiled: October 7, 2003Publication date: April 22, 2004Inventors: H. Michael Shepard, Ming Fai Chan, Michael P. Groziak
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Patent number: 6617437Abstract: Compounds having particular interest as labels and various novel uses in diagnostics and therapeutics are provided which have structure (1) wherein R1 is a binding partner, a linker or H; a and b are 0 or 1, provided that the total of a and b is 0 or 1; A is N or C; X is S, O, —C(O)—, NH or NCH2R6; Y is —C(O)—; Z is taken together with A to form an aryl or heteroaryl ring structure comprising 5 or 6 ring atoms wherein the heteroaryl ring comprises a single O ring heteroatom, a single N ring heteroatom, a single S ring heteroatom, a single O and a single N ring heteroatom separated by a carbon atom, a single S and a single N ring heteroatom separated by a carbon atom, 2 N ring heteroatoms separated by a carbon atom, or 3 N ring heteroatoms at least two of which are separated by a carbon atom, and wherein the aryl or heteroaryl ring carbon atoms are unsubstituted with other than H or at least 1 nonbridging ring carbon atom is substituted with R6 or ═O; R6 isType: GrantFiled: December 21, 1999Date of Patent: September 9, 2003Assignee: Isis Pharmaceuticals, Inc.Inventors: Mark Matteucci, Robert J. Jones, Kuei-Ying Lin
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Publication number: 20030166606Abstract: Disclosed is a new fluorocystosine and derivatives thereof. The fluorocystosine and derivatives thereof provide a pharmaceutical composition exhibiting better anti-cancer characteristics than the conventional composition.Type: ApplicationFiled: January 26, 2003Publication date: September 4, 2003Inventors: Kwan-Hee Kim, Youn-Chul Kim, Ji-Young Kim, Kyeong-Ho Lee, Moon-Jong Noh, Young-Seok Park, Sung-Min Cho, Ho-Jin Park
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Patent number: 6579976Abstract: There can be provided an excellent industrial process for producing compounds having sugar-moiety hydroxyl groups or halogen atoms reduced in nucleic acids or in derivatives thereof by allowing O-thiocarbonyl derivatives of sugar-moiety hydroxyl groups or allowing halogenated derivatives in the sugar-moiety, in the nucleic acids or in derivatives thereof to react with any one of hypophosphorous acids (including salts thereof) and phosphites (esters) which are inexpensive, non-toxic and safely usable as radical reducing agents in industrial scale, in the presence of a radical reaction initiator. The process of the present invention is an industrially useful and highly safe process for reducing sugar-moiety hydroxyl groups and halogen atoms in nucleic acids or derivatives thereof (including nucleic acid-related compounds) at low costs.Type: GrantFiled: October 26, 1999Date of Patent: June 17, 2003Assignee: Ajinomoto Co., Inc.Inventors: Satoshi Takamatsu, Satoshi Katayama, Naoko Hirose, Kunisuke Izawa
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Patent number: 6566344Abstract: This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-&bgr;-L-erythro-pentoftiranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted.Type: GrantFiled: December 14, 2001Date of Patent: May 20, 2003Assignee: Idenix Pharmaceuticals, Inc.Inventors: Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
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Publication number: 20030069414Abstract: Modified nucleosides and methods of making and using the nucleosides are disclosed. The compounds can be prepared by reacting nucleoside starting materials that contain a suitable leaving group at one or more of the carbon atoms in the purine or pyrimidine ring, with a vinylstannane, carbon monoxide, and a palladium catalyst to provide 1-ene-3-one intermediates. These intermediates are then reacted with suitably functionalized primary or secondary amines via a Michael reaction. When the intermediate is a 5-position modified pyrimidine ring, and the amine contains a second hydrogen, it can do a second Michael reaction with the ene-one or the ene-imine in the pyrimidine ring. Appropriate modification of the amine reactant can yield products with various bioactivities. The nucleosides can be used therapeutically as anti-cancer, anti-bacterial or anti-viral drugs. The nucleosides can also be used for diagnostic applications, for example, by incorporating a radiolabel or fluorescent label into the molecule.Type: ApplicationFiled: August 9, 2002Publication date: April 10, 2003Applicant: GILEAD SCIENCES, INC.Inventors: Gary P. Kirschenheuter, Bruce Eaton
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Patent number: 6512107Abstract: The present invention relates to a novel and improved process for preparing 2′-fluoro-5-methyl-&bgr;-L-arabinofuranosyluridine represented by formula (I) which shows anti-viral activity, especially potent anti-viral activity against hepatitis B-virus and Epstein-Barr virus:Type: GrantFiled: July 23, 1998Date of Patent: January 28, 2003Assignee: The University of Georgia Research FoundationInventors: Chung K. Chu, Jinfa Du, Yongseok Choi
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Patent number: 6403568Abstract: The invention provides 4′-C-ethynyl pyrimidine nucleosides (other than 4′-C-ethynylthymidine) represented by formula [I]: wherein B represents a base selected from the group consisting of pyrimidine and derivatives thereof; X represents a hydrogen atom or a hydroxyl group; and R represents a hydrogen atom or a phosphate residue; and a pharmaceutical composition containing any one of the compounds and a pharmaceutically acceptable carrier. Preferably, the composition is used as an anti-HIV agent or a drug for treating AIDS.Type: GrantFiled: August 30, 2001Date of Patent: June 11, 2002Assignee: Yamasa CorporationInventors: Hiroshi Ohrui, Shiro Shigeta, Eiichi Kodama, Haruhiko Machida, Satoru Kohgo, Hiroaki Mitsuya
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Patent number: 6384019Abstract: The invention provides Gemcitabine esters or amides in which the 3′- and/or 5′-OH group and/or the N4-amino group is derivatised with a C18- and/or C20-saturated or mono-unsaturated acyl group, preferably an acyl group selected from oleoyl, elaidoyl, cis-eicosenoyl and trans-eicosenoyl. The Gemcitabine esters and amides are useful as anti-cancer and anti-viral agents.Type: GrantFiled: September 15, 1999Date of Patent: May 7, 2002Assignee: Norsk Hydro ASAInventors: Finn Myhren, Bernt Børretzen, Are Dalen, Marit Liland Sandvold
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Publication number: 20020042391Abstract: The invention provides Gemcitabine esters or amides in which the 3′- and/or 5′-OH group and/or the N4-amino group is derivatised with a C18- and/or C20-saturated or mono-unsaturated acyl group, preferably an acyl group selected from oleoyl, elaidoyl, cis-eicosenioyl and trans-eicosenoyl. The Gemcitabine esters and amides are useful as anti-cancer and anti-viral agents.Type: ApplicationFiled: September 15, 1999Publication date: April 11, 2002Inventors: FINN MYHREN, BERNT BORRETZEN, ARE DALEN, MARIT LILAND SANDVOLD
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Publication number: 20020035086Abstract: The invention relates to compositions comprising acyl derivatives of cytidine and uridine. The invention also relates to methods of treating hepatopathies, diabetes, heart disease, cerebrovascular disorders, Parkinson's disease, infant respiratory distress syndrome and for enhancement of phospholipid biosynthesis comprising administering the acyl derivatives of the invention to an animal.Type: ApplicationFiled: September 28, 2001Publication date: March 21, 2002Applicant: Pro Neuron, Inc.Inventors: Reid Warren von Borstel, Michael Kevin Bamat
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Patent number: 6291670Abstract: The invention provides 4′-C-ethynyl pyrimidine nucleosides (other than 4′-C-ethynylthymidine) represented by formula [I]: wherein B represents a base selected from the group consisting of pyrimidine and derivatives thereof; X represents a hydrogen atom or a hydroxyl group; and R represents a hydrogen atom or a phosphate residue; and a pharmaceutical composition containing any one of the compounds and a pharmaceutically acceptable carrier. Preferably, the composition is used as an anti-HIV agent or a drug for treating AIDS.Type: GrantFiled: May 12, 2000Date of Patent: September 18, 2001Assignee: Yamasa CorporationInventors: Hiroshi Ohrui, Shiro Shigeta, Eiichi Kodama, Haruhiko Machida, Satoru Kohgo, Hiroaki Mitsuya
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Patent number: 6211166Abstract: Novel 5′-deoxy-cytidine derivatives represented by the general formula (I) wherein R1 is a hydrogen atom or a group easily hydrolyzable under physiological conditions; R2 is a hydrogen atom, or —CO—OR4 group [wherein R4 is a saturated or unsaturated, straight or branched hydrocarbon group consisting of one to fifteen carbon atoms, or a group of the formula —(CH2)n—Y (in which Y is cyclohexyl or phenyl; n is an integer from 0 to 4)]; R3 is a hydrogen atom, bromo, iodo, cyano, a C1-4 alkyl group [which may be substituted with halogen atom(s)], a vinyl or ethynyl group [which may be substituted with halogen atom(s), C1-4 alkyl, cycloalkyl, aralkyl, or aromatic ring which may have one or more hetero atom(s)], or an aralkyl group which may be substituted for use in medical therapy, especially tumor therapy.Type: GrantFiled: March 24, 2000Date of Patent: April 3, 2001Assignee: Hoffman-La Roche Inc.Inventors: Kazuo Hattori, Tohru Ishikawa, Hideo Ishitsuka, Yasunori Kohchi, Nobuhiro Oikawa, Nobuo Shimma, Hitomi Suda
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Patent number: 6187914Abstract: The invention relates to nucleoside derivatives bearing electrolabile protector groupings and their use in an oligonucleotide synthesis method comprising at least one step of electronic deprotection.Type: GrantFiled: December 3, 1998Date of Patent: February 13, 2001Assignee: Cis Bio InternationalInventors: Robert Teoule, André Roget, Thierry Livache
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Patent number: RE38090Abstract: The invention relates to a 3′-substituted nucleoside derivative represented by the following general formula (1): wherein B means a nucleic acid base which may have a substituent, Z represents a lower alkynyl or lower alkenyl group which may be substituted by a group represented by the formula: in which Ra, Rb and Rc are individually a lower alkyl group or a phenyl group, or an oxiranyl group which may have at least one lower alkyl group, R1 and R2 individually represent H or an ester-forming residue capable of easily leaving in a living body, and R3 is H, a mono- or polyphosphoric acid residue, or an ester-forming residue capable of easily leaving in a living body, with the proviso that the sugar moiety is ribose, or a pharmaceutically acceptable salt thereof. The 3′-substituted nucleoside derivative according to the invention has an excellent antitumor activity and is hence useful for treatment for and prevention of cancers.Type: GrantFiled: May 26, 2000Date of Patent: April 22, 2003Assignees: Taiho Pharmaceutical Co., Ltd.Inventors: Akira Matsuda, Takuma Sasaki