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| Number | Title | Issue Date |
| 7470784 | Methods for synthesizing 2-chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)--purin-6-amine 2-Chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofiranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy... | 12/30/2008 |
| 7361759 | Method for producing L-biopterin To provide a method for producing L-biopterin on a large industrial scale by using a reagent which is inexpensive and easy to handle, without requiring a use of any particular equipment or plants. A method for porducing a biopterin derivative represented by t... | 04/22/2008 |
| 7291726 | Process for the preparation of 2′-halo-β-L-arabinofuranosyl nucleosides The present invention is directed to the process for the preparation of 2′-deoxy-2′-halo-β-L-arabinofuranosyl nucleosides, and in particular, 2′-deoxy-2′-fluoro-β-L-arabinofuranosyl thymine (L-FMAU), from L-arabinose, which is commercially available and le... | 11/06/2007 |
| 7244717 | Mutagenic nucleoside analogs for the treatment of viral disease The present invention relates to methods of treating viral disease using mutagenic nucleoside analogs. In particular, the invention provides 5-aldehydo-uracil nucleosides and derivatives thereof, and methods of administration thereof to increase the virus mutation r... | 07/17/2007 |
| 6958391 | Method for purifying 5′-protected 2′-deoxypurine nucleosides A method for efficiently purifying 5′ protected 2′-deoxypurine nucleosides, efficient production of which has previously been difficult. Impurities can be separated by obtaining the 5′ protected 2′-deoxypurine nucleoside as an inclusion crystal including a s... | 10/25/2005 |
| 6949640 | Method for synthesizing 2-chloro-9-(2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine 2-Chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin-9-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofuranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy... | 09/27/2005 |
| 6949521 | Therapeutic azide compounds Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs... | 09/27/2005 |
| 6924271 | 3-β-D-ribofuranosylthiazolo[4-5-d]pyridimine nucleosides and uses thereof The invention is directed to 3-β-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 compou... | 08/02/2005 |
| 6894159 | Process for the preparation of 2′-fluoro-5-methyl-beta-L-arabino-furanosyluridine The present invention relates to a novel and improved process for preparing 2′-fluoro-5-methyl-β-L-arabinofuranosyluridine represented by formula (1) which shows anti-viral activity, especially potent anti-viral activity against hepatitis B-virus and Epstein-Barr... | 05/17/2005 |
| 6870048 | Process for the preparation of 2'-halo-β-L-arabinofuranosyl nucleosides The present invention is directed to the process for the preparation of 2′-deoxy-2′-halo-β-L-arabinofuranosyl nucleosides, and in particular, 2′-deoxy-2′-fluoro-β-L-arabinofuranosyl thymine (L-FMAU), from L-arabinose, which is commercially available and le... | 03/22/2005 |
| 6680382 | Process for preparing purine nucleosides The present invention provides for the preparation ଲ-adenine nucleosides by coupling an adenine derivative containing an unprotected exocyclic amino group at the C-6 position and a blocked arabinofuranosyl derivative, in the presence of a base and s... | 01/20/2004 |
| 6579976 | Process for producing 2',3'-diethyl substituted nucleoside derivatives 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... | 06/17/2003 |
| 6512107 | Process for the preparation of 2'-fluoro-5-methyl-ଲ-L-arabinofuranosyluridine The present invention relates to a novel and improved process for preparing 2'-fluoro-5-methyl-ଲ-L-arabinofuranosyluridine represented by formula (I) which shows anti-viral activity, especially potent anti-viral activity against hepatitis B-virus an... | 01/28/2003 |
| 6500946 | Methods for producing nucleoside derivatives and intermediates therefor Novel intermediates of nucleoside derivatives, of which the 6-position of the nucleic acid base moiety is substituted with a halogen atom, are produced. Using those novel intermediates, even substrates, of which the 3'-position of the saccharide moiety is... | 12/31/2002 |
| 6403568 | 4'-C-ethynyl pyrimidine nucleosides and pharmaceutical compositions thereof The invention provides 4'-C-ethynyl pyrimidine nucleosides (other than 4'-C-ethynylthymidine) represented by formula [I]: ##STR1## wherein B represents a base selected from the group consisting of pyrimidine and derivatives thereof; X represents a hydroge... | 06/11/2002 |
| 6376470 | Polymer conjugates of ara-C and ara-C derivatives The present invention is directed to polymeric-prodrug transport forms of the formula: ##STR1## wherein: G is a linear or branched, terminally functionalized polymer residue; Y1 is O, S, or NR1 ; M is X or Q; wherein X is an electron with... | 04/23/2002 |
| 6335322 | Therapeutic agents ##STR1## wherein R is selected from the group consisting of elaidoyl, cis-eicosenoyl and trans-eicosenoyl; and pharmaceutical compositions comprising the Ara-C derivative.... | 01/01/2002 |
| 6333315 | 4'-C-ethynyl purine nucleoside compounds The invention provides 4'-C-ethynyl purine nucleosides represented by formula [I]: ##STR1## wherein B represents a base selected from the group consisting of purine and derivatives thereof; X represents a hydrogen atom or a hydroxyl group; and R repr... | 12/25/2001 |
| 6291670 | 4'-C-ethynyl pyrimidine nucleoside compounds and pharmaceutical compositions The invention provides 4'-C-ethynyl pyrimidine nucleosides (other than 4'-C-ethynylthymidine) represented by formula [I]: ##STR1## wherein B represents a base selected from the group consisting of pyrimidine and derivatives thereof; X represents a hydroge... | 09/18/2001 |
| 6271212 | Prodrug azide compositions and compounds Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the correspo... | 08/07/2001 |
| 6258360 | Prodrugs activated by targeted catalytic proteins Prodrugs that are activated by and conjugated to a catalytic antibody conjugated to a moiety that binds to a tumor cell population are provided.... | 07/10/2001 |
| 6242429 | Arabinosyladenine derivatives Antiviral Ara-A derivatives having resistance to metabolism by adenosinedeaminase (ADA) are 2-substituted arabinosyladenine derivatives represented by the formula (I) and pharmaceutically acceptable salts and hydrates thereof: ##STR1## wherein Z is a... | 06/05/2001 |
| 6121248 | Anti-viral agent Disclosed is an anti-viral agent against varicella-zoster virus or cytomegalovirus comprising, as an active ingredient, 2-thio-5-halogenopyrimidine arabinoside of the formula (1): ##STR1## wherein B denotes a thiopyrimidine base of the formula (2) or... | 09/19/2000 |
| 6103463 | Method of sorting a mixture of nucleic acid strands on a binary array A method of sorting mixtures of nucleic acid strands comprising hybridizing the strands to an array of immobilized oligonucleotides, each of which includes a constant segment adjacent to a variable segment. The constant segment of the immobilized oligonuc... | 08/15/2000 |
| 6090937 | Methods for producing nucleoside derivatives and intermediates therefor Novel intermediates of nucleoside derivatives, of which the 6-position of the nucleic acid base moiety is substituted with a halogen atom, are produced. Using those novel intermediates, even substrates, of which the 3'-position of the saccharide moiety is... | 07/18/2000 |
| 6020483 | Nucleoside modifications by palladium catalyzed methods This invention discloses a method for the preparation of 2'-modified nucleosides, using a palladium catalyst and an alkene functionalized with a heteroatom. Included in the invention are the novel pyrimidines and purines that can be prepared according to ... | 02/01/2000 |
| 5821236 | Tumor treatment with arabinofuranosyl purine derivatives 6-Alkoxy derivatives of Ara-G, and pharmaceutically acceptable esters thereof, are described as being useful in tumor therapy. Novel pharmaceutically acceptable esters, their preparation and pharmaceutical formulations containing them are also disclosed.... | 10/13/1998 |
| 5750675 | 2'-"up" fluorinated 2'-deoxy-arabinofuranosylpurines The present invention provides a compound having the structure: ##STR1## wherein R1 is hydrogen, benzyl or a substituted benzyl group; X is hydrogen, a flouro, an amino or a substituted amino group; Y is hydrogen, a methoxy, a methylthio, a benzylth... | 05/12/1998 |
| 5747472 | Therapeutic methods for using ARA-G derivatives 6-Alkoxy derivatives of Ara-G, and pharmaceutically acceptable esters thereof, are described as being useful in tumour therapy. Novel pharmaceutically acceptable esters, their preparation and pharmaceutical formulations containing them are also disclosed.... | 05/05/1998 |
| 5733890 | Adenylate analogs as potent anti-herpes virus agents Novel adenylate analogs having the following formula are synthesized in the present invention, which are found active against herpes simplex viruses: ##STR1## wherein R1 is hydroxyl, C1 -C4 alkoxy, an amino ester radi... | 03/31/1998 |
| 5705492 | 3'-O-aminoacyl ARA uridines, method of making, and antiviral activity Pyrimidine nucleoside derivatives of formula ##STR1## wherein R1 represents aryl, R2 represents lower alkyl, R3 represents an acyl group derived from an amino acid and R4 represents hydrogen or fluorine and... | 01/06/1998 |
| 5700666 | Process for the production of arabinonucleotides A process for the production of arabinonucleotides of general formula I ##STR1## in which X represents a hydrogen atom or a fluorine atom, is described, which is characterized in that an arabinonucleoside of general formula II ##STR2## in which ... | 12/23/1997 |
| 5661136 | 2-halo-2'-fluoro ARA adenosines as antinoplastic agents The present invention is directed to certain 2'-fluoro, 2-substituted purine nucleosides which are toxic to cancerous cell lines.... | 08/26/1997 |
| 5659027 | Boronated compounds A novel class of pharmaceutically active boronated compounds are provided. The boronated compounds include boronated purine and pyrimidine bases and boronated nucleosides, as well as phosphate esters and oligomers thereof. The compounds are boronated at t... | 08/19/1997 |
| 5654420 | Process for preparing 2'-cyano pyrimidine nucleoside compounds A process for preparing a compound of the formula: ##STR1## wherein R1 is a hydroxyl or an amino which may optionally be substituted; R2 is a hydrogen or a C1 -C4 alkyl; and R4a and R5a | 08/05/1997 |
| 5641758 | Cytarabine derivatives, the preparation and use thereof Novel cytarabine derivatives of the formula ##STR1## where R1, R2 and R3, which can be identical or different, are each selected from the group consisting of hydrogen, aliphatic C2 -C5 -acyl, ben... | 06/24/1997 |
| 5616567 | 2'-Cyano pyrimidine nucleoside compounds The pyrimidine compounds of the present invention are represented by the following formula: ##STR1## and pharmaceutically acceptable salts thereof, wherein, R1 represents a hydroxyl or an amino which may be substituted by an acyl group; R | 04/01/1997 |
| 5565438 | L-nucleosides for the treatment of epstein-bar virus A method for the treatment of a human infected with EBV that includes administering an EBV-treatment amount of an L-nucleoside of the formula: ##STR1## wherein R is 5-methyluracil, and R' is hydrogen, acyl, alkyl or a monophosphate, diphosphate or tr... | 10/15/1996 |
| 5525720 | Synthesis of 2'-"up" fluorinated 2'-deoxy-arabinofuranosyl purines The present invention provides a compound having the structure: ##STR1## wherein R1 is hydrogen, benzyl or a substituted benzyl group; X is hydrogen, a flouro, an amino or a substituted amino group; Y is hydrogen, a methoxy, a methylthio, a benzylth... | 06/11/1996 |
| 5521162 | Aristeromycin analogues of 4',5'-didehydro-5'-fluoro-adenosine and methods of treating neoplastic and viral disease conditions This invention relates to certain aristeromycin/adenosine derivatives which are useful in inhibiting AdoMet-dependent transmethylation and in the treatment of patients afflicted with neoplastic or viral disease states.... | 05/28/1996 |
