The Acyclic Carbon And An Additional Carbon Are Bonded Directly To The Same Oxygen (ethers, Esters, Etc.) Patents (Class 552/105)
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Patent number: 7365132Abstract: A polymer support is provided which comprises protected hydroxypolyC2-4 alkyleneoxy chains attached to a cross-linked polymer wherein the protected hydroxypolyC2-4 alkyleneoxy chain contains from 2 to 10 C2-4 alkyleneoxy groups and wherein the hydroxypolyC2-4 alkyleneoxy chains are protected with an acid labile group. The acid labile protecting group is preferably a poly-aryl methane protecting group. A monomer and process for the preparation of said support are also provided.Type: GrantFiled: April 25, 2003Date of Patent: April 29, 2008Assignee: Avecia Biotechnology Inc.Inventors: David John Moody, Donald Alfred Wellings
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Patent number: 6031117Abstract: The present invention provides arylboronic acid reagents useful for incorporation into modified oligonucleotides and polynucleotides. The modified oligonucleotides and polynucleotides thus produced are useful in bioconjugation reactions for the immobilization and purification of macromolecules.Type: GrantFiled: March 19, 1999Date of Patent: February 29, 2000Assignee: Prolinx IncorporatedInventors: Robert J. Kaiser, Mark L. Stolowitz
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Patent number: 6028103Abstract: The present invention provides a class of chemical compounds useful as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation. The active compounds are substituted triaryl methane compounds or analogues thereof where one or more of the aryl groups is replaced with a heteroaryl, cycloalkyl or heterocycloalkyl group and/or the tertiary carbon atom is replaced with a different atom such as Si, Ge, N or P. The compounds inhibit mammalian cell proliferation, inhibit the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.Type: GrantFiled: March 19, 1997Date of Patent: February 22, 2000Assignees: Children's Medical Center Corporation, Ion Pharmaceuticals, Inc.Inventors: Carlo Brugnara, Jose Halperin, Emile M. Bellot, Jr., Mark Froimowitz, Richard John Lombardy, John J. Clifford, Ying-Duo Gao, Reem M. Haidar, Eugene W. Kelleher, Falguni M. Kher, Adel M. Moussa, Yesh P. Sachdeva, Minghua Sun, Heather N. Taft
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Patent number: 5922890Abstract: New trityl linkers for use in solid phase synthesis comprise compounds of formula II ##STR1## wherein R.sub.4 is alkyl (e.g. C.sub.1-4 alkyl), halogen, NO.sub.2, or hydrogen;Z is a coupling group chosen from acylamido, acyloxy, amino, halogen, thiol or hydroxyl,where acyl is the residue of a carboxylic acid or a residue of formula R.sub.5 CO where R.sub.5 is an organic group;Y is H, a reactive functional group or an attachment to a solid phase;W is O when Y is H or a reactive functional group, or W is --NH--, or --NR.sub.6 --(urethane) when Y is an attachment to a solid phase,where R.sub.6 is an organic group and,each R which, may be the same or different, is C(O)NR.sub.7 R.sub.8, CF.sub.3, F or Cl wherein each R.sub.7 and R.sub.8, which may be the same or different, is H or C.sub.Type: GrantFiled: December 3, 1997Date of Patent: July 13, 1999Assignee: Novartis AGInventor: Konrad Bleicher
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Modified phosphorous intermediates for providing functional groups on the 5' end of oligonucleotides
Patent number: 5726329Abstract: Phosphoramidites of the formula ##STR1## where R is a base-labile protecting group, R.sup.1 and R.sup.Type: GrantFiled: May 8, 1995Date of Patent: March 10, 1998Assignee: La Jolla Pharmaceutical CompanyInventors: David S. Jones, John P. Hachmann, Michael J. Conrad, Stephen Coutts, Douglas Alan Livingston -
Patent number: 5665877Abstract: The present invention provides a novel synthesis of the compounds of Formula (I): ##STR1## The compounds are produced in high yield and without utilizing expensive chromatographic separations. The synthesis is particularly advantageous because it is stereoselective.Type: GrantFiled: May 17, 1996Date of Patent: September 9, 1997Assignee: Eli Lilly and CompanyInventors: Margaret M. Faul, Michael R. Jirousek, Leonard L. Winneroski, II
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Patent number: 5614647Abstract: The present invention provides a novel synthesis of the compounds of Formula (I): ##STR1## The compounds are produced in high yield and without utilizing expensive chromatographic separations. The synthesis is particularly advantageous because it is stereoselective.Type: GrantFiled: May 25, 1995Date of Patent: March 25, 1997Assignee: Eli Lilly and CompanyInventors: Margaret M. Faul, Michael R. Jirousek, Leonard L. Winneroski, II
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Patent number: 5557002Abstract: The present invention provides an industrially advantageous process for preparing a 2-alkyl-3-(biphenyl-4-yl)methyl-3H-imidazo[4,5-b]pyridine derivative represented by the following formula (II) which is a precursor of an antagonist against an angiotensin II receptor useful as an antihypertensive drug, a biphenyl derivative which is a precursor of the substituent of the pyridine derivative, a process for the preparation thereof, and an intermediate useful for the preparation of the biphenyl derivative: ##STR1## The 2-alkyl-3-(biphenyl-4-yl)methyl-3H-imidazo[4,5-b]pyridine derivative can be prepared in a high yield according to the present invention from a 2-amino-5-halogeno-3-nitropyridine derivative through amidation, N-alkylation and reductive cyclization. The halogen atom introduced at the 5-position as a protective group against nitration can be eliminated simultaneously in the step which is conducted thereafter. Thus, this process is industrially advantageous.Type: GrantFiled: June 6, 1995Date of Patent: September 17, 1996Assignees: Eisai Co., Ltd., Eisai Chemical Co., Ltd.Inventors: Yoshio Urawa, Ken Furukawa, Toshikazu Shimizu, Yoji Yamagishi, Tomio Tsurugi, Tomio Ichino
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Patent number: 5541347Abstract: The present invention provides a novel synthesis of the compounds of Formula (I): ##STR1## The compounds are produced in high yield and without utilizing expensive chromatographic separations. The synthesis is particularly advantageous because it is stereoselective.Type: GrantFiled: October 3, 1994Date of Patent: July 30, 1996Assignee: Eli Lilly and CompanyInventors: Margaret M. Faul, Michael R. Jirousek, Leonard L. Winneroski II
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Patent number: 5391785Abstract: Phosphoramidites of the formula ##STR1## where R is a base-labile protecting group, R.sup.1 and R.sup.Type: GrantFiled: July 15, 1992Date of Patent: February 21, 1995Assignee: La Jolla Pharmaceutial CompanyInventors: David S. Jones, John P. Hachmann, Michael J. Conrad, Stephen Coutts, Douglas A. Livingston
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Patent number: 5359100Abstract: Linear or branched oligonucleotide multimers useful as amplifiers in biochemical assays which comprise (1) at least one first single-stranded oligonucleotide unit that is complementary to a single-stranded oligonucleotide sequence of interest, and (2) a multiplicity of second single-stranded oligonucleotide units that are complementary to a single-stranded labeled oligonucleotide. Amplified sandwich nucleic acid hybridizations and immunoassays using the multimers are exemplified.Type: GrantFiled: August 13, 1993Date of Patent: October 25, 1994Assignee: Chiron CorporationInventors: Michael S. Urdea, Brian Warner, Joyce A. Running, Janice A. Kolberg, Jennifer M. Clyne, Ray Sanchez-Pescador, Thomas Horn
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Patent number: 5332845Abstract: Novel phosphorylating reagents are provided which are useful in DNA synthesis and purification procedures. The reagents are substituted phosphines which are particularly useful in the phosphorylation of nucleoside and solid supported oligonucleotides at the 5'-hydroxyl position. Phosphorylation using these reagents is easily and accurately monitored colorimetrically.Type: GrantFiled: February 26, 1993Date of Patent: July 26, 1994Assignee: Chiron CorporationInventors: Michael S. Ureda, Thomas Horn
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Patent number: 5306837Abstract: Novel intermediates useful in the preparation of the optically active antiviral compound [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one are described.Type: GrantFiled: July 15, 1993Date of Patent: April 26, 1994Assignee: E. R. Squibb & Sons, Inc.Inventors: Gregory S. Bisacchi, Toomas Mitt
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Patent number: 5256806Abstract: Novel intermediates useful in the preparation of the optically active antiviral compound [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one are described.Type: GrantFiled: November 12, 1992Date of Patent: October 26, 1993Assignee: E. R. Squibb & Sons, Inc.Inventors: Gregory S. Bisacchi, Toomas Mitt
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Patent number: 5252760Abstract: A method of phosphorylating a nucleoside or an oligonucleotide chain having a free 2', 3' or 5' hydroxyl moiety is provided. The method involves the use of a phosphorylating reagent which is selected such that the extent of phosphorylation can be monitored colorimetrically, easily and accurately. The phosphorylating reagent contains an aromatic species such as a dimethoxytrityl group that is cleavable with acid and colorimetrically detectable upon release.Type: GrantFiled: August 18, 1987Date of Patent: October 12, 1993Assignee: Chiron CorporationInventors: Michael S. Urdea, Thomas Horn
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Patent number: 5189164Abstract: A process for synthesizing syn-(E)-3,5-dihydroxy-7-substituted hept-6-enoic and heptanoic acids and derivatives and intermediates thereof from the corresponding keto-hydroxy compounds, which process comprises: providing a reaction medium comprising sodium borohydride and an alkoxydialkylborane compound; treating the keto-hydroxy compound with said reaction medium under conditions wherein a cyclic boronate ester is formed; and cleaving the cyclic boronate ester to obtain the dihydroxy product.The product compounds, or derivatives thereof, are useful as anti-atherosclerotic agents.Type: GrantFiled: February 20, 1990Date of Patent: February 23, 1993Assignee: Sandoz Ltd.Inventors: Prasad K. Kapa, Kau-Ming Chen
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Patent number: 5189188Abstract: Compounds of the general formula ##STR1## in which the symbols have the meaning given in the description, are highly suitable as color formers in recording materials based on acid developers. They give deep blue, green-blue, green, violet or red shades which have excellent sublimation and light fastness.Type: GrantFiled: October 31, 1990Date of Patent: February 23, 1993Assignee: Bayer AktiengesellschaftInventor: Udo Eckstein
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Patent number: 4983759Abstract: A compound of a 3,5,6-trihydroxyhexanoic acid derivative of the formula: ##STR1## wherein P.sup.1 and P.sup.2 are independently hydrogen atoms or hydroxy-protecting groups, or together form a ring, and R is an alkyl group is effectively prepared by a process comprising steps of:reacting a butyronitrile derivative of the formula: ##STR2## wherein P.sup.1 and P.sup.2 are the same as defined above with an .alpha.-haloacetate of the formula:X--CH.sub.2 --COOR (III)wherein X is a halogen atom, and R is the same as defined above in the presence of a metallic catalyst selected from the group consisting zinc and zinc-copper to form a keto acid derivative of the formula: ##STR3## wherein P.sup.1, P.sup.2 and R are the same as defined above, and then reducing the obtained keto-acid derivative of the formula (IV).Type: GrantFiled: December 20, 1989Date of Patent: January 8, 1991Assignee: Kanegafuchi Chemical Industry Co., Ltd.Inventors: Kenji Inoue, Satomi Takahashi, Keiichi Yonetsu, Noboru Ueyama
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Patent number: 4923641Abstract: Highly concentrated stable solutions of color-forming agents of the general formula ##STR1## wherein x denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy, acyloxy, alkylamino, dialkylamino, acylamino, aralkylamino or arylamino andR denotes alkyl, alkenyl or aralkyl,further isocyclic or heterocyclic rings can be fused onto the rings A, B, C and D and the cyclic and acyclic radicals and the rings A, B, C and D can carry further non-ionic substituents which are customary in dyestuff chemistry, or mixtures thereof, in water-insoluble organic solvents from the group comprising optionally chlorinated hydrocarbons, vegetable oils and phthalic acid esters are used for the preparation of pressure-sensitive recording materials.Type: GrantFiled: September 20, 1988Date of Patent: May 8, 1990Assignee: Bayer AktiengesellschaftInventors: Udo Eckstein, Hubertus Psaar
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Patent number: 4897223Abstract: Color-forming agents of the general formula ##STR1## wherein X denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy, acyloxy, alkoxycarbonyloxy, alkylamino, dialkylamino, acylamino, aralkylamino or arylamino,Q denotes cyano, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, carbamoyl, N-alkylcarbamoyl, N,N-dialkylcarbamoyl, N-alkyl-N-aryl-carbamoyl, acyl, alkoxysulphonyl, aralkoxysulphonyl, sulphamoyl, N-alkylsulphamoyl, N,N-dialkylsulphamoyl, alkylsulphonyl, arylsulphonyl or aralkylsulphonyl andR denotes alkyl, alkenyl or aralkyl,further isocyclic or heterocyclic rings can be fused on to the rings A, B, C and D, and the cyclic and acyclic radicals and the rings A, B, C and D can carry further substituents, are used for the preparation of pressure-sensitive recording materials.Type: GrantFiled: March 1, 1988Date of Patent: January 30, 1990Assignee: Bayer AktiengesellschaftInventors: Udo Eckstein, Hubertus Psaar, Roderich Raue
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Patent number: 4870199Abstract: Process for the synthesis of compounds of the formula ##STR1## in R[R*,S*] enantiomeric form, wherein each P.sub.1 is independently an hydroxy group-protecting group, andR.sub.2z is C.sub.1-4 alkyl, benzyl or allyl,comprising, as a key step when R.sub.2z is R.sub.2x, the reaction of the compound of the formula ##STR2## in (S) enantiomeric form with a compound of the formulaMg.sup. .circle.+2 (.sup..crclbar. OOC--CH.sub.2 --COOR.sub.2x).sub.2to obtain a compound of the formula ##STR3## in (S) enantiomeric form, and, as a key step when R.sub.2z is R.sub.2y, the reaction of a compound of the formula ##STR4## in (S) enantioimeric form with a compound of the formulaLi.sup..sym..crclbar. CH.sub.2 --COOR.sub.2yto obtain a compound of the formula ##STR5## in (S) enantiomeric form, wherein R.sub.2x is primary or secondary C.sub.1-4 alkyl, benzyl or allyl,R.sub.2y is C.sub.1-4 alkyl not containing an asymmetric carbon atom, andR.sub.Type: GrantFiled: March 10, 1988Date of Patent: September 26, 1989Assignee: Sandoz Pharm. Corp.Inventors: Kau-Ming Chen, Goetz E. Hardtmann, Prasad K. Kapa, George T. Lee, Jerome Linder, Sompong Wattanasin