The Acyclic Carbon And An Additional Carbon Are Bonded Directly To The Same Oxygen (ethers, Esters, Etc.) Patents (Class 552/105)
  • Patent number: 7365132
    Abstract: 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: Grant
    Filed: April 25, 2003
    Date of Patent: April 29, 2008
    Assignee: Avecia Biotechnology Inc.
    Inventors: David John Moody, Donald Alfred Wellings
  • Patent number: 6031117
    Abstract: 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: Grant
    Filed: March 19, 1999
    Date of Patent: February 29, 2000
    Assignee: Prolinx Incorporated
    Inventors: Robert J. Kaiser, Mark L. Stolowitz
  • Patent number: 6028103
    Abstract: 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: Grant
    Filed: March 19, 1997
    Date of Patent: February 22, 2000
    Assignees: 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
  • Patent number: 5922890
    Abstract: 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: Grant
    Filed: December 3, 1997
    Date of Patent: July 13, 1999
    Assignee: Novartis AG
    Inventor: Konrad Bleicher
  • Patent number: 5726329
    Abstract: Phosphoramidites of the formula ##STR1## where R is a base-labile protecting group, R.sup.1 and R.sup.
    Type: Grant
    Filed: May 8, 1995
    Date of Patent: March 10, 1998
    Assignee: La Jolla Pharmaceutical Company
    Inventors: David S. Jones, John P. Hachmann, Michael J. Conrad, Stephen Coutts, Douglas Alan Livingston
  • Patent number: 5665877
    Abstract: 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: Grant
    Filed: May 17, 1996
    Date of Patent: September 9, 1997
    Assignee: Eli Lilly and Company
    Inventors: Margaret M. Faul, Michael R. Jirousek, Leonard L. Winneroski, II
  • Patent number: 5614647
    Abstract: 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: Grant
    Filed: May 25, 1995
    Date of Patent: March 25, 1997
    Assignee: Eli Lilly and Company
    Inventors: Margaret M. Faul, Michael R. Jirousek, Leonard L. Winneroski, II
  • Patent number: 5557002
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: September 17, 1996
    Assignees: Eisai Co., Ltd., Eisai Chemical Co., Ltd.
    Inventors: Yoshio Urawa, Ken Furukawa, Toshikazu Shimizu, Yoji Yamagishi, Tomio Tsurugi, Tomio Ichino
  • Patent number: 5541347
    Abstract: 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: Grant
    Filed: October 3, 1994
    Date of Patent: July 30, 1996
    Assignee: Eli Lilly and Company
    Inventors: Margaret M. Faul, Michael R. Jirousek, Leonard L. Winneroski II
  • Patent number: 5391785
    Abstract: Phosphoramidites of the formula ##STR1## where R is a base-labile protecting group, R.sup.1 and R.sup.
    Type: Grant
    Filed: July 15, 1992
    Date of Patent: February 21, 1995
    Assignee: La Jolla Pharmaceutial Company
    Inventors: David S. Jones, John P. Hachmann, Michael J. Conrad, Stephen Coutts, Douglas A. Livingston
  • Patent number: 5359100
    Abstract: 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: Grant
    Filed: August 13, 1993
    Date of Patent: October 25, 1994
    Assignee: Chiron Corporation
    Inventors: Michael S. Urdea, Brian Warner, Joyce A. Running, Janice A. Kolberg, Jennifer M. Clyne, Ray Sanchez-Pescador, Thomas Horn
  • Patent number: 5332845
    Abstract: 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: Grant
    Filed: February 26, 1993
    Date of Patent: July 26, 1994
    Assignee: Chiron Corporation
    Inventors: Michael S. Ureda, Thomas Horn
  • Patent number: 5306837
    Abstract: 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: Grant
    Filed: July 15, 1993
    Date of Patent: April 26, 1994
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Gregory S. Bisacchi, Toomas Mitt
  • Patent number: 5256806
    Abstract: 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: Grant
    Filed: November 12, 1992
    Date of Patent: October 26, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Gregory S. Bisacchi, Toomas Mitt
  • Patent number: 5252760
    Abstract: 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: Grant
    Filed: August 18, 1987
    Date of Patent: October 12, 1993
    Assignee: Chiron Corporation
    Inventors: Michael S. Urdea, Thomas Horn
  • Patent number: 5189164
    Abstract: 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: Grant
    Filed: February 20, 1990
    Date of Patent: February 23, 1993
    Assignee: Sandoz Ltd.
    Inventors: Prasad K. Kapa, Kau-Ming Chen
  • Patent number: 5189188
    Abstract: 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: Grant
    Filed: October 31, 1990
    Date of Patent: February 23, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventor: Udo Eckstein
  • Patent number: 4983759
    Abstract: 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: Grant
    Filed: December 20, 1989
    Date of Patent: January 8, 1991
    Assignee: Kanegafuchi Chemical Industry Co., Ltd.
    Inventors: Kenji Inoue, Satomi Takahashi, Keiichi Yonetsu, Noboru Ueyama
  • Patent number: 4923641
    Abstract: 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: Grant
    Filed: September 20, 1988
    Date of Patent: May 8, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Udo Eckstein, Hubertus Psaar
  • Patent number: 4897223
    Abstract: 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: Grant
    Filed: March 1, 1988
    Date of Patent: January 30, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Udo Eckstein, Hubertus Psaar, Roderich Raue
  • Patent number: 4870199
    Abstract: 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: Grant
    Filed: March 10, 1988
    Date of Patent: September 26, 1989
    Assignee: Sandoz Pharm. Corp.
    Inventors: Kau-Ming Chen, Goetz E. Hardtmann, Prasad K. Kapa, George T. Lee, Jerome Linder, Sompong Wattanasin