Carbon Or Halogen Bonded Directly At The 1- Or 3-position Patents (Class 552/651)
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Publication number: 20140227184Abstract: Methods of halogenating a carbon containing compound having an sp3 C—H bond are provided. Methods of fluorinating a carbon containing compound comprising halogenation with Cl or Br followed by nucleophilic substitution with F are provided. Methods of direct oxidative C—H fluorination of a carbon containing compound having an sp3 C—H bond are provided. The halogenated products of the methods are provided.Type: ApplicationFiled: August 20, 2012Publication date: August 14, 2014Applicant: The Trustees of Princeton UniversityInventors: John T. Groves, Wei Liu, Xiongyi Huang
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Publication number: 20140088053Abstract: The present application discloses 17? hydroxy steroid dehydrogenase (17? HSD) type 1, 3, 10 inhibitors and use thereof (alone and in combination) in the treatment of cancer and other afflictions. 17? HSD1 inhibitors include estradiol derivatives with a nieta-carbamoylbenzyl substituent at C 16. 17? HSD3/HSD10 inhibitors include androsterone derivatives substituted at the C3 position with a sulfonamide piperazine. Also disclosed are compounds that are inhibitors of both 17? HSD1 and 17? HSD3 that have a spiro-morpholine substituent at C20.Type: ApplicationFiled: March 26, 2012Publication date: March 27, 2014Applicant: UNIVERSITÉ LAVALInventors: Donald Poirier, René Maltais, Jenny Roy
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Publication number: 20140018538Abstract: The present invention provides novel high-valent palladium complexes. The complexes typically include multi-dentate ligands that stabilize the octahedral coordination sphere of the palladium(IV) atom. These complexes are useful in fluorinating organic compounds and preparing high-valent palladium fluoride complexes. The invention is particularly useful for fluorinating compounds with 19F for PET imaging.Type: ApplicationFiled: August 19, 2011Publication date: January 16, 2014Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: Eunsung Lee, Adam Seth Kamlet, David C. Powers, Takeru Furuya, Tobias Ritter
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Publication number: 20130331585Abstract: Provided are protected cyclopropylboronic acids that include a substituted cyclopropyl group and a boronic ester group having a protecting group. The protecting group is a pinene-derived iminodiacetic acid (PIDA) group or PIDA-based group.Type: ApplicationFiled: June 6, 2013Publication date: December 12, 2013Inventors: Matthew Duncton, Michael D. Burke
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Patent number: 8586770Abstract: The invention relates to methods to manipulate stem cells in vivo and in vitro to treat, e.g., a condition where cell or tissue repair is needed.Type: GrantFiled: February 18, 2011Date of Patent: November 19, 2013Assignee: Harbor Therapeutics, Inc.Inventor: James M. Frincke
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Patent number: 8536160Abstract: Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+, K+-ATPase. They are useful for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms.Type: GrantFiled: April 11, 2007Date of Patent: September 17, 2013Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Alberto Cerri, Giorgio Fedrizzi, Alessandra Benicchio, Giuseppe Bianchi, Patrizia Ferrari, Mauro Gobbini, Rosamaria Micheletti, Marco Pozzi, Piero Enrico Scotti
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Publication number: 20120316341Abstract: Methods for fluorinating organic compounds are described herein.Type: ApplicationFiled: April 11, 2012Publication date: December 13, 2012Inventors: Tobias Ritter, Pingping Tang
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Publication number: 20090275542Abstract: Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+, K+-ATPase. They are useful for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms.Type: ApplicationFiled: April 11, 2007Publication date: November 5, 2009Applicant: Sigma-Tau Industrie Farmaceutiche Riunite S.P.A.Inventors: Alberto Cerri, Giorgio Fedrizzi, Alessandra Benicchio, Giuseppe Bianchi, Patrizia Ferrari, Mauro Gobbini, Rosamaria Micheletti, Marco Pozzi, Piero Enrico Scotti
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Patent number: 5892069Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.Type: GrantFiled: April 25, 1997Date of Patent: April 6, 1999Assignee: The Children's Medical Center CorporationInventors: Robert John D'Amato, Moses Judah Folkman
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Patent number: 5804576Abstract: Steroids of the formula: ##STR1## useful as cancer preventive agents, anti-obesity agents, anti-hyperglycemic agents, anti-aging agents, and anti-hypercholesterolemic agents and anti-auto-immune agents.Type: GrantFiled: June 6, 1995Date of Patent: September 8, 1998Assignee: Research Corporation Technologies, Inc.Inventors: Arthur G. Schwartz, John R. Williams, Magid Abou-Gharbia, Ann R. Swern, Marvin Louis Lewbart
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Patent number: 5723455Abstract: Novel antiandrogenic agents are provided. An exemplary group of compounds has the structural formula (I) ##STR1## wherein R.sup.1 through R.sup.10, a and b are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat androgen-related clinical conditions are provided, as are methods and compositions for using the compounds as contraceptive agents.Type: GrantFiled: March 11, 1997Date of Patent: March 3, 1998Assignee: SRI InternationalInventors: Masato Tanabe, Wan-Ru Chao, Wesley K. M. Chong, David F. Crowe
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Patent number: 5714481Abstract: Steroids of the formula: ##STR1## useful as cancer preventive agents, anti-obesity agents, anti-hyperglycemic agents, anti-aging agents, and anti-hypercholesterolemic agents and anti-auto-immune agents.Type: GrantFiled: May 31, 1995Date of Patent: February 3, 1998Assignee: Research Corporation Technologies, Inc.Inventors: Arthur G. Schwartz, John R. Williams, Magid Abou-Gharbia, Daniel Swern, deceased, Marvin Louis Lewbart
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Patent number: 5252565Abstract: The present invention is directed to a group of compounds which are haloethyl substituted steroidal enzyme inhibitors. These compounds are useful as aromatase, 19-hydroxylase, and aldosterone biosynthesis inhibitors and they are prepared from the corresponding epoxide.Type: GrantFiled: September 6, 1991Date of Patent: October 12, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Norton P. Peet, Joseph P. Burkhart, J. O'Neal Johnston
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Patent number: 5157031Type: GrantFiled: March 21, 1989Date of Patent: October 20, 1992Assignee: Research Corporation Technologies, Inc.Inventors: Arthur G. Schwartz, Marvin L. Lewbart
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Patent number: 5140106Abstract: A process for the production of 3-deoxy-4-ene steroids of the general formula I ##STR1## is described, in which R.sub.1, R.sub.2 and R.sub.3 mean a hydrogen atom or a methyl group,R.sub.4 represents a lower alkyl group, a phenyl group or a free, esterified or etherified hydroxy group,R.sub.5 symbolizes a hydrogen atom, a vinyl group or the grouping --C.tbd.CR.sub.6 with R.sub.6 meaning a hydrogen atom, an alkyl group with a maximum of 4 carbon atoms or a halogen atom,X represents a methylene group, a fluoromethylene group, an ethylidene group or a vinylidene group,Y and U represent a methylene group or an ethylidene group andZ symbolizes a methylene group, an ethylidene group, a vinylidene group, a chloromethylene group or a hydroxymethylene group and in which the bonds represent three single bonds or one double bond and two single bonds or a conjugated double bond.Type: GrantFiled: January 17, 1991Date of Patent: August 18, 1992Assignee: Schering AktiengesellschaftInventors: Ekkehard Winterfeldt, Ulf Tilstamm, Helmut Hofmeister, Henry Laurent
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Patent number: 5086047Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl, alkylthio and haloalkyl of 1 to 6 carbon atoms, alkenyl and alkynyl of 2 to 6 carbon atoms, optionally substituted arylthio of 6 to 10 carbon atoms, aryl of 6 to 12 carbon atoms, acyl of an organic carboxylic acid of 1 to 12 carbon atoms, --CN, cycloalkyl of 3 to 6 carbon atoms and --(CH.sub.2).sub.m --Re, m is an integer from 1 to 3, Re is --OH or --SH or --Salk, Alk is alkyl of 1 to 6 carbon atoms, X is selected from the group consisting of oxygen, N--O--R.sub.1, ##STR2## or =X is H.sub.2 or ##STR3## R.sub.A and R.sub.B are individually selected from the group consisting of hydrogen, halogen and alkyl of 1 to 6 carbon atoms, R.sub.1 is hydrogen or alkyl of 1 to 6 carbon, R' is hydrogen or acyl, the wavy lines indicate --or -position, Y is selected from the group consisting of oxygen, NOR, ##STR4## or =Y is ##STR5## H.sub.Type: GrantFiled: December 24, 1990Date of Patent: February 4, 1992Assignee: Roussel Uclaf, Department des BrevetsInventors: Jean-Francois Gourvest, Dominique Lesuisse
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Patent number: 5001119Abstract: Compounds of the formula: ##STR1## are useful as anti-cancer, anti-obesity, anti-diabetic, anti-coronary agents, anti-aging agents, anti-hypolipidemic agents and anti-autoimmune agents.Type: GrantFiled: November 25, 1987Date of Patent: March 19, 1991Inventors: Arthur G. Schwartz, Marvin L. Lewbart
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Patent number: 4954446Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutial compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase including using these compounds to reduce prostate size. Also invented are intermediates used in preparing these compounds.Type: GrantFiled: July 14, 1989Date of Patent: September 4, 1990Assignee: SmithKline Beecham CorporationInventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf