Abstract: The present invention provides aminoalkoxy carbazole derivatives, and more specifically, provides compounds of formula (I)
wherein R1, R2, R3, R4, R8 and R9 are described herein. These compounds are 5-HT ligands, and are useful for treating diseases wherein modulation of 5-HT activity is desired.
Abstract: The present invention provides a compressed tablet of an antibacterial oxazolidinone agent which provides high drug load and excellent bioavailability.
Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)
X2—CH2—C*H(OH)—CH2—NH—CO—RN (VIIIA)
and processes for production of pharmacologically useful oxazolidinones.
Abstract: The present invention relates to (2S)-enantiomers of 2-aminoindan derivatives of formula I:
and a novel process for the preparation of them.
Type:
Grant
Filed:
February 14, 2001
Date of Patent:
June 25, 2002
Assignee:
Pharmacia & Upjohn Company
Inventors:
Arthur Glenn Romero, Thomas Andrew Runge, Bradley D. Hewitt, Kjell Anders Ivan Svensson, Chiu-Hong Lin, Kerry Anne Cleek, Susanne R. Haadsma-Svensson
Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)
X2—CH2—C*H(OH)—CH2—NH—CO—RN (VIIIA)
and processes for production of pharmacologically useful oxazolidinones.
Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)
X2—CH2—C*H(OH)—CH2—NH—CO—RN (VIIIA)
and processes for production of pharmacologically useful oxazolidinones.
Abstract: This invention discloses an efficient process for selectively sulfonating the primary alcohol of a diol containing both primary and secondary alcohols.
Type:
Grant
Filed:
February 25, 1998
Date of Patent:
February 27, 2001
Assignees:
Eli Lilly and Company, Wayne State University, University of Hawaii
Abstract: The present invention provides a method for controlling fungal growth, mycotic infections, yeast infections and parasitic infections using a therapeutically effective amount of a compound selected from Compounds (I-V). Further provided is a method for providing mdr inhibition using a therapeutically effective amount of a compound of formula (IA). Also provided is an antifungal composition comprising at least five percent (5%) by weight of a compound selected from Compounds (I-V).
Abstract: Cryptophycin compounds possessing a .beta.-epoxy moiety may be made with high stereoselectivity at various steps in the overall synthetic process. This invention also provides novel intermediates useful in preparing Cryptophycin compounds.
Type:
Grant
Filed:
August 24, 1999
Date of Patent:
November 7, 2000
Assignee:
Eli Lilly and Company
Inventors:
David Warren Hoard, Eric David Moher, Vinod Francis Patel, Bryan Hurst Norman
Abstract: A compound of formula IV ##STR1## wherein G is C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.12 alkenyl, C.sub.2 -C.sub.12 alkynyl or Ar;Ar is an aromatic or heteroaromatic group or a substituted aromatic or heteroaromatic group;R.sup.1 is halo, SR, OR, amino, mono or di-(C.sub.1 -C.sub.6 -alkyl)amino, tri (C.sub.1 -C.sub.6 -alkyl)ammonium, C.sub.1 -C.sub.6 -alkylthio, di(C.sub.1 -C.sub.6 -alkyl)sulfonium, C.sub.1 -C.sub.6 -alkylsulfonyl, or C.sub.1 -C.sub.6 -alkylphosphonyl;R.sup.2 is OH or SH; orR.sup.1 and R.sup.2 taken together form a second bond or together form an epoxide, aziridine, episulfide, or cyclopropyl ring;R is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkanoyl or Ar;R.sup.3 is C.sub.1 -C.sub.6 alkyl;R.sup.4 and R.sup.5 are H; orR.sup.4 and R.sup.5 taken together form a second bond;R.sup.24 is a leaving group; andR.sup.26 is an alcohol protecting group;X is O, NH or (C1-C3 alkyl)N--.
Type:
Grant
Filed:
July 2, 1999
Date of Patent:
October 17, 2000
Assignees:
Eli Lilly and Company, Wayne State University, University of Hawaii
Abstract: This invention provides processes for preparing lactone intermediates useful for the preparation of pharmaceutical compounds such as tetrahydrolipstatin and cryptophycin compounds.
Type:
Grant
Filed:
August 16, 1999
Date of Patent:
August 15, 2000
Assignees:
Eli Lilly and Company, Wayne State University, University of Hawaii
Abstract: A method of treatment of humans suffering from the Coronary Heart Disease Risk Factor (CHDRF) Syndrome which comprises the steps of 1) administering, by a pharmaceutically effective mode, a priming dose of drug composition selected from the group consisting of opiate antagonists, and drugs which substantially equally reduce the amounts of catecholamines bound to catecholamine binding sites for a period of about one to four weeks, and 2) administering a maintenance dose of said selected drug, is disclosed.
Abstract: A method of treatment of humans suffering from the Coronary Heart Disease Risk Factor (CHDRF) Syndrome which comprises administering, by a pharmaceutically effective mode, a drug composition selected from the group consisting of opiate antagonists or anti-opioids, and drugs which substantially equally reduce the amounts of catecholamines bound to all catecholamine binding sites, is disclosed.
Abstract: A method of treatment of humans suffering from hyperlipidemia which comprises administering, by a pharmaceutically effective mode, a drug composition selected from the group consisting of opiate antagonists, and drugs which substantially equally reduce the amounts of catecholamines bound to all catecholamine binding sites, is disclosed.
Abstract: This invention relates to a lubricating composition comprising a major amount of an oil of lubricating viscosity and (A) a minor amount of at least one hydroxyalkyl dithiocarbamate or at least one borate thereof, wherein the dithiocarbamate is derived from an amine other than an alkyl or alkenylsuccinimide. In another aspect the invention relates to a lubricating composition comprising a major amount of an oil of lubricating viscosity, a hydroxyalkyl dithiocarbamate or a borate thereof, and (B) at least one sulfur compound or (C) at least one phosphorus or boron antiwear or extreme pressure agent. The invention also relates to greases, functional fluids and aqueous fluids containing the hydroxyalkyl dithiocarbamates and borates thereof. The lubricants and fluids have improved antiwear and extreme pressure properties including providing improved antiscuff protection.
Type:
Grant
Filed:
August 23, 1996
Date of Patent:
December 16, 1997
Assignee:
The Lubrizol Corporation
Inventors:
Carmen V. Luciani, Syed Q. A. Rizvi, Bernard C. Roell, Jr.
Abstract: Salt compositions are disclosed which comprise: (A) at least one salt moiety derived from: A) at least one salt moiety derived from (A)(I) at least one high-molecular weight polycarboxylic acylating agent, said acylating agent (A)(I) having at least one hydrocarbyl substituent having an average of from about 20 to about 500 carbon atoms, and (A)(II) ammonia, at least one amine, at least one alkali or alkaline earth metal, and/or at least one alkali or alkaline earth metal compound;(B) at least one salt moiety derived from (B)(I) at least one low-molecular weight polycarboxylic acylating agent, said acylating agent (B)(I) optionally having at least one hydrocarbyl substituent having an average of up to about 18 carbon atoms, and (B)(II) ammonia, at least one amine, at least one alkali or alkaline earth metal, and/or at least one alkali or alkaline earth metal compound;said components (A) and (B) being coupled together by (C) at least one compound having (i) two or more primary amino groups, (ii) two or more se
Abstract: A process for preparing an amide of a bis (hydrocarbyl substituted hydroxyaryl) acetic acid by reacting a lactone produced in the reaction between the glyoxylic acid and phenol with a polyamine in the presence of an alcohol solvent is disclosed.
Type:
Grant
Filed:
September 27, 1996
Date of Patent:
May 13, 1997
Assignee:
The Lubrizol Corporation
Inventors:
Richard M. Lange, Mark R. Baker, Stephen H. Stoldt