Oxygen Bonded Directly At The 6- Or 7-position Patents (Class 552/542)
-
Patent number: 10246483Abstract: The present invention provides compounds of Formula I: pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.Type: GrantFiled: February 11, 2016Date of Patent: April 2, 2019Assignee: ENANTA PHARMACEUTICALS, INC.Inventors: Ruichao Shen, Yat Sun Or, Guoqiang Wang
-
Publication number: 20150140059Abstract: This invention relates, e.g., to a synthetic compound, Oxy149, having the structure (Formula I) or a bioactive or pharmaceutical composition comprising Oxy149 and a pharmaceutically acceptable carrier. Methods are also disclosed for using the compound or bioactive or pharmaceutical composition to treat a variety of disorders, including e.g. bone disorders, obesity, cardiovascular disorders, and neurological disorders. Oxy149 can be delivered either locally or systemically.Type: ApplicationFiled: March 15, 2013Publication date: May 21, 2015Inventors: Farhad Parhami, Michael Jung, Frank Stappenbeck, William Pierce, K. Grant Taylor, Kevyn E. Merten
-
Publication number: 20150118277Abstract: This invention relates, e.g., to a synthetic compound, Oxy133, having the structure [Formula I] or a bioactive or pharmaceutical composition comprising Oxy133 and a pharmaceutically acceptable carrier. Methods are also disclosed for using the compound or bioactive or pharmaceutical composition to treat a variety of disorders, including e.g. bone disorders, obesity, cardiovascular disorders, and neurological disorders.Type: ApplicationFiled: March 15, 2013Publication date: April 30, 2015Inventors: Farhad Parhami, Michael E. Jung, Frank Stappenbeck
-
Publication number: 20150086615Abstract: Novel sterol derivatives, the preparation method thereof, pharmaceutical compositions containing them and use thereof for treating diseases involving transformed astrocyte cells or for treating malignant haemopathies. The treatment of glioblastoma multiforme, as well as of other cancers, such as lymphomas, neuroblastomas and melanomas is also described.Type: ApplicationFiled: May 7, 2013Publication date: March 26, 2015Applicant: BETA INNOVInventors: Ludovic Clarion, Marcel Mersel, Didier Petite
-
Publication number: 20140364405Abstract: A method for the treatment of seborrhoea in a patient comprises administering to the patient an effective amount of (24RS) or (24S) scymnol, an ester thereof or a pharmaceutically acceptable salt of a said ester, or of (24R) scymnol.Type: ApplicationFiled: December 14, 2012Publication date: December 11, 2014Applicant: MCFARLANE MARKETING (AUST.) PTY. LTD.Inventors: Theodore Macrides, Andrew Broadbent
-
Publication number: 20140349866Abstract: Methods are described for using genes crucial in TH17 differentiation, IL-12Rbeta 1/IL-23R, CCR6, BATF, AHR, STAT3 and IRF4 as new markers for rosacea. Also described, are methods of their use to diagnose rosacea, to screen inhibitors of Th17 differentiation. In particular, method are described for inhibiting at least one of these genes and using the screened inhibitors in rosacea treatment.Type: ApplicationFiled: June 25, 2012Publication date: November 27, 2014Applicant: GALDERMA RESEARCH & DEVELOPMENTInventor: Martin Steinhoff
-
Publication number: 20140094443Abstract: The invention relates to compounds of Formula A: or a pharmaceutically acceptable salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including obesity, insulin sensitivity, inflammation, cholestasis, and bile desaturation.Type: ApplicationFiled: April 1, 2013Publication date: April 3, 2014Applicant: INTERCEPT PHARMACEUTICALS, INC.Inventor: Intercept Pharmaceuticals, Inc.
-
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
-
Publication number: 20120258184Abstract: A neutral-fat-level-regulating agent, a cholesterol-level-regulating agent, a free-fatty-acid-level-regulating agent or an anti-obesity agent, including: at least one of protopanaxatriol, panaxatriol, protopanaxadiol and panaxadiol which are aglycons of dammarane-type saponins; and a hyperlipemia-ameliorating agent including: at least one of the neutral-fat-level-regulating agent, the cholesterol-level-regulating agent, the free-fatty-acid-level-regulating agent and the anti-obesity agent.Type: ApplicationFiled: June 20, 2012Publication date: October 11, 2012Applicant: Lion CorporationInventors: Hiroaki KAMBAYASHI, Kumiko KITAMURA, Hideaki IWASAKI
-
Publication number: 20120190871Abstract: Disclosed are the isolation, purification and analysis of the triterpenoid compositions (including ergostane and lanostane) in the fruiting body of Antrodia cinnamomea using HPLC and NMR, as well as the stereo structures and the amounts of the triterpenoid compositions. The cytotoxicity of triterpenoids is also revealed. Based on the aforementioned techniques, the presence and amounts of ergostane and lanostane in the drugs, healthcare food or other goods are able to be detected.Type: ApplicationFiled: January 17, 2012Publication date: July 26, 2012Applicant: KAOHSIUNG MEDICAL UNIVERSITYInventors: YANG-CHANG WU, FANG-RONG CHANG, MEI-CHIN LU, YING-CHI DU, TUNG-YING WU, YU-MING HSU
-
Publication number: 20110288061Abstract: The present invention relates to triterpenoid derivatives, benzenoid derivatives, and pharmaceutical compositions containing the same for treating cancers or inflammatory symptoms. According to the present invention, the triterpenoid derivatives and the benzenoid derivatives are respectively represented by the following formulas (I) and (II): wherein, R1, R2, R3, R4, R5, R6, R7, R8, R1?, R2?, R3?, and R4? are defined the same as the specification.Type: ApplicationFiled: May 18, 2011Publication date: November 24, 2011Applicant: National Cheng Kung UniversityInventor: Tian-Shung Wu
-
Publication number: 20110152208Abstract: The present invention disclosed a medical use of cucurbitane triterpenoids represented by the following formula and isolated from Momordica charantia L. of Cucurbitaceae family in the preparation of medications for prevention and treatment of diabetes and obesity. The above cucurbitane triterpenoids may be acted as a glucose uptake stimulator, an agonist for the translocation of glucose transporter 4(GLUT4) to the cell membrane, and an activator of adenosine monophosphate-activated protein kinase (AMPK). They may have potential for the prevention and treatment of diabetes and obesity.Type: ApplicationFiled: January 14, 2009Publication date: June 23, 2011Applicants: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, The Garvan Institute of Medical Research, AustraliaInventors: Yang Ye, David E. James, Minjia Tan, Gregory J. Cooney, Changqiang Ke, Edward W. Kraegen, Tong Chen, Jiming Ye, Xiqiang Li
-
Publication number: 20110009615Abstract: An object of the present invention is to provide a novel method for producing a steroid compound. The present invention provides a method for producing 3,7-dioxo-5?-cholanic acid or ester derivatives thereof, which uses, as raw materials, sterols having double bonds at positions 5 and 24, such as cholesta-5,7,24-trien-3?-ol, ergosta-5,7,24(28)-trien-3?-ol, desmosterol, fucosterol, or ergosta-5,24(28)-dien-3?-ol, and which comprises the following 4 steps: (I) a step of performing oxidation of a hydroxyl group at position 3 and isomerization of a double bond at position 5 to position 4; (II) a step of converting position 24 to a carboxyl group or an ester derivative thereof by the oxidative cleavage of a side chain; (III) a step of introducing an oxygen functional group into position 7; and (IV) a step of constructing a 5?-configuration by reduction of a double bond at position 4.Type: ApplicationFiled: June 30, 2010Publication date: January 13, 2011Applicant: MITSUBISHI CHEMICAL GROUP SCIENCE AND TECHNOLOGY RESEARCH CENTER, INC.Inventors: Jun Takehara, Naoya Fujiwara, Junya Kawai, Kyouko Endou, Kiyoshi Ooyama
-
Publication number: 20100204460Abstract: The present invention relates to natural brassinosteroids of general formula (I), wherein R is CH2 or O—CH2 group, R2 is hydrogen or hydroxyl, R3 is hydroxyl, R24 is alkyl or alkenyl, which are selected from the group consisting of methyl, ethyl, propyl, isopropyl, methylen, ethylen and propylen, and R25 is alkyl selected from the group consisting of methyl and ethyl, and a pharmaceutically acceptable salt thereof, for use for treating hyperproliferation, treating proliferative diseases and reducing adverse effects of steroid dysfunction in mammals. The present invention also provides methods capable to arrest of the cell cycle by natural brassinosteroids resulting in apoptotic changes in cancer cells. More specifically, the present invention relates to use for treatment of the adverse effects of hyperproliferation on mammalian cells in vitro and in vivo, especially treatment of hyperproliferative diseases in mammals by administering compositions containing natural brassinosteroids.Type: ApplicationFiled: August 20, 2008Publication date: August 12, 2010Inventors: Jana Oklestková, Lucie Hoffmannová, Jana Steigerová, Ladislav Kohout, Zdenêk Kolár, Miroslav Strnad
-
Publication number: 20100152150Abstract: The application of marine steroid, i.e. 24-methylene-cholest-3?,5?,6?,19-tetrol, in preparing the medicine of treating neurons damaging is provided in the present invention. The keto-sterols compounds marine steroid YC-1 extracted from Nephthea albida has the action of neuronal protection, and no toxic reaction under the effective protective dosage.Type: ApplicationFiled: August 31, 2006Publication date: June 17, 2010Inventors: Guangmei Yan, Pengxin Qiu, Yijun Huang, Wei Yin, Xingwen Su, Ailing Liu, Hanfel Sang, Xiang Cai
-
Patent number: 7678782Abstract: Disclosed are methods for providing enhanced systemic blood concentrations of orally delivered drugs that are incompletely translocated across the intestinal wall of an animal. Also disclosed are methods for the sustained release of drugs, whether poorly or readily bioavailable via oral delivery to animals. Still further, disclosed are compounds and pharmaceutical compositions that are used in such methods.Type: GrantFiled: July 11, 2006Date of Patent: March 16, 2010Assignee: XenoPort, Inc.Inventors: Mark A. Gallop, Kenneth C. Cundy
-
Publication number: 20090274978Abstract: Photoacid generators generate sulfonic acids of formula (1a) or (1b) upon exposure to high-energy radiation. R1—COOCH2CF2SO3?H+??(1a) R1—O—COOCH2CF2SO3?H+??(1b) R1 is a monovalent C20-C50 hydrocarbon group of steroid structure which may contain a heteroatom. The bulky steroid structure ensures adequate control of acid diffusion. The photoacid generators are compatible with resins and suited for use in chemically amplified resist compositions.Type: ApplicationFiled: April 30, 2009Publication date: November 5, 2009Inventors: Masaki OHASHI, Youichi Ohsawa, Takeshi Kinsho, Takeru Watanabe
-
Publication number: 20090093638Abstract: The present invention relates to compositions and methods for achieving the efficient allylic oxidation of organic molecules, especially olefins and steroids, under aqueous conditions. The invention concerns the use of dirhodium (II,II) “paddlewheel complexes, and in particular, dirhodium carboximate and tert-butyl hydroperoxide as catalysts for the reaction. The use of aqueous conditions is particularly advantageous in the allylic oxidation of 7-keto steroids, which could not be effectively oxidized using anhydrous methods, and in extending allylic oxidation to enamides and enol ethers.Type: ApplicationFiled: October 6, 2008Publication date: April 9, 2009Applicant: UNIVERSITY OF MARYLAND, COLLEGE PARKInventors: Michael P. Doyle, Arthur J. Catino, Hojae Choi, Jason M. Nichols
-
Patent number: 7067682Abstract: Steroid compounds having various oxygen substitution on the steroid nucleus are disclosed. A specific functionality present on many of the steroid compounds is oxygen substitution at both of positions 6 and 7. Thus, certain steroids have oxygen substitution at C6 and C7, and some have specific stereochemistries such as 6? and 7? oxygen substitution, and an alpha hydrogen at the 5 position in addition to having 6? and 7? oxygen substitution. Steroids having 3,4-epoxy functionality are also disclosed. In addition, steroids having C17 pyran and ?-lactone functionality, with oxygen substitution at C6 and C7, or at C15, of the steroid nucleus, are disclosed.Type: GrantFiled: November 6, 2003Date of Patent: June 27, 2006Assignees: Inflazyme Pharmaceuticals Ltd., The University of British Columbia, The University of AlbertaInventors: David L. Burgoyne, Yaping Shen, John M. Langlands, Christine Rogers, Joseph H L Chau, Edward Piers, Hassan Salari
-
Patent number: 7012069Abstract: A compound of formula (I): Each of R1, R2, R3, R4, R4?, R5, R6, R7, R11, R12, R15, R16, and R17, independently, is hydrogen, halo, alkyl, haloalkyl, hydroxy, amino, carboxyl, oxo, sulfonic acid, or alkyl that is optionally inserted with —NH—, —N(alkyl)—, —O—, —S—, —SO—, —SO2—, —O—SO2—, —SO2—O—, —SO3—O—, —CO—, —CO—O—, —O—CO—, —CO—NR?—, or —NR?—CO—; or R3 and R4 together, R4 and R5 together, R5 and R6 together, or R6 and R7 together are eliminated so that a C?C bond is formed between the carbons to which they are attached; each of R8, R9, R10, R13, and R14, independently, is hydrogen, halo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, or amino; n is 0, 1, or 2; A is alkylene, alkenylene, or alkynylene; and each of X, Y, and Z, independently, is alkyl, haloalkyl, —OR?, —SR?, —NR?R?, —N(OR?)R?, or —N(SR?)R?; or X and Y together are ?O, ?S, or ?NR?; wherein each of R? and R?, independently, is hydrogen, alkyl, or haloalkyl.Type: GrantFiled: May 2, 2002Date of Patent: March 14, 2006Assignee: ARCH Development CorporationInventors: Ching Song, Shutsung Liao
-
Patent number: 6686486Abstract: A procedure for oxidizing organic compounds having allylic hydrogen atom(s) involving the steps of reactively contacting the organic compound with a combination of a periodic acid or metal periodate and an alkyl hydroperoxide under conditions of normal as well as elevated pressure of a suitable gas like air. The reaction can conveniently be conducted at temperatures between about 0-65° C. in a cosolvent system of water and organic solvent(s).Type: GrantFiled: August 14, 2000Date of Patent: February 3, 2004Inventors: Padma Marwah, Henry A. Lardy
-
Publication number: 20030171576Abstract: An efficient method for the synthesis of aminosterol compounds such as squalamine and compound 1436 is described. A method of the invention provides for regioselective oxidation and regioselective sulfonation of a fused ring system. The fused ring base can be, for example, a steroid ring base. The aminosterol compounds are effective as, for example, antibiotics, antiangiogenic agents and NHE3 inhibitors.Type: ApplicationFiled: October 11, 2002Publication date: September 11, 2003Inventors: William A. Kinney, Xuehai Zhang, Ronald Michalak
-
Patent number: 6605591Abstract: A method of treating an individual to increase the individual's bone mineral density (BMD) is disclosed. The method includes co-administering a calcitonin-like agent and a DHEA-like agent. Also disclosed are methods for potentiating the effect of treatment with a calcitonin-like agent on BMD and for increasing BMD in an individual being treated with DHEA, e.g., for treatment of systemic lupus erythematosus (SLE).Type: GrantFiled: November 10, 2000Date of Patent: August 12, 2003Assignee: Genelabs Technologies, Inc.Inventor: Kenneth E. Schwartz
-
Publication number: 20030139385Abstract: A method of treating a disorder related to a high cholesterol concentration, comprising administering to a subject in need thereof a compound of formula (I): 1Type: ApplicationFiled: November 8, 2002Publication date: July 24, 2003Inventors: Ching Song, Shutsung Liao
-
Patent number: 6555530Abstract: Analysis of full-blood glucose, serum insulin, serum triglycerides and total serum cholesterol were performed. Glucose levels in blood samples from the oral glucose tolerance test were used for calculation of the incremental Area Under the Curve (AUC0-120 min−baseline). All data are expressed as percentage change of vehicle treated animals (cf. FIGS. 1 and 2).Type: GrantFiled: January 31, 2000Date of Patent: April 29, 2003Assignee: Novo Nordisk A/SInventor: Karsten Wassermann
-
Patent number: 6423702Abstract: A pharmaceutical composition conatining at least one C3-OH ether or fatty acid monoester of 7B-hydroxycholesterol selected from the group consisting of the ethers or esters of palmitic, oleic, hexenoic, decenoic and arachindonic acids or esters. The composition is useful as a cytotoxic agent for the treatment on cells having a high proliferative potential.Type: GrantFiled: April 22, 1998Date of Patent: July 23, 2002Assignee: Centre National de la Recherche Scientifique (CNRS)Inventors: Patrick Behr, Alexandre Kupferberg, Marcel Mersel, Alain Privat
-
Patent number: 6388108Abstract: Newly isolated aminosterol compounds and pharmaceutical compositions based on the aminosterol compounds are described. Methods for the treatment of various disorders, for example, a microbial infection, are also described.Type: GrantFiled: May 29, 2001Date of Patent: May 14, 2002Assignee: Genaera CorporationInventors: Meena Rao, Binyamin Feibush, William Kinney, Michael Zasloff, Lincoln Noecker
-
Patent number: 6384251Abstract: A procedure for oxidizing organic compounds having allylic hydrogen atom(s) involving the steps of reactively contacting the organic compound with a combination of an N-hydroxy dicarboxylic acid imide and a chromium-containing oxidant. The reaction can conveniently be conducted under ambient temperature and pressure conditions, and is conveniently conducted in a co-solvent system of water and organic solvent(s).Type: GrantFiled: November 8, 1999Date of Patent: May 7, 2002Assignee: Humanetics CorporationInventors: Padma Marwah, Henry A. Lardy
-
Patent number: 6369247Abstract: The instant invention involves a process for oxidizing compounds containing an allylic group, i.e. those containing an allylic hydrogen or allylic alcohol group, to the corresponding enones, using a ruthenium-based catalyst in the presence of a hydroperoxide. Particularly, &Dgr;-5-steroidal alkenes can be oxidized to the corresponding &Dgr;-5-7-keto alkenes.Type: GrantFiled: September 30, 1996Date of Patent: April 9, 2002Assignee: Merck & Co., Inc.Inventors: Ross A. Miller, Andrew S. Thompson, Raman K. Bakshi, Edward G. Corley
-
Publication number: 20020007079Abstract: Certain novel sterol derivatives having no hydroxy group in the 3-position can be used to regulate the meiosis in oocytes and in male germ cells. Some of these compounds are useful in the treatment of infertility, whereas other compounds are useful as contraceptives.Type: ApplicationFiled: July 9, 1999Publication date: January 17, 2002Inventors: ANTHONY MURRAY, PETER FAARUP
-
Patent number: 6274746Abstract: The present invention is directed to a process for effecting the allylic oxidation of an allylic compound having at least two allylic hydrogen atoms on the same carbon atom into corresponding &agr;,&bgr;-unsaturated carbonyl compound, using a combination of a metal hypochlorite and an alkyl hydroperoxide in a mixture of suitable conventional organic solvent(s) and/or water at a temperature of between about −5° C. to +25° C.Type: GrantFiled: August 30, 2000Date of Patent: August 14, 2001Inventors: Padma Marwah, Henry A. Lardy, Ashok Kumar Marwah
-
Patent number: 6239073Abstract: Disclosed are compositions and methods for promoting plant growth. The compounds are cyclopropyl-, cyclobutyl-, and cyclopentyl-substituted brassinosteroids having high growth promoting ability. They may be used alone or in combination with other plant growth regulating agents.Type: GrantFiled: November 4, 1999Date of Patent: May 29, 2001Assignee: Exelixis Plant Sciences, Inc.Inventors: Thomas G. Back, Richard P. Pharis, Suanne K. Nakajima
-
Patent number: 6111118Abstract: A procedure for oxidizing organic compounds having allylic hydrogen atom(s) involving the steps of reactively contacting the organic compound with a combination of a periodic acid or metal periodate and an alkyl hydroperoxide under conditions of normal as well as elevated pressure of a suitable gas like air. The reaction can conveniently be conducted at temperatures between about 0-65.degree. C. in a cosolvent system of water and organic solvent(s).Type: GrantFiled: January 11, 1999Date of Patent: August 29, 2000Assignee: Humanetics CorporationInventors: Padma Marwah, Henry A. Lardy
-
Patent number: 6063731Abstract: Disclosed are compositions and methods for promoting plant growth. The compounds are cyclopropyl- and cyclobutyl-substituted brassinosteroids having high growth promoting ability. They may be used alone or in combination with other plant growth regulating agents.Type: GrantFiled: March 30, 1999Date of Patent: May 16, 2000Assignee: Agritope, Inc.Inventors: Thomas G. Back, Richard P. Pharis, Suanne K. Nakajima
-
Patent number: 5869709Abstract: A procedure for oxidizing organic compounds having allylic hydrogen atom(s) involving the steps of reactively contacting the organic compound with a combination of an alkali metal periodate and an alkyl hydroperoxide. The reaction can conveniently be conducted under ambient temperature and pressure conditions, and is conveniently conducted in a cosolvent system of water and organic solvent(s).Type: GrantFiled: May 7, 1997Date of Patent: February 9, 1999Assignee: Humanetics CorporationInventors: Padma Marwah, Henry A. Lardy
-
Patent number: 5834452Abstract: A compound of the formula ##STR1## having progestomimetic activity, wherein the substituents are as defined in the specification and compositions of a compound of formula I and an estrogen compound.Type: GrantFiled: May 22, 1997Date of Patent: November 10, 1998Assignee: Roussel UclafInventors: Jacques Biton, Jean-Pierre Marchandeau, Robert Azerad, Isabelle Lacroix
-
Patent number: 5710143Abstract: Disclosed are anti-obesity agents comprising 3-ketosteroidal compounds as defined in the specification. The present invention also discloses pharmaceutical compositions and use of these compounds in the prevention and treatment of obesity.Type: GrantFiled: March 27, 1996Date of Patent: January 20, 1998Assignee: Institute of Physical and Chemical ResearchInventors: Kunio Suzuki, Tadashi Nakata, Takeshi Shimizu, Kotaro Enomoto
-
Patent number: 5637691Abstract: Compounds having a broad range of antimicrobial activity generally have a structure including asteroid nucleus with a cationic, preferably polyamine, side chain (X) and an anionic side chain (Y). The invention is also directed to compounds of the Formula III: ##STR1## preferably where the steroid ring nucleus is saturated; the steroid ring substituent Z.sub.5 is .alpha.-H; one Z.sub.7 is .beta.-H and the other is .alpha.-H or .alpha.-OH; both substituents Z.sub.12 are hydrogen; X' is a polyamine side chain of the formula --NH--(CH.sub.2).sub.p --NH--(CH.sub.2).sub.q --N(R.sup.II)(R.sup.III) where p and q are each independently 3 or 4, and R.sup.II and R.sup.III are each independently hydrogen or methyl; R' is methyl; and Y' is (C.sub.1 -C.sub.10)-alkyl substituted with a group such as --CO.sub.2 H or --SO.sub.3 H.Type: GrantFiled: August 18, 1994Date of Patent: June 10, 1997Assignee: Magainin Pharmaceuticals, Inc.Inventors: Leah L. Frye, Michael A. Zasloff, William A. Kinney, Robert Moriarty
-
Patent number: 5632997Abstract: A compound of general formula, in substantially pure form, wherein A is a cation. A method for preparation is also disclosed, together with compositions and methods of use thereof. The active principle, isolated from shark tissue, is used for treating liver disfunction, or protecting liver function, in mammals.Type: GrantFiled: June 6, 1995Date of Patent: May 27, 1997Assignee: J. W. Broadbent Nominees Pty. Ltd.Inventors: Takuo Kosuge, Kuniro Tsuji, Hitoshi Ishida, Yoshiki Kosuge
-
Patent number: 5591733Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.Type: GrantFiled: August 2, 1993Date of Patent: January 7, 1997Assignee: University of Southern CaliforniaInventors: Michael B. Bolger, Kelvin W. Gee, Nancy C. Lan, Robert H. Purdy, Seid Mirsadeghi, Syed Hasan Tahir, Delia Belelli
-
Patent number: 5541348Abstract: Novel bile acids according to the general formula ##STR1## wherein R.sub.1 represents a hydroxyl group, R.sub.2 and R.sub.3 both represent a hydrogen or a hydroxyl group, or R.sub.2 represents a hydroxyl group or a .beta. hydroxyl group and R.sub.3 represents a hydrogen or R.sub.3 represents a hydroxyl group and R.sub.2 represents a hydrogen, and R.sub.4 represents a (CH.sub.2).sub.n R.sub.5 wherein n is from 1 to 6, and R.sub.5 represents --0--PO(OH).sub.2, --CH(OH)COOH, a nitrogen containing saturated heterocyclic ring group, NR.sub.6 R.sub.7, wherein R.sub.6 and R.sub.7 are the same or different and each represent hydrogen or a C.sub.1 -C.sub.10 alkyl group or CO--R.sub.8 wherein R.sub.8 represents an amino acid moiety, R-phenylglycine, 12-aminododecanoic acid or 4-aminohippuric acid are synthesized from cholic, deoxycholic, chenodeoxycholic, ursodeoxycholic and lithocholic acids and iodo-derivatives thereof by known processes and/or by novel processes according to the present invention.Type: GrantFiled: March 10, 1994Date of Patent: July 30, 1996Assignee: National Research Council of CanadaInventors: Prabhat Ayra, Graham W. Burton
-
Patent number: 5470574Abstract: A compound of general formula, in substantially pure form, wherein A is a cation. A method for preparation is also disclosed, together with compositions and methods of use thereof.Type: GrantFiled: December 20, 1993Date of Patent: November 28, 1995Assignee: J. W. Broadbent Nominees Pty. Ltd.Inventors: Takuo Kosuge, Kuniro Tsuji, Hitoshi Ishida, Yoshiki Kosuge
-
Patent number: 5451575Abstract: The present invention relates to 24R-scymnol, including its preparation in substantially pure form and to its use in the treatment of liver dysfunction.Type: GrantFiled: December 30, 1993Date of Patent: September 19, 1995Assignee: J. W. Broadbent Nominees Pty., Ltd.Inventors: Yoshiki Kosuge, Takuo Kosuge, Kuniro Tsuji, Hitoshi Ishida
-
Patent number: 5359055Abstract: There are provided pregnane derivatives represented by formula ##STR1## wherein A.sup.1 represents a hydrogen atom or a hydroxyl group, A.sup.2 represents a substituent such as a hydroxyl group when A.sup.1 represents a hydrogen atom, or A.sup.2 represents a hydrogen atom when A.sup.1 represents a hydroxyl group, or A.sup.1 and A.sup.2 are combined together to form an oxo group; D.sup.1 represents a substituent such as a hydroxyl group, and D.sup.2 represents a hydrogen atom, or D.sup.1 and D.sup.2 are combined together to form an epoxy group or a single bond; D.sup.3, D.sup.5 and D.sup.7 each represents a hydrogen atom, D.sup.4 represents a hydroxyl group, and D.sup.6 represents a substituent such as a hydroxyl group, or D.sup.3 and D.sup.4 may be combined together to form an epoxy group or a single bond, or D.sup.4 and D.sup.5 may be combined together to form a single bond, or D.sup.5 and D.sup.6 may be combined together to form an epoxy group or a single bond, or D.sup.6 and D.sup.Type: GrantFiled: November 27, 1991Date of Patent: October 25, 1994Assignee: Kuraray Co., Ltd.Inventors: Jiro Tsuji, Takashi Takahashi, Masao Tsuji, Naoshi Nakagawa, Tetsuo Takigawa
-
Patent number: 5264599Abstract: A process is provided for treating an edible animal fat to reduce the content of components having free hydroxyl groups. The process comprises forming a reaction mixture from the fat and a cyclic anhydride such as succinic or glutaric anhydride, heating the mixture to a temperature promoting conversion of these components to hemisuccinates or hemiglutarates, and subjecting the reacted fat to alkali-refining to remove the converted components as water-soluble soaps. The process is particularly useful for reducing the cholesterol content of the animal fats.Type: GrantFiled: November 8, 1991Date of Patent: November 23, 1993Assignee: Iowa State University Research FoundationInventors: Earl G. Hammond, Ying Chen
-
Patent number: 5210315Abstract: A process for producing an .alpha.-hydroxyketone represented by formula (I): ##STR1## wherein R.sup.1 represents a substituted or unsubstituted alkyl group, a substituted or unsubstituted aralkyl group, or an alkoxycarbonyl group; and R.sup.2 and R.sup.3 each represent a hydrogen atom, a substituted or unsubstituted alkyl group, or a substituted or unsubstituted aralkyl group, provided that they do not simultaneously represent a hydrogen atom; or a pair of R.sup.1 and R.sup.2, a pair of R.sup.1 and R.sup.3, or a pair of R.sup.2 and R.sup.3 is taken together to form a ring; and the pair of R.sup.1 and R.sup.2 and the pair of R.sup.2 and R.sup.3 may form a ring simultaneously, is disclosed, comprising reacting a compound represented by formula (II): ##STR2## wherein R.sup.1, R.sup.2, and R.sup.3 are as defined above, with an oxidizing agent in the presence of a ruthenium compound and water. .alpha.-Hydroxyketones useful as physiologically active substances are produced with good selectivity and in high yield.Type: GrantFiled: October 18, 1991Date of Patent: May 11, 1993Assignee: Takasago International CorporationInventors: Takao Saito, Hidenori Kumobayashi, Shunichi Murahashi
-
Patent number: 5166374Abstract: Compounds of general formula I ##STR1## wherein R.sub.1 is hydrogen or hydroxy, and the hydroxy group at the 7-position can be either in .alpha. or .beta. configuration, are valuable in human therapy. Compounds I can be prepared by reacting with succinic acid carboanions the corresponding derivatives which have previously been protected, and subsequently deprotecting and decarboxylating them.Type: GrantFiled: September 18, 1991Date of Patent: November 24, 1992Assignee: Giuliani S.p.A.Inventors: Roberto Pellicciari, Aldo Roda, Giuliano Frigerio
-
Patent number: 5096898Abstract: Bile acid derivatives of formula I ##STR1## wherein: R is hydrogen or hydroxy;X is a carboxy or a SO.sub.3 H group, have valuable pharmacologic properties.Type: GrantFiled: February 5, 1991Date of Patent: March 17, 1992Assignee: Giuliani S.p.A.Inventors: Roberto Pellicciari, Aldo Roda
-
Patent number: 5057509Abstract: Compounds of general formula I ##STR1## wherein R.sub.1 is hydrogen or hydroxy, and the hydroxy group at the 7-position can be either in .alpha. or .beta. configuration, are valuable in human therapy. Compounds I can be prepared by reacting with succinic acid carbonanions the corresponding derivatives which have previously been protected, and subsequently deprotecting and decarboxylating them.Type: GrantFiled: April 9, 1990Date of Patent: October 15, 1991Assignee: Giuliani S.p.A.Inventors: Roberto Pellicciari, Aldo Roda, Giuliano Frigerio
-
Patent number: RE35517Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.Type: GrantFiled: November 23, 1992Date of Patent: May 20, 1997Assignee: University of Southern CaliforniaInventors: Kelvin W. Gee, Michael B. Bolger, Nancy C. Lan