The Oxygen Is Bonded Directly To A Ring Patents (Class 544/173)
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Patent number: 7166600Abstract: The invention provides novel thiocarbamate alpha-4 inhibitors of the general formula (I) that are resistant to metabolism having improved half-life and/or clearance properties compared to corresponding carbamate compounds wherein substituents L, X, Y, Z, R1–R4, m, n, o and p are as defined herein. Also provided are compositions comprising compounds of formula I and a carrier, diluent or excipient as well as methods of treating a disease or condition mediated by the binding interaction of alpha-4 integrins to its ligands such as inflammatory diseases.Type: GrantFiled: January 11, 2006Date of Patent: January 23, 2007Assignee: Genentech, Inc.Inventor: David Y. Jackson
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Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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Patent number: 7015323Abstract: The invention provides novel thiocarbamate alpha-4 inhibitors of the general formula (I) that are resistant to metabolism having improved half-life and/or clearance properties compared to corresponding carbamate compounds wherein substituents L, X, Y, Z, R1–R4, m, n, o and p are as defined herein. Also provided are compositions comprising compounds of formula I and a carrier, diluent or excipient as well as methods of treating a disease or condition mediated by the binding interaction of alpha-4 integrins to its ligands such as inflammatory diseases.Type: GrantFiled: May 19, 2004Date of Patent: March 21, 2006Assignee: Genentech, Inc.Inventor: David Y. Jackson
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Patent number: 6998400Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol and pharmaceutically acceptable salts and solvates thereof, pharmaceutical compositions comprising them, and processes for their preparation; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, pain, sexual dysfunction, Parkinson's disease, Alzheimer's disease, addiction to cocaine or tobacco products, seasonal affective disorder, chronic fatigue, narcolepsy or cognitive impairment using such compound, salts, solvates or compositions.Type: GrantFiled: May 17, 2002Date of Patent: February 14, 2006Assignee: Smithkline Beecham CorporationInventors: John A. Ascher, Joseph Andrews Johnston, Susan Marie Learned-Coughlin, Alan Bye
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Patent number: 6855820Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol and pharmaceutically acceptable salts and solvates thereof, methods for preparing them, pharmaceutical compositions comprising them, and processes for their preparation; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, sexual dysfunction, Parkinson's disease, Alzheimer's disease, or addiction to cocaine or nicotine-containing (especially tobacco) products using such compound, salts, solvates or compositions.Type: GrantFiled: May 17, 2002Date of Patent: February 15, 2005Assignee: SmithKline Beecham CorporationInventors: Toby Broom, Monica Delpogetto, Richard Atkins, Alan Negus, Paul William Oxley
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Patent number: 6812244Abstract: The instant invention provides novel substituted naphthyl compounds, intermediates, compositions, pharmaceutical formulations, and methods of use.Type: GrantFiled: May 27, 2003Date of Patent: November 2, 2004Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones, Alan David Palkowitz
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Publication number: 20040192688Abstract: This invention relates to novel {overscore (&ohgr;)}-substituted-naphthyloxy-amino alkanes, their preparation and use as antihyperglycemic agents and for the treatment and prevention of cardiovascular disorders (CVS) such as lipid lowering effects.Type: ApplicationFiled: October 27, 2003Publication date: September 30, 2004Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Devdutt Chaturvedi, Atul Kumar, Reema Rastogi, Arvind Srivastava, Priti Tewari, Rehan Ahmad, Ramesh Chander, Anju Puri, Geetika Bhatia, Farhan Rizvi, Anil Kumar Rastogi, Suprabhat Ray
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Patent number: 6787543Abstract: A compound of the formula (I): in which Z, R1, R2, R8, R10, R11, R12, R13 and R14 are each as defined in the description, or a salt thereof. The object compound of the present invention has pharmacological activities such as Tachykinin antagonism, and is useful for manufacture of a medicament for treating or preventing Tachykinin-mediated diseases.Type: GrantFiled: December 20, 2002Date of Patent: September 7, 2004Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kazuhiko Take, Chiyoshi Kasahara, Shinji Shigenaga, Hidenori Azami, Yoshiteru Eikyu, Kazuo Nakai, Masataka Morita
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Patent number: 6784175Abstract: The use of at least one substituted 1-amino-5-phenylpentane-3-ol and/or 1-amino-6-phenylhexane-3-ol compound and/or one of the enantiomers thereof and/or one of the diastereomers thereof and/or one of the physiologically acceptable salts thereof for producing a medicament that has an N-methyl-D-aspartate-(NMDA)-antagonistic effect.Type: GrantFiled: November 18, 2002Date of Patent: August 31, 2004Assignee: Gruenenthal GmbHInventors: Bernd Sundermann, Werner Englberger, Boris Chizh
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Patent number: 6749988Abstract: Novel amine compounds having a nitrogen-containing cyclic structure and a hydrating group such as a hydroxy, ether, ester, carbonyl, carbonate group or lactone ring are useful for use in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.Type: GrantFiled: November 28, 2001Date of Patent: June 15, 2004Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Jun Hatakeyama, Tomohiro Kobayashi, Takeru Watanabe, Takeshi Nagata
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Patent number: 6734213Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol and pharmaceutically acceptable salts and solvates thereof, pharmaceutical compositions comprising them, and processes for their preparation; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, pain, sexual dysfunction, Parkinson's disease, Alzheimer's disease, addiction to cocaine or nicotine-containing (especially tobacco) products, or addiction to alcohol using such compound, salts, solvates or compositions.Type: GrantFiled: May 17, 2002Date of Patent: May 11, 2004Assignee: Smithkline Beecham CorporationInventor: John Joseph Partridge
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Patent number: 6677338Abstract: The present invention relates to the therapeutic use of non-amine tropane analogues that bind to the SERT to treat neuropsychiatric disorders.Type: GrantFiled: February 28, 2002Date of Patent: January 13, 2004Assignees: President and Fellows of Harvard College, Organix, Inc.Inventors: Bertha K. Madras, Peter C. Meltzer
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Patent number: 6656936Abstract: Acylcarnitine analogues having alkyl side chains of 10 to 30 carbon atoms display excellent spermicidal and anti-HIV activity, a well as being potent inhibitors of the growth of Candida albicans.Type: GrantFiled: July 5, 2002Date of Patent: December 2, 2003Assignee: Virginia Tech Intellectual Properties, Inc.Inventors: Prashant S. Savle, Richard D. Gandour, Gustavo F. Doncel
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Patent number: 6638930Abstract: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: April 17, 2001Date of Patent: October 28, 2003Assignee: Merck & Co. Inc.Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
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Patent number: 6562815Abstract: The invention relates to new compounds containing 1-8 active groups of the type 3,3,6,6-polysubstituted 2-morpholinone and having the formula F (A′—Z)m—X (F), wherein m is a number from 1 to 8; X is an organic anchor group of valency m and in case that m is not 1, X may also be a direct bond, SO2, P or PO; A′ is a monovalent group of the formula E containing one linking group; Z is a direct bond, —O—, —S—, —SO—, —SO2— or —NR′14—; provided that Z is —O—, —S—, —SO—, —SO2— or —NR′14— if m is 1 and the linking group in formula E is G3 or G5; G1 is hydrogen; C1-C18alkyl; C2-C18alkyl substituted by OH and/or phenyl; oxyl; OH; C2-C12cyanoalkyl; C2-C12cyanoalkoxy; C1-C18alkoxy; C5-C12cycloalkoxy; C3-C8alkenyl; C3-C8alkynyl; C3-C8alkenyloxy; C7-C12phenylalkyl; C7-C12phenylalkyl substituted by hydroxy, C1-C4alkyl and/or C1-C4Type: GrantFiled: August 16, 2000Date of Patent: May 13, 2003Assignee: Ciba Specialty Chemicals CorporationInventors: Dario Lazzari, Thomas Bolle, Mirko Rossi, Hugh Stephen Laver
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Patent number: 6548679Abstract: The present invention provides compounds of general formula I or II: wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I or II, intermediates and processes useful for preparing compounds of formula I or II, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I or II.Type: GrantFiled: August 17, 2000Date of Patent: April 15, 2003Assignee: The Regents of the University of CaliforniaInventors: Trevor C. McMorris, Michael J. Kelner
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Patent number: 6538134Abstract: The present invention is concerned with 4-benzyl-2-hydroxy-1,4-oxazin-3-one, and novel processes for the preparation therof. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.Type: GrantFiled: June 8, 2001Date of Patent: March 25, 2003Assignee: Merck & Co., Inc.Inventors: Louis S. Crocker, Karel M. Jos Brands, Todd D. Nelson, Philip J. Pye, Jonathan D. Rosen, Kai Rossen
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Patent number: 6531471Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: December 14, 2001Date of Patent: March 11, 2003Assignee: Synaptic Pharmaceutical CorporationInventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
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Patent number: 6503905Abstract: The present invention relates to compounds of the formula I, wherein Z1, Z2, X, Q, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and gastrointestinal disorders.Type: GrantFiled: August 6, 1999Date of Patent: January 7, 2003Assignee: Pfizer IncInventors: Spiros Liras, Martin P. Allen, Barbara E. Segelstein
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Patent number: 6479491Abstract: The present invention relates to compounds of formula (I), any of it enantiomers, or any mixture thereof, or a pharmaceutically acceptable acid addition salt thereof, wherein R1, R2, R3, R4, R11, R12, R13, R14 and R15 each independently are hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, nitro, cyano, amino, acyl, alkylamino, dialkylamino, aminocarbonyl, or acylamino; R5 is hydrogen, alkyl, alkoxyalkyl, or phenylalkyl; X is —CH2—Z—, Z—CH2—, NH—CO—, —CO—NH—, or —CH═CH—; wherein Z is O, S, CH2, or NH; Y is O, —CH2—W—, —W—CH2—; wherein W is O, or S; and n is 0, 1 or 2. The compounds are useful in the treatment of psychotic disorders.Type: GrantFiled: November 13, 2000Date of Patent: November 12, 2002Assignee: Neurosearch A/SInventors: Oskar Axelsson, Dan Peters, Jorgen Scheel-Kruger, Elsebet Ostergaard Nielsen
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Patent number: 6362182Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: October 30, 2000Date of Patent: March 26, 2002Assignee: Synaptic Pharmaceutical CorporationInventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
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Patent number: 6362373Abstract: The disclosed invention comprises a compound having the formula: in which R1 and R2 independently represent a hydrogen or an alkyl group of 4 carbon atoms or greater. Further disclosed is a process for the preparation of the disclosed chiral amino alcohols from a starting amine compound and a limonene oxide.Type: GrantFiled: September 13, 2000Date of Patent: March 26, 2002Assignees: The Dow Chemical CompanyInventors: Christian T. Goralski, Bakthan Singaram, William Chrisman
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Patent number: 6218390Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: December 17, 1998Date of Patent: April 17, 2001Assignee: Synaptic Pharmaceutical CorporationInventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
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Patent number: 6200972Abstract: This invention relates to neurotrophic low molecular weight, small molecule heterocyclic esters and amides having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.Type: GrantFiled: February 23, 1998Date of Patent: March 13, 2001Assignee: GPI NIL Holdings, Inc.Inventors: Jia-He Li, Gregory S. Hamilton
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Patent number: 6140326Abstract: The invention relates to new compounds containing 1-8 active groups of the type 3,3,6,6-polysubstituted 2-morpholinone and having the formula F(A'--Z).sub.m --X (F),wherein m is a number from 1 to 8;X is an organic anchor group of valency m and in case that m is not 1, X may also be a direct bond, SO.sub.2, P or PO;A' is a monovalent group of the formula E ##STR1## containing one linking group; Z is a direct bond, --O--, --S--, --SO--, --SO.sub.2 -- or --NR'.sub.14 --; provided that Z is --O--, --S--, --SO--, --SO.sub.2 -- or --NR'.sub.14 -- if m is 1 and the linking group in formula E is G.sub.3 or G.sub.5 ;G.sub.1 is hydrogen; C.sub.1 -C.sub.18 alkyl; C.sub.2 -C.sub.18 alkyl substituted by OH and/or phenyl; oxyl; OH; C.sub.2 -C.sub.12 cyanoalkyl; C.sub.2 -C.sub.12 cyanoalkoxy; C.sub.1 -C.sub.18 alkoxy; C.sub.5 -C.sub.12 cycloalkoxy; C.sub.3 -C.sub.8 alkenyl; C.sub.3 -C.sub.8 alkynyl; C.sub.3 -C.sub.8 alkenyloxy; C.sub.7 -C.sub.12 phenylalkyl; C.sub.7 -C.sub.12 phenylalkyl substituted by hydroxy, C.sub.1 -C.Type: GrantFiled: September 14, 1998Date of Patent: October 31, 2000Assignee: Ciba Specialty Chemicals CorporationInventors: Dario Lazzari, Thomas Bolle, Mirko Rossi, Hugh Stephen Laver
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Patent number: 6136803Abstract: The present invention provides novel compounds such as certain aryloxy indanamines which are useful as anti-depressants and as inhibitors of synaptic norepinephrine and serotonin uptake. The present invention also provides an improvement in the treatment of depression which comprises inhibiting synaptic serotonin and epinepherine uptake.Type: GrantFiled: December 10, 1998Date of Patent: October 24, 2000Assignee: Merrell Pharmaceuticals Inc.Inventors: Jules Freedman, Mark W. Dudley
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Preparation of a mannich base intermediate for 2-[(4-heterocyclic-phenoxymethyl)-phenoxy]-alkanoates
Patent number: 6136972Abstract: A Mannich base intermediate for 2-[(4-heterocyclic-phenoxymethyl)-phenoxyl]-alkanoates and methods for its preparation are provided. A method for preparation of an alkyl 2-[2-(secondary amino methyl)-5-alkylphenoxy]-alkanoate comprises the steps of: reacting a mixture of m-alkyl phenol, a secondary amine, and an aldehyde, with or without a catalyst, in a first solvent at reflux temperatures to form a 2-[(secondary amino)methyl]-5-alkylphenol. That product is then reacted with an alkyl 2-haloalkanoate, and an alkali metal carbonate, with or without a second catalyst in a second solvent at reflux temperatures to form the 2-[2-(secondary amino methyl)-5-alkylphenoxy]-alkanoate. The aldehyde may be paraformaldehyde, aqueous formaldehyde, formaldehyde, or polymerized acetal derivatives thereof. The first solvent may be acetonitrile or toluene. The catalyst may be an acid catalyst or a base catalyst.Type: GrantFiled: February 22, 2000Date of Patent: October 24, 2000Assignee: FMC CorporationInventors: Gerard A. Crispino, Mark R. Diener -
Patent number: 6130331Abstract: The present invention relates to a process for the preparation of substantially pure N-((S)-(-)-.alpha.-methylbenzyl)-3-(S)-(4-fluorophenyl)-1,4-oxazin-2-one hydrochloride, which comprises selectively crystallising the (S,S)-diastereomer as the hydrochloride salt from a mixture of the (S,R)- and (S,S)-diastereomers in an organic solvent, and collecting the resultant crystalline product.Type: GrantFiled: September 8, 1999Date of Patent: October 10, 2000Assignee: Merck Sharp & Dohme Ltd.Inventors: Michael Stewart Ashwood, Ian Frank Cottrell, Brian Christopher Bishops, John Simon Edwards
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Patent number: 6090796Abstract: This invention is a pharmaceutical composition that inhibits the growth of cancers and tumors in mammals, particularly in human and warm blooded animals. The composition contains N-phosphonoglycine derivatives which are systemic herbicides in combination with chemotherapeutic agents for treatment of cancers and tumors. N-phosphonoglycine derivatives can be used to treat viral infections, particularly herpes infections. Optionally potentiators can be included.Type: GrantFiled: December 24, 1998Date of Patent: July 18, 2000Assignee: The Procter & Gamble CompanyInventor: James Berger Camden
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Patent number: 6046325Abstract: The present invention relates to a process for the preparation of a compound of formula (I): ##STR1## wherein R.sup.1 is a C.sub.1-6 alkyl or arylC.sub.1-4 alkyl group; and R.sup.2 is a hydrogen atom, a halogen atom, or a group selected from C.sub.1-6 alkyl, CF.sub.3 or C.sub.1-6 alkoxy substituted by C.sub.1-4 alkoxy; which comprises reacting an anhydrous or hydrated glyoxal of formula (II) with a compound of formula (III): ##STR2## in the presence of an acid.Type: GrantFiled: September 8, 1999Date of Patent: April 4, 2000Assignee: Merck Sharp & Dohme LimitedInventors: Michael Stewart Ashwood, Brian Christopher Bishop, Ian Frank Cottrell
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Patent number: 6020489Abstract: Water or lipid soluble, pharmacologically active, antioxidant, anti-phospholipase compounds that are chemically defined. The compounds protect mammalian cells by inhibiting PLA.sub.2 and preventing oxidation. In particular, each compound has at least two fatty moieties and no active hydroxy group. The compound may also have at least one ionizable group, which may be a carboxyl group, and each of the fatty moieties has from sixteen to twenty carbon atoms and at least one cis-unsaturated double bond.Type: GrantFiled: March 18, 1997Date of Patent: February 1, 2000Assignee: Virginia Commonwealth UniversityInventors: Richard C. Franson, Raphael M. Ottenbrite
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Patent number: 6015838Abstract: This invention provides aqueous film-forming foamable (AFFF) compositions comprising one or more environmentally-friendly .alpha.-branched fluoroalkylcarbonyl group-containing surfactants.Type: GrantFiled: November 4, 1996Date of Patent: January 18, 2000Assignee: 3M Innovative Properties CompanyInventors: Richard M. Stern, Wei-Qiang Fan
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Patent number: 5959103Abstract: The invention provides naphthofluorene compounds, intermediates, formulations, processes, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions, including hyperlipidemia, and estrogen-dependent cancer.Type: GrantFiled: September 30, 1998Date of Patent: September 28, 1999Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, Jeffrey Alan Dodge, Charles Willis Lugar, III
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Patent number: 5958917Abstract: The present invention provides compounds of formula I ##STR1## wherein R.sub.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.6 alkyl), --OCOO(C.sub.1 -C.sub.6 alkyl), --OCOAr, --OCOOAr, or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);R.sub.2 is --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.6 alkyl), --OCOO(C.sub.1 -C.sub.6 alkyl), --OCOAr, --OCOOAr, or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);R.sub.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; andn is 2 or 3;or a pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: September 24, 1997Date of Patent: September 28, 1999Assignee: Eli Lilly and CompanyInventors: Thomas Alan Crowell, Charles David Jones, Henry Uhlman Bryant
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Patent number: 5904818Abstract: The invention is concerned with a process for the production of a solution of N-methylmorpholine-N-oxide in water, characterized by the following steps:(a) providing an aqueous solution containing N-methylmorpholine and morpholine and exhibiting a pH value of from 6.0 to 9.0, thereafter(b) treating said aqueous solution with a peroxidic oxidant to oxidize N-methylmorpholine to N-methylmorpholine-N-oxide.Type: GrantFiled: April 17, 1997Date of Patent: May 18, 1999Assignee: Lenzing AktiengesellschaftInventors: Wolfram Kalt, Dieter Eichinger, Bruno Mangeng, Heinrich Firgo
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Patent number: 5889000Abstract: The invention provides naphthofluorene compounds, intermediates, formulations, processes, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions, including hyperlipidemia, and estrogen-dependent cancer.Type: GrantFiled: September 22, 1997Date of Patent: March 30, 1999Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, Jeffrey Alan Dodge, Charles Willis Lugar, III
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Patent number: 5869663Abstract: The invention relates to compounds of the formula ##STR1## in which: A is a divalent radical selected from:A.sub.1) --O--CO--A.sub.2) --CH.sub.2 --O--CO--A.sub.3) --O--CH.sub.2 --CO--A.sub.4) --O--CH.sub.2 --CH.sub.2 --A.sub.5) --N(R.sub.1)--CO--A.sub.6) --N(R.sub.1)--CO--CO--A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 --A.sub.8) --O--CH.sub.2 --in which:R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; andAm is a nitrogen-containing heterocycle.Type: GrantFiled: March 18, 1997Date of Patent: February 9, 1999Assignee: SanofiInventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5849801Abstract: 4-amino-5-oxy-2,6,6-tri methyl-2-cycloheptene compounds represented by the following general formula: ##STR1## (wherein R.sup.1 and R.sup.2 each independently represent a hydrogen atom, an alkyl group which may have a substituent, or a phenyl group which may have a hydroxyl group, lower alkoxy group, amino group, nitro group, carboxyl group, lower alkoxycarbonyl group or halogen atom, or R.sup.1, R.sup.2 and the nitrogen atom together represent a saturated nitrogen heterocyclic group; R.sup.3 represents a hydrogen atom, a lower alkyl group or a lower aliphatic acyl group); and W represents an oxo group, oxime group or oxime ether group; and their pharmacologically acceptable salts and solvates.The 4-amino-5-oxy-2,6,6-trimethyl-2-cycloheptene compounds exhibit an effect against rat peripheral arterial occlusion models, spontaneous hypertensive rats and histamine-induced airway contraction models, and are thus useful as remedy for hypertension, peripheral arterial occlusion and bronchial asthma.Type: GrantFiled: July 30, 1997Date of Patent: December 15, 1998Assignee: Tokyo Tanabe Company LimitedInventors: Susumu Yokura, Masao Yajima, Kiyokazu Murakami, Kouichi Matsunaga
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Patent number: 5847129Abstract: The invention is concerned with a process for the destruction of N-nitrosomorpholine in an aqueous solution containing N-nitrosomorpholine and a peroxidic oxidant, characterized in that said aqueous solution is exposed to ultraviolet radiation having a wavelength of substantially 254 nm.Type: GrantFiled: April 17, 1997Date of Patent: December 8, 1998Assignee: Lenzing AktiengesellschaftInventors: Peter Harfmann, Stephan Astegger
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Patent number: 5847213Abstract: There is provided a process for producing a tertiary amine compound in one step without using any subsidiary raw material or any solvent, by subjecting a secondary amine compound and an alcohol to an intermolecular dehydration reaction in a gas phase. The process uses, as a catalyst, an oxide containing an alkali metal element and/or an alkaline earth metal element and silicon.Type: GrantFiled: March 3, 1997Date of Patent: December 8, 1998Assignee: Nippon Shokubai Co., Ltd.Inventors: Akira Kurusu, Yuuji Shimasaki
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Patent number: 5847130Abstract: Aqueous solutions of N-methylmorpholine N-oxide having reduced nitrosamine concentrations are produced by adding catalytic amounts of inorganic carbonate or bicarbonate or carboxylic acid or carboxylate salt.Type: GrantFiled: August 4, 1997Date of Patent: December 8, 1998Assignee: BASF CorporationInventor: Mark Sandison
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Patent number: 5700761Abstract: Compounds of Formula I having herbicidal utility are disclosed: ##STR1## wherein Q, R.sup.1, R.sup.2, V, m and p are defined in the text, including compositions containing such compounds, and a method for controlling weeds employing such compounds.Type: GrantFiled: August 15, 1996Date of Patent: December 23, 1997Assignees: E. I. Du Pont de Nemours and Company, Degussa AktiengesellschaftInventor: John Jolly Kilama
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Patent number: 5693796Abstract: Aqueous solutions of N-methylmorpholine N-oxide having reduced nitrosamine concentrations are produced by adding catalytic amounts of inorganic carbonate or bicarbonate or carboxylic acid or carboxylate salt.Type: GrantFiled: August 14, 1996Date of Patent: December 2, 1997Assignee: BASF CorporationInventor: Mark Sandison
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Patent number: 5686586Abstract: A polycyclic aromatic compound having the formula ##STR1## and its salts have useful therapeutic and cosmetic action particularly in psoriasis.In the formula, X represents --CH.dbd.CH--, O or S,R.sub.1 represents hydrogen, branched alkyl having 3-15 carbon atoms, alkoxy having 1-6 carbon atoms or 1-adamantyl, R.sub.2 represents hydroxy, hydrogen, linear or branched alkyl having 1-15 carbon atoms or alkoxy having 1-6 carbon atoms, with the proviso that R.sub.1 and R.sub.2 are not simultaneously hydrogen, or R.sub.1 and R.sub.2 together with the adjacent carbon atoms of the naphthalene ring form a 5 or 6 chain ring optionally substituted by at least one lower alkyl radical, or interrupted by an oxygen atom,R.sub.3 represents --CH.sub.2 OH or --COR.sub.4, or --CH.sub.3 when R.sub.1 and R.sub.2 taken together form a 5 or 6 chain ring,R.sub.4 represents --OR.sub.5 or ##STR2## R.sub.Type: GrantFiled: October 4, 1996Date of Patent: November 11, 1997Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Braham Shroot, Jacques Eustache, Oliver Watts, Jean-Michel Bernardon, Philippe Nedoncelle
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Patent number: 5668280Abstract: The present invention provides a process for the preparation of substantially pure N-benzyl-3-(S)-(4-fluorophenyl)-1,4-oxazin-2-one which comprises:(i) contacting racemic N-benzyl-3-(4-fluorophenyl)-1,4-oxazin-2-one with (-)-3-bromocamphor-8-sulphonic acid (hereinafter referred to as (-)-3-BCS) in the presence of a racemising agent;(ii) collecting the resultant crystalline (-)-3-BCS salt of N-benzyl-3-(S)-(4-fluorophenyl)-1,4-oxazin-2-one; and(iii) liberating the free base of N-benzyl-3-(S)-(4-fluorophenyl)-1,4-oxazin-2-one by treatment of the (-)-3-BCS salt collected in step (ii) with aqueous base.Type: GrantFiled: May 23, 1996Date of Patent: September 16, 1997Assignee: Merck Sharp & Dohme LimitedInventors: Ramon John Alabaster, Ian Frank Cottrell, Andrew William Gibson, Simon Adrian Johnson
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Patent number: 5639880Abstract: A process for preparing amine oxides of the general formula I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are each C.sub.1 -C.sub.30 -alkyl, C.sub.3 -C.sub.12 -cycloalkyl, C.sub.1 -C.sub.30 -hydroxyalkyl, C.sub.1 -C.sub.30 -aminoalkyl, C.sub.2 -C.sub.30 -alkoxyalkyl, aryl, C.sub.7 -C.sub.20 -aralkyl, C.sub.7 -C.sub.20 -alkylaryl, C.sub.1 -C.sub.8 -alkyl-, C.sub.1 -C.sub.8 -alkoxy- or halogen-monosubstituted, -disubstituted, -trisubstituted, -tetrasubstituted or -pentasubstituted C.sub.3 -C.sub.12 -cycloalkyl, aryl, C.sub.7 -C.sub.20 -aralkyl, C.sub.7 -C.sub.20 -alkylaryl, --[(CH.sub.2).sub.2 --O].sub.n --R.sup.4, --{[CH(CH.sub.3)CH.sub.2 ]--O}.sub.m --R.sup.5, or R.sup.1 and R.sup.2 are together an uninterrupted or oxygen-, nitrogen- or sulfur-interrupted C.sub.3 -C.sub.12 -alkylene diradical chainR.sup.4 and R.sup.5 are each C.sub.1 -C.sub.12 -alkyl, C.sub.3 -C.sub.12 -cycloalkyl, hydroxyl, --COR.sup.6 or --CH.sub.2 --COOR.sup.7, C.sub.3 -C.sub.12 -cycloalkyl, aryl, C.sub.7 -C.sub.20 -aralkyl or C.sub.7 -C.Type: GrantFiled: May 30, 1996Date of Patent: June 17, 1997Assignee: BASF AktiengesellschaftInventors: Ulrich Muller, Klemens Massonne, Karsten Eller, Michael Schulz
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Patent number: 5543422Abstract: Heterocyclic amines of the formulaAr-X-A-NR.sup.1 R.sup.2wherein Ar is a bicyclic or tricyclic aromatic group which is unsubstituted or which bears one or more substituents selected from halo, nitro and cyano groups and alkyl and alkoxy groups each of up to 4 carbon atoms;wherein X is a direct link or is --O--, --S--, --SO-- or --SO.sub.2 -- or has the formula --C(R.sup.3).dbd.CH-- wherein R.sup.3 is hydrogen or alkyl of up to 4 carbon atoms;wherein A is straight or branched alkylene or alkenylene of 3 to 8 carbon atoms which may be interrupted by --O--, --S-- or --NH--;and wherein NR.sup.1 R.sup.2 is a cyclic amino group;or a pharmaceutically acceptable acid addition salt thereof, are of value for therapeutic use, particularly in the treatment of myocardial ischaemia and hypertension and in the treatment of fungal infections.Type: GrantFiled: March 23, 1995Date of Patent: August 6, 1996Assignee: British Technology Group LimitedInventors: Ian G. C. Coutts, Pamela J. Cummins
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Patent number: 5543515Abstract: A process for preparing tertiary amine oxides with a low nitrosamine content by reacting a tertiary amine with an aqueous solution of hydrogen peroxide, which comprises using as starting material tertiary amines whose total content of primary and secondary amines is not more than 0.05% by weight.Type: GrantFiled: August 3, 1994Date of Patent: August 6, 1996Assignee: BASF AktiengesellschaftInventors: Ulrich Koehler, Hardo Siegel, Guenther Seybold
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Patent number: 5519074Abstract: The invention relates to crystalline complex compounds of formula I ##STR1## wherein the general symbols are as defined in claim 1, as corrosion inhibitors in coating compositions for protecting metallic surfaces.Type: GrantFiled: January 12, 1995Date of Patent: May 21, 1996Assignee: Ciba-Geigy CorporationInventors: Andreas Kramer, Adalbert Braig
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Patent number: 5502188Abstract: Aqueous solutions of N-methylmorpholine N-oxide having color numbers below 200 APHA, based on an N-methylmorpholine N-oxide content of 50% by weight, are produced by reacting aqueous hydrogen peroxide solutions with aqueous solutions of N-methylmorpholine having a water content of at least 35% by weight.Type: GrantFiled: June 7, 1995Date of Patent: March 26, 1996Assignee: BASF CorporationInventors: Klemens Massonne, Gerd Konrad, Mark D. Sandison, Gregory E. Moffitt, Lawrence E. James, John Banger