The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/151)
-
Publication number: 20090018114Abstract: The present application relates to cannabinoid receptor ligands containing compounds of formula (I) wherein A, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: July 8, 2008Publication date: January 15, 2009Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Michael J. Dart, Arturo Perez-Medrano, Derek W. Nelson
-
Publication number: 20080207610Abstract: Disclosed are novel isoflavone derivatives having the structure of Formula I which are useful as ALDH-2 inhibitors for treating mammals for dependence upon drugs of addiction, for example addiction to dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and alcohol.Type: ApplicationFiled: January 24, 2008Publication date: August 28, 2008Inventors: Jeff Zablocki, Matthew Abelman, Michael Organ, Yaroslav Bilokin, Robert Jiang, Elfatih Elzein, Tetsuya Kobayashi, Rao Kalla, Thao Perry, Xiaofen Li, Ivan Diamond, Lina Yao, Peidong Fan, Maria Pia Arolfo, Zhan Jiang
-
Publication number: 20080206312Abstract: Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation.Type: ApplicationFiled: January 24, 2008Publication date: August 28, 2008Inventors: Alan D. Robertson, Shaun Jackson, Vijaya Kenche, Cindy Yaip, Hishani Parbaharan, Phil Thompson
-
Publication number: 20080188423Abstract: The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.Type: ApplicationFiled: December 21, 2007Publication date: August 7, 2008Inventors: Joseph R. Garlich, Donald L. Durden, Mary Patterson, Jingdong Su, Robert G. Suhr
-
Patent number: 7405211Abstract: Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation.Type: GrantFiled: October 12, 2004Date of Patent: July 29, 2008Assignee: AstraZeneca ABInventors: Alan D. Robertson, Shaun Jackson, Vijaya Kenche, Cindy Yaip, Hishani Parbaharan, Phil Thompson
-
Patent number: 7262296Abstract: The present invention relates to novel compounds possessing specific hot, pungent and spicy taste when subjected to direct pungency evaluation, which may be useful as food additives and anti-oxidants, however the said compounds do not add to any nutritional value but the synthesised compounds can possess useful pharmacological properties which is expected to find application in new test models for the development of anti-inflammatory drugs, bioavailability enhancers and for the study of hepatic drug metabolising mechanism; also relates to a process for preparing the said compounds.Type: GrantFiled: December 15, 2005Date of Patent: August 28, 2007Assignee: Council of Scientific and Industrial ResearchInventors: Subhash Chandra Taneja, Surrinder Koul, Jawahir Lal Koul, Beenu Moza, Sukhdev Swami Handa
-
Patent number: 7226918Abstract: The invention relates to the use of compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, in the preparation of a medicament for inhibiting the activity of DNA-PK, wherein R1 and R2 are independently hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; X and Y are selected from CR4 and O, O and CR?4 and NR?4 and N, where the unsaturation is in the appropriate place in the ring, and where one of R3 and R4 or R?4 is an optionally substituted C3-20 heteroaryl or C5-20 aryl group, and the other of R3 and R4 or R?4 is H, or R3 and R4 or R?4 together are -A-B—, which collectively represent a fused optionally substituted aromatic ring. The compounds also selectively inhibit the activity of DNA-PK compared to PI 3-kinase and/or ATM.Type: GrantFiled: August 14, 2002Date of Patent: June 5, 2007Assignee: Cancer Research Technology LimitedInventors: Niall Morrison Barr Martin, Graeme Cameron Murray Smith, Roger John Griffin, Bernard Thomas Golding, Ian Robert Hardcastle, David Richard Newell, Hilary Alan Calvert, Nicola Jane Curtin, Laurent Jean Martin Rigoreau, Xiao-ling Fan Cockcroft, Vincent Junior Ming-lai Loh, Paul Workman, Florence Irene Raynaud, Bernard Paul Nutley
-
Patent number: 7057040Abstract: The present invention relates to novel compounds possessing specific hot, pungent and spicy taste when subjected to direct pungency evaluation, which may be useful as food additives and anti-oxidants, however the said compounds do not add to any nutritional value but the synthesised compounds can possess useful pharmacological properties which is expected to find application in new test models for the development of anti-inflammatory drugs, bioavailability enhancers and for the study of hepatic drug metabolising mechanism; also relates to a process for preparing the said compounds.Type: GrantFiled: February 7, 2002Date of Patent: June 6, 2006Assignee: Council of Scientific and Industrial ResearchInventors: Subhash Chandra Taneja, Surrinder Koul, Jawahir Lal Koul, Beenu Moza, Sukhdev Swami Handa
-
Patent number: 6949537Abstract: The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.Type: GrantFiled: April 5, 2004Date of Patent: September 27, 2005Assignee: Semafore Pharmaceuticals, Inc.Inventors: Joseph R. Garlich, Donald L. Durden, Mary Patterson, Jingdong Su, Robert G. Suhr
-
Patent number: 6846817Abstract: The invention provides nicotine receptor agonists of formula I: wherein R1, x, y, and n have any of the values given in the specification, or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising such a compound or salt, methods for preparing such a compound or salt, and methods for modulating (e.g. antagonizing or activating) nicotine receptors with such a compound or salt.Type: GrantFiled: November 30, 2001Date of Patent: January 25, 2005Assignee: Regents of the University of MinnesotaInventor: S. Mbua Ngale Efange
-
Patent number: 6844336Abstract: This invention describes the new 4-fluoroalkyl-2H-benzopyrans of general formula I, in which Z is a straight-chain or branched-chain alkyl group with up to 5 carbon atoms that is fluorinated in at least one place, preferably a trifluoromethyl group, and R1, R2, X, Y and n have the meanings that are indicated in the description. The new compounds have at their disposal strong antiestrogenic action. In addition, they can have at their disposal estrogenic action that occurs in a tissue-selective manner. They can be used for the production of pharmaceutical agents, especially for the treatment of estrogen-dependent diseases and tumors and pharmaceutical agents for hormone replacement therapy (HRT) as well as for the prevention and treatment of osteoporosis.Type: GrantFiled: March 15, 2001Date of Patent: January 18, 2005Assignee: Schering AGInventors: Hermann Kuenzer, Rolf Jautelat, Ludwig Zorn, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier
-
Publication number: 20040242870Abstract: The invention provides a method, compounds, and compositions for inhibiting the replication or proliferation of a virus. In accordance with the invention, at least one cannabichromene derivative is exposed to the virus, a host cell, or an infected cell under conditions sufficient to inhibit the replication or proliferation of the virus.Type: ApplicationFiled: April 5, 2004Publication date: December 2, 2004Applicant: Immugen Pharmaceuticals, Inc.Inventor: Craig R. Travis
-
Publication number: 20040110750Abstract: Compounds of formula (I′) wherein the two OH— substituents in the phenyl moiety are in a position ortho to one another and R1 in a position ortho to one of the hydroxy groups; and X, R1 to R6 are as defined in claims, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.Type: ApplicationFiled: March 31, 2003Publication date: June 10, 2004Inventors: Jarmo Pystynen, Martti Ovaska, Jukka Vidgren, Timo Lotta, Marjo Yliperttula-Ikonen
-
Publication number: 20040087586Abstract: The present invention provides 2-heterosubstituted 3-aryl-4H-benzopyran-4-one compounds for the treatment of cancers, namely breast cancer. This invention further provides a method of synthesis of 2-(alkylthio)isoflavones that can be carried out at ambient conditions. This invention further provides a method of synthesis of the 2-heterosubstituted 3-aryl-4H-benzopyran-4-one from a 2-(alkylthio)isoflavone. The invention further provides methods of using the 2-heterosubstituted 3-aryl-4H-benzopyran-4-one compounds for the treatment of breast cancer in mammals.Type: ApplicationFiled: August 4, 2003Publication date: May 6, 2004Inventors: Robert W. Brueggemeier, Young-Woo Kim
-
Patent number: 6699860Abstract: This invention is related to novel di-substituted aminomethyl chroman derivatives which are useful in the treatment of beta-3 receptor-mediated conditions.Type: GrantFiled: December 7, 2001Date of Patent: March 2, 2004Assignee: Bayer Pharmaceuticals CorporationInventors: Gaetan H. Ladouceur, William H. Bullock, Steven R. Magnuson, Stephen J. O'Connor, Roger A. Smith, Quanrong Shen, Qingjie Liu, Ning Su, Emil J. Velthuisen, Ann-Marie Campbell, Paul P. Ehrlich
-
Publication number: 20040034017Abstract: This invention describes the new 4-fluoroalkyl-2H-benzopyrans of general formula I, 1Type: ApplicationFiled: January 7, 2003Publication date: February 19, 2004Inventors: Hermann Kuenzer, Rolf Jautelat, Ludwig Zorn, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier
-
Publication number: 20040029914Abstract: Novel compounds are useful as chemotherapeutic, chemopreventative, and antiangiogenic agents are provided. The compounds are flavanoids, including flavanones, flavanols, and chalcones.Type: ApplicationFiled: April 18, 2003Publication date: February 12, 2004Inventors: Nurulain Zaveri, Wan-Ru Chao
-
Patent number: 6642380Abstract: A novel fluorescent group-containing carbodiimide compound having at least one group selected from a carboxyl group, a sulfo group, a phosphono group and a phospho group which have substitution of an alkali metal, an alkaline earth metal or a basic group containing a nitrogen or phosphorus atom, which is prepared by using a novel fluorescent group-containing carbodiimide compound precursor having a halogen atom or a sulfonic acid group.Type: GrantFiled: March 23, 2000Date of Patent: November 4, 2003Assignee: Nisshinbo Industries, Inc.Inventors: Naoki Kimura, Namiko Shiohata, Yoko Yoshikawa
-
Patent number: 6638972Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: GrantFiled: October 3, 2002Date of Patent: October 28, 2003Assignee: WyethInventors: Michael Gerard Kelly, Lynne Padilla Greenblatt, Gan Zhang, Yvette L. Palmer, Steven Edward Lenicek
-
Publication number: 20030186975Abstract: Compounds of formula (I′) wherein the two OH— substituents in the phenyl moiety are in a position ortho to one another and R1 in a position ortho to one of the hydroxy groups; and X, R1 to R6 are as defined in claims, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.Type: ApplicationFiled: March 31, 2003Publication date: October 2, 2003Inventors: Jarmo Pystynen, Martti Ovaska, Jukka Vidgren, Timo Lotta, Marjo Yliperttula-Ikonen
-
Publication number: 20030171372Abstract: The invention provides a method, compounds, and compositions for inhibiting the replication or proliferation of a virus. In accordance with the invention, at least one cannabichromene derivative is exposed to the virus, a host cell, or an infected cell under conditions sufficient to inhibit the replication or proliferation of the virus.Type: ApplicationFiled: January 16, 2003Publication date: September 11, 2003Applicant: Immugen Pharmaceuticals, Inc.Inventor: Craig R. Travis
-
Patent number: 6608089Abstract: Compounds having the formula (I) Z—OCH2—C≡CCH2—NRR1 (I) or a pharmaceutically acceptable salt or solvate thereof wherein Z can represent the formula (1A) or (1B). The compounds possess antiproliferative activity and are useful as modulators of multiple drug resistance in cancer chemotherapy. The compounds may also be useful for the manufacture of a medicament for the treatment or prevention of neoplasms, menopausal disorders and osteoporosis.Type: GrantFiled: February 15, 2002Date of Patent: August 19, 2003Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Piero Valenti
-
Publication number: 20030119816Abstract: The invention concerns novel products of formula (I) wherein: R1 represents a carbocyclic or heterocyclic radical optionally substituted; R2 and R3 are such that one represents hydrogen and the other represents piperidinyl optionally substituted; R4 represents hydrogen, alkyl or phenyl optionally substituted, said products being in all isomeric and salt forms and used as medicines.Type: ApplicationFiled: September 4, 2002Publication date: June 26, 2003Inventors: Jean-Luc Haesslein, Dominique Lefrancois, Eric Uridat, Jidong Zhang
-
Publication number: 20030105096Abstract: The present invention relates to the therapeutic use of non-amine tropane analogues that bind to the SERT to treat neuropsychiatric disorders.Type: ApplicationFiled: February 28, 2002Publication date: June 5, 2003Inventors: Bertha K. Madras, Peter C. Meltzer
-
Publication number: 20030100556Abstract: The present invention relates to new new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives compound having the formula (I) 1Type: ApplicationFiled: November 1, 2002Publication date: May 29, 2003Inventors: Stefan Berg, Martin Nylof, Svante Ross, Seth-Olov Thorberg
-
Publication number: 20030100774Abstract: This invention provides a process for the stereospecific preparation of 2-yl-chroman and -chromene derivatives of the formula: 1Type: ApplicationFiled: October 4, 2002Publication date: May 29, 2003Applicant: WyethInventor: Jonathan L. Gross
-
Publication number: 20030078260Abstract: This invention relates to novel 2,6-substituted chroman derivatives which are useful in the treatment of beta-3 adrenoreceptor-mediated conditions.Type: ApplicationFiled: April 22, 2002Publication date: April 24, 2003Inventors: Stephen J. O'Connor, Gaetan H. Ladouceur, William H. Bullock, Ann-Marie Campbell, Miao Dai, Robert Dally, Jacques Dumas, Holia N. Hatoum-Mokdad, Uday Khire, Wendy Lee, Qingjie Liu, Derek B. Lowe, Steven R. Magnuson, Ning Qi, Tatiana E. Shelekhin, Quanrong Shen, Roger A. Smith, Ming Wang
-
Patent number: 6552054Abstract: The invention provides chromone derivatives of the following general formula, a process for preparing such chromone derivatives and a prophylactic and therapeutic agent comprising such chromone derivatives for bone diseases and chondropathy: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 is a hydrogen atom or hydrocarbon group; R3 is a hydrogen atom, hydrocarbon group or halogen; n is an integer of 0-3; or a salt thereof.Type: GrantFiled: March 1, 2002Date of Patent: April 22, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Masahiro Kawase, Akira Mori
-
Publication number: 20030069192Abstract: 3-Deoxyflavonoid compounds and methods for inhibiting T-cell activity and treating diseases and disorders (e.g., autoimmune disorders, inflammatory disorders, diabetes, ALS, MS, rheumatoid arthritis, etc.). In some cases the efficacy and/or duration of action of luteolin and/or other 3-dioxyflavinoid compounds may be increased by administering such compounds along with Rutin, a Rutin congener and/or a Rutin derivative. Also, in some cases, first pass metabolism of luteolin or other 3-deoxyflavinoids may be avoided by administering such compounds by parenteral routes (e.g., sublingual, buccal, intranasal, injection, etc.).Type: ApplicationFiled: September 6, 2002Publication date: April 10, 2003Applicant: SynorX, Inc.Inventors: Thomas P. Lahey, V.J. Rajadhyaksha
-
Publication number: 20030055056Abstract: The present invention discloses new and useful compounds including methyl p-hydroxyphenyllactate, its analogues, chemical derivatives and chemically related compounds and their use as antitumor and immune suppressive agents, as inhibitors of proliferative cell growth and as prophylactic agents to inhibit and prevent cancer and non-malignant cell growth.Type: ApplicationFiled: February 15, 2002Publication date: March 20, 2003Inventors: Ezio Bombardelli, Piero Valenti
-
Publication number: 20030013705Abstract: This invention is related to novel carboxyl substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.Type: ApplicationFiled: August 21, 2002Publication date: January 16, 2003Inventors: Richard D. Connell, Timothy G. Lease, Jeremy L. Baryza
-
Publication number: 20020183318Abstract: A marked up versions of the abstract showing insertions and deletions are included in Appendix A.Type: ApplicationFiled: February 15, 2002Publication date: December 5, 2002Inventors: Ezio Bombardelli, Piero Valenti
-
Patent number: 6372739Abstract: Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having the following structure, as well as pharmaceutical compositions containing the same: wherein R1, R2, R3, n and p are as defined here. Methods are also disclosed for modulating ER in cells and/or tissues expressing the same, such as bone, breast, prostate, uterus, CNS or the cardiovascular system. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, and adverse reproductive effects associated with exposure to environmental chemicals or natural hormonal imbalances.Type: GrantFiled: July 2, 2001Date of Patent: April 16, 2002Assignee: Signal Pharmaceuticals, Inc.Inventors: Bernd M. Stein, David Wesley Anderson, Leah M. Gayo-Fung, Mary Doubleday, Graziella I. Shevlin, Adam Kois, Sak Khammungkhune, Ravi Kumar Jalluri, Shripad S. Bhagwat, Jeffrey A. McKie
-
Patent number: 6359132Abstract: A process for the production of a Mannich reagent comprises reacting formaldehyde, especially paraformaldehyde, with a secondary amine in the complete or almost complete absence of a solvent. An alternative comprises reacting a diaminomethane produced from a secondary amine, formaldehyde, especially paraformaldehyde, as well as water with one another in about equimolar amounts. The invention is also concerned with a process for the aminomethylation of &dgr;-tocopherol or of tocopherol mixtures containing this and comprises using a Mannich reagent which has been produced in the above manner. After completion of this aminomethylation process excess Mannich reagent can be separated by distillation and can be reacted with water and formaldehyde, especially paraformaldehyde, in order to regenerate further Mannich reagent suitable for use in the aminomethylation, this regeneration representing a further aspect of the invention. Finally, the invention includes certain novel bis(aminomethyl)-&ggr;-tocopherols.Type: GrantFiled: February 23, 2001Date of Patent: March 19, 2002Assignee: Roche Vitamins Inc.Inventors: Robert Karl Müller, Heinz Schneider
-
Patent number: 6316494Abstract: The present invention relates to therapeutically active compounds of formula I a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in the prevention or treatment of estrogen related diseases or syndromes.Type: GrantFiled: October 27, 1997Date of Patent: November 13, 2001Assignee: Novo Nordisk A/SInventors: Poul Jacobsen, Svend Treppendahl, Paul Stanley Bury, Anders Kanstrup, Lise Brown Christiansen
-
Patent number: 6291456Abstract: Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having the following structure, as well as pharmaceutical compositions containing the same: wherein R1, R2, R3, n and p are as defined here. Methods are also disclosed for modulating ER in cells and/or tissues expressing the same, such as bone, breast, prostate, uterus, CNS or the cardiovascular system. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, and adverse reproductive effects associated with exposure to environmental chemicals or natural hormonal imbalances.Type: GrantFiled: January 27, 2000Date of Patent: September 18, 2001Assignee: Signal Pharmaceuticals, Inc.Inventors: Bernd M. Stein, David Wesley Anderson, Leah M. Gayo-Fung, May S. Sutherland, Mary Doubleday, Graziella I. Shevlin, Adam Kois, Sak Khammungkhune, Ravi Kumar Jalluri, Shripad S. Bhagwat, Jeffrey A. McKie
-
Patent number: 6194450Abstract: Novel pharmaceutically/cosmetically-active polyaromatic heterocyclic compounds have the structural formula (I): in which Z is a divalent radical selected from among —O—, —S— or —Nr′— and Ar is either a radical having the following structural formula (II): or a radical having the following structural formula (III): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: July 23, 1998Date of Patent: February 27, 2001Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Bruno Charpentier, Philippe Diaz, Philippe Nedoncelle
-
Patent number: 6150356Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure ##STR1## where A, B, D, Q, X.sup.1, R, R.sup.1, X.sup.2 and R.sup.2 are as defined herein. These compounds are useful as antiarrhythmic agents. In addition, a method is provided for preventing cardiac arrhythmia employing the above compounds.Type: GrantFiled: August 17, 1999Date of Patent: November 21, 2000Assignee: Bristol-Myers Squibb CompanyInventors: John Lloyd, Heather J. Finlay, Wayne Vaccaro, Karnail S. Atwal, Michael F. Gross, Kerry L. Spear
-
Patent number: 6124284Abstract: Novel compounds of formula (1) together with their salts and solvates have a number of uses in medicine, in particular as central muscle relaxants.Type: GrantFiled: July 16, 1998Date of Patent: September 26, 2000Assignee: Glaxo Wellcome Inc.Inventors: James Leroy Kelley, Gregory Cooksey Rigdon, Barrett Randolph Cooper, Ed Williams McLean, David Lee Musso, Gloria Faye Orr, Jeffrey Leaman Selph, Virgil Lee Styles
-
Patent number: 6066731Abstract: A process for the production of a Mannich reagent comprises reacting formaldehyde, especially paraformaldehyde, with a secondary amine in the complete or almost complete absence of a solvent. An alternative comprises reacting a diaminomethane produced from a secondary amine, formaldehyde, especially paraformaldehyde, as well as water with one another in about equimolar amounts. The invention is also concerned with a process for the aminomethylation of .delta.-tocopherol or of tocopherol mixtures containing this and comprises using a Mannich reagent which has been produced in the above manner. After completion of this aminomethylation process excess Mannich reagent can be separated by distillation and can be reacted with water and formaldehyde, especially paraformaldehyde, in order to regenerate further Mannich reagent suitable for use in the aminomethylation, this regeneration representing a further aspect of the invention. Finally, the invention includes certain novel bis(aminomethyl)-.gamma.-tocopherols.Type: GrantFiled: March 22, 1996Date of Patent: May 23, 2000Assignee: Roche Vitamins Inc.Inventors: Robert Karl Muller, Heinz Schneider
-
Patent number: 6034256Abstract: A class of benzopyran, derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I' ##STR1## wherein X, A.sup.1, A.sup.2, A.sup.3, A.sup.4, R, R", R.sup.1 and R.sup.2 are as described in the specification.Type: GrantFiled: April 17, 1998Date of Patent: March 7, 2000Assignee: G.D. Searle & Co.Inventors: Jeffery S Carter, Mark G Obukowicz, Balekudru Devadas, John J Talley, David L Brown, Matthew J Graneto, Stephen R Bertenshaw, Donald J Rogier, Jr., Srinivasan R Nagarajan, Cathleen E Hanau, Susan J Hartmann, Cindy L Ludwig, Suzanne Metz
-
Patent number: 5994390Abstract: The present invention relates to therapeutically active compounds of formula I ##STR1## a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in the prevention or treatment of estrogen related diseases or syndromes.Type: GrantFiled: October 27, 1997Date of Patent: November 30, 1999Assignee: Novo NordiskInventors: Poul Jacobsen, Svend Treppendahl, Paul Stanley Bury, Anders Kanstrup, Lise Brown Christiansen
-
Patent number: 5969140Abstract: Naphthalene derivatives of the formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are each H, protected or unprotected OH, one of R.sup.3 and R.sup.4 is protected or unprotected hydroxymethyl, and the other is H, lower alkyl, or protected or unprotected hydroxymethyl, R.sup.5 and R.sup.6 are the same or different and are each H, substituted or unsubstituted lower alkyl, substituted or unsubstituted phenyl or protected or unprotected NH.sub.2, or both combine together with the adjacent N to form substituted or unsubstituted heterocyclic group, and pharmaceutically acceptable salts thereof, these compounds showing excellent bronchoconstriction inhibitory activity, and hence, being useful in the prophylaxis or treatment of asthma.Type: GrantFiled: July 2, 1998Date of Patent: October 19, 1999Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Tatsuzo Ukita, Katsuo Ikezawa, Shinsuke Yamagata
-
Aromatic derivatives substituted by a ribose, their preparation process and their use as medicaments
Patent number: 5968939Abstract: A subject of the invention is the compounds of formula (I): ##STR1## having antibiotic properties.Type: GrantFiled: July 22, 1998Date of Patent: October 19, 1999Assignee: Hoechst Marion RousselInventors: Fabienne Chatreaux, Michel Klich, Laurent Schio -
Patent number: 5955607Abstract: Compounds of the formula I ##STR1## having the meanings of the substituents indicated in the claims are outstandingly efficacious substances for producing medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.Type: GrantFiled: September 25, 1998Date of Patent: September 21, 1999Assignee: Hoechst Marion Roussel DeutschlandInventors: Joachim Brendel, Uwe Gerlach, Hans Jochen Lang, Klaus Weidmann
-
Patent number: 5889003Abstract: A compound of general formula (I): ##STR1## in which: R.sub.1 represents alkyl,X represents oxygen, --CHR'-- or --CR'.dbd.,R' is chosen from hydrogen and alkyl,R.sub.2 represents optionally substituted alkyl as is defined in the description, cycloalkyl or polycycloalkyl as are defined in the description,R.sub.3 represents hydrogen or hydroxyl,Alk represents alkylene, andY is as defined in the description,and medicinal products containing the same are useful as PDE IV inhibitors.Type: GrantFiled: September 26, 1997Date of Patent: March 30, 1999Assignee: Adir Et CompagnieInventors: Alain Dhainaut, Guy Lewin, Emmanuel Canet, Michel Lonchampt, Yves Rolland
-
Patent number: 5872118Abstract: Novel compounds of formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each selected from hydrogen and fluoro and at least one and not more than two is fluoro;R.sup.5 is selected from hydrogen and C.sub.1 -C.sub.4 alkyl;R.sup.6 is selected from hydrogen, C.sub.1 -C.sub.4 ally and hydroxy; orR.sup.5 and R.sup.6 together with the ring carbon form a carbonyl group;R.sup.7 is selected from hydrogen and hydroxy,R.sup.8 and R.sup.9 are each selected from hydrogen, C.sub.1 -C.sub.4 alkyl and cyclo(C.sub.3 or C.sub.4) alkyl or together with the nitrogen form a morpholino group; andX is selected from a bond, methylene and --O-- and is always a bond or --O-- when any of R.sup.5, R.sup.6 and R.sup.7 is other than hydrogen and is always a bond when R.sup.5 and R.sup.6 together with the ring carbon form a carbonyl group;and their salts and solvates have a number of uses as central muscle relaxants. In particular, treatment of conditions associated with abnormally raised skeletal muscle tone.Type: GrantFiled: December 18, 1995Date of Patent: February 16, 1999Assignee: Glaxo Wellcome Inc.Inventors: James Leroy Kelley, Gregory Cooksey Rigdon, Barrett Randolph Cooper, Ed Williams McLean, David Lee Musso, Gloria Faye Orr, Jeffrey Leaman Selph, Virgil Lee Styles
-
Patent number: 5869478Type: GrantFiled: June 7, 1995Date of Patent: February 9, 1999Assignee: Bristol-Myers Squibb CompanyInventors: Charles Z. Ding, Karnail S. Atwal
-
Patent number: 5856479Abstract: Using the fluorescent group-containing carbodiimide compound represented-by the following formula (I) as the label and the like in the nucleic acid detection method, immunoassay, or chemiluminescence assay, labeling can be made efficiently for a short time, a nucleic acid derived from nature can be labelled, and highly sensitive assay is enabled.B--Y.sup.3 --N.dbd.C.dbd.N--Y.sup.2 --W--Y.sup.1 --?A!.sub.n --F(I)wherein F represents a fluorescent group;A represents a moiety selected from the group consisting of --CH.sub.2 --, --NHCO--, --CONH--, --O--, --S--, --NR-- wherein R is an alkyl group, --COO--, --OCO--, --NHSO.sub.2 --, and --SO.sub.2 NH--;n is 0 or 1;W represents a direct bond or a quaternary ammonium group;Y.sup.1, Y.sup.2 and Y.sup.3 each represents an alkylene group which may have a functional group in its main chain; andB represents H or a monovalent organic group which may be the same as or different from that represented by --W--Y.sup.1 --?A!.sub.n --F.Type: GrantFiled: May 16, 1997Date of Patent: January 5, 1999Assignee: Nisshinbo Industries, Inc.Inventors: Osamu Suzuki, Gen Masuda, Namiko Shiohata, Kazuko Matsumoto
-
Patent number: 5849798Abstract: Novel pharmaceutically/cosmetically-active polyaromatic heterocyclic compounds have the structural formula (I): ##STR1## in which Z is a divalent radical selected from among --O--, --S-- or --Nr'-- and Ar is either a radical having the following structural formula (II): ##STR2## or a radical having the following structural formula (III): ##STR3## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: March 14, 1996Date of Patent: December 15, 1998Assignee: Centre International De Recherches Dermatologiques GaldermaInventors: Bruno Charpentier, Philippe Diaz, Philippe Nedoncelle