The Aryl Ring Or Ring System Is Polycyclo Patents (Class 564/352)
  • Patent number: 9035097
    Abstract: Disclosed is a process for preparing an aryloxyalkylene amine compound via an aminoethylation reaction comprising: a) reacting an aromatic hydroxyl compound in the presence of a basic catalyst with a 2-oxazolidinone compound of the formula II to form an intermediate reaction product; wherein R3 is selected from the group consisting of hydrogen or lower alkyl having 1 to 6 carbon atoms, R4 is selected from the group consisting of hydrogen, straight or branched chain alkyl having from one to six carbon atoms, phenyl, alkaryl, or arylalkyl; and b) reacting the intermediate product of step a) with a polyalkylene polyamine.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: May 19, 2015
    Assignee: Chevron Oronite Company LLC
    Inventors: Patrick J. McDougall, James Saenz, David Lao
  • Publication number: 20140377791
    Abstract: The present invention relates to a compound which is a novel two-photon absorbing fluorescent substance, a production method for the compound, a fluorescence sensor and molecular probe able to sense various substrates or enzyme activity or the like using the same, and a method of sensing enzyme activity or the like using the same. More specifically, the present invention relates to a novel two-photon absorbing fluorescent substance which has the high photo-stability and large two-photon absorption cross-section value of acedan which is a two-photon absorbing fluorescent substance, and has the high fluorescence efficiency of coumarin which is a one-photon absorbing fluorescent substance, while exhibiting absorption and emission characteristics at a longer wavelength than existing acedan and coumarin and so being advantageous in in-vivo imaging.
    Type: Application
    Filed: March 21, 2013
    Publication date: December 25, 2014
    Inventors: Kyo Han Ahn, Dokyoung Kim
  • Publication number: 20140073814
    Abstract: Disclosed is a process for preparing an aryloxyalkylene amine compound via an aminoethylation reaction comprising: a) reacting an aromatic hydroxyl compound in the presence of a basic catalyst with a 2-oxazolidinone compound of the formula II to form an intermediate reaction product; wherein R3 is selected from the group consisting of hydrogen or lower alkyl having 1 to 6 carbon atoms, R4 is selected from the group consisting of hydrogen, straight or branched chain alkyl having from one to six carbon atoms, phenyl, alkaryl, or arylalkyl; and b) reacting the intermediate product of step a) with a polyalkylene polyamine.
    Type: Application
    Filed: September 12, 2012
    Publication date: March 13, 2014
    Applicant: Chevron Oronite Company LLC
    Inventors: Patrick J. McDougall, James Saenz, David Lao
  • Patent number: 8629135
    Abstract: A class of compounds useful in pharmaceutical compositions and methods for treating or preventing cancer is described. The compounds' ability to inhibit RET kinase is quantified, i.e., their respective RET IC50 and EC50 values are described. One such compound, known as cyclobenzaprine and herein as SW-01, has been identified as RET-specific with an IC50 of 300 nM. SW-01 inhibits RET autophosphorylation and blocks the growth and transformation of thyroid cancer cell lines. It has been further tested in pancreatic cancer, breast cancer, and SCLC cell lines. The compounds show utility for inhibition of survival and proliferation of tumor cells.
    Type: Grant
    Filed: July 14, 2009
    Date of Patent: January 14, 2014
    Assignee: Queen's University at Kingston
    Inventors: Taranjit S. Gujral, Lois M. Mulligan, Vinay K. Singh
  • Patent number: 8546615
    Abstract: The present invention relates to solid racemic dapoxetine, solid dapoxetine S(+)enantiomer, processes for their preparation and their use in the pharmaceutically active compound dapoxetine acid addition salt, and pharmaceutical compositions thereof.
    Type: Grant
    Filed: November 13, 2009
    Date of Patent: October 1, 2013
    Assignee: Symed Labs Limited
    Inventors: Dodda Mohan Rao, Pingili Krishnareddy, Aadepu Jithender
  • Publication number: 20130150453
    Abstract: The present invention relates to solid racemic dapoxetine, solid dapoxetine S(+)enantiomer, processes for their preparation and their use in the pharmaceutically active compound dapoxetine acid addition salt, and pharmaceutical compositions thereof.
    Type: Application
    Filed: November 13, 2009
    Publication date: June 13, 2013
    Applicant: SYMED LABS LIMITED
    Inventors: Dodda Mohan Rao, Pingili Krishnareddy, Aadepu Jithender
  • Publication number: 20120101327
    Abstract: The present invention concerns an apparatus and a method for stimulating brain tissue with pulsed electromagnetic fields weaker than the limit for elicitation of the action potentials of the cells of the tissue to be stimulated, the apparatus comprising: at least one electrically conducting coil positioned at a bitemporal position such that hippocampus is stimulated by at least one magnetic field upon supplying a pulse to said coil as well as a coil positioned at a occipital and parietal position; and a pulse generation means operationally connected to said at least one coil for supplying a series of current pulses for conduction, allowing generation of pulsed electromagnetic fields sufficiently strong to cause protein activation, and weaker than the limit for elicitation of the action potentials of the cells of the tissue to be stimulated.
    Type: Application
    Filed: June 22, 2010
    Publication date: April 26, 2012
    Inventors: Steen Dissing, Mogens Unden
  • Publication number: 20110201598
    Abstract: A class of compounds useful in pharmaceutical compositions and methods for treating or preventing cancer is described. The compounds' ability to inhibit RET kinase is quantified, i.e., their respective RET IC50 and EC50 values are described. One such compound, known as cyclobenzaprine and herein as SW-01, has been identified as RET-specific with an IC50 of 300 nM. SW-01 inhibits RET autophosphorylation and blocks the growth and transformation of thyroid cancer cell lines. It has been further tested in pancreatic cancer, breast cancer, and SCLC cell lines. The compounds show utility for inhibition of survival and proliferation of tumour cells.
    Type: Application
    Filed: July 14, 2009
    Publication date: August 18, 2011
    Inventors: Taranjit S. Gujral, Lois M. Mulligan, Vinay K. Singh
  • Publication number: 20100191475
    Abstract: Materials, methods and a computer system are provided which facilitate the identification and characterization of modulators of potassium ion channels, particularly the HERG channel.
    Type: Application
    Filed: March 4, 2010
    Publication date: July 29, 2010
    Inventors: Scott Perschke, Ming Liu
  • Patent number: 7081465
    Abstract: This invention relates to novel {overscore (?)}-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: Grant
    Filed: October 27, 2003
    Date of Patent: July 25, 2006
    Assignee: Council of Scientific and Industrial Research
    Inventors: Devdutt Chaturvedi, Atul Kumar, Reema Rastogi, Arivend Srivastava, Priti Tewari, Rehan Ahmad, Ramaesh Chander, Anju Puri, Geetika Bhatia, Farhar Rivizvi, Anil Kumar Rastogi, Suprabhat Ray
  • Patent number: 6610705
    Abstract: The invention relates to novel diaryl naphthyl methane compounds having general formula I as shown herein below, and said compounds useful in the treatment of esterogen related disease or syndrome, Pharmaceutical compositions comprising said novel methane derivatives, process for the preparation of the novel methane derivatives and methods for the treatment of esterogen related diseases or syndrome.
    Type: Grant
    Filed: March 31, 2000
    Date of Patent: August 26, 2003
    Assignee: Council of Scientific and Industrial Research
    Inventors: Neeta Srivastava, Arvinder Grover
  • Patent number: 6545053
    Abstract: Compounds having a &bgr;-3 adrenaline receptor agonist and are useful as drugs for the treatment and prevention of diabetes, obesity, hyperlipemia, etc., represented by a general formula (I) and salts thereof, and a process for producing these, and their intermediates, wherein R represents hydrogen or methyl; R1 represents hydrogen, halogen, hydroxy, benzyloxy, amino, or hydroxymethyl; R2 represents hydrogen, hydroxymethyl, NHR3, SO2NR4R4′, or nitro; R6 represents hydrogen or lower alkyl; and X represents methylene, R9 represents hydrogen, one of R7 and R8 represent hydrogen, and the other thereof represents hydrogen, amino, acetylamino, or hydroxy.
    Type: Grant
    Filed: November 16, 2000
    Date of Patent: April 8, 2003
    Assignee: Asahi Kasei Kogyo Kabushiki Kaisha
    Inventors: Shiro Miyoshi, Kohei Ogawa
  • Publication number: 20020115715
    Abstract: Amine and amide derivatives of the formula: 1
    Type: Application
    Filed: February 7, 2002
    Publication date: August 22, 2002
    Inventors: Scott L. Dax, James McNally, Mark Youngman
  • Patent number: 6437137
    Abstract: The invention is a process for preparing a compound of formula Ia comprising reducing the compound of formula IIId wherein R3 is 1-piperidinyl, 1-pyrrolidinyl, dimethylamino, diethylamino or 1-hexamethyleneimino, R1a, R1b, R2a, R2b, and n are as defined in the specification, with a reducing agent in the presence of a solvent, heating to reflux.
    Type: Grant
    Filed: April 21, 1995
    Date of Patent: August 20, 2002
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, George J. Cullinan, Jeffrey A. Dodge, Kennan J. Fahey, Charles D. Jones, Charles W. Lugar, Brian S. Muehl
  • Patent number: 6057371
    Abstract: The invention relates to methods for the treatment of central nervous system disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof. Unexpectedly, certain of the sigma receptor ligands of the present invention have selectivity for the sigma receptor over the DA, PCP and 5-HT.sub.1A receptors.
    Type: Grant
    Filed: June 10, 1992
    Date of Patent: May 2, 2000
    Assignee: Virginia Commonwealth University
    Inventor: Richard A. Glennon
  • Patent number: 6004959
    Abstract: The present invention describes certain alkyloxyamino-substituted fluorenones which inhibit protein kinase C, as well as pharmaceutical compositions including these compounds and methods of using these compounds to control protein kinase C activity in mammals, including humans. More specifically, the present compounds are useful for the treatment of neoplastic disease states, disorders associated with abnormal blood flow (including hypertension, ischemia, atherosclerosis, coagulation disorders), and inflammatory diseases (including immune disorders, asthma, lung fibrosis, and psoriasis).
    Type: Grant
    Filed: April 18, 1997
    Date of Patent: December 21, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Winton D. Jones, Fred L. Ciske, Robert J. Dinerstein, Keith A. Diekema
  • Patent number: 5773469
    Abstract: The invention relates to diaryl antimicrobial compounds of the general formula: ##STR1## where G, E L, J, q, m, X, Ar, W, p, n and A are as described herein, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.
    Type: Grant
    Filed: June 18, 1996
    Date of Patent: June 30, 1998
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Ramesh M. Kanojia, James P. Demers, Dennis J. Hlasta, Sigmond G. Johnson, Dieter H. Klaubert
  • Patent number: 5736568
    Abstract: Compounds of the formula I ##STR1## including pharmaceutically acceptable salts thereof are disclosed in which R.sub.1, R.sub.2, R.sub.3, and R.sub.4 independently represent hydrogen, hydroxy, halo, halogenated alkyl, halogenated alkoxy, alkyl, alkoxy, cyano, a carbamoyl group, carbonyl group, or R.sub.1 and R.sub.2 together with the phenyl ring represent a naphthalene ring (optionally substituted); L.sub.1 represents C.sub.2-6 alkylene; R.sub.5 represents hydrogen or alkyl, R.sub.6 represents hydrogen or alkyl, phenylalkyl (optionally substituted) or R.sub.5 and R.sub.6 together with the nitrogen atom to which they are attached represent a saturated 3-7 membered heterocyclic ring; L.sub.2 represents a C.sub.1-6 alkylene chain; and R.sub.7 and R.sub.8 independently represent hydrogen or alkyl or R.sub.7 and R.sub.8 together with the nitrogen atom to which they are attached represent a saturated 3-7 membered heterocyclic ring.
    Type: Grant
    Filed: November 25, 1996
    Date of Patent: April 7, 1998
    Assignee: Knoll Aktiengesellschaft
    Inventors: Paul Rafferty, Gerald Bernard Tometzki
  • Patent number: 5698733
    Abstract: Disclosed are 9-deoxyprostaglandins which are useful in the treatment of glaucoma and ocular hypertension. Some of these 9-deoxyprostaglandins are novel. Also disclosed are ophthalmic, pharmaceutical compositions comprising such prostaglandins.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: December 16, 1997
    Assignee: Alcon Laboratories, Inc.
    Inventors: Mark R. Hellberg, Thomas R. Dean, Paul W. Zinke, Robert D. Selliah, John E. Bishop
  • Patent number: 5420294
    Abstract: This invention provides a method of selectively antagonizing the 5-HT.sub.1A receptor in mammals by administering aryloxypropanolamines. Aryloxypropanolamines are also claimed.
    Type: Grant
    Filed: December 22, 1993
    Date of Patent: May 30, 1995
    Assignee: Eli Lilly and Company
    Inventors: Edward E. Beedle, David W. Robertson, David T. Wong
  • Patent number: 5358971
    Abstract: Optically active or racemic compounds are provided having the formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are selected from the group consisting of H and OA with the provision that at least one of R.sub.2, R.sub.3 and R.sub.4 is H, that R.sub.2 and R.sub.4 are not both OA; A is H or is selected from the group consisting of hydrocarbyl radicals, said hydrocarbyl radicals being further optionally substituted with radicals selected from the group consisting of ##STR2## R.sub.5 is selected from the group consisting of alkyl and aromatic residues, preferably radicals having between 1 and 12 carbon atoms, including alkyl, alkyl substituted with aryl radicals, and aryl radicals substituted with alkyl radicals; n is an integer between 1 and 4; R.sub.6 is an alkyl chain comprising between 1 and 4 carbon atoms; X is oxygen; and R.sub.1 is selected from the group consisting of ##STR3## wherein Y is as defined in the specification, and a is an integer of from zero to 3.
    Type: Grant
    Filed: October 4, 1993
    Date of Patent: October 25, 1994
    Assignee: Whitby Research, Inc.
    Inventors: James V. Peck, Gevork Minaskanian
  • Patent number: 5310756
    Abstract: Novel aryloxyphenylpropylamines having the formula ##STR1## wherein X is H, cyano, halogen, halogenoalkyl, C.sub.1-6 -alkoxy, C.sub.1- -alkyl, C.sub.1-5 -alkanoyl, C.sub.3-5 -alkylene, aryloxy- or aralkoxy, andR is 3,4-methylenedioxy, aryl or heteroaryl which are optionally substituted with one or more cyano, halogeno, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkenyl, trifluoromethyl, C.sub.3-5 -alkylene, aryloxy or aralkoxy; andR.sup.1 and R.sup.2 independently is C.sub.1-10 -alkyl, C.sub.3-7 -cycloalkyl, C.sub.2-10 -alkenyl, C.sub.3-6 -cycloalkyl-C.sub.1-5 -alkyl, optionally substituted with C.sub.1-5 -alkoxy or cyano; orR.sup.1 and R.sup.2 may together form a carbocyclic ring and a salt thereof with a pharmaceutically acceptable acid,provided however that R.sup.1 is not C.sub.3-7 -cycloalkyl, C.sub.1-10 -alkyl, or alkenyl which may be straight, branched or cyclic, unsubstituted or substituted with C.sub.1-4 -alkoxy, aryloxy or cycloalkyl or cycloalkylalkyl, when X is H and R.sup.2 is a methyl group.
    Type: Grant
    Filed: June 12, 1992
    Date of Patent: May 10, 1994
    Assignee: Novo Nordisk A/S
    Inventors: Palle Jakobsen, Jorgen Drejer
  • Patent number: 5274003
    Abstract: Optically active or racemic compounds are provided having the formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H and OH with the provision that at least one of R.sub.2, R.sub.3 and R.sub.4 is H, that R.sub.2 and R.sub.4 are not both OH; X is oxygen; and R.sub.1 is selected from the group consisting of ##STR2## wherein Z is oxygen, nitrogen or sulfur, wherein Y is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido, halogen, hydrocarbyl and heteroatom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms, and a is an integer of from zero to 3. These compounds are capable of binding selectivity of one or more dopamine D.sub.2 receptors, for instance, in humans.
    Type: Grant
    Filed: February 18, 1992
    Date of Patent: December 28, 1993
    Assignee: Whitby Research, Inc.
    Inventors: James V. Peck, Gevork Minaskanian
  • Patent number: 5272144
    Abstract: Aryloxy- and heteroaryloxy-alkylene derivatives of amines of formula ##STR1## wherein each of A and B is a group of formula (i) to (iii): ##STR2## wherein Y is --O--, --S-- or --NR-- in which R is hydrogen or C.sub.1 -C.sub.6 alkyl; each of R.sub.3, R.sub.4, R.sub.5 and R.sub.6 is independently:a) hydrogen, halogen, hydroxy, cyano or nitro;b) C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by halogen,c) C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio;d) C.sub.1 -C.sub.6 alkyl-sulfonyl;e) a substituted amine group --NR.sub.7 R.sub.8 ;f) a --COR.sub.12 group; org) two adjacent groups of R.sub.3, R.sub.4, R.sub.5 and R.sub.6, taken together, form a C.sub.1 -C.sub.4 alkylenedioxy group;each of R.sub.1 and R.sub.2 independently is hydrogen, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 alkenyl or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl; or R.sub.1 and R.sub.
    Type: Grant
    Filed: June 13, 1991
    Date of Patent: December 21, 1993
    Assignee: Farmitalia Carlo Erba s.r.l.
    Inventors: Piero Melloni, Philippe Dostert, Arturo D. Torre, Alberto Bonsignori
  • Patent number: 5216178
    Abstract: Novel aminoalkylthiodibenzoxepins, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as analgesic, antidepressant and anticonvulsant agents. A process for selectively reducing olefins by alkaline earth metals in loweralkanols is also disclosed.
    Type: Grant
    Filed: August 15, 1991
    Date of Patent: June 1, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
  • Patent number: 5192765
    Abstract: Amines of the following formula: ##STR1## where the variables are defined in the specification are useful in the treatment of diseases associated with altered motility and/or tone of smooth muscle.
    Type: Grant
    Filed: June 6, 1991
    Date of Patent: March 9, 1993
    Assignee: Pfizer Inc.
    Inventors: David Alker, Robert J. Bass, Peter E. Cross
  • Patent number: 5145870
    Abstract: Novel aryloxyphenylpropylamines having the formula ##STR1## wherein X is H, cyano, halogen, halogenoalkyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkyl, C.sub.1-5 -alkanoyl, C.sub.3-5 -alkylene, aryloxy or aralkoxy, andR is 3,4-methylenedioxy, aryl or heteroaryl which are optionally substituted with one or more cyano, halogeno, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkenyl, trifluoromethyl, C.sub.3-5 -alkylene, aryloxy or aralkoxy; andR.sup.1 and R.sup.2 independently is C.sub.1-10 -alkyl, C.sub.3-7 -cycloalkyl, C.sub.2-10 -alkenyl, C.sub.3-6 -cycloalkyl-C.sub.1-5 -alkyl, optionally substituted with C.sub.1-5 -alkoxy or cyano;R.sup.1 and R.sup.2 may together form a carbocyclic ring and a salt thereof with a pharmaceutically acceptable acid,provided however that R.sup.1 is not C.sub.3-7 -cycloalkyl, C.sub.1-10 -alkyl, or alkenyl which may be straight, branched or cyclic, unsubstituted or substituted with C.sub.1-4 -alkoxy, aryloxy or cycloalkyl or cycloalkylalkyl, when X is H and R.sup.2 is a methyl group.
    Type: Grant
    Filed: May 24, 1990
    Date of Patent: September 8, 1992
    Assignee: Novo Nordisk A/S
    Inventors: Palle Jakobsen, Jorgen Drejer
  • Patent number: 5135947
    Abstract: The present invention provides 1-phenyl-3-naphthalenyloxypropanamines which are selective inhibitors of serotonin uptake.
    Type: Grant
    Filed: August 1, 1990
    Date of Patent: August 4, 1992
    Assignee: Eli Lilly and Company
    Inventors: David W. Robertson, David T. Wong, Dennis C. Thompson
  • Patent number: 5004755
    Abstract: The present invention relates to a new laevorotatory basic derivative of 9,10-ethanoanthracene, namely R-(-)-.alpha.-[(methylamino)methyl]-9,10-ethanoanthracene-9(10H)-ethanol of the formula I ##STR1## and the acid addition salts thereof, to pharmaceutical compositions containing these new substances and to a method for treating dysphoric conditions, psychovegetative or psychosomatic disorders.
    Type: Grant
    Filed: August 28, 1987
    Date of Patent: April 2, 1991
    Assignee: Ciba-Geigy Corporation
    Inventor: Angelo Storni
  • Patent number: 4994616
    Abstract: A novel herbicide of formula I ##STR1## wherein R.sub.1 represents a halogen atom or an alkyl, haloalkoxy, haloalkyl or alkoxycarbonyl group;R.sub.2 represents a hydrogen or halogen atom;each of R.sub.3 to R.sub.6 independently represents a hydrogen or halogen atom or a cyano, alkyl, haloalkyl, alkoxy or haloalkoxy group;R.sub.7 represents a hydrogen or halogen atom, or an alkyl, haloalkoxy, haloalkyl or alkoxycarbonyl group;and A represents a nitrogen atom or a --CH-- group, together with its formulation and use as a herbicide, and its preparation.
    Type: Grant
    Filed: April 12, 1988
    Date of Patent: February 19, 1991
    Assignee: Ube Industries, Ltd.
    Inventor: David Munro
  • Patent number: 4968679
    Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.
    Type: Grant
    Filed: May 22, 1989
    Date of Patent: November 6, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 4956388
    Abstract: The present invention provides 3-aryloxy-3-substituted propanamines capable of inhibiting the uptake of serotonin and norepinephrine.
    Type: Grant
    Filed: January 12, 1990
    Date of Patent: September 11, 1990
    Assignee: Eli Lilly and Company
    Inventors: David W. Robertson, David T. Wong, Joseph H. Krushinski, Jr.
  • Patent number: 4873262
    Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.
    Type: Grant
    Filed: December 15, 1987
    Date of Patent: October 10, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 4853408
    Abstract: Novel 4-phenylpropyl-indoles of the formula ##STR1## wherein R and R.sub.1 are individually selected from the group consisting of hydrogen, linear alkyl of 1 to 5 carbon atoms, branched alkyl of 3 to 5 carbon atoms, cycloalkyl of 3 to 7 carbon atoms cycloalkylalkyl of 4 to 7 carbon atoms and optionally substituted aralkyl of 7 to 12 carbon atoms or R.sub.1 and R taken together with the nitrogen atom form an optionally unsaturated heterocycle containing another heteroatom selected from the group consisting of oxygen, sulfur and nitrogen optionally substituted with a member of the group consisting of alkyl of 1 to 5 carbon atoms, phenyl, naphthyl and aralkyl of 7 to 12 carbon atoms, a together with b forms .dbd.0 or a together with c form a carbon-carbon bond, b is hydrogen or with a forms .dbd.0, c is hydrogen or with a forms a carbon-carbon bond, the dotted line is an optional carbon-carbon bond, A is --(CH.sub.2).sub.n --, is an integer from 2 to 5, R.sub.
    Type: Grant
    Filed: April 17, 1986
    Date of Patent: August 1, 1989
    Assignee: Roussel Uclaf
    Inventors: Francois Clemence, Jacques Guillaume, Gilles Hamon
  • Patent number: 4831051
    Abstract: New aromatic derivatives having an activity antagonistic to calcium and corresponding to formula: ##STR1## in which: A represents a chain having any one of the following structures: ##STR2## Ar represents a group of structure: ##STR3## n takes the value 1 or 2 when R is different from H; m takes the value 2 or 3.
    Type: Grant
    Filed: January 22, 1988
    Date of Patent: May 16, 1989
    Assignee: Delande S.A.
    Inventors: Guy R. Bourgery, Alain P. Lacour, Bernard M. Pourrias, Raphael Santamaria
  • Patent number: 4792551
    Abstract: Compounds useful for treating inflammation, pain and swelling, represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: Y and Z are each independently halo, alkyl or alkoxy;l and m are each independently integers of 0-4;b is an integer of 2-12; andX is selected from the group consisting of:--NR.sup.1 R.sup.2, --NR.sup.1 (CH.sub.2 CH.sub.2 OH), ##STR2## in which R.sup.1 and R.sup.2 are independently H, alkyl or cycloalkyl;R.sup.3 is H, alkyl or CH.sub.2 CH.sub.2 OH; andn is an integer of 3-7.
    Type: Grant
    Filed: July 15, 1983
    Date of Patent: December 20, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter H. Nelson, Stefan H. Unger, Thomas R. Thieme
  • Patent number: 4792570
    Abstract: Compounds useful for treating inflammation, swelling and associated pain, represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: a is an integer of 0-3;b is an integer of 0-2;n is an integer of 3-12;each X and each Y are independently -halo, --R.sup.1, -alkoxy, or -phenyl; andB is selected from the group consisting of:--NR.sup.1 R.sup.2, --NR.sup.1 (CH.sub.2 CH.sub.2 OH), ##STR2## in which R.sup.1 and R.sup.2 are independently H, alkyl or cycloalkyl;R.sup.3 is H, alkyl or --CH.sub.2 CH.sub.2 OH; andm is an integer of 3-8.Novel compounds are those wherein n is at least 6 if both a and b are 0.
    Type: Grant
    Filed: April 6, 1984
    Date of Patent: December 20, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter H. Nelson, James P. Dunn, Stefan H. Unger, Thomas R. Thieme
  • Patent number: 4732896
    Abstract: New aromatic derivatives having an activity antagonistic to calcium and corresponding to formula: ##STR1## in which: A represents a chain having any one of the following structures: ##STR2## Ar represents a group of structure: ##STR3## n takes the value 1 or 2 when R is different from H; m takes the value 2 or 3.
    Type: Grant
    Filed: June 26, 1985
    Date of Patent: March 22, 1988
    Assignee: Delalande S.A.
    Inventors: Guy R. Bourgery, Alain P. Lacour, Bernard M. Pourrias, Raphael Santamaria
  • Patent number: 4661297
    Abstract: Basic ethers of 7-oxo-7H-benzo(c) fluorene have been shown to evidence a pronounced antineoplastic and immunosuppressive effect in mammals suffering from leukemia. The technique for preparing the described ethers and the addition salts thereof with pharmaceutically acceptable organic and inorganic acids involves the aminoalkylation of 5-hydroxy-7-oxo-7H-benzo(c) fluorene and its corresponding nuclear substituted derivatives on the hydroxylic oxygen atom.
    Type: Grant
    Filed: September 14, 1982
    Date of Patent: April 28, 1987
    Assignee: SPOFA, spojene podniky pro zdravotnickou vyrobu
    Inventors: Jiri Krepelka, Iva Vancurova, Karel Rezabek, Milan Melka, Vojtech Pujman, Stanislava Pokorna, Ruzena Reichlova, Slavjanka Cernochova
  • Patent number: 4605673
    Abstract: The invention is concerned with 7H-dibenzo(a,c)-cyclohepten-5-one-(7) derivatives of general formula I ##STR1## wherein R.sup.1 and R.sup.2 can be the same or different, a hydrogen atom, an alkyl radical containing 1 to 3 carbon atoms, or, together with the nitrogen atom to which they are attached form a heterocyclic ring containing 3 to 6 carbon atoms,n is 2 or 3R.sup.3 is a hydrogen atom or a halogen atom andX is either a methylene radical or an oxygen atomand the pharmacologically acceptable salts thereof with inorganic and organic acids.The invention is furthermore concerned with analogous processes for the preparation thereof and their application for controlling psychic diseases and gastric and/or intestinal ulcers.
    Type: Grant
    Filed: December 19, 1983
    Date of Patent: August 12, 1986
    Assignee: Warner-Lambert Company
    Inventors: Gerhard Satzinger, Edgar Fritschi, Manfred Herrmann
  • Patent number: 4588719
    Abstract: A class of bicyclic benzenoid aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.
    Type: Grant
    Filed: October 24, 1984
    Date of Patent: May 13, 1986
    Assignee: William H. Rorer, Inc.
    Inventors: William L. Studt, Donald E. Kuhla, Henry F. Campbell
  • Patent number: 4543352
    Abstract: A class of naphthalene aminoalkylene ether and thioether compounds exhibiting pharmacological activity including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions are disclosed.
    Type: Grant
    Filed: April 29, 1983
    Date of Patent: September 24, 1985
    Assignee: William H. Rorer, Inc.
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
  • Patent number: 4508732
    Abstract: Basic ethers of the formula ##STR1## wherein Z is CH.sub.3 -NR.sup.2 -CH.sub.2 CH.sub.2 -CHR.sup.1 --, (1-R.sup.2 -3-piperidyl)-CHR.sup.3 --, (1-R.sup.2 -2-piperidyl)-CH.sub.2 -CHR.sup.3 -- or 1-R.sup.2 -3-R.sup.4 -- hexahydroazepinyl; R.sup.1 is cyclopropyl or Ar; R.sup.2 is H, alkyl of 1-4 C atoms, alkenyl of 2-4 C atoms, cycloalkylalkyl of 4-8 C atoms or benzyl; R.sup.3 is H or Ar; R.sup.4 is H or alkyl of 1-4 C atoms, Y is --O-CHQ.sup.1 -CHQ.sup.2 -CH.sub.2 --, --O-CHQ.sup.1 -CHQ.sup.2 -CO--, --O-CQ.sup.1 .dbd.CQ.sup.2 -CO-- or --CH.sub.2 -CHQ.sup.1 -CHQ.sup.2 -CO--; Q.sup.1 and Q.sup.2 are independently each H, alkyl of 1-4 C atoms, cycloalkyl or alkylcycloalkyl each of 3-6 total C atoms or Ar; and Ar is phenyl or phenyl substituted by F, Cl, alkoxy or alkylthio, each of 1-4 C atoms, methylenedioxy or CF.sub.3 ; with the proviso that when Z is (CH.sub.3).sub.2 N-CH.sub.2 CH.sub.2 -CHR.sup.1 in 7-position and Y is --O-C(C.sub.6 H.sub.5).dbd.CH-CO-- or --O-C(C.sub.6 H.sub.5).dbd.C(CH.sub.3)-CO--, R.sup.
    Type: Grant
    Filed: January 21, 1983
    Date of Patent: April 2, 1985
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Hans-Heinrich Hausberg, Helmut Prucher, Jurgen Uhl, Christoph Seyfried, Klaus Minck
  • Patent number: 4376123
    Abstract: Basic ethers of the formula ##STR1## wherein Z is CH.sub.3 --NR.sup.2 --CH.sub.2 CH.sub.2 --CHR.sup.1 --, (1-R.sup.2 -3-piperidyl)-CHR.sup.3 --, (1-R.sup.2 -2-piperidyl)-CH.sub.2 --CHR.sup.3 - or 1-R.sup.2 -3-R.sup.4 -hexahydroazepinyl; R.sup.1 is cyclopropyl or Ar; R.sup.2 is H, alkyl of 1-4 C atoms, alkenyl of 2-4 C atoms, cycloalkylalkyl of 4-8 C atoms or benzyl; R.sup.3 is H or Ar; R.sup.4 is H or alkyl of 1-4 C atoms, Y is --O--CHQ.sup.1 --CHQ.sup.2 --CH.sub.2 --, --O--CHQ.sup.1 --CHQ.sup.2 --CO--, --O--CQ.sup.1 .dbd.CQ.sup.2 --CO-- or --CH.sub.2 --CHQ.sup.1 --CHQ.sup.2 --CO--; Q.sup.1 and Q.sup.2 are independently each H, alkyl of 1-4 C atoms, cycloalkyl or alkylcycloalkyl each of 3-6 total C atoms or Ar; and Ar is phenyl or phenyl substituted by F, Cl, alkoxy or alkylthio, each of 1-4 C atoms, methylenedioxy or CF.sub.3 ; with the proviso that when Z is (CH.sub.3 ).sub.2 N--CH.sub.2 CH.sub.2 --CHR.sup.1 in 7-position and Y is --O--C(C.sub.6 H.sub.5).dbd.CH--CO-- or --O--C(C.sub.6 H.sub.5).dbd.C(CH.sub.
    Type: Grant
    Filed: December 15, 1980
    Date of Patent: March 8, 1983
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Hans-Heinrich Hausberg, Helmut Prucher, Jurgen Uhl, Christoph Seyfried, Klaus Minck
  • Patent number: 4327214
    Abstract: Substituted alkylammonium salts of the formula ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are hydrogen, C.sub.1-4 -alkyl, fluorine, chlorine or bromine, X is oxygen or sulfur, n denotes one of the integers 2, 3 and 4, A denotes quinuclidine or pyrrolizidine, or --NR.sup.4 R.sup.5 R.sup.6, R.sup.4, R.sup.5 and R.sup.6 denoting C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl or C.sub.2-6 -alkynyl which are unsubstituted or substituted by halogen, cyano or C.sub.1-4 -alkoxy, or R.sup.5 and R.sup.6, as alkylene groups, may be part of an unsubstituted or C.sub.1-2 -alkyl-substituted 5- or 6-membered heterocycle with 1 to 3 heteroatoms in the ring, and Z is the anion of any non-phytotoxic acid HZ, the manufacture of such compounds, agents for regulating plant growth containing these compounds, and the use thereof for regulating plant growth.
    Type: Grant
    Filed: September 12, 1980
    Date of Patent: April 27, 1982
    Assignee: BASF Aktiengesellschaft
    Inventors: Costin Rentzea, Hubert Sauter, Johann Jung
  • Patent number: 4313005
    Abstract: This invention relates to a process for reducing amidine formation during reduction of organonitriles. The process comprises including a boron compound in the reaction medium in sufficient amount to complex the amidine compound as it is formed.
    Type: Grant
    Filed: April 3, 1980
    Date of Patent: January 26, 1982
    Assignee: Air Products and Chemicals, Inc.
    Inventors: Michael E. Ford, Randall J. Daughenbaugh
  • Patent number: 4231942
    Abstract: There are described new styryl compounds of the formula ##STR1## in which X is .dbd.CH.sub.2, --O--, --S-- or the grouping .dbd.NR.sub.3 wherein R.sub.3 is hydrogen or an alkyl group having 1 to 4 carbon atoms,Z is the --O-- or --S-- atom,A is a straight-chain or branched-chain alkylene group having 2 to 4 carbon atoms,R.sub.1 is an unsubstituted or substituted alkyl group,R.sub.2 is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, halogen or phenoxy, andY is --CN, --COOR.sub.4, --SO.sub.2 R.sub.4 or CONR.sub.3 R.sub.5 wherein R.sub.3 has the meaning given above, R.sub.4 is a C.sub.1 -C.sub.4 -alkyl group or the phenyl group, R.sub.5 is hydrogen or is the same as R.sub.4,and the benzene rings B, C and D can be further substituted in particular by nonionic substituents, and also the production thereof and their use as dyes for dyeing and printing synthetic fibre materials, particularly those made from aromatic polyesters.
    Type: Grant
    Filed: March 12, 1979
    Date of Patent: November 4, 1980
    Assignee: Ciba-Geigy Corporation
    Inventor: Stefan Koller