Carbocyclic Ring Bonded Directly To The Nitrogen Patents (Class 548/559)
  • Publication number: 20140045910
    Abstract: Novel amino-pyrrolinic derivatives, their pharmacologically acceptable salts and use thereof in the prevention and/or treatment of metabolic syndrome.
    Type: Application
    Filed: April 17, 2012
    Publication date: February 13, 2014
    Inventors: Pascal Bousquet, Jean Daniel Ehrhardt, Lyne Fellmann, Vincent Gasparik, Hugues Greney, Mohamed Hadjeri, Andre Mann, Nathalie Niederhoffer, Stephan Schann
  • Publication number: 20120238615
    Abstract: Compounds are described herein useful for treating diseases and conditions by modulation of one or more alpha adrenergic receptor, in particular the alpha 2C receptor. The compounds can include N-(2,3-substituted phenyl)-3,4-dihydro-2H-pyrrol-5-amine derivatives.
    Type: Application
    Filed: October 20, 2010
    Publication date: September 20, 2012
    Applicant: Allergan, Inc.
    Inventors: Ken Chow, Liming Wang, Wenkui K. Fang, Evelyn G. Corpuz, Daniel W. Gil
  • Publication number: 20120208821
    Abstract: Compounds are described herein useful for treating diseases and conditions by modulation of one or more alpha adrenergic receptor. The compounds can include a naphthalene, a quinoline, a benzoimidazole or an isoquinoline as a core structure. Methods of making, using and formulating these compounds are described.
    Type: Application
    Filed: October 6, 2010
    Publication date: August 16, 2012
    Applicant: ALLERGAN, INC
    Inventors: Ken Chow, Liming Wang, Wenkui K. Fang, Evelyn G. Corpuz, Santosh C. Sinha, Daniel W. Gil, Mohammad I. Dibas, John E. Donello
  • Publication number: 20090023757
    Abstract: The present invention relates to a novel process for preparing compounds of formula (IA), which are potent and specific antagonists of corticotropin-releasing factor (CRF) receptors, from intermediate compounds of formula (I), by a coupling reaction catalysed by copper.
    Type: Application
    Filed: April 6, 2006
    Publication date: January 22, 2009
    Inventors: Daniele Andreotti, Sergio Bacchi, Monica Delpogetto, Simone Guelfi, Alcide Perboni, Arianna Ribecai, Simone Spada, Paolo Stabile, Marsia Tampieri
  • Patent number: 7414142
    Abstract: Compounds of formula I, wherein R1-R9 and n are defined herein, and pharmaceutical compositions and kits containing these compounds are provided. Also provided are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I or formula II, wherein R3-R5, R10, and R11 are defined herein.
    Type: Grant
    Filed: September 18, 2006
    Date of Patent: August 19, 2008
    Assignee: Wyeth
    Inventors: Puwen Zhang, Jeffrey Curtis Kern, Eugene Anthony Terefenko, Eugene John Trybulski
  • Patent number: 7176312
    Abstract: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.
    Type: Grant
    Filed: October 12, 2002
    Date of Patent: February 13, 2007
    Assignees: The Scripps Research Institute, IRM LLC
    Inventors: Sheng Ding, Qiang Ding, Nathanael S. Gray
  • Patent number: 6933390
    Abstract: The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of further catalysts at room temperature.
    Type: Grant
    Filed: July 15, 2004
    Date of Patent: August 23, 2005
    Assignee: Warner-Lambert Company
    Inventors: Hubert Barth, Klaus Steiner, Simon Schneider, Ulrich Bayer, Manfred Westermayer, Ulrike Wolfsperger, Hans-Jürgen Betche
  • Patent number: 6916346
    Abstract: Primary intermediates for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein R is selected from C1 to C5 alkyl or hydroxyalkyl, a C3 to C6 cyclic ring containing hetero atoms selected from O, S and N atoms, and —CH2—Ar where Ar is an aromatic ring wherein the aromatic ring may be substituted with one or two hydroxy C1 to C3 alkoxy, or amino groups.
    Type: Grant
    Filed: May 5, 2004
    Date of Patent: July 12, 2005
    Assignee: The Procter & Gamble Company
    Inventors: Mu-Ill Lim, Yuh-Guo Pan
  • Patent number: 6350761
    Abstract: This invention is directed to benzenamine derivatives of formula (I): wherein A, W, m, n, R1, R2, R3, R4, R5 and R6 are defined herein. These compounds are useful as anti-coagulants.
    Type: Grant
    Filed: July 24, 2000
    Date of Patent: February 26, 2002
    Assignee: Berlex Laboratories, Inc.
    Inventors: William J. Guilford, Steven T. Sakata, Kenneth J. Shaw, Shung Wu, Wei Xu, Zuchun Zhao
  • Patent number: 6300366
    Abstract: Compound of formula (I): in which: n is 1 or 2, X represents alkylene, alkenylene, alkynylene or optionally substituted arylene or heteroarylene, R10 represents hydrogen or alkyl and R11 and R12 together form a bond, or alternatively R12 represents hydrogen or alkyl and R10 and R11 together form a bond, R2, R3 and R4 each independently of the others represents hydrogen, alkyl, hydroxyalkyl, alkoxy, alkoxycarbonyl, aryl, arylalkyl or aryloxyalkyl, or two of R2, R3 and R4 form a cycloalkyl radical. Medicinal products containing the same are useful in the treatment of cardiovascular diseases.
    Type: Grant
    Filed: November 16, 2000
    Date of Patent: October 9, 2001
    Assignee: Adir et Compagnie
    Inventors: Pascal Bousquet, Jean-Daniel Ehrhardt, Véronique Bruban, Josiane Feldman, Stephan Schann, Elisabeth Scalbert, Bruno Pfeiffer, Pierre Renard
  • Patent number: 5998459
    Abstract: The invention relates to a pharmaceutical composition comprising a pyrrole derivative of the following formula [1] or a pharmaceutically acceptable salt thereof, or a solvate of either of them, as an active ingredient. ##STR1## (wherein R.sup.1 represents hydrogen or alkoxycar91 bonylamino, R.sup.2 represents alkyl, aryl which may be substituted, aromatic heterocyclyl which may be substituted, unsubstituted amino, monoalkylamino, dialkylamino, or cyclic amino which may be substituted; R.sup.3 represents cyano or carbamoyl; R.sup.4 represents hydrogen or alkyl; E represents alkylene; q is equal to 0 or 1, A represents methyl, aryl which may be substituted, or aromatic heterocyclyl which may be substituted). The pharmaceutical composition of the invention is effective for the treatment of pollakiuria or urinary incontinence.
    Type: Grant
    Filed: December 8, 1997
    Date of Patent: December 7, 1999
    Inventors: Masami Tsuda, Mitsushi Tanaka, Ayatsugu Nakamura
  • Patent number: 5962506
    Abstract: Compounds of Formula I ##STR1## are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is an dialkoxyphosphonate, or .alpha.-hydroxyamide group and Z is an acyl or .alpha.-ketocarbamate functionality. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid support, are also disclosed.
    Type: Grant
    Filed: July 7, 1997
    Date of Patent: October 5, 1999
    Assignee: Pharmacopeia, Inc.
    Inventors: Carolyn DiIanni Carroll, Roland Ellwood Dolle, III, Yvonne Class Shimshock, Timothee Felix Herpin
  • Patent number: 5783576
    Abstract: New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.
    Type: Grant
    Filed: August 9, 1996
    Date of Patent: July 21, 1998
    Assignee: Boehringer Ingelheim KG
    Inventors: Otto Roos, Georg Speck, Walter Losel, Dietrich Arndts, Wolf-Dietrich Bechtel
  • Patent number: 5773459
    Abstract: The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 30, 1998
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Gerald McMahon
  • Patent number: 5612483
    Abstract: Nitro-substituted aromatics can be directly aminated with amines in the presence of simple bases and oxygen.
    Type: Grant
    Filed: September 6, 1995
    Date of Patent: March 18, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventor: Manfred Jautelat
  • Patent number: 5344933
    Abstract: An azomethine dye is disclosed, represented by the general formula (I), (II) or (III): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each independently represents a hydrogen atom or nonmetallic atom group; X represents --OH or --NR.sup.5 R.sup.6 ; R.sup.5 and R.sup.6 each independently represents a hydrogen atom, alkyl group, aryl group or heterocyclic group; R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12 and R.sup.13 each independently represents a hydrogen atom or nonmetallic atom group; and R.sup.1 and R.sup.2, and/or R.sup.2 and R.sup.5, and/or R.sup.5 and R.sup.6, and/or R.sup.6 and R.sup.3, and/or R.sup.3 and R.sup.4, and/or R.sup.7 and R.sup.8, and/or R.sup.9 and R.sup.10, and/or R.sup.11 and R.sup.12, and/or R.sup.12 and R.sup.13 may be connected to each other to form a cyclic structure.
    Type: Grant
    Filed: September 10, 1992
    Date of Patent: September 6, 1994
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hisashi Mikoshiba, Katsuyoshi Yamakawa, Kozo Sato, Koushin Matsuoka
  • Patent number: 5332833
    Abstract: The .beta.-oxo-.beta.-benzenepropanethioamide derivative of the present invention has potassium channel opening action and is useful for treatment of hypertension, asthma, hypersensitive colon syndrome, and enteritis through pharmacological actions including blood vessel dilation, bronchial tract dilation, relaxation of gastrointestinal tract smooth muscle, and the like. The present invention also includes a pharmaceutical composition containing, as the active ingredient, the compound of the present invention and a method for producing the same.
    Type: Grant
    Filed: December 23, 1992
    Date of Patent: July 26, 1994
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Tetsuo Sekiya, Mikio Tsutsui, Tetsuro Shimpuku, Tatsuo Nagano, Junko Hayashi, Asami Seino
  • Patent number: 5298659
    Abstract: Azomethines can be prepared by the condensation of cycloalkanones and anilines in the presence of acid homogeneous catalysts while the water of reaction is removed azeotropically, the condensation being carried out in a continuous reaction in a column-like reactor to which a temperature profile is applied, the starting materials being fed in in the low-temperature region, and, of the reaction products, the water of reaction to be removed azeotropically being discharged also in the low-temperature region and the azomethine produced being discharged in the high-temperature region.
    Type: Grant
    Filed: January 14, 1993
    Date of Patent: March 29, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhard Langer, Hans-Josef Buysch, Paul Wagner
  • Patent number: 5003081
    Abstract: Pyrrole derivatives of the formula ##STR1## or the tautomers thereof, where R.sup.1 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, hetaryl or amino, it being possible for these radicals to be substituted,R.sup.2 is hydrogen, alkyl, benzyl, alkenyl, cycloalkyl or phenylR.sup.3 is hydrogen, alkyl, benzyl or alkenyl, or R.sup.2 and R.sup.3 together are ##STR2## where T.sup.1, T.sup.2 and T.sup.3 have the meanings mentioned in the description, or R.sup.2 and R.sup.3 together with the nitrogen connecting them are a heterocyclic radical,R.sup.4 is cyano, or carbamoyl or thiocarbamoyl, each of which can be substituted, or --C(NH.sub.2).dbd.N--OH,R.sup.5 is halogen, hydroxyl, alkanoyloxy or benzoyloxy andR.sup.6 is hydrogen, alkyl, phenyl, cyano, halogen, nitro, hydroxysulfonyl, alkanoyl, benzoyl or ##STR3## where T.sup.4 is alkyl or phenyl and T.sup.5 is the radical of an active methylene compound, hydroxyimino or the radical of a primary amine,with the proviso that R.sup.1, R.sup.2 and R.sup.
    Type: Grant
    Filed: January 8, 1990
    Date of Patent: March 26, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Juergen Pfister, Matthias Wiesenfeldt, Karl-Heinz Etzbach
  • Patent number: 4909834
    Abstract: 1-Trifluoromethylphenyl-2-(substituted phenyl)iminopyrrolidines of the formula ##STR1## in which R is H, halogen, or C.sub.1 -C.sub.4 alkyl; R' is CF.sub.3, CH.sub.3, CF.sub.2 CHF.sub.2, OCF.sub.2 CHF.sub.2, OCHF.sub.2, OCF.sub.3, SCH.sub.3, S(O)CH.sub.3, SO.sub.2 CH.sub.3, methoxyiminomethyl, methoxyimino-1-ethyl, benzoyloxyiminomethyl, and benzoyloxyimino-1-ethyl; and X and Y are independently H, halogen, CN or CF.sub.3, are useful as herbicidal agents.
    Type: Grant
    Filed: December 27, 1988
    Date of Patent: March 20, 1990
    Assignee: ICI Americas Inc.
    Inventor: Frank X. Woolard
  • Patent number: 4897397
    Abstract: Certain aryl-alkynoic, alkenoic and alkanoic acids and derivatives and their use in treating inflammation, allergy and hyperproliferative skin disease are disclosed.
    Type: Grant
    Filed: December 16, 1988
    Date of Patent: January 30, 1990
    Assignee: Schering Corporation
    Inventors: Neng Y. Shih, David J. Blythin
  • Patent number: 4892871
    Abstract: The invention is directed to azido-substituted octopamine agonists and the radiolabeled derivatives thereof. The invention also relates to past controlling compositions comprising the azido-substituted octopamine agonists of the invention.The invention also relates to methods of controlling invertebrate pests by bringing the pest into contact with an invertebrate pest-controlling composition of the invention and to an apparatus for controlling invertebrate pests utilizing the pest-controlling compositions of the invention. The pest-controlling compositions may be used alone or in conjunction with ultraviolet light.The invention also relates to methods for the isolation of octopamine receptor proteins utilizing the radiolabeled azido-substituted octopamine agonists of the invention.
    Type: Grant
    Filed: April 12, 1988
    Date of Patent: January 9, 1990
    Assignee: The General Hospital Corporation
    Inventor: James A. Nathanson
  • Patent number: 4831132
    Abstract: Novel ortho-(mono-substituted amino)phenylimines being intermediates to psychotropic drugs and other drugs are economically and industrially prepared by reacting anilines with nitriles in the presence of a boron trifluoride ether adduct and a halide-type Lewis acid, if necessary together with an organic base. Furthermore, the imines can be hydrolyzed with an acid to afford the corresponding ketones.
    Type: Grant
    Filed: December 30, 1986
    Date of Patent: May 16, 1989
    Assignee: Shionogi & Co., Ltd.
    Inventors: Tsutomu Sugasawa, Kazuyuki Sasakura
  • Patent number: 4785119
    Abstract: Disclosed is a novel compound of 3-aminopyrrolidine having the formula (I): ##STR1## in which R.sup.1 is hydrogen, an alkyl, an aralkyl or an aryl.
    Type: Grant
    Filed: October 7, 1986
    Date of Patent: November 15, 1988
    Assignee: Tokyo Kasei Kogyo Co., Ltd.
    Inventors: Kou Hojo, Anji Sakamoto, Masumi Tsutsumi, Tamotsu Yamada, Kazuhiko Nakazono, Kazuya Ishimori
  • Patent number: 4579951
    Abstract: This invention relates to novel substituted (azacycloalk-2-yl)iminophenols that are useful in the treatment of diarrhea.
    Type: Grant
    Filed: March 19, 1984
    Date of Patent: April 1, 1986
    Assignee: G. D. Searle & Co.
    Inventors: Barnett S. Pitzele, Stella S. T. Yu, Robert W. Hamilton
  • Patent number: 4533739
    Abstract: This invention relates to the novel use of certain aromatic substituted amidines as antidiarrheals.
    Type: Grant
    Filed: October 12, 1982
    Date of Patent: August 6, 1985
    Assignee: G. D. Searle & Co.
    Inventors: Barnett S. Pitzele, Stella S. T. Yu, Robert W. Hamilton, Alan E. Moormann
  • Patent number: 4473394
    Abstract: This invention relates to pyrrole sulfonamides which are useful as herbicides. Typical of the pyrrole sulfonamides of the instant application in N-[(4-methoxy-6-methyl-1,3,5-triazin-2-yl)aminocarbonyl]-2,5-dimethyl-1H-p yrrole-3-sulfonamide.
    Type: Grant
    Filed: September 27, 1982
    Date of Patent: September 25, 1984
    Assignee: E. I. DuPont De Nemours & Company
    Inventors: John C. Budzinski, George Levitt
  • Patent number: 4383112
    Abstract: Chiral Schiff bases according to the general formula: ##STR1## and transition metal complexes thereof, wherein C.sup.* is an asymmetric carbon atom, R.sup.1 and R.sup.2, which may be the same or different are alkyl, aralkyl, aryl or alkaryl, R.sup.3 is hydrogen, alkyl, aralkyl, aryl or alkaryl, R.sup.4 and R.sup.5, which may be the same or different, are hydrogen or lower alkyl or, where n is 1, may with the cyclic ring to which CR.sup.4 R.sup.
    Type: Grant
    Filed: July 8, 1980
    Date of Patent: May 10, 1983
    Assignee: Imperial Chemical Industries Limited
    Inventors: Dale A. Laidler, David J. Milner
  • Patent number: 4377522
    Abstract: There are presented novel benzodiazepine derivatives of the formula ##STR1## wherein R.sup.1 is lower alkyl, lower hydroxyalkyl or lower dialkylaminoalkyl, R.sup.2 and R.sup.3 each are lower alkyl, R.sup.4 is halogen, R.sup.5, R.sup.7 and R.sup.8 each are hydrogen or halogen and R.sup.6 is nitro, amino, lower alkylamino, lower dialkylamino or a group of the formula H.sub.2 N--C(CH.sub.3).sub.2 --CO--NH--, R.sup.9 R.sup.10 N--CO--NH-- or ##STR2## and either R.sup.9 is hydrogen or lower alkyl and R.sup.10 is lower alkyl or lower hydroxyalkyl or R.sup.9 and R.sup.10 together with the nitrogen atom are a 3- to 7-membered heterocycle which, provided it is at least 5-membered, can contain as a ring member an oxygen or sulfur atom or a group of the formula >N--R in which R is hydrogen or lower alkyl,and their pharmaceutically acceptable acid addition salts.
    Type: Grant
    Filed: July 6, 1981
    Date of Patent: March 22, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Quirico Branca, Albert E. Fischli, Andre Szente