Nitrogen Attached Indirectly To Ring Nitrogen Of The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 540/592)
  • Patent number: 9334240
    Abstract: The present invention is in relation to preparation of Imipramine Pamoate by a simple two-step process. The process provides new form of Imipramine Pamoate. The present invention is cost effective, involves mild conditions to beget said compound.
    Type: Grant
    Filed: April 23, 2014
    Date of Patent: May 10, 2016
    Assignee: R.L. FINE CHEM
    Inventors: Andagar Ramakrishna Ramesha, Anjan Kumar Roy
  • Publication number: 20150018543
    Abstract: The present invention relates to 4H-pyrido[1,2-a]pyrimidin-4-one compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.
    Type: Application
    Filed: April 28, 2014
    Publication date: January 15, 2015
    Applicants: Institut Pasteur Korea, INSERM (Institut National de la Sante et de la Recherche Medicale)
    Inventors: Priscille BRODIN, Thierry CHRISTOPHE, Zaesung NO, Jaeseung KIM, Auguste GENOVESIO, Denis Philippe Cedric FENISTEIN, Heekyoung JEON, Fanny Anne EWANN, Sunhee KANG, Saeyeon LEE, Min Jung SEO, Eunjung PARK, Monica CONTRERAS DOMINGUEZ, Ji Youn NAM, Eun Hye KIM
  • Publication number: 20140200210
    Abstract: The present invention relates to a pharmaceutical composition for treating, preventing or improving premature ejaculation, which is taken on demand prior to sexual activity, the composition comprising clomipramine hydrochloride in an amount of 14 to 16 mg, preferably about 15 mg, as an active ingredient. More preferably, the composition of the present invention further comprises pregelatinized starch and sodium starch glycolate. The pharmaceutical composition of the present invention can provide rapid onset of efficacy, reduce a dissolution (absorption) deviation according to the patient's gastrointestinal pH conditions and minimize side effects.
    Type: Application
    Filed: June 28, 2012
    Publication date: July 17, 2014
    Applicant: CTC BIO, INC.
    Inventors: Hong-Ryeol Jeon, Do-Woo Kwon, Bong-Sang Lee, Seong-Shin Kwak, Sun-Ahe Lee, Hyun-Jung Park, Jeong-Hwa Yoo
  • Patent number: 8716278
    Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: May 6, 2014
    Assignee: Pisgah Laboratories, Inc.
    Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
  • Patent number: 8653065
    Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: February 18, 2014
    Assignee: Pisgah Laboratories, Inc.
    Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
  • Patent number: 8586575
    Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.
    Type: Grant
    Filed: April 10, 2012
    Date of Patent: November 19, 2013
    Assignee: Pisgah Laboratories, Inc.
    Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
  • Patent number: 8435979
    Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are triphenyl methane analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, inflammatory, degenerative and vascular diseases, and parasitic infections. The compounds are triphenyl methane analogs of imipramine blue and analogs thereof, as defined herein. The compounds are believed to function by inhibiting tNOX expression, the effects of ROS, and/or the production of HIF2. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.
    Type: Grant
    Filed: December 21, 2009
    Date of Patent: May 7, 2013
    Assignees: Emory University, The United States of America as represented by the Dept of Veterans Affairs
    Inventor: Jack L. Arbiser
  • Publication number: 20120190847
    Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are triphenyl methane analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, inflammatory, degenerative and vascular diseases, including various ocular diseases, and parasitic infections. Representative triphenyl methane analogs include triphenyl methane analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function by inhibiting tNOX expression, the effects of ROS, and/or the production of HIF2. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.
    Type: Application
    Filed: March 6, 2012
    Publication date: July 26, 2012
    Inventor: Jack L. Arbiser
  • Publication number: 20120095217
    Abstract: Fluorinated compounds and methods of making fluorinated compounds are described herein.
    Type: Application
    Filed: January 8, 2010
    Publication date: April 19, 2012
    Inventors: Tobias Ritter, Laura Brass, Curtis Keith, Alan Watson, David J. Greenblatt
  • Publication number: 20120071465
    Abstract: The present invention relates to the compounds useful in the prevention and/or treatment of tumours. More specifically the present invention relates to inhibitors of the activity of the electron transport chains and/or the mitochondrial TCA cycle in glioma-initiating cells (GICs) for use in a method for preventing and/or treating tumours presenting glioma-initiating cells (GICs) in a subject who has undergone a prior removal of a tumour glioma bulk. The present invention further provides a pharmaceutical composition containing the inhibitors of the invention and a screening method for identifying the inhibitors of the invention.
    Type: Application
    Filed: May 20, 2010
    Publication date: March 22, 2012
    Inventors: Virginie Clement, Ivan Radovanovic
  • Patent number: 8039461
    Abstract: An amorphous form of imipramine pamoate, morphologically pure forms, and mixtures of amorphous and morphologically pure imipramine pamoate characterized by differential scanning calorimetry, fourier transform infrared, and powder x-ray diffraction, and pharmaceutical compositions formed therefrom.
    Type: Grant
    Filed: August 23, 2007
    Date of Patent: October 18, 2011
    Assignee: Pisgah Laboratories, Inc.
    Inventors: Vicki Haynes Audia, David William Bristol, Joseph Pike Mitchener, Jr., Clifford Riley King
  • Publication number: 20110243960
    Abstract: The disclosure provides an antigenic composition useful for immunization against P. acnes, K. pneumoniae, S. aureus, or Streptococcus pyogenes. The disclosure provides a method for producing a vaccine for preventing infection and screening agents useful for preventing infection.
    Type: Application
    Filed: December 3, 2009
    Publication date: October 6, 2011
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Richard L. Gallo, Chun-Ming Huang
  • Publication number: 20110245493
    Abstract: The present invention relates to the delivery of drug amines through an inhalation route. Specifically, it relates to aerosols containing drug amines that are used in inhalation therapy. In one aspect of the present invention, a method of delivering an amine drug in an aerosol form is provided. The method comprises: a) heating a coating, which includes an amine drug salt on a substrate contained in a device to a temperature sufficient to volatilize the amine drug from the coating, h) by said heating, forming an amine drug vapor, and c) during said heating, drawing air through said device, condensing said vapor to form aerosol particles containing less than 10% degradation products of the compound.
    Type: Application
    Filed: April 1, 2011
    Publication date: October 6, 2011
    Applicant: ALEXZA PHARMACEUTICALS, INC.
    Inventors: Joshua D. RABINOWITZ, Alejandro C. Zaffaroni
  • 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: 20100311727
    Abstract: Therapeutic amine-arylsulfonamide conjugate compounds, of the general formula: wherein R? is [D-W-], hydroxyl, or alkoxyl; R? is independently [D-W?-], hydrogen, alkoxy, alkyl, cycloalkyl, alkenyl, alkynyl or aryl, or R? and R? together with the nitrogen atom to which they are attached form a 4-, 5-, 6-, 7- or 8-membered ring optionally containing one or two further heteroatoms independently selected from nitrogen, oxygen and sulfur; D is independently a therapeutic amine radical comprising at least one nitrogen atom and optionally at least one oxygen atom coupled to W or W? by a nitrogen or oxygen atom; W and W? are a chemical bond or linker; wherein either R? is [D-W-] or at least one R? is [D-W?-], and pharmaceutically acceptable esters, amides, salts or solvates thereof, pharmaceutical compositions containing same, methods for their preparation, and their use in treating psychiatric, neurologic and metabolic disorders are disclosed.
    Type: Application
    Filed: June 8, 2010
    Publication date: December 9, 2010
    Applicant: ALGEBRA, INC.
    Inventors: Philip F. MORGAN, James L. KELLEY
  • Publication number: 20100311728
    Abstract: Provided herein methods of screening for potential antidepressant compounds effective to increase production of cellular CDP-diacylglycerol and synthesis of inositol phospholipid in depression-related areas of the brain. Also, provided are methods of diagnosing and treating depressive or mood disorders in a subject by administering these screened antidepressant compounds. Further provided is a method of determining the therapeutic efficacy of an antidepressant drug regimen by comparing the ratio of CDP-diacylglycerol/inositol phosphate after treatment to a basal ratio in a subject.
    Type: Application
    Filed: July 23, 2010
    Publication date: December 9, 2010
    Inventor: Ashiwel S. Undieh
  • 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
  • Publication number: 20100160296
    Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are triphenyl methane analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, inflammatory, degenerative and vascular diseases, and parasitic infections. The compounds are triphenyl methane analogs of imipramine blue and analogs thereof, as defined herein. The compounds are believed to function by inhibiting tNOX expression, the effects of ROS, and/or the production of HIF2. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.
    Type: Application
    Filed: December 21, 2009
    Publication date: June 24, 2010
    Applicant: EMORY UNIVERSITY
    Inventor: Jack L. Arbiser
  • Publication number: 20100159596
    Abstract: Methods and small molecule compounds for stem cell differentiation are provided.
    Type: Application
    Filed: September 16, 2009
    Publication date: June 24, 2010
    Applicants: Burnham Institute for Medical Research, Human BioMolecular Research Institute
    Inventors: Mark Mercola, Marcia Dawson, John Cashman
  • Patent number: 7718649
    Abstract: An amorphous form of imipramine pamoate, morphologically pure forms, and mixtures of amorphous and morphologically pure imipramine pamoate characterized by differential scanning calorimetry, fourier transform infrared, and powder x-ray diffraction, and pharmaceutical compositions formed therefrom.
    Type: Grant
    Filed: November 10, 2006
    Date of Patent: May 18, 2010
    Assignee: Pisgah Labs, Inc.
    Inventors: Clifford Riley King, David William Bristol, Vicki Haynes Audia, Joseph Pike Mitchener, Jr.
  • Publication number: 20090259039
    Abstract: Drug substances comprising a pharmaceutically acceptable organic acid addition salt of amine containing pharmaceutically active compounds useful for the treatment of a therapeutic ailment administration and exhibiting prophylactic properties when employed in non-therapeutic administration.
    Type: Application
    Filed: April 3, 2008
    Publication date: October 15, 2009
    Inventors: David William Bristol, Clifford Riley King, Joseph Pike Mitchener, JR., Vicki Haynes Audia
  • Patent number: 7056911
    Abstract: The invention relates to pharmaceutically active compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention and particularly useful for the treatment or prophylaxis of diseases associated with parasitic infection such as pneumocystis pneumonia, toxoplasmosis, cryptosporidiosis, leischmaniasis and malaria.
    Type: Grant
    Filed: January 25, 2000
    Date of Patent: June 6, 2006
    Assignee: Dana-Farber Cancer Institute
    Inventor: Andre Rosowsky
  • Patent number: 6908915
    Abstract: A compound having a general formula (II) wherein R1 is saturated or unsaturated alkyl, amino-alcohol, diamino, cycloalkyl, and C(?O)(CH2)nNR?R?, (CH2)nCHOHCH2NR?R?, wherein n is an integer, RQ, RT, R?, and R? are each independently a hydrogen, halogen, hydroxyl, saturated, unsaturated, aliphatic, or branched alkyl, substituted or unsubstituted (CH2)m-(hetero)aryl, and sulfonylamide; q and r are each an integer independently selected from 1-4; and pharmaceutically acceptable salts thereof, and the new therapeutic uses thereof and similar compounds as defibrillating, and/or anti-fibrillatory, and/or anti-arrhythmic and/or anti-ischemic drugs.
    Type: Grant
    Filed: August 27, 2000
    Date of Patent: June 21, 2005
    Assignee: Technion Research & Development Foundation Ltd.
    Inventors: Mordechai Erez, Ofra Levy, Ehud Keinan
  • Publication number: 20040142921
    Abstract: Disclosed is the preparation and pharmaceutical use of substituted arylalcanoic acid derivatives of Formula I, wherein ring A, ring B, R1, R2, R3, R4, R5, X, Alk1, Alk2, Ar1, and Ar2 are as defined in the specification. These compounds, as selective agonists activating peroxisome proliferator-activated receptors (PPAR), in particularly the RXR/PPARalpha, RXR/PPARgamma, and RXR/PPARdelta heterodimers, are useful in the treatment and/or prevention of type 2 diabetes and associated metabolic syndrome such as hypertension, obesity, insulin resistance, hyperlipidemia, hyperglycemia, hypercholesterolemia, atherosclerosis, coronary artery disease, and other cardiovascular disorders with improved side effects profile commonly associated with conventional PPARgamma agonists.
    Type: Application
    Filed: November 18, 2003
    Publication date: July 22, 2004
    Inventors: Xian-Ping Lu, Zhibin Li, Chenzhong Liao, Leming Shi, Zhende Liu, Baoshun Ma, Zhiqiang Ning, Song Shan, Tuo Deng
  • Patent number: 6569849
    Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula wherein X, Y, Z, A, R1, R2, r and s are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to secretion and circulation of insulin antagonising peptides.
    Type: Grant
    Filed: October 3, 1997
    Date of Patent: May 27, 2003
    Assignee: Novo Nordisk A/S
    Inventors: Tine Krogh Jorgensen, Rolf Hohlweg, Peter Madsen, Knud Erik Andersen, Svend Treppendahl, Uffe Bang Olsen, Zdenek Polivka, Alexandra Silhankova, Karel Sindelar, Vladimir Valenta, Tomas Kalisz
  • Patent number: 6384217
    Abstract: 5-Cyano-10-Hydroxy-10,11-Dihydro-5H-Dibenzi[b,f]azepine and the process for its preparation.
    Type: Grant
    Filed: February 17, 2001
    Date of Patent: May 7, 2002
    Assignee: Farchemia S.R.L.
    Inventors: Citterio Attilio, Breviglieri Gabriele, Giacomo Bruno
  • Patent number: 6214816
    Abstract: The compounds are N-substituted azaheterocyclic compounds of formula I wherein R1 and R2 independently are hydrogen, halogen, trifluoromethyl, hydroxy, C1-6-alkyl or C1-6-alkoxy; and Y is >N—CH2— wherein only the underscored atom participates in the ring system; and X is —C(R6R7)—, —CH2CH2—, —CH═CH—CH2—, —CH2—CH═CH—, —CH2—(C═O)—, —(C═O)—CH2—, —CH2CH2CH2—, —CH═CH—, CH(R10)CH2—, —CH2CH(R10) or —(C═O)— wherein R6 and R7 independently are hydrogen or C1-6-alkyl and wherein R10 is C1-6-alkyl or phenyl; and r is 0, 1 or 2; and Z is selected from wherein A is —CH2—, —O—, —S— or —N(R5)— wherein R5 is H or C1-6-alkyl; and R3 is —(CH2)pCOR4 wherein p is 1, 2, 3 or 4 and R4 is OH, NH2, NHOH or C1-6-alkoxy; or a pharmaceutically acceptable salt th
    Type: Grant
    Filed: March 10, 1999
    Date of Patent: April 10, 2001
    Assignee: Novo Nordisk A/S
    Inventors: Rolf Hohlweg, Tine Krogh Jørgensen, Knud Erik Andersen, Uffe Bang Olsen, Zdenék Polivka, Karel Sindelar
  • Patent number: 6071901
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids andy esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: April 1, 1998
    Date of Patent: June 6, 2000
    Assignee: Novo Nordisk A/S
    Inventors: Florenzio Zaragossa Dorwald, Knud Erik Andersen, Rolf Hohlweg, Peter Madsen, Tine Krogh J.o slashed.rgensen, Uffe Bang Olsen, Henrik Sune Andersen, Svend Treppendahl, Polivka Zdenek, Silhankova Alexandra, Sindelar Karel
  • Patent number: 6040302
    Abstract: The present invention relates to 1,4-disubstituted piperazines of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for the treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.
    Type: Grant
    Filed: March 18, 1999
    Date of Patent: March 21, 2000
    Assignee: Novo Nordisk A/S
    Inventors: Rolf Hohlweg, Peter Madsen, Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Brett Watson, Zdenek Polivka, Otylie Konigova, Martina Kovandova, Alexandra Silhankova, Vladimir Valenta
  • Patent number: 5929235
    Abstract: An aromatic tertiary amine compound of formula (I): ##STR1## wherein (A) and (B) are each a substituted or unsubstituted vinylene or o-arylene group; R.sup.1 to R.sup.4 are each a halogen atom, or a substituted or unsubstituted alkyl, aryl, alkoxy, aryloxy, dialkylamino, N-alkyl-N-arylamino or diarylamino group; R.sup.5 is a halogen atom, or a substituted or unsubstituted alkyl, alkoxy or dialkylamino group; h, i, j, k and l are each an integer of 0-4; and m is an integer of 1-6.
    Type: Grant
    Filed: August 19, 1997
    Date of Patent: July 27, 1999
    Assignee: Fuji Photo Film Co., Ltd.
    Inventor: Tadahisa Sato
  • Patent number: 5916889
    Abstract: The present invention relates to 1,4-disubstituted piperazines of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for the treatment of indications caused by or related to the secretion and circulation of insulin antagonizing peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.
    Type: Grant
    Filed: October 3, 1997
    Date of Patent: June 29, 1999
    Assignee: Novo Nordisk A/S
    Inventors: Rolf Hohlweg, Peter Madsen, Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Brett Watson, Zdenek Polivka, Otylie Konigova, Martina Kovandova, Alexandra Silhankova, Vladimir Valenta
  • Patent number: 5731307
    Abstract: The instant invention is directed to compounds, compositions and antipsychotic methods of use wherein the compounds are of formula I: ##STR1## wherein Y is an imide or benzoyl alkyl group and X is a cycloalkyl, phenyl or dibenzoazepinyl group.
    Type: Grant
    Filed: June 16, 1997
    Date of Patent: March 24, 1998
    Assignee: Pfizer, Inc.
    Inventor: Kishor A. Desai
  • Patent number: 5721254
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: October 18, 1995
    Date of Patent: February 24, 1998
    Assignee: Novo Nordisk A/S
    Inventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
  • Patent number: 5716949
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: March 28, 1996
    Date of Patent: February 10, 1998
    Assignee: Novo Nordisk A/S
    Inventors: Henrik Sune Andersen, Knud Erik Andersen, Rolf Hohlweg, Peter Madsen, Tine Krogh J.o slashed.rgensen, Uffe Bang Olsen
  • Patent number: 5693649
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: October 18, 1995
    Date of Patent: December 2, 1997
    Assignee: Novo Nordisk A/S
    Inventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
  • Patent number: 5688788
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: November 18, 1997
    Assignee: Novo Nordisk A/S
    Inventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
  • Patent number: 5668129
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: March 27, 1996
    Date of Patent: September 16, 1997
    Assignee: Novo Nordisk A/S
    Inventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
  • Patent number: 5629421
    Abstract: There are provided a hydrazone compound represented by formula (I), an electrophotographic photoreceptor which has a photosensitive layer containing the compound on an electrically conductive support, and an organic electroluminescent element containing the compound as a charge transporting material: ##STR1## wherein Ar.sub.1 represents a substituted or unsubstituted phenylene group, a substitued or unsubstituted naphthylene group, a substitued or unsubstituted biphenylene group, or a substituted or unsubstituted anthrylene group, Ar.sub.2 represents a substituted or unsubstituted aryl group, R.sub.1 and R.sub.2 each independently represents a hydrogen atom, a halogen atom, an unsubstituted alkyl group, or an unsubstituted alkoxy group, R.sub.3 represents an unsubstituted alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group, Z represents an ethylene group or a vinylene group, and n is 0 or 1.
    Type: Grant
    Filed: January 18, 1996
    Date of Patent: May 13, 1997
    Assignee: Hodagaya Chemical Co., Ltd.
    Inventors: Atsushi Takesue, Yasuo Murakami, Takanobu Watanabe, Mitsutoshi Anzai
  • Patent number: 5614419
    Abstract: Immunoassay methods and reagents for the specific quantification of amitriptyline or nortriptyline in a test sample are disclosed employing antibodies prepared with amitriptyline or nortriptyline derivatives of the Formula III: ##STR1## wherein for amitriptyline, R is CH.sub.3, and for nortriptyline, R is H. The present invention also describes the synthesis of unique fluorescein tracers of the structure of Formula IV and Formula V: ##STR2## wherein for a specific amitriptyline immunoassay, W.sub.1 is a heteroatom linked to the aromatic ring at the 2 or 3 position, and for a specific nortriptyline immunoassay, W.sub.2 is two heteroatoms linked together and attached to the aromatic ring at the 2 or 3 position, and wherein Q is a detectable moiety, preferably fluorescein or a fluorescein derivative.
    Type: Grant
    Filed: August 5, 1994
    Date of Patent: March 25, 1997
    Assignee: Abbott Laboratories
    Inventors: Maciej Adamczyk, Jeffrey R. Fishpaugh, Donald Johnson, Daryl E. Hartter
  • Patent number: 5599929
    Abstract: An improved method for preparing opipramol (I) is disclosed, wherein iminostilbene (II) is reacted with 1-bromo-3-chloropropane in the presence of a weak base selected from a hydrogen phosphate salt and an acetate salt and in the presence of a phase transfer agent to produce N-(3-halopropyl)iminostilbene (III), which is mixture of N-(3-chloropropyl)iminostilbene and N-(3-bromopropyl)iminostilbene, and then N-(3-halopropyl)iminostilbene is reacted with N-(2-hydroxyethyl)piperazine to form opipramol, as shown in the following equations, where X is chlorine or bromine.
    Type: Grant
    Filed: November 9, 1994
    Date of Patent: February 4, 1997
    Assignee: Taro Pharmaceutical Industries Ltd
    Inventors: Daniella Gutman, Mishel Ashkar
  • Patent number: 5599815
    Abstract: Compounds represented by the formula (I) and pharmacologically acceptable salts thereof: ##STR1## These compounds have little extrapyramidal effect and thus are effective as an anti-psychotic agent having few side effects.
    Type: Grant
    Filed: December 20, 1994
    Date of Patent: February 4, 1997
    Assignee: Meiji Seika Kabushiki Kaisha
    Inventors: Yoshimasa Fukuda, Toshiro Sasaki, Yuuko Nakatani, Yasuyuki Ichimaru, Taiichiro Imanishi
  • Patent number: 5595989
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: January 3, 1995
    Date of Patent: January 21, 1997
    Assignee: Novo Nordisk A/S
    Inventors: Knud E. Andersen, Uffe B. Olsen, Hans Petersen, Frederik Gr.o slashed.nvald, Ursula Sonnewald, Tine K. J.o slashed.rgensen, Henrik S. Andersen
  • Patent number: 5578500
    Abstract: Immunoassay methods and reagents for the specific quantification of imipramine or desipramine in a test sample are disclosed. The measurement of imipramine or desipramine is accomplished in a specific immunoassay employing antibodies prepared with imipramine or desipramine derivatives of the Formula III: ##STR1## wherein P is an immunogenic carrier material, X is two heteroatoms, Y is a linking group comprising from 1 to 6 carbon atoms and P is an immunogenic carrier material, and wherein for imipramine, R is CH.sub.3, and for desipramine, R is H.The present invention also describes the synthesis of unique labeled reagents of the structure of the Formula IV: ##STR2## wherein Z is a linking group comprising 1 to 4 carbon atoms and 0 to 2 heteroatoms and Q is a detectable moiety, preferably fluorescein or a fluorescein derivative, and wherein for imipramine, R.sub.1 is CH.sub.3, and for desipramine, R.sub.1 is H.
    Type: Grant
    Filed: August 5, 1994
    Date of Patent: November 26, 1996
    Assignee: Abbott Laboratories
    Inventors: Maciej Adamczyk, Charles A. Harrington, Donald Johnson
  • Patent number: 5569653
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 29, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 5208330
    Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl, or oxygen-bridged diaryllowerallyl; A is a direct bond or (CHR.sub.3).sub.m, m being 1-3; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.5 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl; Y is O, S or NR.sub.7 ; and each R.sub.2, each R.sub.3 and R.sub.
    Type: Grant
    Filed: February 25, 1992
    Date of Patent: May 4, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Gregory M. Shutske, Richard C. Effland
  • Patent number: 5204348
    Abstract: Novel heterocyclic compounds, which are represented by the following general formula, useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.
    Type: Grant
    Filed: December 3, 1991
    Date of Patent: April 20, 1993
    Assignee: Mitsui Toatsu Chemicals Inc.
    Inventors: Nobuyuki Fukazawa, Makoto Odate, Tsuneji Suzuki, Kengo Otsuka, Takashi Tsuruo, Wakao Sato
  • Patent number: 5182387
    Abstract: Novel bis-dibenzoazepine compounds useful in the treatment of malaria and drug-resistant malaria.
    Type: Grant
    Filed: October 30, 1991
    Date of Patent: January 26, 1993
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Jules Freedman, Alan J. Bitonti
  • Patent number: 4847374
    Abstract: N,N-(dibenzohexatrienylene)urea medicaments can be manufactured in a smooth one-step reaction by reacting a corresponding N,N-(dibenzohexatrienylene)amine with cyanic acid.
    Type: Grant
    Filed: January 19, 1988
    Date of Patent: July 11, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Georg Acklin, Ernst Aufderhaar, Gunter Kaupp, Bernhard Raz, Ulrich Vogel
  • Patent number: 4772697
    Abstract: Tricyclic antidepressant functionalized compounds are provided for conjugation through a side chain to antigenic compounds, particularly poly(amino acids), and enzymes. The antigenic conjugates are employed for the production of antibodies and together with the enzyme conjugates find particular use in immunoassays for the determination or detection of the total amount of tricyclic antidepressants present in a sample.
    Type: Grant
    Filed: August 21, 1986
    Date of Patent: September 20, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Christine G. Collins, Marcel R. Pirio, Prithipal Singh
  • Patent number: 4668671
    Abstract: This invention describes tricyclic derivatives which are useful as histamine H.sub.1 -antagonists. A particular compound of this invention is 3-[3-(pyrido[3,2-b][1,4]-benzothiazin-10-yl)propylamino]-4-(pyrid-4-ylmeth ylamino)-1,2,5-thiadiazole-1-oxide.
    Type: Grant
    Filed: April 23, 1986
    Date of Patent: May 26, 1987
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Andrew D. Gribble, Robert J. Ife