Beta Hydroxy Phenethylamines (i.e., Hydroxy And The Benzene Ring Are Bonded Directly To The Same Carbon Of The Chain Which Consists Of Two Carbons; H Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/363)
  • Patent number: 9193669
    Abstract: Provided are compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Grant
    Filed: February 7, 2014
    Date of Patent: November 24, 2015
    Assignee: ACUCELA INC.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Feng Hong, Ryo Kubota, Jennifer Gage
  • Patent number: 8895738
    Abstract: Disclosed are compounds of Formula 1, wherein R1 is phenyl or pyridinyl, each optionally substituted with Q and up to 3 substituents independently selected from R2; each R2 is independently halogen, cyano, SF5, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio or C1-C4 haloalkylthio; and Q is phenyl or pyridinyl, each optionally substituted with up to 5 substituents independently selected from the group consisting of halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy and C1-C4 haloalkoxy. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: November 25, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventor: Thomas Francis Pahutski, Jr.
  • Patent number: 8389771
    Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Grant
    Filed: August 3, 2011
    Date of Patent: March 5, 2013
    Assignee: Acucela, Inc.
    Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
  • Patent number: 8299307
    Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Grant
    Filed: June 30, 2008
    Date of Patent: October 30, 2012
    Assignee: Acucela Inc.
    Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Mark W Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
  • Publication number: 20110152332
    Abstract: The present invention relates to novel pesticidal azolidine derivatives as well as to oxazolidinone derivatives and their use as pesticides for combating animal parasites which occur in the agrochemical field and in the field of veterinary medicine, respectively. wherein X, m, R?, Q, G, U, l, A1 to A4 and R are as defined herein.
    Type: Application
    Filed: November 1, 2010
    Publication date: June 23, 2011
    Applicant: Bayer CropScience AG
    Inventors: Tetsuya Murata, Mamoru Hatazawa, Peter Brüchner, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Görgens
  • Publication number: 20100093865
    Abstract: Provided are sulphur-linked compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: September 2, 2009
    Publication date: April 15, 2010
    Applicant: Acucela, Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Ryo Kubota
  • Publication number: 20090280483
    Abstract: The present invention provides methods for screening compounds which inhibit activation of a member of the IL-6 signaling pathways, comprising: (a) a positive screening step using a cell capable of being killed by IL-6 stimulation to select compounds which inhibit death of the cell when it is stimulated by IL-6; and then (b) a biochemical screening step to further select compounds which inhibit activation of a member of the IL-6 signaling pathways by a biochemical means from the compounds selected in step (a). The present invention also provides compounds which inhibit activation of a member of the IL-6 signaling pathways identified using said methods.
    Type: Application
    Filed: November 22, 2005
    Publication date: November 12, 2009
    Inventors: Toshio Kitamura, Toshiyuki Kawashima
  • Publication number: 20090112025
    Abstract: The present invention provides a novel hydrogenation catalyst, process of preparing the catalyst and process for the preparation of optically active L-norephedrine, [(1R,2S)-2-amino-1-phenyl-1-propanol] by a catalytic hydrogenation process, said catalyst comprising of finely divided nickel metal containing a metal from group III A of the periodic table as an activator and a metal from group VI B or VIII as promoter,
    Type: Application
    Filed: February 4, 2008
    Publication date: April 30, 2009
    Applicant: Emmellen Biotech Pharmaceuticals Limited
    Inventor: Sunil Vaman Joshi
  • Publication number: 20090062353
    Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: June 30, 2008
    Publication date: March 5, 2009
    Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
  • Patent number: 7402698
    Abstract: The present invention is directed to secondary amino- and cycloamino-cycloalkanol derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
    Type: Grant
    Filed: October 12, 2004
    Date of Patent: July 22, 2008
    Assignee: Wyeth
    Inventors: Paige Erin Mahaney, Michael Byron Webb, Lori Krim Gavrin, Eugene John Trybulski
  • Patent number: 7214826
    Abstract: The invention relates to amine compounds as well as methods and materials involved in modulating neurotransmitter reuptake. Specifically, the invention provides amine compounds, methods for synthesizing amine compounds, and methods for inhibiting neurotransmitter reuptake.
    Type: Grant
    Filed: May 25, 2005
    Date of Patent: May 8, 2007
    Assignees: Mayo Foundation for Medical Education and Research, Virginia Tech Intellectual Properties, Inc.
    Inventors: Elliott Richelson, Paul R. Carlier
  • Patent number: 7087765
    Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).
    Type: Grant
    Filed: March 9, 2004
    Date of Patent: August 8, 2006
    Assignee: NPS Pharmaceuticals, Inc.
    Inventors: Alan L. Mueller, Scott T. Moe
  • Patent number: 7064236
    Abstract: The invention relates to substituted 1-aryl-but-3-enylamine and 1-aryl-but-2-enylamine compounds, to a method for the production thereof, to medicaments containing said compounds and to their use in the production of medicaments.
    Type: Grant
    Filed: January 5, 2004
    Date of Patent: June 20, 2006
    Assignee: Grunenthal GmbH
    Inventors: Bernd Sundermann, Corinna Sundermann, Helmut Buschmann, Babette-Yvonne Koegel
  • Patent number: 6995286
    Abstract: A process for making optically pure (R) and (S) salbutamol comprises obtaining the (R) or (S) isomer of either salbutamol or a salbutamol precursor in substantially optically pure form by resolving a racemic or optically impure mixture of enantiomers of salbutamol or of said precursor with either (L) or (D) tartaric acid, and where necessary converting said isomer of said precursor into either (R or (S) salbutamol respectively; then optionally converting said optically pure (R) and/or (S) salbutamol into a pharmaceutically acceptable salt.
    Type: Grant
    Filed: December 10, 2001
    Date of Patent: February 7, 2006
    Assignee: Cipla Limited
    Inventors: Yusuf Khwaja Hamied, Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao
  • Patent number: 6700018
    Abstract: The invention relates to amine compounds as well as methods and materials involved in modulating neurotransmitter reuptake. Specifically, the invention provides amine compounds, methods for synthesizing amine compounds, and methods for inhibiting neurotransmitter reuptake.
    Type: Grant
    Filed: July 17, 2001
    Date of Patent: March 2, 2004
    Assignees: Mayo Foundation for Medical Education and Research, Virginia Tech Intellectual Properties
    Inventors: Elliott Richelson, Paul R. Carlier
  • Patent number: 6653508
    Abstract: Substituted 3-amino-2-benzyl-1-phenlypropane derivatives, methods for preparing them, pharmaceutical compositions containing them, and methods of using them to treat various medical conditions.
    Type: Grant
    Filed: January 16, 2002
    Date of Patent: November 25, 2003
    Assignee: Gruenenthal GmbH
    Inventors: Michael Sattlegger, Helmut Buschmann, Babette-Yvonne Koegel
  • Patent number: 6586633
    Abstract: The present invention relates to amine derivatives represented by formula (1) or salts thereof. R3 represents C1-C3 alkyl, hydroxylated C1-C5 alkyl, C1-C5 acyl; C2-C5 alkenyl, or a halogen atom; and k, l, and m are each an integer of 1 to 4.) Exhibiting excellent antifungal effect, these compounds are highly useful as antifungal agents, antifungal compositions, drugs, etc.
    Type: Grant
    Filed: April 5, 2001
    Date of Patent: July 1, 2003
    Assignee: Pola Chemical Industries, Inc.
    Inventors: Masayuki Yuasa, Yukio Kawazu, Toshimitsu Suzuki, Toshiro Majima, Takao Itoh, Takuji Nakashima, Akira Nozawa, Hiroyuki Takimoto, Kouji Yokoyama
  • Patent number: 6576793
    Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.
    Type: Grant
    Filed: August 14, 2000
    Date of Patent: June 10, 2003
    Assignee: Theravance, Inc.
    Inventors: Edmund J. Moran, John H. Griffin, Seok-Ki Choi
  • 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
  • Patent number: 6528686
    Abstract: An (R)-2-amino-1-phenylethanol derivative shown by the general formula (IIa) wherein R1 and R5 represent a hydrogen atom, etc.; R2, R3 and R4 independently represent a halogen atom, etc., or a salt thereof, can readily be produced (1) by permitting a microorganism belonging to the genus Rhodosporidium, the genus Comamonas or the like to act on a mixture of corresponding (R)-form and (S)-form to asymmetrically utilize, or (2) by permitting a microorganism belonging to the genus Lodderomyces, the genus Pilimelia or the like to act on a corresponding aminoketone derivative to asymmetrically reduce. An (R,R)-1-phenyl-2-[(2-phenyl-1-alkylethyl)amino]ethanol derivative having a high optical purity can easily be obtained from the compound of the formula (IIa) or a salt thereof. Said derivative is useful as an intermediate for producing an anti-obesity agent and so on.
    Type: Grant
    Filed: June 19, 2000
    Date of Patent: March 4, 2003
    Assignee: Daicel Chemical Industries, Ltd.
    Inventors: Hidekazu Akamatsu, Noritsugu Yamasaki
  • Patent number: 6495685
    Abstract: A process for preparing a piperazine derivative represented by the formula (V): comprising reacting 1-methyl-3-phenylpiperazine with 2-chloro-3-cyanopyridine in an aprotic polar organic solvent in the presence of a base and an alkali metal halide. The piperazine derivative and its oxalate are compounds useful as preparation intermediates of mirtazapine.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: December 17, 2002
    Assignee: Sumika Fine Chemicals Co., Ltd.
    Inventors: Chiharu Maeda, Eiichi Iishi, Weiqi Wang, Yoshiyuki Imamiya
  • Publication number: 20020143034
    Abstract: A compound of the formula (I): 1
    Type: Application
    Filed: April 10, 2002
    Publication date: October 3, 2002
    Applicant: Fujisawa Pharmaceutical Co. Ltd.
    Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Takeshi Kato, Naoaki Fujii, Kenichi Washizuka, Yasuyo Tomishima, Hisashi Takasugi, Yutaka Kohno, Nobuhiro Yamamoto, Naoko Unami, Hirohumi Ishikawa
  • Patent number: 6458817
    Abstract: This invention provides compounds of Formula I having the structure wherein R1, R2, R3, R4, R5, R6, Y, Z, m, n, and are as defined hereinbefore or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: October 1, 2002
    Assignee: Wyeth
    Inventors: Dominick Anthony Quagliato, Patrick Michael Andrae
  • Patent number: 6420613
    Abstract: A method of preparing a reduced product by efficiently reducing an unsaturated organic compound by using, as a reducing agent, a trichlorosilane which is industrially cheaply available and is easy to handle, and a reducing agent therefor. A reduced product of an unsaturated organic compound is obtained by mixing the unsaturated organic compound and a trichlorosilane together to reduce the unsaturated organic compound in the presence of a compound that forms a silicon complex having five coordinations upon acting on the trichlorosilane such as an N-formylated product of a secondary amine having not less than 3 carbon atoms. The invention further provides a reducing agent comprising a particular silicon complex.
    Type: Grant
    Filed: December 11, 2000
    Date of Patent: July 16, 2002
    Assignee: Tokuyama Corporation
    Inventors: Fumiaki Iwasaki, Yoshihiro Matsumura, Osamu Onomura, Kenji Tanaka
  • Patent number: 6211245
    Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hyproxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).
    Type: Grant
    Filed: November 4, 1998
    Date of Patent: April 3, 2001
    Assignee: NPS Pharmaceuticals, Inc.
    Inventors: Alan L. Mueller, Scott T. Moe
  • Patent number: 6114582
    Abstract: An (R)-2-amino-1-phenylethanol derivative shown by the general formula (IIa) ##STR1## wherein R.sup.1 and R.sup.5 represent a hydrogen atom, etc.; R.sup.2, R.sup.3 and R.sup.4 independently represent a halogen atom, etc., or a salt thereof, can readily be produced (1) by permitting a Microorganism belonging to the genus Rhodosporidium, the genus Comamonas or the like to act on a mixture of corresponding (R)-form and (S)-form to asymmetrically utilize, or (2) by permitting a microorganism belonging to the genus Lodderomyces, the genus Pilimelia or the like to act on a corresponding aminoketone derivative to asymmetrically reduce. An (R,R)-1-phenyl-2-[(2-phenyl-1-alkylethyl) amino]ethanol derivative having a high optical purity can easily be obtained from the compound of the formula (IIa) or a salt thereof. Said derivative is useful as an intermediate for producing an anti-obesity agent and so on.
    Type: Grant
    Filed: June 11, 1998
    Date of Patent: September 5, 2000
    Assignee: Daicel Chemical Industries, Ltd.
    Inventors: Kazuaki Furukawa, Takayuki Abe, Hidekazu Akamatsu
  • Patent number: 6008412
    Abstract: The present invention relates to processes for resolving N-methyl-3(R,S)-hydroxy-3-phenylpropylamine and N,N-dimethyl-3 (R,S) -hydroxy-3-phenylpropylamine with the isomers of mandelic acid and the resulting salts.
    Type: Grant
    Filed: March 26, 1999
    Date of Patent: December 28, 1999
    Assignee: Eli Lilly and Company
    Inventor: Andrew Michael Ratz
  • Patent number: 5656619
    Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 12, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5545745
    Abstract: The invention relates to a method for producing albuterol by the resolution of a mixture of enantiomers of methyl 5-[2-[(1,1-dimethylethyl)amino]-1-hydroxyethyl]-2-(phenylmethoxy)benzoate or .alpha.-[[(1,1-dimethylethyl)amino]methyl]-4-(phenylmethoxy)-1,3-benzenedi methanol using a chiral acid such as (+/-) di-toluoyltartaric acid or (+/-) di-benzoyltartaric acid.
    Type: Grant
    Filed: January 20, 1995
    Date of Patent: August 13, 1996
    Assignee: Sepracor, Inc.
    Inventors: Yun Gao, Charles M. Zepp
  • Patent number: 5527821
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: June 18, 1996
    Assignee: Pharmacia AB
    Inventors: Nils-Erik Willman, Bengt C. H. Sjogren, Lennart G. Nordh, Gustav L. Persson
  • Patent number: 5519062
    Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.
    Type: Grant
    Filed: May 23, 1994
    Date of Patent: May 21, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Hamer, Brian S. Freed, Gregory H. Merriman
  • Patent number: 5442118
    Abstract: A method for the enantioselective reduction of an .alpha.-iminoketone to an .alpha.-aminoalcohol is disclosed. The method utilizes a borane reducing agent as the reducing agent and a chiral 1,3,2-oxazaborole as the catalyst. The method is applied to the synthesis of R-albuterol from methyl 5-acetylsalicylate in high yield and high optical purity.
    Type: Grant
    Filed: April 22, 1994
    Date of Patent: August 15, 1995
    Assignee: Sepracor, Inc.
    Inventors: Yun Gao, Yaping Hong, Charles M. Zepp
  • Patent number: 5283359
    Abstract: The preparation of arylethanolamines, and in particular albuterol (salbutamol), together with their novel boron, acetal and hemi-acetal intermediates is described.
    Type: Grant
    Filed: March 1, 1993
    Date of Patent: February 1, 1994
    Assignee: Schering Corp.
    Inventors: Chou-Hong Tann, T. K. Thiruvengadam, John Chiu, Michael Green, Timothy L. McAllister, Cesar Colon, Junning Lee
  • Patent number: 5283262
    Abstract: The invention provides compounds of the general formula (I) ##STR1## or a physiologically acceptable salt or solvate thereof, wherein Q represents a 1- or 2-naphthalenyl group.The compounds have a stimulant action at .beta..sub.2 -adrenoreceptors and may be used in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.
    Type: Grant
    Filed: December 23, 1991
    Date of Patent: February 1, 1994
    Assignee: Glaxo Group Limited
    Inventors: William L. Mitchell, Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, David Hartley
  • Patent number: 5248823
    Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: December 4, 1992
    Date of Patent: September 28, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5235103
    Abstract: A process for the preparation of phenylethanolaminotetralins of formula ##STR1## wherein X is hydrogen, a halogen, a trifluoromethyl or a lower alkyl group and R.sup.o is hydrogen or a methyl group substituted by a carboxy or a lower carbalkoxy group, which comprises treating a mandelic acid with a 2-amino-7-hydroxytetralin, optionally alkylating with a lower alkyl haloacetate and reducing the amido group of the mandelamide into a methyleneamino group. The mandelamides intermediates are novel.
    Type: Grant
    Filed: December 15, 1992
    Date of Patent: August 10, 1993
    Assignee: Sanofi
    Inventors: Robert Boigegrain, Roberto Cecchi, Sergio Boveri
  • Patent number: 5198587
    Abstract: Phenethylamine derivatives shown by the general formula ##STR1## wherein Ro represents a lower alkyl group; R.sub.1 represents a lower alkyl group or a lower alkoxy group; R.sub.2 represents hydrogen atom or a hydroxyl group; R.sub.3 and R.sub.4 each represents hydrogen atom or a lower alkyl group; R.sub.5 represents hydrogen atom or a lower alkoxy group; X represents oxygen atom or a methylene group; m is an integer of 1-3; and n is an integer of 0-2 and the acid addition salts thereof.These compounds exhibit a strong .alpha.-adrenergic blocking action and are useful as an antihypertensive agent.
    Type: Grant
    Filed: July 30, 1991
    Date of Patent: March 30, 1993
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kazuo Imai, Kunihiro Niigata, Takashi Fujikura, Shinichi Hashimoto, Toichi Takenaka, Kazuo Honda
  • Patent number: 5198586
    Abstract: A process for the preparation of phenylethanolaminotetralins of formula ##STR1## wherein X is hydrogen, a halogen, a trifluoromethyl or a lower alkyl group and R.degree. is hydrogen or a methyl group substituted by a carboxy or a lower carbalkoxy group, which comprises treating a mandelic acid with a 2-amino-7-hydroxytetralin, optionally alkylating with a lower alkyl haloacetate and reducing the amido group of the mandelamide into a methyleneamino group. The mandelamides intermediates are novel.
    Type: Grant
    Filed: October 25, 1990
    Date of Patent: March 30, 1993
    Assignee: Sanofi
    Inventors: Robert Boigegrain, Roberto Cecchi, Sergio Boveri
  • Patent number: 5189219
    Abstract: The present invention is concerned with the preparation of erythro N-substituted vicinal aminoalcohol derivatives from hydroxyl-protected cyanohydrin derivatives by successive Grignard reaction, transimination using a primary amine, reduction of the resulting imine and removal of the hydroxyl-protecting group. The products are obtained either as a racemate or in an optically pure form, depending upon the stereochemical composition of the cyanohydrin derivatives.
    Type: Grant
    Filed: December 19, 1991
    Date of Patent: February 23, 1993
    Assignee: Duphar International Research B.V.
    Inventors: Johannes Brussee, Arne van der Gen, Cornelis G. Kruse
  • Patent number: 5171753
    Abstract: Derivatives of 2-amino-1-phenylethanol were prepared from substituted amines and benzoin, stilbene oxide or styrene oxide to give compounds of Formula: ##STR1## where R is H or (un)substituted phenyl and C is a linking group or terminal group. The compounds of this invention can inhibit ulceration in in-vivo studies in rats.
    Type: Grant
    Filed: May 15, 1991
    Date of Patent: December 15, 1992
    Assignee: A. H. Robins Company, Incorporated
    Inventors: Harry R. Munson, Jr., Robert F. Boswell
  • Patent number: 5130339
    Abstract: New phenylethanolaminomethyltetralins of formula (I) ##STR1## wherein E represents hydrogen, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, phenyl, nitro, halogen, or trifluoromethyl,L represents hydrogen, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkyoxy, phenyl, nitro, or halogen, orE and L taken together represent a group --CH.dbd.CH--CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 --, andG represents hydrogen, chloro, hydroxy or an --OG' group wherein G' represents a (C.sub.1 -C.sub.4 (alkyl group either unsubstituted or substituted with hydroxy, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkoxycarbonyl, carboxy, or (C.sub.3 -C.sub.7)cycloalkyl; a (C.sub.3 -C.sub.7)cycloalkyl group; or a (C.sub.2 -C.sub.4)alkanoyl group; and salts thereof, are described which showed to be active as intestinal motility modulating agents and intraocular hypertension lowering agents.
    Type: Grant
    Filed: December 28, 1990
    Date of Patent: July 14, 1992
    Assignee: Sanofi
    Inventors: Roberto Cecchi, Umberto Guzzi
  • Patent number: 5128479
    Abstract: Oxidized diphenylheteroalkanes of the formula I ##STR1## where R.sup.1 to R.sup.6 and A have the meanings specified in the description, and the preparation thereof are described. The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: January 29, 1990
    Date of Patent: July 7, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5124334
    Abstract: The invention relates to benylalcohol phospholipase A.sub.2 inhibitors, pharmaceutical compositions containing them, and methods of treating phospholipase A.sub.2 -mediated conditions in mammals by administration of a therapeutically effective amount of such a benzylalcohol phospholipase A.sub.2 inhibitor.
    Type: Grant
    Filed: July 28, 1989
    Date of Patent: June 23, 1992
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventor: Wendell W. Wilkerson
  • Patent number: 5109023
    Abstract: The invention provides a method of treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis, utilizing the compounds of the formula ##STR1## or a physiological acceptable salt or solvate thereof, wherein Q represents a 1- or 2- naphthalenyl group.
    Type: Grant
    Filed: December 5, 1990
    Date of Patent: April 28, 1992
    Assignee: Glaxo Group Limited
    Inventors: William L. Mitchell, Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, David Hartley
  • Patent number: 5047433
    Abstract: N-alkyl derivatives of 2-amino-6,7-dimethoxy tetraline having general formula (I) ##STR1## wherein R is selected from hydrogen, ethyl, n-propyl and methyl cyclopropyl;R.sub.1 is selected from hydrogen, hydroxy and --OR.sub.3 wherein R.sub.3 is selected from methyl, ethyl and n-propyl; andR.sub.2 is selected from hydrogen, methyl, hydroxy, trifluoromethyl, fluoro and methoxy,are endowed with potent antihypertensive activity.
    Type: Grant
    Filed: December 21, 1987
    Date of Patent: September 10, 1991
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Mauro Marzi, Maria O. Tinti, Romano Di Fabio, Domenico Misiti
  • Patent number: 4990668
    Abstract: Described is a process for preparing a racemic or chiral aryloxypropanolamine (1) or arylethanolamine (2) of the formula ##STR1## wherein Ar is aryl, substituted aryl, heteroaryl, or aralkyl and R is alkyl, substituted alkyl, aralkyl, or WB wherein W is a straight or branched chain alkylene of from 1 to about 6 carbon atoms and wherein B is --NR.sub.2 COR.sub.3, --NR.sub.2 CONR.sub.3 R.sub.4, --NR.sub.2 SO.sub.2 R.sub.3, --NR.sub.2 SO.sub.2 NR.sub.3 R.sub.4, or --NR.sub.2 COOR.sub.5, where R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.3 and R.sub.5 are not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.3 or --NR.sub.3 COOR.sub.5, or R.sub.3 and R.sub.4 may together with N form a 5- to 7-membered heterocyclic group.The process can be used to prepare beta-blocking agents, useful in the treatment of cardiac conditions.
    Type: Grant
    Filed: December 4, 1985
    Date of Patent: February 5, 1991
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Khuong H. X. Mai, Ghanshyam Patil, William L. Matier
  • Patent number: 4935409
    Abstract: Animal growth promoters of the formula ##STR1## The intermediates of the formula ##STR2## are also new.
    Type: Grant
    Filed: April 27, 1988
    Date of Patent: June 19, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hartmund Wollweber, Jurgen Stoltefuss, Friedrich Berschauer
  • Patent number: 4918231
    Abstract: A process for the production of 1,2-amino alcohols, in improved yields, comprising the steps of:(1) reacting a silylated cyanohydrin compound with a Grignard reagent;(2) treating the reaction product of Step 1 with either a reducing agent, or an organolithium compound;(3) hydrolyzing the reaction product of Step 2;(4) isolating the resulting 1,2-amino alcohol.The 1,2-amino alcohols thus formed are useful as pharmaceuticals or precursors therefor.
    Type: Grant
    Filed: December 15, 1988
    Date of Patent: April 17, 1990
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Larry R. Krepski, Steven M. Heilmann, Jerald K. Rasmussen
  • Patent number: RE35128
    Abstract: The present invention is concerned with the preparation of erythro N-substituted vicinal aminoalcohol derivatives from hydroxyl-protected cyanohydrin derivatives by successive Grignard reaction, transimination using a primary amine, reduction of the resulting imine and removal of the hydroxyl-protecting group. The products are obtained either as a racemate or in an optically pure form, depending upon the stereochemical composition of the cyanohydrin derivatives.
    Type: Grant
    Filed: June 7, 1994
    Date of Patent: December 19, 1995
    Assignee: Duphar International Research B.V.
    Inventors: Johannes Brussee, Arne van der Gen, Cornelis G. Kruse
  • Patent number: RE43844
    Abstract: A process for making optically pure (R) and (S) salbutamol comprises obtaining the (R) or (S) isomer of either salbutamol or a salbutamol precursor in substantially optically pure form by resolving a racemic or optically impure mixture of enantiomers of salbutamol or of said precursor with either (L) or (D) tartaric acid, and where necessary converting said isomer of said precursor into either (R or (S) salbutamol respectively; then optionally converting said optically pure (R) and/or (S) salbutamol into a pharmaceutically acceptable salt.
    Type: Grant
    Filed: December 10, 2001
    Date of Patent: December 4, 2012
    Assignee: Cipla Limited
    Inventors: Yusuf Khwaja Hamied, Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao