Additional Chalcogen Bonded Directly To The Hetero Ring Patents (Class 540/526)
  • Patent number: 9499544
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: November 22, 2016
    Assignee: WOCKHARDT LIMITED
    Inventors: Sachin Bhagwat, Prasad Keshav Deshpande, Satish Bhawsar, Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Shivaji Sampatrao Pawar, Sunil Bhaginath Jadhav, Sanjay Kisan Dabhade, Vikas Vitthalrao Deshmukh, Bharat Dhond, Satish Birajdar, Mohammad Usman Shaikh, Deepak Dekhane, Piyush Ambalal Patel
  • Patent number: 9127004
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: September 8, 2015
    Assignee: Wockhardt Ltd.
    Inventors: Sachin Bhagwat, Prasad Keshav Deshpande, Satish Bhawsar, Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Shivaji Sampatrao Pawar, Sunil Bhaginath Jadhav, Sanjay Kisan Dabhade, Vikas Vitthalrao Deshmukh, Bharat Dhond, Satish Birajdar, Mohammad Usman Shaikh, Deepak Dekhane, Piyush Ambalal Patel
  • Patent number: 9006230
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: April 14, 2015
    Assignee: Wockhardt Ltd.
    Inventors: Sachin Bhagwat, Prasad Keshav Deshpande, Satish Bhawsar, Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Shivaji Sampatrao Pawar, Sunil Bhaginath Jadhav, Sanjay Kisan Dabhade, Vikas Vitthalrao Deshmukh, Bharat Dond, Satish Birajdar, Mohammad Usman Shaikh, Deepak Dekhane, Piyush Ambalal Patel
  • Publication number: 20150031670
    Abstract: Compounds of the formula (I), in which R1, R3, R5, R6, R7, R, X and Y have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.
    Type: Application
    Filed: March 21, 2013
    Publication date: January 29, 2015
    Applicant: MERCK PATENT GmbH
    Inventors: Timo Heinrich, Frank Zenke, Mireille Krier, Manja Friese-Hamim, Jeyaprakashnarayanan Seenisamy
  • Publication number: 20120190579
    Abstract: The present invention relates to a product comprising a solid substrate and a moiety of formula (I) linked thereto: wherein X, X? and R are as defined herein. The product is useful for immobilising target molecules such as molecules of biochemical interest to solid substrates for numerous applications, such as affinity chromatography, ELISA, biotechnological assay techniques and solid phase peptide synthesis.
    Type: Application
    Filed: August 9, 2010
    Publication date: July 26, 2012
    Applicant: UCL Business PLC
    Inventors: Mark Smith, Stephen Caddick, James Baker
  • Patent number: 7803793
    Abstract: This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing matrix metalloproteases. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.
    Type: Grant
    Filed: September 21, 2007
    Date of Patent: September 28, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: Yue-Mei Zhang, Bangping Xiang, Shyh-Ming Yang, Kenneth Rhodes, Robert Scannevin, Paul Jackson, Davraj Chakravarty, Xiaodong Fan, Lawrence J. Wilson, Prabha Karnachi
  • Publication number: 20090298781
    Abstract: The present invention relates to compounds of formula (I) as well as to drug conjugates based on compounds of formula (I) acting as apoptosis inhibitors, as well as to processes for their preparation, to pharmaceutical compositions containing them and their use in medicine.
    Type: Application
    Filed: November 22, 2006
    Publication date: December 3, 2009
    Applicant: CONSEJO SUPERIOR DE
    Inventors: Enrique Perez Payá, Maria Jesús Vicent Docon, Mar Orzaez Calatayud, Laura Mondragon Martinez, Angél Messeguer Paypoch, Alejadra Moure Fernandez, Gloria Sanclimens Perez De Rozas, Gema Malet Engra
  • Patent number: 7585855
    Abstract: The invention relates to the preparation of substituted caprolactams, a method for the preparation thereof, compositions containing them and the use thereof as a medicament, particularly as anticancer agents.
    Type: Grant
    Filed: August 19, 2008
    Date of Patent: September 8, 2009
    Assignee: Aventis Pharma SA
    Inventors: Jidong Zhang, Neerja Bhatnagar
  • Patent number: 7414078
    Abstract: The present invention is directed to novel themisone derivative compounds that have been modified to prevent the formation of the toxic metabolite, 2-phenyl-acrylamide. Compositions comprising such derivative compounds have activity as anesthetics and as neuroprotective agents.
    Type: Grant
    Filed: November 18, 2005
    Date of Patent: August 19, 2008
    Assignee: University of Virginia Patent Foundation
    Inventor: Milton L. Brown
  • Patent number: 7378410
    Abstract: This invention relates to certain substituted lactam compounds of the formula (I), particularly caprolactam compounds, which are useful for the treatment of cancer
    Type: Grant
    Filed: July 23, 2004
    Date of Patent: May 27, 2008
    Assignee: Novartis AG
    Inventors: Kenneth Walter Bair, Frederick Ray Kinder, Jr., Richard William Versace
  • Patent number: 7153846
    Abstract: The present invention relates to bengamide derivatives which are formed, during fermentation, by the microorganism Myxococcus virescens ST200611 (DSM 15898), to their use for treating cancer diseases, to pharmaceuticals which comprise bengamide derivatives, to a process for preparing bengamides of the formula (V) and to the microorganism Myxococcus virescens ST200611 (DSM 15898)
    Type: Grant
    Filed: October 22, 2004
    Date of Patent: December 26, 2006
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Holger Hoffmann, Sabine Haag-Richter, Michael Kurz, Heiko Tietgen
  • Patent number: 6953789
    Abstract: The present invention provides a compound represented by Formula: wherein ring A and ring B may be same or different and each is an optionally substituted homocyclic or heterocyclic ring and the like, each R1 may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group, an optionally substituted heterocyclic group or SR2, etc., X1 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group or —NR3—, etc, X2 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group, —NR4—, —O— or —S(O)p— (wherein p is 0, 1 or 2), each Y may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, a halogen atom, a carboxyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, SR5, an oxo group, a thioxo group, an optionally substituted imino group, a nitro group, a cyano group, etc.
    Type: Grant
    Filed: January 13, 2004
    Date of Patent: October 11, 2005
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Toshiro Yamashita, Hiroshi Nara, Masayuki Takizawa, Koji Yoshimura
  • Patent number: 6943179
    Abstract: Novel compounds of the formula I in which X, Y, Z, R, R1, R2 and R3 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of tromboembolic diseases and for the treatment of tumors
    Type: Grant
    Filed: February 27, 2002
    Date of Patent: September 13, 2005
    Assignee: Merck Patent GmbH
    Inventors: Werner Mederski, Bertram Cezanne, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
  • Patent number: 6544981
    Abstract: Lactam inhibitors are provided which have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, and prodrug esters thereof, wherein n is 1 to 5; and and R1, R2, R3, R4, R5 , R6, R7, R8, R9, R10, R10a, R11 and R12 are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants. A method for treating cardiovascular diseases associated with thromboses is also provided.
    Type: Grant
    Filed: June 5, 2001
    Date of Patent: April 8, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Philip D. Stein, Stephen P. O'Connor, Yan Shi, Chi Li
  • Patent number: 6545148
    Abstract: The present invention relates to an improved process for preparing certain substituted caprolactam compounds which comprises acylating an aminocaprolactam compound with a lactone compound in the presence of a weak base and a polar, organic solvent, and hydrolyzing the resultant diamide compound in a mixture of solvents to obtain the desired caprolactam compound.
    Type: Grant
    Filed: March 11, 2002
    Date of Patent: April 8, 2003
    Assignee: Novartis AG
    Inventors: David Daqiang Xu, Wenming Liu
  • Publication number: 20030055041
    Abstract: The present invention relates to certain substituted caprolactam carbonate and ether compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.
    Type: Application
    Filed: May 17, 2002
    Publication date: March 20, 2003
    Inventors: Frederick Ray Kinder, Richard William Versace, Kenneth Walter Bair
  • Patent number: 6525042
    Abstract: Sulfonyl derivatives represented by general formula (I), salts of the same, and solvates of both: and application of them as drugs: [wherein R1 is hydrogen, hydroxyl, nitro or the like; R2 and R3 are each independently hydrogen, halogeno or the like; R4 and R5 are each dependently hydrogen, halogeno or the like; Q1 is an optionally substituted saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group or the like; Q2 is a single bond, oxygen or the like; Q3 is, e.g., a group represented by formula (a): T1 is carbonyl or the like; and X1 and X2 are each independently methylidyne or nitrogen]. These compounds exhibit potent Fxa inhibiting activities and serve as excellent anticoagulants which speedily exert satisfactory and persistent anti-thrombotic effects through oral administration and little cause adverse effects.
    Type: Grant
    Filed: March 28, 2000
    Date of Patent: February 25, 2003
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Syozo Kobayashi, Satoshi Komoriya, Masayuki Ito, Tsutomu Nagata, Akiyoshi Mochizuki, Noriyasu Haginoya, Takayasu Nagahara, Haruhiko Horino
  • Patent number: 6455521
    Abstract: A condensed thiophene compound of the formula (I) wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof and hydrates thereof. The compound of the formula (I) of the present invention is useful as a novel antipsychotic agent which is effective for both positive symptoms and negative symptoms of schizophrenia, which is associated with less side effects such as extrapyramidal motor disorder and the like and which is less associated with serious side effects such as agranulocytosis and the like. In addition, this compound is also useful as a therapeutic agent of Alzheimer's disease and manic-depressive illness.
    Type: Grant
    Filed: April 19, 2001
    Date of Patent: September 24, 2002
    Assignee: Mitsubishi Pharma Corporation
    Inventors: Koji Seio, Hiroshi Tanaka, Toshiyuki Kohara, Kenji Hashimoto, Masatake Fujimura, Hideki Horiuchi, Hiroshi Yasumatsu, Koreichi Kimura
  • Patent number: 6452001
    Abstract: The invention relates to compounds of the formula wherein R1, R2 are independently from each other aryl or heteroaryl, wherein the heteroaryl group contains one or two heteroatoms, selected from N, O, or S, and wherein the aryl or heteroaryl groups are optionally substituted by 1 to 3 substituents, which are independently from each other halogen, CF3, lower alkoxy or lower alkyl; R3 is hydrogen, lower alkyl, —(CH2)nN(R)2, —(CH2)n-heteroaryl or is a —(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R4 is ═O, ═N(CH2)nCH3 or ═N(CH2)nN(R)2; R3 and R4 may be together with the N and C atoms to which they are attached the group —CR5═N—N═; R5 is hydrogen, —(CH2)nN(R)2, —(CH2)n-heteroaryl or is a —(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R is hydrogen or lower alkyl;
    Type: Grant
    Filed: May 14, 2001
    Date of Patent: September 17, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Annick Goergler, Thierry Godel, Reinhard Heck
  • Publication number: 20020128474
    Abstract: The present invention relates to an improved process for preparing certain substituted caprolactam compounds which comprises acylating an aminocaprolactam compound with a lactone compound in the presence of a weak base and a polar, organic solvent, and hydrolyzing the resultant diamide compound in a mixture of solvents to obtain the desired caprolactam compound.
    Type: Application
    Filed: March 11, 2002
    Publication date: September 12, 2002
    Inventors: David Daqiang Xu, Wenming Liu
  • Patent number: 6420415
    Abstract: Compounds represented by general formula (1) or salts thereof which have a matrix metalloprotease inhibitory activity and are useful as drugs, wherein the rings A and B represent each an optionally substituted homocycle or heterocycle, etc.; R1s are the same or different and each represents hydrogen, optionally substituted hydrocarbyl, acyl, etc.; X1 represents a bond, optionally substituted divalent aliphatic hydrocarbyl, etc.; X2 represents a bond, optionally substituted divalent aliphatic hydrocarbyl, —O—, etc.; Ys are the same or different represents hydrogen, optionally substituted hydrocarbyl, oxo, etc.; m is 0 or 1; n is an integer of 1 to 3; q1 is an integer of 1 to 2n+4; and q2 is an integer of 0 to 2n+3, provided that q1+q2 is 2n+4.
    Type: Grant
    Filed: March 20, 2001
    Date of Patent: July 16, 2002
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Toshiro Yamashita, Hiroshi Nara, Masayuki Takizawa, Koji Yoshimura
  • Patent number: 6413954
    Abstract: The present invention relates to certain substituted caprolactam carbonate and ether compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.
    Type: Grant
    Filed: May 8, 2001
    Date of Patent: July 2, 2002
    Assignee: Novartis AG
    Inventors: Frederick Ray Kinder, Jr., Richard William Versace, Kenneth Walter Bair
  • Patent number: 6335443
    Abstract: A process for the synthetic generation of high affinity, iron binding compounds known as Exochelins, and more particularly, to a synthetic process for making Exochelins and to modifications to these newly synthesized compounds to vary their physiological properties, including applications of these newly synthesized and utile compounds for diagnosing and treating disease in mammals.
    Type: Grant
    Filed: March 5, 1999
    Date of Patent: January 1, 2002
    Assignee: Keystone Biomedical, Inc.
    Inventors: Leo S. Geraci, Stuart G. Levy, James P. Hudspeth, Richard L. Buswell, Jay F. Stearns
  • Patent number: 6262222
    Abstract: Copolymers containing N-vinyllactam derivatives protected at 3-position are provided and represented by the following formula. The copolymers are used as a photoresist material suitable for deep uv process so that high sensitivity and resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in PED stability can be accomplished by use of the photoresist.
    Type: Grant
    Filed: October 8, 1998
    Date of Patent: July 17, 2001
    Assignee: Hyundai Electronics Industries Co., Ltd.
    Inventors: Jin Baek Kim, Min Ho Jung, Jong Ho Cheong
  • Patent number: 6255479
    Abstract: A method for preparing an &agr;-oxolactam comprising, reacting a corresponding &agr;-diazolactam with an oxygen donor, in the presence of a transition metal catalyst, to yield the corresponding &agr;-oxolactam.
    Type: Grant
    Filed: December 29, 1998
    Date of Patent: July 3, 2001
    Assignee: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, Akireddy Srinivasa Rao
  • Patent number: 6239127
    Abstract: The present invention relates to certain substituted caprolactam compounds of formula (I), where R1 is (C1-6)alkyl or (C3-6)cycloalkyl; R2 hydrogen or (C1-6)alkyl; X is (C1-12)alkynylene; (C2-12)alkynylene; m is 0 or 1; and R3 is (C3-8)cycloalkyl; or an aromatic ring system selected from (II, III, IV and V), where R4 is hydrogen, chloro, or methoxy; R5 is hydrogen, chloro, (C1-18)alkyl or (C1-18)alkoxy, and Z is oxygen, sulfur, N—H, or N—CH3; or a pharmaceutically acceptable acid addition salt thereof, where possible, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.
    Type: Grant
    Filed: November 17, 1999
    Date of Patent: May 29, 2001
    Assignee: Novartis AG
    Inventors: Frederick Ray Kinder, Jr., Kenneth Walter Bair, Christopher Turchik Jagoe, Richard William Versace, Sompong Wattanasin
  • Patent number: 6174879
    Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.
    Type: Grant
    Filed: March 17, 1999
    Date of Patent: January 16, 2001
    Assignee: University of British Columbia
    Inventors: Bernard A. MacLeod, Michael J. A. Walker, Richard A. Wall
  • Patent number: 5994346
    Abstract: Exochelins can be used to prevent damage to organs for transplant from the formation or presence of the .circle-solid.OH radical. In particular, the invention is directed to the administration of exochelins to the organ prior to or coincidental with removal from a donor, storage, implantation in a recipient or in conjunction with reestablishment of flow of body fluids to the organ.
    Type: Grant
    Filed: October 30, 1997
    Date of Patent: November 30, 1999
    Assignee: Regents of the University of California
    Inventors: Marcus A. Horwitz, Lawrence D. Horwitz
  • Patent number: 5929097
    Abstract: The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF-.alpha. converting enzyme (TACE, tumor necrosis factor-.alpha.
    Type: Grant
    Filed: October 6, 1997
    Date of Patent: July 27, 1999
    Assignee: American Cyanamid Company
    Inventors: Jeremy Ian Levin, Mila T. Du, Aranapakam Mudumbai Venkatesan, Frances Christy Nelson, Arie Zask, Yansong Gu
  • Patent number: 5869024
    Abstract: In accordance with the present invention a novel method and composition for using nonionic contrast media to reduce the risk of clot formation in a diagnostic procedure is disclosed. Novel compositions for such method are also disclosed. The present method comprises employing a triiodinated phenyl contrast agent having a heterocyclic group or a dimeric triiodinated phenyl contrast agent having one or more heterocyclic groups.
    Type: Grant
    Filed: June 5, 1992
    Date of Patent: February 9, 1999
    Assignee: Bracco International B.V.
    Inventors: Ramachandran S. Ranganathan, Michael F. Tweedle, Paul W. Wedeking
  • Patent number: 5856477
    Abstract: The azepine intermediates of the formula ##STR1## wherein R.sub.6 and R.sub.7 are other than hydrogen are disclosed. These intermediates can be reacted with acylmercaptocarboxylic acids of the formula ##STR2## to give the pharmaceutically active products.
    Type: Grant
    Filed: July 30, 1996
    Date of Patent: January 5, 1999
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Jeffrey A. Robl
  • Patent number: 5856318
    Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl;wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 11, 1997
    Date of Patent: January 5, 1999
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
  • Patent number: 5837677
    Abstract: The invention is directed toward the use of desferri-Exochelins to destroy cancer cells or retard or eliminate the growth of those cancer cells.
    Type: Grant
    Filed: June 25, 1997
    Date of Patent: November 17, 1998
    Assignee: Keystone Biomedical, Inc.
    Inventors: Lawrence D. Horwitz, Kathryn B. Horwitz
  • Patent number: 5750680
    Abstract: N-vinyllactam derivatives protected at the 3-position are provided and represented by the following formula (I). These are polymerized into homo- and copolymers for use in microlithography of semiconductor manufacture. The polymers are used as a photoresist material suitable for a deep UV process so that pictures of high sensitivity and high resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in pattern formation can be accomplished through the use of the photoresist of the invention.
    Type: Grant
    Filed: September 12, 1996
    Date of Patent: May 12, 1998
    Assignees: Hyundai Electronics Industries Co., Ltd., Korea Advanced Institute of Science & Technology
    Inventors: Jin Baek Kim, Min Ho Jung, Kyeong Ho Chang
  • Patent number: 5721209
    Abstract: Exochelins can be used to prevent damage to living tissue from the formation or presence of the (.cndot.OH) radical. In particular, the invention is directed to the administration of exochelins to infarcted myocardium prior to or coincidental with reperfusion to prevent damage to myocardium from iron mediated free radical formation. Also presented is the chemical structure of exochelins and modified exochelins as well as other applications of these materials in the treatment and diagnosis of disease in mammals.
    Type: Grant
    Filed: February 3, 1995
    Date of Patent: February 24, 1998
    Assignee: The Regents of the University of California
    Inventors: Lawrence D. Horwitz, Marcus A. Horwitz, Bradford W. Gibson, Joseph Reeve
  • Patent number: 5696256
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: December 9, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yasuyuki Kando, Hideki Uneme, Isao Minamida
  • Patent number: 5693630
    Abstract: Compounds of the general formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Z is a saturated or unsaturated 3 to 6 carbon chain,m is 2 or 3,R.sub.1 is a hydrogen atom, or a straight or branched C.sub.1-4 alkyl group,R.sub.2, R.sub.3 and R.sub.13 are situated in the ortho, meta, or para position of the phenyl ring and are the same or different and selected from the following groups: H, OH, OR.sub.14, halogen, CO.sub.2 R.sub.9, CN, CF.sub.3, NO.sub.2, NH.sub.2, COCH.sub.3,OSO.sub.2 CF.sub.3,OSO.sub.2 CH.sub.3,CONR.sub.10 R.sub.11, OCOR.sub.12, whereinR.sub.9, R.sub.12 and R.sub.14 is a straight or branched C.sub.1-4 alkyl group,R.sub.10 and R.sub.11 are the same or different and represents hydrogen or a straight or branched C.sub.1-6 alkyl group,R is 1) ##STR2## processes for their preparation, pharmaceutical preparations containing them and the use of the compounds in the treatment psychiatric disorders.
    Type: Grant
    Filed: October 26, 1994
    Date of Patent: December 2, 1997
    Assignee: Astra Aktiebolag
    Inventors: Stefan Bengtsson, Sven Hellberg, Nina Mohell, Lian Zhang, Gerd Hallnemo, David Jackson, Bengt Ulff
  • Patent number: 5677444
    Abstract: A novel and simple method is proposed for the synthetic preparation of an N,N-disubstituted .beta.-ketothioamide compound represented by the general formulaR.sup.1 R.sup.2 N--CS--CH.sub.2 --CO--R.sup.3,in which R.sup.1 and R.sup.2 are each a monovalent hydrocarbon group or each a divalent hydrocarbon group jointly forming a cyclic structure together with the nitrogen atom and R.sup.3 is a hydrogen atom, a monovalent hydrocarbon group or a divalent hydrocarbon group forming a cyclic structure jointly with R.sup.1, R.sup.1 being a divalent hydrocarbon group and R.sup.2 being a monovalent hydrocarbon group. The method comprises:(a) mixing an N,N-disubstituted amide compound represented by the general formulaR.sup.1 R.sup.2 N--CO--R.sup.3,and a bis(trialkylsilyl)thioketene compound represented by the general formula(R.sub.3 Si).sub.2 C.dbd.C.dbd.
    Type: Grant
    Filed: September 15, 1995
    Date of Patent: October 14, 1997
    Assignee: Japan as represented by Director General of Agency of Industrial Science and Technology
    Inventors: Tohru Tsuchiya, Isao Shibuya, Yoichi Taguchi, Akihiro Oishi, Kazumasa Honda
  • Patent number: 5610318
    Abstract: This invention is directed to a process for preparing a compound containing a persalt activators and salts thereof which are derived from imidocarboxylic acids and sulfimidocarboxylic acids of the formula I: ##STR1## in which A is a group of the formula ##STR2## n is the number 0, 1 or 2, R.sup.1 is hydrogen, chlorine, bromine, C.sub.1 -C.sub.20 -alkyl, C.sub.2 -C.sub.20 -alkenyl, aryl, or alkylaryl,R.sup.2 is hydrogen, chlorine, bromine, --SO.sub.3 M, --CO.sub.2 M or --OSO.sub.3 M, X is C.sub.1 -C.sub.19 -alkylene or arylene,B is a group of the formula C.dbd.O or SO.sub.2,L is a leaving group.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: March 11, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Frank Jaekel, Gerd Reinhardt, Wolf-Dieter M uller
  • Patent number: 5591846
    Abstract: New nonionic radiographic contrast agents having the formula ##STR1## wherein Y is a single bond, ##STR2## R.sub.1, R.sub.1 ' and R.sub.2 are the same or different and are hydrogen, alkyl or hydroxyalkyl.Hydroxyalkyl refers to such alkyl groups having 1 or more hydroxy groups. Preferred hydroxyalkyl groups include: ##STR3## R.sub.3 and R.sub.4 are the same or different and are hydrogen, methyl or --CH.sub.2 CH.sub.2 OH; R.sub.5 is hydrogen, alkyl, --CH.sub.2 CH.sub.2 OH, CH.sub.2 OH or OH and R.sub.6 is alkyl, --CH.sub.2 CH.sub.2 OH, CH.sub.2 OH, OH or hydrogen and may be the same or different than R.sub.5 and m is zero or one, with the proviso that no methylene or methine carbon atom of the heterocyclic ring is attached to both a nitrogen and an oxygen atom with the additional proviso that when Y is a single bond, m is not zero. These new contrast agents are water soluble and have desirable low osmolality and anticoagulant properties.
    Type: Grant
    Filed: October 27, 1993
    Date of Patent: January 7, 1997
    Assignee: Bracco International B.V.
    Inventors: Ramachandran S. Ranganathan, Thangavel Arunchalam, Edmund R. Marinelli, Radhakrishna K. Pillai
  • Patent number: 5552397
    Abstract: Compounds of the formula ##STR1## are disclosed as possessing inhibitory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents. Processes for preparing these compounds are also disclosed.
    Type: Grant
    Filed: December 1, 1993
    Date of Patent: September 3, 1996
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Donald S. Karanewsky, Jeffrey A. Robl
  • Patent number: 5438118
    Abstract: Peptide mimics, having a constrained peptide backbone conformation, are HIV protease inhibitors. A compound of this invention is, for example, 3-Benzyl-5(alaninyl-1-aminoethyl)-2,3,6,7-tetrahydro-N-azepinyl-2-propiony l-valinyl-valinyl methyl ester.
    Type: Grant
    Filed: July 26, 1993
    Date of Patent: August 1, 1995
    Assignee: SmithKline Beechman Corp.
    Inventors: James F. Callahan, William F. Huffman, Michael L. Moore, Kenneth A. Newlander
  • Patent number: 5399557
    Abstract: This invention provides a pyrroloazepine compound represented by the following formula (I) or (II): ##STR1## wherein Z.sub.1, Z.sub.2, R, A and Y are defined in the claims. The pyrroloazepine compounds according to the present invention are drugs having excellent anti-serotonin action. Coupled with their high safety, they can therefore be used as novel therapeutics for ischemic heart diseases. In addition, the compounds of the present invention include those having anti-.alpha..sub.1 action. Such compounds are effective as hypotensive drugs. Pyrroloazepine compounds according to the present invention are therefore extremely useful as therapeutics for a wide variety of circulatory diseases.
    Type: Grant
    Filed: April 7, 1993
    Date of Patent: March 21, 1995
    Assignee: Suntory Limited
    Inventors: Akira Mizuno, Mikiko Miya, Norio Inomata, Toshio Tatsuoka, Takafumi Ishihara
  • Patent number: 5376529
    Abstract: This invention relates to novel methods for the release of nucleic acids from cells in complex biological samples or specimens to prepare and make available the nucleic acid material present for a hybridization assay or for extraction. Novel methods for hybridization of nucleic acids are also presented. In particular methods are described for isolating nucleic acid from a sample containing a complex biological mixture of nucleic acid and non-nucleic acids wherein the sample is combined with a hybridization medium comprising a lactam which promotes and enables nucleic acid pairing when complementary nucleic acid is introduced. The lactam is preferably about 5 to about 70% of the hybridization medium and is most preferably 2-pyrrolidone, N-ethyl-2-pyrrolidone, N-cyclohexyl-2-pyrrolidone, N-dodecyl-2-pyrrolidone, N-methyl-2-pyrrolidone, N-hydroxyethyl-2-pyrrolidone, N-methyl-2-piperidone, 2-.epsilon.-caprolactam, N-methyl-2-caprolactam, 2-piperidone or N-(4-hydroxybenzyl)pyrrolidone.
    Type: Grant
    Filed: December 13, 1991
    Date of Patent: December 27, 1994
    Assignee: MicroProbe Corporation
    Inventors: Jeffrey Van Ness, Nicolaas M. J. Vermeulen
  • Patent number: 5308520
    Abstract: Various heterocyclic compounds have been discovered that impart improved fuel economy and friction modification to lubricant and fuel compositions. These heterocyclic compounds of the invention preferably contain nitrogen and may be further reacted with hydrocarbyl carboxylic acid acylating reactants or hydrocarbyl phenolic reactants to give higher molecular materials. These higher molecular weight materials have higher oil-solubility and impart dispersancy properties to lubricant and fuel compositions.
    Type: Grant
    Filed: July 31, 1989
    Date of Patent: May 3, 1994
    Assignee: The Lubrizol Corporation
    Inventors: Joseph W. Pialet, Paul E. Adams
  • Patent number: 5192759
    Abstract: 1,2,3,4-tetrahydronaphthlamines of formula (1) ##STR1## wherein R is H or OCH.sub.3 ; ##STR2## is either at 1 or 2 position R.sub.1 is H;R.sub.2 is selected from:L-prolyl, optionally N-substituted with acetyl or carbobenzoxy,L-pyroglutamyl,(pyrrolidin-2-one-1-yl)acetyl,3-carboxy-2-hydroxypropyl:or R.sub.1 and R.sub.2 taken together with the nitrogen atom form the ring ##STR3## wherein n=1,2,3 and R.sub.3 -H, OH are nootropic substances potent enhancers of learning processes and memory.Orally or parenterally administrable pharmaceutical compositions in unit dosage form comprise between about 100 and about 500 mg of a compound of formula (1).
    Type: Grant
    Filed: December 18, 1991
    Date of Patent: March 9, 1993
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Fabio Giannessi, Orlando Ghirardi, Domenico Misiti, Maria O. Tinti, Roberto Cozzolino
  • Patent number: 5136053
    Abstract: A method for producing a cyclic alkyleneimine, which comprises reacting a cyclic ether with a compound of the formula NH.sub.2 R wherein R is a hydrogen atom or an alkyl group, in a vapor phase in the presence of a solid acid catalyst, wherein the reaction is conducted under a pressure of at least 0.5 kg/cm.sup.2 G as the total pressure of partial pressures of the reactants and the reaction product.
    Type: Grant
    Filed: March 2, 1990
    Date of Patent: August 4, 1992
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Hitoshi Sugiyama, Tomoyuki Mori
  • Patent number: 5124444
    Abstract: This invention relates to novel methods for the extraction of nucleic acid. In particular methods are described for isolating nucleic acid from a sample containing a complex biological mixture of nucleic acid and non-nucleic acids wherein the sample is combined with an extraction solution comprising a lactam and then the nucleic acid material is isolated from the resulting combined solution. The resulting combined solution is mixed and becomes biphasic and the nucleic acid material is isolated from the aqueous phase by precipitation with ethanol. The lactam is preferably about 5 to about 70% of the extraction solution and is most preferably 2-pyrrolidone, N-ethyl-2-pyrrolidone, N-cyclohexyl-2-pyrrolidone, N-dodecyl-2-pyrrolidone, N-methyl-2-pyrrolidone, N-hydroxyethyl-2-pyrrolidone, N-methyl-2-piperidone, 2-.epsilon.-caprolactam, N-methyl-2-caprolactam, 2-piperidone or N-(4-hydroxybenzyl)pyrrolidone. Methods for selectively isolating DNA, ribosomal RNA and plasmid DNA are also disclosed.
    Type: Grant
    Filed: July 24, 1989
    Date of Patent: June 23, 1992
    Assignee: MicroProbe Corporation
    Inventors: Jeffrey Van Ness, Nicolaas Vermuelen, B. Melina Cimler
  • Patent number: 5106730
    Abstract: This invention relates to novel methods for the release of nucleic acids from cells in complex biological samples or specimens to prepare and make available the nucleic acid material present for a hybridization assay or for extraction. Novel methods for hybridization of nucleic acids are also presented. In particular methods are described for isolating nucleic acid from a sample containing a complex biological mixture of nucleic acid and non-nucleic acids wherein the sample is combined with a hybridization medium comprising a lactam which promotes and enables nucleic acid pairing when complementary nucleic acid is introduced. The lactam is preferably about 5 to about 70% of the hybridization medium and is most preferably 2-pyrrolidone, N-ethyl-2-pyrrolidone, N-cyclohexyl-2-pyrrolidone, N-dodecyl-2-pyrrolidone, N-methyl-2-pyrrolidone, N-hydroxyethyl-2-pyrrolidone, N-methyl-2-piperidone, 2-.epsilon.-caprolactam, N-methyl-2-caprolactam, 2-piperidone or N-(4-hydroxybenzyl)pyrrolidone.
    Type: Grant
    Filed: July 27, 1990
    Date of Patent: April 21, 1992
    Assignee: MicroProbe Corporation
    Inventors: Jeffrey Van Ness, Nicolaas M. J. Vermeulen
  • Patent number: 5098916
    Abstract: Certain propanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, henalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.15 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R.sup.16 and R.sup.
    Type: Grant
    Filed: March 29, 1990
    Date of Patent: March 24, 1992
    Assignee: G. D. Searle & Co.
    Inventors: Nancy M. Gray, Brian K. Cheng