Plural Seven-membered Hetero Rings Patents (Class 540/525)
  • Patent number: 8765731
    Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: July 1, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: James A. Henderson, John Maxwell, Louis Vaillancourt, Mark Morris, Ronald Grey, Jr., Simon Giroux, Laval Chan Chun Kong, Sanjoy Kumar Das, Bingan Liu, Carl Poisson, Caroline Cadilhac, Monica Bubenik, T. Jagadeeswar Reddy, Guy Falardeau, Constantin Yannopoulos, Jian Wang, Oswy Z. Pereira, Youssef L. Bennani, Albert C. Pierce, Govinda Rao Bhisetti, Kevin M. Cottrell, Valerie Marone
  • Patent number: 8623945
    Abstract: This invention relates to a process for stabilizing polymers with oligomeric carbodiimides containing at least one heterocyclic end group and stabilizers. The oligomeric carbodiimides may be compounds of the general formula (I): where A1, A2 are each independently, identically or differently, hydrocarbon groups having 2 to 20 carbon atoms, B1, B2 are each independently, identically or differently, heterocycles, C1-C30-alcohols, polyetherols, polyesterols, amines, polyether amines, polyester amines, thioalcohols, polyether thiols, polyester thiols; R1, R2 are each independently, identically or differently: n is an integer from 2 to 100, and A1, A2, B1 and B2 may each be substituted at any desired position by C1-C20-alkyl, C2-C20-alkenyl, C2-C20-alkynyl, C1-C20-alkoxy, carbonyl oxygen (?O) or halogen, with the proviso that at least one B1 or B2 substituent is a heterocyclic end group. The invention also relates to compositions of the oligomeric carbodiimides and mixtures.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: January 7, 2014
    Assignee: BASF SE
    Inventors: Theo Smit, Laurence Pottie, Simone Schillo, Volker Frenz, Roelof van der Meer
  • Publication number: 20130157997
    Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.
    Type: Application
    Filed: November 16, 2012
    Publication date: June 20, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventor: Vertex Pharmaceuticals Incorporated
  • Publication number: 20120238676
    Abstract: Oligomeric carbodiimides comprising at least one heterocyclic end group are used as stabilizers for polymers. The oligomeric carbodiimides may be compounds of the general formula (I), where A1, A2 are each independently, identically or differently, hydrocarbon groups having 2 to 20 carbon atoms, B1, B2 are each independently, identically or differently, heterocycles, C1-C30-alcohols, polyetherols, polyesterols, amines, polyether amines, polyester amines, thioalcohols, polyether thiols, polyester thiols, R1, R2 are each independently, identically or differently, n is an integer from 2 to 100, and wherein A1, A2, B1 and B2 may each be substituted at any desired position by C1-C20-alkyl, C2-C20-alkenyl, C2-C20-alkynyl, C1-C20-alkoxy, carbonyl oxygen (?O) or halogen, with the proviso that at least one B1 or B2 substituent is a heterocyclic end group. Processes for stabilizing polymers against hydrolysis using oligomeric carbodiimides are also disclosed.
    Type: Application
    Filed: March 15, 2012
    Publication date: September 20, 2012
    Applicant: BASF SE
    Inventors: THEO SMIT, LAURENCE POTTIE, SIMONE SCHILLO, VOLKER FRENZ, ROELOF VAN DER MEER
  • Publication number: 20120165519
    Abstract: The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.
    Type: Application
    Filed: March 6, 2012
    Publication date: June 28, 2012
    Applicant: Cephalon, Inc.
    Inventors: Gulzar Ahmed, Henry Joseph Breslin, Jason Burke, Matthew A. Curry, James L. Diebold, Bruce Dorsey, Benjamin J. Dugan, Daming Feng, Diane E. Gingrich, Tao Guo, Keith S. Learn, Joseph G. Lisko, Rong-qiang Liu, Eugen Mesaros, Karen Milkiewicz, Gregory R. Ott, Jay P. Theroff, Tho V. Thieu, Rabindranath Tripathy, Theodore L. Underiner, Gregory J. Wells, Craig A. Zificsak
  • Publication number: 20100221259
    Abstract: The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.
    Type: Application
    Filed: May 10, 2010
    Publication date: September 2, 2010
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Hiromu HABASHITA, Masaya KOKUBO, Shiro SHIBAYAMA, Hideaki TADA, Tatsuya TANIHIRO
  • Patent number: 7563784
    Abstract: The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.
    Type: Grant
    Filed: April 25, 2006
    Date of Patent: July 21, 2009
    Assignee: SmithKline Beecham Corporation
    Inventors: Maxwell D. Cummings, Robert W. Marquis, Jr., Yu Ru, Scott K. Thompson, Daniel F. Veber, Dennis S. Yamashita
  • Publication number: 20090093628
    Abstract: An amide or lactam is produced by conducting a rearrangement of a corresponding oxime compound in the presence of a cyclic compound containing a structure represented by following Formula (1) as a ring constituent and a fluorinated alcohol: wherein Z represents a halogen atom or an —OR group, where R represents an organic group. Z is preferably chlorine atom. Exemplary fluorinated alcohols include fluorine-containing branched-chain aliphatic alcohols represented by following Formula (3): wherein Rf1 and Rf2 may be the same as or different from each other and each represent a perfluoroalkyl group having one to eight carbon atoms; and “n” denotes an integer of 0 to 8. According to this process, amides or lactams can be simply produced in high yields without causing large amounts of by-products.
    Type: Application
    Filed: February 27, 2007
    Publication date: April 9, 2009
    Inventors: Yasutaka Ishii, Tatsuya Nakano, Takahiro Iwahama
  • Patent number: 7405209
    Abstract: The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
    Type: Grant
    Filed: June 14, 2005
    Date of Patent: July 29, 2008
    Assignees: SmithKline Beecham Corporation, SmithKline Beecham p.l.c.
    Inventors: Robert Wells Marquis, Jr., Yu Ru, Daniel Frank Veber, Maxwell David Cummings, Scott Kevin Thompson, Dennis Shinji Yamashita
  • Patent number: 7071184
    Abstract: The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.
    Type: Grant
    Filed: March 7, 2001
    Date of Patent: July 4, 2006
    Assignee: SmithKline Beecham Corporation
    Inventors: Maxwell D. Cummings, Robert W. Marquis, Jr., Daniel F. Veber, Dennis S. Yamashita
  • Patent number: 7030201
    Abstract: The present invention relates to bottom antireflective coating compositions and polymers useful in making such compositions.
    Type: Grant
    Filed: November 26, 2003
    Date of Patent: April 18, 2006
    Assignee: AZ Electronic Materials USA Corp.
    Inventors: Huirong Yao, Shuji Ding-Lee, Hengpeng Wu, Zhong Xiang
  • Patent number: 6958329
    Abstract: This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Grant
    Filed: November 4, 2002
    Date of Patent: October 25, 2005
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: Richard E. Olson
  • Patent number: 6852713
    Abstract: Lactam derivatives of the general formula are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed.
    Type: Grant
    Filed: April 16, 2003
    Date of Patent: February 8, 2005
    Assignee: Adolor Corporation
    Inventors: Roland E. Dolle, Paul Anson Tuthill
  • Patent number: 6699988
    Abstract: The invention relates to a process for the preparation of N,N′-carbonylbislactams by reaction of phosgene with at least one lactam which is characterized in that the tertiary amine is chosen from the group consisting of non-nucleophilic aliphatic tertiary amines. N,N′-Carbonylbislactams of high purity are thus obtained with good yields, both in the laboratory and on the industrial scale.
    Type: Grant
    Filed: April 23, 2001
    Date of Patent: March 2, 2004
    Assignee: SNPE
    Inventors: Hubert Bonnard, Laurence Ferruccio, Jean-Pierre Senet, Pierre-Yves Le Roy
  • Publication number: 20040024203
    Abstract: Compounds of formula (I) are disclosed. The compounds inhibit the action of gamma secretase, and hence find use in the treatment and prevention of Alzheimer's disease.
    Type: Application
    Filed: April 11, 2003
    Publication date: February 5, 2004
    Inventors: Ian Churcher, Alan John Nadin, Andrew Pate Owens
  • Patent number: 6566376
    Abstract: The invention provides compounds of general formula (I) wherein R1, R2, R3, R4, A, Q, U, V, W, X, Y and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, especially for the treatment of chemokine receptor related diseases and conditions.
    Type: Grant
    Filed: September 8, 2000
    Date of Patent: May 20, 2003
    Assignee: AstraZeneca UK Limited
    Inventors: Andrew J G Baxter, Stephen J Brough, Thomas McInally
  • Patent number: 6495540
    Abstract: This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Grant
    Filed: March 27, 2001
    Date of Patent: December 17, 2002
    Assignee: Bristol - Myers Squibb Pharma Company
    Inventor: Lorin A. Thompson
  • Patent number: 6476016
    Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described.
    Type: Grant
    Filed: July 17, 2001
    Date of Patent: November 5, 2002
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Aihua Wang, Bruce Edward Tomczuk, Tianbao Lu, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
  • Patent number: 6448394
    Abstract: The invention relates to a process for the preparation of an N-alkyl or N-aryl carbamoyl derivative in which an amine is contacted with a carbonic acid derivative according to the general formula: where fragments X in the form of XH are a lactam, oxime, imide or triazole. In particular the invention relates to the preparation of a blocked isocyanate according to a process in which no isocyanate is used. The invention also relates to the use of the N-alkyl or N-aryl carbamoyl derivative prepared according to the process according to the invention in a coating.
    Type: Grant
    Filed: March 23, 2001
    Date of Patent: September 10, 2002
    Assignee: DSM N.V.
    Inventors: Jacobus A. Loontjens, Bartholomeus J. M. Plum
  • Publication number: 20020028932
    Abstract: The invention relates to a process for the preparation of an N-alkyl or N-aryl carbamoyl derivative in which an amine is contacted with a carbonic acid derivative according to the general formula: 1
    Type: Application
    Filed: March 23, 2001
    Publication date: March 7, 2002
    Inventors: Jacobus A. Loontjens, Bartholomeus J.M. Plum
  • Patent number: 6344450
    Abstract: Lactam inhibitors are provided which have the structure X is wherein Y is O or S and R4 is  R7O— or R8 and R1, R2, R3, R5, R6, R7, and R8, are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants, and are inhibitors of tryptase and thus are useful in treating asthma. Methods for treating cardiovascular diseases associated with thromboses and for treating asthma and related diseases are also provided.
    Type: Grant
    Filed: August 7, 2000
    Date of Patent: February 5, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory S. Bisacchi, Steven M. Seiler, R. Michael Lawrence, James C. Sutton, Jr., William A. Slusarchyk, Guohua Zhao
  • Patent number: 6051678
    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: March 13, 1997
    Date of Patent: April 18, 2000
    Assignee: Hyundai Electronics Industries Co., Ltd.
    Inventors: Jin Baek Kim, Min Ho Jung, Jong Ho Cheong
  • Patent number: 5972237
    Abstract: Heterocyclic compounds IR.sup.1 --X--L (I)whereL is a cyclic carbamate residue, a lactonoxy residue or a lactam residue,X is an oxygen-containing group ##STR1## where A is a linker, and R.sup.1 is an organic radical or a group L,are used as activators for inorganic peroxy compounds, in particular as cold bleach activators or optical brighteners in detergents, cleaners and bleaches and in disinfectants.
    Type: Grant
    Filed: November 17, 1997
    Date of Patent: October 26, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Muller, Thomas Wehlage, Wolfgang Trieselt, Alfred Oftring, Elisabeth Kappes, Gunter Oetter, Dieter Boeckh, Roland Ettl, Albert Hettche
  • Patent number: 5955606
    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: February 19, 1998
    Date of Patent: September 21, 1999
    Assignee: Hyundai Electronics Industries Co., Ltd.
    Inventors: Jin Baek Kim, Min Ho Jung, Kyeong Ho Chang
  • 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: 5561235
    Abstract: Bleaching compositions, laundry and automatic dishwashing detergent compositions comprising multiple-substituted bleach activators which have at least one quaternary nitrogen atom,, are provided. More specifically, the invention relates to compositions which provide enhanced cleaning/bleaching benefits though the selection of multiple-substituted quaternary bleach activators having specific leaving groups with a conjugate acid aqueous pK.sub.a above 13 and with advantageous ratios of rate of perhydrolysis to rate of hydrolysis and of rate of perhydrolysis to rate of diacylperoxide production. Included are preferred activator compounds and methods for washing fabrics, hard surfaces, and tableware using the activators.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 1, 1996
    Assignee: The Procter & Gamble Company
    Inventors: Eugene P. Gosselink, Gregory S. Miracle, Alan D. Willey, Michael E. Burns, Kevin L. Kott, Mark R. Sivik, Lucille F. Taylor
  • Patent number: 5336706
    Abstract: The present invention relates to novel piperidine-triazine compounds of the formula (I) ##STR1## in which R.sub.1 is e.g. hydrogen or methyl, A.sub.1 is e.g. >N--CH.sub.3, R.sub.2 is e.g. --(CH.sub. 2).sub.2-6 --, R.sub.3 is e.g. 2,2,6,6-tetramethyl-4-piperidyl or 1,2,2,6,6-pentamethyl-4-piperidyl, or --A.sub.1 --R.sub.2 -- is a direct bond and, in this case, R.sub.3 is e.g. a group ##STR2## is a group of the formula (IVa) or (IVc) ##STR3## q and m are e.g. zero, X.sub.1 is e.g. a group of the formula (Va)--A.sub.4 --R.sub.9 --A.sub.5 -- (Va)in which A.sub.4 and A.sub.5 which are identical or different are e.g. an >N--R.sub.8 group where R.sub.8 is e.g. hydrogen, 2,2,6,6-tetramethyl-4-piperidyl or 1,2,2,6,6-pentamethyl-4-piperidyl, R.sub.9 is e.g. --(CH.sub.2).sub.2-6 --, n is e.g. a number from 1 to 10, Y.sub.1 is e.g. OH, ONa, OK or a group --X.sub.1 Z with Z being hydrogen or methyl and Y.sub.2 is e.g. hydrogen or methyl.
    Type: Grant
    Filed: September 29, 1993
    Date of Patent: August 9, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Valerio Borzatta, Roberto Scrima, Graziano Vignali
  • Patent number: 5300640
    Abstract: A novel herbicidal pyrimidine derivative represented by the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y.sup.1, Y.sup.2, Y.sup.3, X and Z are as defined herein.
    Type: Grant
    Filed: December 19, 1991
    Date of Patent: April 5, 1994
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Mitsumori Hiratsuka, Naonori Hirata, Kazuo Saito, Hideyuki Shibata
  • Patent number: 5300647
    Abstract: Hindered amines based on various 2,2,6,6-tetraalkylated nitrogen-containing heterocyclic moieties wherein the hindered nitrogen atom on the ring is substituted with O-acyl, O-carbamoyl or O-carbonate substituents and the 4-position of the ring is substituted with a variety of groups, are effective as light stabilizers in diverse substrate systems.
    Type: Grant
    Filed: May 28, 1993
    Date of Patent: April 5, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Roger F. Malherbe, Roland A. E. Winter, James P. Galbo
  • Patent number: 5190937
    Abstract: Novel compounds of formula (I), and pharmaceutically acceptable salts thereof; their preparation; compositions containing them; and their use in the treatment of conditions in which degradation of connective tissue and other proteinaceous components of the body occurs: ##STR1## in which, R.sub.1 is --OH; alkoxy; aryloxy or aralkyloxy in each of which the aryl group is optionally substituted; --NR.sub.6 R.sub.7, where each of R.sub.6 and R.sub.7 is independently hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are bonded form a 5-, 6- or 7-membered ring with an optional oxygen or sulphur atom or an optionally substituted second nitrogen atom in the ring; or a group:--NH--CH(R.sub.8)--C(O)--R.sub.9where R.sub.8 is hydrogen; alkyl optionally substituted by --OH, alkoxy, --NR.sub.6 R.sub.7 as defined for R.sub.1, guanidine, --CO.sub.2 H, --CONH.sub.2, --SH, or --S--alkyl; or --CH.sub.2 --Ar where Ar is optionally substituted aryl or heteroaryl; and R.sub.
    Type: Grant
    Filed: January 11, 1991
    Date of Patent: March 2, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Roger E. Markwell, Ian Hughes
  • Patent number: 5187275
    Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl or alkoxy, --A.sub.1 --R.sub.2 --N(R.sub.3)-- and --X.sub.1 --(X.sub.2 --X.sub.3).sub.m -- are selected linking groups, Y.sub.1 and Y.sub.2 are selected terminal moieties and n is 1 to 50, are effective light, heat and oxidation stabilizers for a variety of organic materials.
    Type: Grant
    Filed: September 30, 1991
    Date of Patent: February 16, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Valerio Borzatta, Roberto Scrima, Graziano Vignali
  • Patent number: 5149823
    Abstract: A novel class of sulfonamoyl-substituted 1,6-diaza[4.4]spirodilactams, having a sulfonamoyl substituent on the hydrocarbyl group attached to each spiro ring nitrogen atom, is useful for the preparation of polymers, including polyamides and as latent curing agents for epoxy resins.
    Type: Grant
    Filed: August 9, 1990
    Date of Patent: September 22, 1992
    Assignee: Shell Oil Company
    Inventor: Pen-Chung Wang
  • Patent number: 5106971
    Abstract: The prior art solvent process for the manufacture of an oxo-piperazinyl triazine (PIP-T) compound required carrying out the reaction between an appropriately hindered cyclic amine and cyanuric chloride in the presence of caustic catalyst, in alkylbenzene solution, typically toluene. The chloride ions generated during the reaction, in presence of water present in the reaction zone, produced serious corrosion and resulted in off-color product which had a melt absorptivity greater than 3.5 mL/gm.cm. This "color" in the product made the product generally unmarketable. Another process to make a PIP-T termed "the solventless" process used no toluene solvent, and no caustic but required such a very large excess of amine that the catalytic function of the amine.HCl salt went unnoticed.
    Type: Grant
    Filed: April 12, 1991
    Date of Patent: April 21, 1992
    Assignee: The B. F. Goodrich Company
    Inventors: George Kletecka, Victor L. Ledesma, Ronald M. Kovach
  • Patent number: 5041545
    Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.
    Type: Grant
    Filed: April 6, 1989
    Date of Patent: August 20, 1991
    Assignee: Atochem North America, Inc.
    Inventor: Terry N. Myers
  • Patent number: 4970205
    Abstract: Invented are sulfonic acid substituted analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size. Also invented are intermediates used in preparing these compounds.
    Type: Grant
    Filed: December 23, 1988
    Date of Patent: November 13, 1990
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
  • Patent number: 4970306
    Abstract: The invention relates to trans-cyclohexane-1,4-diisocyanate which is completely or partially blocked with epsilon-caprolactam and a method of manufacturing the same wherein 1 mole trans-cyclohexane-1,4-diisocyanate is reacted with 1 to 2 moles epsilon-caprolactam, without or with the presence of solvents. These blocked diisocyanates are used for polyurethane powders.
    Type: Grant
    Filed: December 9, 1988
    Date of Patent: November 13, 1990
    Assignee: Huels Aktiengesellschaft
    Inventors: Rainer Gras, Elmar Wolf
  • Patent number: 4959361
    Abstract: The invention relates to compounds of the formula ##STR1## wherein X is --CH.dbd.CH-- or S; R.sub.1 is lower alkyl, lower alkoxy or trifluoromethyl;R.sub.2 is hydrogen, lower alkyl, lower alkoxy, hydroxy or alkanoyloxy;R.sub.3 and R.sub.4, independently, are hydrogen, chlorine, fluorine, lower alkyl or lower alkoxy;s is an integer from 0 to 1, provided that when s is 1,R.sub.2 cannot be hydroxy, lower alkoxy or alkanoyloxy;R.sub.5 is a radical of the formula R.sub.6 --(CH.sub.2).sub.n -- or R.sub.7 --O--(CH.sub.2).sub.m --wherein R.sub.6 and R.sub.7 are aryl or a heterocyclic radical, n is an integer of from 0 to 2 and m is an integer of from 1 to 2, provided that, when n is 0, R.sub.6 must be attached through a carbon to carbon bond, and provided that R.sub.7 is always attached through a carbon to oxygen bond,and, when at least one asymmetric carbon is present, its enantiomers and racemates, and pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: October 3, 1988
    Date of Patent: September 25, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Armin Walser
  • Patent number: 4886890
    Abstract: This invention relates to quaternary compounds having the formula ##STR1## wherein W.sup.- is an anion; m and n are integers having a value of from 1 to 4; R is alkylene having from 3 to 8 carbon atoms; R.sub.1 is a radical having from 8 to 25 carbon atoms and is selected from the group of alkyl, alkenyl and alkoxy alkylene and each of R.sub.2, R.sub.3 and R.sub.4 is a radical having from 1 to 25 carbon atoms and is alkyl, alkoxy or ##STR2## where p has a value of from 1 to 4 and X is hydrogen or methyl. The invention also relates to the preparation and use of said diquaternized compounds.
    Type: Grant
    Filed: September 29, 1988
    Date of Patent: December 12, 1989
    Assignee: GAF Corporation
    Inventors: Ratan K. Chaudhuri, David J. Tracy, Robert B. Login
  • Patent number: 4868298
    Abstract: A continuous method for the high-yield, one-step, solvent-free manufacture of blocked polyisocyanurate compounds useful as curing agents in powder coating compositions. The preferred method of manufacture is to pre-mix a blocking agent and a polymerization catalyst (BAC mix) prior to injection with an organic isocyanate monomer having two or more isocyanate groups (herein termed a polyisocyanate) into a preheated reaction zone wherein the BAC mix and the polyisocyanate react to form the blocked polyisocyanurate compound that is obtained after discharge from the reaction zone and cooling.
    Type: Grant
    Filed: June 22, 1988
    Date of Patent: September 19, 1989
    Assignee: Cargill, Incorporated
    Inventor: Larry F. Brinkman
  • Patent number: 4801586
    Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein X and Y, each, may represent sulfur, oxygen or two hydrogen atoms, A is a branched or a straight chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having 1-4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkylformyl; m is 3-7; q is 2m-2x, wherein x equals the number of double bonds in the lactam ring and may be 1, 2 or 3, and R is CH.sub.3, ##STR2## wherein R" is H or halogen.
    Type: Grant
    Filed: October 7, 1986
    Date of Patent: January 31, 1989
    Assignee: Nelson Research & Development Co.
    Inventors: Gevork Minaskanian, James V. Peck
  • Patent number: 4792603
    Abstract: A method for producing a polyether-polyamide block copolymer is disclosed, comprising copolymerizing, in the presence of an anionic polymerization catalyst, a lactam and a polyether prepolymer presented by the formula: ##STR1## wherein R.sup.1 is an aliphatic hydrocarbon residual group having 2 to 6 carbon atoms, R.sup.2 is an aliphatic hydrocarbon residual group having 3 to 12 carbon atoms, and n is an integer of 4 to 450. The polyester prepolymer is prepared by reacting a polyoxyalkylene having two terminal hydroxy groups with an N-chlorocarbonyl lactam. The polyether-polyamide block according to the invention has high impact strength and is substantially colorless.
    Type: Grant
    Filed: October 2, 1986
    Date of Patent: December 20, 1988
    Assignee: Sumitomo Chemical Co., Ltd.
    Inventors: Takeo Saegusa, Jiro Horikawa, Masahiro Niwano, Takenobu Kanazawa
  • Patent number: 4767769
    Abstract: Compounds of formula I ##STR1## in which R.sub.1 and R.sub.2, which may be the same or different, are hydrogen, a C.sub.1 to C.sub.3 alkyl group or R.sub.1 and R.sub.2 together with the nitrogen to which they are attached form an optionally substituted heterocyclic ring; R.sub.3 and R.sub.4, which may be the same or different are hydrogen, a C.sub.1 to C.sub.3 alkyl or an optionally substituted C.sub.3 to C.sub.6 cycloalkyl group, or R.sub.3 and R.sub.4 together with the nitrogen to which they are attached form an optionally substituted heterocyclic ring; m is 0, 1 or 2; p is 0, 1 or 2; E is an alkylene group connected to or interrupted by an oxygen or a sulphur atom; J is hydrogen or a substituent group; and their pharmaceutically acceptable salts have utility as histamine H.sub.2 -receptor antagonists.
    Type: Grant
    Filed: June 23, 1987
    Date of Patent: August 30, 1988
    Assignee: The Boots Company PLC
    Inventors: Michael H. Hockley, Roger B. Titman
  • Patent number: 4755535
    Abstract: This invention provides compositions comprising a physiologically-active agent and an azacycloalkene having at least one double bond in the ring and of the general formula ##STR1## wherein X and Y, each, may represent sulfur, oxygen or two hydrogen atoms, A is a straight or branched chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having 1-4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkylformyl; m is 3-7; q is 2m-2x, wherein x equals the number of double bonds in the lactam ring and may be 1, 2 or 3; and R is --CH.sub.3, ##STR2## wherein R" is H or halogen in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.
    Type: Grant
    Filed: April 23, 1986
    Date of Patent: July 5, 1988
    Assignee: Nelson Research & Development Co.
    Inventors: Gevork Minaskanian, James V. Peck
  • Patent number: 4698412
    Abstract: Copolymers of propylene oxide and N-epoxy propyl lactams having the structures ##STR1## wherein R is ##STR2## a has a value of 1-3; p has a value of 1-2; m has a value of 0-1; k has a value of 2-200; w and z each have a value of 2-50 x and y have a value of 2-100; and also the process for preparing the aforementioned copolymers as well as their use as surfactants.
    Type: Grant
    Filed: March 2, 1987
    Date of Patent: October 6, 1987
    Assignee: GAF Corporation
    Inventors: David J. Tracy, Robert B. Login, Mohamed M. Hashem
  • Patent number: 4666902
    Abstract: Tetrahydropyridazinones of the formula I ##STR1## wherein R denotes an optionally substituted carbocyclic or heterocyclic radical, R.sup.1 denotes hydrogen; alkyl; aralkyl, which is optionally substituted in the aryl part; or acyl, and R.sup.2 denotes hydrogen; alkyl, which can optionally be substituted; or optionally substituted phenyl; and their acid addition compounds, if these can be prepared.The tetrahydropyridazinone derivatives of the formula I according to the invention and their physiologically acceptable salts exhibit useful pharmacological actions.
    Type: Grant
    Filed: June 8, 1984
    Date of Patent: May 19, 1987
    Assignee: Cassella Aktiengesellschaft
    Inventors: Gerhard Zoller, Rudi Beyerle, Melitta Just, Piero Martorana, Helmut Bohn, Rolf-Eberhard Nitz
  • Patent number: 4650608
    Abstract: A novel star block copolymer represented by the general formula as shown below and a process for the production thereof are described. The copolymer has superior physical properties, particularly impact strength and, furthermore, is reduced in coloration. Thus the copolymer can find numerous uses; for example, it can be used in preparation of fibers, foams, automotive parts, and electrical components. The copolymer is produced by copolymerizing a star-shaped polyether prepolymer and a lactam, said prepolymer being prepared by reacting a star-shaped polyoxyalkylene having at least 3 terminal hydroxy groups and an N-chlorocarbonyl lactam, in the presence of an anionic polymerization catalyst. ##STR1## In this formula, all the symbols are as defined hereinbefore.
    Type: Grant
    Filed: August 6, 1985
    Date of Patent: March 17, 1987
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Saegusa Takeo, Jiro Horikawa, Masahiro Niwano, Takenobu Kanazawa
  • Patent number: 4644051
    Abstract: The invention concerns a simple process for preparing an ester acyllactam and/or esteramide acyllactam by the catalytic condensation of imide and alcohol, characterized in that a polyol and an acyllactam compound are reacted in the liquid state in the presencce of a halide, carboxylate or acetylacetonate from beryllium, magnesium, calcium, strontium, barium, boron, aluminium, zinc or cadmium.The invention is important for the preparation of compounds which may be used in the preparation of nylon block copolymers, more in particular in RIM-nylon systems (Reaction Injection Moulding), since when the compounds obtained according to the present invention are used in a RIM system, a very fast lactam polymerization takes place, and it therefore also relates to the preparation of nylon block copolymers.
    Type: Grant
    Filed: December 26, 1984
    Date of Patent: February 17, 1987
    Assignee: Stamicarbon B.V.
    Inventor: Albert A. Van Geenen
  • Patent number: 4639442
    Abstract: A class of benzocyclobutene aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.
    Type: Grant
    Filed: November 1, 1985
    Date of Patent: January 27, 1987
    Assignee: William H. Rorer, Inc.
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
  • Patent number: 4628075
    Abstract: A composition containing acid halide functional materials, which are useful in the preparation of nylon block polymers, selected from the group consisting of: ##STR1## wherein, X is a halogen;b is an integer equal to 2 or more;R.sub.1 is an alkyl, aryl, aralkyl, alkyloxy, halogen, aryloxy, or aralkyloxy group; andZ is a segment of: (1) a polyether, provided said polyether is not solely polyarylene polyether; (2) a polyester containing polyether or polymeric hydrocarbon segments (3) a polysiloxane; or (4) combinations thereof.
    Type: Grant
    Filed: July 3, 1985
    Date of Patent: December 9, 1986
    Assignee: DSM RIM Nylon VOF
    Inventors: James D. Gabbert, Albert Y. Garner, Ross M. Hedrick
  • Patent number: 4626385
    Abstract: An N-substituted carbamoyl-lactam compound of the formula ##STR1## wherein R is a di-valent radical derived from polytetramethylene glycol, R' is an at least divalent radical derived from a diisocyanate, Y is a C.sub.3 -C.sub.14 ring-forming alkylene group, and a has a value of at least 1 and is a number corresponding to the mean functionality of the aforesaid polyisocyanate minus 1. A process for preparing the N-substituted carbamoyl-lactam compound is also described.
    Type: Grant
    Filed: May 21, 1985
    Date of Patent: December 2, 1986
    Inventors: Kaneyoshi Ashida, Jozef L. M. van der Loos