Plural Seven-membered Hetero Rings Patents (Class 540/525)
-
Patent number: 8765731Abstract: 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: GrantFiled: November 16, 2012Date of Patent: July 1, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: 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: 8623945Abstract: 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: GrantFiled: March 15, 2012Date of Patent: January 7, 2014Assignee: BASF SEInventors: Theo Smit, Laurence Pottie, Simone Schillo, Volker Frenz, Roelof van der Meer
-
Publication number: 20130157997Abstract: 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: ApplicationFiled: November 16, 2012Publication date: June 20, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
-
Publication number: 20120238676Abstract: 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: ApplicationFiled: March 15, 2012Publication date: September 20, 2012Applicant: BASF SEInventors: THEO SMIT, LAURENCE POTTIE, SIMONE SCHILLO, VOLKER FRENZ, ROELOF VAN DER MEER
-
Publication number: 20120165519Abstract: 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: ApplicationFiled: March 6, 2012Publication date: June 28, 2012Applicant: 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: 20100221259Abstract: 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: ApplicationFiled: May 10, 2010Publication date: September 2, 2010Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Masaya KOKUBO, Shiro SHIBAYAMA, Hideaki TADA, Tatsuya TANIHIRO
-
Patent number: 7563784Abstract: 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: GrantFiled: April 25, 2006Date of Patent: July 21, 2009Assignee: SmithKline Beecham CorporationInventors: Maxwell D. Cummings, Robert W. Marquis, Jr., Yu Ru, Scott K. Thompson, Daniel F. Veber, Dennis S. Yamashita
-
Publication number: 20090093628Abstract: 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: ApplicationFiled: February 27, 2007Publication date: April 9, 2009Inventors: Yasutaka Ishii, Tatsuya Nakano, Takahiro Iwahama
-
Patent number: 7405209Abstract: 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: GrantFiled: June 14, 2005Date of Patent: July 29, 2008Assignees: 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: 7071184Abstract: 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: GrantFiled: March 7, 2001Date of Patent: July 4, 2006Assignee: SmithKline Beecham CorporationInventors: Maxwell D. Cummings, Robert W. Marquis, Jr., Daniel F. Veber, Dennis S. Yamashita
-
Patent number: 7030201Abstract: The present invention relates to bottom antireflective coating compositions and polymers useful in making such compositions.Type: GrantFiled: November 26, 2003Date of Patent: April 18, 2006Assignee: AZ Electronic Materials USA Corp.Inventors: Huirong Yao, Shuji Ding-Lee, Hengpeng Wu, Zhong Xiang
-
Patent number: 6958329Abstract: 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: GrantFiled: November 4, 2002Date of Patent: October 25, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Richard E. Olson
-
Patent number: 6852713Abstract: Lactam derivatives of the general formula are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed.Type: GrantFiled: April 16, 2003Date of Patent: February 8, 2005Assignee: Adolor CorporationInventors: Roland E. Dolle, Paul Anson Tuthill
-
Patent number: 6699988Abstract: 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: GrantFiled: April 23, 2001Date of Patent: March 2, 2004Assignee: SNPEInventors: Hubert Bonnard, Laurence Ferruccio, Jean-Pierre Senet, Pierre-Yves Le Roy
-
Publication number: 20040024203Abstract: 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: ApplicationFiled: April 11, 2003Publication date: February 5, 2004Inventors: Ian Churcher, Alan John Nadin, Andrew Pate Owens
-
Patent number: 6566376Abstract: 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: GrantFiled: September 8, 2000Date of Patent: May 20, 2003Assignee: AstraZeneca UK LimitedInventors: Andrew J G Baxter, Stephen J Brough, Thomas McInally
-
Patent number: 6495540Abstract: 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: GrantFiled: March 27, 2001Date of Patent: December 17, 2002Assignee: Bristol - Myers Squibb Pharma CompanyInventor: Lorin A. Thompson
-
Patent number: 6476016Abstract: 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: GrantFiled: July 17, 2001Date of Patent: November 5, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Aihua Wang, Bruce Edward Tomczuk, Tianbao Lu, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
-
Patent number: 6448394Abstract: 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: GrantFiled: March 23, 2001Date of Patent: September 10, 2002Assignee: DSM N.V.Inventors: Jacobus A. Loontjens, Bartholomeus J. M. Plum
-
Publication number: 20020028932Abstract: 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: 1Type: ApplicationFiled: March 23, 2001Publication date: March 7, 2002Inventors: Jacobus A. Loontjens, Bartholomeus J.M. Plum
-
Patent number: 6344450Abstract: 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: GrantFiled: August 7, 2000Date of Patent: February 5, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Gregory S. Bisacchi, Steven M. Seiler, R. Michael Lawrence, James C. Sutton, Jr., William A. Slusarchyk, Guohua Zhao
-
Patent number: 6051678Abstract: 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: GrantFiled: March 13, 1997Date of Patent: April 18, 2000Assignee: Hyundai Electronics Industries Co., Ltd.Inventors: Jin Baek Kim, Min Ho Jung, Jong Ho Cheong
-
Patent number: 5972237Abstract: 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: GrantFiled: November 17, 1997Date of Patent: October 26, 1999Assignee: BASF AktiengesellschaftInventors: Reinhard Muller, Thomas Wehlage, Wolfgang Trieselt, Alfred Oftring, Elisabeth Kappes, Gunter Oetter, Dieter Boeckh, Roland Ettl, Albert Hettche
-
Patent number: 5955606Abstract: 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: GrantFiled: February 19, 1998Date of Patent: September 21, 1999Assignee: Hyundai Electronics Industries Co., Ltd.Inventors: Jin Baek Kim, Min Ho Jung, Kyeong Ho Chang
-
Patent number: 5750680Abstract: 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: GrantFiled: September 12, 1996Date of Patent: May 12, 1998Assignees: Hyundai Electronics Industries Co., Ltd., Korea Advanced Institute of Science & TechnologyInventors: Jin Baek Kim, Min Ho Jung, Kyeong Ho Chang
-
Patent number: 5561235Abstract: 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: GrantFiled: June 7, 1995Date of Patent: October 1, 1996Assignee: The Procter & Gamble CompanyInventors: Eugene P. Gosselink, Gregory S. Miracle, Alan D. Willey, Michael E. Burns, Kevin L. Kott, Mark R. Sivik, Lucille F. Taylor
-
Patent number: 5336706Abstract: 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: GrantFiled: September 29, 1993Date of Patent: August 9, 1994Assignee: Ciba-Geigy CorporationInventors: Valerio Borzatta, Roberto Scrima, Graziano Vignali
-
Patent number: 5300647Abstract: 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: GrantFiled: May 28, 1993Date of Patent: April 5, 1994Assignee: Ciba-Geigy CorporationInventors: Roger F. Malherbe, Roland A. E. Winter, James P. Galbo
-
Patent number: 5300640Abstract: 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: GrantFiled: December 19, 1991Date of Patent: April 5, 1994Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsumori Hiratsuka, Naonori Hirata, Kazuo Saito, Hideyuki Shibata
-
Patent number: 5190937Abstract: 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: GrantFiled: January 11, 1991Date of Patent: March 2, 1993Assignee: Beecham Group p.l.c.Inventors: Roger E. Markwell, Ian Hughes
-
Patent number: 5187275Abstract: 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: GrantFiled: September 30, 1991Date of Patent: February 16, 1993Assignee: Ciba-Geigy CorporationInventors: Valerio Borzatta, Roberto Scrima, Graziano Vignali
-
Patent number: 5149823Abstract: 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: GrantFiled: August 9, 1990Date of Patent: September 22, 1992Assignee: Shell Oil CompanyInventor: Pen-Chung Wang
-
Patent number: 5106971Abstract: 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: GrantFiled: April 12, 1991Date of Patent: April 21, 1992Assignee: The B. F. Goodrich CompanyInventors: George Kletecka, Victor L. Ledesma, Ronald M. Kovach
-
Patent number: 5041545Abstract: 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: GrantFiled: April 6, 1989Date of Patent: August 20, 1991Assignee: Atochem North America, Inc.Inventor: Terry N. Myers
-
Patent number: 4970205Abstract: 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: GrantFiled: December 23, 1988Date of Patent: November 13, 1990Assignee: SmithKline Beecham CorporationInventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
-
Patent number: 4970306Abstract: 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: GrantFiled: December 9, 1988Date of Patent: November 13, 1990Assignee: Huels AktiengesellschaftInventors: Rainer Gras, Elmar Wolf
-
Patent number: 4959361Abstract: 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: GrantFiled: October 3, 1988Date of Patent: September 25, 1990Assignee: Hoffmann-La Roche Inc.Inventor: Armin Walser
-
Patent number: 4886890Abstract: 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: GrantFiled: September 29, 1988Date of Patent: December 12, 1989Assignee: GAF CorporationInventors: Ratan K. Chaudhuri, David J. Tracy, Robert B. Login
-
Patent number: 4868298Abstract: 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: GrantFiled: June 22, 1988Date of Patent: September 19, 1989Assignee: Cargill, IncorporatedInventor: Larry F. Brinkman
-
Patent number: 4801586Abstract: 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: GrantFiled: October 7, 1986Date of Patent: January 31, 1989Assignee: Nelson Research & Development Co.Inventors: Gevork Minaskanian, James V. Peck
-
Patent number: 4792603Abstract: 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: GrantFiled: October 2, 1986Date of Patent: December 20, 1988Assignee: Sumitomo Chemical Co., Ltd.Inventors: Takeo Saegusa, Jiro Horikawa, Masahiro Niwano, Takenobu Kanazawa
-
Patent number: 4767769Abstract: 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: GrantFiled: June 23, 1987Date of Patent: August 30, 1988Assignee: The Boots Company PLCInventors: Michael H. Hockley, Roger B. Titman
-
Patent number: 4755535Abstract: 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: GrantFiled: April 23, 1986Date of Patent: July 5, 1988Assignee: Nelson Research & Development Co.Inventors: Gevork Minaskanian, James V. Peck
-
Patent number: 4698412Abstract: 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: GrantFiled: March 2, 1987Date of Patent: October 6, 1987Assignee: GAF CorporationInventors: David J. Tracy, Robert B. Login, Mohamed M. Hashem
-
Patent number: 4666902Abstract: 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: GrantFiled: June 8, 1984Date of Patent: May 19, 1987Assignee: Cassella AktiengesellschaftInventors: Gerhard Zoller, Rudi Beyerle, Melitta Just, Piero Martorana, Helmut Bohn, Rolf-Eberhard Nitz
-
Patent number: 4650608Abstract: 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: GrantFiled: August 6, 1985Date of Patent: March 17, 1987Assignee: Sumitomo Chemical Company, LimitedInventors: Saegusa Takeo, Jiro Horikawa, Masahiro Niwano, Takenobu Kanazawa
-
Patent number: 4644051Abstract: 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: GrantFiled: December 26, 1984Date of Patent: February 17, 1987Assignee: Stamicarbon B.V.Inventor: Albert A. Van Geenen
-
Patent number: 4639442Abstract: 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: GrantFiled: November 1, 1985Date of Patent: January 27, 1987Assignee: William H. Rorer, Inc.Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
-
Patent number: 4628075Abstract: 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: GrantFiled: July 3, 1985Date of Patent: December 9, 1986Assignee: DSM RIM Nylon VOFInventors: James D. Gabbert, Albert Y. Garner, Ross M. Hedrick
-
Patent number: 4626385Abstract: 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: GrantFiled: May 21, 1985Date of Patent: December 2, 1986Inventors: Kaneyoshi Ashida, Jozef L. M. van der Loos