Ring Chalcogen In The Additional Hetero Ring Patents (Class 544/374)
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Patent number: 6387908Abstract: Epoxysuccinamide derivatives of the formula (1): wherein R1 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or aralkyl; R2 is alkyl, alkenyl, alkynyl, aryl, or aralkyl; R3 is hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, heterocyclic, or heterocyclic-alkyl; X is —O— or —NR4— (R4 is hydrogen, alkyl, aryl, aralkyl, heterocyclic, or heterocyclic-alkyl); Y1 is OR5, SR6, or NR7R8; and Y2 is hydrogen or alkyl. The compounds are useful as remedies for bone diseases and arthritis.Type: GrantFiled: May 5, 2000Date of Patent: May 14, 2002Assignee: Nippon Chemiphar Co., Ltd.Inventors: Yutaka Nomura, Toshihiro Takahashi, Yasushi Yoshino, Koichiro Nishioka
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Patent number: 6340700Abstract: A compound of the formula wherein the substituents are defined as in the specification and their pharmaceutically acceptable salts having NOS and ROS activity.Type: GrantFiled: September 22, 1999Date of Patent: January 22, 2002Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auguet
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Patent number: 6340701Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.Type: GrantFiled: November 22, 2000Date of Patent: January 22, 2002Assignee: Immunogen INCInventors: Ravi V. J. Chari, Walter A. Blättler
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Publication number: 20020002168Abstract: A compound of the formula 1Type: ApplicationFiled: May 22, 2001Publication date: January 3, 2002Inventor: Harry R. Howard
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Patent number: 6335445Abstract: A compound selected from the group consisting of a compound of the formula wherein A is selected from the group consisting of and the other substituents are defined in the specification having an inhibitory activity of NO-synthase enzymes producing nitrogen mono-oxide and/or an activity which traps the reactive oxygen species.Type: GrantFiled: December 7, 1999Date of Patent: January 1, 2002Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auguet, Jeremiah Harnett
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Publication number: 20010041705Abstract: A compound of the formula 1Type: ApplicationFiled: May 22, 2001Publication date: November 15, 2001Inventor: Harry R. Howard
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Patent number: 6313293Abstract: The present invention relates to a process for the preparation of amides, comprising reacting amines with carboxylic acids in the presence of silicon amines. The present invention further relates to a process for the preparation of quinazoline derivatives, comprising reacting amines with carboxylic acids in the presence of silicon amines to obtain amides and contacting the resultant amides with quinazoline.Type: GrantFiled: March 1, 2000Date of Patent: November 6, 2001Assignee: Development Center for BiotechnologyInventors: Wen-Chih Chou, Ming-Chen Chou, Yann-Yu Lu, Shyh-Fong Chen
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Patent number: 6313294Abstract: The present invention provides a process for preparing an amide, which comprises reacting an amine with an ester in a molten form in the absence of a solvent.Type: GrantFiled: July 8, 1998Date of Patent: November 6, 2001Assignee: Development Center for BiotechnologyInventors: Wen-Chih Chou, Chang-Wei Tan, Shyh-Fong Chen, Hao Ku
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Patent number: 6281210Abstract: The present invention provides a compound of formula I which have potent activities against gram positive and gram-negative bacteria.Type: GrantFiled: December 6, 2000Date of Patent: August 28, 2001Assignee: Pharmacia & Upjohn CompanyInventor: Jackson B. Hester, Jr.
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Patent number: 6281214Abstract: A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: wherein R1, R2, R3, R4, and R5 are defined in the specification, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis. The compounds exhibit dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism.Type: GrantFiled: October 5, 1998Date of Patent: August 28, 2001Assignee: Eisai Co., LtdInventors: Kozo Akasaka, Masahiro Yonaga, Akiharu Kajiwara, Kunizo Higurashi, Kohshi Ueno, Satoshi Nagato, Makoto Komatsu, Noritaka Kitazawa, Masataka Ueno, Yoshiharu Yamanishi, Yoshimasa Machida, Yuki Komatsu, Naoyuki Shimomura, Norio Minami, Toshikazu Shimizu, Atsushi Nagaoka
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Patent number: 6197750Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.Type: GrantFiled: October 22, 1998Date of Patent: March 6, 2001Assignee: Idun Pharmaceuticals, Inc.Inventors: Donald S. Karanewsky, Robert J. Ternansky
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Patent number: 6187924Abstract: Compounds of formula (I) are useful as therapeutic agents, by virtue of having MMP and TNF inhibitory activity.Type: GrantFiled: November 12, 1998Date of Patent: February 13, 2001Assignee: Darwin Discovery, Ltd.Inventors: Andrew Douglas Baxter, David Alan Owen, John Gary Montana, Robert John Watson
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Patent number: 6156787Abstract: The present invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof: ##STR1## where A is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, arylC.sub.1-6 alkyl, aryl, S(O),R.sup.1, OR.sup.1 or NR.sup.1 R.sup.6 ;R.sup.1 is hydrogen; C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkenyl each of which is optionally substituted by amino, C.sub.1-6 alkylamino, di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkoxy, C.sub.1-6 alkylaminocarbonyl, one, two or three hydroxy groups, one, two or three halogen atoms or a four, five or six-membered saturated heterocyclic ring containing a nitrogen atom and optionally either an oxygen atom or a further nitrogen atom which ring is optionally substituted by C.sub.1-4 alkyl on the further nitrogen atom; aryl, arylC.sub.1-6 alkyl, arylC.sub.2-6 alkenyl or arylC.sub.2-6 alkynyl optionally substituted on the aryl ring by halogen, nitro, cyano, C.sub.Type: GrantFiled: April 22, 1999Date of Patent: December 5, 2000Assignee: Merck Sharp & Dohme LimitedInventors: Howard Barff Broughton, Mark Stuart Chambers
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Patent number: 6147212Abstract: The invention relates to new amino acid derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein group B is --A.sup.2 --NR.sup.2 R.sup.3 or R.sup.5, wherein group R.sup.5 is ##STR1## and R.sup.1, A.sup.1, A.sup.2, R.sup.2, R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.9, X, Y, Z, t and u have the meanings described in the specification, as well as the preparation and use thereof. The novel compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: July 8, 1998Date of Patent: November 14, 2000Assignee: Boehringer Ingelheim KGInventors: Franz Esser, Gerd Schnorrenberg, Horst Dollinger, Birgit Jung, Erich Burger
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Patent number: 6143740Abstract: The invention provides a method of inhibiting cancer cell growth, and thereby of treating cancer comprising administering to a mammal afflicted with cancer an effective amount of the compound of formula (I), wherein the variables of R.sub.1, and R.sub.2 have the meanings defined in the specification. The present invention also provides novel compounds of formula (I) as well as novel pharmaceutical compositions and intermediates useful for preparing compounds of formula (I). The figure illustrates the structure and binding activity of compounds of the invention and some of the rifamycin analogs.______________________________________ ##STR1##______________________________________ Compounds R.sub.1 = ______________________________________ A1 --OH A2 --OH A3 --OH A4 --OH A5 --OH A6 --OH A7 --OH - A8 ##STR2## ______________________________________ Compounds R.sub.Type: GrantFiled: August 16, 1999Date of Patent: November 7, 2000Assignee: Georgetown UniversityInventors: Dajun Yang, Shaomeng Wang, Alan P. Kozikowski, Marc E. Lippman
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Patent number: 6136808Abstract: This invention relates to a taxane derivative represented by the following formula (1): ##STR1## (wherein A represents a substituted piperazino or piperidino group, X represents an alkyl, pyridyl, thienyl, furyl, cycloalkyloxy or the like and Y represents H or trialkylsilyl) and also to a drug containing the same.This compound has high solubility in water and also has excellent antitumor activities.Type: GrantFiled: March 16, 2000Date of Patent: October 24, 2000Assignee: Kabushiki Kaisha Yakult HonshaInventors: Atsuhiro Abe, Hideaki Shimizu, Seigo Sawada, Takanori Ogawa, Hiroshi Nagata
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Patent number: 6114335Abstract: The present invention relates to novel benzoylguanidine derivatives, processes for preparing them and their use in the preparation of pharmaceutical compositions.The novel benzoylguanidine derivatives correspond to general formula (I) ##STR1## which benzoylguanidine derivatives are useful in the treatment of ischemia.Type: GrantFiled: September 25, 1998Date of Patent: September 5, 2000Assignee: Boehringer Ingelheim KGInventors: Erich Buerger, Christian Eickmeier, Otto Roos
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Patent number: 6080860Abstract: Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted Quinazolines), Meobentine and Bethanidine and novel intermediates suitable for use in such methods of synthesis are taught.Type: GrantFiled: September 29, 1997Date of Patent: June 27, 2000Assignee: Brantford Chemicalss Inc.Inventors: Khashayar Karimian, Keshava Murthy, Darren Hall
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Patent number: 6051571Abstract: Disclosed are methods for treating a patient with an acute central nervous system or cardiovascular disorder or a neurodegenerative, autoimmune or inflammatory disease using a pharmaceutical composition containing a pharmaceutically acceptable carrier and an effective amount of a furan nitrone compound.Type: GrantFiled: May 24, 1999Date of Patent: April 18, 2000Assignee: Centaur Pharmaceuticals, Inc.Inventors: Judith A. Kelleher, Kirk R. Maples, Lowell David Waterbury, Hong Xu, Yong-Kang Zhang
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Patent number: 6040444Abstract: Disclosed are processes for preparing furan nitrone compounds using a furan carbonyl compound and a hydroxylamine compound.Type: GrantFiled: May 24, 1999Date of Patent: March 21, 2000Assignee: Centaur Pharmaceuticals, Inc.Inventors: Allan L. Wilcox, Yong-Kang Zhang
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Patent number: 6030952Abstract: The present invention provides novel heteroaryl compounds having the general formula (I): ##STR1## their pharmaceutical compositions to be used as human and veterinary medicine, particularly in the treatment of dermatological, rheumatic, respiratory, cardiovascular and ophthalmologic conditions, and their use in cosmetic compositions.Type: GrantFiled: October 13, 1998Date of Patent: February 29, 2000Assignee: Centre International de Recherches Dermatologioues galdermaInventors: Philippe Diaz, Bruno Charpentier
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Patent number: 6017935Abstract: The present invention relates to novel taxane derivatives wherein, the taxol ring is substituted by sulfur groups on the C-7, their use as antitumor agents and pharmaceutical formulations.Type: GrantFiled: April 14, 1998Date of Patent: January 25, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Harold Mastalerz, John F. Kadow
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Patent number: 5942507Abstract: Disclosed are furan nitrone compounds and pharmaceutical compositions containing such compounds. The disclosed compounds are useful as analytical reagents for detecting free radicals and as therapeutics for treating a wide variety of medical dysfunctions and diseases.Type: GrantFiled: July 17, 1997Date of Patent: August 24, 1999Assignee: Centaur Pharmaceuticals, Inc.Inventors: Judith A. Kelleher, Kirk R. Maples, Lowell David Waterbury, Allan L. Wilcox, Hong Xu, Yong-Kang Zhang
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Patent number: 5935959Abstract: The present invention is directed to a compound of the following formula (I) inclusive of its salt ##STR1## ?wherein R.sup.1 represents either carboxy which may be esterified or amidated carboxy which may be substituted; R.sup.2 represents hydrogen or lower alkyl and may be linked to R.sup.3 or R.sup.4 to form a ring; R.sup.3 and R.sup.4 may be the same or different and each represents hydrogen, lower alkyl which may be substituted, or a sulfide group which may be substituted, and R.sup.3 and R.sup.4 may conjoinedly form a ring; R.sup.5 represents a substituted phenyl group of formula (II) ##STR2## (wherein R.sup.6 represents halogen or alkoxy) or a substituted sulfonyl group of formula (III)--SO.sub.2 --R.sup.7 (III)(wherein R.sup.7 represents either aryl which may be substituted by lower alkyl or amino which may be substituted); n is to 0 or 1! and to a method for producing the same compound, which is useful for the treatment of cysteine protease-associated diseases.Type: GrantFiled: January 7, 1998Date of Patent: August 10, 1999Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Jun Inoue, Yuka Yoshida, Ying-She Cui, Mitsuyoshi Azuma
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Patent number: 5919777Abstract: The present invention relates to novel compounds of the general formula I ##STR1## which can be used for treating medical disorders resulting from a deficiency in growth hormone.Type: GrantFiled: April 23, 1997Date of Patent: July 6, 1999Assignee: Novo Nordisk A/SInventors: Thomas Kruse Hansen, Bernd Pesche, Knud Erik Andersen
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Patent number: 5919931Abstract: A process is provided for the manufacture of: where R is: ##STR1## comprising reacting: ##STR2## wherein R.sub.1 may be selected from H, Methyl, Ethyl and suitable lower alkyl groups, C.sub.n H.sub.2n+1 (where n is from 3 to 5) or any other suitable group and thereafter if desired converting the resultant product to a salt thereof.Type: GrantFiled: April 4, 1996Date of Patent: July 6, 1999Assignee: Brantford Chemicals Inc.Inventors: K. S. Keshava Murthy, Gamini Weeratunga, Tianhao Zhou, Bhaskar Reddy Guntoori
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Patent number: 5914351Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.Type: GrantFiled: December 12, 1997Date of Patent: June 22, 1999Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
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Patent number: 5900415Abstract: This invention encompasses compounds of formula (I) and the pharmaceutically ##STR1## acceptable salts thereof, wherein W,X,Y,A,T,R.sub.1 -R.sub.4,B,Ar,n and m are described herein and are useful in treating feeding disorders and certain cardiovascular diseases due to the binding of these compounds to human Neuropeptide Y1 receptors.Type: GrantFiled: April 29, 1997Date of Patent: May 4, 1999Assignee: Pfizer Inc.Inventors: John Matthew Peterson, Charles Albert Blum, Guolin Cai, Alan Jeffrey Hutchison
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Patent number: 5892037Abstract: The invention relates to compounds obtainable by polymerization of esters or phenol ethers of the formula V ##STR1## and/or of the formula VI ##STR2## in which m and n are each 0 or 1, and A, E, R.sup.1 to R.sup.6 and X are as defined in claim 1, and up to 50 mol % of other, ethylenically unsaturated compounds. The homopolymers and copolymers according to the invention can advantageously be employed for the stabilization of organic polymers against the harmful effect of light, oxygen and/or heat.Type: GrantFiled: March 12, 1996Date of Patent: April 6, 1999Assignee: Ciba Specialty Chemicals CorporationInventor: Alfred Steinmann
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Patent number: 5866577Abstract: An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group.The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.Type: GrantFiled: September 5, 1997Date of Patent: February 2, 1999Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Takayasu Nagahara, Naoaki Kanaya, Kazue Inamura, Yukio Yokoyama
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Patent number: 5861512Abstract: Intermediates of structural formula ##STR1## can be made by reacting a primary or secondary amine with glycosidol or an activated derivative thereof. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.Type: GrantFiled: September 16, 1997Date of Patent: January 19, 1999Assignee: Merck & Co., Inc.Inventors: David Askin, Kai Rossen, Paul Reider, Richard J. Varsolona, Ralph P. Volante, Kenneth M. Wells
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Patent number: 5852021Abstract: Polymorph B of (1-diphenylmethyl)-4-?3-(2-phenyl-1,3-dioxolan-2-yl)propyl!piperazine have been identified. A process for its preparation and its use are described.Type: GrantFiled: December 27, 1996Date of Patent: December 22, 1998Assignee: Ferrer Internacional, S.A.Inventors: Rafael Foguet Ambros, Lluis Anglada Burniol, Manuel Raga Carreno, Jose A. Ortiz Hernandez, Aurelio Sacristan Munoz, Josep M. Castello Barenys
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Patent number: 5852011Abstract: Disclosed are compounds represented by the following chemical formula (I) and pharmacologically acceptable salts thereof which are novel compounds useful as anticancer agents, antiviral agents or antimicrobial agents.Type: GrantFiled: January 19, 1996Date of Patent: December 22, 1998Assignee: Mitsui Chemicals, Inc.Inventors: Akio Matsunaga, Yuki Nakajima, Hiroshi Kohno, Hironori Komatsu, Hajime Edatsugi, Daiji Iwata, Kimiko Takezawa
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Patent number: 5852018Abstract: Piperazine derivatives of formula (A): ##STR1## wherein .sub.-------- denotes an optional bond, provided that either .sub.----.sup.a.sub.---- and .sub.----.sup.c.sub.---- are both bonds and .sub.----.sup.b.sub.---- and .sub.----.sup.d.sub.---- are not bonds, or .sub.----.sup.b.sub.---- and .sub.----.sup.d.sub.---- are both bonds and .sub.----.sup.a.sub.---- and .sub.----.sup.c.sub.---- are not bonds; each of R.sub.14 and R.sub.15 is independently selected from hydrogen and C.sub.1 -C.sub.6 alkyl which is unsubstituted or substituted by an organic functional group; and each of R.sub.1 to R.sub.10, which may be the same or different, is independently hydrogen or an organic functional group; and the pharmaceutically acceptable salts and esters thereof have utility as modulators of multiple drug resistance (MDR).Type: GrantFiled: November 4, 1996Date of Patent: December 22, 1998Assignee: Xenova LimitedInventors: Justin Stephen Bryans, Christopher John Latham, Stephen James Brocchini
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Patent number: 5849912Abstract: A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are defined in the specification, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis. The compounds exhibit dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism.Type: GrantFiled: May 12, 1997Date of Patent: December 15, 1998Assignee: Eisai Co., Ltd.Inventors: Kozo Akasaka, Masahiro Yonaga, Akiharu Kajiwara, Kunizo Higurashi, Kohshi Ueno, Satoshi Nagato, Makoto Komatsu, Noritaka Kitazawa, Masataka Ueno, Yoshiharu Yamanishi, Yoshimasa Machida, Yuki Komatsu, Naoyuki Shimomura, Norio Minami, Toshikazu Shimizu, Atsushi Nagaoka
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Patent number: 5849745Abstract: A compound of formula (I): ##STR1## In which: R.sub.1 represents linear or branched (C.sub.1 -C.sub.6) alkyl,X represents oxygen or sulfur,R.sub.2 represents optionally substituted alkyl, alkoxy, optionally substituted phenyl, optionally substituted cycloalkyl, 4-(2,3-dithiacyclopent-1-yl)butyl, pyridyl or optionally substituted amino or any one of the groups as defined in the description,R.sub.3 represents hydrogen or cycloalkyl, formyl, optionally substituted phenyl, pyridyl or optionally substituted alkyl,the isomers thereof, the addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal compounds containing them are useful for the treatment of chronic or cellular ischemia.Type: GrantFiled: December 15, 1997Date of Patent: December 15, 1998Assignee: ADIR et CompagnieInventors: Michel Wierzbicki, Marie-Fran.cedilla.oise Boussard, Serge Labidalle, Daniel Guyot, Yves Rolland, Jean-Paul Tillement, Bernard Testa, Aime Crevat
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Patent number: 5834447Abstract: A method of controlling Take-all disease of plants by applying, preferably to the seed prior to planting, a fungicide of the formula ##STR1## wherein Z.sub.1 and Z.sub.2 are C or N and are part of an aromatic ring selected from benzene, pyridine, thiophene, furan, pyrrole, pyrazole, thiazole, and isothiazole;A is selected from --C(X)--amine, --C(O)--SR.sub.3, --NH--C(X)R.sub.4, and --C(.dbd.NR.sub.3)--XR.sub.7 ;B is --W.sub.m --Q(R.sub.2).sub.3 or selected from o-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ;Q is C, Si, Ge, or Sn;W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W is selected from --C(R.sub.3).sub.p H.sub.(2-p) --, --N(R.sub.3).sub.m H.sub.(1-m) --, --S(O).sub.Type: GrantFiled: December 8, 1995Date of Patent: November 10, 1998Assignee: Monsanto CompanyInventors: Dennis Paul Phillion, Diane Susan Braccolino, Matthew James Graneto, Wendell Gary Phillips, Karey Alan Van Sant, Daniel Mark Walker, Sai Chi Wong
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Patent number: 5834506Abstract: This invention pertains to improved antiviral activity of 6,6-disubstituted-5,6-dihydropyran-2-ones caused by judicious placement of certain polar substituents at the 3 and/or 6 positions.The same substituents which enhance the cellular activity also diminish cytotoxicity further enhancing the desirable properties of these agents as antivirals.Type: GrantFiled: June 27, 1997Date of Patent: November 10, 1998Assignee: Warner-Lambert CompanyInventors: Frederick Earl Boyer, Jr., John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Susan Elizabeth Hagen, Harriet Wall Hamilton, Elizabeth Ann Lunney, Larry James Markoski, Josyula Venkata Nagendra Vara Prasad, Bradley Dean Tait
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Patent number: 5808062Abstract: The present invention relates to novel tri- and tetrasubstituted pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The pyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized pyrones and of related structures.Type: GrantFiled: October 12, 1994Date of Patent: September 15, 1998Assignee: Warner-Lambert CompanyInventors: John Michael Domagala, Edmund Lee Ellsworth, Elizabeth Lunney, Daniel Fred Ortwine, Kimberly Suzanne Para, Josyula Venkata Nagendra Vara Prasad, Tomi Sawyer, Bradley Dean Tait
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Patent number: 5807853Abstract: A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: ##STR1## to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Novel compounds of formulas 5.0, 5.1 and 5.2, wherein R is --C(R.sup.20)(R.sup.21)(R.sup.46), and 5.3, 5.3A and 5.3B, wherein R is --N(R.sup.25)(R.sup.48), are disclosed. Also disclosed are processes for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3. Further disclosed are novel compounds which are intermediates in the process for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3.Type: GrantFiled: May 25, 1995Date of Patent: September 15, 1998Assignee: Schering CorporationInventors: W. Robert Bishop, Ronald J. Doll, Alan K. Mallams, F. George Njoroge, Joanne M. Petrin, John J. Piwinski, Ronald L. Wolin, Arthur G. Taveras, Stacy W. Remiszewski
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Patent number: 5789440Abstract: The present invention relates to novel 5,6-dihydropyrone derivatives and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The 5,6-dihydropyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized 5,6-dihydropyrones and of related structures.Type: GrantFiled: October 12, 1994Date of Patent: August 4, 1998Assignee: Warner-Lambert CompanyInventors: Edmund Lee Ellsworth, Elizabeth Lunney, Bradley Dean Tait
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Patent number: 5789405Abstract: An oxaspiro ?2,5!octane derivative of the formula: ##STR1## useful in inhibiting angiogenesis in solid tumors.Type: GrantFiled: June 5, 1991Date of Patent: August 4, 1998Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Chiyoshi Kasahara, Takehiko Ohkawa, Masashi Hashimoto
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Patent number: 5756504Abstract: Compounds of the formula X--Y--R, or the pharmaceutically acceptable salts and esters thereof, wherein X is ##STR1## Y is --SO.sub.2 --, --(CH.sub.2).sub.p -- or --CO--(CH.sub.2).sub.p --; R is unsubstituted or substituted phenyl where said substitutents are one or more of R.sup.5, R.sup.6 or R.sup.7 ; R.sup.1 is hydrogen, cyano, phenyl, --CONHR.sup.2, --CONR.sup.2 R.sup.2, --(CH.sub.2).sub.m --OR.sup.2, --(CH.sub.2).sub.p --S(O).sub.r --R.sup.2, --(CH.sub.2).sub.m --CO.sub.2 R.sup.2, --(CH.sub.2).sub.m --N.sub.3, --(CH.sub.2).sub.m --NH.sub.2 or --(CH.sub.2).sub.m --NR.sup.2 R.sup.2 ; R.sup.2 is hydrogen, C.sub.3-8 cycloalkyl or C.sub.1-5 alkyl; R.sup.5 and R.sup.6 are each independently selected from hydrogen, C.sub.1-5 alkoxy, halogen or --(CH.sub.2).sub.n --N(R.sup.2)--C(O)--R.sup.18 ; R.sup.7 is hydrogen or ##STR2## R.sup.11 is selected from hydrogen, C.sub.1-5 alkyl-carbonyl, --Z--R.sup.13, ##STR3## or substituted C.sub.Type: GrantFiled: September 23, 1996Date of Patent: May 26, 1998Assignee: Merck & Co., Inc.Inventors: Mark G. Bock, Ben E. Evans, J. Christopher Culberson, Kevin F. Gilbert, Kenneth E. Rittle, Peter D. Williams
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Patent number: 5750696Abstract: Dioxacycloalkane compounds of the formula ?1! ##STR1## wherein A is ##STR2## wherein W is ##STR3## X is --CO-- or --SO.sub.2 --; Y is --CH.sub.2 --, --O-- or --NR.sup.25 --; and R.sup.1 is an aralkyl which may be substituted by lower alkoxy;R.sup.2 is a hydrogen atom or a lower alkyl;R.sup.3 is --(CH.sub.2)d-SR.sup.26 or ##STR4## R.sup.4 and R.sup.5 are each a hydrogen atom or a lower alkyl; and E is --C(R.sup.29)(R.sup.30)-- or --CH.sub.2 CH.sub.2 --, pharmaceutically acceptable salts thereof, intermediates for producing said compounds, and methods for producing said intermediates. The compounds of the formula ?1! have a strong inhibitory activity against renin and show continuous hypotensive action by oral administration. They are useful as hypotensive agents or therapeutic agents for heart failure.Type: GrantFiled: February 21, 1995Date of Patent: May 12, 1998Assignee: Japan Tobacco Inc.Inventors: Saizo Shibata, Yasuki Yamada, Koji Ando, Kiyoshi Fukui, Ikuro Nakamura, Itsuo Uchida
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Patent number: 5693803Abstract: Intermediates of structural formula ##STR1## can be made by reacting a primary or secondary amine with glycosidol or an activated derivative thereof. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.Type: GrantFiled: June 7, 1995Date of Patent: December 2, 1997Assignee: Merck & Co., Inc.Inventors: David Askin, Kai Rossen, Paul Reider, Richard J. Varsolona, Ralph P. Volante, Kenneth M. Wells
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Patent number: 5686609Abstract: The invention relates to compounds of the formula ##STR1## in which: m is 2 or 3;Ar and Ar' independently are a thienyl group; a substituted or unsubstituted phenyl group; or an imidazolyl group; it also being possible for Ar' to be a benzothienyl group which is unsubstituted or substituted by a halogen; a naphthyl group which is unsubstituted or substituted by a halogen; a biphenyl group; or a substituted or unsubstituted indolyl;X is hydrogen;X' is hydrogen or a hydroxyl group or is joined to X" below to form a carbon-carbon bond, or X and X' together form an oxo group or a dialkylaminoalkoxyimino group of the formula .dbd.N--O--(CH.sub.2).sub.p --Am, in which p is 2 or 3 and Am is a dialkylamino group;Y is a nitrogen atom or a group C(X"), in which X" is hydrogen or forms a carbon-carbon bond with X';Q is hydrogen, a C.sub.1 -C.sub.4 alkyl group or an aminoalkyl group of the formula --(CH.sub.2).sub.Type: GrantFiled: March 11, 1994Date of Patent: November 11, 1997Assignee: SanofiInventors: Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5686454Abstract: The invention is directed to a series of novel compounds of the formula ##STR1## where Y is carbonyl or sulfonyl; R.sup.7 and R.sup.8 are alkyl, or R.sup.7 and R.sup.8, together with the carbon to which they are attached, form a C.sub.3-6 carbocyclic ring; R.sup.9 and R.sup.10 are each independently selected from hydrogen, hydroxyl, oximido, methyl, carboxyl, carboxyalkyl, unsubstituted or substituted alkoxycarbonyl, alkylcarbonyloxyalkyl, cyanoalkyl, hydroxyalkyl or unsubstituted amino; R.sup.11 is hydrogen, oxo, --N(R.sup.12)--CO--R.sup.13 or --CO--N(R.sup.14)--R.sup.15 ; R.sup.12 is hydrogen or unsubstituted or substituted alkyl; R.sup.13 is alkoxyl, unsubstituted or substituted heterocyclic rings selected from ##STR2## or unsubstituted or substituted alkyl; and R.sup.14 and R.sup.15 are each independently selected from hydrogen or unsubstituted or substituted alkyl. The Y moiety cannot be bonded to the camphor ring at the 3 or 6 positions.Type: GrantFiled: January 16, 1996Date of Patent: November 11, 1997Assignee: Merck & Co., Inc.Inventors: Mark G. Bock, Doug W. Hobbs
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Patent number: 5650412Abstract: Compounds of formula ##STR1## are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: October 26, 1995Date of Patent: July 22, 1997Assignee: Merck & Co., Inc.Inventors: Byeong Moon Kim, Joseph P. Vacca
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Patent number: 5648352Abstract: The invention is directed to a series of novel piperazinylcamphorsulfonyl compounds where the camphor ring is substituted by amides, amines, alkanes, alkenes, alkylamines, halogens, hydroxy, carboxy, alkoxycarbonyl and heterocyclic tings. Such compounds are oxytocin antagonists useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery.Type: GrantFiled: May 26, 1995Date of Patent: July 15, 1997Assignee: Merck & Co., Inc.Inventors: Mark G. Bock, Jill M. Erb, Doug W. Hobbs, James B. Hoffman, Joseph M. Pawluczyk, Debra S. Perlow, Daniel F. Veber, Peter D. Williams
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Patent number: 5637711Abstract: Intermediates of structural formula ##STR1## can be made by reacting a primary or secondary amine with glycosidol or an activated derivative thereof. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.Type: GrantFiled: June 7, 1995Date of Patent: June 10, 1997Assignee: Merck & Co., Inc.Inventors: David Askin, Paul Reider, Kai Rossen, Richard J. Varsolona, Ralph P. Volante, Kenneth M. Wells