Spiro Patents (Class 544/70)
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Patent number: 7332491Abstract: Disclosed are new dihydropteridinones of general formula (I) whereby the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.Type: GrantFiled: August 24, 2005Date of Patent: February 19, 2008Assignee: Boehringer Ingelheim International, GmbHInventors: Matthias Grauert, Matthias Hoffmann, Martin Steegmaier, Christian Eickmeier, Gisela Schnapp, Norbert Redemann, Flavio Solca, Jens Juergen Quant
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Patent number: 7309787Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: July 6, 2006Date of Patent: December 18, 2007Assignee: Allergan, Inc.Inventor: Julie A. Wurster
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Publication number: 20070281917Abstract: The invention encompasses series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: ApplicationFiled: May 29, 2007Publication date: December 6, 2007Inventors: B. Narasimhulu Naidu, Margaret E. Sorenson
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Patent number: 7304081Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: GrantFiled: May 4, 2005Date of Patent: December 4, 2007Assignee: Incyte CorporationInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang
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Patent number: 7273859Abstract: The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates useful for making the pyrimidone compounds.Type: GrantFiled: April 20, 2005Date of Patent: September 25, 2007Assignee: Bristol-Myers Squibb CompanyInventor: B. Narasimhulu Naidu
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Publication number: 20070213526Abstract: Processes are provided for purifying a compound of the structure: wherein, A, B, T, Q and R1 are defined herein, and wherein the process includes dissolving the compound of formula I in a solution containing acetone, water and a base at about 30° C.; filtering the solution containing the compound of formula I at about 30° C.; and precipitating the purified compound of formula I by adjusting the filtered solution to an acidic pH. Desirably, the compound of formula I is 5-(2-thioxospiro[cyclohexane-1,3-[3H]indol]-5-yl)-1-methylpyrrole-2-carbonitrile or tanaproget.Type: ApplicationFiled: March 5, 2007Publication date: September 13, 2007Applicant: WyethInventors: Mahmut Levent, Panolil Raveendranath, Bogdan Wilk, Donald Carl Boop, Marinus Cornelis Hofman
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Patent number: 7214676Abstract: The invention provides compounds which are PDE7 inhibitors, having the following formula (I), (II) and (III) in which X1, X2, X3, X4, X, Y, Z, A and Z1 are as defined in the description, methods for preparing them and their use for the treatment of disorders for which therapy by a PDE7 inhibitor is relevant.Type: GrantFiled: May 24, 2004Date of Patent: May 8, 2007Assignee: Warner-Lambert Company LLCInventors: Patrick Bernardelli, Pierre Ducrot, Edwige Lorthiois, Febrice Vergne
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Patent number: 7144890Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts thereof, for use as therapeutically active substances. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors including obesity.Type: GrantFiled: January 25, 2005Date of Patent: December 5, 2006Assignee: Hoffman-La Roche Inc.Inventors: Jean-Marc Plancher, Sven Taylor
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Patent number: 7122662Abstract: This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which exhibits strong anticoagulation action. The invention also relates to a pharmacophore which was derived from the compound and is useful in molecular designing of the FXa inhibitor.Type: GrantFiled: December 16, 2004Date of Patent: October 17, 2006Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Hidemitsu Nishida, Fumihiko Saitoh, Kousuke Harada, Ikuya Shiromizu, Takafumi Mukaihira
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Patent number: 7081457Abstract: Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: wherein R1 and R2 are selected from the group of H, optionally substituted C1 to C6 alkyl, alkenyl, alkynyl, or alkynyl groups C3 to C8 cycloalkyl, aryl, substituted aryl, or heterocyclic groups, or CORA or NRBCORA; or R1 and R2 are fused to form an optionally substituted ring structure as defined herein; RA and RB are as defined herein; R3 is H, OH, NH2, CORC, or optionally substituted C1 to C6 alkyl, C3 to C6 alkenyl, or alkynyl groups; RC is as defined herein; Q1 is S, NR7, or CR8R9; R5 is an optionally trisubstituted benzene ring or an optionally substituted five or six membered heterocyclic ring.Type: GrantFiled: May 6, 2002Date of Patent: July 25, 2006Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Puwen Zhang, Andrew Fensome, Eugene A. Terefenko, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley, Jay E. Wrobel, Mark A. Collins
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Patent number: 6916807Abstract: The present invention relates to triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said ring X is a 5-7 membered heterocyclic ring, and wherein A, Y, B, G, and W are as defined in the specification; and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.Type: GrantFiled: April 25, 2003Date of Patent: July 12, 2005Assignee: Pfizer Inc.Inventors: Kevin D. Freeman-Cook, Mark C. Noe
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Patent number: 6900201Abstract: The present invention relates to N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein ring X is a 5-7 membered heterocyclic ring, and wherein A, Y, B, and G are as defined in the specification; and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.Type: GrantFiled: April 25, 2003Date of Patent: May 31, 2005Assignee: Pfizer Inc.Inventors: Mark C. Noe, Kevin Freeman-Cook
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Patent number: 6872719Abstract: Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a —CH3, —(CH2)3CH3, —CH2CH2OH, —CH2CH2OCH3, —CH2CH2OCH2CH2OH, —CH2CH2OCH2CH2OCH3, group; and the salts, solvates and N-oxides thereof. Compounds according to the invention are potent and selective inhibitors of ?4 integrins. The compounds are of use in modulating cell adhesion and in particular are of use in the prophylaxis and treatment of diseases or disorders including inflammation in which the extravasation of leukocytes plays a role and the invention extends to such a use and to the use of the compounds for the manufacture of a medicament for treating such diseases or disorders.Type: GrantFiled: July 16, 2003Date of Patent: March 29, 2005Assignee: Celltech R & D LimitedInventors: Julien Alistair Brown, Stuart Bailey, Stephen Brand
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Publication number: 20040267013Abstract: Specific photochromic 3H-naphtho[2,1-b]-pyran compounds useful with various types of synthetic resin materials to form photochromic articles, especially ophthalmic lenses, and photochromic articles formed with such compounds. The compounds of the invention have especially long-wave absorption maxima in the open form thereof and enable violet to blue tints to be obtained when used in photochromic articles.Type: ApplicationFiled: July 2, 2004Publication date: December 30, 2004Applicant: Rodenstock GmbHInventors: Claudia Mann, Manfred Melzig, Udo Weigand
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Publication number: 20040225124Abstract: The invention relates to a process for the preparation of a compound of the formula (I) by reacting a compound of the formula (II) with a compound of the formula (III) characterised by dissolving the compounds of the formula (II) and formula (III) in a water-inmiscible organic solvent in the presence of a phase transfer catalyst, reacting with a.) an aqeuos solution of a base, or b.) a base in solid form directly and if desired transforming the compound of formula (I) thus obtained into its salt.Type: ApplicationFiled: June 7, 2004Publication date: November 11, 2004Inventors: Eva Csikos, Csaba Gonczi, Felix Hajdu, Istvan Hermecz, Gergely Heja, Gergelyne Heja, Csilla Majlath, Lajos Nagy, Andrea Csutor Santane, Toborne Szomor, Gyorgyne Szvoboda
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Patent number: 6756371Abstract: The compounds of formula (I) in which R1, R2, A, B and Ar have the meanings as given in the description are novel effective PDe4 inhibitorsType: GrantFiled: April 12, 2002Date of Patent: June 29, 2004Assignee: Altana Pharma AGInventor: Geert Jan Sterk
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Patent number: 6727247Abstract: A compound of formula I and a method of treatment of diseases, related to modulation of the adenosine A2 receptor system comprising administering a compound of formula to a person in need of such treatment.Type: GrantFiled: December 3, 2002Date of Patent: April 27, 2004Assignee: Hoffman-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Patent number: 6720420Abstract: The present invention provides oxazine compounds having aromatic, heteroaromatic, or aliphatic substituents at the 2 position of the oxazine moiety.Type: GrantFiled: December 21, 2001Date of Patent: April 13, 2004Assignee: Johnson & Johnson Vision Care, Inc.Inventors: Weili Zhao, Erick M. Carreira
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Patent number: 6706878Abstract: A compound of formula wherein n, m, p, X, Y, W, A, G and D are as defined in the specification, enantiomers thereof, pharmaceutically acceptable salts thereof, processes for preparing them, composition containing them, and their use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders.Type: GrantFiled: March 24, 2003Date of Patent: March 16, 2004Assignee: Astrazeneca ABInventors: Eifion Phillips, Robert Mack, John Macor, Simon Semus
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Patent number: 6703502Abstract: A compound of formula wherein n is 0 or 1; m is 0 or 1; p is 0 or 1; X is oxygen or sulfur; Y is CH, N or NO; W is oxygen, H2 or F2; A is N or C(R2); G is N or C(R3); D is N or C(R4); with the proviso that no more than one of A, G, and D is nitrogen, but at least one of Y, A, G, and D is nitrogen or NO; R1 is hydrogen or C1 to C4 alkyl; R2, R3, and R4 are independently hydrogen, halogen, C1, C4 alkyl, C2, C4 alkenyl, C2-C4 alkynyl, aryl, heteroaryl, OH, OC1, C4 alkyl, CO2R1, —CN, —NO2, —NR5R6, —CF3, —OSO2CF3 or R2 and R3, or R3 and R4, respectively, may together form another six membered aromatic or heteroaromatic ring sharing A and G, or G and D, respectively, containing between zero and two nitrogen atoms, and substituted with one to two of the following substituents: independently hydrogen, halogen, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, aryl, heteroaryl, OH, OC1-C4 alkyl, CO2R1, —CN, —NO2, —NR5R6, —CF3, —OSO2CF3; R5 andType: GrantFiled: March 8, 2002Date of Patent: March 9, 2004Assignee: AstraZeneca ABInventors: Eifion Phillips, Robert Mack, John Macor, Simon Semus
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Patent number: 6686466Abstract: The present invention provides photochromic oxazine compounds and methods for their manufacture, which compounds are useful as photochromic compounds. The compounds of the invention have aromatic substituents on the 2 position of the oxazine moiety.Type: GrantFiled: November 13, 2001Date of Patent: February 3, 2004Assignee: Johnson & Johnson Vision Care, Inc.Inventors: Weili Zhao, Erick M. Carreira
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Patent number: 6683709Abstract: Photochromic pyran compounds and their use in synthetic resin objects of all types, especially for ophthalmic applications, particularly spiro compounds having a fluorene structure derived from naphthopyrans, which are known as spirofluorenopyrans. By introducing respectively only one strongly electron donating or withdrawing group at specific positions in the periphery of the pyran dye, photochromic compounds obtained which in the excited state are distinguished by an expanded color spectrum, while simulataneously offering comparably good bleaching rates and good durability.Type: GrantFiled: February 7, 2002Date of Patent: January 27, 2004Assignee: Rodenstock GmbHInventors: Claudia Mann, Udo Weigand, Manfred Melzig
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Publication number: 20040009976Abstract: This invention relates to certain novel imidazoline compounds and analogues thereof, to their use for the treatment of diabetes, diabetic complications, metabolic disorders, or related diseases where impaired glucose disposal is present, to pharmaceutical compositions comprising them, and to processes for their preparation.Type: ApplicationFiled: April 30, 2002Publication date: January 15, 2004Inventors: Kumiko Takeuchi, Michael Robert Jirousek, Michael Paal, Gerd Ruhter, Theo Schotten
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Publication number: 20030194698Abstract: The present invention generally relates to an assay for identifying inhibitors of Human Papillomavirus (HPV), comprising:Type: ApplicationFiled: February 5, 2003Publication date: October 16, 2003Applicant: Boehringer Ingelheim (Canada) Ltd.Inventors: Peter White, Christiane Yoakim
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Patent number: 6627634Abstract: Bicyclic heterocycles of general formula wherein: Ra to Rd, A to C and X are as defined herein, the tautomers, the stereoisomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, diseases of the lungs and respiratory tract, and the preparation thereof.Type: GrantFiled: March 23, 2001Date of Patent: September 30, 2003Assignee: Boehringer Ingelheim Pharma KGInventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
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Publication number: 20030171373Abstract: This invention relates to certain spirocyclic compounds substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.Type: ApplicationFiled: January 29, 2003Publication date: September 11, 2003Inventors: Matthew J. Fisher, Joseph A. Jakubowski, John J. Masters, Jeffrey T. Mullaney, Michael Paal, Gerd Ruhter, Kenneth J. Ruterbories, Robert M. Scarborough, Theo Schotten, Wolfgang Stenzel
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Patent number: 6600039Abstract: The invention relates to a process for the preparation of a compound of formula (I) and the salts thereof by reacting the compound of formula (II) with the compound of formula (III), which comprises carrying out the reaction in dimethyl sulfoxide, at a temperature between 10° C. and 40° C., preferably at room temperature and transforming the resulting base of formula (I), if desired, into its salt by a method known per se.Type: GrantFiled: April 17, 2002Date of Patent: July 29, 2003Assignee: Sanofi-SynthelaboInventors: Gergely Héja, Éva Csikós, Tünde Erösné Takácsy, Csaba Gönczi, Judit Halász, István Hermecz, Csilla Majláth, Lajos Nagy, Andrea Sántáné Csutor, Péter Sárosi, Kálmán Simon, Tiborné Szomor, Györgyné Szvoboda
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Publication number: 20030099910Abstract: The present invention relates to a photochromic spirobenzopyran compound of the formula (1) and its derivatives, a spirobenzopyran group having unsaturated terminal groups, a polymer prepared therefrom, a method for the production thereof, a composition comprising said spirobenzopyran or said spirobenzopyran group-containing polymer and a photochromic switch film using the same: 1Type: ApplicationFiled: August 24, 1999Publication date: May 29, 2003Inventors: EUN-KYOUNG KIM, YUN-KI CHOI, SAM-ROK KEUM
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Patent number: 6548679Abstract: The present invention provides compounds of general formula I or II: wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I or II, intermediates and processes useful for preparing compounds of formula I or II, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I or II.Type: GrantFiled: August 17, 2000Date of Patent: April 15, 2003Assignee: The Regents of the University of CaliforniaInventors: Trevor C. McMorris, Michael J. Kelner
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Publication number: 20030064978Abstract: There are provided novel compounds of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the Specification and optical isomers, racemates and tautomers thereof and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme nitric oxide synthase.Type: ApplicationFiled: August 9, 2002Publication date: April 3, 2003Inventors: Christopher Walpole, Hua Yang
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Publication number: 20030064985Abstract: A compound of formula (I) or its enantiomers or diastereoisomers thereof: 1Type: ApplicationFiled: December 17, 2001Publication date: April 3, 2003Inventors: Christiane Yoakim, Bruno Hache, William W. Ogilvie, Jeffrey O'Meara, Peter White, Nathalie Goudreau
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Patent number: 6511975Abstract: A compound of the formula (I) wherein R1 and R2 is a substituted or unsubstituted aryl group, or a substituted or unsubstituted heteroaryl group. A is CH2, CO or SO2. B is a single bond, alkylene or alkenylene. D is O or S. E is alkylene or alkenylene. wherein G is a substituted or unsubstituted cycloalkene ring, or a substituted cycloalkane ring. Ar is a substituted or unsubstituted aryl ring, or a substituted or unsubstituted heteroaryl ring. R3 is alkyl. n is 1-3. The invention includes a pharmacologically acceptable salt, ester or other derivative of a compound of the formula (I). The invention also provides pharmaceutical compositions and methods of treating specified diseases utilizing a compound of formula (I).Type: GrantFiled: July 13, 2000Date of Patent: January 28, 2003Assignee: Sankyo Company, LimitedInventors: Takahide Nishi, Takeshi Yamaguchi, Yukiko Iio, Toshiyasu Takemoto, Katsuyoshi Nakajima
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Patent number: 6509334Abstract: This invention provides compounds of Formula (I): wherein R1 and R2 may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alkynyl, CORC; RC is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl, alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R5 is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR6 and containing one or two independent substituents from the group including H, halogen, CN, N02, amino, and C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 aType: GrantFiled: April 19, 2000Date of Patent: January 21, 2003Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.Inventors: Puwen Zhang, Eugene A. Terefenko, Andrew Fensome, Jay E. Wrobel, Horace Fletcher, III, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Publication number: 20020169315Abstract: Photochromic pyran compounds and their use in synthetic resin objects of all types, especially for ophthalmic applications, particularly spiro compounds having a fluorene structure derived from naphthopyrans, which are known as spirofluorenopyrans. By introducing respectively only one strongly electron donating or withdrawing group at specific positions in the periphery of the pyran dye, photochromic compounds obtained which in the excited state are distinguished by an expanded color spectrum, while simulataneously offering comparably good bleaching rates and good durability.Type: ApplicationFiled: February 7, 2002Publication date: November 14, 2002Inventors: Claudia Mann, Udo Weigand, Manfred Melzig
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Patent number: 6479489Abstract: Pesticidal and herbicidal substituted spirocyclic 1-H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) is which A and B together with the carbon atom to which they are bonded represent an unsubstituted or substituted 5-6-membered cycle which is interrupted by at least one hetero atom, n represents a number 0, 1, 2, or 3, G represents hydrogen (a) or the groups E represents a metal ion equivalent or an ammonium ion, and the other radicals have various definitions.Type: GrantFiled: June 3, 1999Date of Patent: November 12, 2002Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Krüger, Hans-Joachim Santel, Markus Dollinger, Christoph Erdelen, Ulrike Wachendorff-Neumann
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Patent number: 6472398Abstract: Certain novel spiropiperidine derivatives of structural formula Ia wherein the substituents are as defined herein are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: March 20, 2001Date of Patent: October 29, 2002Assignee: Merck & Co., Inc.Inventors: Brenda L. Palucki, Ravi P. Nargund
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Patent number: 6469076Abstract: A photochromic compound which by itself develops a color tone of a neutral tint, exhibits a large fading rate and offers a good photochromic light resistance.Type: GrantFiled: April 30, 2001Date of Patent: October 22, 2002Assignee: Tokuyama CorporationInventors: Junji Momoda, Yasuko Komuro
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Patent number: 6451843Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols, their preparation and the use of such ketoenols as pesticides and/or herbicides. The novel arylphenyl-substituted cyclic ketoenols are of the formula (I) in which CKE refers to the cyclic ketoenol and W, X, Y and Z are as defined in the specification.Type: GrantFiled: January 2, 2001Date of Patent: September 17, 2002Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Reiner Fischer, Alan Graff, Udo Schneider, Thomas Bretschneider, Christoph Erdelen, Wolfram Andersch, Mark Wilhelm Drewes, Markus Dollinger, Ingo Wetcholowsky, Dieter Feucht, Rolf Pontzen, Randy Allen Myers
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Patent number: 6444819Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH; R1, R2 and R3 independently represent organic or inorganic substituents; R4 and R4′ independently represent hydrogen, alkyl or form a ring with the atom to which they are attached; R5 represents hydrogen, alkyl, alkoxy, or alkylthio, and R6 represents hydrogen or alkyl; or R5 and R6 form a ring together with the atoms to which they are attached; and R7, R8, R9, R10, and R11 independently represent hydrogen or alkyl, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.Type: GrantFiled: October 11, 2001Date of Patent: September 3, 2002Assignee: Neurogen CorporationInventors: Renata Xavier Kover, Salva Terdjanian, Jennifer Tran, Andrew Thurkauf
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Patent number: 6436929Abstract: The present invention provides compounds which are agonists of the progesterone receptor and have the structures: wherein R1 and R2 are independent substituents selected from the group of H, optionally substituted C1 to C6 alkyl, alkenyl, alkynyl, or alkynyl groups C3 to C8 cycloalkyl, aryl, substituted aryl, or heterocyclic groups, or CORA or NRBCORA; or R1 and R2 are fused to form an optionally substituted 3 to 8 membered Spiro cyclic alkyl or alkenyl ring or a Spiro cyclic ring containing one to three heteroatoms selected from O, S and N; RA is selected from H, amino, or optionally substituted C1 to C3 alkyl, aryl, C1 to C3 alkoxy, or C1 to C3 aminoalkyl groups; RB is H, C1 to C3 alkyl, or substituted C1 to C3 alkyl; R3 is H, OH, NH2, CORC, or optionally substituted C1 to C6 alkyl, C3 to C6 alkenyl, or alkynyl groups; RC is selected from H or optionally substituted C1 to C3 alkyl, aryl, C1 to C3 alkoxy, or C1 to C3 aminoalkyl groups; Q1 is S, NR7, or CR8R9; R5 is an optionally trisubstituType: GrantFiled: April 19, 2000Date of Patent: August 20, 2002Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Puwen Zhang, Andrew Fensome, Eugene A. Terefenko, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley, Jay E. Wrobel, Mark A. Collins
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Publication number: 20020094983Abstract: This invention provides compounds which are agonists and antagonists of the progesterone receptor having the general structure: 1Type: ApplicationFiled: December 17, 2001Publication date: July 18, 2002Inventors: Puwen Zhang, Andrew Fensome, Eugene A. Terefenko, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Patent number: 6416922Abstract: The present invention related to an azomethine dye precursor represented by the following general formula (1) and the image-forming material and image-forming method using the azomethine dye precursor: wherein Ar represents an aryl group or a heterocyclic group which may each have a substituent; X represents a bivalent group linking a carbon atom and a nitrogen atom; and Cp represent a coupler residue which may or may not form a ring.Type: GrantFiled: January 29, 2001Date of Patent: July 9, 2002Assignee: Fuji Photo Film Co., Ltd.Inventors: Hiroshi Sato, Masatoshi Yumoto, Yoshimitsu Arai, Hirotaka Matsumoto
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Patent number: 6369056Abstract: This invention provides compounds of the formula: wherein: A, B and D are N or CH, with the proviso that A, B and D can not all be CH; R1 and R2 are independent substituents selected from H, CORA, NRBCORA, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or groups; or R1 and R2 are fused to form an optionally substituted 3 to 8 membered spirocyclic or heterocyclic ring; RA is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; RB is H, C1 to C3 alkyl, or substituted C1 to C3 alkyl; R3 is H, OH, NH2, or optionally substituted alkyl, or alkenyl, or CORC; RC is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; R4 is a substituted benzene ring or a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR5; RF is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; RG is H, alkyl, or substituted alkyl; R5 is H or alkyl; Q is O, S, NR6, or CR7R8; R6 is CN, SO2CF3, or optionally substituted alkyl, cycType: GrantFiled: April 19, 2000Date of Patent: April 9, 2002Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.Inventors: Puwen Zhang, Arthur A. Santilli, Andrew Fensome, Eugene A. Terefenko, Andrew Q. Viet, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Patent number: 6369057Abstract: Compounds of the formula I or Ia in which n and the substituents R1, R5 and x have the meaning mentioned have an antiviral activity.Type: GrantFiled: April 7, 1995Date of Patent: April 9, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Uta-Maria Billhardt, Manfred Rösner, Günther Riess, Irvin Winkler, Rudolf Bender
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Patent number: 6331625Abstract: Photochromic spirofluorenopyran compounds corresponding to the general formula (I): in which B, B′, R1 to R4 and G have the meanings defined herein. The compounds of the invention are useful in the production of photochromic articles, particularly articles made of synthetic resin materials, and exhibit rapid darkening and brightening rates, as well as long useful service lives. By appropriate selection of substituents, it is possible to adjust the properties of the compounds such as absorption maxima (color), brightening rate, etc.Type: GrantFiled: April 25, 2000Date of Patent: December 18, 2001Assignee: Optische Werke G. RodenstockInventors: Claudia Mann, Udo Weigand, Manfred Melzig
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Patent number: 6288059Abstract: A compound of formula (I), a pharmaceutically acceptable salt or ester or other derivative thereof: R1 is optionally substituted cycloalkyl or optionally substituted saturated heterocyclic group. R2 is optionally substituted aryl or optionally substituted heteroaryl. A is methylene, carbonyl or sulfonyl. B is a single bond, alkylene or alkenylene. D is oxygen or sulfur. G is alkylene or alkenylene. L is —N(R3)— or —C(R4)(R5)—. R3 is optionally substituted aryl or optionally substituted heteroaryl. R4 is H, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl or optionally substituted saturated heterocyclic group. R5 is alkyl optionally substituted with amino, amino, optionally substituted acylamino, OH, optionally substituted hydroxyalkyl, alkoxy or —CO—R6. R6 is alkyl, alkoxy or amine residue. R4 together with R5 forms a cycloalkane ring, cycloalkene ring, or saturated heterocyclic ring. R7 is alkyl.Type: GrantFiled: June 5, 2000Date of Patent: September 11, 2001Assignee: Sankyo Company, LimitedInventors: Takahide Nishi, Takeshi Yamaguchi
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Patent number: 6225466Abstract: Photochromic spirofluorenopyran compounds corresponding to the general formula (I): in which B, B′, R1 to R4 and G have the meanings defined herein. The compounds of the invention are useful in the production of photochromic articles, particularly articles made of synthetic resin materials, and exhibit rapid darkening and brightening rates, as well as long useful service lives. By appropriate selection of substituents, it is possible to adjust the properties of the compounds such as absorption maxima (color), brightening rate, etc.Type: GrantFiled: May 28, 1999Date of Patent: May 1, 2001Assignee: Optische Werke G. RodenstockInventors: Claudia Mann, Udo Weigand, Manfred Melzig
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Patent number: 6180623Abstract: Compounds having kappa opioid agonist activity, compositions containing them and methods of using them as analgesics and anti-pruritic agents are provided. The compounds of formula IV have the structure: wherein X9; R1, R2, R3, R4; and n are as described in the specification.Type: GrantFiled: November 8, 1999Date of Patent: January 30, 2001Assignee: Adolor CorporationInventors: Lawrence I. Kruse, An-Chih Chang, Diane L. DeHaven-Hudkins, John J. Farrar, Forrest Gaul, Virendra Kumar, Michael Anthony Marella, Alan L. Maycock, Wei Yuan Zhang
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Patent number: 6159967Abstract: Compounds of the formula and quaternary ammonium ions thereof, wherein R.sup.1 and R.sup.2 are the same or different and are carbocyclic aryl or aromatic heterocyclic; A is methylene, carbonyl or sulfonyl; B is a single bond, C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4, alkenylene; D is oxygen; E is C.sub.2 alkylene; G is C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4 alkenylene; and L is --C(R.sup.4)(R.sup.5), wherein R.sup.4 and R.sup.5 together with the carbon atom to which they are attached represent a C.sub.5 -C.sub.10 cycloalkyl or a C.sub.5 -C.sub.10 heterocyclic. Especially preferred are compounds wherein L represents ##STR1## wherein J is a C.sub.1 -C.sub.6 alkylene; Ar is a ring carbocyclic or aromatic heterocyclic and S*.fwdarw.O is a sulfoxide in which the sulfur atom is in the 5-configuration. The compounds have tachykinin receptor antagonist activity and exhibit an activity against both the NK.sub.1 and NK.sub.2 receptors.Type: GrantFiled: December 2, 1996Date of Patent: December 12, 2000Assignee: Sankyo Company, LimitedInventors: Takahide Nishi, Koki Ishibashi, Katsuyoshi Nakajima, Tetsuya Fukazawa, Hitoshi Kurata, Takeshi Yamaguchi, Kazuhiro Ito
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Patent number: 6153126Abstract: Described are novel photochromic six-membered heterocyclic-fused naphthopyran compounds, examples of which are naphthopyran compounds having an oxazino group fused to one side of the naphtho portion of the naphthopyran and having certain substituents at the position ortho to the oxygen atom of the naphthopyran ring. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds.Type: GrantFiled: February 7, 2000Date of Patent: November 28, 2000Assignee: PPG Industries Ohio, Inc.Inventor: Anil Kumar