The Five-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/373)
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Patent number: 7087611Abstract: The present invention relates to new and useful processes for the preparation of the anhydrate form of 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one hydrochloride.Type: GrantFiled: August 30, 2004Date of Patent: August 8, 2006Assignee: Apotex Pharmachem Inc.Inventors: Carlos Zetina-Rocha, Allan W. Rey, Stephen E. Horne
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Patent number: 7084143Abstract: The invention relates to compounds of formula (I) wherein R1, R2, R4 and R5 have the meaning given in Claim 1. Said compounds are potent 5-HT2A-antagonists and are suitable for the treatment of psychosis, schizophrenia, depression, neurological disorders, memory disorders. Parkinson's disease, amytrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders, e.g. nervous bulimia and anorexia and premenstrual syndrome and/or for positively influencing compulsive behaviors (obsessive-compulsive disorder, OCD).Type: GrantFiled: December 17, 2004Date of Patent: August 1, 2006Assignee: Merck Patent GmbHInventors: Henning Boettcher, Christoph Seyfried
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Patent number: 7074796Abstract: The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C and no bond when W is N or CH; R1 and R2 are independently selected from hydrogen and halogen, provided at least one of R1 and R2 is a halogen atom; R3 is selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, aryloxy, aralkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, nitro and cyano n is 2, 3, 4 or 5; X is CH2, O, S, CO, CS, SO or SO2; and Q is a group of formula wherein Z is a chain of 3 to 4 chain members; wherein the chain members are selected from C, CH, CH2, CO, N and NH, provided that only one of the chain members may be N or NH, and said chain optionally containing one or two double bonds; hvad med acyl?? R4, R5, R6, R7, R8, R9 and R10 are independently selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6Type: GrantFiled: June 27, 2002Date of Patent: July 11, 2006Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jan Kehler, Jakob Felding
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Patent number: 7067513Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as aggression, anxiety disorders, autism, vertigo, depression, disturbances of cognition, disturbances of memory, Parkinson's disease, schizophrenia, and psychotic disorders. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0–2; R5 and R6 are independently H or alkyl (1–3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3–5, and R7 is alkyl (1–3C), alkoxy (1–3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2–4, and salts thereof.Type: GrantFiled: August 22, 2000Date of Patent: June 27, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Roelof Van Hes, Johannes A. M. Van der Heijden, Cornelis G Kruse, Jacobus Tipker, Martinus T. M Tulp, Gerben M Visser, Bernard J Van Vliet
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Patent number: 7060704Abstract: Compounds with 5HT7 receptor affinity (some of which are novel) useful for lowering IOP, improving blood flow to the optic nerve head and the retina, providing neuroprotection, and treating retinal diseases are disclosed. The Compounds are also useful for treating sleep disorders, depression, and other psychiatric disorders, such as, schizophrenia, anxiety, obsessive compulsive disorder, circadian rhythm disorders, and centrally and peripherally mediated hypertension. Compositions and methods for their use are also disclosed.Type: GrantFiled: April 7, 2005Date of Patent: June 13, 2006Assignee: Alcon Manufacturing, Ltd.Inventors: Jesse A. May, Thomas R. Dean, Najam A. Sharif, Hwang-Hsing Chen
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Patent number: 7041668Abstract: The present invention discloses and claims benzimidazole compounds of formula (I): in which A is aryl or heteroaryl; R1 is selected from optionally substituted alkyl, alkoxy, aryl or heteroaryl, NH-lower alkyl or NH-cycloalkyl, or halogen, NH2; 1-imidazolyl or SO2Me; R2 is selected from optionally substituted —CO-alkyl, —CO-cycloalkyl, —CO-aralkyl, —CO-aryl, —CO-alkoxy, aryl or aralkyl, or —CO-amino, CO—NHR3 or CO—R3R4 wherein R3 and R4 are selecteded independently from hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, fluoroalkyl, alkynyl, heteroalkyl, alkylheteroalkyl, aryl, aralkyl or together form an alkylene chain optionally containing one to 4 heteroatoms; a pharmaceutically acceptable salt or a prodrug thereof; the use of compounds of formula (I) for the treatment of cancer, and pharmaceutical compositions comprising a compound of formula (I) and one or more pharmaceutically acceptable adjuvants or diluents.Type: GrantFiled: March 25, 2004Date of Patent: May 9, 2006Assignee: Aventis Pharma S.A.Inventors: Francois Clerc, Francois Hamy, Isabelle Depaty, Odile Angouillant-Boniface, Stéphanie Deprets, Chantal Carrez, Manfred Roesner
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Patent number: 7034029Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptorType: GrantFiled: January 16, 2004Date of Patent: April 25, 2006Assignee: WyethInventors: Michael Gerard Kelly, Derek Cecil Cole
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Patent number: 7030123Abstract: The invention provides a compound of Formula (I). Wherein R1, R2, R3, R10 and R11 have the meanings given in the description. Such compounds are predicted to cause the selective destruction of tumour vasculature. They may therefore be used to inhibit and/or reverse, and/or alleviate symptoms of angiogenesis and/or any disease state associated with angiogenesis.Type: GrantFiled: May 25, 2001Date of Patent: April 18, 2006Assignee: AstraZeneca ABInventors: Jean-Claude Arnould, Thomas Geoffrey Bird, Francis Thomas Boyle, David Charles Blakey
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Patent number: 7030241Abstract: The invention relates to the mesylates of a group of piperazine derivatives and to a process for the preparation of these mesylates in an economic way in the high yield and of high purity. According to the process of the invention the synthesis of the piperazine ring and the mesylate formation are combined in a single reaction step.Type: GrantFiled: February 14, 2002Date of Patent: April 18, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Marcel P. M. van Aar, Stefanus J. Schouten, Jan Zorgdrager, Michiel C. Heslinga
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Patent number: 7026314Abstract: Provided herein is a compound of the formula (I) wherein said compound is useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating, disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B antagonists. Also provided herein are processes for making compounds of Formula (I) and intermediate compounds.Type: GrantFiled: January 15, 2002Date of Patent: April 11, 2006Assignee: AstraZeneca ABInventors: Marc Chapdelaine, Timothy Davenport, Markus Haeberlein, Carey Horchler, John McCauley, Edward Pierson, Daniel Sohn
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Patent number: 7022708Abstract: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I: wherein R1, R2, R3, R4, and R5 are as defined herein; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.Type: GrantFiled: October 16, 2003Date of Patent: April 4, 2006Assignee: Roche Palo Alto LLCInventors: Robin Douglas Clark, Ralph New Harris, III, David Bruce Repke
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Patent number: 7019004Abstract: The invention provides compounds of formula (I) wherein X, Y, R1, R2, R3 and R4 are as defined in the description, and the preparation thereof.Type: GrantFiled: May 7, 2001Date of Patent: March 28, 2006Assignee: Novartis AGInventors: Daniel Berney, Robin Breckenridge, Peter Neumann, Gideon Shapiro, Max Peter Seiler, Thomas J. Troxler
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Patent number: 6969729Abstract: The present invention relates to ion channel activating agents. More particularly, the present invention relates to a particular class of chemical compounds that has proven useful as openers of SKCa and IKCa channels. In further aspects, the present invention relates to the use of these SK/IK channel activating agents for the manufacture of medicaments and pharmaceutical compositions comprising the SK/IK channel activating agents.Type: GrantFiled: October 16, 2002Date of Patent: November 29, 2005Assignee: Neurosearch A/SInventors: Bo Skaaning Jensen, Tino Dyhring Jørgensen, Philip K. Ahring, Palle Christophersen, Dorte Strøbaek, Lene Teuber, Søren Peter Olesen
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Patent number: 6958338Abstract: The present invention relates to 4-, 5-, 6- or 7-methylene substituted indolyl derivatives of formula I wherein R is aryl or heteroaryl, where said aryl or heteroaryl groups may be substituted one or more times with a substituent selected from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, C1-6-alkoxy, C1-6-alkylthio, hydroxy, hydroxy-C1-6-alkyl trifluoromethyl, trifluoromethylsulfonyl, C1-6-alkylsulfonyl, amino, C1-6-alkylamino, di-(C1-6-alkyl)amino, acyl, aminocarbonyl and a methylene dioxy group; X is N, C or CH; provided that the dotted line indicates a bond when X is C and no bond when X is N or CH; R1 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, aryl, aryl-C1-6-alkyl, acyl, thioacyl, C1-6-alkylsulfonyl, trifluoromethylsulfonyl or arylsulfonyl; and R2 and R3 are independently selected from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyType: GrantFiled: February 4, 2003Date of Patent: October 25, 2005Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jan Kehler
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Patent number: 6936611Abstract: Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovascular disorders.Type: GrantFiled: January 12, 2004Date of Patent: August 30, 2005Assignee: Eli Lilly and CompanyInventors: John Walter Liebeschuetz, Christopher William Murray, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley, Scott Martin Sheehan, David Birenbaum Engel, Brian Morgan Watson, Peter Robert Guzzo, Michael John Mayer
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Patent number: 6916812Abstract: Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of the melanocortin receptors. The compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders such as obesity, diabetes, and sexual dysfunction.Type: GrantFiled: October 4, 2002Date of Patent: July 12, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Graham S. Poindexter, Guanglin Luo, Ling Chen
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Patent number: 6914064Abstract: The present invention relates to a novel 1,4-disubstituted piperazine derivatives of Formula I, and their pharmaceutically acceptable acid addition salts having excellent uro-selective ?1-adrenoceptor antagonistic activity exceeding those of previously described compounds. The compounds of the present invention hold promise for treating the symptoms of benign prostatic hyperplasia (BPH). The invention also relates to methods for making the novel compounds, pharmaceutical compositions containing the compounds, and method of treating the symptoms of benign prostatic hyperplasia using the compounds.Type: GrantFiled: November 30, 2001Date of Patent: July 5, 2005Assignee: Ranbaxy Laboratories LimitedInventors: Nitya Anand, Sanjay Jain, Neelima Sinha, Anita Chugh, Laxminarayan G. Hegde, Jang Bahadur Gupta
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Patent number: 6906090Abstract: The invention provides the use of certain isatin and oxindole derivatives in the preparation of a medicament for use in the treatment of mycobacterial disease.Type: GrantFiled: March 4, 1999Date of Patent: June 14, 2005Assignee: AstraZeneca ABInventor: Ramachandran Janakiraman
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Patent number: 6903117Abstract: A compound of formula (I): or a salt thereof, or a solvate thereof, wherein Ra represents a group R5 which is hydrogen, alkyl or optionally substituted aryl and Rb represents a moiety of formula (a): wherein X represents a hydroxy or an alkoxy group wherein the alkyl group may be substitued or unsubstituted or X represents a group NRsRt wherein Rs and Rt each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, an optionally substituted heterocyclic group or an optionally substituted heterocyclylalkyl group, or Rs and Rt together with the nitrogen to which they are attached form a heterocyclic group; R1 represents an alkyl or a substituted or unsubstituted aryl group; and R2, R3 and R4 each independently represent hydrogen, alkyl, aryl or substituted aryl; R6 and R7 each independently represent hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamiType: GrantFiled: November 20, 2002Date of Patent: June 7, 2005Assignee: Nikem Research S.R.L.Inventors: Carlo Farina, Stefania Gagliardi, Guy Marguerite Marie Gerard Nadler
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Patent number: 6900206Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with sulfonylureido piperazine derivatives of Formula I. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. wherein: Z is Q is selected from the group consisting of: —W— is — represents a carbon-carbon bond or does not exist; and A is NR13R14.Type: GrantFiled: June 9, 2003Date of Patent: May 31, 2005Assignee: Bristol-Myers Squibb CompanyInventors: John F. Kadow, Alicia Regueiro-Ren, Qiufen May Xue
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Patent number: 6894052Abstract: Disclosed herein are novel compounds and methods for the treatment of disorders of the lower urinary tract. The novel compounds are diarylalkylpiperazine derivatives. The methods comprise the administration of the novel compounds of the invention, and other compounds that bind to 5HT1A receptors, for treating disorders of the lower urinary tract.Type: GrantFiled: July 31, 1998Date of Patent: May 17, 2005Assignee: Recordati S.A. Chemical and Pharmaceutical CompanyInventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
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Patent number: 6890921Abstract: This invention relates to a series of arylsubstituted piperazines, of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the ?-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.Type: GrantFiled: March 15, 2000Date of Patent: May 10, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Linda Jolliffe, William Murray, Virginia Pulito, Allen Reitz, Xiaobing Li, Linda Mulcahy, Cynthia Maryanoff, Frank Villani
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Patent number: 6869957Abstract: This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.Type: GrantFiled: September 23, 2003Date of Patent: March 22, 2005Assignee: Eli Lilly and CompanyInventors: Sung Y. Cho, Thomas A. Crowell, Bruce D. Gitter, Philip A. Hipskind, J. Jeffry Howbert, Joseph H. Krushinski, Jr., Karen L. Lobb, Brian S. Muehl, James A. Nixon
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Patent number: 6864260Abstract: The invention is directed to methods to inhibit p38-? kinase using compounds which contain a phenyl group linked through a piperazine ring to a substituted indole.Type: GrantFiled: May 28, 2002Date of Patent: March 8, 2005Assignee: Scios, Inc.Inventors: Babu J. Mavunkel, Sarvajit Chakravarty, John J. Perumattam, Sundeep Dugar, Qing Lu, Xi Liang
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Patent number: 6855710Abstract: The present invention relates to new substituted indolinones of general formula wherein X and R1 to R5 are defined as in claim 1, the isomers and the salts thereof which have valuable properties. The above compounds of general formula I wherein R1 denotes a hydrogen atom, a C1-3-alkyl group or a prodrug group have valuable pharmacological properties, particularly an inhibiting effect on various kinases, on viral cyclin and on receptor tyrosine kinases, and the other compounds of the above general formula I wherein R1 does not represent a hydrogen atom, a C1-3-alkyl group or a prodrug group are valuable intermediate products for the preparation of the abovementioned compounds.Type: GrantFiled: September 19, 2003Date of Patent: February 15, 2005Assignee: Boehringer Ingelheim Pharma KGInventors: Rainer Walter, Wolfgang Grell, Armin Heckel, Frank Himmelsbach, Wolfgang Eberlein, Gerald Roth, Jacobus C.A. van Meel, Norbert Redemann, Walter Spevak, Ulrike Tontsch-Grunt, Thomas von Rueden
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Patent number: 6846820Abstract: This invention relates to certain indole-2-carboxamides of formula (I) and the pharmaceutically acceptable salts and prodrugs thereof, wherein R6 is carboxy, (C1-C8)alkoxycarbonyl, C(O)NR8R9 or C(O)R12, useful as inhibitors of glycogen phosphorylase, methods of treating glycogen phosphorylase dependent diseases or conditions with such compounds and pharmaceutical compositions comprising such compounds.Type: GrantFiled: June 17, 2003Date of Patent: January 25, 2005Assignee: Pfizer Inc.Inventors: Dennis J. Hoover, Bernard Hulin, William H. Martin, Judith L. Treadway
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Patent number: 6846818Abstract: The present invention relates to cyclooxygenase-2 (COX-2) selective inhibitors of formula I: pharmaceutical compositions containing them, to their medicinal use, and to their preparations. The compounds of the invention are particularly useful in the treatment or alleviation of inflammation and inflammation associated disorders, such as, for example, rheumatoid arthritis and osteoarthritis, and in the relief of pain, such as, for example, pain associated with surgery or trauma, in mammals, preferably felines and canines.Type: GrantFiled: April 16, 2003Date of Patent: January 25, 2005Assignee: Pfizer Inc.Inventors: Kristin Lundy DeMello, Brian S. Bronk, Rhonda Marie Crosson
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Patent number: 6838461Abstract: Compounds of the formula I in which R1, R2, R4 and R5 have the meanings indicated in claim 1, are potent 5-HT2A antagonists and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkingson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia, nervous anorexia, premenstrual syndrome and/or for positively affecting compulsive behavior (obsessive-compulsive disorder, OCD).Type: GrantFiled: July 7, 2000Date of Patent: January 4, 2005Assignee: Merck Patent GmbHInventors: Henning Boettcher, Christoph Seyfried
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Publication number: 20040266784Abstract: Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.Type: ApplicationFiled: April 9, 2004Publication date: December 30, 2004Inventors: Terrance P. Snutch, Gerald W. Zamponi, Hassan Pajouhesh, Francesco Belardetti, Hossein Pajouhesh
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Publication number: 20040266762Abstract: The invention relates to indole derivatives which are used as drugs for treating tumor diseases, in particular when there is drug resistance against other active compounds and where there is a metastasizing carcinoma.Type: ApplicationFiled: June 2, 2004Publication date: December 30, 2004Inventor: Matthias Gerlach
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Publication number: 20040259883Abstract: A thiazolidine derivative represented by the formula (I) 1Type: ApplicationFiled: April 21, 2004Publication date: December 23, 2004Inventors: Hiroshi Sakashita, Tomohiro Yoshida, Hiroshi Kitajima, Masahiro Takeuchi, Yoshihito Tanaka, Takuya Yoshimura, Fumihiko Akahoshi, Yoshiharu Hayashi
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Publication number: 20040259843Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.Type: ApplicationFiled: February 27, 2004Publication date: December 23, 2004Inventors: David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
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Publication number: 20040254374Abstract: Compounds of formula (I) 1Type: ApplicationFiled: June 1, 2004Publication date: December 16, 2004Inventors: Stuart Donald Jones, Daniel Jon Sall, Michael Robert Wiley
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Publication number: 20040248902Abstract: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I: 1Type: ApplicationFiled: June 25, 2004Publication date: December 9, 2004Inventors: Colin Charles Beard, Robin Douglas Clark, Lawrence Emerson Fisher, Ralph New Harris, David Bruce Repke
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Publication number: 20040242589Abstract: The invention relates to novel compounds of formula (I) having affinity for the 5-HT6 receptor preparation, to compositions containing them and their use in the treatment of various disorders, including CNS disoders.Type: ApplicationFiled: February 6, 2004Publication date: December 2, 2004Inventors: Steven Mark Bromidge, Christopher Norbert Johnson, Gregor James MacDonald, Mervyn Thompson, David R Witty
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Patent number: 6825201Abstract: The invention comprises substituted indole, azaindole and related heterocyclic amidopiperazine derivatives of general Formula I wherein: Q is —may represent a bond; A is selected from the group consisting of C1-6alkoxy, C1-6alkyl, C3-7cycloalkyl, phenyl, and heteroaryl; wherein said heteroaryl may be monocyclic or bicyclic and may be comprised of three to eleven atoms selected from the group consisting of C, N, NR9, O, and S, and wherein each ring of said phenyl and heteroaryl is optionally substituted with one to five same or different substituents selected from the group consisting of R19-R23; T is U is NR7, O, or S; V is C(H)kR1, O or N(R7′)k; W is CR3 or NR10; X is CR4 or NR10; Y is CR5 or NR10; Z is CR6 or NR10; k is 0 or 1; and m, n, and p are each independently 0, 1, or 2 provided that the sum of m, n, and p must equal 1 or 2; compositions thereof and their use as antiviral agents, particularly for treating HIV infection.Type: GrantFiled: April 22, 2002Date of Patent: November 30, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, Owen B. Wallace, Nicholas A. Meanwell, Zhongxing Zhang, John A. Bender, John F. Kadow, Kap-Sun Yeung
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Publication number: 20040235833Abstract: The invention relates to indole derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The indole derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: ApplicationFiled: March 12, 2004Publication date: November 25, 2004Applicant: Pfizer IncInventors: Alan Daniel Brown, Justin Stephen Bryans, Mark Edward Bunnage, Paul Alan Glossop, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Simon John Mantell
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Publication number: 20040235859Abstract: The present invention is a chemical compound of formula (I) 1Type: ApplicationFiled: June 23, 2004Publication date: November 25, 2004Inventors: David Reginald Adams, Jonathan Mark Bentley, James Edward Paul Davidson, Claire Elizabeth Dawson, Ashley Roger George, Howard Langham Mansell, Patrizio Mattei, Jacques Mizrahi, Matthias Heinrich Nettekoven, Robert Mark Pratt, Stephan Roever, Jonathan Richard Anthony Roffey, Jean-Luc Specklin, Henri Stalder, Kerry Wilkinson
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Publication number: 20040235753Abstract: Compounds according to general formula 1, wherein G1 is NR6R7 or a group according to general formula 3 and G2 NR24R25 or a fused polycyclic group are novel. They are selective and potent oxytocin agonists. Pharmaceutical compositions of such compounds are useful in the treatment of, inter alia, erectile dysfunction.Type: ApplicationFiled: December 24, 2003Publication date: November 25, 2004Inventors: Gray Robert William Pitt, Michael Bryan Roe, David Philip Rooker
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Patent number: 6821966Abstract: The invention is directed to methods to inhibit p38-&agr; kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein represents a single or double bond; B is —Wi—COXjY wherein Y is COR2 or an isostere thereof and R2 is hydrogen or a noninterfering substituent, each of W and X is a spacer of 2-6 Å, and each of i and j is independently 0 or 1; each R3 is independently a noninterfering substituent, where n is 0-3; Z3 is NR7 or O; wherein R7 is H or a noninterfering substituent; one Z2 is CA or CR8A and the other is CR1, CR12, NR6 or N wherein each R1, R6 and R8 is independently hydrogen or noninterfering substituent; wherein A is: such that Z1 is CR5 or N wherein R5 is hydrogen or a noninterfering substituent; each of l and k is an integer from 0-2 wherein the sum of l and k is 0-3; Ar is an aryl group substituted with 0-5 noninterfering substituents, wherein two noninterfeType: GrantFiled: November 20, 2001Date of Patent: November 23, 2004Assignee: Scios, Inc.Inventors: Sundeep Dugar, John Perumattam, Gregory Luedtke, Xuefei Tan, Qing Lu
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Publication number: 20040220171Abstract: This invention relates to compounds of formula 1Type: ApplicationFiled: July 8, 2003Publication date: November 4, 2004Applicant: AVENTIS PHARMACEUTICALS INCInventors: Heinz Pauls, Yong Gong, Julian Levell, Peter Astles, Paul R. Eastwood
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Publication number: 20040220183Abstract: The invention relates to new hydroxyindoles of the Formula, 1Type: ApplicationFiled: May 27, 2004Publication date: November 4, 2004Inventors: Norbert Hofgen, Ute Egerland, Hildegard Poppe, Degenhard Marx, Stefan Szelenyi, Thomas Kronbach, Emmanuel Polymeropoulos, Sabine Heer
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Publication number: 20040214820Abstract: The present invention relates to 3-guanidinocarbonyl-1-heteroaryl-indole derivatives, pharmaceutical compositions comprising such derivatives, methods of treatment comprising administering such derivatives, and processes for their preparation.Type: ApplicationFiled: December 31, 2003Publication date: October 28, 2004Applicant: AVENTIS PHARMA DEUTSCHLAND GmbHInventors: Heinz-Werner Kleemann, Jean-Christophe Carry, Pascal Desmazeau, Serge Mignani, Jean Bouoquerel, Arielle Genevois-Borella, Baptiste Ronan
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Publication number: 20040215014Abstract: A invention relates to N auroyl cyclic amine derivatives and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: ApplicationFiled: December 17, 2003Publication date: October 28, 2004Inventors: Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, Riccardo Novelli, Roderick Alan Porter
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Patent number: 6809098Abstract: The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity. The invention also relates to pharmaceutical formulations, the use of a compound of the present invention in the manufacture of a medicament, a method of therapeutic treatment using such a compound and processes for producing the compounds.Type: GrantFiled: August 21, 2002Date of Patent: October 26, 2004Assignee: AstraZeneca ABInventors: Michael Wardleworth, Alexander Graham Dossetter, Christopher Thomas Halsall
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Publication number: 20040209893Abstract: The invention relates to piperazine derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to their medical use. The novel compounds are antagonists of tachykinins, including substance P and other neurokinins.Type: ApplicationFiled: May 4, 2004Publication date: October 21, 2004Inventors: Giuseppe Alvaro, Romano Di Fabio, Riccardo Giovannini, Giuseppe Guercio, Yves St-Denis, Antonella Ursini
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Publication number: 20040204422Abstract: The invention relates to N-[(piperazinyl)hetaryl]arylsulfonamide compounds of the general formula I 1Type: ApplicationFiled: April 14, 2003Publication date: October 14, 2004Applicant: Abbott GmbH & Co. KG.Inventors: Wilfried M. Braje, Andreas Haupt, Wilfried Lubisch, Roland Grandel, Karla Drescher, Herve Geneste, Liliane Unger, Daryl R. Sauer
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Publication number: 20040204407Abstract: The present invention relates to 5-sulfonamido substituted indolinones that modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: ApplicationFiled: March 8, 2004Publication date: October 14, 2004Applicant: SUGEN Inc.Inventors: Peng Cho Tang, Congxin Liang, Todd Miller, Kenneth E. Lipson
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Publication number: 20040198720Abstract: 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: ApplicationFiled: February 20, 2004Publication date: October 7, 2004Inventors: Steven W. Andrews, Julie A. Wurster, Edward H. Wang, Thomas Malone
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Patent number: 6797708Abstract: This invention provides substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.Type: GrantFiled: November 22, 2002Date of Patent: September 28, 2004Assignee: WyethInventors: John C. McKew, Steven Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark