Bicyclo Ring System Which Is Indole (including Hydrogenated) Patents (Class 546/201)
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Publication number: 20090093469Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: ApplicationFiled: December 15, 2008Publication date: April 9, 2009Applicant: WYETHInventors: Callain Younghee Kim, Paige Erin Mahaney, Eugene John Trybulski, Puwen Zhang, Eugene Anthony Terefenko, Casey Cameron McComas, Michael Anthony Marella, Richard Dale Coghlan, Gavin David Heffernan, Stephen Todd Cohn, An Thien Vu, Joseph Peter Sabatucci, Fei Ye
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Publication number: 20090076005Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.Type: ApplicationFiled: December 28, 2007Publication date: March 19, 2009Applicant: Xcovery, Inc.Inventors: Congxin Liang, Ming Qi, Shu Gao, Zhigang Li
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Publication number: 20090076004Abstract: There is provided compounds of formula (I), wherein X1, Q, T, Y, R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation.Type: ApplicationFiled: December 22, 2005Publication date: March 19, 2009Inventors: Benjamin Pelcman, Kristofer Olofsson, Martins Katkevics, Vita Ozola, Edgars Suna, Ivars Kalvins, Peteris Trapencieris, Dace Katkevica, Wesley Schaal
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Publication number: 20090069565Abstract: The present invention relates to compounds of formula I, in which R0; R1; R2; R3; R4; R5; R6; R7; Q; V, G and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is indicated. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as pharmaceuticals for treating the foregoing conditions, and pharmaceutical preparations comprising them.Type: ApplicationFiled: May 12, 2008Publication date: March 12, 2009Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Mark NAZARE, Melanie Essrich, David William WILL, Hans MATTER, Kurt RITTER, Volkmar WEHNER
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Publication number: 20090069321Abstract: The present invention relates to cyanomethyl substituted N-acyl tryptamines of the formula I in which R1, R2, R3, R4, R5, Q, X and W have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.Type: ApplicationFiled: July 29, 2008Publication date: March 12, 2009Inventors: Lars WORTMANN, Marcus Koppitz, Florian Peter Liesener, Thomas Frenzel, Hans-Peter Muhn, Anna Schrey, Ronald Kuehne
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Publication number: 20090069245Abstract: The present invention provides novel compounds that have been demonstrated to be modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, iso forms and variants thereof). These compounds are useful as antagonists of the ghrelin receptor as well as inverse agonist, partial agonist or a combination of these activities as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, diabetes, central nervous system disorders, genetic disorders, and hyperproliferative disorders.Type: ApplicationFiled: April 30, 2007Publication date: March 12, 2009Applicant: THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUNDInventors: Cyril Y. Bowers, Gloria S. Tannenbaum, David H. Coy, Simon J. Hocart
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Publication number: 20090060968Abstract: The present invention relates to compounds that inhibit phosphatases, compositions thereof, and methods of using those compounds and compositions for treating diseases.Type: ApplicationFiled: September 12, 2008Publication date: March 5, 2009Inventors: Jeffrey O. Saunders, Gregory F. Miknis, Alexandre J. Buckmelter, Kevin W. Hunt, James F. Blake, Guy P.A. Vigers, Xicheng Sun
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Patent number: 7498328Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them.Type: GrantFiled: July 17, 2006Date of Patent: March 3, 2009Assignee: Laboratorias Del Dr. Esteve, S.A.Inventors: Ramón Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
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Publication number: 20090054407Abstract: The present invention provides a nitrogen-containing heterocyclic compound represented by formula (I): {wherein W represents a nitrogen atom or —CH—; X represents —C(?O)— or —CHR4— (wherein R4 represents a hydrogen atom, or the like); R1 represents a group represented by the following formula: [wherein Q1 represents a nitrogen atom or —CR8— (wherein R8 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like). Q2 represents —NR15— (wherein R15 represents a hydrogen atom, or the like) and R5 and R6 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like]; and R2 and R3 may be the same or different and each represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like} or a pharmaceutically acceptable salt thereof, and the like.Type: ApplicationFiled: April 19, 2006Publication date: February 26, 2009Applicant: Kyowa Hakko Kogyo Co., Ltd.Inventors: Chikara Murakata, Nobuyoshi Amishiro, Toshiyuki Atsumi, Yoshinori Yamashita, Takeshi Takahashi, Ryuichiro Nakai, Hisashi Tagaya, Hiroko Takahashi, Jun Funahashi, Junichiro Yamamoto, Yuichi Fukuda
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Publication number: 20090054451Abstract: The present invention is directed to novel piperidine derivatives and to the use of piperidine derivatives of formula I as agonists of chemokine receptor activity.Type: ApplicationFiled: August 4, 2008Publication date: February 26, 2009Applicant: Euroscreen S.A.Inventors: Jacques Huck, Frederic Ooms, Christian Tyrchan, Hamid R. Hoveyda
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Publication number: 20090048219Abstract: The invention describes novel organic nitric oxide enhancing salts of nonsteroidal antiinflammatory drugs (NSAIDs) and novel compositions comprising at least one organic nitric oxide enhancing salt of an NSAID, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one organic nitric oxide enhancing salt of an NSAID, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent.Type: ApplicationFiled: May 23, 2006Publication date: February 19, 2009Applicant: NITROMED INC.Inventor: David S. Garvey
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Publication number: 20090029979Abstract: This invention relates to compounds which bind to serotonin receptors inside or outside the central nervous system, in particular compounds which bind to the 5-HT2 or 5-HT7 receptors, their preparation and use, compositions containing them, and methods of treatment using them.Type: ApplicationFiled: July 7, 2006Publication date: January 29, 2009Applicant: BIO-MEDISINSK INNOVASJON ASInventors: Jo Klaveness, Bjarne Brudeli, Finn Olav Levy
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Publication number: 20090012055Abstract: Novel substituted piperidines of the general formulae (I) and (II) with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent.Type: ApplicationFiled: February 6, 2008Publication date: January 8, 2009Inventors: Peter Herold, Robert Mah, Stefan Stutz, Aleksandar Stojanovic, Vincenzo Tschinke, Nathalie Jotterand
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Publication number: 20080318923Abstract: It is intended to provide a drug which is efficacious against pathological conditions relating to arginine-vasopressin V1b receptor. More particularly speaking, it is intended to provide a drug which has a therapeutic or preventive effect on depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, hypertension, digestive diseases, drug addiction, epilepsy, brain infarction, brain ischemia, brain edema, head injury, inflammation, immune diseases, alopecia and so on. As the results of intensive studies, a novel 1,3-dihydro-2H-indol-2-one compound and a pyrrolidin-2-one compound fused with a heteroaromatic ring, which are highly selective antagonists of arginine-vasopressin V1b receptor, have high metabolic stabilities and show favorable brain penetration and high plasma concentrations, are found, thereby achieving the above objective.Type: ApplicationFiled: January 30, 2006Publication date: December 25, 2008Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Yoshinori Sekiguchi, Takeshi Kuwada, Masato Hayashi, Dai Nozawa, Yuri Amada, Tsuyoshi Shibata, Shuji Yamamoto, Hiroshi Ohta, Taketoshi Okubo, Takeshi Koami
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Publication number: 20080318933Abstract: The present invention relates to novel indole derivatives such as compounds of the formula (I): which possess antagonist potency at the 5-HT6 receptor and the use of such compounds or pharmaceutically acceptable salts or solvates thereof in the treatment of Alzheimer's disease and other CNS disorders.Type: ApplicationFiled: October 5, 2005Publication date: December 25, 2008Inventors: Mahmood Ahmed, Christopher Norbert Johnson, Neil Derek Miller, Peter Henry Milner, Dean Andrew Rivers, David R Witty
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Patent number: 7465811Abstract: Sulfonylindoline compounds of formula I, wherein R1 through R4, Y and Z have defined meanings, a process for preparation of such compounds, and the use as pharmaceutically active substances, particularly for the treatment or inhibition of neurodegeneration, cardiovascular disease, inflammatory disease, hypercholesterolemia, dyslipidemia, obesity or diabetes.Type: GrantFiled: November 30, 2007Date of Patent: December 16, 2008Assignee: Laboratoires Fournier S.A.Inventors: Luc Lebreton, Christine Dumas, Christine Massardier, Michel Bondoux
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Publication number: 20080300276Abstract: The invention relates to new heterocyclic carboxylic acid amide derivatives of formula (I)—wherein the meaning of X is hydrogen or halogen atom, hydroxy, cyano, C1-C4 alkylsulfonamido optionally substituted by a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted by a halogen atom or halogen atoms, arylsulfonamido groups, is —CH? group or —N? atom, Z is one or more hydrogen or halogen atom, C1-C4 alkyl, C1-C4 alkoxy, cyano, trifluromethyl, trifluoromethoxy group and to the salts thereof, which are antagonists of NMDA receptor or are intermediates for preparing thereof.Type: ApplicationFiled: July 21, 2005Publication date: December 4, 2008Inventors: Istvan Borza, Csilla Horvath, Sandor Farkas, Istvan Gyertyan, Jozsef Nagy, Sandor Kolok, Kornel Galgoczy, Katalin Saghy
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Patent number: 7459466Abstract: Substituted 2-(2,6-dioxopiperidin-3-yl)-phthalimides and 1-oxo-2-(2,6-dioxopiperidin-3-yl)isoindolines reduce the levels of TNF? in a mammal. A typical embodiment is 1-oxo-2-(2,6-dioxo-3-methylpiperidin-3-yl)-4,5,6,7-tetrafluoroisoindoline.Type: GrantFiled: January 14, 2005Date of Patent: December 2, 2008Assignee: Celgene CorporationInventors: George W. Muller, David I. Stirling, Roger Shen-Chu Chen
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Patent number: 7452891Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: January 28, 2005Date of Patent: November 18, 2008Assignee: Schering CorporationInventors: John W. Clader, Hubert B. Josien, Anandan Palani, Tin Yau Chan
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Patent number: 7449459Abstract: The invention relates to compounds of general formula I as well as the production and use thereof as a medication.Type: GrantFiled: March 23, 2007Date of Patent: November 11, 2008Assignee: Bayer Schering Pharma AGInventors: Bernd Buchmann, Dirk Kosemund, Bernd Menzenbach, Martin Fritsch
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Publication number: 20080269291Abstract: The invention is directed to novel indolecarboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): where R1, R2, R3 and X are defined below. These compounds are useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, in particular in the treatment and prevention of disorders mediated by IKK2 mechanisms including inflammatory and tissue repair disorders. Such disorders include rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease).Type: ApplicationFiled: November 17, 2006Publication date: October 30, 2008Inventors: Jeffrey K. Kerns, Jakob Busch-Petersen, Huijie Li, Jeffrey Charles Boehm, Hong Nie, John J. Taggart
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Publication number: 20080261944Abstract: The present invention relates to indole compounds of the formula (I): wherein R1, R2, R3, R4, A, E and X are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.Type: ApplicationFiled: June 8, 2005Publication date: October 23, 2008Inventors: Stefania Colarusso, Immacolata Conte, Joerg Habermann, Frank Narjes, Simona Ponzi
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Patent number: 7435744Abstract: The present invention relates to a compound of formula (I): wherein: V and U are hydrogen, halogen, C1-C4 alkylamino, or together form a group that contains one or more heteroatoms, and that taken together with one or more: (a) hydrogen atoms; (b) carbon atoms; (c) —CH? groups; (d) —CH2— groups; or (e) additional heteroatoms of the same or different type; or any combination thereof, form a 4-7 membered homocyclic or heterocyclic ring, wherein the homocyclic or heterocyclic ring may combine with the phenyl group to form a bicyclic ring, and wherein the homocyclic or heterocyclic ring or the bicyclic ring may contain one or more oxo, thioxo, amino, mercapto, trifluoromethyl, C1-C4 alkyl, ?S or —SH groups; W: is —CO—, —CH2— or —CH2—(C1-C4 alkyl)-; X: is —CO—; Y: is —O—, C1-C4 alkylene, C1-C4 alkynylene, cycloalkylene, aminocarbonyl, —NH—, —N(C1-C4 alkyl)-, -C1-C4 alkylene-N(C1-C4 alkyl)-, —CH2O—, —CH(OH)— or —OCH2—; Z: is hydrogen, halogen, nitro, amino, C1-C4 alkyl, C1-C4 alkoxy, cyano, trifluoromethType: GrantFiled: January 21, 2004Date of Patent: October 14, 2008Assignee: Gedeon Richter Vegyeszeti Gyar RTInventors: Gyorgy Domány, Csilla Horváth, Gizella Bartáné Szalai, József Nagy, Sándor Kolok, Éva Kovácsné Bozó, István Borza, István Vágó, Attila Bielik, Györgyi Ignáczné Szendrei, György Keserü, Sándor Farkas
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Publication number: 20080242671Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: ApplicationFiled: March 25, 2008Publication date: October 2, 2008Applicant: IRM LLCInventors: Hong Liu, Phillip Alper, Arnab Chatterjee, David Tully, Badry Bursulaya, David Woodmansee, Robert Epple, Jennifer Leslie Harris, Jun Li
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Patent number: 7427632Abstract: Compounds of formula (I) in which R1, n, Z, R3 and R4 have any of the meanings given in the specification, are inhibitors of the serine protease Factor Xa and are useful in the treatment of thrombotic disorders.Type: GrantFiled: December 22, 2003Date of Patent: September 23, 2008Assignee: Eli Lilly and CompanyInventors: Scott Martin Sheehan, Brian Morgan Watson, John Walter Liebeschuetz
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Publication number: 20080227815Abstract: A crystal of 1-[1-[2-(7-methoxy-2,2-dimethyl-4-oxochroman-8-yl)-ethyl]piperidin-4-yl]-N-methyl-1H-indole-6-carboxamide fumarate which has peaks at chemical shifts of about 124.0 ppm and about 26.8 ppm in a 13C solid NMR spectrum.Type: ApplicationFiled: May 11, 2006Publication date: September 18, 2008Inventors: Takahisa Sakaguchi, Yuichi Suzuki, Koichi Ito, Jun Niijima, Mamoru Miyazawa, Toshikazu Shimizu, Masaharu Gotoda, Naoko Suzuki, Takashi Hasebe
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Publication number: 20080227814Abstract: The present invention relates to a selective estrogen receptor modulator selected from the group consisting of: (I) or a pharmaceutical salt thereof; useful, e.g., for treating endometriosis and uterine leiomyoma.Type: ApplicationFiled: January 18, 2005Publication date: September 18, 2008Inventors: Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Owen Brendan Wallace
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Patent number: 7425566Abstract: The invention relates to compounds of formula: and to solvates and/or hydrates thereof, with affinity for and selectivity towards the V1b receptors or both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to a process for preparing them, to the intermediate compounds of formula (II) which are useful for preparing them, to pharmaceutical compositions containing them and to their use for preparing medicinal products.Type: GrantFiled: February 24, 2005Date of Patent: September 16, 2008Assignee: Sanofi-AventisInventors: Richard Roux, Claudine Serradeil-le Gal, Jean Wagnon
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Publication number: 20080221114Abstract: A compound of the following formula (I): wherein A is a group of the following formula (I-A): wherein X is an oxygen atom or a sulfur atom, R4 is a hydrogen atom, a C1-6 alkyl group, or other, R5 is a hydrogen atom or other; or a heteroaryl group or other optionally substituted with a halogen, a C1-6 alkyl, a C1-6 alkoxy, or other; R1 and R2 are the same or different and are a hydrogen atom, a C1-6 alkyl group or other; R3 is a hydrogen atom, a halogen atom, a C1-6 alkoxy group, or other; Ra and Rb are the same or different and are a hydrogen atom or a C1-6 alkyl group; and n is an integer of 0-5; or a pharmaceutically acceptable acid addition salt thereof, which can selectively act on mitochondrial benzodiazepine receptor and is useful as a medicament for treating/preventing anxiety disorder, depression, epilepsy, dementia, and so on.Type: ApplicationFiled: January 11, 2006Publication date: September 11, 2008Inventors: Katsunori Kondo, Kaoru Masumoto, Hitoshi Kohayakawa
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Publication number: 20080214615Abstract: This invention relates to N-methylaminomethyl-isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: ApplicationFiled: September 14, 2007Publication date: September 4, 2008Inventors: George W. Muller, Roger Shen-Chu Chen
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Publication number: 20080214542Abstract: The invention concerns compounds of general formula (I), a method for preparing same, as well as their use as therapeutic agent.Type: ApplicationFiled: November 29, 2005Publication date: September 4, 2008Applicant: BIOPROJETInventors: Marc Capet, Denis Danvy, Catherine Dartois, Nicolas Levoin, Marcel Morvan, Isabelle Berrebi-Bertrand, Thierry Calmels, Philippe Robert, Jean-Charles Schwartz, Jeanne-Marie Lecomte
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Publication number: 20080206886Abstract: The present invention relates to a diagnostic contrast agent comprising a water dispersible, near-infrared tricarbocyanine, enamine-functionalized dye having a Stoke shift of greater than 50 and represented by five general formulae. The present invention also relates to a method for making a dye-conjugate utilizing the novel dye and a method of identifying a biological compound using the novel dye conjugate.Type: ApplicationFiled: February 28, 2007Publication date: August 28, 2008Inventors: Ruizheng Wang, John W. Harder, David A. Stegman, William J. Harrison, Hans F. Schmitthenner
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Patent number: 7417058Abstract: The present invention is related to benzsulfonamide derivatives of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzsulfonamide derivatives. Said benzsulfonamide derivatives are ef-ficient modulators of the JNK pathway, they are in particular efficient and selective in-hibitors of JNK 2 and 3. The present invention is furthermore related to novel benzsul-fonamide derivatives as well as to methods of their preparation (I). The compounds of formula I according to the present invention being suitable pharma-ceutical agents are those wherein Ar1 is a substituted or unsubstituted aryl or heteroaryl group. X is O or S, preferably O.R1 is hydrogen or a C1-C6-alkyl group, preferably H.R2 is hydrogen, —COOR3, —CONR3R3?, OH, a C1-C4 alkyl substituted with an OH group, a hydrazido carbonyl group, a sulfate, a sulfonate, an amine or an ammonium salt; n is either 0 or 1, preferably 1.Type: GrantFiled: September 27, 2001Date of Patent: August 26, 2008Assignee: Laboratoires Serono S.A.Inventors: Serge Halazy, Dennis Church, Stephen J. Arkinstall, Marco Biamonte, Montserrat Camps, Jean-Pierre Gotteland, Thomas Rueckle
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Patent number: 7408067Abstract: Compounds comprising an aza-cyclic portion and an aromatic portion linked via a sulphur atom are disclosed. The compounds disclosed are selective modulators of beta 4 subtype nicotinic acetylcholine receptors and are useful for the treatment of dysfunctions of the central and autonomic nervous systems.Type: GrantFiled: July 29, 2002Date of Patent: August 5, 2008Assignee: Merck + Co., Inc.Inventors: Peter Charles Astles, Stephen Richard Baker, Celine Bonnefous, Jean Michel Vernier, Martine Keenan, Adam Jan Sanderson
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Patent number: 7405306Abstract: The invention discloses and claims therapeutic uses of compounds of general formula (I) Wherein X, R1, R2 and R3 are as described herein. The invention further discloses processes for preparing them, and novel intermediates therefor.Type: GrantFiled: October 4, 2007Date of Patent: July 29, 2008Assignee: Sanofi-AventisInventors: Jacques Froissant, Benoit Marabout, Frank Marguet, Frederic Puech
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Publication number: 20080167344Abstract: The present invention is concerned with novel indol-3-yl-carbonyl-piperidine-benzopyrrolone, -benzoxazolone and -benzotriazole derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of formula (I) wherein X, Y and R1 to R10 are as described in the specification.Type: ApplicationFiled: December 19, 2007Publication date: July 10, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Patent number: 7396940Abstract: Combinatorial libraries that contains various different 4, 5 fused 3-substituted-2-pyrrolocarboxylic acids for screening pharmacological activity and methods of synthesizing said libraries.Type: GrantFiled: October 1, 2004Date of Patent: July 8, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Jianping Cai, Robert Alan Goodnow, Jr.
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Publication number: 20080161316Abstract: The present invention is concerned with novel indol-3-yl-carbonyl-piperidine-benzopyrrolone, -benzoxazolone and -benzotriazole derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of formula (I) wherein X, Y and R1 to R10 are as described in the specification.Type: ApplicationFiled: December 19, 2007Publication date: July 3, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20080161315Abstract: The present invention is concerned with novel indol-3-yl-carbonyl-piperidine-benzopyrrolone, -benzoxazolone and -benzotriazole derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of formula (I) wherein X, Y and R1 to R10 are as described in the specification.Type: ApplicationFiled: December 19, 2007Publication date: July 3, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20080153878Abstract: The present invention provides novel indanone derivatives which can be advantageously used for treating and/or preventing of a medical condition for which inhibition of a cholinesterase is desired.Type: ApplicationFiled: December 11, 2007Publication date: June 26, 2008Applicant: Reviva Pharmaceuticals, Inc.Inventors: Laximinarayan Bhat, Prabhu Prasad Mohapatra
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Publication number: 20080146587Abstract: Compounds of formula I or formula II: or pharmaceutically acceptable salts thereof, wherein m, n, p, Ar R1, R2, R4, and R5 are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds.Type: ApplicationFiled: November 8, 2007Publication date: June 19, 2008Inventors: Joe Timothy Bamberg, Counde O'Yang, Meng Sui, Shu-Hai Zhao
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Patent number: 7388095Abstract: The present invention relates to compounds of formula I wherein R1 to R4 and G are as defined in the description and claims and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: November 27, 2006Date of Patent: June 17, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
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Publication number: 20080139548Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention concerns compounds of formula (I) wherein R1 to R11, X and Y are as defined in the specification.Type: ApplicationFiled: November 29, 2007Publication date: June 12, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20080139618Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention concerns compounds of formula (I) wherein R1 to R11, X and Y are as defined in the specification.Type: ApplicationFiled: November 29, 2007Publication date: June 12, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20080139550Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. Present invention is concerned with compounds of the general formula (I) wherein R1 to R6, R8 to R14, R12,, R13,, X and Y are as defined in the specification.Type: ApplicationFiled: November 30, 2007Publication date: June 12, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20080139556Abstract: A composition for binding FKBP proteins is disclosed, along with a method of treating conditions associated with neuronal degeneration, wherein said composition comprises a compound of formula I, wherein, R, R1, R2, R3 and X are as defined herein.Type: ApplicationFiled: December 6, 2006Publication date: June 12, 2008Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: Raymond W. KOSLEY, Bruce Baron, Patrick Jimonet, John G. Jurcak, Stephen J. Shimshock, Xu-yang Zhao, Rosy Sher, Paul J. Mueller, Jennifer Beall, Matthieu Barrague, Joseph W. Guiles
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Publication number: 20080139547Abstract: The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: ApplicationFiled: February 7, 2008Publication date: June 12, 2008Applicant: PHARMACYCLICS, INC.Inventor: Martin SENDZIK
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Publication number: 20080139549Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. Present invention is concerned with compounds of the general formula (I) wherein R1 to R6, R8 to R14, R12?, R13?, X and Y are as defined in the specification.Type: ApplicationFiled: November 30, 2007Publication date: June 12, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20080139619Abstract: A subject of the present application is novel derivatives of benzimidazole and imidazo-pyridine which have a good affinity for certain sub-types of melanocortin receptors, in particular the MC4 receptors. They are particularly useful for treating pathological conditions and diseases in which one or more melanocortin receptors are involved. The invention also relates to pharmaceutical compositions containing said products.Type: ApplicationFiled: January 31, 2008Publication date: June 12, 2008Inventors: Lydie Poitout, Valerie Brault, Carole Sackur, Pierre Roubert, Pascale Plas
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Publication number: 20080139552Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. Present invention is concerned with compounds of the general formula (I) wherein R1 to R6, R8 to R14, R12?, R13?, X and Y are as defined in the specification.Type: ApplicationFiled: November 30, 2007Publication date: June 12, 2008Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider