Spiro Ring System Patents (Class 514/409)
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Publication number: 20090227563Abstract: The present invention concerns boosting the activity of crop protection materials comprising active ingredients from the class of the phenyl-substituted cyclic ketoenols through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.Type: ApplicationFiled: December 11, 2006Publication date: September 10, 2009Applicant: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Dieter Feucht, Udo Bickers, Hans Philipp Huff, Erwin Hacker, Rainer Süssmann
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Publication number: 20090215795Abstract: A cyclic amidine derivative represented by the formula: [wherein R1, R2 and R3 represent hydrogen, C1-6 alkyl, aryl-C1-6 alkyl, etc.; R4, R5 and R7 represent hydrogen, C1-6 alkyl, etc.; Z represents 0 or 1; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; n represents 1 or 2; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; Ar represents hydrogen, a group represented by the formula: [wherein R10-R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc., and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocycle], etc.] or a salt thereof.Type: ApplicationFiled: July 17, 2008Publication date: August 27, 2009Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Shuichi Suzuki, Makoto Kotake, Mitsuaki Miyamoto, Tetsuya Kawahara, Akiharu Kajiwara, Ieharu Hishinuma, Kazuo Okano, Syuhei Miyazawa, Richard Clark, Fumihiro Ozaki, Nobuaki Sato, Masanobu Shinoda, Atsushi Kamada, Itaru Tsukada, Fumiyoshi Matsuura, Yoshimitsu Naoe, Taro Terauchi, Yoshiaki Oohashi, Osamu Ito, Hiroshi Tanaka, Takashi Musha, Motoji Kogushi, Tsutomu Kawata, Toshiyuki Matsuoka, Hiroko Kobayashi, Ken-ichi Chiba, Akifumi Kimura, Naoto Ono
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Publication number: 20090215624Abstract: The invention relates to novel alkoxyalkyl spirocyclic tetramic and tetronic acids of the formula (I), in which A, B, D, Q1, Q2, Q3, Q4, G, W, X, Y and Z are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or microbicides, and also to selective herbicidal compositions comprising, firstly, the alkoxyalkyl spirocyclic tetramic and tetronic acids and, secondly, at least one crop plant compatibility-improving compound.Type: ApplicationFiled: October 20, 2006Publication date: August 27, 2009Applicant: Bayer CropScience AGInventors: Reiner Fischer, Oliver Gaertzen, Stefan Lehr, Dieter Feucht, Olga Malsam, Mark Wilhelm Drewes, Eva-Maria Franken, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Chris Hugh Rosinger, Thomas Bretschneider, Guido Bojack, Jan Dittgen
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Publication number: 20090209513Abstract: The present invention concerns boosting the activity of crop protection materials comprising active ingredients from the class of the phenyl-substituted cyclic ketoenols through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.Type: ApplicationFiled: December 11, 2006Publication date: August 20, 2009Applicant: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Peter Marczok, Udo Reckmann, Christian Arnold, Waltraud Hempel, Erich Sanwald, Rolf Pontzen
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Publication number: 20090209598Abstract: This invention relates to resorcine derivatives of formula (I) wherein R1 is phenyl or a 5- to 6-membered heteroaromatic ring which may contain 1 to 3 heteroatoms selected from oxygen, nitrogen and sulfur, wherein phenyl or the heteroaromatic ring may be fused to a ring selected from phenyl and a 5- to 6-membered saturated, partially unsaturated or aromatic heterocyclic ring which may contain 1 to 3 heteroatoms selected from oxygen, nitrogen and sulfur, wherein phenyl or the 5- to 6-membered heteroaromatic ring or the respective fused ring systems may be unsubstituted or substituted by any combination of 1 to 6 optionally substituted groups R3, wherein R3 is halogen, cyano, nitro, hydroxy, mercapto, amino, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, haloalkyl, haloalkenyl, haloalkynyl, halocycloalkyl, halocycloalkenyl, alkoxy, alkenyloxy, alkynyloxy, haloalkoxy, haloalkenyloxy, haloalkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkylthio, haloalkenylthio, haloalkynylthio, alkylamino, alkenylaminoType: ApplicationFiled: November 10, 2006Publication date: August 20, 2009Inventors: Michael Puhl, Markus Kordes, Matthias Pohlman, Norbert Götz, Michael Rack, Jürgen Langewald, Felix Schneider, Douglas D. Anspaugh, Deborah L. Culbertson, Hassan Oloumi-Sadeghi, David G. Kuhn
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Publication number: 20090209568Abstract: The present invention relates to compounds having pharmacological activity towards the sigma (?) receptor, and more particularly to spiro[benzopyran] or spiro[benzofuran] derivatives, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis.Type: ApplicationFiled: April 23, 2007Publication date: August 20, 2009Inventor: Bernhard Wünsch
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Publication number: 20090162420Abstract: The invention relates to a salt of an ACE inhibitor dicarboxylic acid with an organic amine and/or an alkali compound, a transdermal therapeutic system comprising the salt, and a method of producing the transdermal therapeutic system.Type: ApplicationFiled: December 5, 2006Publication date: June 25, 2009Inventors: Karin Klokkers, Michael Helfrich, Jörg Nink
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Patent number: 7550499Abstract: The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.Type: GrantFiled: May 10, 2005Date of Patent: June 23, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Huji Tuerdi, Hannguang J. Chao, Jennifer X. Qiao, Tammy C. Wang, Timur Gungor
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Publication number: 20090156624Abstract: The present invention provides methods of parasitic infections, thymoma, and lymphoid malignancies in a subject by administering to the subject a therapeutically effective amount of one or more of the compounds of the invention.Type: ApplicationFiled: January 29, 2008Publication date: June 18, 2009Applicant: Praecis Pharmaceuticals IncInventors: Gary L. Olson, Christopher Self, Lily Lee, Charles Michael Cook, Jens Birktoft, Barry Morgan, Christopher C. Arico-Muendel
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Publication number: 20090156626Abstract: Spirocyclic cyclohexane compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them.Type: ApplicationFiled: February 17, 2009Publication date: June 18, 2009Applicant: GRENENTHAL GmbHInventors: Claudia Hinze, Otto Aulenbacher, Bernd Sundermann, Stefan Oberboersch, Elmar Friderichs, Werner Englberger, Babette-Yvonne Koegel, Klaus Linz, Hans Schick, Helmut Sonnenschein, Birgitta Henkel, Valerie Sarah Rose, Michael Jonathan Lipkin
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Patent number: 7538135Abstract: Compounds of the formula provide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases (IBDs), ulcerative colitis and Crohn's disease, and conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.Type: GrantFiled: July 7, 2004Date of Patent: May 26, 2009Assignee: Novartis AGInventor: Thalaththani Ralalage Vedananda
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Patent number: 7534790Abstract: Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.Type: GrantFiled: November 21, 2007Date of Patent: May 19, 2009Assignee: Cardiome Pharma Corp.Inventors: Allen I. Bain, Gregory N. Beatch, Cindy J. Longley, Bertrand M. C. Plouvier, Tao Sheng, Michael J. A. Walker, Richard A. Wall, Sandro L. Yong, Jeff Jiqun Zhu, Alexander B. Zolotoy
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Patent number: 7528156Abstract: The invention provides compounds of general formula (D wherein m, n, Q, Z1, Z2, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: November 22, 2004Date of Patent: May 5, 2009Assignee: AstraZeneca ABInventors: Tomas Eriksson, Tomas Klingstedt, Tesfaledet Mussie
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Publication number: 20090111842Abstract: Spirocyclic cyclohexane compounds corresponding to formula I a process for manufacturing such compounds, pharmaceutical compositions that contain such compounds, and the use of such spirocyclic cyclohexane compounds for the production of pharmaceuticals, and particularly for the treatment of pain.Type: ApplicationFiled: October 27, 2008Publication date: April 30, 2009Applicant: Gruenenthal GmbHInventors: Beatrix Merla, Stefan Oberboersch, Bernd Sundermann, Werner Englberger, Hagen-Heinrich Hennies, Babette-Yvonne Koegel, Stephan Schunk, Heinz Graubaum
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Patent number: 7524856Abstract: The invention provides compounds of formula (I) wherein m, R1, n, R2, q, p, X, Y, R3, R4, t and, R5 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: December 20, 2004Date of Patent: April 28, 2009Assignee: AstraZeneca ABInventors: Nafizal Hossain, Svetlana Ivanova
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Publication number: 20090105289Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11 ?-hydroxy-Steroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.Type: ApplicationFiled: October 12, 2005Publication date: April 23, 2009Applicant: Novo Nordisk A/SInventors: John Paul Kilburn, Henrik Sune Anderson, Gita Camilla Tejlgaard Kampen
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Publication number: 20090099223Abstract: The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.Type: ApplicationFiled: December 17, 2008Publication date: April 16, 2009Applicant: WyethInventors: Andrew Fensome, Gary S. Grubb, Diane Deborah Harrison, Richard Craig Winneker
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Publication number: 20090099164Abstract: 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 16, 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: 20090099247Abstract: Compounds of the formula (I) in which A, B, G, W, X, Y and Z can have the meanings given in the description are highly suitable for controlling animal pests such as insects and/or spider mites and/or nematodes by treating the soil/growth substrate by drenching or drip application or dipping or soil injection.Type: ApplicationFiled: September 23, 2008Publication date: April 16, 2009Inventors: Thomas E. Macom, Reiner Fischer, Gerhard Baron, Erich Sanwald, Reed Nathan Royalty, Xavier Alain Marie Van Waetermeulen, Udo Reckmann, Alexandra Gladbach, Stephen Krueger, Peter Marczok
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Publication number: 20090099180Abstract: The present invention discloses novel compounds of Formula (I): having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.Type: ApplicationFiled: April 25, 2007Publication date: April 16, 2009Inventors: Thomas Edward Mabry, Owen Brendan Wallace, Yanping Xu, Nancy June Snyder, Leonard Larry Winneroski, JR.
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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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Patent number: 7514466Abstract: Methods for purifying a compound of formula I are provided, wherein A, B X, Q, and R1 are defined herein. The methods include mixing the compound of formula I and a solvent; adding a base to the solvent; and precipitating purified compound of formula I.Type: GrantFiled: April 25, 2005Date of Patent: April 7, 2009Assignee: WyethInventors: Bogdan Kazimierz Wilk, Arkadiy Zinoviy Rubezhov, Anthony Francis Hadfield, Jean Louise Helom
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Publication number: 20090082393Abstract: Compounds of formula (I): (A)m·(B)n??(I) wherein A represents an angiotensin-converting enzyme inhibitor compound containing at least one salt-forming basic function, B represents a compound containing at least one salt-forming acid function and at least one NO donor group, m represents the number of acid functions of B that have been converted to a salt and n represents the number of basic functions of A that have been converted to a salt, the bond or bonds between A and B being of the ionic type. Medicinal products containing the same which are useful in treating cardiovascular pathologies.Type: ApplicationFiled: September 17, 2008Publication date: March 26, 2009Applicant: LES LABORATOIRES SERVIERInventors: Guillaume De Nanteuil, Bernard Portevin, Philippe Gloanec, Jean-Gilles Parmentier, Alain Benoist, Tony Verbeuren, Alain Rupin, Christine Courchay, Serge Simonet
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Publication number: 20090069362Abstract: The present invention is directed to novel spiro-benzo[C]chromene derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders mediated by one or more estrogen receptors. The compounds of the invention are useful in the treatment of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.Type: ApplicationFiled: November 11, 2008Publication date: March 12, 2009Inventors: Xuqing Zhang, Zhihua Sui
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Patent number: 7498338Abstract: The invention provides compounds of formula (I) wherein m, R1, n, R2, q, X, Y, Z, t, R3, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: November 15, 2004Date of Patent: March 3, 2009Assignee: AstraZeneca ABInventors: Andrew Baxter, Nafizal Hossain, Svetlana Ivanova, Marguerite Mensonides-Harsema, Austen Pimm, James Reuberson
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Publication number: 20090054382Abstract: Provided herein are pharmaceutical compositions comprising one or more phosphodiesterase inhibitors of type IV (“PDE-IV”), and at least one other active ingredients selected from muscarinic receptor antagonists (MRA), ?2-agonists, p38 MAP Kinase inhibitors, and corticosteroids and optionally one or more pharmaceutically acceptable excipients and/or other therapeutic agents. In addition, methods of treating autoimmune, inflammatory or allergic diseases or disorders are provided.Type: ApplicationFiled: October 19, 2006Publication date: February 26, 2009Inventors: Abhijit Ray, Sunanda G. Dastidar, Rajkumar Shirumalla, Suman Gupta
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Publication number: 20090042967Abstract: The present invention relates to pharmaceutical agents which are agents for the prophylaxis or treatment of hypogonadism, male climacteric disorder, frailty, cachexia or osteoporosis; the pharmaceutical agents frailty suppressants, muscle strength enhancers, muscle increasing agents, cachexia suppressants, body weight decrease suppressants, agents for the prophylaxis or treatment of prostate hypertrophy, amyotrophy or muscle loss caused by a disease or an agent for reducing the prostate weight.Type: ApplicationFiled: August 6, 2008Publication date: February 12, 2009Applicant: Takeda Pharmaceutical Company LimitedInventor: Atsushi Hasuoka
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Publication number: 20090029858Abstract: The invention relates to novel spirocyclic 3?-alkoxytetramic acids and -tetronic acids of the formula (I), in which A, B, D, Q1, Q2, G, W, X, Y and Z are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or microbicides, and also to selective herbicidal compositions comprising firstly the spirocyclic 3?-alkoxytetramic acids and -tetronic acids and secondly at least one compound which improves crop plant tolerance.Type: ApplicationFiled: June 18, 2005Publication date: January 29, 2009Applicant: BAYER CROPSCIENCE AKTIENGESELLSCHAFTInventors: Reiner Fischer, Oliver Gaertzen, Stefan Lehr, Thomas Bretschneider, Dieter Feucht, Olga Malsam, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Chris Rosinger
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Publication number: 20090030006Abstract: The present invention provides a compound of Formula (I): wherein R1, R2, R3 and R4 are each independently selected from a hydrogen atom, an optionally substituted C1-C6 alkyl group, an optionally substituted C7-C14 aralkyl group and —C(?O)Rx; Rx represents an optionally substituted C1-C6 alkyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted C1-C6 alkoxy group or —NReRf; Ar1 represents an optionally substituted aromatic carbocyclic ring or an optionally mono-substituted aromatic heterocyclic ring; Q represents —(CH2)m-(L)p- or -(L)p-(CH2)m—; m represents an integer selected from 0 to 2, n represents an integer selected from 1 and 2, and p represents an integer selected from 0 and 1; L represents —O—, —S— or —NR5—; and A represents an optionally substituted aryl group or an optionally substituted heteroaryl group, a prodrug thereof and a pharmaceutically acceptable salt thereof, as well as a pharmaceutical preparation or pharmaceutical coType: ApplicationFiled: January 27, 2006Publication date: January 29, 2009Inventors: Takamitsu Kobayashi, Tsutomu Sato, Masahiro Nishimoto
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Publication number: 20090022689Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: July 9, 2008Publication date: January 22, 2009Inventors: Yat Sun Or, Lu Ying, Ce Wang, Yao-Ling Qiu
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Patent number: 7476688Abstract: A cyclic amidine derivative represented by the formula: [wherein R1, R2 and R3 represent hydrogen, C1-6 alkyl, aryl-C1-6 alkyl, etc.; R4, R5 and R7 represent hydrogen, C1-6 alkyl, etc.; Z represents 0 or 1; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; n represents 1 or 2; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; Ar represents hydrogen, a group represented by the formula: [wherein R10-R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc., and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocycle], etc.] or a salt thereof.Type: GrantFiled: April 19, 2002Date of Patent: January 13, 2009Assignee: EISAI R&D Management Co., Ltd.Inventors: Shuichi Suzuki, Masanobu Shinoda, Motoji Kogushi, Hiroko Kobayashi
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Publication number: 20090012100Abstract: The present invention relates to the use of selective insecticidal compositions, characterized in that they comprise an effective amount of an active compound combination comprising (a) at least one compound of the formula (I) in which CKE, W, X, Y and Z are as defined in the description, and (b) at least one crop plant compatibility-improving compound, from the group of compounds mentioned in the description, for controlling insects and/or arachnids, and to a method for controlling insects and/or arachnids using the compositions.Type: ApplicationFiled: July 18, 2005Publication date: January 8, 2009Inventors: Reiner Fischer, Udo Reckmann, Christopher Hugh Rosinger, Erich Sanwald, Christian Arnold
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Publication number: 20090012120Abstract: An ylide-based aza-Payne rearrangement of 2,3-aziridin-1-ols leads to an efficient process for the preparation of pyrrolidines. The aza-Payne rearrangement under the basic reaction conditions favors the formation of epoxy amines. Subsequent nucleophilic attack of the epoxide by the ylide yields a bis-anion, which upon a 5-exo-tet ring closure yields the desired pyrrolidine, thus completing the relay of the 3-membered the 5-membered nitrogen containing ring system. This process takes place with complete transfer of stereochemical fidelity, and can be applied to sterically hindered aziridinols.Type: ApplicationFiled: May 9, 2007Publication date: January 8, 2009Applicant: Board of Trustees of Michigan State UniversityInventors: Babak Borhan, Jennifer M. Schomaker, Somnath Bhattacharjee, Keith Korthals
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Publication number: 20080318776Abstract: The invention relates to novel 2,6-diethyl-4-methylphenyl-substituted tetramic acid derivatives of the formula (I) in which A, B, D and G are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selectively herbicidal compositions comprising, firstly, the 2,6-diethyl-4-methylphenyl-substituted tetramic acid derivatives of the formula (I) and, secondly, at least one crop plant tolerance promoter compound.Type: ApplicationFiled: October 21, 2005Publication date: December 25, 2008Inventors: Reiner Fischer, Stefan Lehr, Mark Wilhelm Drewes, Dieter Feucht, Olga Malsam, Guido Bojack, Christian Arnold, Thomas Auler, Marin Jeffrey Hills, Heinz Kehne, Chris Rosinger
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Publication number: 20080312306Abstract: Novel polymorph Form II and III, solvate Forms I, II, III, and IV, and the hydrate of 5-(4?-fluoro-2?-oxo-1?,2?-dihydrospiro[cyclopropane-1,3?-indol]-5?-yl)-1-methyl-1H-pyrrole-2-carbonitrile are provided, as are methods for preparing the same. Pharmaceutical compositions and kits containing these novel polymorphs, solvates, and hydrate, and combinations thereof are further provided, as are methods of contraception; treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, hormone-dependent carcinomas; treating symptoms of premenstrual syndrome and premenstrual dysphoric disorder; providing hormone replacement therapy; stimulating food intake; synchronizing estrus; or treating symptoms of premenstrual syndrome using one or more of these polymorphs, solvates, or hydrate.Type: ApplicationFiled: June 13, 2008Publication date: December 18, 2008Applicant: WyethInventors: Mahmoud Mirmehrabi, John Leo Considine, Yuping Niu, Abdolsamad Tadayon, Subodh Deshmukh, Jennifer Q. Liang, Yanzhong Wu
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Publication number: 20080306041Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably ?-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds.Type: ApplicationFiled: January 23, 2006Publication date: December 11, 2008Inventor: David S. Garvey
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Publication number: 20080305955Abstract: The invention relates to novel spiroketal-substituted cyclic ketoenols of the formula (I) in which A, B, Q1, Q2, D, G, W, X, Y, and Z are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or microbicides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, spiroketal-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound.Type: ApplicationFiled: February 8, 2006Publication date: December 11, 2008Applicant: Bayer CropScience AGInventors: Thomas Bretschneider, Reiner Fischer, Oliver Gaertzen, Stefan Lehr, Mark Wilhelm Drewes, Dieter Feucht, Olga Malsam, Udo Reckmann, Christian Arnold, Thomas Auler, Waltraud Hempel, Martin Jeffrey Hills, Heinz Kehne, Christopher Hugh Rosinger, Erich Sanwald
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Publication number: 20080293753Abstract: The invention relates to quaternary ?-aminocarboxyamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, X, q and n are as defined in claim 1, for treating diseases and conditions mediated by modulation of voltage-gated sodium channels.Type: ApplicationFiled: October 6, 2006Publication date: November 27, 2008Inventors: Giuseppe Alvaro, David Amantini, Markus Bergauer, Francesca Bonetti, Roberto Profeta
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Publication number: 20080293685Abstract: This invention relates to diamondoid derivatives which exhibit therapeutic activity. Specifically, the diamondoid derivatives herein exhibit therapeutic effects in the treatment of viral disorders. Also provided are methods of treatment, prevention and inhibition of viral disorders in a subject in need.Type: ApplicationFiled: May 22, 2008Publication date: November 27, 2008Applicant: Chevron U.S.A. Inc.Inventors: Deyuan Kong, Frederick W. Lam, Steven F. Sciamanna, Earl Shelton, Shenggao Liu, Robert M. Carlson
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Publication number: 20080293678Abstract: The invention describes compositions and kits comprising at least qrie organic nitric oxide enhancing salt of an angiotensin converting enzyme inhibitor, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia.Type: ApplicationFiled: March 17, 2006Publication date: November 27, 2008Applicant: NitroMed, Inc.Inventor: David S. Garvey
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Publication number: 20080287435Abstract: The novel active compound combinations of certain cyclic ketoenols and ethiprole have very good insecticidal and acaricidal properties.Type: ApplicationFiled: February 14, 2006Publication date: November 20, 2008Applicant: Bayer CropScience AGInventors: Reiner Fischer, Heike Hungenberg, Wolfgang Thielert
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Patent number: 7449475Abstract: The invention provides compounds of formula (I) wherein m R1, n, R2, q, X, Y, Z, R3, R4, R5, R6, R7, R8, t, and R9 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: July 7, 2003Date of Patent: November 11, 2008Assignee: AstraZeneca ABInventors: Nafizal Hossain, Svetlana Ivanova, Marguerite Mensonides-Harsema
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Patent number: 7439263Abstract: Compounds of formula (I): wherein: X1 represents an atom or group selected from CR4aR4b, O, S(O)q1 and NR5, wherein R4a, R4b, q1 and R5 are as defined in the description, m1 represents zero or an integer from 1 to 4 inclusive, m2 represents an integer from 1 to 4 inclusive, n1 and n2, which may be identical or different, each represent an integer from 1 to 3 inclusive, R1 represents hydrogen or a group selected from carboxy, alkoxycarbonyl, optionally substituted carbamoyl and optionally substituted alkyl, R2 represents hydrogen or alkyl, Ak represents an optionally substituted alkylene chain, p represents zero, 1 or 2, R3 represents hydrogen or cyano, X2 and X3, which may be identical or different, each represent either S(O)q2, or CR6aR6b, wherein q2, R6a and R6b are as defined in the description, its optical isomers, where they exist, and its addition salts with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful as DPP-IV inhibitors.Type: GrantFiled: May 18, 2005Date of Patent: October 21, 2008Assignee: Les Laboratoires ServierInventors: Guillaume De Nanteuil, Alain Benoist, Murielle Combettes, Elizabeth Harley
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Publication number: 20080221141Abstract: Spirocyclic cyclohexane compounds useful in pharmaceutical compositions for use in the treatment of substance dependency.Type: ApplicationFiled: October 10, 2007Publication date: September 11, 2008Applicant: GRUENENTHAL GMBHInventors: Elmar FRIDERICHS, Babette-Yvonne KOEGEL, Klaus LINZ
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Patent number: 7410978Abstract: A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (Cmin) and maximum (Cmax) blood levels of about 0.5-2.5 ng/ml and about 2.0-6.0 ng/ml, respectively.Type: GrantFiled: November 4, 2004Date of Patent: August 12, 2008Assignee: Supernus Pharmaceuticals, Inc.Inventors: Argaw Kidane, Henry H. Flanner, Padmanabh Bhatt, Arash Raoufinia
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Publication number: 20080171788Abstract: The invention relates to a medicament for IBS, which comprises a dual antagonist for 5-HT2B and 5-HT7 receptors having selective binding affinities for 5-HT2B and 5-HT7 receptors. The pharmaceutical composition of the invention is useful as a drug which is excellent in the therapeutic effect on IBS and shows lessened side effects occurring in the existing remedies for IBS, because it showed good pharmacological actions in comparison with the case of independently using a 5-HT2B receptor antagonist having selective binding affinity for 5-HT2B receptor or a 5-HT7 receptor antagonist having selective binding affinity for 5-HT7 receptor.Type: ApplicationFiled: February 7, 2006Publication date: July 17, 2008Inventors: Shinobu Akuzawa, Hiroyuki Ito, Toshihiro Watanabe, Hiroyoshi Yamada
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Publication number: 20080171753Abstract: A compound represented by, e.g. the formula (I): [wherein X, Y, Z, and W each independently represent optionally substituted methine; A, B, and D each independently represent —C(O)—, etc.; Q represents a methine or a nitrogen; and R represents the formula (II-1), optionally substituted with lower alkyl, etc.; (wherein R6 represents a lower alkyl, etc; and R7 and R8 each independently represents a lower alkyl, etc.)] or a pharmaceutically acceptable salt of the compound. The compounds and salt have antagonistic activity against a histamine H3 receptor or inverse agonistic activity against a histamine H3 receptor. They are useful in the prevention or treatment of metabolic diseases, circulatory diseases, or neurotic diseases.Type: ApplicationFiled: September 6, 2005Publication date: July 17, 2008Inventors: Makoto Jitsuoka, Norikazu Ohtake, Nagaaki Sato, Shigeru Tokita, Daisuke Tsukahara
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Patent number: 7396846Abstract: This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.Type: GrantFiled: March 31, 2003Date of Patent: July 8, 2008Assignee: Eli Lilly and CompanyInventors: Britta Evers, Ruehter Gerd, Eva Maria Martin De La Nava, Mark Joseph Tebbe
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Patent number: 7393858Abstract: The present invention relates to compounds of formula (Ia) wherein A, B, n, m, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are defined herein, and pharmaceutically acceptable salts thereof; the compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.Type: GrantFiled: March 4, 2004Date of Patent: July 1, 2008Assignee: Merck Sharp & Dohme Ltd.Inventors: Olivier Dirat, Jason Matthew Elliott, Ian Thomas Huscroft, Richard Alexander Jelley, Janusz Jozef Kulagowski, Piotr Antoni Raubo, Duncan Edward Shaw, Francine Sternfeld, Christopher John Swain
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Publication number: 20080153817Abstract: Compounds of formula (I): are useful in the treatment of diseases associated with deposition of ?-amyloid in the brain.Type: ApplicationFiled: July 29, 2004Publication date: June 26, 2008Inventors: Dirk Beher, Michela Bettati, Graham David Checksfield, Ian Churcher, Victoria Alexandra Doughty, Paul Joseph Oakley, Abdul Quddus, Martin Richard Teall, Jonathan David Wrigley