Chalcogen Bonded Directly To The Bicyclo-carbocyclic Ring System Patents (Class 546/206)
-
Publication number: 20120184735Abstract: A 2,3-dihydro-1H-indene-2-yl urea derivative represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:Type: ApplicationFiled: September 30, 2010Publication date: July 19, 2012Applicant: TORAY INDUSTRIES, INC.Inventors: Hiroaki Kaneko, Hideki Kawai, Yosuke Iura, Hideki Inoue, Mie Kaino, Hiroyuki Meguro, Tazuru Uchida
-
Publication number: 20120178741Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: March 21, 2012Publication date: July 12, 2012Applicant: JANSSEN PHARMACEUTICA N.V.Inventors: Kristof Van Emelen, Leo Jacobus Jozel Backx, Sven Franciscus Anna Van Brandt, Patrick René Angibaud, Isabelle Noélle Constance Pilatte, Marc Gustaaf Celine Verdonck, Hans Louis Jos De Winter, Jimmy Arnold Viviane Van heusden
-
Publication number: 20120142930Abstract: Novel compounds are continually sought after to treat and prevent diseases and disorders. The invention relates to N-(2-oxo-1-phenylpiperidin-3-yl)sulfonamides useful for being biologically and pharmacologically screened, and to contribute to the exploration and identification of new lead molecules that are capable of modulating the functional activity of a biological target.Type: ApplicationFiled: December 21, 2011Publication date: June 7, 2012Inventors: Josep CASTELLS BOLIART, David Enrique MIGUEL CENTENO, Marta PASCUAL GILABERT
-
Patent number: 8188077Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: GrantFiled: March 16, 2011Date of Patent: May 29, 2012Assignee: Abbott LaboratoriesInventors: Hong Ding, Steven W. Elmore, Laura A. Hexamer, Aaron R. Kunzer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Michael D. Wendt
-
Publication number: 20120129888Abstract: Novel compounds are continually sought after to treat and prevent disorders. The invention relates to N-(2-oxo-1-phenylpiperidin-3-yl)sulfonamides useful for contributing to the search and identification of new lead compounds which can modulate the functional activity of a biological target.Type: ApplicationFiled: December 22, 2011Publication date: May 24, 2012Inventors: JOSEP CASTELLS BOLIART, David Enrique Miguel Centeno, Marta Pascual Gilabert
-
Publication number: 20120122708Abstract: New compounds are continually sought after for the treatment and prevention of disorders. The invention relates to N-(2-oxo-1-phenylpiperidin-3-yl)sulfonamides which can be biologically and pharmacologically traced, in order to be used in the search for, and identification of, new lead compounds that can modulate the functional activity of a biological target.Type: ApplicationFiled: December 29, 2011Publication date: May 17, 2012Inventors: JOSEP CASTELLS BOLIART, David Enrique MIGUEL CENTENO, Marta PASCUAL GILABERT
-
Patent number: 8124783Abstract: Disclosed herein the process for producing 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2yl)methyl]piperidine or its salt thereof employing novel intermediates.Type: GrantFiled: December 30, 2004Date of Patent: February 28, 2012Assignee: Jubilant Organosys LimitedInventors: Shailendra Kumar Dubey, Amit Kumar Sharma, Beena S. Rani, Soumendu Paul, Rajesh Kumar Thaper, Dubey Sushil Kumar, Jag Mohan Khanna
-
Publication number: 20120022070Abstract: Novel classes of molecular chaperone Heat shock protein 90 (Hsp90) inhibitors are disclosed. These compounds are useful in treating and preventing cancer and other Hsp90-related diseases and conditions, such as inflammation and neurodegenerative disorders. Methods of treating and preventing cancer and other Hsp90 related diseases and conditions are disclosed that include administering to the subject a therapeutically effective amount of an Hsp90 inhibitor. Methods of preparing the novel Hsp90 inhibitors are also provided.Type: ApplicationFiled: October 6, 2009Publication date: January 26, 2012Applicant: EMORY UNIVERSITYInventors: Jaeki Min, Pahk Thepchatri, Yuhong Du, Dennis C. Liotta, Haian Fu
-
Publication number: 20120015960Abstract: Provided are compounds for inhibiting Snail-p53 binding and therapeutic agents for cancer including the compounds as an effective component. The Snail-p53 binding inhibitors induce expression of p53 in K-Ras mutant cell lines, thereby enabling effective treatment or prevention of K-Ras mutant cancer, such as, pancreatic cancer, lung cancer, cholangioma, and colon cancer, of which diagnosis or treatment is not easy.Type: ApplicationFiled: November 23, 2009Publication date: January 19, 2012Applicants: The Industry & Academic Cooperation in Chungnam National University, Pusan National University Industry-University Cooperation FoundationInventors: Bum Joon Park, Nam Chul Ha, Sun Hye Lee, Gyu Yong Song, Jee Hyun Lee
-
Publication number: 20110313159Abstract: A novel camphor-derived ?-amino alcohol compound is disclosed. The novel camphor-derived ?-amino alcohol compound can be used in asymmetric addition of organozinc to aromatic and aliphatic aldehydes, including linear aliphatic ones, thus generating corresponding secondary alcohols in high yields and enantiomeric excess.Type: ApplicationFiled: June 18, 2010Publication date: December 22, 2011Inventors: Biing-Jiun UANG, Chi-Rui Wu, Hsyueh-Liang Wu
-
Publication number: 20110281847Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.Type: ApplicationFiled: June 23, 2011Publication date: November 17, 2011Applicant: ELI LILLY AND COMPANYInventors: Robert Dean Dally, Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Timothy Alan Shepherd, Owen Brendan Wallace
-
Publication number: 20110230663Abstract: The present invention relates to novel process for preparing Donepezil hydrochloride of formula (I)Type: ApplicationFiled: November 30, 2009Publication date: September 22, 2011Applicant: ALEMBIC LIMITEDInventors: Ravi Ponnaiah, Ashok Prasad, Dineshkumar Ramabhai Panchasara, Gajanan Jijaba Chavan, Bhavesh Hareshbhai Prajapati, Ilesh Mahendrabhai Patel
-
Publication number: 20110218217Abstract: This invention relates to novel piperidine-4-propionamide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: August 25, 2009Publication date: September 8, 2011Applicant: NEUROSEARCH A/SInventors: Dan Peters, John Paul Redrobe, Elsebet Østergaard Nielsen
-
Publication number: 20110196149Abstract: A method for the fluoridation of an iodonium salt with a fluoride ion source which can be carried out in an aqueous reaction solvent.Type: ApplicationFiled: April 18, 2011Publication date: August 11, 2011Applicant: GE HEALTHCARE LIMITEDInventors: HARRY JOHN WADSWORTH, PETER ANTHONY DEVENISH
-
Patent number: 7994328Abstract: The present invention relates to an improved process for the preparation of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride of Formula I.Type: GrantFiled: February 8, 2007Date of Patent: August 9, 2011Assignee: Aurobindo Pharma Ltd.Inventors: Mahesh Nagarimadugu, Arun Kumar Gupta, Ramesh Dandala, Sivakumaran Meenakshisunderam
-
Publication number: 20110178088Abstract: This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.Type: ApplicationFiled: March 21, 2011Publication date: July 21, 2011Applicant: XENTION LIMITEDInventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
-
Publication number: 20110160246Abstract: Methods and compositions are provided for reducing aggregation of neurodegenerative proteins associated with neurotoxicity or other proteins. The compounds comprise a first domain or targeting element for binding to the target proteins linked to a second domain or recruiting element that binds to an aggregation inhibiting protein, e.g. a prolyl isomerase. By associating the aggregating forming proteins or neuronal cells under conditions where aggregating proteins are produced with the compound and the aggregation inhibiting protein, aggregation is reduced. The subject agents can be used in assays, investigating the etiology of the neuronal diseases and for prophylaxis and therapy.Type: ApplicationFiled: November 11, 2010Publication date: June 30, 2011Inventors: Isabella A. Graef, Gerald R. Crabtree, Jason E. Gestwicki
-
Publication number: 20110160247Abstract: The present invention relates to an aralkyl alcohol piperidine derivative and use as antidepressant thereo. The said aralkyl alcohol piperidine derivative has a triple inhibition effect on the reuptaking of 5-HT, NA and DA. The derivative may be administered to the patient in need of such treatment in the form of composition by oral administration, injection and the like.Type: ApplicationFiled: June 8, 2009Publication date: June 30, 2011Applicants: JIANGSU GOWORTH INVESTMENT CO. LTD, SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRYInventors: Jianqi Li, Kai Gao, Wangping Cai, Yongyong Zheng
-
Patent number: 7960412Abstract: The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; ??(I-1) formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Ra and Rb are the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R? represents 1 to 4 independent hydrogen atoms and the like; and R? represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.Type: GrantFiled: August 20, 2009Date of Patent: June 14, 2011Assignee: Eisai R&D Management Co., Ltd.Inventors: Shinichi Hamaoka, Noritaka Kitazawa, Kazumasa Nara, Atsushi Sasaki, Atsushi Kamada, Tadashi Okabe
-
Publication number: 20110130568Abstract: The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.Type: ApplicationFiled: February 23, 2009Publication date: June 2, 2011Inventors: Roman Manetsch, Hong-Gang Wang, Xiandong Hu, Sameer Kulkami, Jiazhi G. Sun
-
Publication number: 20110112076Abstract: The present invention provides a compound of formula (I) said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).Type: ApplicationFiled: July 13, 2009Publication date: May 12, 2011Inventors: Leslie Wighton McQuire, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi, Sven Weiler
-
Publication number: 20110105759Abstract: It is intended to provide a process for producing 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-ylidene]methylpiperidine represented by the structural formula (I): (I) which is useful as an intermediate material for a pharmaceutical or a solvate thereof in which impurity content is further reduced and operation is simple and suitable for industrial production by reacting 5,6-dimethoxy-1-indanone with 1-benzyl-4-formylpiperidine in a reaction solvent in the presence of a base and then gradually crystallizing a target substance in a reaction mixture in a high temperature region.Type: ApplicationFiled: July 24, 2006Publication date: May 5, 2011Inventors: Akio Imai, Akihiko Shimotani, Tomio Tsurugi, Yukio Narabu
-
Publication number: 20110086880Abstract: This invention relates to novel alkyl substituted piperidine derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: December 16, 2010Publication date: April 14, 2011Inventors: Dan PETERS, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Jørgen Scheel-Krüger, Birgitte L. Eriksen
-
Publication number: 20110077271Abstract: The present invention provides a process for preparing donepezil or a salt thereof, the process comprising reducing a 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methylene]pyridonium halide of formula II, wherein X is bromide or chloride, in the presence of an ionic compound, a solvent, a catalyst and a source of hydrogen, to form donepezil and optionally converting the donepezil to the salt thereof.Type: ApplicationFiled: March 24, 2009Publication date: March 31, 2011Applicant: CIPLA LIMITEDInventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Srinivas Laxminarayan Pathi
-
Patent number: 7915420Abstract: The invention provides novel GlyT2 inhibiting compounds useful in modulating, treating, or preventing: anxiolytic disorders; a condition requiring treatment of injured mammalian nerve tissue; a condition amenable to treatment through administration of a neurotrophic factor; a neurological disorder; or obesity; an obesity-related disorder.Type: GrantFiled: July 19, 2007Date of Patent: March 29, 2011Assignee: Janssen Pharmaceutica NVInventors: Charles Q. Huang, Timothy W. Lovenberg, Alejandro Santillán, Jr., Liu Y. Tang, Ronald L. Wolin
-
Publication number: 20110039888Abstract: The present invention relates, generally, to asymmetric ?-functionalization and to asymmetric ?,?-bisfunctionalization of ketones and aldehydes and, in particular, to chiral auxiliaries suitable for use in effecting such functionalizations and to methods of using same.Type: ApplicationFiled: April 21, 2009Publication date: February 17, 2011Inventors: Don M. Coltart, Daniel Lim
-
Patent number: 7888510Abstract: It was an object of the present invention to provide novel compounds that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrome, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man.Type: GrantFiled: July 29, 2004Date of Patent: February 15, 2011Assignee: Laboratorios del Dr. Esteve S.A.Inventors: Antoni Jover Torrens, Josep Mas Prio, Alberto Dordal Zueras, Maria Angeles Fisas Escasany, Helmut-Heinrich Buschmann
-
Publication number: 20110009449Abstract: This invention relates to N-aryl-N-piperidin-4-yl-propionamide derivatives for use as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy, such as for the treatment of pain, and to pharmaceutical compositions comprising the compounds, and to novel compounds.Type: ApplicationFiled: December 18, 2008Publication date: January 13, 2011Inventors: Dan Peters, Birgitte L. Eriksen, Gordon Munro, Elsebet Østergaard Nielsen
-
Publication number: 20100311793Abstract: Preparation methods of mesylate, para-toluenesulfonate, succinate, tartrate, sulphate, nitrate, phosphate, salicylate, fumarate, maleate, gallate, acetylsalicylate, benzenesulphonate, citrate, aspartate, glutaminate, lactate, gluconate, ascorbate, malonate, malate, sorbate, acetate or formate of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine (i.e., Donepezil). Novel polymorphs formed from these salts and their preparation methods. Co-crystals formed from Donepezil hydrochloride and maleic acid, fumaric acid, citric acid, salicylic acid, tartaric acid or succinic acid.Type: ApplicationFiled: March 26, 2010Publication date: December 9, 2010Applicant: TIANJIN HEMAY BIO-TECH CO., LTDInventor: Hesheng Zhang
-
Publication number: 20100292266Abstract: Certain oxazolyl piperidine compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).Type: ApplicationFiled: May 25, 2007Publication date: November 18, 2010Inventors: Richard Apodaca, James Guy Breitenbucher, Alison L. Chambers, Mark Seierstad, Wei Xiao
-
Patent number: 7829560Abstract: 1,4 disubstituted napthylenes, of formula (I), are disclosed. These compounds may be useful in treating cell-proliferative diseases.Type: GrantFiled: July 8, 2005Date of Patent: November 9, 2010Assignee: Arqule, Inc.Inventors: Mark A. Ashwell, Yanbin Liu, Syed Ali, Jason Hill, Woj Wrona
-
Processes for producing 1-benzyl-4-[(5,6-dimethoxy-1indanon)-2-yl]methylpiperidine and hydrochloride
Patent number: 7795438Abstract: Processes for preparing 1-benzyl-4-[(5,6-dimethoxy-lindanon)-2-yl]methylpiperidine (donepezil), which is useful as an intermediate for medicines, and for producing 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride (donepezil hydrochloride), which is useful as a medicine. The process for donepezil hydrochloride production comprises catalytically hydrogenating the compound represented by the structural formula (III) [1-benzyl-4-[(5,6-dimethoxy-lindanon)-2-ylidene]methylpiperidine] with a Raney nickel catalyst under mild conditions and subsequently treating it with hydrochloric acid. Thus, impurities are further diminished. The operations are simple and the process is suitable for industrial production.Type: GrantFiled: April 27, 2005Date of Patent: September 14, 2010Assignee: Eisai R&D Management Co., LtdInventors: Akio Imai, Hiroshi Nishimura -
Patent number: 7772399Abstract: The present invention provides a novel process for the preparation of amorphous form of donepezil hydrochloride.Type: GrantFiled: April 2, 2003Date of Patent: August 10, 2010Assignee: Hetero Drugs LimitedInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Attunuri Narasa Reddy
-
Publication number: 20100143505Abstract: The present invention relates to new indanone inhibitors of acetylcholinesterase, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 9, 2009Publication date: June 10, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar, Manouchehr M. Shahbaz
-
Publication number: 20100113793Abstract: The present invention relates to the preparation of highly pure donepezil of formula I or salt thereof, by hydrogenating indanonylidenyl compound of formula II, using platinum catalysts.Type: ApplicationFiled: March 20, 2007Publication date: May 6, 2010Applicant: IND-SWIFT LABORATORIES LIMITEDInventors: Ashvin Kumar Aggarwal, Chidambaram Vankatesran Srinivasan, Lalit Wadhwa
-
Publication number: 20100113792Abstract: Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R1 represents a hydrogen atom or a methyl group; R2 is a group bound in a p- or m-position relative to a methylene group and represents a chlorine atom bound in a p-position, a bromine atom bound in a p-position, a methyl group bound in a p-position, a chlorine atom bound in a m-position or a bromine atom bound to in a m-position; X represents a methylene or an oxygen atom; and n represents an integer of 1 to 3.Type: ApplicationFiled: February 4, 2009Publication date: May 6, 2010Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Tomohiro Toyoda, Hidefumi Yoshinaga
-
Publication number: 20100105916Abstract: A process for preparing highly pure donepezil, particularly donepezil hydrochloride, is provided comprising hydrogenating compound 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-ylidene]methyl-piperidine or its hydrochloride salt with a noble metal catalyst or a derivative thereof, in the presence of at least one additive, wherein the additive contains at least one heteroatom, e.g., a sulfur, phosphorous, or nitrogen heteroatom.Type: ApplicationFiled: April 23, 2009Publication date: April 29, 2010Applicant: Sterling Biotech LimitedInventors: Raju Mahadev Kharatkar, Sachin Vinayakrao Pande, Nilesh Liladhar Bonde, Godfree Pavalu Fernandes, Sugata Chatterjee
-
Publication number: 20100099703Abstract: The present invention relates to phenylamino-substituted piperidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans or animals.Type: ApplicationFiled: October 31, 2007Publication date: April 22, 2010Inventors: Mónica Garcia-López, Josep Mas-Prio, Antonio Torrens-Jover
-
Publication number: 20100055682Abstract: This application concerns methods and compositions that can be used for detecting the Alzheimer disease in mammals, particularly in humans. It describes in particular serum markers for Alzheimer's disease and the way they are used for diagnostic procedures. It also concerns tools and/or kits that can be used for applying these procedures (reagents, probes, primers, antibodies, chips, cells, etc.) with the preparation thereof and the way to use them. The invention can be used to detect the presence or the progression of Alzheimer illness in mammals, including at early stages of the disease.Type: ApplicationFiled: May 14, 2007Publication date: March 4, 2010Inventors: Fabien Schweighoffer, Laurent Bracco
-
Publication number: 20100048549Abstract: The invention relates to (hetero)arylsulfonylamino based peptidomimetics of formula (I), wherein A, D, E, J, Q1 R1, R2, R3, p and j are defined as disclosed, or a pharmaceutically acceptable salt or ester thereof. Compounds of formula (I) possess high affinity and selectivity for the somatostatin receptor subtypes sst1 and/or sst4 and can be used for the treatment or diagnosis of diseases or conditions wherein sst1 and/or sst4 agonists or antagonists are indicated to be useful.Type: ApplicationFiled: May 16, 2006Publication date: February 25, 2010Inventors: Jussi Tomperi, Harri Salo, Oili Kallatsa, Pia Knuuttila, Päivi Laakso, Iisa Höglund, Anna-Marja Hoffrén, Kurt Kokko, Pauli Saarenketo, Mia Engström, Siegfried Wurster
-
Publication number: 20090325930Abstract: The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; ??(I-1) formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Ra and Rb are the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R? represents 1 to 4 independent hydrogen atoms and the like; and R? represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.Type: ApplicationFiled: August 20, 2009Publication date: December 31, 2009Inventors: Shinichi Hamaoka, Noritaka Kitazawa, Kazumasa Nara, Atsushi Sasaki, Atsushi Kamada, Tadashi Okabe
-
Publication number: 20090298879Abstract: The present invention relates to impurities of donepezil, or a pharmaceutically acceptable salt thereof, which may be produced during synthesis and storage of donepezil, or a pharmaceutically-acceptable salt thereof, and to methods of identifying such impurities. The invention also relates to the use of these impurities in analytical techniques and to product that contain certain low levels of these impurities in particular the following impurities are disclosed: formula (I) and formula (II).Type: ApplicationFiled: May 18, 2007Publication date: December 3, 2009Applicant: PLIVA Hrvatska d.o.o.Inventors: Irena Krizmanic, Lidija Lerman, Zrinka Samardzic, Katarzyna Kaczorowska, Andrzej Manikowski, Barbara Zioro, Ivica Grebenar, Jasna Dogan Koruznjak
-
Publication number: 20090275556Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein R1, X, Z, R2, X1, Ar, n, R3 and R4 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR8 and accordingly are useful for the treatment of a variety of inflammatory and allergic disorders.Type: ApplicationFiled: August 27, 2008Publication date: November 5, 2009Inventors: Mingshi Dai, Bing Guan, Roert A. Bennett, Douglas F. Burdi, Shomir Ghosh, Gang Li, Charles Minor, Tracy J. Jenkins
-
Publication number: 20090253746Abstract: The invention relates to an improved process for preparing 2-(1-benzylpiperidin-4-ylmethyliden)-5,6-dimethoxyin-dan-1-one (a key intermediate in the synthesis of donepezil hydrochloride), crystalline polymorph forms of this key intermediate and their use thereof for producing donepezil hydrochloride. In particular, the invention provides an improved method for producing the intermediate 2-(1-benzylpiperidin-4-ylmethyliden)-5,6-dimethoxyindan-1-one. The process includes reacting 5,6-dimethoxyin-dan-1-one with 1-benzylpiperidine-4-carbaldehyde using potassium hydroxide in an aqueous solvent. The aqueous solvent can be a mixture of an organic solvent and water Where the organic solvent is not miscible with water, the reaction may be performed in the presence of a phase transfer catalyst.Type: ApplicationFiled: November 14, 2006Publication date: October 8, 2009Inventor: Nuria Soldevilla Madrid
-
Patent number: 7598271Abstract: The invention relates to a compound, and pharmaceutically acceptable salts, having the formula I: wherein: R represents an alkyl or alkynyl group having 1-4 carbon atoms, or a phenyl group optionally substituted by C1-4 alkyl, alkylthio, alkoxy, halogen, nitro, acylamino, methylsulfonyl or methylenedioxy, or represents tetrahydronaphthyl, R1 represents hydrogen, trifluoro (C1-4) alkyl, alkyl or alkynyl, X represents hydrogen, alkyl having 1-4 carbon atoms, alkoxy, trifluoroalkyl, hydroxy, halogen, methylthio or aralkoxy, R2 represents: a C1-C10 alkyl group, a phenyl group optionally substituted by one or more of the following groups: a C1-C10 alkyl group, a halogen group, a nitro group, hydroxy group, and/or an alkoxy group.Type: GrantFiled: November 30, 1998Date of Patent: October 6, 2009Assignee: Noven Therapeutics, LLCInventors: Franciscus Bernardus Gemma Benneker, Frans Van Dalen, Jacobus Maria Lemmens, Theodorus Hendricus Antonium Peters, Frantisek Picha
-
Patent number: 7592459Abstract: The present invention provides a crystalline donepezil maleate, which is used as an intermediate in the preparation of donepezil hydrochloride. Also provided are novel processes for producing same in substantially pure form and a process for producing pharmaceutically pure amorphous donepezil hydrochloride therefrom.Type: GrantFiled: September 27, 2005Date of Patent: September 22, 2009Assignee: Chemagis Ltd.Inventors: Oded Arad, Lior Zelikovitch, Mohammed Alnabari, Michael Brand, Irina Gribun, Ada Salman, Meital Shiffer, Moty Shookrun, Orna Kurlat, Moshe Bentolila, Joseph Kaspi
-
Publication number: 20090233966Abstract: Compounds of general formula (I) or a salt thereof in which R1 is preferably an aromatic DNA binding subunit are oxidation-activated prodrugs. The compounds are expected to be converted into an epoxide at the alkene to which R2 is attached by cytochrome P450, in particular CYPIBI, expressed at high levels in tumours. R3 preferably comprises a Nitrogen mustard to provide a prodrug which has 2 alkylating groups. The prodrugs are expected to be activated preferentially in tumour cells.Type: ApplicationFiled: March 16, 2006Publication date: September 17, 2009Applicant: School of Pharmacy, University of LondonInventors: Mark Searcey, Laurence Hylton Patterson, Klaus Pors, Maxwell Casely-Hayford
-
Patent number: 7585977Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and/or uterine leiomyoma/leiomyomata.Type: GrantFiled: April 9, 2008Date of Patent: September 8, 2009Assignee: Eli Lilly and CompanyInventors: Robert Dean Dally, Jeffrey Alan Dodge, Scott Alan Frank, Scott Alan Jones, Timothy Alan Shepherd, Owen Brendan Wallace, Kin Chlu Fong, Conrad Wilson Hummel, George Sal Lewis
-
Patent number: 7576103Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.Type: GrantFiled: December 21, 2005Date of Patent: August 18, 2009Assignee: Roche Palo Alto LLCInventors: Ralph New Harris, III, Nancy Elisabeth Krauss, James M. Kress, David Bruce Repke, Russell Stephen Stabler
-
Patent number: 7572787Abstract: The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.Type: GrantFiled: August 25, 2006Date of Patent: August 11, 2009Assignee: Biovitrum ABInventors: Patrizia Caldirola, Ulf Bremberg, Gary Johansson, Andrew Mott, Annika Jenmalm Jensen, Katarina Beierlien, Markus Thor, Lars Tedenborg