Spiro Patents (Class 544/6)
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Patent number: 12186307Abstract: In various aspects and embodiments the invention provides a method of treating epilepsy in a subject in need thereof, the method comprising providing to the subject an effective amount of an FLNA modulator. In various embodiments, the FLNA modulator is PTI-125 or kartogenin. In various embodiments, the epilepsy is epilepsy associated with focal cortical dysplasia (FCD) type II or tuberous sclerosis complex (TSC).Type: GrantFiled: February 13, 2020Date of Patent: January 7, 2025Assignee: Yale UniversityInventors: Angelique Bordey, Longbo Zhang
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Patent number: 11618237Abstract: This disclosure describes co-extruded multilayer articles including at least one continuous layer and one discontinuous layer, as well as systems and techniques for the manufacture of co-extruded multilayer articles. For example, a co-extruded multilayer article is described that includes a body having a plurality of layers, where a first layer of the plurality of layers is formed from a first material and is continuous along a longitudinal axis of the body, and a second layer of the plurality of layers is formed from a second material and is discontinuously co-extruded along the longitudinal axis.Type: GrantFiled: March 5, 2020Date of Patent: April 4, 2023Assignee: 3M INNOVATIVE PROPERTIES COMPANYInventors: Robert M. Biegler, Mark A. Hoisington, Craig R. Hoff, Anton F. Jachim, Jeffrey M. Maki, Derek W. Patzman, Thomas J. Blong, Jay M. Jennen, Erik A. Aho, David V. Mahoney
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Patent number: 11542290Abstract: The present invention provides phenothiazine compounds, processes for their preparation, pharmaceutical compositions comprising the compounds, and the use of the compounds or the compositions in the treatment of various diseases or conditions, for example ribosomal disorders and ribosomopathies, e.g. Diamond Blackfan anemia (DBA).Type: GrantFiled: April 5, 2019Date of Patent: January 3, 2023Assignee: CAMP4 THERAPEUTICS CORPORATIONInventors: David A. Bumcrot, Alfica Sehgal, Donald L. Hertzog
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Patent number: 9611264Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, wherein the variables R1, R2 and R3 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: GrantFiled: September 22, 2016Date of Patent: April 4, 2017Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Lei Zhang, Brian Thomas O'Neill, Patrick Robert Verhoest, Romelia del Carmen Salomon Ferrer
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Patent number: 9580396Abstract: In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): (structurally represented) or tautomers thereof, and pharmaceutically acceptable salts of said compounds, wherein R1, R2, R3, X, Y, s, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.Type: GrantFiled: December 16, 2013Date of Patent: February 28, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Jared N. Cumming, Jack D. Scott, Jr., Andrew W. Stamford, Ulrich Iserloh, Santhosh Francis Neelamkavil, Pengcheng Patrick Shao, Jonathan E. Wilson
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Patent number: 9489013Abstract: In its many embodiments, the present invention provides certain C2-ring-substituted thiadiazine compounds, including compounds Formula (I): (structure represented) or tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R4, ring A, RA, m, -L1-, RL, and ring C are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.Type: GrantFiled: December 16, 2013Date of Patent: November 8, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Jared N. Cumming, David Earl Kaelin, Jr., Jack D. Scott, Andrew W. Stamford, Ulrich Iserloh
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Patent number: 9233982Abstract: The present invention provide compounds of Formula (I) used as BACE inhibitors for the treatment of neurodegenerative diseases.Type: GrantFiled: May 10, 2013Date of Patent: January 12, 2016Assignee: Ares Trading S.A.Inventors: Anna Quattropani, Dominique Swinnen
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Publication number: 20150141413Abstract: The present invention provides a compound of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.Type: ApplicationFiled: May 21, 2013Publication date: May 21, 2015Inventors: Hans Hilpert, Thomas Woltering
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Publication number: 20150111882Abstract: The present invention provide compounds of Formula (I) used as BACE inhibitors for the treatment of neurodegenerative diseases.Type: ApplicationFiled: May 10, 2013Publication date: April 23, 2015Applicant: Ares Trading S.A.Inventors: Anna Quattropani, Dominique Swinnen
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Publication number: 20150087826Abstract: Compounds are provided having a structure according to Formula (I): wherein A1, A2, A3, Y, R1, R2, R3, R4, R5, R6, m, n and p are defined herein. Further provided are pharmaceutical compositions including the compounds provided and methods of making and using the compounds and compositions as provided, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.Type: ApplicationFiled: December 1, 2014Publication date: March 26, 2015Inventors: Ying-Zi Xu, Dean R. Artis, Simeon Bowers, Roy K. Hom, Hing L. Sham, Shendong Yuan
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Publication number: 20150087825Abstract: Compounds are provided having a structure according to Formula (I): wherein A1, A2, A3, Y, R1, R2, R3, R4, R5, R6, m, n and p are defined herein. Further provided are pharmaceutical compositions including the compounds provided and methods of making and using the compounds and compositions as provided, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.Type: ApplicationFiled: December 1, 2014Publication date: March 26, 2015Inventors: Ying-Zi Xu, Dean R. Artis, Simeon Bowers, Roy K. Hom, Hing L. Sham, Shendong Yuan
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Publication number: 20150073137Abstract: Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.Type: ApplicationFiled: November 13, 2014Publication date: March 12, 2015Inventors: Masakuni KORI, Toshihiro IMAEDA, Shinji NAKAMURA, Masashi TOYOFUKU, Eiji HONDA, Yasutomi ASANO, Osamu UJIKAWA, Michiyo MOCHIZUKI
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Publication number: 20140303152Abstract: Benzothiazinethione derivatives of formula (I), their preparative methods and uses are provided. Benzothiazinethione derivatives of the invention have significant effect of inhibiting Mycobacterium tuberculosis.Type: ApplicationFiled: June 15, 2011Publication date: October 9, 2014Applicant: SICHUAN UNIVERSITYInventors: Luoting Yu, Yuquan Wei
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Publication number: 20140296226Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, L, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: September 21, 2012Publication date: October 2, 2014Inventors: Ryan White, Yuan Cheng, Ana Elena Minatti, Bryant Yang, Xiao Mei Zheng, Patricia Lopez, Jason B. Human, Oleg Epstein, Ted Judd, Kelvin Sham, Qiufen Xue
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Publication number: 20140225040Abstract: The present invention relates to compounds for use in electronic devices, preferably organic electroluminescent devices. The invention furthermore relates to processes for the preparation of these compounds and to electronic devices comprising these compounds, preferably in a function as matrix materials and/or as electron-transport materials.Type: ApplicationFiled: July 3, 2012Publication date: August 14, 2014Applicant: Merck Patent GmbH Patents & Scientific InformationInventors: Amir Hossain Parham, Christof Pflumm, Anja Jatsch
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Publication number: 20140200213Abstract: In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein each of the variables shown in the formula are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.Type: ApplicationFiled: August 21, 2012Publication date: July 17, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Wen-Lian Wu, Duane A. Burnett, Andrew W. Stamford, Jared N. Cumming, Theodros Asberom, Chad Bennett, Thavalakulamgara K. Sasiskumar, Jack D. Scott
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Publication number: 20140148448Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: January 30, 2014Publication date: May 29, 2014Applicant: Janssen Pharmaceutica NVInventors: Carl R. ILLIG, Shelley K. BALLENTINE, Jinsheng CHEN, Renee Louise DESJARLAIS, Sanath K. MEEGALLA, Mark WALL, Kenneth WILSON
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Publication number: 20140128371Abstract: The present invention relates to compounds of Formula (I): to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.Type: ApplicationFiled: January 13, 2014Publication date: May 8, 2014Applicant: ASTRAZENECA ABInventors: Kevin BARVIAN, Gregory Steven BASARAB, Madhusudhan Reddy GOWRAVARAM, Sheila Irene HAUCK, Fei ZHOU
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Publication number: 20140107109Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.Type: ApplicationFiled: December 18, 2013Publication date: April 17, 2014Inventors: Richard T. LEWIS, Jennifer R. ALLEN, Yuan CHENG, Deborah CHOQUETTE, Oleg EPSTEIN, Angel GUZMAN-PEREZ, Paul E. HARRINGTON, Zihao HUA, Randall W. HUNGATE, Jason Brooks HUMAN, Ted JUDD, Qingyian LIU, Patricia LOPEZ, Ana Elena MINATTI, Philip OLIVIERI, Karina ROMERO, Shannon RUMFELT, Robert M. RZASA, Laurie SCHENKEL, John STELLWAGEN, Ryan WHITE, Qiufen XUE, Xiao ZHENG, Wenge ZHONG
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Publication number: 20140045828Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: June 27, 2013Publication date: February 13, 2014Inventors: Jian CHEN, Wenge ZHONG, Bryant YANG, Wenyuan QIAN, Patricia LOPEZ, Ryan WHITE, Matthew WEISS, Tedd JUDD, Timothy POWERS, Yuan CHENG, Thomas DINEEN, Oleg EPSTEIN, Jason HUMAN, Jonathan D. LOW, Isaac E. MARX, Ana Elena MINATTI, Michele POTASHMAN, Nick A. PARAS, Qingyian LIU
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Patent number: 8598340Abstract: The present invention can provide new spirooxazine radical derivatives of the following general formula (1) which have chromic property enabling the distinction between the radical species and the cation species on the basis of absorption wavelength:Type: GrantFiled: November 2, 2012Date of Patent: December 3, 2013Assignee: NEC CorporationInventor: Atsumasa Sawada
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Publication number: 20130274212Abstract: The present invention relates to sesterterpene compounds, to the precursors thereof that are hydrolysable in a living body, or to the pharmaceutically acceptable salts thereof, and also relates to the prevention and treatment efficacy of the sesterterpene compounds with respect to non-insulin dependent diabetes mellitus, diabetic complications (renal failure and foot ulcers caused by diabetes), alcoholic, non-alcoholic, and viral fatty liver diseases, obesity, hyperlipidemia, atherosclerosis, cardiovascular diseases such as atherosclerotic stroke, and cerebropathies (Parkinsonism, schizophrenia and Alzheimer's disease). In addition, the present invention relates to compositions for functional foods, functional beverages, functional cosmetics, and functional feed.Type: ApplicationFiled: September 7, 2011Publication date: October 17, 2013Applicant: SNU R&DB FOUNDATIONInventors: Heon Joong Kang, Dong Hwan Won, In Ho Yang, Eun Oh Kim, Jung Ah Kim, Awadut Gajendra Giri, Venkat Reddy Mallepally
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Publication number: 20130237533Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.Type: ApplicationFiled: April 24, 2013Publication date: September 12, 2013Applicant: G1 Therapeutics, Inc.Inventors: Francis X. Tavares, Jay C. Strum
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Publication number: 20130237534Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.Type: ApplicationFiled: April 24, 2013Publication date: September 12, 2013Applicant: G1 Therapeutics, Inc.Inventors: Francis X. Tavares, Jay C. Strum
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Patent number: 8501733Abstract: A compound represented by the general formula (I): or a pharmaceutically acceptable salt thereof, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.Type: GrantFiled: July 24, 2009Date of Patent: August 6, 2013Assignee: Eisai R&D Management Co., Ltd.Inventors: Takafumi Motoki, Toshihiko Kaneko, Noboru Yamamoto, Afzal Khan
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Publication number: 20130190291Abstract: Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.Type: ApplicationFiled: August 9, 2011Publication date: July 25, 2013Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masakuni Kori, Toshihiro Imaeda, Shinji Nakamura, Masashi Toyofuku, Eiji Honda, Yasutomi Asano, Osamu Ujikawa, Michiyo Mochizuki
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Patent number: 8450308Abstract: The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.Type: GrantFiled: August 14, 2009Date of Patent: May 28, 2013Assignee: Vitae Pharmaceuticals, Inc.Inventors: Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
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Publication number: 20130072678Abstract: The present invention can provide new spirooxazine radical derivatives of the following general formula (1) which have chromic property enabling the distinction between the radical species and the cation species on the basis of absorption wavelength:Type: ApplicationFiled: November 2, 2012Publication date: March 21, 2013Applicant: NEC CORPORATIONInventor: NEC CORPORATION
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Patent number: 8389511Abstract: The present invention relates to a compound of the following formula (I) or a pharmaceutically acceptable salt thereof, being useful as a renin inhibitor. [wherein R1a is halogen, etc.; R1m is H, etc.; G1 is —N(R1b)—, etc.; G2 is —CO—, etc.; G3 is —C(R1c)(R1d)—, etc.; G4 is oxygen, etc.; R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are independently the same or different, H, etc.; R3 is H, optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are independently the same or different, and a group: -A-B (said A is single bond, etc., and said B is H, etc.), etc.; and n is 1, etc.Type: GrantFiled: December 19, 2008Date of Patent: March 5, 2013Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Hiroyuki Nakahira, Yohei Ikuma, Nobuhisa Fukuda, Kozo Yoshida, Hidenori Kimura, Satoshi Suetsugu, Akira Fusano, Kiyoto Sawamura, Junya Ikeda, Yoshio Nakai
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Publication number: 20130018045Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, A, B, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.Type: ApplicationFiled: July 12, 2012Publication date: January 17, 2013Applicant: ABBOTT LABORATORIESInventors: Keith W. Woods, Chunqui Lai, Thomas D. Penning, Julie M. Miyashiro
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Publication number: 20120329773Abstract: This invention relates to bicyclic ring system substituted amide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: ApplicationFiled: December 13, 2011Publication date: December 27, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Riccardo GIOVANNINI, Dieter HAMPRECHT, Barbara KISTLER, Iain LINGARD
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Patent number: 8329896Abstract: The present invention can provide new spirooxazine radical derivatives of the following general formula (1) which have chromic property enabling the distinction between the radical species and the cation species on the basis of absorption wavelength:Type: GrantFiled: December 20, 2007Date of Patent: December 11, 2012Assignee: NEC CorporationInventor: Atsumasa Sawada
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Publication number: 20120270838Abstract: The present invention relates to a compound represented by the following formula (1): wherein W, X, Y, R1, R2, R33, R34, m and n are as defined in the claims, or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: April 27, 2010Publication date: October 25, 2012Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Toru Esaki, Yoshikazu Nishimura, Yoshiaki Isshiki, Naoki Okamoto, Yoshiyuki Furuta, Akemi Mizutani, Masateru Ohta, Wayne Wen Lai, Tomoya Kotake
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Publication number: 20120245026Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are useful as pesticides.Type: ApplicationFiled: November 30, 2010Publication date: September 27, 2012Applicant: Syngenta Crop Protection LLCInventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
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Publication number: 20120157448Abstract: The invention provides novel tricyclic compounds of Formula I? that inhibit ?-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.Type: ApplicationFiled: November 22, 2011Publication date: June 21, 2012Inventors: Adam Cook, Indrani W. Gunawardana, Kevin W. Hunt, Nicholas C. Kallan, Andrew T. Metcalf, Brad Newhouse, Tony P. Tang, Allen A. Thomas, Michael Siu, Malcolm Huestis, Matthew Volgraf
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Publication number: 20120101271Abstract: Selective intramolecular C—H amination via metalloradical activation of azides: synthesis of 1,3-diamines under neutral and nonoxidative conditions. One aspect of the present invention is the synthesis of 1,3-diamines by intramolecular C—H amination of sulfamoyl azides. More specifically, sulfamoyl azides may be selectively aminated via metalloradical activation of azides, preferably with Co(II) porphyrins. In a particularly preferred embodiment, the Co(II) porphyrin is a D2h-symmetric porphyrin.Type: ApplicationFiled: October 21, 2011Publication date: April 26, 2012Inventors: X. Peter Zhang, Hongjian Lu
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Publication number: 20120083488Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).Type: ApplicationFiled: June 9, 2010Publication date: April 5, 2012Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
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Publication number: 20120077799Abstract: Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.Type: ApplicationFiled: August 9, 2011Publication date: March 29, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masakuni KORI, Toshihiro IMAEDA, Shinji NAKAMURA, Masashi TOYOFUKU, Eiji HONDA, Yasutomi ASANO, Osamu UJIKAWA, Michiyo MOCHIZUKI
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Publication number: 20120065195Abstract: The invention provides novel spirotetrahydronaphthalene compounds of Formula ? that inhibit ?-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.Type: ApplicationFiled: March 31, 2011Publication date: March 15, 2012Inventors: Christopher T. Clark, Adam Cook, Indrani W. Gunawardana, Kevin W. Hunt, Nicholas C. Kallan, Michael Siu, Allen A. Thomas, Matthew Volgraf
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Publication number: 20120041194Abstract: The present invention provides nitrogen and sulfur-containing heterocycle compounds to be used as scaffolds and, in particular, nitrogen and sulfur-containing heterocycle compounds having a thiomorpholine core. The compounds herein described may be useful in treating diseases such as diabetes, obesity, cancer, cardiovascular, Alzheimer's, inflammatory, antidepressant, rheumatoid arthritis, multiple sclerosis, allergic rhinitis, asthma as well as viral and bacterial infections. The compounds herein described may also be useful in treating CNS disorders such as but not limited to Schizophrenia, Alzheimer's disease (AD).Type: ApplicationFiled: August 29, 2009Publication date: February 16, 2012Applicant: Triad Multitech Pharmaceuticals, Inc.Inventor: Murty N. Armilli
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Publication number: 20120022249Abstract: A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt, or a solvate thereof.Type: ApplicationFiled: September 23, 2011Publication date: January 26, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Naotake KOBAYASHI, Kazuo UEDA, Naohiro ITOH, Shinji SUZUKI, Gaku SAKAGUCHI, Akira KATO, Akira YUKIMASA, Akihiro HORI, Yuji KORIYAMA, Hidekazu HARAGUCHI, Ken YASUI, Yasuhiko KANDA
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Publication number: 20120016116Abstract: A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt, or a solvate thereof.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Naotake KOBAYASHI, Kazuo UEDA, Naohiro ITOH, Shinji SUZUKI, Gaku SAKAGUCHI, Akira KATO, Akira YUKIMASA, Akihiro HORI, Yuji KORIYAMA, Hidekazu HARAGUCHI, Ken YASUI, Yasuhiko KANDA
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Patent number: 8071586Abstract: The invention is concerned with novel heterocyclyl compounds of formula (I) wherein A, X, Y1, Y2, Y3, R3, R4, R5, R6, R7, R8, R9, R10, m, n and p are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.Type: GrantFiled: July 8, 2009Date of Patent: December 6, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
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Patent number: 8067620Abstract: A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites. The compounds of the invention unexpectedly provide a single-dose cure for malaria, as well as prophylactic activity against the same. The compounds are also active against schistosomiasis and cancer.Type: GrantFiled: October 31, 2007Date of Patent: November 29, 2011Assignee: Medicines for Malaria Venture MMVInventors: Jonathan L. Vennerstrom, Yuxiang Dong, Susan A. Charman, Sergio Wittlin, Jacques Chollet, Darren J. Creek, Xiaofang Wang, Kamaraj Spiraghavan, Lin Zhou, Hugues Matile, William N. Charman
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Publication number: 20110251186Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: March 14, 2011Publication date: October 13, 2011Applicant: Amgen Inc.Inventors: Jian J. CHEN, Wenge ZHONG, Bryant YANG, Wenyuan QIAN, Patricia LOPEZ, Ryan WHITE, Matthew WEISS, Ted JUDD, Timothy POWERS, Yuan CHENG, Thomas DINEEN, Oleg EPSTEIN, Jonathan LOW, Isaac MARX, Ana Elena MINATTI, Michele POTASHMAN, Nick A. PARAS
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Publication number: 20110224155Abstract: The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.Type: ApplicationFiled: June 3, 2008Publication date: September 15, 2011Applicant: SENOMYX INC.Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Xiaodong Li, Feng Zhang, Guy Servant, Qing Chen, Vincent Darmohusodo, Richard Fine, Joseph R. Fotsing, Jeffrey Robert Hammaker, Xinshan Kang, Rachel D.A. Kimmich, Boris Klebansky, Haitian Liu, Goran Petrovic, Marketa Rinnova, Sara Adamski-Werner, Jeffrey Yamamoto, Hong Zhang, Albert Zlotnik, Mark Zoller, Karen Zoller
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Publication number: 20110218192Abstract: The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.Type: ApplicationFiled: August 14, 2009Publication date: September 8, 2011Applicant: VITAE PHARMACEUTICALS, INC.Inventors: Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
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Publication number: 20110195960Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: April 6, 2011Publication date: August 11, 2011Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
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Publication number: 20110190278Abstract: The present invention relates to a compound of the following formula (I) or a pharmaceutically acceptable salt thereof, being useful as a renin inhibitor. [wherein R1a is halogen, etc.; R1m is H, etc.; G1 is —N(R1b)—, etc.; G2 is —CO—, etc.; G3 is —C(R1c)(R1d)—, etc.; G4 is oxygen, etc.; R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are independently the same or different, H, etc.; R3 is H, optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are independently the same or different, and a group: -A-B (said A is single bond, etc., and said B is H, etc.), etc.; and n is 1, etc.Type: ApplicationFiled: December 19, 2008Publication date: August 4, 2011Inventors: Hiroyuki Nakahira, Yohei Ikuma, Nobuhisa Fukuda, Kozo Yoshida, Hidenori Kimura, Satoshi Suetsugu, Akira Fusano, Kiyoto Sawamura, Junya Ikeda, Yoshio Nakai
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Publication number: 20110160193Abstract: The present invention relates to novel benzothiazinone derivatives and their use as antibacterial agents in infectious diseases of mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and leprosy caused by mycobacteria. The present invention aims at the generation of new compounds with activity against mycobacteria as potential new tuberculosis drugs to overcome problems concerning resistance and drug intolerance. The solution of the present invention is a compound of formula I wherein R1 to R6 are as defined in the specification.Type: ApplicationFiled: December 22, 2010Publication date: June 30, 2011Applicant: Leibniz Institute for Natural Product Research and Infection Biology E.V.Inventors: A. Vadim Makarov, Stewart T. Cole, Ute Möllmann