Carbocyclic Ring Containing Patents (Class 546/194)
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Publication number: 20090312304Abstract: 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4-substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed.Type: ApplicationFiled: December 28, 2005Publication date: December 17, 2009Inventors: Werner Breitenstein, Takeru Ehara, Claus Ehrhardt, Philipp Grosche, Yuko Hitomi, Yuki Iwaki, Takanori Kanazawa, Kazuhide Konishi, Juergen K. Maibaum, Keiichi Masuya, Atsuko Nihonyanagi, Nils Ostermann, Masaki Suzuki, Atsushi Toyao, Fumiaki Yokokawa
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Publication number: 20090312308Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.Type: ApplicationFiled: July 24, 2007Publication date: December 17, 2009Applicant: IRM LLCInventors: Dai Cheng, Dong Han, Wenqi Gao, Jiqing Jiang, Shifeng Pan, Yongqin Wan, Qihui Jin
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Publication number: 20090312368Abstract: The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-thrombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.Type: ApplicationFiled: July 2, 2007Publication date: December 17, 2009Applicant: ASTRAZENECA ABInventor: Johan Johansson
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Publication number: 20090306047Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: June 8, 2009Publication date: December 10, 2009Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
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Publication number: 20090306136Abstract: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3, Z, p and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: April 13, 2007Publication date: December 10, 2009Inventors: Akira Matsumura, Hidenori Mikamiyama, Bin Shao, Naoki Tsuno, Jiangchao Yao
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Publication number: 20090306043Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, R?, Ar, m, n, and o are as defined herein. The invention also relates to pharmaceutical compositions containing compounds of formula I and methods for the manufacture of such compounds and compositions. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: June 2, 2009Publication date: December 10, 2009Inventors: Philippe Jablonski, Kenichi Kawasaki, Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer
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Publication number: 20090298878Abstract: The invention relates to oxime compounds of Formula (I) and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X is hydrogen, optionally substituted aryl, optionally substituted heteroaryl or the like; Y is CO, SO2, CR3R4 or the like; Z is optionally substituted lower alkyl, optionally substituted aryl or the like; W is optionally substituted lower alkylene or optionally substituted lower alkenylene, R3 and R4 are each independently hydrogen, lower alkyl or the like; p is 0, 1, or 2 and q is 0, 1 or 2. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: July 12, 2007Publication date: December 3, 2009Inventors: Akira Matsumura, Hidenori Mikamiyama, Naoki Tsuno, Donald J. Kyle, Bin Shao, Jiangchao Yao
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Publication number: 20090299071Abstract: A triazole derivative or pharmaceutically acceptable salt thereof is provided, the triazole derivative being represented by formula (I): wherein * represents an asymmetric carbon and takes R configuration or S configuration; and R1 represents a structure represented by formula (II) or (III): represents single bond or double bond wherein Y represents a hydrogen atom or an oxygen atom; and R2 and R3 each independently represent a hydrogen atom, an alkyl group, an aryl group, an alkoxy group, a formyl group, a carboxyl group, an alkylcarbonyl group, an arylcarbonyl group, an alkoxycarbonyl group, a carbamoyl group, an amino group, an alkylcarbonylamino group, an arylcarbonylamino group, a cyano group, a nitro group or a halogen atom.Type: ApplicationFiled: May 29, 2009Publication date: December 3, 2009Applicant: FUJIFILM FINECHEMICALS CO., LTD.Inventor: Takashi NAGAYAMA
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Patent number: 7625914Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.Type: GrantFiled: December 20, 2005Date of Patent: December 1, 2009Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel
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Patent number: 7625896Abstract: The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of such compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: November 8, 2006Date of Patent: December 1, 2009Assignee: Hoffman-La Roche Inc.Inventors: Lothar Kling, Ulrike Reiff, Manfred Schwaiger, Georg Tiefenthaler, Wolfgang von der Saal, Thomas von Hirschheydt
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Patent number: 7625889Abstract: The present invention relates to a series of substituted bis aryl and heteroaryl compounds of formula (I): Wherein X, Y, Z, A, B, D, Ar, R1 and R2 are as defined herein. The compounds of this invention are selective 5HT2A antagonists, and are therefore, useful in treating a variety of diseases including but not limited to a wide variety of sleep disorders as disclosed and claimed herein.Type: GrantFiled: July 25, 2007Date of Patent: December 1, 2009Assignee: Aventis Pharmaceuticals Inc.Inventors: Paul Robert Eastwood, Hazel Hunt, David Mark Fink, Helen Katherine Smith, Richard Simon Todd
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Patent number: 7622486Abstract: The present invention provides new heterocyclic compounds, particularly substituted pyridines, methods and compositions for making and using these heterocyclic compounds, and methods for treating a variety of diseases and disease states, including atherosclerosis, arthritis, restenosis, diabetic nephropathy, or dyslipidemia, or disease states mediated by the low expression of Perlecan.Type: GrantFiled: September 23, 2005Date of Patent: November 24, 2009Assignee: Reddy US Therapeutics, Inc.Inventors: Manojit Pal, Christopher W. Alexander, Ish Khanna, Javed Iqbal, Ram Pillarisetti, Santanu Maitra, Gayla W. Roberts, Lavanya Sagi, Chintakunta Vamsee Krishna, Jennepalli Sreenu
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Publication number: 20090286766Abstract: Provided is an agent for treating or preventing urinary frequency, urinary urgency and urinary, incontinence which are associated with overactive bladder, a lower urinary tract disease such as interstitial cystitis and chronic prostatitis accompanied by lower urinary tract pain, and various diseases accompanied by pain. A novel azolecarboxamide derivative in which an azole ring such as thioazole or oxazole is bonded to a benzene ring, pyridine ring or pyrimidine ring through carboxamide was confirmed to have a potent trkA receptor-inhibitory activity and found to be an agent for treating or preventing lower urinary tract disease and various diseases accompanied by pain, which is excellent in efficacy and safety, and thus the present invention was accomplished.Type: ApplicationFiled: April 19, 2007Publication date: November 19, 2009Applicant: ASTELLAS PHARMA INC.Inventors: Keizo Sugasawa, Kenichi Kawaguchi, Takaho Matsuzawa, Ryushi Seo, Hironori Harada, Akira Suga, Tomoaki Abe, Hidenori Azami, Shunichiro Matsumoto, Takashi Shin, Masayuki Tanahashi, Toru Watanabe
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Patent number: 7618970Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.Type: GrantFiled: June 27, 2005Date of Patent: November 17, 2009Assignee: Incyte CorporationInventors: Chu-Biao Xue, Changsheng Zheng, Hao Feng, Michael Xia, Joseph Glenn, Ganfeng Cao, Brian W. Metcalf
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Publication number: 20090281307Abstract: Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: ApplicationFiled: August 26, 2008Publication date: November 12, 2009Inventors: Kristen L. Arienti, James G. Breitenbucher, Daniel J. Buzard, James P. Edwards, Michael D. Hack, Alice Lee-Dutra, Haripada Khatuya
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Publication number: 20090281308Abstract: Compounds that interact with the CXCR4 receptor are described. These compounds are useful in treating, for Example, HIV infection and inflammatory conditions such as rheumatoid arthritis, as well as asthma or cancer, and are useful in methods to elevate progenitor and stem cell counts as well as methods to elevate white blood cell counts.Type: ApplicationFiled: May 15, 2009Publication date: November 12, 2009Inventors: Gary J. BRIDGER, Ernest J. MCEACHERN, Renato SKERLJ, Dominique SCHOLS, Ian BAIRD, Al KALLER, Curtis HARWIG, Yongbao ZHU, Gang CHEN, Krystyna SKUPINSKA, Markus METZ
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Publication number: 20090281116Abstract: The invention relates to compounds having the formula (I): Wherein R1, R2, R3, R4, R5, R6, R7 and R9 and A-R9 are as defined herein. Also disclosed are the preparative methods for the compounds of formula (I) and their use in therapy.Type: ApplicationFiled: May 14, 2009Publication date: November 12, 2009Applicant: SANOFI-AVENTISInventors: Francis Barth, Christian Congy, Laurent Hortala, Murielle Rinaldi-Carmona
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Publication number: 20090275748Abstract: Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: ApplicationFiled: August 26, 2008Publication date: November 5, 2009Inventors: James P. Edwards, Michael D. Hack, David E. Kindrachuk, Jennifer D. Venable
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Publication number: 20090275609Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: April 22, 2009Publication date: November 5, 2009Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
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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
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Patent number: 7612094Abstract: Compounds of formula (I) possess unexpectedly high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders. In one embodiment, the invention features a compound of the general formula (I).Type: GrantFiled: April 4, 2003Date of Patent: November 3, 2009Assignee: Biogen Idec MA Inc.Inventors: Wen-Cherng Lee, Lihong Sun, Feng Shan, Claudio Chuaqui, Zhongli Zheng, Russell C. Petter
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Publication number: 20090270611Abstract: Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: ApplicationFiled: August 26, 2008Publication date: October 29, 2009Inventors: James P. Edwards, Michael D. Hack, David E. Kindrachuk, Jennifer D. Venable
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Publication number: 20090270393Abstract: The present invention aims to provide an iminopyridine derivative compound having an ?1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: April 22, 2009Publication date: October 29, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: MASATO YOSHIDA, NOBUKI SAKAUCHI, AYUMU SATO
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Publication number: 20090270613Abstract: Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: ApplicationFiled: August 26, 2008Publication date: October 29, 2009Inventors: James P. Edwards, Michael D. Hack, David E. Kindrachuk, Jennifer D. Venable
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Publication number: 20090270382Abstract: Disclosed are amide, thioamide, urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases.Type: ApplicationFiled: April 17, 2009Publication date: October 29, 2009Inventors: Bhasker R. Aavula, Sampath-Kumar Anandan, Richard D. Gless, JR.
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Publication number: 20090264405Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.Type: ApplicationFiled: October 30, 2006Publication date: October 22, 2009Inventors: Amjad Ali, Julianne A. Hunt, Florida Kallashi, Jennifer Kowalchick, Dooseop Kim, Cameron J. Smith, Peter J. Sinclair, Ramzi F. Sweis, Gayle E. Taylor, Christopher F. Thompson, Liya Chen, Nazia Quraishi
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Publication number: 20090264647Abstract: Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: ApplicationFiled: August 26, 2008Publication date: October 22, 2009Inventors: Kristen L. Arienti, James G. Breitenbucher, Daniel J. Buzard, James P. Edwards, Michael D. Hack, Alice Lee-Dutra
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Publication number: 20090264466Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: ApplicationFiled: January 23, 2009Publication date: October 22, 2009Inventors: Xiangping Qian, Hong Jiang, Bradley P. Morgan, David J. Morgans, JR.
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Publication number: 20090264646Abstract: Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: ApplicationFiled: August 26, 2008Publication date: October 22, 2009Inventors: James P. Edwards, Michael D. Hack, David E. Kindrachuk, Jennifer D. Venable
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Publication number: 20090258868Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: December 10, 2008Publication date: October 15, 2009Inventors: Zhaoning Zhu, Brian A. McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
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Publication number: 20090258851Abstract: The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula II are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: April 6, 2007Publication date: October 15, 2009Inventors: LIN Chu, Bing Li, Anthony K. Ogawa, Hyun O. Ok, Debra L Ondeyka, Minal Patel, Rosemary Sisco, Feroze Ujjainwalla, Jinyou Xu
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Publication number: 20090258900Abstract: Amide derivatives represented by the formula (I): wherein: A is a cycloalkyl group, an aryl group or a heteroaryl group; X is a nitrogen atom or CR17; Y is —NRa—, —(CRbRb?)m-, and the like; m is 0 to 4; and R1 to R17 may be the same or different and each is a hydrogen atom, a halogen atom, a cyano group, a nitro group, a carboxyl group, a formyl group, a hydroxyl group, an ammonium group, an alkyl group optionally having one or more substituents, -ZR18 and the like, Z is —O—, —S(O)p-, —S(O)pO—, —NH—, —NR19-, and the like; or a pharmaceutically acceptable salt thereof, a hydrate thereof, or a solvate thereof may be applied to pharmaceutical use such as anti-inflammatory and analgesic action and the like.Type: ApplicationFiled: June 19, 2009Publication date: October 15, 2009Applicant: AJINOMOTO CO. INCInventors: Tadakiyo Nakagawa, Tamotsu Suzuki, Kaoru Takenaka, Shinichi Fujita, Youji Yamada, Yoichiro Shima, Tatsuya Okuzumi, Toshihiko Yoshimura, Masanao Yoshida, Masahiro Murata
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Patent number: 7601843Abstract: There are provided compounds represented by the following general formula (I): [where R1 is 5-methylpyridin-2-yl, p-tolyl or mesityl, R2 is one of the following general formulas (II)-(IX): (where R3 is C1-C4 alkyl, R4 is H or C1-C4 alkyl, R5 is H, 3-pyridylmethyl or 4-pyridylmethyl, and R6 is 2,4-dihydroxybenzyl, 3-pyridylmethyl or 4-pyridylmethyl), or when R1 is mesityl, R2 is the following formula (X)], and pharmaceutically acceptable salts thereof. The compounds exhibit pruritus-inhibiting action, and are useful for prevention or of itching and pruritus caused by reaction against insect-inflicted wounds, reaction against environmental allergens, skin infections or external parasite infections, or caused to renal dialysis patient.Type: GrantFiled: May 6, 2004Date of Patent: October 13, 2009Assignees: Kyorin Pharmaceutical Co., Ltd, Nisshin Seifun Group Inc.Inventors: Yukiko Muraki, Tomokazu Fujimoto, Takuya Kishimoto
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Publication number: 20090253674Abstract: The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction.Type: ApplicationFiled: May 15, 2009Publication date: October 8, 2009Inventors: Alan Daniel Brown, Andrew Antony Calabrese, David Ellis
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Publication number: 20090253744Abstract: Certain novel N-acylated spiropiperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: ApplicationFiled: September 24, 2007Publication date: October 8, 2009Inventors: Raman K. Bakshi, James P. Dellureficio, Qingmei Hong, Tianying Jian, Jian Liu, Ravi P. Nargund, Zhixiong Ye
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Patent number: 7598392Abstract: The disclosure relates to 2-amido-4-phenylthiazole derivatives of general formula (I) below: in which R1, R2, R3, Y, m, n, and p are as defined in the disclosure; as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic use thereof.Type: GrantFiled: April 18, 2007Date of Patent: October 6, 2009Assignee: sanofi-aventisInventors: Pierre Casellas, Daniel Floutard, Pierre Fraisse, Samir Jegham
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Publication number: 20090247534Abstract: The present invention provides organic compounds of the following structure; A-L1-B-C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: ApplicationFiled: March 28, 2007Publication date: October 1, 2009Inventors: Michael H. Serrano-Wu, Young-Shin Kwak, Wenming Liu
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Publication number: 20090246137Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: March 25, 2009Publication date: October 1, 2009Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
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Patent number: 7595399Abstract: The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.Type: GrantFiled: February 4, 2004Date of Patent: September 29, 2009Assignee: Genentech, Inc.Inventors: David Y. Jackson, Frederick C. Sailes, Daniel P. Sutherlin
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Publication number: 20090239810Abstract: The present invention relates to piperidine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: March 20, 2009Publication date: September 24, 2009Applicant: Forest Laboratories Holdings LimitedInventors: Kumar Sundaresan, P.Bala Koteswara Rao, Bharathiraja Ainan, Hariharasubramanian Ayyamperumal, Girish A R, Srinivas Tatiparthy, Ganesh Prabhu, Hosahalli Subramanya, Alexander Bischoff
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Publication number: 20090239905Abstract: Compounds of formula I: modulate the action of gamma secretase, and hence find use in treatment of Alzheimer's disease and related conditions.Type: ApplicationFiled: March 27, 2007Publication date: September 24, 2009Inventors: Joanne Clare Hannam, Sascha Hartmann, Andrew Madin, Mark Peter Ridgill
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Patent number: 7592373Abstract: Compounds of formula (I) wherein A, B, b, W, X, Y, Z, R1, R2, and R3 have the meanings given in claim 1, pharmaceutical compositions these compounds, and methods of preventing or treating metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia, and diabetes using these compounds.Type: GrantFiled: December 23, 2004Date of Patent: September 22, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Thorsten Lehmann-Lintz, Ralf R. H. Lotz, Philipp Lustenberger, Stephan Georg Mueller, Gerald Juergen Roth, Klaus Rudolf, Marcus Schindler, Dirk Stenkamp, Leo Thomas
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Patent number: 7592358Abstract: Alkyne compounds having MCH-receptor antagonistic activity, which are useful for preparing pharmaceutical compositions for the treatment of metabolic disorders and/or eating disorders, particularly obesity and diabetes.Type: GrantFiled: April 13, 2005Date of Patent: September 22, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Dirk Stenkamp, Stephan Georg Mueller, Philipp Lustenberger, Thorsten Lehmann-Lintz, Gerald Juergen Roth, Klaus Rudolf, Marcus Schindler, Leo Thomas, Ralf Lotz
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Publication number: 20090233965Abstract: The invention provides compounds of formula (I), wherein R1, R2, R3, R4, R5 and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions and their use in therapy (I).Type: ApplicationFiled: April 23, 2007Publication date: September 17, 2009Applicant: ASTRAZENECA ABInventors: Andrew Bailey, Antonio Mete, Garry Pairaudeau, Michael Stocks, Mark Wenlock
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Patent number: 7589087Abstract: Benzoimidazol-2-yl pyridines, pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, including allergy, asthma, autoimmune diseases, and pruritis.Type: GrantFiled: March 30, 2007Date of Patent: September 15, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: James P. Edwards, David E. Kindrachuk, Jennifer D. Venable
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Patent number: 7589204Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).Type: GrantFiled: April 1, 2009Date of Patent: September 15, 2009Assignee: SmithKline Beecham CorporationInventors: Michael Youngman, Wieslaw Mieczyslaw Kazmierski, Hanbiao Yang, Christopher Joseph Aquino
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Publication number: 20090227566Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor. An example of a compound of formula (I) is (a).Type: ApplicationFiled: November 10, 2005Publication date: September 10, 2009Inventors: Ankush Baburao Argade, Theodore Goodson, JR., David Kent Herron, Sajan Joseph, Salvatore Donato Lepore, Angela Lynn Marquart, John Joseph Masters, David Mendel, Leander Merritt, Andrew Michael Ratz, Gerald Floyd Smith, Anne Lousie Tebbe, Michael Robert Wiley, Ying Kwong Yee
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Publication number: 20090227558Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, 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: April 24, 2009Publication date: September 10, 2009Inventors: Patrick Rene Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
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Publication number: 20090227629Abstract: The present invention relates to compounds of formula (I), salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof. wherein R1, R2, R3, R4, R5, R6 and n are as defined in the description.Type: ApplicationFiled: January 8, 2007Publication date: September 10, 2009Inventors: Clive Leslie Branch, Jacqueline Anne Macritchie, Howard Marshall, Roderick Alan Porter, Simone Spada
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Patent number: 7585978Abstract: A process of preparing a stable parenteral solution of a 1,4-dihydropyridine salt, such as nicardipine hydrochloride, in an acidic aqueous medium. The presence of L-arginine in the solution enhances the solubility of the salt, which is poorly soluble in water. An aqueous, injectable isotonic solution at pH about 3.5-3.6 consists essentially of nicardipine hydrochloride, L-arginine, and a sugar alcohol. An improved single pot manufacturing process for obtaining unsymmetrical 1,4-dihydropyridines by using more than one mole equivalent of aldehyde with respect to the other reactants (amino crotonate and acetoacetate ester). The reaction can be conducted in a solvent present at 20 times the amount of any one component. A process for changing one polymorph of nicardipine hydrochloride (Form A) into another (Form B), and a separate process for the reverse (Form B into Form A).Type: GrantFiled: November 28, 2006Date of Patent: September 8, 2009Assignee: Navinta LLCInventors: Christopher N. Jobdevairakkam, Jayaraman Kannappan
