Piperidine Ring Patents (Class 544/129)
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Publication number: 20100022539Abstract: Certain isoxazole compounds are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.Type: ApplicationFiled: September 15, 2009Publication date: January 28, 2010Inventors: Nicholas I. Carruthers, Chandravadan R. Shah, Devin M. Swanson
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Patent number: 7645755Abstract: The invention is directed to compounds of Formula I: wherein A, X, 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: GrantFiled: April 20, 2006Date of Patent: January 12, 2010Assignee: Janssen Pharmaceutical N.V.Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Sanath K. Meegalla, M. Jonathan Rudolph, Mark J. Wall, Kenneth J. Wilson, Renee L. Desjarlais, Carl L. Manthey, Christopher Flores, Christopher J. Molloy
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SELECTED CGRP ANTAGONISTS, PROCESSES FOR PREPARING THEM AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS
Publication number: 20100004228Abstract: The present invention relates to the CGRP antagonists of general formula I wherein R1, R2, R3 and R4 are as defined in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I wherein one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, their use and processes for preparing them.Type: ApplicationFiled: June 17, 2009Publication date: January 7, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan Georg MUELLER, Klaus RUDOLF, Philipp LUSTENBERGER, Gerhard SCHAENZLE, Marco SANTAGOSTINO, Dirk STENKAMP, Kirsten ARNDT, Henri DOODS -
Publication number: 20090318447Abstract: The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R1, R2, R3, R4, R5, R6, R7, n, Het and Ar are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.Type: ApplicationFiled: April 15, 2005Publication date: December 24, 2009Inventors: David John Nash, Roderick Alan Porter
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Publication number: 20090318690Abstract: Disclosed is a compound represented by the general formula (I) or a salt thereof: wherein any one of R1, R2 and R3 represents a group represented by the formula: —(CH2)m-NR11R12 (wherein m is 1 or 2; and R11 and R12 independently represent a hydrogen atom or a C1-6 alkyl group or may, together with a nitrogen atom to which R11 and R12 are bound, form a 4- or 5-membered cyclic group); the remaining two or R1, R2 and R3 independently represent a group represented by the formula: —(O)n-R21 (wherein n is 0 or 1; and R21 represents a hydrogen atom, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or the like); and R4 represents a C1-6 alkyl group which may have a substituent or the like.Type: ApplicationFiled: April 27, 2007Publication date: December 24, 2009Applicant: Eisai R&D Management Co., Ltd.Inventors: Atsushi Sasaki, Kohshi Ueno, Yuichi Suzuki, Shinichi Hamaoka, Daisuke Shimmyo, Yoshinori Takahashi, Toshiki Kurokawa, Yuji Kazuta, Hiroo Ogura, Tatsuto Fukushima
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Publication number: 20090306059Abstract: A compound having the general formula (I), pharmacologically acceptable salts thereof or prodrugs thereof: [wherein R1 represents a hydrogen atom, a C1-C6 alkyl group which may be substituted, a C3-C6 cycloalkyl group which may be substituted, a C1-C6 alkoxy group which may be substituted or a C6-C10 aryl group which may be substituted; R2 represents a hydrogen atom, a halogen atom, a carboxy group, a C2-C7 alkoxycarbonyl group, a carbamoyl group, a cyano group, a C1-C6 alkyl group, a halogeno C1-C6 alkyl group, a C1-C6 alkyl group substituted by a heteroaryl group, a C1-C6 alkoxy group, a halogeno C1-C6 alkoxy group, a hydroxy C1-C6 alkyl group, a C2-C12 alkoxyalkyl group, a formyl group, a C2-C7 alkanoyl group, a C4-C7 cycloalkylcarbonyl group, a C2-C7 alkylcarbamoyl group, a di(C1-C6 alkyl)carbamoyl group, a group of formula R4—CO—CR5R6—(CH2)m—, a group of formula R7—CO—(CH2)l—N(R8)— or a sulfamoyl C1-C6 alkyl group; R3 represents a substituted C1-C6 alkyl group, a heterocyclyl group or a heterocyclType: ApplicationFiled: May 26, 2006Publication date: December 10, 2009Inventors: Tomio Kimura, Naoki Tanaka, Hiroyuki Kobayashi, Atsuhiro Sugidachi
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Patent number: 7618961Abstract: The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: GrantFiled: May 22, 2001Date of Patent: November 17, 2009Assignee: Biovitrum ABInventors: Tjeerd Barf, Rikard Emond, Guido Kurz, Jerk Vallgårda, Marianne Nilsson
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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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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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Patent number: 7608617Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: June 22, 2007Date of Patent: October 27, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Silvia Gatti McArthur, Cornelia Hertel, Matthias Heinrich Nettekoven, Jean-Marc Plancher, Susanne Raab, Olivier Roche, Rosa Maria Rodriguez-Sarmiento, Franz Schuler
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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: 20090227585Abstract: The present invention is directed to substituted N-heterocycle derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: ApplicationFiled: May 18, 2009Publication date: September 10, 2009Applicant: WyethInventors: Paige Erin Mahaney, Lori Krim Gavrin, Douglas John Jenkins
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Patent number: 7585858Abstract: Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: May 26, 2005Date of Patent: September 8, 2009Assignee: Abbott LaboratoriesInventors: Steven W. Elmore, Milan Bruncko, Cheol-Min Park
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Publication number: 20090215772Abstract: The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbylamino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.Type: ApplicationFiled: April 13, 2006Publication date: August 27, 2009Applicant: Astex Therapeutics LimitedInventors: Gianni Chessari, Miles Stuart Congreve, Eva Figueroa Navarro, Martyn Frederickson, Christopher Murray, Alison Jo-Anne Woolford, Maria Grazia Carr, Michael Alistair O'Brien, Andrew James Woodhead, Robert Downham, Theresa Rachel Phillips
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Publication number: 20090216013Abstract: This invention relates to compounds of formula (I) which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.Type: ApplicationFiled: August 8, 2008Publication date: August 27, 2009Applicant: Novo Nordisk A/SInventors: Anthony Murray, Jesper Lau, Lone Jeppesen, Per Vedso, Michael Ankersen, Jane Marie Lundbeck, Marit Kristiansen, Maria Carmen Valcarce-Lopez, Dharma Rao Polisetti, Govindan Subramanian, Robert Carl Andrews, Daniel P. Christen, Jeremy T. Cooper, Kalpathy Chidambareswara Santhosh
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Patent number: 7576083Abstract: The present invention is directed to morpholinyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.Type: GrantFiled: April 29, 2005Date of Patent: August 18, 2009Assignee: Merck & Co., Inc.Inventors: Craig W. Lindsley, Scott E. Wolkenberg, Zhijian Zhao
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Publication number: 20090203695Abstract: The present application relates to new compounds of formula (I), to pharmaceutical compositions comprising the compounds, to processes for their preparation, and to the use of the compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.Type: ApplicationFiled: December 5, 2008Publication date: August 13, 2009Applicant: Biovitrum ABInventors: Michael Higginbottom, Viet-Anh Anne Horgan (nee Nguyen), Iain Simpson
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Publication number: 20090203696Abstract: Disclosed are compounds according to formula (I): wherein A, Q, X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. The disclosure also relates to pharmaceutical compositions containing a compound of formula (I), to processes for preparing the compounds of formula (I), and to methods of using the compounds of formula (I).Type: ApplicationFiled: December 15, 2008Publication date: August 13, 2009Applicant: SANOFI-AVENTISInventors: Jozsef Zsolt BOCSKEI, Gary MCCORT, Hans MATTER, Henning STEINHAGEN, Berangere THIERS
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Publication number: 20090181949Abstract: The present invention relates to a group of novel 1H-imidazole derivatives, to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component. These 1H-imidazole derivatives are potent cannabinoid-CB1 receptor agonists, partial agonists or antagonists, useful for the treatment of psychiatric and neurological disorders, as well as and other diseases involving cannabinoid neurotransmission. The compounds have the general formula (I) wherein R and R1-R4 have the meanings given in the specification.Type: ApplicationFiled: September 2, 2008Publication date: July 16, 2009Inventors: Cornelis G. KRUSE, Josephus H.M. LANGE, Arnoldus H.J. HERREMANS, Herman H. VAN STUIVENBERG
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Publication number: 20090181948Abstract: The present invention provides a diamine derivative or the like represented by the general formula (I): {wherein Q represents an oxygen atom or the like, RG represents a hydrogen atom or the like, RI represents (wherein p and r may be the same or different, and each represents 0 or the like, RA represents a hydrogen atom or the like, and RB and RC may be the same or different, and each represents a hydrogen atom or the like), RH represents a hydrogen atom or the like, and RJ represents: (wherein q and s may be the same or different, and each represents 0 or the like, RD represents a hydrogen atom or the like, and RE and RF may be the same or different, and each represents a hydrogen atom or the like) or the like}, etc.Type: ApplicationFiled: January 31, 2006Publication date: July 16, 2009Applicant: KYOWA HAKKO KOGYO CO., LTD.Inventors: Setsuya Sasho, Takashi Seishi, Eri Atsumi, Mariko Osakada, Ryo Hirose, Shinichiro Toki, Katsuyoshi Tsukii, Shiro Shirakura
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Patent number: 7560546Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.Type: GrantFiled: August 5, 2003Date of Patent: July 14, 2009Assignee: Merck & Co., Inc.Inventors: Christopher J. Dinsmore, Douglas C. Beshore, Jeffrey M. Bergman, Craig W. Lindsley
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Patent number: 7550486Abstract: The present application describes modulators of chemokine receptor activity of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis, including methods of preparing and intermediates thereof.Type: GrantFiled: January 11, 2008Date of Patent: June 23, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Soo S. Ko, George V. Delucca
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Publication number: 20090156465Abstract: The present invention relates to ?-amino acid derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.Type: ApplicationFiled: December 12, 2006Publication date: June 18, 2009Inventors: Jitendra A. Sattigeri, Shahadat Ahmed, Murugaiah M.S. Andappan, Sachin Sethi, Lalima Sharma, Chanchal Kumar Pal, Sachin Ramesh Kandalkar, Dipak C. Mahajan, Kaushal Kishore, Sumati Bhatia, Anil G. Gadhave, Vinay S. Bansal, Joseph Alexanand Davis
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Publication number: 20090156572Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B is an aromatic ring optionally having substituent(s), ring C is a cyclic group optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group, a heterocyclic group optionally having substituent(s) or an amino group optionally having substituent(s), R2 is an optionally halogenated C1-6 alkyl group, m and n are each an integer of 0 to 5, m+n is an integer of 2 to 5, and is a single bond or a double bond, or a salt thereof and the like. Since the compound has a superior tachykinin receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of various diseases such as lower urinary tract diseases, gastrointestinal diseases, central nervous system diseases and the like.Type: ApplicationFiled: December 2, 2008Publication date: June 18, 2009Inventors: Yoshinori Ikeura, Junya Shirai, Hideyuki Sugiyama, Yuji Nishikimi, Taku Kamei, Nobuki Sakauchi
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Publication number: 20090143372Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: October 31, 2007Publication date: June 4, 2009Inventors: Jianghe Deng, Jeffrey K. Kerns, Qi Jin, Guoliang Lin, Xichen Lin, Michael Lindenmuth, Christopher Neipp, Hong Nie, Sonia M. Thomas, Katherine L. Widdowson
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Patent number: 7538222Abstract: Disclosed herein are compounds of Formula I, or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof. Also disclosed are methods of inhibiting an activity of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Disclosed are also methods of inhibiting an activation of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Furthermore, methods of treating psychotic disease using a compound of Formula I are disclosed.Type: GrantFiled: December 12, 2005Date of Patent: May 26, 2009Assignee: ACADIA Pharmaceuticals, Inc.Inventors: Carl-Magnus Andersson, Nathalie Schlienger, Alma Fejzic, Eva Louise Hansen, Jan Pawlas
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Publication number: 20090131403Abstract: The compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof specifically binds CCR5, so it is useful for preventing and/or treating CCR5-related diseases, for example, various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis, etc.), immunological diseases (autoimmune diseases, rejection in organ transplantation, immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (infection with human immunodeficiency virus, acquired immunodeficiency syndrome, etc.), allergic diseases (atopic dermatitis, urticaria, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis, etc.), ischemic reperfusion injury, acute respiratory distress syndrome, shock accompanying bacterial infection diabetes cancer metastasis and so on.Type: ApplicationFiled: March 9, 2007Publication date: May 21, 2009Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Shinya Kusuda, Toshihiko Nishiyama, Kazuya Hashimura, Junya Ueda, Shiro Shibayama
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Publication number: 20090111983Abstract: Cycloalkylcarbonylamino acid derivatives, which are raw material intermediates of a novel cycloalkane carboxamide derivative that selectively inhibits cathepsin K, and a production process thereof, are provided. A cycloalkylcarbonylamino acid derivative represented by the following general formula (I), or a pharmaceutically acceptable salt thereof: (wherein, R1 and R2 represent alkyl groups, alkenyl groups, alkynyl groups, aromatic hydrocarbon groups, heterocyclic groups or the like, and ring A represents a cyclic alkylidene group having 5, 6 or 7 carbon atoms).Type: ApplicationFiled: July 10, 2007Publication date: April 30, 2009Applicant: SEIKAGAKU CORPORATIONInventors: Nobuo Kobayashi, Tsuneo Koji, Hisatomo Kunii
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Publication number: 20090111808Abstract: The present patent application concerns compounds of formula (I) with R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.Type: ApplicationFiled: April 25, 2006Publication date: April 30, 2009Inventors: Isabelle Bertrand, Marc Capet, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Olivia Poupardin-Olivier, Philippe Robert, Jean-Charles Schwartz, Olivier Labeeuw
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Patent number: 7521449Abstract: The invention relates to compounds corresponding to formula (I): in which: Ar represents a mono- or disubstituted phenyl; R1 represents an unsubstituted or substituted phenyl; R2 represents: a pyridyl; an unsubstituted or substituted phenyl; a benzyl that is unsubstituted or substituted on the phenyl; R2 may moreover represent: a heterocyclic radical; R3 represents various values. The invention also comprises methods for the compounds preparation, formulations comprising them and therapeutic applications thereof.Type: GrantFiled: January 9, 2007Date of Patent: April 21, 2009Assignee: Sanofi-AventisInventors: Xavier Emonds-Alt, Vincenzo Proietto
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Publication number: 20090076005Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.Type: ApplicationFiled: December 28, 2007Publication date: March 19, 2009Applicant: Xcovery, Inc.Inventors: Congxin Liang, Ming Qi, Shu Gao, Zhigang Li
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Publication number: 20090069325Abstract: The present invention relates to the compounds of formula (I): in which: and the remaining variables are defined herein. The present invention also relates to a process for preparing such compounds and use of such compounds in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.Type: ApplicationFiled: November 10, 2008Publication date: March 12, 2009Applicant: AstraZeneca ABInventors: Christopher Luckhurst, Matthew Perry, Hitesh Sanganee, Brian Springthorpe
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Publication number: 20090062278Abstract: The present invention concerns 5- or 6-substituted-benzimidazole derivatives having inhibitory activity on the replication of the respiratory syncytial virus and having the formula a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein Q is Ar2, R6, pyrrolidinyl substituted with R6, piperidinyl substituted with R6 or homopiperidinyl substituted with R6, G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle; one of R2a and R2b is cyanoC1-6alkyl, cyanoC2-6alkenyl, Ar3C1-6alkyl, Het1C1-6alkyl, N(R8aR8b)C1-6alkyl, Ar3C2-6alkenyl, Het1C2-6alkenyl, Ar3aminoC1-6alkyl, Het1aminoC1-6alkyl, Ar3thioC1-6alkyl, Het1thioC1-6alkyl, Ar3sulfonylC1-6alkyl, Het1sulfonylC1-6alkyl, Ar3aminocarbonyl, Het1aminocarbonyl, Ar3(CH2)naminocarbonyl, Het1(CH2)naminocarbonyl, Ar3carbonylamino, Het1carbonylamino, Ar3(CH2)ncarbonylamino, Het1(CH2)ncarbonylamino, and the other one of R2a and R2b is hydrogen; in case R2aType: ApplicationFiled: October 17, 2008Publication date: March 5, 2009Inventors: Jean-Francois Bonfanti, Koenraad Jozef Lodewijk Andries, Jerome Michel Claude Fortin, Philippe Muller, Frederic Marc Maurice Doublet, Christophe Meyer, Rudy Edmond Willebrords, Tom Valerius Josepha Gevers, Philip Maria Martha Bern Timmerman
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Patent number: 7491827Abstract: 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: GrantFiled: July 14, 2004Date of Patent: February 17, 2009Assignee: Millennium Pharmaceuticals, Inc.Inventors: Mingshi Dai, Bing Guan, Robert A. Bennett, Douglas F. Burdi, Shomir Ghosh, Gang Li, Charles Minor, Tracy J. Jenkins
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Publication number: 20090043091Abstract: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and RN1 is selected from hydrogen, an optionally substituted C1-7 alkyl group, an optionally substituted C3-20 heterocyclyl group, an optionally substituted C5-20 aryl group, an acyl group, an ester group and an amido group, and its use as a pharmaceutical.Type: ApplicationFiled: September 19, 2008Publication date: February 12, 2009Applicant: KUDOS PHARMACEUTICALS LIMITEDInventors: Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Laurent Jean Martin Rigoreau, Marc Geoffrey Hummersone, Roger John Griffin
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Publication number: 20090023733Abstract: The present invention provides a compound of a formula (I): [Chemical formula should be inserted here. Please see paper copy] wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state.Type: ApplicationFiled: March 6, 2007Publication date: January 22, 2009Inventors: Peter Cage, Mark Furber, Christopher Luckhurst, Matthew Perry, Brian Springthorpe
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Publication number: 20090018132Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.Type: ApplicationFiled: July 1, 2008Publication date: January 15, 2009Inventors: Andrew P. Degnan, George O. Tora, Derek J. Denhart, Vivekananda M. Vrudhula, John E. Macor, Joanne J. Bronson
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Publication number: 20090012055Abstract: Novel substituted piperidines of the general formulae (I) and (II) with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent.Type: ApplicationFiled: February 6, 2008Publication date: January 8, 2009Inventors: Peter Herold, Robert Mah, Stefan Stutz, Aleksandar Stojanovic, Vincenzo Tschinke, Nathalie Jotterand
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Publication number: 20080306068Abstract: The present invention provides kinase inhibitors of Formula I:Type: ApplicationFiled: June 15, 2005Publication date: December 11, 2008Applicant: Eli Lilly and CompanyInventors: Tiechao Li, Mark Andrew Pobanz, Chuan Shih, Yong Wang, Boyu Zhong, Jesus Andres Blas, Alfonso De Dios, Beatriz Lopez De Uralde-Garmendia, Luisa Maria Martin Cabrejas
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Patent number: 7452891Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: January 28, 2005Date of Patent: November 18, 2008Assignee: Schering CorporationInventors: John W. Clader, Hubert B. Josien, Anandan Palani, Tin Yau Chan
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Publication number: 20080280890Abstract: The present disclosure provides compounds that include hydroxylamines of formula I or II, pharmaceutical compositions, and methods for their use. The methods utilize hydroxylamine compounds and/or their pharmaceutical compositions for the treatment of angiogenesis, hepatitis, complement-mediated pathologies, drusen-mediated pathologies, macular degeneration and certain other ophthalmic conditions, inflammation, arthritis, and related diseases and for the inhibition of complement activation.Type: ApplicationFiled: February 15, 2008Publication date: November 13, 2008Inventor: Ghanshyam Patil
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Publication number: 20080280881Abstract: The present invention concerns morpholinyl containing benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle Q is R7, pyrrolidinyl substituted with R7, piperidinyl substituted with R7 or homopiperidinyl substituted with R7; one of R2a and R3a is selected from halo, optionally mono- or polysubstituted C1-6alkyl, optionally mono- or polysubstituted C2-6alkenyl, nitro, hydroxy, Ar2, N(R4aR4b), N(R4aR4b)sulfonyl, N(R4aR4b)carbonyl, C1-6alkyloxy, Ar2oxy, Ar2C1-6alkyloxy, carboxyl, C1-6alkyloxycarbonyl, or —C(=Z)Ar2; and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen, C1-6alkyl or halogen and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen,Type: ApplicationFiled: June 17, 2008Publication date: November 13, 2008Inventors: Jean-Francois Bonfanti, Koenraad Josef Lodewijk Andries, Jerome Michel Claude Fortin, Philippe Muller, Frederic Marc Maurice Doublet, Christophe Meyer, Rudy Edmond Willebrords, Tom Valerius Josepha Gevers, Philip Maria Martha Born Timmerman
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Publication number: 20080214539Abstract: The invention includes benzisoxazole piperidine compositions and methods of using them for modulating sleep.Type: ApplicationFiled: April 26, 2006Publication date: September 4, 2008Inventors: Daniel Coughlin, James F. White, Kazumi Shiosaki, David G. Hangauer, Michael Solomon, Dale M. Edgar
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Publication number: 20080200460Abstract: Compounds of formula (I): wherein: when X is NR5, Y is absent or is CH2; when X is CH2, Y is absent, CH2, NR6, O, S, S(O) or S(O)2; Z is a 5- or 6-membered heterocyclyl ring; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).Type: ApplicationFiled: December 15, 2005Publication date: August 21, 2008Inventors: Dearg Brown, John Oldfield, Howard Tucker
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Publication number: 20080194562Abstract: The invention provides compounds of the formula (I) or a salt, tautomer, solvate or N-oxides thereof; wherein: R1 is selected from (a) 2,6-dichlorophenyl; (b) 2,6-difluorophenyl; (c) a 2,3,6-trisubstituted phenyl group wherein the substituents are fluorine, chlorine, methyl or methoxy; and (d) a group R0 wherein R0 is a 3-12 membered carbocyclic or heterocyclic group; or optionally substituted C1-8 hydrocarbyl; R2a and R2b are each hydrogen or methyl; and R3 is as defined in the claims. The compounds have activity as inhibitors of Cyclin Dependent Kinases (CDK) and Glycogen Synthase Kinases (GSK) kinases and are useful in the treatment or prophylaxis of disease states or conditions mediated by the kinases.Type: ApplicationFiled: January 20, 2006Publication date: August 14, 2008Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Paul Graham Wyatt, Valerio Berdini, Adrian Liam Gill, Gary Trewartha, Andrew James Woodhead, Eva Figueroa Navarro, Michael Alistair O'Brien, Theresa Rachael Phillips
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Publication number: 20080167288Abstract: The present invention provides compounds of the formula: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.Type: ApplicationFiled: February 15, 2008Publication date: July 10, 2008Applicant: Lncyte CorporationInventors: Yun Long Li, Jincong Zhuo, David Burns, Wanqing Yao, Ravi Kumar Jalluri
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Patent number: 7390804Abstract: An N-containing five-membered ring compound of formula (I) wherein all symbols are the same as described in the specification, and a non-toxic salt thereof. The compound of formula (I) has an inhibitory activity against cysteine protease and therefore it is useful as an agent for the prophylaxis and/or treatment of inflammatory diseases, diseases induced by apoptosis, diseases induced by disorders of immune responses, autoimmune diseases, diseases induced by decomposition of proteins which compose organism, shock, circulatory system disorders, blood coagulation systems disorders, malignant tumors, acquired immune deficiency syndrome (AIDS) and AIDS-related complex (ARC), parasitic diseases, nerve degeneration diseases, pulmonary disorders, bone resorption diseases, endocrinesthenia, etc.Type: GrantFiled: December 22, 2004Date of Patent: June 24, 2008Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kazuyuki Ohmoto, Iori Itagaki
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Publication number: 20080139556Abstract: A composition for binding FKBP proteins is disclosed, along with a method of treating conditions associated with neuronal degeneration, wherein said composition comprises a compound of formula I, wherein, R, R1, R2, R3 and X are as defined herein.Type: ApplicationFiled: December 6, 2006Publication date: June 12, 2008Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: Raymond W. KOSLEY, Bruce Baron, Patrick Jimonet, John G. Jurcak, Stephen J. Shimshock, Xu-yang Zhao, Rosy Sher, Paul J. Mueller, Jennifer Beall, Matthieu Barrague, Joseph W. Guiles
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Patent number: 7384943Abstract: The present invention relates to new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives having the formula (I) wherein X is N; Y is NR2CH2, CH2NR2, NR2CO, CONR2, NR2SO2 or NR2CONR2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycoalkyl or (CH2)n-aryl, wherein aryl is a heteromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5; and n is 0-4; as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or a pharmaceutically acceptable salt or solvate thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds.Type: GrantFiled: June 5, 2006Date of Patent: June 10, 2008Assignee: AstraZeneca ABInventors: Stefan Berg, Martin Nylöf, Svante Ross, Seth-Olov Thorberg
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Publication number: 20080081813Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: ApplicationFiled: March 27, 2002Publication date: April 3, 2008Inventors: Lieven Meerpoel, Marcel Viellevoye