Nitrogen Bonded Directly At 2-position Patents (Class 544/292)
-
Patent number: 8053434Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.Type: GrantFiled: September 1, 2009Date of Patent: November 8, 2011Assignee: Rigel Pharmaceuticals, Inc.Inventors: Pingyu Ding, Ankush Argade, Dane Goff, Rajinder Singh, Esteban Masuda, Vanessa Taylor, Sacha Holland
-
Publication number: 20110230505Abstract: Dihydroquinazoline compounds, compositions containing them, the use of the compounds and compositions for the treatment of Alzheimer's disease are described.Type: ApplicationFiled: November 20, 2009Publication date: September 22, 2011Applicant: PURDUE RESEARCH FOUNDATIONInventor: Arun K. Ghosh
-
Publication number: 20110195979Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 and Ar are as defined in description and in claims, can be used as a medicament.Type: ApplicationFiled: February 7, 2011Publication date: August 11, 2011Inventors: Li Chen, Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Lisha Wang, Jim Zhen Wu, Wengang Yang
-
Publication number: 20110152521Abstract: [4-(3-aminophenyl)-6,7-dimethoxyquinazolin-2-yl]methylamine with a favorable yield and high purity can be produced by subjecting a compound represented by the following formula (I) to a step of reacting with methylamine and a step of deprotection if desired: wherein L represents a protective group of amino.Type: ApplicationFiled: August 15, 2008Publication date: June 23, 2011Applicant: Eisai R&D Management Co., Ltd.Inventor: Jun Niijima
-
Publication number: 20110130413Abstract: This invention relates to the discovery of prodrugs of substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential for cardiovascular side-effects and which should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to prodrugs of certain imidazoquinazoline derivatives which have the general formula (I) shown below wherein the substituents have the meanings defined in claim 1 and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: June 2, 2011Applicant: Shire LLCInventors: Bernard Golding, Peter Cicala, Richard Franklin, Angus Macleod
-
Patent number: 7947696Abstract: Novel phenylquinazoline derivatives of the formula (I), in which R1, R2, R3, R4 and R5 have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: GrantFiled: April 24, 2006Date of Patent: May 24, 2011Assignee: Merck Patent GmbHInventors: Hans-Michael Eggenweiler, Michael Wolf, Hans-Peter Buchstaller
-
Publication number: 20110118258Abstract: Compounds of general formula (I); or a stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof, wherein R1, R2, R3, R4, R5, R6, R8 and R9 are as defined herein, are useful for the treatment of diseases and conditions which are mediated by excessive or inappropriate Hsp90 activity such as cancers, viral infection and inflammatory diseases or conditions.Type: ApplicationFiled: May 15, 2008Publication date: May 19, 2011Inventors: Stephen Martin Courtney, Mark Whittaker, Owen Clifford Mather, Christopher John Yarnold, Oliver Robin Barker, Christian Aldo Georges Napoleon Montalbetti, Thomas Hesterkamp, Mihaly Daniel Gardiner
-
Patent number: 7943768Abstract: A compound of formula (I) P—W—C(?X)-L-Q??(I) wherein P is an optionally substituted aryl or heteroaryl group; W is an optionally substituted 6 or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 independently selected from Oxygen and Nitrogen, X is selected from Oxygen, Nitrogen and Sulphur; L is an optional C1-4 linker; and Q is an optionally substituted 4-7 membered aliphatic ring: for use in the treatment of chemokine mediated diseases or disorders.Type: GrantFiled: December 18, 2006Date of Patent: May 17, 2011Assignee: AstraZeneca ABInventors: Justin Fairfield Bower, Peter Wedderburn Kenny, Jeffrey Philip Poyser
-
Publication number: 20110112062Abstract: This invention relates to novel compounds of the Formula I, II, III, IHa, NIb, IV, IVa, IVb, IVc, IVd, IVe, V, Va, Vb1 V1, V1a, VIb, VII, Vi1a, VIIb, VIII, V111a, VIIIb, IX, IXa, X, and Xa, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.Type: ApplicationFiled: April 21, 2009Publication date: May 12, 2011Inventors: David A. Claremon, Linghang Zhuang, Yuanjie Ye, Suresh B. Singh, Colin M. Tice
-
Publication number: 20110112118Abstract: 2,4-Diaminoquinazolines of formulae I-IV and VI are useful for treating spinal muscular atrophy (SMA).Type: ApplicationFiled: January 20, 2011Publication date: May 12, 2011Applicant: FAMILIES OF SPINAL MUSCULAR ATROPHYInventors: Jasbir Singh, Mark E. Gurney
-
Patent number: 7939540Abstract: A compound represented by the following formula (I), salt thereof, or hydrate thereof, can effectively relieve itch caused by atopic disease or the like: wherein R represents hydroxyl, C1-6 alkoxy optionally substituted with C1-6 alkoxy, or amino optionally substituted with C1-6 alkyl.Type: GrantFiled: February 20, 2007Date of Patent: May 10, 2011Assignee: Eisai R&D Management Co., Ltd.Inventors: Kazuki Miyazaki, Kazutomi Kusano, Yasutaka Takase, Osamu Asano, Manabu Shirato, Hisashi Wakita, Naoto Ishii, Takao Saeki, Tomoko Saeki, legal representative, Mai Saeki, legal representative
-
Patent number: 7932262Abstract: The invention provides quinazoline compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.Type: GrantFiled: April 5, 2007Date of Patent: April 26, 2011Assignee: Novartis AGInventors: Savithri Ramurthy, Xiaodong Lin, Sharadha Subramanian, Alice Rico, Xiaojong M. Wang, Rama Jain, Jeremy M. Murray, Stephen E. Basham, Robert L. Warne, Wei Shu, Yasheen Zhou, Jeffrey Dove, Mina Aikawa, Payman Amiri, Weibo Wang, Johanna M. Jansen, Allan S. Wagman, Keith B. Pfister, Simon Ng
-
Publication number: 20110065735Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: March 17, 2011Applicant: Shire LLCInventors: Bernard Golding, Richard Franklin, Peter Cicala
-
Patent number: 7906522Abstract: The present invention provides 2-aminoquinazoline derivatives represented by formula (I): wherein R1 and R2 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, and the like; X represents a bond or CR7aR7b wherein R7a and R7b may be the same or different and each represents a hydrogen atom, and the like; when X is a bond, R3 represents substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group; when X is CR7aR7b wherein R7a and R7b have the same meanings as defined above, respectively, R3 represents substituted or unsubstituted lower alkoxy, substituted or unsubstituted aryl, and the like; R4 represents a hydrogen atom, hydroxy, substituted or unsubstituted lower alkoxy, and the like; and R5 represents a hydrogen atom, substituted or unsubstituted aryl, and the like, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 28, 2006Date of Patent: March 15, 2011Assignee: Kyowa Hakko Kirin Co., LtdInventors: Kuniyuki Kishikawa, Hidetomo Imase, Hajime Kashima, Kiyotoshi Mori, Toshihide Ikemura, Yoshisuke Nakasato, Misato Tomuro
-
Patent number: 7897627Abstract: The present invention relates to compounds of formula wherein Ar, Het, R1 and n are as defined herein and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. Compounds of formula I are orexin receptor antagonists and are useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder and sleep disorders associated with neurological diseases.Type: GrantFiled: December 15, 2008Date of Patent: March 1, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
-
Publication number: 20110039845Abstract: A 2-aminoquinazoline derivative represented by formula (I) {wherein R1 represents a hydrogen atom, or the like, R2 represents a hydrogen atom, R3 represents formula (II) [wherein A1 represents formula (III), or the like, R8 represents lower alkyl, or the like, and R9 represents optionally substituted aryl, or the like], R4 represents hydroxy, or the like, and R5 represents optionally substituted aryl, or the like}, or a pharmaceutically acceptable salt thereof is provided.Type: ApplicationFiled: April 23, 2009Publication date: February 17, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Hajime Kashima, Tomoyuki Nishikawa, Yusuke Yamada, Toshihiro Seike, Yoshisuke Nakasato, Hiroshi Umehara
-
Publication number: 20100311965Abstract: An object of the present invention is to provide compounds which are useful as protein kinase inhibitors.Type: ApplicationFiled: December 26, 2008Publication date: December 9, 2010Applicants: CARNA BIOSCIENCES INC., CRYSTAL GENOMICS, INC.Inventors: Masaaki Sawa, Koichi Yokota, Hideki Moriyama, Myoungyoup Shin, Seonggu Ro, Joong Myung Cho
-
Publication number: 20100298289Abstract: The present invention concerns heterobicyclic compounds of formula (I) processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: October 7, 2008Publication date: November 25, 2010Applicant: UCB PHARMA, S.A.Inventors: Gilles Raphy, Cecile Pegurier, Hans Meissner, Roland Knight, David Alan Owen
-
Publication number: 20100247534Abstract: A compound of formula I wherein m, n, A, B, D, E, G, H, Y, R1, R2, R3, R4, R5, and R8, are described herein.Type: ApplicationFiled: June 10, 2010Publication date: September 30, 2010Inventors: James A. Johnson, John Lloyd, Alexander Kover
-
Publication number: 20100240671Abstract: The present invention relates to substituted heterocyclic compounds of Formula I or XI: or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine II4 receptor inhibitors useful in the treatment of histamine II4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.Type: ApplicationFiled: March 19, 2010Publication date: September 23, 2010Applicant: INCYTE CORPORATIONInventors: Jincong ZHUO, Thomas P. MADUSKUIE, Ding-quan QIAN, Wenqing YAO
-
Publication number: 20100234324Abstract: Novel quinazolinamide derivatives of the formula (I), in which R1-R3 have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: June 16, 2008Publication date: September 16, 2010Applicant: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Hans-Michael Eggenweiler, Christian Sirrenberg, Hans-Peter Buchstaller
-
Patent number: 7790733Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, and n are as described in the specification and pharmaceutically acceptable acid addition salts thereof. The compounds of formula I can be used for the treatment of 5-HT5A receptor antagonists related diseases, which include depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, disorders of eating behaviors, sexual dysfunction, sleep disorders, withdrawal from abuse of drugs, motor disorders such as Parkinson's disease, dementia in Parkinson's disease, neuroleptic-induced Parkinsonism and tardive dyskinesias, as well as other psychiatric disorders and gastrointestinal disorders such as irritable bowel syndrome.Type: GrantFiled: June 21, 2006Date of Patent: September 7, 2010Assignee: Hoffman-La Roche Inc.Inventors: Alexander Alanine, Luca Claudio Gobbi, Sabine Kolczewski, Thomas Luebbers, Jens-Uwe Peters, Lucinda Steward
-
Patent number: 7790732Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3 are as described in the specification and pharmaceutically acceptable acid addition salts and tautomers thereof. Compounds of formula I have good activity on the 5-HT5A receptor. Therefore, the invention provides a method for treating diseases related to this receptor, for example, anxiety, depression, sleep disorders and schizophrenia.Type: GrantFiled: June 21, 2006Date of Patent: September 7, 2010Assignee: Hoffman-La Roche Inc.Inventors: Alexander Alanine, Luca Claudio Gobbi, Sabine Kolczewski, Thomas Luebbers, Jens-Uwe Peters, Lucinda Steward
-
Publication number: 20100216767Abstract: The invention provides novel compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.Type: ApplicationFiled: December 20, 2007Publication date: August 26, 2010Inventors: Mina Aikawa, Payman Amiri, Steven Bashman, Jeffrey Dove, Rama Jain, Xiaodong Lin, Jeremy Murray, Savithri Ramurthy, Alice Rico, Wei Shu, Sharadha Subramanian, Xiaojing Michael Wang, Robert L. Warne, Yasheen Zhou
-
Patent number: 7781441Abstract: The present invention relates to compounds of formula I wherein R, R1, R2, R3, R4, aryl, n, and m are as defined in the specification and pharmaceutically acceptable acid addition salts and tautomeric forms thereof. Such compounds have good activity on the 5-HT5A receptor. Therefore, the invention provides methods for the treatment of certain CNS disorders with such compounds.Type: GrantFiled: April 27, 2006Date of Patent: August 24, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Luca Claudio Gobbi, Sabine Kolczewski, Thomas Luebbers, Jens-Uwe Peters, Lucinda Steward
-
Patent number: 7772232Abstract: A compound of formula I wherein m, n, A, B, D, E, G, H, Y, R1, R2, R3, R4, R5, and R8, are described herein. Said compounds being useful as inhibitors of potassium channel function and in the treatment of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.Type: GrantFiled: April 13, 2005Date of Patent: August 10, 2010Assignee: Bristol-Myers Squibb CompanyInventors: James A. Johnson, John Lloyd
-
Publication number: 20100174073Abstract: The present invention relates to novel N-[3-[(4-acyl-/aroyl-substituted amino-6,7-dimethoxy-2-quinazolinyl)methylamino]propyl]tetrahydro-2-furancarboxamide derivatives, and a process for the preparation thereof. The novel compounds are useful for preparing alfuzosin or a pharmaceutically acceptable salt thereof in high yield and purity.Type: ApplicationFiled: May 2, 2008Publication date: July 8, 2010Applicant: ACTAVIS GROUP PTC EHFInventors: Uday Rajaram Bapat, Jose Paul Potams, Narasimhan Subramanian, Jon Valgeirsson
-
Publication number: 20100125078Abstract: The present invention relates to a compounds of formula I wherein R1, R2, R3, R4, R5, and n are as defined herein and to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. The present compounds 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: November 9, 2009Publication date: May 20, 2010Inventors: Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
-
Publication number: 20100120803Abstract: The present invention relates to 3,4-dihydroquinazoline derivatives, a process of preparing them and a pharmaceutical composition including them. The 3,4-dihydroquinazoline derivatives of the present invention have excellent T-type calcium channel blocking effect and anti-cancer activity.Type: ApplicationFiled: May 6, 2008Publication date: May 13, 2010Applicant: DONGWOO SYNTECH CO., LTD.Inventors: Jae Yeol Lee, Dong Joon Choo, Young Deuk Kim, Chun Rim Oh
-
Publication number: 20100121052Abstract: The invention provides novel compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.Type: ApplicationFiled: June 9, 2009Publication date: May 13, 2010Inventors: Rama Jain, Xiaodong Lin, Simon C. Ng, Keith B. Pfister, Savithri Ramurthy, Alice Rico, Sharadha Subramanian, Xiaojing Michael Wang
-
Patent number: 7700608Abstract: A method for the treatment of thrombocythemia in a subject comprising administering a therapeutically effective amount of compounds having the formulas (I) through (III) or equilibrating forms thereof.Type: GrantFiled: August 3, 2005Date of Patent: April 20, 2010Assignee: Shire Holdings AGInventor: Richard Franklin
-
Publication number: 20100093772Abstract: A method for the treatment of thrombocythemia in a subject comprising administering a therapeutically effective amount of compounds having the formulas (I) through (III) or equilibrating forms thereof.Type: ApplicationFiled: October 16, 2009Publication date: April 15, 2010Applicant: Shire Holdings AGInventor: Richard Franklin
-
Patent number: 7691866Abstract: New substituted quinazoline, quinoxaline, quinoline and isoquinoline compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: GrantFiled: October 15, 2004Date of Patent: April 6, 2010Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: Savithri Ramurthy, Paul A. Renhowe, Sharadha Subramanian
-
Patent number: 7687625Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 protease that comprise a compound comprising the formula: wherein Q is selected from the group of CO, SO, SO2, or C?NR9; and R1, R2, R3 and R4 are as defined herein.Type: GrantFiled: March 24, 2004Date of Patent: March 30, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Jun Feng, Stephen L. Gwaltney, Stephen W. Kaldor, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
-
Patent number: 7678803Abstract: The current invention is directed toward compounds and pharmaceutically acceptable salts of Formula I wherein Q1 is CR1, Q2 is N, Q4 and Q5 are each CR1, Q3 is CR2, X1 is N or CRc, Y is CRc, X2 and X3 are each C(R5)(R6), R7 is O. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer The current invention is also directed toward pharmaceutical compositions comprising compounds of the invention.Type: GrantFiled: August 24, 2007Date of Patent: March 16, 2010Assignee: Serenex, Inc.Inventors: Kenneth He Huang, James Veal, Thomas Barta, Emilie D. Smith, Wei Ma, Andy Ommen
-
Publication number: 20100056506Abstract: The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein: R1, R2, Z1, t, and ring A are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of JNK, such as diabetes, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: ApplicationFiled: April 19, 2007Publication date: March 4, 2010Applicant: PFIZER PRODUCTS INC.Inventors: Liming Huang, Song Liu, Elizabeth A. Lunney, Simon P. Planken
-
Publication number: 20100056377Abstract: Disclosed are: a substance which has an activity of inhibiting the intracellular signaling from a plant-derived cytokinin receptor and which can control the growth or differentiation of a plant. Also, disclose is a method for searching for a chemical substance capable of promoting the growth of a root of a plant, which comprises measuring the level of intracellular signaling from the receptor in a system where a cell having the receptor is contacted with a chemical substance having an agonistic activity on the receptor and a substance to be tested, comparing the level of intracellular signaling measured in the preceding step with a level of intracellular signaling measured in the absence of the chemical substance, and determining the chemical substance as being a chemical substance capable of promoting the growth of a root of a plant based on the difference obtained by the comparison; and others.Type: ApplicationFiled: November 22, 2007Publication date: March 4, 2010Inventors: Asako Nagasawa, Yuto Arata, Hideki Uneme
-
Publication number: 20100048561Abstract: The invention provides quinazoline compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.Type: ApplicationFiled: April 5, 2007Publication date: February 25, 2010Applicant: NOVARTIS VACCINES & DIAGNOSTICS, INC.Inventors: Savithri Ramurthy, Xiaodong Lin, Sharadha Subramanian, Alice C. Rico, Xiaojing M. Wang, Rama Jain, Jeremy M. Murray, Steven E. Basham, Robert L. Warne, Wei Shu, Yasheen Zhou, Jeffrey Dove, Mina Aikawa, Payman Amiri, Weibo Wang, Johanna M. Jansen, Allan S. Wagman, Keith B. Pfister, Simon Ng
-
Patent number: 7662828Abstract: Substituted 5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-2-yl and 5,6,7,8-tetrahydro-quinazolin-2-yl compounds, corresponding to formula I processes for the production thereof, pharmaceutical preparations containing these compounds the use thereof for the production of pharmaceutical preparations and related method of treating or inhibiting certain disorders or conditions, including pain.Type: GrantFiled: October 27, 2006Date of Patent: February 16, 2010Assignee: Gruenenthal GmbHInventors: Stefan Oberbörsch, Bernd Sundermann, Corinna Sundermann, Michael Haurand, Hagen-Heinrich Hennies, Edward Bijsterveld
-
Publication number: 20100004256Abstract: Heteroaryl-fused macrocyclic 2,4-diaminopyrimidine compounds of formula (I) wherein W, G1, G2, A1 and R1 are defined in the description, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions, and disorders using such compounds and compositions are described herein.Type: ApplicationFiled: May 5, 2009Publication date: January 7, 2010Applicant: Abbott LaboratoriesInventors: Huaqing Liu, Irene Drizin, Marlon D. Cowart, Robert J. Altenbach
-
Publication number: 20090253678Abstract: Macrocyclic pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions, and disorders using such compounds and compositions are described herein.Type: ApplicationFiled: March 27, 2009Publication date: October 8, 2009Applicant: ABBOTT LABORATORIESInventors: Huaqing Liu, Irene Drizin, John R. Koenig, Marlon D. Cowart, Chen Zhao, Brian D. Wakefield, Lawrence A. Black, Robert J. Altenbach
-
Publication number: 20090221822Abstract: The present invention relates to a process for the preparation of dihydroquinazolines, which are used for the production of medicaments.Type: ApplicationFiled: June 2, 2006Publication date: September 3, 2009Applicant: Bayer HealthCare AGInventors: Käthe Goossen, Oliver Kuhn, Mathias Berwe, Joachim Krüger, Hans-Christian Militzer
-
Publication number: 20090182140Abstract: An alicyclic heterocyclic compound represented by the following formula or a pharmaceutically acceptable salt thereof: wherein ring A is a heterocyclic ring, ring B is a carbocyclic ring, a heterocyclic ring etc., P1 and P2 are CH or N, q and r are 0 to 2, X is —NH—, —O—, —CH2—, etc., Y is —CH2—, —CO—, —SO2—, etc., Z is —CO—, —SO2—, etc., and R3 is carbocyclic group, heterocyclic group, hydroxyl, alkoxy or amino, is useful as a controlling agent of the function of CCR4 useful for the prevention or treatment for bronchial asthma, atopic dermatitis, etc.Type: ApplicationFiled: November 30, 2006Publication date: July 16, 2009Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Shigeru Furukubo, Hiroshi Miyazaki
-
Publication number: 20090163485Abstract: The present invention relates to compounds of formula wherein Ar, Het, R1 and n are as defined herein and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. Compounds of formula I are orexin receptor antagonists and are useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder and sleep disorders associated with neurological diseases.Type: ApplicationFiled: December 15, 2008Publication date: June 25, 2009Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
-
Patent number: 7550590Abstract: Compounds, pharmaceuticals, kits, and methods are provided for use with DPP-IV and other S9 protease that comprise a compound comprising the formula: wherein Q is selected from the group of CO, SO, SO2, or C?NR9; and R1, R2, R3 and R4 are as defined herein.Type: GrantFiled: March 24, 2004Date of Patent: June 23, 2009Assignee: Takeda Pharmaceutical Company LimitedInventors: Jun Feng, Stephen L. Gwaltney, Stephen W. Kaldor, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
-
Patent number: 7544691Abstract: The invention relates to the guanine derivatives of general formula (I), and to hydrates or solvents thereof, for use as neuropeptide FF receptor antagonists in the treatment of pains and hyperalgesia, of withdrawal symptoms of addiction to alcohol, psychotropic drugs or nicotine and in the prevention of or recovery from these addictions, for the regulation of insulin release, food intake, memory functions, blood pressure, electrolyte and energy metabolism, and in the treatment of urinary incontinenceType: GrantFiled: September 3, 2004Date of Patent: June 9, 2009Assignee: Actelion Pharmaceuticals, Ltd.Inventors: Volker Breu, Anja Fecher, Heinz Fretz, Thomas Giller, Kurt Hilpert, Olivier Valdenaire
-
Publication number: 20090143355Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds of Formula I and II wherein R, R1 and R2 for each formula are defined herein. The invention further includes analogs, prodrugs and pharmaceutically acceptable salts and derivatives of Formulas I and II, as well as pharmaceutical compositions, medicaments and methods thereof for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: January 29, 2009Publication date: June 4, 2009Applicant: Amgen Inc.Inventors: Chester Chenguang Yuan, Kevin Yang, Simon Van Der Plas, Babak Riahi, Michele Potashman, Vinod F. Patel, Rana Nomak, Aiwen Li, Qi Huang, Jean-Christophe Harmange, Benny C. Askew, JR.
-
Publication number: 20090137583Abstract: The present invention provides 2-aminoquinazoline derivatives represented by formula (I): wherein R1 and R2 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, and the like; X represents a bond or CR7aR7b wherein R7a and R7b may be the same or different and each represents a hydrogen atom, and the like; when X is a bond, R3 represents substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group; when X is CR7aR7b wherein R7a and R7b have the same meanings as defined above, respectively, R3 represents substituted or unsubstituted lower alkoxy, substituted or unsubstituted aryl, and the like; R4 represents a hydrogen atom, hydroxy, substituted or unsubstituted lower alkoxy, and the like; and R5 represents a hydrogen atom, substituted or unsubstituted aryl, and the like, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 28, 2006Publication date: May 28, 2009Applicant: KYOWA HAKKO KOGYO CO., LTD.Inventors: Kuniyuki Kishikawa, Hidetomo Imase, Hajime Kashima, Kiyotoshi Mori, Toshihide Ikemura, Yoshisuke Nakasato, Misato Tomuro
-
Publication number: 20090105211Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.Type: ApplicationFiled: March 14, 2008Publication date: April 23, 2009Applicant: Exelixis, Inc.Inventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
-
Publication number: 20090069562Abstract: An improved process for the preparation of N-[3-[(4-amino-6,7-dimethoxy-2-quinazolinyl)methylamino]propyl]tetrahydrofuran-2-carboxamide of Formula (I), by reacting N1-(4-amino-6,7-dimethoxyquinazolin-2-yl)-N1-methyl propane-1,3-diamine (V) with tetrahydrofuran-2-carboxylic acid or its reactive derivative in a solvent.Type: ApplicationFiled: December 11, 2006Publication date: March 12, 2009Inventors: Joseph Prabahar Koilpillai, Magesh Subramanian, Uppalalah Mallela, Sivakumaran Meenakshlsunderam