Bicyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/593)
-
Publication number: 20090192141Abstract: The present invention relates to inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.Type: ApplicationFiled: February 20, 2009Publication date: July 30, 2009Applicant: ABBOTT LABORATORIESInventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Steven Fung, Peer B. Jacobson, Lynne E. Rueter, Marina I. Strakhova, Jiahong Wang, James T. Link, Yixian Chen, Hwan-soo Jae, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Qi Shuai, Bryan K. Sorensen, Martin Winn, Dariusz Wodka, Hong Yong
-
Publication number: 20090181947Abstract: The present invention relates to novel bicyclic enamino(thio)carbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.Type: ApplicationFiled: March 19, 2007Publication date: July 16, 2009Applicant: Bayer CropScience AGInventors: Peter Jeschke, Robert Velten, Thomas Schenke, Michael Edmund Beck, Olga Malsam, Udo Reckmann, Ralf Nauen, Ulrich Görgens, Leonardo Pitta, Christian Arnold, Erich Sanwald
-
Publication number: 20090181946Abstract: Benzazepinone compounds represented by Formula (I), or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, urinary incontinence, pruritis, itchiness, allergic dermatitis, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: June 5, 2007Publication date: July 16, 2009Inventors: Scott B. Hoyt, Clare London, Dong Ok, William H. Parsons
-
Publication number: 20090149444Abstract: A compound of the formula (I): wherein R1 represents a C1-C6 alkyl, (C1-C6 alkyl)amino, di(C1-C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are the same or different and represent hydrogen or a C1-C6 alkyl; Ra represents hydrogen, C1-C6 alkyl or C2-C6 alkenyl or together with R2 represents a C1-C3 alkylene; Arom represents a heteroaryl; A represents a C1-C6 alkylene; E represents a single bond, oxygen, sulphur or R4NR4—, wherein R4 is hydrogen or C1-C7 alkenoyl; X1 and X2 both represent oxygen; X2 is attached at the 3-position or the 4-position; or a pharmacologically acceptable salt or ester thereof. The compound has superior acetylcholinesterase inhibitory action and selective serotonin reuptake inhibitory action, and is useful for treating Alzheimer's disease, depression, Huntington's chorea, Pick's disease, tardive dyskinesia, compulsive disorders or panic disorders.Type: ApplicationFiled: January 29, 2009Publication date: June 11, 2009Applicant: BTG INTERNATIONAL LIMITEDInventors: Kazuo Koyama, Shinji Marumoto, Narihiro Toda, Hiroshi Kogen, Keiko Suzuki
-
Publication number: 20090131410Abstract: Provided are muscarinic receptor antagonists, which can be useful in treating various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. Also provided are processes for preparing compounds described herein, pharmaceutical compositions thereof, and methods for treating diseases mediated through muscarinic receptors.Type: ApplicationFiled: October 5, 2006Publication date: May 21, 2009Inventors: Naresh Kumar, Kirandeep Kaur, Suman Gupta, Anita Chugh, Mohammad Salman, Raj Kumar Shirumalla, Shivani Malhotra
-
Publication number: 20090118260Abstract: The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.Type: ApplicationFiled: October 16, 2008Publication date: May 7, 2009Applicants: AMR TECHNOLOGY, INC., BRISTOL-MYERS SQUIBB COMPANYInventors: Bruce F. MOLINO, Shuang LIU, Aruna SAMBANDAM, Peter R. GUZZO, Min HU, Congxiang ZHA, Kassoum NACRO, David D. MANNING, Matthew L. ISHERWOOD, Kristen N. FLEMING, Wenge CUI, Richard E. OLSON
-
Publication number: 20090105224Abstract: The invention relates to tetrahydrobenzazepines of the general formula I in which the variables Ar, A, B, Y, R1 and R2 have the meanings indicated in claim 1, as well as the N-oxides of these compounds, the physiologically tolerated acid addition salts of these compounds and the physiologically tolerated acid addition salts of the N-oxides. The invention also relates to a pharmaceutical composition that comprises at least one tetrahydrobenzazepine compound of the formula I, the physically tolerated acid addition salt of I, the N-oxide of compound of the formula I and/or the physically tolerated acid addition salts of the N-oxides of I, and further to the use of a compound according to the present invention for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists.Type: ApplicationFiled: December 17, 2004Publication date: April 23, 2009Inventors: Wilfried Braje, Andreas Haupt, Wilfried Lubisch, Roland Grandel, Karla Drescher, Herve Geneste, Liliane Unger, Daryl R. Sauer
-
Publication number: 20090075978Abstract: The present invention relates to substituted propiolic acid amides, to methods for the production thereof, to medicaments containing these compounds and to the use thereof for producing medicaments.Type: ApplicationFiled: June 26, 2008Publication date: March 19, 2009Applicant: Grunenthal GmbHInventors: Michael HAURAND, Klaus SCHIENE, Sven KUHNERT, Melanie REICH, Saskia ZEMOLKA
-
Publication number: 20090062253Abstract: The present invention relates to compounds and methods useful as modulators of CB2 for the treatment or prevention of disease states including, but not limited to pain, autoimmune disease, malabsorption syndrome, pulmonary disease, osteoporosis, muscle spasm in cancer, neuromuscular disorder, and atherosclerosis progression.Type: ApplicationFiled: August 28, 2008Publication date: March 5, 2009Applicant: KALYPSYS, INC.Inventors: Timothy C. Gahman, Cunxiang Zhao, Hengyuan Lang, Mark Eben Massari
-
Publication number: 20090062258Abstract: The present invention provides a compound represented by the formula (I) and a salt thereof wherein: ring A is a 5-membered aromatic heterocycle optionally having substituent(s); R1 is a hydrogen atom or a hydrocarbon group optionally having substituent(s); W is an oxygen atom or a sulfur atom; X1 and X2 may be the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s) or a heterocyclic group, or, X1 and X2 in combination, optionally, form an oxygen atom, a sulfur atom or ?NR2; ring B is an aromatic ring optionally further having substituent(s); Y is a bond, C1-6 alkylene C2-6 alkenylene or C2-6 alkynylene, optionally having substituent(s); and Z is —SOnR3 or —COR4, which are useful as a pharmaceutical agent having GnRH antagonistic action.Type: ApplicationFiled: February 2, 2006Publication date: March 5, 2009Applicant: Takeda Pharmaceutical Company LimitedInventors: Kazumasa Hamamura, Tsuneo Oda, Tomohiro Kaku, Tomohiro Suzaki
-
Publication number: 20090054402Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.Type: ApplicationFiled: April 16, 2008Publication date: February 26, 2009Applicant: Abbott LaboratoriesInventors: Xilu Wang, Xiaohong Song, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Lisa A. Hasvold, Le Wang, Zhi-Fu Tao, Aaron R. Kunzer
-
Patent number: 7488725Abstract: Compounds are provided having the formula: wherein R1, R2, R2?, R3, R3?, R4, R4?, R5, X, Y and Z are as defined herein.Type: GrantFiled: October 30, 2006Date of Patent: February 10, 2009Assignee: Bristol-Myers Squibb Co.Inventors: Stephen P. O'Connor, Lawrence G. Hamann
-
Publication number: 20080306041Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably ?-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds.Type: ApplicationFiled: January 23, 2006Publication date: December 11, 2008Inventor: David S. Garvey
-
Publication number: 20080306045Abstract: The invention relates to chemical entities of formula (I): and/or pharmaceutically acceptable derivative(s) thereof. The invention also relates to processes for the preparation of compounds of formula (I), pharmaceutical compositions containing compounds of formula (I) and to the use of compounds of formula (I) in medicine, particularly in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.Type: ApplicationFiled: November 22, 2006Publication date: December 11, 2008Inventors: Laure Camus, Reshma Chudasama, Caroline Jane Day, Deepali Deshmukh, John Gerald Gleason, John David Harling, Chao-Pin Lee, Paula Saklatvala, Stefan Senger, Sarah Vallance, John Watson, Nigel Stephen Watson, Robert John Young, Barbara Yuan
-
Publication number: 20080275026Abstract: Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.Type: ApplicationFiled: June 20, 2008Publication date: November 6, 2008Inventors: Peter Hudson, Andrzej Roman Batt, Celine Marguerite Simone Heeney, Andrew John Baxter, Michael Bryan Roe, Peter Andrew Robson
-
Patent number: 7446115Abstract: One aspect of the present invention relates to novel peptidomometic compounds. A second aspect of the present invention relates to the use of the novel peptidomimetic compounds as ligands—agonists or antagonists—for various cellular receptors, e.g., G-protein-coupled receptors and opioid receptors, and various cellular ion channels, e.g., sodium and calcium. In certain embodiments, compounds of the present invention preferentially or selectively inhibit sodium or calcium ion channels. In certain embodiments, compounds of the present invention preferentially or selectively agonize or antagonize ? opioid receptors. In certain embodiments, compounds of the present invention preferentially or selectively inhibit sodium or calcium ion channels and agonize or antagonize ?-opioid receptors.Type: GrantFiled: August 29, 2006Date of Patent: November 4, 2008Assignee: Sepracor, Inc.Inventors: Paul E. Persons, Joanne M. Holland, James R. Hauske
-
Publication number: 20080261951Abstract: This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ?O, —O(CH2)pO— or —S(CH2)S—; W1 is either O or S; X1 and X2 are both H, or together are ?O or ?S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n—; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.Type: ApplicationFiled: June 23, 2008Publication date: October 23, 2008Inventors: Doreen Mary Ashworth, Gary Robert William Pitt, Peter Hudson, Christopher Martyn Yea, Richard Jeremy Franklin
-
Publication number: 20080234251Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.Type: ApplicationFiled: August 17, 2006Publication date: September 25, 2008Applicant: ARRAY BIOPHARMA INC.Inventors: George A. Doherty, C. Todd Eary, Robert D. Groneberg, Zachary Jones
-
Publication number: 20080234250Abstract: The invention concerns compounds according to general formulae 1, wherein G1 is an amine. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents.Type: ApplicationFiled: August 18, 2005Publication date: September 25, 2008Inventor: Gary Robert William Pitt
-
Publication number: 20080221083Abstract: The present invention relates generally to amide containing heterobicyclic containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-3 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13 and MMP-3 inhibitors.Type: ApplicationFiled: November 20, 2007Publication date: September 11, 2008Inventors: Matthias Hochgurtel, Harald Bluhm, Heiko Kroth, Michael Essers, Christian Gege, Arthur Taveras
-
Patent number: 7419975Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula IType: GrantFiled: April 6, 2005Date of Patent: September 2, 2008Assignee: Novartis AGInventors: Mark Gabriel Palermo, Sushil Kumar Sharma, Christopher Straub, Run-Ming Wang, Leigh Scott Zawel, Yanlin Zhang, Zhuoliang Chen, Yaping Wang, Fan Yang, Wojciech Wrona, Gang Liu, Mark G. Charest, Feng He
-
Patent number: 7410961Abstract: The present invention is further directed to compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R16, R17, R18, R19, R20, R21 and R22 are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.Type: GrantFiled: January 14, 2005Date of Patent: August 12, 2008Assignee: Merck & Co., Inc.Inventors: Lihu Yang, Sander G. Mills, Changyou Zhou, Stephen D. Goble, Alexander Pasternak
-
Publication number: 20080161287Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.Type: ApplicationFiled: October 25, 2007Publication date: July 3, 2008Applicant: Takeda Pharmaceutical Company, LtdInventors: Mitsuru Shiraishi, Masanori Baba, Katsuji Aikawa, Naoyuki Kanzaki, Masaki Seto, Yuji Lizawa
-
Publication number: 20080153805Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R1, R2, R3, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: ApplicationFiled: December 6, 2007Publication date: June 26, 2008Inventors: Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander
-
Patent number: 7390798Abstract: The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache.Type: GrantFiled: February 9, 2005Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Theresa M. Williams, Christopher S. Burgey, Thomas J. Tucker, Craig A. Stump, Ian M. Bell
-
Patent number: 7375100Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: June 3, 2004Date of Patent: May 20, 2008Assignee: Pfizer IncInventors: Alan Daniel Brown, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite
-
Patent number: 7368444Abstract: The present invention relates to the compound presented by formula (I) (wherein all symbols in formula (I) are the same mean as the description shown in the specification.), mitocondorial benzogeazepin receptor (MBR) antagonist comprising the compound, the preventive and/or treatment medicine against diseases caused by stress of which an active ingredient is the compound. Since the compound represented by formula (I) has MBR antagonistic activity, and controls the production of neurosteroid, it is useful as the preventive and/or treatment medicine against diseases caused by stress.Type: GrantFiled: February 13, 2003Date of Patent: May 6, 2008Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Takuya Seko, Seishi Katsumata, Masashi Kato, Jun-ichiro Manako, Kazuyuki Ohmoto
-
Patent number: 7365196Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.Type: GrantFiled: March 15, 2001Date of Patent: April 29, 2008Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
-
Patent number: 7304051Abstract: Amidophenyl-sulfonylamino-quinoxaline compounds of formula (I) are CCK2 modulators useful in the treatment of CCK2 mediated diseases.Type: GrantFiled: August 4, 2004Date of Patent: December 4, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Brett D. Allison, Michael D. Hack, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen
-
Patent number: 7304050Abstract: Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I as disclosed herein can be used in a variety of applications, including using the invention compounds to treat bacterial infections.Type: GrantFiled: September 1, 2004Date of Patent: December 4, 2007Assignee: Pfizer Inc.Inventors: Susan Hagen, Vara Prasad Venkata Nagendra Josyula
-
Patent number: 7288651Abstract: Certain methods are disclosed that are useful in the preparation of CCK2 active amidophenyl-sulfonylamino-quinoxaline compounds of the formula: wherein R1, R2, Ra and Rb are defined.Type: GrantFiled: August 4, 2004Date of Patent: October 30, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Xiaohu Deng, Jimmy T. Liang, Neelakandha Mani, Chennagiri R. Pandit
-
Patent number: 7262185Abstract: The present invention provides a novel benzazepine derivative represented by formula: wherein, R1 is a 5- or 6-membered aromatic ring, R2 is lower alkyl group, etc., Y is an optionally substituted imino group, ring A and ring B are independently an optionally substituted aromatic ring, W is formula —W1—X2—W2— (W1 and W2 are independently S(O)m1 (m1 is 0, 1, or 2), etc., and X2 is an optionally substituted alkylene group etc.), a preparation method and use thereof.Type: GrantFiled: August 7, 2002Date of Patent: August 28, 2007Assignee: Takeda Chemical Industries Ltd.Inventors: Mitsuru Shiraishi, Masanori Baba, Masaki Seto, Yoshio Aramaki, Naoyuki Kanzaki, Naoki Miyamoto, Yuji Iizawa
-
Patent number: 7238685Abstract: The invention relates to novel benzo-fused heterocycles and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.Type: GrantFiled: July 31, 2002Date of Patent: July 3, 2007Assignee: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, Christoph Boss, Martine Clozel, Walter Fischli, Thomas Weller, Judith Marfurt
-
Patent number: 7192950Abstract: The invention relates to novel benzazepines and related heterocyclic derivatives (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.Type: GrantFiled: December 19, 2001Date of Patent: March 20, 2007Assignee: Actelion Pharmaceuticals, Ltd.Inventors: Hamed Aissaoui, Martine Clozel, Thomas Weller, Ralf Koberstein, Thierry Sifferlen, Walter Fischli
-
Patent number: 7183271Abstract: A novel 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivative or a pharmaceutically acceptable salt thereof, which is useful as an agent for treating or preventing nocturia and/or diabetes insipidus, is provided.Type: GrantFiled: April 26, 2004Date of Patent: February 27, 2007Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Koshio, Issei Tsukamoto, Akio Kakefuda, Seijiro Akamatsu, Chikashi Saitoh
-
Patent number: 7176195Abstract: Compounds according to general formulae (1 and 2), wherein G1 is an azepine derivative and G2 is a group according to general formulae (9–11) are new. Compounds according to the invention are vasopressin V2 receptor agonists.Type: GrantFiled: June 21, 2001Date of Patent: February 13, 2007Assignee: Ferring BVInventors: Doreen Ashworth, Gary R. W. Pitt, Peter Hudson, Christopher Yea, Richard J. Franklin, Graeme Semple, David Paul Jenkins
-
Patent number: 7169772Abstract: 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivatives, which have excellent arginine vasopressin V2 activity and are useful for a drug for the treatment of central diabetes insipidus and/or nocturia.Type: GrantFiled: November 13, 2002Date of Patent: January 30, 2007Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Koshio, Issei Tsukamoto, Takahiro Kuramochi, Seijiro Akamatsu, Chikashi Saitoh
-
Patent number: 7141562Abstract: Compound of the Formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein: X is CH or N, Y is C or S, Z is —SO2— or —(CRaRb)r—, n is 1 or 2, R2 is aryl or heteroaryl, and R1, R3, R4, R5, R6, R7, R8, R9, Ra, Rb, m, p, q and r, are as defined herein. The compounds are modulators of the 5-HT6 receptor and are useful for treatment of central nervous system disorders. Also provided are methods for preparing, compositions comprising, and methods for using Compounds of Formula I.Type: GrantFiled: November 6, 2003Date of Patent: November 28, 2006Assignee: Roche Palo Alto LLCInventors: Hans Maag, Meng Sui, Shu-Hai Zhao
-
Patent number: 7101869Abstract: Novel compounds according to the formula and pharmaceutically acceptable salts, solvates, or hydrates thereof; wherein each occurrence of A is independently selected from CH or N; X is selected from the group consisting of —CH2—, —O—, —NH—, (C1-C6)alkylamino-, (C1-C6)alkylaminocarbonylamino-, (C1-C6)alkylcarbonylamino-, (C1-C6)alkylsulfonylamino-, phenylsulfonylamino-, carbonyl, —NH—C(O)—, —N(C1-C6)alkyl-C(O)—, —S(O)y— where y is 0, 1 or 2, and; n in —(CH2)n— is 1, 2 or 3; and R1, R2, and R3 are as described herein; pharmaceutical compositions that including these compounds, and methods for the treatment of autoimmune disease, inflammation, allergy, transplant rejection, and other circumstances where administration of an immunosuppressive agent is of therapeutic benefit.Type: GrantFiled: November 22, 2002Date of Patent: September 5, 2006Assignee: Pfizer Inc.Inventors: Todd A. Blumenkopf, Eileen Elliott Mueller, Eric Jan Roskamp
-
Patent number: 7091199Abstract: The compounds are of the class of thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.Type: GrantFiled: September 13, 2000Date of Patent: August 15, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: George E. Lee, John G. Jurcak, Timothy A. Ayers
-
Patent number: 7091352Abstract: Compounds of the formula (I) below, or pharmacologically acceptable salts, esters or other derivatives thereof: wherein A is furan, thiophene, pyrazole, imidazole, isoxazole or isothiazole; R1 is a substituted or unsubstituted aryl or a substituted or unsubstituted heteroaryl; R2 is a substituted or unsubstituted heteroaryl; and R3 is a bicyclic amino group; provided that the substituents R1 and R2 are bonded to the two atoms of the cyclic group A which are adjacent to the atom of the cyclic group A to which the substituent R2 is bonded. The compounds inhibit the production of inflammatory cytokines.Type: GrantFiled: July 22, 2003Date of Patent: August 15, 2006Assignee: Sankyo Company, LimitedInventors: Tomio Kimura, Akira Nakao
-
Patent number: 7074781Abstract: This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ?O, —O(CH2)pO— or —S(CH2)pS—; W1 is either O or S; X1 and X2 are both H, or together are ?O or ?S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n—; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.Type: GrantFiled: January 4, 2001Date of Patent: July 11, 2006Assignee: Ferring BVInventors: Doreen Mary Ashworth, Gary Robert William Pitt, Peter Hudson, Christopher Martyn Yea, Richard Jeremy Franklin
-
Patent number: 7067513Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as aggression, anxiety disorders, autism, vertigo, depression, disturbances of cognition, disturbances of memory, Parkinson's disease, schizophrenia, and psychotic disorders. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0–2; R5 and R6 are independently H or alkyl (1–3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3–5, and R7 is alkyl (1–3C), alkoxy (1–3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2–4, and salts thereof.Type: GrantFiled: August 22, 2000Date of Patent: June 27, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Roelof Van Hes, Johannes A. M. Van der Heijden, Cornelis G Kruse, Jacobus Tipker, Martinus T. M Tulp, Gerben M Visser, Bernard J Van Vliet
-
Patent number: 7008938Abstract: A benzene-fused heteroring derivative 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 immune diseases (autoimmune diseases, infectious diseases, etc.), inflammatory diseases (inflammatory bowel diseases, multiple cerebrosclerosis, arthritis, etc.), nerve degeneration diseases (Alzheimer's disease, muscular dystrophy, etc.), bone resorption diseases (osteoporosis, etc.), respiratory system diseases, diabetes, shock, etc.Type: GrantFiled: July 29, 2004Date of Patent: March 7, 2006Assignee: Nokia CorporationInventors: Kazuyuki Ohmoto, Iori Itagaki
-
Patent number: 6995154Abstract: The invention provides compounds of formula I: wherein R1 to R5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds, compositions, or salts to treat cancer. In embodiments, R4 and R5 taken together can be a 3, 4, or 5 membered saturated or unsaturated chain comprising members selected from the group consisting of non-peroxide oxygen, sulfur, N(X), and carbon, optionally substituted by oxo; wherein each X is independently absent or is H, O, (C1–C4)alkyl, phenyl or benzyl; and wherein at least one of the chain members is an N—H group.Type: GrantFiled: October 21, 2003Date of Patent: February 7, 2006Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Jung Sun Kim, Leroy Fong Liu
-
Patent number: 6972286Abstract: The present invention provides oxazolidinones having a benzannelated 6- or 7-membered heterocycle as antibacterial agents.Type: GrantFiled: November 14, 2001Date of Patent: December 6, 2005Assignee: Pharmacia and Upjohn CompanyInventors: Paul D. Johnson, Paul Adrian Aristoff, Toni-Jo Poel, Lisa Marie Thomasco
-
Patent number: 6953787Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.Type: GrantFiled: April 10, 2003Date of Patent: October 11, 2005Assignee: Arena Pharmaceuticals, Inc.Inventors: Brian Smith, Jeffrey Smith
-
Patent number: 6936602Abstract: Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R1 is a 5- to 6-membered aromatic ring which bears a substituent represented by the general formula: R-Z1-X-Z2- (wherein R1 is hydrogen or optionally substituted hydrocarbyl; X is optionally substituted alkylene; and Z1 and Z2 are each a heteroatom) and may be further substituted, with R being optionally bonded to the aromatic ring to form another ring; Y is optionally substituted imino; and R2 and R3 are each optionally substituted aliphatic hydrocarbyl or an optionally Substituted hetero-alicyclic group.Type: GrantFiled: June 15, 2000Date of Patent: August 30, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Masanori Baba, Yoshio Aramaki, Naoyuki Kanzaki, Osamu Nishimura
-
Patent number: 6924280Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.Type: GrantFiled: February 21, 2003Date of Patent: August 2, 2005Assignee: Pfizer Inc.Inventors: Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
-
Patent number: 6919332Abstract: The present invention relates to N-substituted-heteroaryloxy-aryloxy-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, A, Y, B, G, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.Type: GrantFiled: April 28, 2003Date of Patent: July 19, 2005Assignee: Pfizer Inc.Inventors: Mark C. Noe, Lilli Ann Wolf-Gouveia