Polycyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/213.01)
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Publication number: 20080199522Abstract: The present invention was completed based on these discoveries and relates to in a hydrogel-forming compression-coated solid pharmaceutical preparation comprising a core tablet containing drug and outer layer made from hydrogel-forming polymer substance and hydrophilic base, the improvement, a timed-release compression-coated solid composition for oral administration, said composition comprising (1) drug and freely erodible filler are mixed with the core tablet, (2) the percentage erosion of the core tablet is approximately 40 to approximately 90%, and (3) the outer layer essentially does not contain the same drug as the above-mentioned drug. By releasing a drug after a specific lag time, it becomes possible to effectively deliver a drug to a specific site in the digestive tract.Type: ApplicationFiled: August 20, 2007Publication date: August 21, 2008Applicant: Astellas Pharma, Inc.Inventors: Toyohiro Sawada, Kazuhiro Sako, Tatsunobu Yoshioka, Shunsuke Watanabe
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Publication number: 20080188458Abstract: The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: ApplicationFiled: January 30, 2008Publication date: August 7, 2008Inventors: Kap-Sun Yeung, John F. Kadow, Katharine A. Grant-Young
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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
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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
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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
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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
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Publication number: 20080085296Abstract: An apparatus and method for reducing post-operative ileus and/or gastric stasis is described. The method can include applying to the intestine a therapeutically effective amount of a composition comprising a drug that is effective in reducing post-operative ileus and/or gastric stasis, such as by introducing the composition through a surgical access device, such as a trocar or endoscope. The apparatus can include a sheet of material, a surgical fastener, or a buttress comprising the composition.Type: ApplicationFiled: September 18, 2007Publication date: April 10, 2008Inventors: Darrel M. Powell, Mark Pomeroy, Michael A. Murray, Carl J. Shurtleff
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Patent number: 7335677Abstract: Novel compounds that are inhibitors of one or most post-proline cleaving proteases, e.g. dipeptidyl peptidase IV, according to general formula (1). R1 is H or CN, X1 is O, S, CH2, CHF, CF2, CH(CH3), C(CH3)2 or CH(CN), and b is 1 or 2. G1 is H or a group according to the formula —CH2—X2—(CH2)a-G3 and G2 is H or a group according to the formula —CH2—(CH29a-G3, provided that one of G1 and G2 is H and the other is not H. X2 is O, S, or CH2, and a is 0, 1 or 2, provided that when a is 1 then X2 is CH2. G3 is a group according to one of general formulae 2-4, where the variables have meaning given in the description. The compounds are useful in the treatment of i.a.Type: GrantFiled: October 23, 2002Date of Patent: February 26, 2008Assignee: Ferring B.V.Inventors: David M. Evans, Doreen M. Ashworth
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Publication number: 20080026081Abstract: The present invention relates to methods of treatment using the compound (+)-isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)-1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylate, as a sole active agent or in combination with other pharmacological agents.Type: ApplicationFiled: November 19, 2004Publication date: January 31, 2008Inventors: Axel Unterbeck, Michael De Vivo, Gregory M. Rose
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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
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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
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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
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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
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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
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Patent number: 7169773Abstract: The present invention provides a compound of formula I comprising: a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof.Type: GrantFiled: June 30, 2005Date of Patent: January 30, 2007Assignee: SmithKline Beecham CorporationInventors: Jerzy Ryszard Szewczyk, Kelly H. Donaldson
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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
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Patent number: 7160876Abstract: Compounds of formula (I) wherein n is 0, 1, or 2; X is O, S, —NH—, and —N-alkyl-; Ar1 is a 6-membered aromatic ring; and Ar2 is a fused bicycloheterocycle. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formula (I) and methods for using such compounds and compositions.Type: GrantFiled: December 22, 2003Date of Patent: January 9, 2007Assignee: Abbott LaboratoriesInventors: Jianguo Ji, Tao Li
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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
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Patent number: 7067510Abstract: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1–C4 alkyl), —OCOC6H5, —OCO(C1–C6 alkyl), or —OSO2(C2–C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1–C4 alkyl), —OCOC6H5, —OCO(C1–C6 alkyl), —OSO2(C2–C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; X is —S— or —HC?CH—; G is —O—, —S—, —SO—, SO2, or —N(R5)—, wherein R5 is —H or C1–C4 alkyl; and Y is —O—, —S—, —NH—, —NMe-, or —CH2—; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.Type: GrantFiled: July 11, 2003Date of Patent: June 27, 2006Assignee: Eli Lilly and CompanyInventor: Owen Brendan Wallace
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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
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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
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Patent number: 6953791Abstract: 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: October 11, 2005Assignee: Pfizer, Inc.Inventors: Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
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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
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Patent number: 6855707Abstract: Disclosed are methods for modifying or regulating at least one of glucose or lipid metabolism disorders which comprises administering to a human or vertebrate subject a D1 dopamine agonist in conjunction with a dopamine D2 agonist where the conjoined administration is effective to improve at least one of the following lipid and glucose metabolic indices: body weight, body fat, plasma insulin, plasma glucose and plasma lipid, and plasma lipoprotein. In preferred embodiments, the administration of the D1 dopamine agonist and the D2 dopamine agonist is conducted at a predetermined time.Type: GrantFiled: September 10, 2001Date of Patent: February 15, 2005Assignee: Pliva D.D.Inventor: Anthony H. Cincotta
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Patent number: 6815440Abstract: Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and -carboxylic acids Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course of which is involved an increased activity of matrix-degrading metalloproteinases.Type: GrantFiled: March 3, 2003Date of Patent: November 9, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Eckart Bartnik, Klaus-Ulrich Weithmann
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Patent number: 6812345Abstract: Compounds of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids such as lowering LDL cholesterol and/or increasing HDl cholesterol, and treating hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis and pharmaceutically acceptable salts thereof, wherein X is O, S, SO, SO2 or NR7; Z is n is 0 or 1; R1 and R2 are the same or different and are independently selected from alkyl, arylalkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, heteroaryl or cycloheteroalkyl; and R3 to R10 are as defined herein.Type: GrantFiled: June 24, 2003Date of Patent: November 2, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Jeffrey A. Robl, Bang-Chi Chen, Chong-Qing Sun
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Patent number: 6809092Abstract: 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 22, 2002Date of Patent: October 26, 2004Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kazuyuki Ohmoto, Iori Itagaki
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Patent number: 6762178Abstract: Hydroxamic acids having the formula are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.Type: GrantFiled: June 14, 2001Date of Patent: July 13, 2004Assignee: Wyeth Holdings CorporationInventors: Jeremy I. Levin, James M. Chen
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Patent number: 6686351Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-&bgr;. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.Type: GrantFiled: February 27, 2002Date of Patent: February 3, 2004Assignee: Signal Pharmaceuticals, Inc.Inventors: Shripad S. Bhagwat, Leah M. Gayo-Fung, Qi Chao
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Patent number: 6667302Abstract: 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, 0, (C1-C4)alkyl, phenyl or benzyl; and wherein at least one of the chain members is an N—H group.Type: GrantFiled: June 13, 2001Date of Patent: December 23, 2003Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. La Voie, Jung Sun Kim, Leroy Fong Liu
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Patent number: 6638925Abstract: New derivatives of benzazepine, particularly of benzofuro[3a,3,2,ef][2]benzazepin of the general formula (I) and new compounds of the general formula (III) Drugs, containing compounds of formulas (I) and/or (III), which can be used successfully for the treatment of Alzheimer's disease and related dementia conditions, as well as for the treatment of Langdon-Down syndrome, are also described.Type: GrantFiled: February 11, 1999Date of Patent: October 28, 2003Assignee: Sanochemia Ltd.Inventors: Laszlo Czollner, Johannes Frohlich, Ulrich Jordis, Bernhard Kuenburg
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Patent number: 6630463Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): wherein A represents, for example, a heteroaryl group which contains at least one nitrogen atom and may have a substituent, B represents, for example, a heteroarylene group, a —CONH— group or a group represented by the formula —CR6═CR7— in which R6 and R7 represents H, a lower alkyl group or the like, D represents an arylene group, a heteroarylene group or the like, n1 stands for 0 or 1, M represents, for example, a hydroxyl group or a lower alkoxy group; or a physiologically acceptable salt thereof. As a retinoic-related compound replacing retinoic acid, it permits the provision of a preventive and/or therapeutic for various diseases.Type: GrantFiled: July 23, 2001Date of Patent: October 7, 2003Assignee: Eisai Co. Ltd.Inventors: Kouichi Kikuchi, Katsuya Tagami, Hiroyuki Yoshimura, Shigeki Hibi, Mitsuo Nagai, Shinya Abe, Makoto Okita, Takayuki Hida, Seiko Higashi, Naoki Tokuhara, Seiichi Kobayashi
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Patent number: 6627636Abstract: Compounds of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids such as lowering LDL cholesterol and/or increasing HDl cholesterol, and treating hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis and pharmaceutically acceptable salts thereof, wherein X is O, S, SO, SO2 or NR7; Z is n is 0 or 1; R1 and R2 are the same or different and are independently selected from alkyl, arylalkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, heteroaryl or cycloheteroalkyl; and R3 to R10 are as defined herein.Type: GrantFiled: December 4, 2001Date of Patent: September 30, 2003Assignee: Bristol-Myers Squibb CompanyInventor: Jeffrey A. Robl
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Patent number: 6602864Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.Type: GrantFiled: June 3, 1998Date of Patent: August 5, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Yong Mi Choi-Sledeski, Henry W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong
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Patent number: 6593322Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially ER-&bgr;. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natureal hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.Type: GrantFiled: September 21, 2000Date of Patent: July 15, 2003Assignee: Signal Pharmaceuticals, Inc.Inventors: Shripad S. Bhagwat, Leah Marie Gayo-Fung, Bernd M. Stein, Qi Chao, Anthony R. Gangloff, Jeffrey A. McKie, Kenneth D. Rice
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Patent number: 6562828Abstract: A compound of the formula [I] wherein R1, R2 and R3 are the same or different and each is hydrogen atom, wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof. The compound of the present invention, a salt thereof and a prodrug thereof are useful as factor Xa inhibitor and blood coagulation inhibitor, and are useful for the prophylaxis and/or treatment of diseases caused by blood coagulation or thrombus.Type: GrantFiled: October 6, 2000Date of Patent: May 13, 2003Assignee: Japan Tobacco Inc.Inventors: Susumu Katoh, Katsuyuki Yokota, Mikio Hayashi
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Patent number: 6534496Abstract: The object of the present invention is to provide a prophylactic and/or therapeutic drug for obesity and obesity-associated diseasestor diabetes with a reduced risk for central side effects and high universality in usage. Another object of the present invention is to provide a pharmaceutical composition comprising a compound of the following formula: wherein Ar represents phenyl which may be substituted and/or condensed; n represents an integer of 1 to 10; R represents hydrogen or a hydrocarbon group which may be substituted, which may not be the same in its n occurrences; R may be bound to either Ar or a substituent for Ar; Y represents an amino group which may be subsituted or a nitrogen-containing saturated heterocyclic group which may be substituted, or a salt thereof, which can be used for a thermogenic agent, an antiobesity agent, a lipolytic agent, or a prophylactic and/or treating drug for obesity-associated diseases.Type: GrantFiled: October 7, 1999Date of Patent: March 18, 2003Assignee: Takeda Chemical Industries, Inc.Inventors: Yuji Ishihara, Yukio Fujisawa, Naoki Furuyama
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Patent number: 6525043Abstract: The present invention relates to the use of a particular class of chemical compounds as modulators of SKCa, IKCa and BKCa channels, and to pharmaceutical compositions comprising the SK/IK/BK channel modulating agents.Type: GrantFiled: October 25, 2001Date of Patent: February 25, 2003Assignee: NeuroSearch A/SInventors: Bo Skaaning Jensen, Lene Teuber, Dorte Strobaek, Palle Christophersen, Soren Peter Olesen
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Patent number: 6514964Abstract: The invention comprises novel compounds that are effective in the prophylaxis and treatment of diseases, such as integrin receptors mediated diseases, in particular, diseases or conditions mediated by integrin receptors, such as &agr;v&bgr;3, &agr;v&bgr;5, &agr;v&bgr;6 and the like. The invention encompasses novel compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of such diseases and disorders. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: September 26, 2000Date of Patent: February 4, 2003Assignee: Amgen Inc.Inventors: Zhidong Chen, Celia Dominguez, Ellen Grenzer-Laber, Nianhe Han, Longbing Liu, Ofir A. Moreno, Melvin C. Rutledge, Andrew S. Tasker
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Patent number: 6495542Abstract: A compound of formula (I): wherein A is an optionally substituted heterocyclic group, R is a lower alkoxy; Z is C═O or CH2; and B is benzazapinyl, which may be optionally substituted, or a salt thereof, that possesses vasopressin antagonistic activity and is useful as a vasopressin antagonist.Type: GrantFiled: October 16, 2000Date of Patent: December 17, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Yuki Sawada, Kazuhiko Osoda, Teruo Oku
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Patent number: 6468971Abstract: Kappa-opioid agonists prevent the impairment of renal function otherwise caused by the combination of gaseous anesthesia and surgery or severe trauma. Not only do these agents preserve renal function and maintain urine output, they also maintain plasma electrolyte concentration and osmolality by reducing renal loss of sodium and potassium when compared to other diuretic agents. The preservation of urine flow as well as the ability to retain body sodium, potassium, calcium, and osmolality during surgery or severe trauma under gaseous anesthesia are novel and unique properties associated only with kappa opioid agonists. To date, no other clinically-used diuretic agent has been shown to provide constant urine flow, or to retain electrolytes during anesthesia and surgery. The kappa opioid agonists may be used in surgical patients with normal cardiovascular function, but are particularly useful in patients with compromised cardiovascular and/or renal function.Type: GrantFiled: September 2, 1998Date of Patent: October 22, 2002Assignee: Board of Supervisors of Louisiana State University and Agricultural and Mechanical CollegeInventor: Daniel R. Kapusta
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Patent number: 6436923Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-&bgr;. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.Type: GrantFiled: March 17, 2000Date of Patent: August 20, 2002Assignee: Signal Pharmaceuticals, Inc.Inventors: Shripad S. Bhagwat, Leah M. Gayo-Fung, Bernd M. Stein, Qi Chao, Anthony R. Gangloff, Jeffrey A. McKie, Kenneth D. Rice
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Publication number: 20020103234Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): 1Type: ApplicationFiled: July 23, 2001Publication date: August 1, 2002Applicant: Eisai Co. Ltd.Inventors: Kouichi Kikuchi, Katsuya Tagami, Hiroyuki Yoshimura, Shigeki Hibi, Mitsuo Nagai, Shinya Abe, Makoto Okita, Takayuki Hida, Seiko Higashi, Naoki Tokuhara, Seiichi Kobayashi
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Patent number: 6413955Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.Type: GrantFiled: October 2, 2000Date of Patent: July 2, 2002Assignee: Merck & Co., Inc.Inventors: Ben C. Askew, Garry R. Smith
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Publication number: 20020065266Abstract: The present invention relates to the use of a particular class of chemical compounds as modulators of SKCa, IKCa and BKCa channels, and to pharmaceutical compositions comprising the SK/IK/BK channel modulating agents.Type: ApplicationFiled: October 25, 2001Publication date: May 30, 2002Inventors: Bo Skaaning Jensen, Lene Teuber, Dorte Strobaek, Palle Christophersen, Soren Peter Olesen
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Publication number: 20020065284Abstract: This invention is directed to compounds of the formula 1Type: ApplicationFiled: March 30, 2001Publication date: May 30, 2002Inventors: Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
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Patent number: 6380184Abstract: Benzoazepines of the following formula wherein R1, R1a, R2, R9k, L, Q, X, Y and Z are as described herein, and analogs thereof are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.Type: GrantFiled: October 12, 1999Date of Patent: April 30, 2002Assignee: Bristol-Myers Squibb Co.Inventor: James J. Li
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Publication number: 20020049194Abstract: A benzoheterocyclic derivative of the following formula [1]: 1Type: ApplicationFiled: June 6, 2001Publication date: April 25, 2002Inventors: Hidenori Ogawa, Kazumi Kondo, Hiroshi Yamashita, Keizo Kan, Takayuki Matsuzaki, Tomoichi Shinohara, Yoshihisa Tanada, Muneaki Kurimura, Michiaki Tominaga, Yoichi Yabuuchi
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Patent number: 6369221Abstract: Disclosed are thiazolobenzoheterocycles of the general formula Including their isomers, racemates, enantioners and salts thereof, as well as processes for preparing these compounds and medicaments containing them.Type: GrantFiled: January 18, 2000Date of Patent: April 9, 2002Assignee: Aventis Pharma S.A.Inventors: Jean-Claude Hardy, Jean Bouquerel, Patrick Nemecek, Jean-François Peyronel
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Publication number: 20020028802Abstract: The subject matter of the present invention concerns a process for the isolation of the alkaloid galanthamine; the galanthamine itself which has been produced according to this process; the use of the galanthamine thus produced in galenic preparations; and the galanthamine thus produced for treating narrow-angle glaucoma, Alzheimer's disease, as well as alcohol and nicotine dependence.Type: ApplicationFiled: November 9, 2001Publication date: March 7, 2002Inventors: Thomas Hille, Hans-Rainer Hoffmann, Mirko Kreh, Rudolf Matusch