1,4-thiazines Patents (Class 544/56)
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Patent number: 10968174Abstract: The present invention pertains generally to the field of chemical synthesis, and more particularly to methods for the chemical synthesis of a thiosulfonic acid of Formula (1) by a step of periodate mediated oxidative coupling of a thiosulfonic acid of Formula (2) with an aniline of Formula (3), as described herein. The present invention also relates to such methods which incorporate one or more additional (subsequent and/or preceding) steps, for example, to prepare compounds of Formula (5) from compounds of Formula (1); to prepare compounds of Formula (6) from compounds of Formula (5); and to prepare compounds of Formula (2) from compounds of Formula (4), as described herein.Type: GrantFiled: December 21, 2017Date of Patent: April 6, 2021Assignee: WisTa Laboratories Ltd.Inventors: James Peter Sinclair, Sarah Louise Nicoll, John Mervyn David Storey, Christopher Paul Larch
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Patent number: 9072758Abstract: [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogues and a prophylactic and/or therapeutic agent against diabetes, obesity, or the like. [Means of solving the problem] A compound of Formula (III): (where f is 0 to 2; g is 1 to 4; j is 0 to 3; k is 0 to 2; n is 0 to 2; p is 0 to 4; h is 0 to 3; q1 id 0 to 3; q2 is 0 or 1; r1 is 0 to 2 (with the proviso that q1+q2+r1 is 0 to 5); J1a is —CR11a—, N; J2 is —CR12aR12b—, —CR12c—; T is —CH2—, O, —S(O)i— (i is an integer of 0 to 2) or —NR7—; X is O, S, or —NR7—; ring A?? is a benzene ring, a pyridine ring; ring B? is a benzene ring, a pyridine ring, a pyrimidine ring; and R1 to R14 are specific groups), a salt of the compound, or a solvate of the salt or the compound.Type: GrantFiled: April 11, 2012Date of Patent: July 7, 2015Assignee: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Akihiro Okano, Munetaka Ohkouchi, Muneyoshi Makabe
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Patent number: 9040525Abstract: [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogues and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (1): (where n is 0 to 2; p is 0 to 4; h is 0 to 3; j is 0 to 3; k is 0 to 2; a ring B is an aryl group or a heteroaryl group; X is O, S, or —NR7—; J1 is —CR11aR11b— or —NR11c—; J2 is —CR12aR12b— or —NR12c—; and R1 to R12c are specific groups), a salt of the compound, or a solvate of the salt or the compound.Type: GrantFiled: October 11, 2011Date of Patent: May 26, 2015Assignee: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Akihiro Okano, Munetaka Ohkouchi, Muneyoshi Makabe
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Publication number: 20150141413Abstract: The present invention provides a compound of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.Type: ApplicationFiled: May 21, 2013Publication date: May 21, 2015Inventors: Hans Hilpert, Thomas Woltering
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Patent number: 9006234Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic[4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: GrantFiled: July 2, 2012Date of Patent: April 14, 2015Assignee: Medivation Technologies, Inc.Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty
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Publication number: 20140001443Abstract: Embodiments of the present invention are directed to a compound represented by Formula 1 below and an organic light-emitting device including the compound.Type: ApplicationFiled: November 13, 2012Publication date: January 2, 2014Applicant: Samsung Display Co. Ltd.Inventors: Jung-Sub Lee, Seung-Gak Yang
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Patent number: 8546381Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: GrantFiled: March 24, 2009Date of Patent: October 1, 2013Assignee: Medivation Technologies, Inc.Inventors: David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain
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Patent number: 8232391Abstract: Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection.Type: GrantFiled: July 9, 2010Date of Patent: July 31, 2012Assignee: Janssen Pharmaceutica NVInventors: Brett D. Allison, Laurent Gomez, Cheryl A. Grice, Michael D. Hack, Brian J. Morrow, S. Timothy Motley, Alejandro Santillan, Jr., Karen J. Shaw, Kimberly L. Schwarz, Liu Y. Tang, Hariharan Venkatesan, John J. M. Wiener
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Publication number: 20120041193Abstract: Disclosed herein are vinyl-bromides, vinyl-boronic acids and vinyl-boronic acid derivatives useful as synthetic intermediates for the preparation of therapeutic agents. Also disclosed are methods of synthesis of vinyl-bromides, vinyl-boronic acids and vinyl-boronic acid derivatives.Type: ApplicationFiled: August 10, 2011Publication date: February 16, 2012Applicant: Frontier Scientific, Inc.Inventors: Shivanand K. Math, Homayoun H. Mokri, James B. LaMunyon, Dustin R. Cefalo, Charles A. Testa
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Aminothiolester compounds, pharmaceutical and cosmetic compositions containing same and uses thereof
Patent number: 8026231Abstract: The invention relates to novel aminothiol ester compounds having the general formula (I): and to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (cancers and precancers, dermatological, rheumatic and ophthalmological complaints in particular) or in cosmetic compositions. The invention also relates to a pharmaceutical or cosmetic composition, characterized in that it comprises, as active agent, a compound of general formula (I) in combination with a pharmaceutically or cosmetically acceptable support.Type: GrantFiled: March 28, 2006Date of Patent: September 27, 2011Assignee: CNRSInventors: Guy Fournet, Gerard Anthony Quash, Jacques Gore -
Patent number: 7947675Abstract: Compounds of the formula (I), in which the radicals R1 to R3 and AR are as defined in the description, processes for the preparation thereof, the use thereof in the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.Type: GrantFiled: February 16, 2006Date of Patent: May 24, 2011Assignee: Merck Patent GmbHInventors: Bruno Roux, Isabelle Berard
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Patent number: 7939537Abstract: Pyridopyrimidine carboxamide compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein R1, R2, R3, R4, R5 and R6 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: September 26, 2006Date of Patent: May 10, 2011Assignee: Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.p.A.Inventors: Vincenzo Summa, Olaf Kinzel, Monica Donghi
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Publication number: 20110003794Abstract: The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.Type: ApplicationFiled: August 30, 2010Publication date: January 6, 2011Inventor: Brian A Johns
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Patent number: 7763602Abstract: Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).Type: GrantFiled: June 11, 2008Date of Patent: July 27, 2010Assignee: Lupin LimitedInventors: Sudershan Kumar Arora, Neelima Sinha, Sanjay Jain, Ram Shankar Upadhayaya, Gourhari Jana, Shankar Ajay, Rakesh Kumar Sinha
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Patent number: 7728027Abstract: The present disclosure generally relates to a process for synthesizing methyl ((1S)-1-(((2S)-2-(5-(4?-(2-((2S)-1-((2S)-2-((methoxycarbonyl)amino)-3-methylbutanoyl)-2-pyrrolidinyl)-1H-imidazol-5-yl)-4-biphenylyl)-1H-imidazol-2-yl)-1-pyrrolidinyl)carbonyl)-2-methylpropyl)carbamate dihydrochloride salt. The present disclosure also generally relates to intermediates useful in this process.Type: GrantFiled: July 17, 2008Date of Patent: June 1, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Shawn K. Pack, Peng Geng, Michael J. Smith, Jason Hamm
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Publication number: 20100125068Abstract: The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim kinases, and tyrosine kinase using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with protein kinases using such compounds.Type: ApplicationFiled: January 15, 2010Publication date: May 20, 2010Inventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, David A. Parry
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Patent number: 7705042Abstract: The invention relates to arylamide and hetereoarylamide compounds of Formula I: wherein A, X, R2 and W are set forth in the specification, as well as tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: GrantFiled: October 20, 2005Date of Patent: April 27, 2010Assignee: Janssen Pharmaceutica NVInventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Sanath Meegalla, Jonathan Rudolph, Mark J. Wall, Kenneth J. Wilson, Renee DesJarlais, Carl L. Manthey, Christopher M. Flores, Christopher J. Molloy
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Publication number: 20100099667Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: March 24, 2009Publication date: April 22, 2010Inventors: David T. Hung, Andrew Asher Protter, Sarjavit Chakravarty, Rajendra Parasmal Jain
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Patent number: 7671198Abstract: The invention provides 8-azabicyclo[3.2.1 ]octyl intermediates useful for the preparation of 5-HT4 receptor agonist compounds. The invention also provides processes for the preparation of such useful intermediates.Type: GrantFiled: February 15, 2007Date of Patent: March 2, 2010Assignee: Theravance, Inc.Inventors: Daniel Genov, Junning Lee, Jyanwei Liu
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Publication number: 20100012931Abstract: Provided are a polycyclic compound of a compound having such a structure that two benzene rings bond to a central benzene ring each other to form a fused ring and another fused ring bonds to a terminal thereof, and an organic electroluminescence device including one or more organic thin film layers containing a light emitting layer between a cathode and an anode, in which at least one of the organic thin film layers includes the polycyclic compound of the present invention. The organic electroluminescence device has high luminous efficiency, no defect in pixels, and long lifetime. In addition, provided is a polycyclic compound realizing the organic electroluminescence device.Type: ApplicationFiled: September 2, 2009Publication date: January 21, 2010Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Tomoki KATO, Masaki Numata, Kazuki Nishimura, Toshihiro Iwakuma, Chishio Hosokawa, Kei Yoshida
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Patent number: 7638512Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: GrantFiled: June 23, 2008Date of Patent: December 29, 2009Assignee: WyethInventors: An Thien Vu, Paige Erin Mahaney, Stephen Todd Cohn
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Patent number: 7619246Abstract: A compound represented by Formula 1 and an organic light emitting device including the same: where Ar is a substituted or unsubstituted C6-C26 aryl group; X is O, S, R1 and R2 are hydrogen, a halogen, a C1-C12 alkyl group, a C6-C26 aryl group, or a substituted group thereof; R3, R4, R5, R6, R7 and R8 are each independently hydrogen or a substituted or unsubstituted C1-C12 alkyl group; R9 through R22 are each independently hydrogen, a C1-C30 alkyl group, a C1-C30 alkoxy group, a C6-C30 aryl group, a C6-C30 arylalkyl group, a C6-C30 aryloxy group, a C5-C30 heteroaryl group, a C5-C30 heteroarylalkyl group, a C5-C30 heteroaryloxy group, a C5-C20 cycloalkyl group, a C5-C30 heterocycloalkyl group, or a substituted group thereof. An organic light emitting device using the compound has low operating voltage, high color purity, and high efficiency.Type: GrantFiled: December 7, 2006Date of Patent: November 17, 2009Assignee: Samsung Mobile Display Co., Ltd.Inventors: Jhun-Mo Son, Eun-Sun Yu, O-Hyun Kwon, Young-Mok Son, Yu-Jin Kim
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Publication number: 20090275567Abstract: Compounds of formula (I): which possess cell-cycle inhibitory activity are described.Type: ApplicationFiled: May 24, 2007Publication date: November 5, 2009Inventors: Clifford Jones, Martin Pass, David Rudge
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Publication number: 20090105232Abstract: The invention relates to antibiotic cyclohexyl or piperidinyl carboximide derivatives of formula (I) wherein R1 represents hydrogen, halogen, (C1-C4)alkyl, (C1-C4)alkoxy, cyano or COOR2, R2 being (C1-C4)alkyl; one or two of U, V, W and X represent(s) N and the remaining represent each CH, or, in the case of X, may also represent CRX, RX being a halogen atom; either B represents N and A represents CH2CH2 or CH(OR3)CH2, or B represents CH or C(OR4) and A represents OCH2, CH2CH(OR5), CH(OR6)CH2, CH(OR7)CH(OR8), CH?CH or CH2CH2; each of R3, R4, R5, R6, R7, and R8 represents independently hydrogen, SO3H, PO3H2, CH2OPO3H2 or COR9, R9 being either CH2CH2COOH or such that R9—COOH is naturally occurring amino acid or dimethylaminoglycine; and to salts of such compounds of formula (I).Type: ApplicationFiled: March 22, 2007Publication date: April 23, 2009Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Christian Hubschwerlen, Jean-Philippe Surivet, Georg Rueedi, Cornelia Zumbrunn-Acklin
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Patent number: 7511036Abstract: Provided are compounds of the formula (and pharmaceutically acceptable salts thereof): wherein: R is hydrogen, methyl, hydroxymethyl or ?-hydroxyethyl; R1 and R2 are independently selected from hydrogen, C1-C6 alkyl, C1-C6 hydroxyalkyl, C3-C8 cycloalkyl, C1-C6 alkenyl, C1-C6 alkynyl, amino, monoalkylamino, dialkylaminoalkyl, and pyrrolidin-1-ylalkyl; and Y is selected from the group consisting of C1-C6 alkyl, substituted and unsubstituted aryl; with the provisos that: (a) if Y is aryl, then at least one of R1 and R2 is other than hydrogen, and (b) if R2 is hydrogen R1 is other than methyl. Also provided are pharmaceutical compositions containing the compounds, and methods for the preparation of the compounds. The compounds are useful, among other things, as prodrugs which can be converted under acidic conditions to thiazolium agents. The compounds can be administered to mammals, including humans, for treatment of various indications.Type: GrantFiled: March 27, 2006Date of Patent: March 31, 2009Assignee: Synvista Therapeutics, Inc.Inventors: Emily Reinhard, Elliot Katten
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Publication number: 20090048256Abstract: The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc., R3 is an alkyl group etc., E is one of the following groups of the formula (i) to (iv): Q1 is a single bond, an alkylene group or a group of the formula: —N(R7)—, R7 is a hydrogen atom or an alkyl group, Q2 is a single bond, an oxygen atom or an alkylene group, R4 is a cycloalkyl group, a group of the formula: —N(R5)(R6) etc., one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: —N(R8)(R9) etc., D is an oxygen atom etc., RA1 is an amino group etc., RA2 is an optionally substituted aliphatic heterocyclic group, R is an alkyl group optionally substituted by one to three halogen atom(s) etc., one of R8 and R9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc.Type: ApplicationFiled: October 20, 2006Publication date: February 19, 2009Inventors: Yasunori Moritani, Ritsuo Imashiro, Atsushi Sato
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Publication number: 20080280892Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials.Type: ApplicationFiled: October 17, 2006Publication date: November 13, 2008Inventors: Nathalie Cailleau, David Thomas Davies, Joel Michael Esken, Alan Joseph Hennessy, Senthil Kumar Kusalakumari Sukumar, Roger Edward Markwell, Timothy James Miles, Neil David Pearson
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Publication number: 20080261961Abstract: Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant, melanomas, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, leukemias, papillary thyroid carcinoma, non small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocyctosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.Type: ApplicationFiled: April 18, 2008Publication date: October 23, 2008Applicant: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo, Michael D. Kaufman
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Publication number: 20080214532Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: ApplicationFiled: March 21, 2006Publication date: September 4, 2008Inventors: Harald Walter, Camilla Corsi, Josef Ehrenfreund, Clemens Lamberth, Hans Tobler
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Patent number: 7419542Abstract: The invention is directed to a method or use of 2,9-dichloro-quinacridone as an alpha crystal phase inhibitor and optionally, 4,11-dichloroquinacridone during the beta-quinacridone or gamma-quinacridone crude pigment particle size reduction processes. The invention is also directed to solid solutions of quinacridone comprising about 98 to about 80 weight % gamma or beta-quinacridone, about 0.1 to about 10 weight % 2,9-dichloroquinacridone and about 0.1 to about 10 weight % 4,11-dichloroquinacridone.Type: GrantFiled: July 18, 2006Date of Patent: September 2, 2008Assignee: Ciba Specialty Chemicals CorporationInventors: Yingxia He, Colin Dennis Campbell, Gordian Schilling, Rhonda Carter, Melissa Wagner, James Thomas Will, Kevin Rodney Gerzevske
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Patent number: 7345174Abstract: The present invention provides the compound having the formula: wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, —O—, —S—, —NH—, or —CH2—; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.Type: GrantFiled: June 22, 2006Date of Patent: March 18, 2008Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia University in the City of New YorkInventors: Ronald Breslow, Sandro Belvedere, Leland Gershell, Thomas A. Miller, Paul A. Marks, Victoria M. Richon, Richard A. Rifkind
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Patent number: 7332511Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: August 1, 2005Date of Patent: February 19, 2008Assignee: Amgen Inc.Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Hui-Ling Wang, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Celia Dominguez, James Richard Falsey, Christopher Hulme, Jodie Katon, Thomas Nixey, Vassil I. Ognyanov, Liping H. Pettus, Robert Michael Rzasa
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Patent number: 7320984Abstract: The invention provides a morphinan derivative of the Formula (I): wherein R1 is methyl, cyclopropylmethyl or the like; R2 and R3 are hydroxy, methoxy, acetoxy or the like; both Y and Z are valence bonds, —C(?O)— or the like; X is C2-C5 carbon chain (one of the carbon atoms may be substituted by oxygen, sulfur or nitrogen) constituting a part of the ring structure, or the like; (R4)k is substituted or non-substituted benzene fused ring, carbonyl group or the like; R9 is hydrogen or the like; R10 and R11 are bound to represent —O—, or the like, and R6 is hydrogen or the like or a pharmaceutically acceptable acid addition salt thereof. The invention also provides a therapeutic or prophylactic agent for urinary frequency or urinary incontinence, comprising as an effective ingredient the morphinan derivative or the pharmaceutically acceptable acid addition salt thereof; a method for therapy or prophylaxis of the diseases.Type: GrantFiled: October 8, 2003Date of Patent: January 22, 2008Assignee: Toray Industries, Inc.Inventors: Naoki Izumimoto, Koji Kawai, Kuniaki Kawamura, Morihiro Fujimura, Toshikazu Komagata
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Patent number: 7259163Abstract: Novel anti-viral agents of Formula wherein: A represents OR1, NR1R2, or R1 wherein R1 and R2 are hydrogen, C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; B represents C(O)R3 wherein R3 is C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; C represents C1-6alkyl, aryl, heteroaryl or heterocyclyl; D represents a saturated or unsaturated optionally substituted 6-membered heterocyclic ring; E represents hydrogen or C1-6alkyl; F represents hydrogen, C1-6alkyl, aryl or heteroaryl; and G represents hydrogen, C1-6alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; and salts, solvates and esters thereof, processes for their preparation and methods of using them in HCV treatment are provided.Type: GrantFiled: October 30, 2002Date of Patent: August 21, 2007Assignee: Glaxo Group LimitedInventors: Gianpaolo Bravi, Rossella Guidetti, David Haigh, Charles David Hartley, Peter David Howes, Deborah Lynette Jackson, Victoria Lucy Helen Lovegrove, Pritom Shah, Martin John Slater, Katrina Jane Wareing
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Patent number: 7244725Abstract: Disclosed are compounds of the formula: where variables Z, X, R15, R2, R3, and RC are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.Type: GrantFiled: September 10, 2003Date of Patent: July 17, 2007Assignees: Elan Pharmaceuticals, Inc., Pharmacia & Upjohn CompanyInventors: Varghese John, Michel Maillard, James P. Beck, Eric T. Baldwin, Robert Hughes, Shon R. Pulley, Ruth TenBrink
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Patent number: 7166609Abstract: Pyrimidine-4,6-dicarboxylic acid diamides of the formula I are suitable for selectively inhibiting collagenase (MMP 13). The pyrimidine-4,6-dicarboxylic acid diamides can therefore be used for treating degenerative joint diseases.Type: GrantFiled: November 3, 2003Date of Patent: January 23, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Otmar Klingler, Reinhard Kirsch, Joerg Habermann, Klaus-Ulrich Weithmann, Christian Engel, Bernard Pirard
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Patent number: 7112582Abstract: The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof. wherein one of A and B denotes hydrogen and the other an optionally substituted fused bicyclic heteroaryl group; and X is S.Type: GrantFiled: May 1, 2003Date of Patent: September 26, 2006Assignee: WyethInventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Itsuki Yamamura, Tsuyoshi Takasaki, Atul Agarwal, Osvaldo dos Santos, Fuk-Wah Sum, Yang-I Lin
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Patent number: 7101428Abstract: The invention is directed to a method or use of 2,9-dichloro-quinacridone as a crystal phase inhibitor during the beta-quinacridone or gamma-quinacridone crude pigment particle size reduction processes. 2,9-dichloroquinacridone is added to the milling composition of the crude gamma or crude beta quinacridone.Type: GrantFiled: November 12, 2004Date of Patent: September 5, 2006Assignee: Ciba Specialty Chemicals CorporationInventors: Yingxia He, Colin Campbell, Gordian Schilling, Rhonda Carter
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Patent number: 7101874Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof wherein Y is —S(?O)n—, —S(?NR8)—, or —S(?NR8)(?O)—; Z is —NHC(?O)R1, —NHC(?S)R1, —NH-het1, —O-het1, —S-het1, or -het2. The compounds of formula I are useful as antibacterial agents.Type: GrantFiled: February 22, 2005Date of Patent: September 5, 2006Assignee: Pharmacia and Upjohn CompanyInventors: Mikhail F. Gordeev, Adam Renslo, Gary W. Luehr, Stuart Lam, Neil E. Westlund, Dinesh Vinoobhai Patel
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Patent number: 7078402Abstract: The invention relates to novel aminothiol ester compounds having the general formula (I): and to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (cancers and precancers, dermatological, rheumatic and ophthalmological complaints in particular) or in cosmetic compositions. The invention also relates to a pharmaceutical or cosmetic composition, characterized in that it comprises, as active agent, a compound of general formula (I) in combination with a pharmaceutically or cosmetically acceptable support.Type: GrantFiled: May 31, 2001Date of Patent: July 18, 2006Assignee: Centre National de la Recherche Scientifique (CNRS)Inventors: Guy Fournet, Gerard Anthony Quash, Jacques Gore
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Patent number: 6943196Abstract: An NF-?B inhibitor having as an active ingredient a benzoquinone derivative represented by the general formula (1) wherein R1, R2, and R3 are each independently H, alkyl having 1 to 5 carbons, or alkoxy having 1 to 5 carbons; R4 is H, hydroxymethyl, alkyl, or carboxyl which is optionally esterified or amidated; Z is represented by the formula (A); and, n is an integer from 0 to 6, or its hydroquinone form or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 19, 1999Date of Patent: September 13, 2005Assignee: Daiichi Suntory Pharma Co., Ltd.Inventors: Yoichi Nunokawa, Kenji Suzuki, Masayuki Saitoh
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Patent number: 6897210Abstract: The invention relates to quinazoline derivatives of formula (I) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selectedType: GrantFiled: November 3, 2003Date of Patent: May 24, 2005Assignees: Zeneca Limited, Zeneca Pharma S. A.Inventors: Andrew Peter Thomas, Craig Johnstone, Edward Clayton, Elaine Sophie Elizabeth Stokes, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin
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Patent number: 6884813Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof wherein A is a structure i, ii, iii, or iv X is CR7; Y is —S(?O)n—, —S(?NR8)—, or —S(?NR8)(?O)—; Z is —NHC(?O)R1, —NHC(?S)R1, —NR-het1, —O-het1, —S-het1, or -het2; and n is independently 0, 1, or 2. The compounds of formula I are useful as antimicrobials against a number of human and veterinary pathogens.Type: GrantFiled: January 21, 2003Date of Patent: April 26, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Adam Renslo, Gary W. Luehr, Stuart Lam, Neil E. Westlund, Dinesh V. Patel
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Patent number: 6855174Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein X is selected from halogen and R5SO4 where the halogen is preferably Cl, Br or I; R, R1 and R2 are each individually selected from C1 to C22 alkyl and C1 to C22 mono or dihydroxyalkyl, or two of R, R1 and R2 together with the nitrogen atom to which they are attached form a C3 to C6 saturated or unsaturated ring optionally containing in the ring one or more additional hetero atoms selected from O, S and N atoms; R3 and R4 are each individually selected from C1 to C6 alkyl, C1 to C6 hydroxyalkyl, C1 to C6 alkoxy, C1 to C6 aminoalkyl or R3 and R4 together form a C1 to C5 alkylene group; and R5 is selected from C1 to C22 alkyl and C1 to C22 mono or dihydroxyalkyl.Type: GrantFiled: May 4, 2004Date of Patent: February 15, 2005Assignee: The Procter & Gamble CompanyInventors: Mu-Ill Lim, Yuh-Guo Pan, Gottfried Wenke
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Patent number: 6750337Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein X is selected from halogen and R5SO4 where the halogen is preferably Cl, Br or I; R, R1 and R2 are each individually selected from C1 to C22 alkyl and C1 to C22 mono or dihydroxyalkyl, or two of R, R1 and R2 together with the nitrogen atom to which they are attached form a C3 to C6 saturated or unsaturated ring optionally containing in the ring one or more additional hetero atoms selected from O, S and N atoms; R3 and R 4 are each individually selected from C1 to C6 alkyl, C1 to C6 hydroxyalkyl, C1 to C6 alkoxy, C1 to C6 aminoalkyl or R3 and R4 together form a C1 to C5 alkylene group; and R5 is selected from C1 to C22 alkyl and C1 to C22 mono or dihydroxyalkyl.Type: GrantFiled: January 18, 2002Date of Patent: June 15, 2004Assignee: The Procter & Gamble CompanyInventors: Mu-Ill Lim, Yuh-Guo Pan, Gottfried Wenke
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Patent number: 6743564Abstract: Amine compounds having a cyano group are useful in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.Type: GrantFiled: December 6, 2001Date of Patent: June 1, 2004Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Jun Hatakeyama, Tomohiro Kobayashi, Takeru Watanabe
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Patent number: 6673803Abstract: The invention relates to quinazoline derivatives of formula (I) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl);R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl groupType: GrantFiled: February 25, 2002Date of Patent: January 6, 2004Assignee: Zeneca LimitedInventors: Andrew Peter Thomas, Craig Johnstone, Elaine Sophie Elizabeth Stokes, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin
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Patent number: 6667342Abstract: Compounds of formula (I), pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, wherein: Ring X is phenyl or a six membered heteroaryl ring containing one or two ring nitrogens where said nitrogens are optionally oxidised to form the N-oxide; R1 and R2 are substituents as defined within; R3 and R4 are defined within and are alkyl or halo alkyl or together form a halocycloalkyl ring; R5 is a substituent as defined within; Y—Z is a linking group as defined within; are useful in the production of a elevation of PDH activity in a warm-blooded animal such as a human being. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are described.Type: GrantFiled: August 22, 2000Date of Patent: December 23, 2003Assignee: Astrazeneca ABInventors: David S Clarke, Jeremy N Burrows, Paul Ro Whittamore, Roger J Butlin, Thorsten Nowak
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Patent number: 6638930Abstract: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: April 17, 2001Date of Patent: October 28, 2003Assignee: Merck & Co. Inc.Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
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Publication number: 20030143481Abstract: An image forming material includes an image forming layer containing a water-insoluble and alkali-soluble resin, a light-heat converting agent and a compound represented by the following general formula (1). In general formula (1), R1 to R3 independently represent an organic group, where R1 represents a residue forming a ring containing a N1 atom, R2 and R3 may bond to each other to form a ring or at least one of R2 and R3 may bond to R1 to form a ring and X− represents a conjugate base of an organic acid or inorganic acid. The ring containing the N1 atom is preferably a piperidine ring.Type: ApplicationFiled: July 24, 2002Publication date: July 31, 2003Applicant: FUJI PHOTO FILM CO., LTD.Inventors: Kaoru Iwato, Tadahiro Sorori