Thiadiazines Patents (Class 544/8)
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Patent number: 11473026Abstract: An aminal compound is injected into a fluid gas stream including at least one acid gas to reduce the amount of acid gas in the fluid gas stream. Having two reactive sites present in the aminal compound enables a much higher efficiency of acid gas capture than a simple alkanolamine, which isn't effective, for example, under dilute circumstances.Type: GrantFiled: May 30, 2019Date of Patent: October 18, 2022Assignee: Foremark Performance ChemicalsInventors: Jon Bingham, Marlon O. Treasure
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Patent number: 11229642Abstract: Disclosed herein are methods of reducing neutropenia that is caused by chemotherapy or radiation therapy by administering plinabulin to a subject.Type: GrantFiled: June 5, 2017Date of Patent: January 25, 2022Assignee: BeyondSpring Pharmaceuticals, Inc.Inventors: Lan Huang, George Kenneth Lloyd, Ramon Mohanlal
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Patent number: 10980813Abstract: Provided is an antifungal composition containing a cyclic N-sulfonylamine compound, a cyclic N-sulfonylimine compound or a cyclic N-sulfonyloxaziridine compound, each having an antifungal activity, as an active ingredient. An antifungal composition containing a compound represented by the formula (1): wherein ring A is an optionally further substituted 5- to 7-membered heterocycle, and the 5- to 7-membered heterocycle is optionally condensed with 1 or 2 rings selected from an optionally substituted benzene ring and an optionally substituted 5- to 7-membered heterocycle, X is —N?, —NR2— or —O—; Y1 is a hydrogen atom, and Y2 is a hydroxy group or Y1 and Y2 may be joined to form a bond or —O—; R1 is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; and R2 is a hydrogen atom or an optionally substituted hydrocarbon group, or a salt thereof as an active ingredient.Type: GrantFiled: February 27, 2018Date of Patent: April 20, 2021Assignee: SEED RESEARCH INSTITUTE CO., LTD.Inventors: Teruhiko Ishikawa, Morita Iwami
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Patent number: 10683299Abstract: The present invention relates to compounds of the formula (I), or pharmaceutically acceptable salts, enantiomer or diastereomer thereof, wherein R1 to R4 and Q are as described above. The compounds may be useful for the treatment or prophylaxis of hepatitis B virus infection.Type: GrantFiled: January 14, 2019Date of Patent: June 16, 2020Assignee: HOFFMANN LA ROCHE INC.Inventors: Xingchun Han, Xianfeng Lin, Hong Shen, Taishan Hu, Zhisen Zhang
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Patent number: 10624897Abstract: The invention provides a series of chlorobenzene substituted azaaryl compounds having activity in inhibiting cancer cell growth and low toxicity to normal cells. Particularly, the compounds of the invention have stronger inhibition effect on bladder cancer and liver cancer.Type: GrantFiled: July 20, 2016Date of Patent: April 21, 2020Assignee: Taipei Medical UniversityInventors: Yun Yen, Jing-Ping Liou, Chun-Han Chen
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Patent number: 10112958Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variables R1, R2 and R3 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: GrantFiled: July 11, 2017Date of Patent: October 30, 2018Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Lei Zhang, Brian Thomas O'Neill, Patrick Robert Verhoest, Peter Justin Mikochik, John Charles Murray, Xinjun Hou
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Patent number: 10071998Abstract: In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R2, ring A, RA, m, ring B, RB, and n are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.Type: GrantFiled: January 15, 2016Date of Patent: September 11, 2018Inventors: Wen-Lian Wu, Shuwen He, Shawn P. Walsh, Jared N. Cumming
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Patent number: 9896438Abstract: 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: GrantFiled: August 12, 2015Date of Patent: February 20, 2018Assignee: HOFFMANN-LA ROCHE INC.Inventors: Lilli Anselm, Bjoern Bartels, Cosimo Dolente, Wolfgang Guba, Haap Wolfgang, Jens-Uwe Peters, Thomas Woltering, Ulrike Obst Sander, Mark Rogers-Evans
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Patent number: 9751895Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variables R1, R2 and R3 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: GrantFiled: September 22, 2016Date of Patent: September 5, 2017Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Lei Zhang, Brian Thomas O'Neill, Patrick Robert Verhoest, Peter Justin Mikochik, John Charles Murray, Xinjun Hou
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Patent number: 9428476Abstract: In its many embodiments, the present invention provides provides certain S-imino-S-oxo iminothiadiazine compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein RN, R1, R2, R3, R4, ring A, RA, m, L1, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.Type: GrantFiled: March 11, 2014Date of Patent: August 30, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Tanweer A. Khan, Jack D. Scott, Jared N. Cumming
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Patent number: 9422277Abstract: In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein the middle ring (referred to herein as “ring B”) of the tricyclic substituent is an optionally substituted 5-membered ring, and each of the remaining variables shown in the formula are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.Type: GrantFiled: October 14, 2013Date of Patent: August 23, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Eric J. Gilbert, Jared N. Cumming, Andrew W. Stamford, Younong Yu, Jack D. Scott, Ulrich Iserloh
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Patent number: 9416129Abstract: In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): (I) and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein the middle ring (referred to herein as “ring B”) of the tricyclic substituent is an optionally substituted 6-membered ring, and each of the remaining variables shown in the formula are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.Type: GrantFiled: October 14, 2013Date of Patent: August 16, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Eric J. Gilbert, Jared N. Cumming, Andrew W. Stamford, Younong Yu, Jack D. Scott, Ulrich Iserloh, Lingyan Wang, John P. Caldwell
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Patent number: 9029362Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, -L2-, and -L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to ?-amyloid (“A?”) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimer's disease, are also disclosed.Type: GrantFiled: March 21, 2014Date of Patent: May 12, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming
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Patent number: 8952148Abstract: The present invention relates to a process for the preparation of substantially pure Taurolidine.Type: GrantFiled: November 18, 2011Date of Patent: February 10, 2015Assignee: Biophore India Pharmaceuticals Pvt LtdInventors: Manik Reddy Pullagurla, Jagadeesh Babu Rangisetty, Neelam Naidu Dokula
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Publication number: 20140296222Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, -L2-, and -L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to ?-amyloid (“A?”) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimer's disease, are also disclosed.Type: ApplicationFiled: March 21, 2014Publication date: October 2, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh
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Publication number: 20140296223Abstract: This invention relates to a method for regulating skin pigmentation of a subject, comprising the step of administering the agent for inhibiting the expression or activation of Microphthalmia Transcription Factor (MITF) to the subject who is in need of regulation of skin pigmentation.Type: ApplicationFiled: August 31, 2012Publication date: October 2, 2014Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: David E. Fisher, Rizwan Haq, Hans Ragnar Valdemar Widlund
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Publication number: 20140275032Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, X5, X6, Y, Z, G, R1a, R2a, R1b, R2b, R3, R4, R5 and R6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Genentech, Inc.Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Stuart Ward
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Patent number: 8796479Abstract: A process for recovering a lipid from a lipid containing material, comprising subjecting the lipid containing material to superheated steam and recovering the lipid in a liquid state.Type: GrantFiled: July 22, 2005Date of Patent: August 5, 2014Inventor: David Kenneth Pinches
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Publication number: 20140155390Abstract: The present invention relates to a compound of Formula 1, 2 or 3: wherein A is N or —CR0—, where R0 is hydrogen, C1-C6 linear or branched chain alkyl, etc., Z is —CRe—, or, —N—, where Re is hydrogen, C1-C6 linear or branched chain alkyl,etc.; R1 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R2 are independently hydrogen or C1-C6 linear or branched chain alkyl; R3 and R4 are independently hydrogen, C1-C6 linear or branched chain alkyl, etc.;. R5 and R6 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; R8 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R9 and R10 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.Type: ApplicationFiled: December 2, 2013Publication date: June 5, 2014Applicant: Pfizer Inc.Inventors: James Thomas Anderson, Eugene Lvovich Piatnitski Chekler, Edmund L. Ellsworth, Bruce Kipp Erickson, Adam Matthew Gilbert, Anthony P. Ricketts, David P. Thompson, Rayomand Jal Unwalla, Patrick Robert Verhoest
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Patent number: 8729071Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): (I) and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, L2-, and L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to ?-amyloid (A?) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers disease, are also disclosed.Type: GrantFiled: October 6, 2010Date of Patent: May 20, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming
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Publication number: 20140087978Abstract: A method of converting an inactive biocide into an active biocide comprises: contacting the inactive biocide with an activating agent, wherein the activating agent is capable of chemically reacting with the inactive biocide; and causing or allowing a chemical reaction to take place between the inactive biocide and the activating agent, wherein the chemical reaction produces the active biocide. The methods can also include deactivating the active biocide via a chemical reaction between the active biocide and a deactivating agent.Type: ApplicationFiled: September 27, 2012Publication date: March 27, 2014Applicant: HALLIBURTON ENERGY SERVICES, INCInventor: Jay P. DEVILLE
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Publication number: 20140057871Abstract: [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: ApplicationFiled: April 11, 2012Publication date: February 27, 2014Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Akihiro Okano, Munetaka Ohkouchi, Muneyoshi Makabe
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Publication number: 20140038948Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.Type: ApplicationFiled: June 25, 2013Publication date: February 6, 2014Applicant: Plexxikon Inc.Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
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Publication number: 20140024636Abstract: Provided is a sulfamide derivative having an adamantyl group represented by the following Formula 1, or a pharmaceutically acceptable salt thereof. The sulfamide derivative suppresses the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1), and is useful in the treatment of various diseases that are mediated by 11?-HSD1.Type: ApplicationFiled: March 30, 2012Publication date: January 23, 2014Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Ki Young Kim, Jin Hee Ahn, Seung Kyu Kang, Sang Dal Rhee, Myung Ae Bae, Sung Hoon Ahn, Hee Youn Kim, Won Hoon Jung, Nam Sook Kang
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Publication number: 20130303524Abstract: The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C, D, E, F, G, H, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.Type: ApplicationFiled: May 10, 2013Publication date: November 14, 2013Inventors: Ross Bersot, Paul Humphries
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Patent number: 8563543Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (a) and include tautomers, solvates, prodrugs, esters, and deuterates thereof, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, ring C, m, n, p, q, -L1-, -L2-, L3-, and L4- is selected independently and as defined herein. The compounds of the invention have, surprisingly and advantageously, improved solution stability. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers Disease, are also disclosed.Type: GrantFiled: October 6, 2010Date of Patent: October 22, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh, Lingyan Wang, Wei Li
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Publication number: 20130237522Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: ApplicationFiled: April 19, 2013Publication date: September 12, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Kai GERLACH, Roland PFAU, Norbert HAUEL, Iris KAUFFMANN-HEFNER, Georg DAHMANN, Herbert NAR, Sandra HANDSCHUH, Wolfgang WIENEN, Annette SCHULER-METZ
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Publication number: 20130237700Abstract: The present invention relates to a process for the preparation of substantially pure Taurolidine.Type: ApplicationFiled: November 18, 2011Publication date: September 12, 2013Applicant: BIOPHORE INDIA PHARMACEUTICALS PVT. LTD.Inventors: Manik Reddy Pullagurla, Jagadeesh Babu Rangisetty, Neelam Naidu Dokula
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Publication number: 20130237531Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.Type: ApplicationFiled: April 19, 2013Publication date: September 12, 2013Inventors: Guoxian Wu, Jiazhong Zhang, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, James Tsai
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Publication number: 20130203739Abstract: [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: ApplicationFiled: October 11, 2011Publication date: August 8, 2013Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Akihiro Okano, Munetaka Ohkouchi, Muneyoshi Makabe
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Publication number: 20130053347Abstract: The present invention relates to the biology and mechanism of action of the naturally occurring compound Narciclasine, especially as an anti-cancer agent for brain tumors. The invention provides new insights on the target molecule of Amaryllidaceae isocarbostyril derivatives as for example Narciclasine and provides new prodrugs of these Amaryllidceae isocabostyril constituents for treating cancer, specifically cancers or tumors located in the brain.Type: ApplicationFiled: May 3, 2010Publication date: February 28, 2013Applicant: Universite Libre de BruxellesInventors: Veronique Mathieu, Gwendoline Van Goietsenoven, Jacques Dubois, Florence Lefranc-Kiss, Laurent Ingrassia, Robert Kiss
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Patent number: 8377928Abstract: The present invention relates to 3-Aminosulfonyl Substituted Indole Derivatives of Formula (I): The invention also relates to compositions comprising at least one 3-Aminosulfonyl Substituted Indole Derivative, and methods of using the 3-Aminosulfonyl Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: GrantFiled: November 13, 2008Date of Patent: February 19, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin X. Chen, Stuart B. Rosenblum, F. George Njoroge, Joseph A. Kozlowski
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Publication number: 20130040930Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: April 27, 2011Publication date: February 14, 2013Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Kazuhiro Maeda, Jun-ichi Endoh, Akiko Tarao, Kaoru Tashiro, Seigo Ishibuchi, Hidemasa Hikawa
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Patent number: 8314098Abstract: The present invention has searched for a variety of compounds which show IL-12/IL-23 production-inhibitory activities and herein provides a pharmaceutical composition and an agent for preventing or treating IL-12/IL-23 excess production-related diseases, which comprise the compound.Type: GrantFiled: June 27, 2011Date of Patent: November 20, 2012Assignee: Ajinomoto Co., Inc.Inventors: Takashi Yamamoto, Ayatoshi Andou, Nobuhiko Hayakawa, Masatsugu Noguchi, Kanna Kuribayashi, Agung Eviryanti, Ryohei Yokoyama, Shunsuke Fukuda, Toshihiko Sugiura, Shunsuke Kageyama, Yoichiro Shima, Misato Noguchi
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Patent number: 8288381Abstract: The present invention relates to compounds of Formula I: wherein R1, R2, R3, A1, A2, A3, A4 and D have the meaning described herein. The present invention also relates to pharmaceutical compositions comprising such compounds and therapeutic uses thereof.Type: GrantFiled: November 10, 2010Date of Patent: October 16, 2012Assignee: Genentech, Inc.Inventors: Zhonghua Pei, Joseph P. Lyssikatos, Kevin Hon Luen Lau, Wendy Lee, Kirk D. Robarge
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Publication number: 20120227545Abstract: This invention relates to a process for the recovery of precious metal/s from a precious metal-containing material in an aqueous leach slurry or solution. The process includes the step of contacting the precious metal/s in the leach slurry or solution with a ligand selected from dithiooxamide (rubeanic acid), or a substituted dithiooxamide. The leaching of PGMs, gold and silver from their ores using the ligand of the present invention may take place under aqueous alkaline conditions, avoiding both corrosive acidic conditions and the use of cyanide.Type: ApplicationFiled: July 21, 2010Publication date: September 13, 2012Applicant: ANGLO OPERATIONS LIMITEDInventors: Diandree Padayachee, Makhosazane Chucky Kunene, Marga Retha Burger, Noko Simon Phala
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Patent number: 8232272Abstract: The present invention relates to novel benzimidazole-dihydrothiadiazinone derivatives as fructose-1,6-bisphosphatase inhibitors, to processes for the preparation thereof and to the use thereof in therapy, especially for the treatment of diabetes.Type: GrantFiled: October 13, 2008Date of Patent: July 31, 2012Assignee: Merck Patent Gesellschaft mit beschränkter HaftungInventors: Gerard Botton, Caroline Leriche, Annick Arbellot de Vacqueur, Annick Audet, Johannes Gleitz
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Publication number: 20120189642Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (a) and include tautomers, solvates, prodrugs, esters, and deuterates thereof, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, ring C, m, n, p, q, -L1-, -L2-, L3-, and L4- is selected independently and as defined herein. The compounds of the invention have, surprisingly and advantageously, improved solution stability. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers Disease, are also disclosed.Type: ApplicationFiled: October 6, 2010Publication date: July 26, 2012Applicant: Schering CorporationInventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh, Lingyan Wang, Wei Li
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Publication number: 20120183563Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): (I) and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-,L2-, and L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to ?-amyloid (A?) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers disease, are also disclosed.Type: ApplicationFiled: October 6, 2010Publication date: July 19, 2012Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh, Jeffrey A. Misiaszek, Guoqing Li
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Patent number: 8211886Abstract: Compounds of the formula (I), which are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed for the treatment of tumours.Type: GrantFiled: August 6, 2008Date of Patent: July 3, 2012Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Patent number: 8173645Abstract: Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: GrantFiled: March 20, 2008Date of Patent: May 8, 2012Assignee: Takeda San Diego, Inc.Inventors: Zacharia Cheruvallath, Jun Feng, Prasuna Guntupalli, Stephen L. Gwaltney, Joanne Miura, Mark Sabat, Mingnam Tang
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Publication number: 20120101271Abstract: Selective intramolecular C—H amination via metalloradical activation of azides: synthesis of 1,3-diamines under neutral and nonoxidative conditions. One aspect of the present invention is the synthesis of 1,3-diamines by intramolecular C—H amination of sulfamoyl azides. More specifically, sulfamoyl azides may be selectively aminated via metalloradical activation of azides, preferably with Co(II) porphyrins. In a particularly preferred embodiment, the Co(II) porphyrin is a D2h-symmetric porphyrin.Type: ApplicationFiled: October 21, 2011Publication date: April 26, 2012Inventors: X. Peter Zhang, Hongjian Lu
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Patent number: 8063042Abstract: The invention is concerned with novel heterocyclyl compounds of formula (I) wherein A, X, Y, R3, R4, R5, R6, R7, R8, R9, R10, m and n are as herein defined, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.Type: GrantFiled: July 10, 2008Date of Patent: November 22, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin
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Publication number: 20110195960Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; 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 rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: April 6, 2011Publication date: August 11, 2011Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
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Patent number: 7973035Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; 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 rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: GrantFiled: June 16, 2008Date of Patent: July 5, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
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Publication number: 20110130391Abstract: The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.Type: ApplicationFiled: December 29, 2010Publication date: June 2, 2011Inventors: Richard G. Wilde, James J. Takasugi, Seongwoo Hwang, Ellen M. Welch, Guangming Chen
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Publication number: 20110077236Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: ApplicationFiled: December 2, 2010Publication date: March 31, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Kai GERLACH, Roland PFAU, Norbert HAUEL, Iris KAUFFMANN-HEFNER, Georg DAHMANN, Herbert NAR, Sandra HANDSCHUH, Wolfgang WIENEN, Annette SCHULER-METZ
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Patent number: 7902186Abstract: Compounds of the formula (I), in which R1, R2, m, Q and B have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: October 25, 2006Date of Patent: March 8, 2011Assignee: Merck Patent GmbHInventors: Oliver Schadt, Dieter Dorsch, Melanie Schultz, Andree Blaukat
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Publication number: 20110044918Abstract: The present invention relates to the cosmetic use of a compound of formula (I) and also the cosmetically acceptable salts thereof, solvates thereof and isomers thereof, for non-therapeutic skincare.Type: ApplicationFiled: October 29, 2010Publication date: February 24, 2011Applicant: L'OREALInventors: Xavier Marat, Benoit Muller
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Publication number: 20100311733Abstract: Compounds of the formula (I), in which R1, Q and Het have the meanings indicated in Claim 1), are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: August 6, 2008Publication date: December 9, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT ESCHRANKTER HAFTUNGInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat