Thiadiazines Patents (Class 544/8)
  • Patent number: 10683299
    Abstract: 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: Grant
    Filed: January 14, 2019
    Date of Patent: June 16, 2020
    Assignee: HOFFMANN LA ROCHE INC.
    Inventors: Xingchun Han, Xianfeng Lin, Hong Shen, Taishan Hu, Zhisen Zhang
  • Patent number: 10624897
    Abstract: 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: Grant
    Filed: July 20, 2016
    Date of Patent: April 21, 2020
    Assignee: Taipei Medical University
    Inventors: Yun Yen, Jing-Ping Liou, Chun-Han Chen
  • Patent number: 10112958
    Abstract: 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: Grant
    Filed: July 11, 2017
    Date of Patent: October 30, 2018
    Assignee: 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
  • Patent number: 10071998
    Abstract: 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: Grant
    Filed: January 15, 2016
    Date of Patent: September 11, 2018
    Inventors: Wen-Lian Wu, Shuwen He, Shawn P. Walsh, Jared N. Cumming
  • Patent number: 9896438
    Abstract: 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: Grant
    Filed: August 12, 2015
    Date of Patent: February 20, 2018
    Assignee: 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
  • Patent number: 9751895
    Abstract: 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: Grant
    Filed: September 22, 2016
    Date of Patent: September 5, 2017
    Assignee: 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
  • Patent number: 9428476
    Abstract: 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: Grant
    Filed: March 11, 2014
    Date of Patent: August 30, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tanweer A. Khan, Jack D. Scott, Jared N. Cumming
  • Patent number: 9422277
    Abstract: 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: Grant
    Filed: October 14, 2013
    Date of Patent: August 23, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Eric J. Gilbert, Jared N. Cumming, Andrew W. Stamford, Younong Yu, Jack D. Scott, Ulrich Iserloh
  • Patent number: 9416129
    Abstract: 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: Grant
    Filed: October 14, 2013
    Date of Patent: August 16, 2016
    Assignee: 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
  • Patent number: 9029362
    Abstract: 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: Grant
    Filed: March 21, 2014
    Date of Patent: May 12, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming
  • Patent number: 8952148
    Abstract: The present invention relates to a process for the preparation of substantially pure Taurolidine.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: February 10, 2015
    Assignee: Biophore India Pharmaceuticals Pvt Ltd
    Inventors: Manik Reddy Pullagurla, Jagadeesh Babu Rangisetty, Neelam Naidu Dokula
  • Publication number: 20140296222
    Abstract: 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: Application
    Filed: March 21, 2014
    Publication date: October 2, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh
  • Publication number: 20140296223
    Abstract: 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: Application
    Filed: August 31, 2012
    Publication date: October 2, 2014
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: David E. Fisher, Rizwan Haq, Hans Ragnar Valdemar Widlund
  • Publication number: 20140275032
    Abstract: 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: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Genentech, Inc.
    Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Stuart Ward
  • Patent number: 8796479
    Abstract: 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: Grant
    Filed: July 22, 2005
    Date of Patent: August 5, 2014
    Inventor: David Kenneth Pinches
  • Publication number: 20140155390
    Abstract: 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: Application
    Filed: December 2, 2013
    Publication date: June 5, 2014
    Applicant: 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
  • Patent number: 8729071
    Abstract: 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: Grant
    Filed: October 6, 2010
    Date of Patent: May 20, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming
  • Publication number: 20140087978
    Abstract: 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: Application
    Filed: September 27, 2012
    Publication date: March 27, 2014
    Applicant: HALLIBURTON ENERGY SERVICES, INC
    Inventor: Jay P. DEVILLE
  • Publication number: 20140057871
    Abstract: [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: Application
    Filed: April 11, 2012
    Publication date: February 27, 2014
    Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Akihiro Okano, Munetaka Ohkouchi, Muneyoshi Makabe
  • Publication number: 20140038948
    Abstract: 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: Application
    Filed: June 25, 2013
    Publication date: February 6, 2014
    Applicant: Plexxikon Inc.
    Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
  • Publication number: 20140024636
    Abstract: 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: Application
    Filed: March 30, 2012
    Publication date: January 23, 2014
    Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: 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
  • Publication number: 20130303524
    Abstract: 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: Application
    Filed: May 10, 2013
    Publication date: November 14, 2013
    Inventors: Ross Bersot, Paul Humphries
  • Patent number: 8563543
    Abstract: 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: Grant
    Filed: October 6, 2010
    Date of Patent: October 22, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh, Lingyan Wang, Wei Li
  • Publication number: 20130237522
    Abstract: 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: Application
    Filed: April 19, 2013
    Publication date: September 12, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning PRIEPKE, Kai GERLACH, Roland PFAU, Norbert HAUEL, Iris KAUFFMANN-HEFNER, Georg DAHMANN, Herbert NAR, Sandra HANDSCHUH, Wolfgang WIENEN, Annette SCHULER-METZ
  • Publication number: 20130237531
    Abstract: 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: Application
    Filed: April 19, 2013
    Publication date: September 12, 2013
    Inventors: Guoxian Wu, Jiazhong Zhang, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, James Tsai
  • Publication number: 20130237700
    Abstract: The present invention relates to a process for the preparation of substantially pure Taurolidine.
    Type: Application
    Filed: November 18, 2011
    Publication date: September 12, 2013
    Applicant: BIOPHORE INDIA PHARMACEUTICALS PVT. LTD.
    Inventors: Manik Reddy Pullagurla, Jagadeesh Babu Rangisetty, Neelam Naidu Dokula
  • Publication number: 20130203739
    Abstract: [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: Application
    Filed: October 11, 2011
    Publication date: August 8, 2013
    Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Akihiro Okano, Munetaka Ohkouchi, Muneyoshi Makabe
  • Publication number: 20130053347
    Abstract: 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: Application
    Filed: May 3, 2010
    Publication date: February 28, 2013
    Applicant: Universite Libre de Bruxelles
    Inventors: Veronique Mathieu, Gwendoline Van Goietsenoven, Jacques Dubois, Florence Lefranc-Kiss, Laurent Ingrassia, Robert Kiss
  • Patent number: 8377928
    Abstract: 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: Grant
    Filed: November 13, 2008
    Date of Patent: February 19, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin X. Chen, Stuart B. Rosenblum, F. George Njoroge, Joseph A. Kozlowski
  • Publication number: 20130040930
    Abstract: 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: Application
    Filed: April 27, 2011
    Publication date: February 14, 2013
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Kazuhiro Maeda, Jun-ichi Endoh, Akiko Tarao, Kaoru Tashiro, Seigo Ishibuchi, Hidemasa Hikawa
  • Patent number: 8314098
    Abstract: 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: Grant
    Filed: June 27, 2011
    Date of Patent: November 20, 2012
    Assignee: 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
  • Patent number: 8288381
    Abstract: 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: Grant
    Filed: November 10, 2010
    Date of Patent: October 16, 2012
    Assignee: Genentech, Inc.
    Inventors: Zhonghua Pei, Joseph P. Lyssikatos, Kevin Hon Luen Lau, Wendy Lee, Kirk D. Robarge
  • Publication number: 20120227545
    Abstract: 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: Application
    Filed: July 21, 2010
    Publication date: September 13, 2012
    Applicant: ANGLO OPERATIONS LIMITED
    Inventors: Diandree Padayachee, Makhosazane Chucky Kunene, Marga Retha Burger, Noko Simon Phala
  • Patent number: 8232272
    Abstract: 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: Grant
    Filed: October 13, 2008
    Date of Patent: July 31, 2012
    Assignee: Merck Patent Gesellschaft mit beschränkter Haftung
    Inventors: Gerard Botton, Caroline Leriche, Annick Arbellot de Vacqueur, Annick Audet, Johannes Gleitz
  • Publication number: 20120189642
    Abstract: 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: Application
    Filed: October 6, 2010
    Publication date: July 26, 2012
    Applicant: Schering Corporation
    Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh, Lingyan Wang, Wei Li
  • Publication number: 20120183563
    Abstract: 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: Application
    Filed: October 6, 2010
    Publication date: July 19, 2012
    Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh, Jeffrey A. Misiaszek, Guoqing Li
  • Patent number: 8211886
    Abstract: 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: Grant
    Filed: August 6, 2008
    Date of Patent: July 3, 2012
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
  • Patent number: 8173645
    Abstract: 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: Grant
    Filed: March 20, 2008
    Date of Patent: May 8, 2012
    Assignee: Takeda San Diego, Inc.
    Inventors: Zacharia Cheruvallath, Jun Feng, Prasuna Guntupalli, Stephen L. Gwaltney, Joanne Miura, Mark Sabat, Mingnam Tang
  • Publication number: 20120101271
    Abstract: 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: Application
    Filed: October 21, 2011
    Publication date: April 26, 2012
    Inventors: X. Peter Zhang, Hongjian Lu
  • Patent number: 8063042
    Abstract: 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: Grant
    Filed: July 10, 2008
    Date of Patent: November 22, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin
  • Publication number: 20110195960
    Abstract: 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: Application
    Filed: April 6, 2011
    Publication date: August 11, 2011
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
  • Patent number: 7973035
    Abstract: 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: Grant
    Filed: June 16, 2008
    Date of Patent: July 5, 2011
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
  • Publication number: 20110130391
    Abstract: 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: Application
    Filed: December 29, 2010
    Publication date: June 2, 2011
    Inventors: Richard G. Wilde, James J. Takasugi, Seongwoo Hwang, Ellen M. Welch, Guangming Chen
  • Publication number: 20110077236
    Abstract: 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: Application
    Filed: December 2, 2010
    Publication date: March 31, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning PRIEPKE, Kai GERLACH, Roland PFAU, Norbert HAUEL, Iris KAUFFMANN-HEFNER, Georg DAHMANN, Herbert NAR, Sandra HANDSCHUH, Wolfgang WIENEN, Annette SCHULER-METZ
  • Patent number: 7902186
    Abstract: 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: Grant
    Filed: October 25, 2006
    Date of Patent: March 8, 2011
    Assignee: Merck Patent GmbH
    Inventors: Oliver Schadt, Dieter Dorsch, Melanie Schultz, Andree Blaukat
  • Publication number: 20110044918
    Abstract: 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: Application
    Filed: October 29, 2010
    Publication date: February 24, 2011
    Applicant: L'OREAL
    Inventors: Xavier Marat, Benoit Muller
  • Publication number: 20100311733
    Abstract: 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: Application
    Filed: August 6, 2008
    Publication date: December 9, 2010
    Applicant: MERCK PATENT GESELLSCHAFT MIT ESCHRANKTER HAFTUNG
    Inventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
  • Publication number: 20100298278
    Abstract: The invention relates to the substituted 1,2-ethylenediamines of general formula (I), wherein the groups R1 to R13, A, B, L and i are defined as in the description and the claims. The invention also relates to the use thereof in the treatment of Alzheimer's disease (AD) and similar diseases.
    Type: Application
    Filed: August 8, 2006
    Publication date: November 25, 2010
    Inventors: Christian Eickmeier, Klaus Fuchs, Niklas Heine, Stefan Peters, Cornelia Dorner-Ciossek, Sandra Handschuh, Herbert Nar, Klaus Klinder
  • Publication number: 20100286129
    Abstract: 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: Application
    Filed: October 13, 2008
    Publication date: November 11, 2010
    Inventors: Gerard Botton, Caroline Leriche, Annick Arbellot De Vacqueur, Annick Audet, Johannes Gleitz
  • Publication number: 20100260711
    Abstract: The present invention relates to 3-Aminosulfonyl Substituted Indole Derivatives, 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: Application
    Filed: November 13, 2008
    Publication date: October 14, 2010
    Applicant: Schering Corporation
    Inventors: Kevin X. Chen, Stuart B. Rosenblum, F. George Njoroge, Joseph A. Kozlowski