Chalcogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/310.1)
-
Patent number: 10294208Abstract: The present invention relates to bendamustine derivatives and related compounds of formula (VII), (VIII) and (IX), and medical uses thereof in particular in cancer therapy.Type: GrantFiled: July 11, 2017Date of Patent: May 21, 2019Assignee: SYNBIAS PHARMA AGInventor: Helmut Schickaneder
-
Patent number: 9688670Abstract: The present invention provides a medicament for treating a disease involving Nav 1.7 such as neuropathic pain, nociceptive pain, inflammatory pain, small-fiber neuropathy, erythromelalgia, paroxysmal extreme pain disorder, dysuria, and multiple sclerosis, which comprises a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1a, R1b, R1c and R1d are hydrogen, halogen, cyano, C1-4 alkyl, C1-4 alkoxy, or the like, provided that at least one of R1a, R1b, R1c and R1d is C6-10 aryl, C6-10 aryloxy, or the like, R2 and R3 are hydrogen, C1-6 alkyl, C3-10 cycloalkyl, or the like, R4 is hydrogen, C1-6 alkyl, C3-7 cycloalkyl, or the like, m is 1, 2 or 3, L is CR7R8, and R7 and R8 are hydrogen, hydroxyl, C1-4 alkyl, C1-4 alkoxy, or the like.Type: GrantFiled: December 30, 2016Date of Patent: June 27, 2017Assignee: Sumitomo Dainippon Pharma Co., Ltd.Inventors: Masafumi Komiya, Kohei Iwamoto, Toshio Kanai, Shingo Mizushima, Keiji Adachi, Kuniko Urashima
-
Patent number: 9643932Abstract: The present invention relates to an improved process for the synthesis of bendamustine, in particular, bendamustine hydrochloride of the formula (VI) and its intermediate 1-methyl-5-[bis(2-chloroethyl)amino]-1H-benzimidazol-2-yl]lithium butanoate of formula (V), both having a purity of ?99%, which is simple, convenient, economical, does not use hazardous chemicals and is industrially viable.Type: GrantFiled: December 19, 2014Date of Patent: May 9, 2017Assignee: Fresenius Kabi Oncology LimitedInventors: Bhuwan Bhaskar Mishra, Nikunj Shambhubhai Kachhadia, Vinod Singh Tomar, Saswata Lahiri
-
Patent number: 9452988Abstract: The present invention is directed to bendamustine esters and bendamustine amides and their use for the treatment of cancer.Type: GrantFiled: November 12, 2013Date of Patent: September 27, 2016Assignee: Ignyta, Inc.Inventors: Roger P. Bakale, Peter D. Brown, Jian Chen, Anthony S. Drager, Rachel Y. Labell, Robert E. McKean, Piyush R. Patel, Renee C. Roemmele, Bradley McIntyre
-
Patent number: 9149464Abstract: The present invention is directed to bendamustine esters and bendamustine amides and their use for the treatment of cancer.Type: GrantFiled: May 13, 2015Date of Patent: October 6, 2015Assignee: IGNYTA, INC.Inventors: Roger P. Bakale, Peter D. Brown, Jian Chen, Anthony S. Drager, Rachel Y. Labell, Robert E. McKean, Piyush R. Patel, Renee C. Roemmele
-
Publication number: 20150105561Abstract: The present invention relates to an improved process for the synthesis of bendamustine, in particular, bendamustine hydrochloride of the formula (VI) and its intermediate 1-methyl-5-[bis(2-chloroethyl)amino]-1H-benzimidazol-2-yl]lithium butanoate of formula (V), both having a purity of ?99%, which is simple, convenient, economical, does not use hazardous chemicals and is industrially viable.Type: ApplicationFiled: December 19, 2014Publication date: April 16, 2015Inventors: Bhuwan Bhaskar Mishra, Nikunj Shambhubhai Kachhadia, Vinod Singh Tomar, Saswata Lahiri
-
Patent number: 9006454Abstract: The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.Type: GrantFiled: March 26, 2010Date of Patent: April 14, 2015Assignee: Merck Serono S.A.Inventors: Siva Sanjeeva Rao Thunuguntla, Hosahalli Subramanya, Satish Reddy Kunnam, Sekhar Reddy Sanivaru Vijay, Chakrapani Bingi, Raviraj Kusanur, Matthias Schwarz, Michael Arlt
-
Publication number: 20150087617Abstract: The invention provides indole and indoline derivatives and slats thereof, compositions comprising them and uses thereof for the treatment of diseases and disorders.Type: ApplicationFiled: April 2, 2013Publication date: March 26, 2015Inventors: Abraham Nudelman, Marta Weinstock-Rosin
-
Patent number: 8987469Abstract: The present invention relates to a method for preparation of alkyl 4-[5-[bis(2 -hydroxyethyl)amino]-1-methyl-1H-benzimidazol-2-yl]butanoate (7) from 2-fluoro-5-nitroaniline, comprising the steps of: (a) conversion of 2-fluoro-5-nitroaniline to 5-(2-fluoro-5-nitroanilino)-5 -oxopentanoic acid (1) using glutaric anhydride, conversion of compound (1) to methylammonium 5-[2-(methylamino)-5-nitroanilino]-5-oxopentanoate (2) using methylamine; conversion of compound (2) to 5[2-(methylamino)-5-nitroanilino]-5-oxopentanoic acid (3) and condensation of compound (3) to 4-(1-methyl-5-nitro-1H-benzimidazol-2-yl)butanoic acid (4); (b) esterification of the product (4) of step a) to alkyl 4-(1-methyl-5-nitro 1H-benzimidazol-2-yl)butanoate (5); (c) reduction of the product of step b) to alkyl 4-(5-amino-l-methyl-1H-benzimidazol-2-yl)butanoate (6), and (d) conversion of the product of step c) to alkyl 4-[5-[bis(2-hydroxyethyl)amino]-1-methyl -1H-benzimidazol-2-yl]butanoate (7).Type: GrantFiled: July 23, 2013Date of Patent: March 24, 2015Assignee: Heyl Chemisch-pharmazeutische Fabrik GmbH & Co. KGInventors: Michael Frey, Dirk-Detlef Walther
-
Publication number: 20150051258Abstract: Novel solid forms of bendamustine hydrochloride are described, as well as methods of their preparation and use.Type: ApplicationFiled: November 3, 2014Publication date: February 19, 2015Inventors: Martin Ian Cooper, Laurent D. Courvoisier, Mark Eddleston, Robert E. McKean
-
Publication number: 20150011591Abstract: The present invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof; wherein R, R1, R2, R3, R4, m, and n are as defined herein, to pharmaceutical compositions comprising said compound, and to methods of treating diseases or conditions mediated by elevated persistent sodium current, such as an ocular disorder, multiple sclerosis, seizure disorder, and chronic pain.Type: ApplicationFiled: September 24, 2014Publication date: January 8, 2015Inventors: George R. Ehring, Ellen Chao, Herman Ng, Hau Ton, Jia Chian Li, Joseph S. Adorante, Michael E. Garst, Howard B. Rind, Mark R. Hansen, Alfred Arthur Avey, JR., Lloyd Jay Dolby, Shervin Esfandiari, Vivian R. MacKenzie, Jeremiah Andrew Marsden, David Charles Muchmore
-
Publication number: 20150004533Abstract: An actinic ray-sensitive or radiation-sensitive resin composition in the present invention contains a nitrogen-containing compound (N) which is represented by the following general formula (N1): wherein, in the general formula (N1), X represents a group including a hetero atom; L represents a single bond or an alkylene group; R2 represents a substituent, in the case where a plurality of R2's are present, they may be the same as or different from each other and a plurality of R2's may be bonded to each other to form a ring; R3 represents a hydrogen atom or a substituent; and n represents an integer of 0 to 4.Type: ApplicationFiled: September 5, 2014Publication date: January 1, 2015Applicant: FUJIFILM CORPORATIONInventors: Shuji HIRANO, Hiroo TAKIZAWA, Hideaki TSUBAKI
-
Patent number: 8912186Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.Type: GrantFiled: October 16, 2009Date of Patent: December 16, 2014Assignee: Universitaet des SaarlandesInventors: Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi
-
Patent number: 8883836Abstract: Novel solid forms of bendamustine hydrochloride are described, as well as methods of their preparation and use.Type: GrantFiled: March 7, 2014Date of Patent: November 11, 2014Assignee: Cephalon, Inc.Inventors: Martin Ian Cooper, Laurent D. Courvoisier, Mark Eddleston, Robert E. McKean
-
Publication number: 20140322278Abstract: Compositions and methods are provided for modulating the physiological activation of tissue transglutaminase (TG2); which methods can include inhibiting the activation of TG2 associated with enteric inflammatory disorders, which disorders may include celiac disease, irritable bowel syndrome, Crohn's Disease, dermatitis herpetiformis, and the like. In other embodiments of the invention, methods are provided for reducing undesirable paracellular transport in enteric tissues, in particular the paracellular transport of molecules greater than about 500 mw, e.g. peptides, including without limitation immunogenic gluten peptides.Type: ApplicationFiled: June 19, 2012Publication date: October 30, 2014Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Thomas DiRaimondo, Xi Jin, Cornelius Kloeck, Chaitan Khosla
-
Publication number: 20140315960Abstract: The present invention relates to novel depot formulations (prodrugs) comprising an immobility promoting unit linked via an ester to an active pharmaceutical ingredient, i.a. common NSAIDs. The novel depot formulations are suitable for intra-articular injections and are soluble at slightly acidic pH to facilitate ease of injection, and sparingly soluble at physiological pH thereby precipitating at the site of administration. The precipitate will slowly dissolve and the active drug is released from dissolved depot formulation following esterase mediated cleavage of the ester link between the immobility promoting unit and the active pharmaceutical agent.Type: ApplicationFiled: October 31, 2012Publication date: October 23, 2014Inventor: Claus Selch LARSEN
-
Patent number: 8859780Abstract: The present invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof; wherein R, R1, R2, R3, R4, m, and n are as defined herein, to pharmaceutical compositions comprising said compound, and to methods of treating diseases or conditions mediated by elevated persistent sodium current, such as an ocular disorder, multiple sclerosis, seizure disorder, and chronic pain.Type: GrantFiled: December 27, 2012Date of Patent: October 14, 2014Assignee: Allergan, Inc.Inventors: George R. Ehring, Ellen Chao, Herman Ng, Hau Ton, Jia Chian Li, Joseph S. Adorante, Michael S. Garst, Howard B. Rind, Mark R. Hansen, Alfred Arthur Avey, Jr., Lloyd Jay Dolby, Shervin Esfandiari, Vivian R. MacKenzie, Jeremiah Andrew Marsden, David Charles Muchmore
-
Publication number: 20140275567Abstract: An alkyl ester of 4-(5-(bis(2-hydroxyethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butyric acid, such as ethyl 4-(5-(bis(2-hydroxyethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoate, is obtained by reacting an alkyl ester of 4-(5-amino-1-methyl-1H-benzo[d]imidazol-2-yl)butyric acid with 2-hydroxyacetaldehyde under reducing conditions.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: JOHNSON MATTHEY PLCInventors: Xing Fu, Saroop Singh Matharu
-
Publication number: 20140275566Abstract: Wet bendamustine hydrochloride monohydrate may be dried by a two stage process wherein rapid drying is first carried out to provide a partially dried product, which is then further dried using an inert gas of controlled relative humidity to yield dry bendamustine hydrochloride monohydrate.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: JOHNSON MATTHEY PLCInventors: Xing Fu, Jeremy Clinton Wilt
-
Publication number: 20140249196Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit cdk5-mediated phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: ApplicationFiled: November 20, 2012Publication date: September 4, 2014Inventors: Theodore Mark Kamenecka, Patrick R. Griffin, Amy S. Ripka, Jeffrey O. Saunders
-
Patent number: 8809327Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.Type: GrantFiled: February 28, 2012Date of Patent: August 19, 2014Assignee: Janssen Pharmaceutica, NVInventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
-
Patent number: 8802865Abstract: The present invention is directed to a novel 2-substituted benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: GrantFiled: October 1, 2013Date of Patent: August 12, 2014Assignee: Janssen Pharmaceutica, NVInventors: Vernon C Alford, Jr., James C Lanter, Raymond A Ng
-
Publication number: 20140187598Abstract: Novel solid forms of bendamustine hydrochloride are described, as well as methods of their preparation and use.Type: ApplicationFiled: March 7, 2014Publication date: July 3, 2014Applicant: Cephalon, Inc.Inventors: Martin Ian Cooper, Laurent D. Courvoisier, Mark Eddleston, Robert E. McKean
-
Publication number: 20140148490Abstract: The present invention provides pharmaceutical formulations of lyophilized bendamustine suitable for pharmaceutical use. The present invention further provides methods of producing lyophilized bendamustine. The pharmaceutical formulations can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases.Type: ApplicationFiled: January 31, 2014Publication date: May 29, 2014Applicant: Cephalon, Inc.Inventors: Jason Edward Brittain, Joe Craig Franklin
-
Publication number: 20140142153Abstract: Aspects of the present appliction relate to pharmaceutical formulations comprising bendamustine or its pharmaceutically acceptable salts, isomers, racemates, enantiomers, hydrates, solvates, metabolites, polymorphs, and mixtures therof, suitable for phamaceutical use. Aspects further provide methods of producing stable bendamustine compositions.Type: ApplicationFiled: January 25, 2012Publication date: May 22, 2014Applicants: DR. REDDY'S LABORATORIES, INC., DR. REDDY'S LABORATORIES LTD.Inventors: Chandrasekhar Kocherlakota, Tarun Singh, Nagaraju Banda, Nirmal Khati, Sachin Sharma, Prasad Vure, Aparna Mulupuru, Navin Vaya, Amit Anil Charkha
-
Publication number: 20140121384Abstract: The present invention provides a process for the preparation of 1H-benzimidazol-1-methyl-5-N,N-di(2-hydroxyethyl)-2-butanoic acid ethyl ester. The present invention also provides a process for the preparation of bendamustine hydrochloride. The present invention further provides a process for the purification of bendamustine hydrochloride.Type: ApplicationFiled: May 24, 2012Publication date: May 1, 2014Applicant: Hetero Research FoundationInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reedy, Dasari Muralidhara Reddy, Bandi Vamsi Krishna
-
Publication number: 20140121383Abstract: The present invention relates to an improved process for the synthesis of bendamustine, in particular, bendamustine hydrochloride of the formula (VI) and its intermediate 1-Methyl-5-[bis(2-chloroethyl)amino]-1H-benzimidazol-2-yl]lithium butanoate of formula (V), both having a purity of ?99%, which is simple, convenient, economical, does not use hazardous chemicals and industrially viable.Type: ApplicationFiled: September 20, 2012Publication date: May 1, 2014Applicant: FRESENIUS KABI ONCOLOGY LIMITEDInventor: FRESENIUS KABI ONCOLOGY LIMITED
-
Patent number: 8669279Abstract: Novel solid forms of bendamustine hydrochloride are described, as well as methods of their preparation and use.Type: GrantFiled: May 1, 2013Date of Patent: March 11, 2014Assignee: Cephalon, Inc.Inventors: Martin Ian Cooper, Laurent D. Courvoisier, Mark Eddleston, Robert E. McKean
-
Publication number: 20140031560Abstract: The present invention relates to a method for preparation of alkyl 4-[5-[bis(2-hydroxyethyl)amino]-1-methyl-1H-benzimidazol-2-yl]butanoate (7) from 2-fluoro-5-nitroaniline, comprising the steps of: (a) conversion of 2-fluoro-5-nitroaniline to 5-(2-fluoro-5-nitroanilino)-5-oxopentanoic acid (1) using glutaric anhydride, conversion of compound (1) to methylammonium 5-[2-(methylamino)-5-nitroanilino]-5-oxopentanoate (2) using methylamine; conversion of compound (2) to 5-[2-(methylamino)-5-nitroanilino]-5-oxopentanoic acid (3) and condensation of compound (3) to 4-(1-methyl-5-nitro-1H-benzimidazol-2-yl)butanoic acid (4); (b) esterification of the product (4) of step a) to alkyl 4-(1-methyl-5-nitro1H-benzimidazol-2-yl)butanoate (5); (c) reduction of the product of step b) to alkyl 4-(5-amino-1-methyl-1H-benzimidazol-2-yl)butanoate (6), and (d) conversion of the product of step c) to alkyl 4-[5-[bis(2-hydroxyethyl)amino]-1-methyl-1H-benzimidazol-2-yl]butanoate (7)Type: ApplicationFiled: July 23, 2013Publication date: January 30, 2014Applicant: Heyl Chemisch-pharmazeutische Fabrik GmbH & Co. KGInventors: Michael Frey, Dirk-Detlef Walther
-
Publication number: 20140018373Abstract: A fused heterocyclic compound the formula (1): wherein A1 represents —NR8—, and the like; A2 represents a nitrogen atom, and the like; A3 represents a nitrogen atom, and the like; R1 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R2, R3, R4, and R5 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more halogen atoms, and the like; R6 and R7 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R8 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group W, and the like; n represents 0, 1 or 2. The compound has an excellent activity of controlling pests.Type: ApplicationFiled: December 22, 2011Publication date: January 16, 2014Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Hayato Takyo, Masaki Takahashi, Takamasa Tanabe, Yoshihiko Nokura, Mai Ito, Atsushi Iwata
-
Publication number: 20140017701Abstract: The invention provides chimeric 3-phosphoinositide-dependent protein kinase 1 (PDK1), the PIF-binding pocket of which has mutations to mimic a second protein kinase, its production and use. The invention further provides a method for screening for compounds interacting with the PIF-pocket of an AGC kinase.Type: ApplicationFiled: February 24, 2012Publication date: January 16, 2014Inventors: Ricardo M. Biondi, Laura A. L. Lopez Garcia, Jörg O. Schulze
-
Publication number: 20130338205Abstract: The present invention provides pharmaceutical formulations of lyophilized bendamustine suitable for pharmaceutical use. The present invention further provides methods of producing lyophilized bendamustine. The pharmaceutical formulations can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases.Type: ApplicationFiled: August 19, 2013Publication date: December 19, 2013Applicant: Cephalon, Inc.Inventors: Jason Edward Brittain, Joe Craig Franklin
-
Patent number: 8604217Abstract: A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine and tyrosine kinases and a serine/threonine and tyrosine kinases modulating agent. Novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, new derivatives of tetrahalogenated benzimidazole with serine/threonine and tyrosine kinases inhibitory properties, preferably selected from the group of PIM, HIPK, DYRK, CLK, CDK, FLT, PKG, Haspin, MER, TAO, MNK, TRK kinases which exhibit superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on serine/threonine and tyrosine kinases, such as but not limited to leukemias and solid tumors.Type: GrantFiled: December 28, 2011Date of Patent: December 10, 2013Assignee: Selvita S.A.Inventors: Krzysztof Brzózka, Wojciech Czardybon, Aleksandra Sabiniarz, Mariusz Millik, Renata Windak, Adrian Zarebski, Nicolas Beuzen
-
Patent number: 8598078Abstract: Compounds of Formula I wherein the substituents are as defined in Claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: August 21, 2008Date of Patent: December 3, 2013Assignee: Syngenta Crop Protection, LLCInventors: Olivier Loiseleur, Roger Graham Hall, André Denis Stoller, Gerald Wayne Craig, André Jeanguenat, Andrew Edmunds
-
Publication number: 20130317234Abstract: The present invention relates to a process for the preparation of 4-{5-{Bis-(2-hydroxyl-ethyl)-amino}-1-methyl-1H-Benzoimidazol-2yl}-butyric acid alkyl ester of formula IV, a key intermediate in the process for the preparation of Bendamustine HCl (I)Type: ApplicationFiled: July 14, 2011Publication date: November 28, 2013Applicant: BIOPHORE INDIA PHARMACEUTICALS PVT. LTDInventors: Manik Reddy Pullagurla, Jagadeesh Babu Rangisetty, S. I. Davis Presley, Radha Nagarapu
-
Publication number: 20130310571Abstract: Improved methods for the preparation and purification of bendamustine hydrochloride are described; such as method of preparing bendamustine hydrochloride comprising contacting a compound of formula HBI: with thionyl chlorideType: ApplicationFiled: January 18, 2012Publication date: November 21, 2013Applicant: Cephalon, IncInventors: Anton H. Gayring, Scott A. Miller
-
Patent number: 8586616Abstract: The present invention is directed to novel benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: GrantFiled: December 16, 2010Date of Patent: November 19, 2013Assignee: Janssen Pharmaceutica, NVInventors: Raymond Ng, Zhihua Sui, Jihua Guan, James C. Lanter, Vernon C. Alford, Jr.
-
Publication number: 20130289032Abstract: The present invention relates to particular esters of bendamustine and related compounds, and medical uses thereof.Type: ApplicationFiled: April 25, 2013Publication date: October 31, 2013Inventors: Helmut SCHICKANEDER, Armin Buschauer, Guenther Bernhardt, Christian Schickaneder, Michael Limmert, Stefan Huber
-
Publication number: 20130245086Abstract: Novel solid forms of bendamustine hydrochloride are described, as well as methods of their preparation and use.Type: ApplicationFiled: May 1, 2013Publication date: September 19, 2013Applicant: Cephalon, Inc.Inventors: Martin Ian Cooper, Laurent D. Courvoisier, Mark Eddleston, Robert E. McKean
-
Publication number: 20130217888Abstract: The present invention provide processes for the preparation of Bendamustine hydrochloride monohydrate of formula (I) The present application also provides a process of purification of Bendamustine hydrochloride or monohydrate to get substantially pure Bendamustine hydrochloride monohydrate crystalline Form-SM. The said Bendamustine hydrochloride monohydrate crystalline Form-SM is characterized by X-ray powder diffraction pattern comprising at least 5 characteristic peaks selected from the XRPD 2 theta degrees peaks at 7.42, 10.60, 11.17, 16.43, 17.94, 22.89, 26.33, 28.77, 30.28, 31.92, 40.89±0.1 2?°. The present application also provides a process for the preparation of Bendamustine hydrochloride monohydrate crystalline Form-SM useful in making pharmaceutical composition for the treatment of cancer or similar proliferative disorders.Type: ApplicationFiled: August 29, 2011Publication date: August 22, 2013Applicant: SHAILPA MEDICARE LIMITEDInventors: Vimal Kumar Shrawat, Seshachalam Unnam, Vinod Kumar Singh, Prashant Purohit
-
Publication number: 20130204009Abstract: There is provided a more industrially advantageous process for preparing novel pyridine derivatives expected to be used as medicines. A process for preparing 3-[(6-hydroxy-1-methyl-1H-benzimidazol-2-yl)methoxy]benzoic acid esters as intermediates with high quality, in short steps and in a high yield, as well as novel benzoic acid esters as their precursors and a process for preparing the same.Type: ApplicationFiled: February 26, 2013Publication date: August 8, 2013Applicant: Daiichi Sankyo Company, LimitedInventor: Daiichi Sankyo Company, Limited
-
Publication number: 20130184471Abstract: The present invention relates to a process for preparing bendamustine hydrochloride, derivatives and related compounds thereof.Type: ApplicationFiled: January 16, 2013Publication date: July 18, 2013Applicant: Arevipharma GmbHInventor: Arevipharma GmbH
-
Patent number: 8481751Abstract: Methods are provided for the production of bendamustine alkyl ester, bendamustine, as well as derivatives thereof. With the methods the production of these compounds is possible in reproducibly high yields. To this end, hydroxyl-group-containing esters are used as the starting material, whose hydroxyl groups are substituted in a simple way by halogen groups. This substitution is possible in the presence of (i) oxalyl chloride and (ii) dialkylformamide, dialkyl acetamide or dimethyl sulfoxide. In a subsequent reaction, the resulting esters can be hydrolyzed to form the acid.Type: GrantFiled: December 22, 2011Date of Patent: July 9, 2013Assignee: Heraeus Precious Metals GmbH & Co. KGInventors: Kai Groh, Holger Rauter, Dirk Born
-
Publication number: 20130172389Abstract: The present invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof; wherein R, R1, R2, R3, R4, m, and n are as defined herein, to pharmaceutical compositions comprising said compound, and to methods of treating diseases or conditions mediated by elevated persistent sodium current, such as an ocular disorder, multiple sclerosis, seizure disorder, and chronic pain.Type: ApplicationFiled: December 27, 2012Publication date: July 4, 2013Applicant: Allegan, Inc.Inventor: Allergan, Inc.
-
Publication number: 20130158273Abstract: The present application relate to processes for the preparation of bendamustine and its pharmaceutically acceptable salts.Type: ApplicationFiled: December 22, 2010Publication date: June 20, 2013Applicants: DR. REDDY'S LABORATORIES, INC., DR. REDDY'S LABORATORIES, LTD.Inventors: Rajasekhar Kadaboina, Veerender Murki, Venkat Rao Badisa, Nageshwar Gunda
-
Patent number: 8461351Abstract: A sterically bulky stabilizer that includes an alkylated-benzimidazolone compound, where the sterically bulky stabilizer is associated non-covalently with a benzimidazolone pigment, and the presence of the sterically bulky stabilizer limits the extent of particle growth and aggregation, to afford nanoscale pigment particles.Type: GrantFiled: July 28, 2011Date of Patent: June 11, 2013Assignees: Xerox Corporation, National Research Council of CanadaInventors: Rina Carlini, Darren Andrew Makeiff
-
Publication number: 20130144068Abstract: The present application is directed to methods of sterilizing bendamustine and its pharmaceutically acceptable salt forms. Preferred sterilization methods include dry heat sterilization, gamma irradiation, and e beam radiation. Sterile pharmaceutical compositions are also described.Type: ApplicationFiled: January 9, 2013Publication date: June 6, 2013Applicant: Cephalon, Inc.Inventor: Cephalon, Inc..
-
Patent number: 8445524Abstract: Novel solid forms of bendamustine hydrochloride are described, as well as methods of their preparation and use.Type: GrantFiled: November 22, 2011Date of Patent: May 21, 2013Assignee: Cephalon, Inc.Inventors: Robert E. McKean, Hans-Joachim Jänsch, Veronique Courvoisier
-
Patent number: 8440172Abstract: The invention concerns preparations, particularly cosmetic or pharmaceutical/dermatological preparations, containing phenylbenzimidazole sulfonic acid (i.e. 2-phenylbenzimidazole-5-sulfonic acid) neutralised with basic amino acids such as arginine, lysine, ornithine and histidine so that the pH of the preparation can be at or below 7.0 without incurring crystallization of the phenylbenzimidazole sulfonic acid.Type: GrantFiled: July 9, 2007Date of Patent: May 14, 2013Assignee: Symrise AGInventors: William Johncock, Jürgen Claus
-
Patent number: 8420829Abstract: New methods for the preparation of bendamustine, and the pharmaceutical salts thereof, are described. Novel compounds useful for the preparation of bendamustine are also described.Type: GrantFiled: April 5, 2011Date of Patent: April 16, 2013Assignee: Cephalon, Inc.Inventors: Jian Chen, Katrin Przyuski, Renee Caroline Roemmele