The present invention relates to a lectin for use in the treatment, reduction in progression and curing of inflammation in a subject in need thereof. Pharmaceutical compositions comprising said lectin are also described. The lectin may comprise an amino acid sequence having sequence of SEQ ID NO: 1 or at least 60% homology to SEQ ID NO: 2.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
A61P 19/02 - Médicaments pour le traitement des troubles du squelette des troubles articulaires, p. ex. arthrites, arthroses
2.
AN IMPROVED PROCESS FOR MANUFACTURING OF VALPROIC ACID AND/OR ITS SALT
The present invention provides an improved process for manufacturing of Valproic acid, intermediates, and sodium salt of valproic acid (Divalproex sodium). The present invention provides sequential additions of reactants and/or catalyst or reagents and/or solvent(s) which is most effective to achieve maximum conversion efficiency, less or no impurity formation, which overall results in increased yield as well as purity not less than 99%. Furthermore, it involves use of green solvents (recover and/or recycle easily); mild & cheaper catalyst or reagent; reduced reaction time and steps to be performed. In the present invention, synthesis of valproic acid is carried out without isolating any intermediate compound; and divalproex sodium is synthesised by heating valproic acid without use of solvent at about 60°C to about 110°C. The obtained compound of formula (Divalproex sodium) is substantially free of impurities.
C07C 53/128 - Acides contenant au moins cinq atomes de carbone le groupe carboxyle étant lié à un atome de carbone lié lui-même à plusieurs autres atomes de carbone, p. ex. néo-acides
C07C 51/41 - Préparation de sels d'acides carboxyliques par conversion de ces acides ou de leurs sels en sels ayant la même partie acide carboxylique
C07C 51/08 - Préparation d'acides carboxyliques, de leurs sels, halogénures ou anhydrides à partir de nitriles
C07C 253/30 - Préparation de nitriles d'acides carboxyliques par des réactions n'impliquant pas la formation de groupes cyano
C07C 255/19 - Nitriles d'acides carboxyliques ayant des groupes cyano liés à des atomes de carbone acycliques contenant des groupes cyano et des groupes carboxyle, autres que des groupes cyano, liés au même squelette carboné acyclique saturé
3.
PROTEIN COMPOSITIONS FOR THE TREATMENT OF INFLAMMATORY DISEASES
The present invention relates to the pharmaceutical compositions of lectin proteins and its use for the prevention, treatment and cure of inflammation, including inflammatory disease. The invention specifically relates to the pharmaceutical compositions for topical application comprising lectin proteins and its use for prevention, treatment and cure of inflammation due to chemotherapy and/or radiotherapy. The lectin may comprise an amino acid sequence having sequence of SEQ ID NO: 1 or at least 70% homology to SEQ ID NO: 1.
The present invention relates to the protein for treatment of infectious disease caused by Coronaviridae. In particular, the invention relates to a recombinant Sclerotium rolfsii lectin for use in the treatment, reduction in progression and curing of SARS-COV2 disease in a subject in need thereof. Pharmaceutical compositions comprising said recombinant Sclerotium rolfsii lectin are also described. The recombinant Sclerotium rolfsii lectin protein may comprise an amino acid sequence having at least 70% homology to SEQ ID NO: 1.
The present invention relates to the lectin protein for the treatment and prevention of neurodegenerative diseases. The invention further relates to the recombinant lectin protein is derived from Sclerotium rolfsii lectin having sequence 60% homologous to SEQ ID NO: 4 for the treatment and prevention of Neurodegenerative diseases. The invention specifically relates to lectin protein and its variants is derived from Sclerotium rolfsii lectin having sequence 60% homologous to SEQ ID NO: 4 for the treatment of prevention of Parkinson's disease, Alzheimer's disease, Dementia and symptoms of dementia.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p. ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
C07K 14/37 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant de champignons
The present disclosure provides a modified protein sequence i.e., recombinantly expressed glycan binding protein. The said glycan binding protein is a variant of Sclerotium Rolfsii Lectin and is modified to include attributes like enhanced molecule stability, reduced N-terminal methionine impurities and aid in conjugation of protein to other biological and chemical agent(s).
C07K 14/37 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant de champignons
A61K 47/64 - Conjugués médicament-peptide, médicament-protéine ou médicament-acide polyaminé, c.-à-d. l’agent de modification étant un peptide, une protéine ou un acide polyaminé lié par covalence ou complexé à un agent thérapeutiquement actif
7.
RECOMBINANT PROTEINS, COMPOSITIONS AND METHODS OF STABILIZATION THEREOF
The present invention relates to recombinant proteins, compositions and methods of stabilization thereof. The invention specifically relates to the stable recombinant protein of SEQ ID NO: 1 and composition comprising recombinant protein of SEQ ID NO: 1. The invention further relates to method of preparing, storing and stabilizing recombinant protein of SEQ ID NO: 1 and its composition for longer shelf life.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
A61K 47/18 - AminesAmidesUréesComposés d’ammonium quaternaireAcides aminésOligopeptides ayant jusqu’à cinq acides aminés
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
8.
A STABLE PHARMACEUTICAL COMPOSITION AND PROCESS FOR PREPARING THEREOF
The present invention provides a binder free an immediate release oral stable pharmaceutical composition and process for preparing the same. Said pharmaceutical composition comprising a crystalline solriamfetol or a pharmaceutically acceptable salt thereof; and one or more pharmaceutically acceptable excipients, wherein pharmaceutically acceptable salt is solriamfetol hydrochloride in anhydrous crystalline Form A.
The present invention relates to a recombinant plasmid, methods and compositions for the expression of recombinant proteins with minimal N-terminal initiator methionine. The present invention also provides strategies for efficient removal of N-terminal initiator methionine in recombinant proteins expressed at industrial scale and provides method for producing proteins with minimal N-terminal initiator methionine.
The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; wherein Q is a group of formula Q1 or Q2; wavy bond represents the points of attachment; wherein R1 is —NRaRb; R2 is hydrogen or a C1-C10 alkyl group; Ra and Rb independently represent hydrogen or a C1-C10 alkyl group, and use of these compounds as kinase inhibitors and compositions comprising the compounds of the present invention.
The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; wherein Q is a group of formula Q1 or Q2; wavy bond represents the points of attachment; wherein R1 is —NRaRb; R2 is hydrogen or a C1-C10 alkyl group; Ra and Rb independently represent hydrogen or a C1-C10 alkyl group, and use of these compounds as kinase inhibitors and compositions comprising the compounds of the present invention.
The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; wherein Q is a group of formula Q1 or Q2; wavy bond represents the points of attachment; wherein R1 is —NRaRb; R2 is hydrogen or a C1-C10 alkyl group; Ra and Rb independently represent hydrogen or a C1-C10 alkyl group, and use of these compounds as kinase inhibitors and compositions comprising the compounds of the present invention.
(wavy bond)
A recombinant lectin for use in a method of treatment of cancer by inhibiting angiogenesis in a subject. The treatment comprises administration of a therapeutically effective amount of the recombinant lectin.
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
A61P 19/02 - Médicaments pour le traitement des troubles du squelette des troubles articulaires, p. ex. arthrites, arthroses
13.
SUBSTITUTED TRICYCLIC COMPOUNDS AND THEIR USE IN COVID-19
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
A61P 31/14 - Antiviraux pour le traitement des virus ARN
14.
SUBSTITUTED TRICYCLIC COMPOUNDS AND THEIR USE IN ULCERATIVE COLITIS
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
A61P 1/00 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif
15.
RECOMBINANT PROTEIN FOR TREATING SARS-COV2 DISEASE
Sclerotium rolfsiiSclerotium rolfsiiSclerotium rolfsiiSclerotium rolfsii lectin protein may comprise an amino acid sequence having at least 70% homology to SEQ ID NO:1.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
The present invention relates to the protein for treatment of infectious disease caused by Coronaviridae. In particular, the invention relates to a recombinant Sclerotium rolfsii lectin for use in the treatment, reduction in progression and curing of SARS-COV2disease in a subject in need thereof. Pharmaceutical compositions comprising said recombinant Sclerotium rolfsii lectin are also described. The recombinant Sclerotium rolfsii lectin protein may comprise an amino acid sequence having at least 70% homology to SEQ ID NO:1.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
The present disclosure provides a modified protein sequence i.e., recombinantly expressed glycan binding protein. The said glycan binding protein is a variant of Sclerotium Rolfsii Lectin and is modified to include attributes like enhanced molecule stability, reduced N-terminal methionine impurities and aid in conjugation of protein to other biological and chemical agent(s).
A61K 38/00 - Préparations médicinales contenant des peptides
A61K 47/64 - Conjugués médicament-peptide, médicament-protéine ou médicament-acide polyaminé, c.-à-d. l’agent de modification étant un peptide, une protéine ou un acide polyaminé lié par covalence ou complexé à un agent thérapeutiquement actif
The present disclosure relates to protein-drug conjugates. The present disclosure specifically relates to the protein-drug conjugates, wherein the protein is a lectin protein having amino acid sequence of SEQ ID NO: 1; or lectin protein having at least 70% sequence identity to SEQ ID NO: 1. The disclosure further relates to process and composition of protein-drug conjugates and method of use thereof.
A61K 47/64 - Conjugués médicament-peptide, médicament-protéine ou médicament-acide polyaminé, c.-à-d. l’agent de modification étant un peptide, une protéine ou un acide polyaminé lié par covalence ou complexé à un agent thérapeutiquement actif
C07K 14/37 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant de champignons
C07K 14/375 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant de champignons provenant de Basidiomycetes
C12N 15/31 - Gènes codant pour des protéines microbiennes, p. ex. entérotoxines
The present disclosure relates to protein-drug conjugates. The present disclosure specifically relates to the protein-drug conjugates, wherein the protein is a lectin protein having amino acid sequence of SEQ ID NO: 1; or lectin protein having at least 70% sequence identity to SEQ ID NO: 1. The disclosure further relates to process and composition of protein-drug conjugates and method of use thereof.
A61K 47/64 - Conjugués médicament-peptide, médicament-protéine ou médicament-acide polyaminé, c.-à-d. l’agent de modification étant un peptide, une protéine ou un acide polyaminé lié par covalence ou complexé à un agent thérapeutiquement actif
The present disclosure provides a modified protein sequence i.e., recombinantly expressed glycan binding protein. The said glycan binding protein is a variant of Sclerotium Rolfsii Lectin and is modified to include attributes like enhanced molecule stability, reduced N-terminal methionine impurities and aid in conjugation of protein to other biological and chemical agent(s).
C07K 14/37 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant de champignons
A61K 47/64 - Conjugués médicament-peptide, médicament-protéine ou médicament-acide polyaminé, c.-à-d. l’agent de modification étant un peptide, une protéine ou un acide polyaminé lié par covalence ou complexé à un agent thérapeutiquement actif
The present invention relates to the pharmaceutical compositions of lectin proteins and its use for the prevention, treatment and cure of inflammation, including inflammatory disease. The invention specifically relates to the pharmaceutical compositions for topical application comprising lectin proteins and its use for prevention, treatment and cure of inflammation due to chemotherapy and/or radiotherapy. The lectin may comprise an amino acid sequence having sequence of SEQ ID NO: 1 or at least 70% homology to SEQ ID NO: 1.
A61K 38/16 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés
A61P 1/02 - Préparations stomatologiques, p. ex. médicaments pour le traitement des caries, des aphtes, des périodontites
A61P 1/04 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif des ulcères, des gastrites ou des œsophagites par reflux, p. ex. antiacides, antisécrétoires, protecteurs de la muqueuse
22.
PROTEIN COMPOSITIONS FOR THE TREATMENT OF INFLAMMATORY DISEASES
The present invention relates to the pharmaceutical compositions of lectin proteins and its use for the prevention, treatment and cure of inflammation, including inflammatory disease. The invention specifically relates to the pharmaceutical compositions for topical application comprising lectin proteins and its use for prevention, treatment and cure of inflammation due to chemotherapy and/or radiotherapy. The lectin may comprise an amino acid sequence having sequence of SEQ ID NO: 1 or at least 70% homology to SEQ ID NO: 1.
A61K 38/16 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés
A61P 1/02 - Préparations stomatologiques, p. ex. médicaments pour le traitement des caries, des aphtes, des périodontites
A61P 1/04 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif des ulcères, des gastrites ou des œsophagites par reflux, p. ex. antiacides, antisécrétoires, protecteurs de la muqueuse
23.
RECOMBINANT PROTEINS, COMPOSITIONS AND METHODS OF STABILIZATION THEREOF
The present invention relates to recombinant proteins, compositions and methods of stabilization thereof. The invention specifically relates to the stable recombinant protein of SEQ ID NO: 1 and composition comprising recombinant protein of SEQ ID NO: 1. The invention further relates to method of preparing, storing and stabilizing recombinant protein of SEQ ID NO: 1 and its composition for longer shelf life.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
24.
RECOMBINANT PROTEINS, COMPOSITIONS AND METHODS OF STABILIZATION THEREOF
The present invention relates to recombinant proteins, compositions and methods of stabilization thereof. The invention specifically relates to the stable recombinant protein of SEQ ID NO: 1 and composition comprising recombinant protein of SEQ ID NO: 1. The invention further relates to method of preparing, storing and stabilizing recombinant protein of SEQ ID NO: 1 and its composition for longer shelf life.
A61J 1/05 - Récipients spécialement adaptés à des fins médicales ou pharmaceutiques pour recueillir, stocker ou administrer du sang, du plasma ou des liquides à usage médical
A61K 47/18 - AminesAmidesUréesComposés d’ammonium quaternaireAcides aminésOligopeptides ayant jusqu’à cinq acides aminés
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61K 38/16 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés
A61K 9/19 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p. ex. poudres lyophilisées
The present invention relates to stable formulations of recombinant proteins. The invention specifically relates to the formulations of recombinant lectins derived from Sclerotium rolfsii lectin. The formulation comprises recombinant lectin derived from Sclerotium rolfsii lectin and a pharmaceutically acceptable excipient. The invention also relates to the stable liquid and/or lyophilized formulations comprising recombinant lectins derived from Sclerotium rolfsii lectin.
A61K 47/18 - AminesAmidesUréesComposés d’ammonium quaternaireAcides aminésOligopeptides ayant jusqu’à cinq acides aminés
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61K 47/22 - Composés hétérocycliques, p. ex. acide ascorbique, tocophérol ou pyrrolidones
A61K 9/19 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p. ex. poudres lyophilisées
26.
COMBINATION OF CHEMOTHERAPY WITH RECOMBINANT S. ROLFSII LECTIN
The present invention relates to the combination chemotherapy with recombinant lectin protein. The invention specifically relates to the cytotoxic effect of recombinant lectin protein having amino acid sequence of SEQ ID NO: 1 in combination with other therapeutic agents, wherein the other therapeutic agents are anti-cancer agents. The combinations are highly synergistic and efficacious against several cancers.
A61K 31/435 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
The present disclosure provides an extended release composition of tofacitinib for oral administration, and methods of making the composition. The extended release composition employs a matrix drug core comprising tofacitinib or a pharmaceutically acceptable salt thereof and at least one release controlling polymer. The matrix drug core is surrounded by a soluble functional coating comprising at least one coating polymer and at least one pharmaceutically acceptable excipient.
The present invention relates to the lectin protein for the treatment and prevention of neurodegenerative diseases. The invention further relates to the recombinant lectin protein is derived from Sclerotium rolfsii lectin having sequence 60% homologous to SEQ ID NO: 4 for the treatment and prevention of Neurodegenerative diseases. The invention specifically relates to: lectin protein and its variants is derived from Sclerotium rolfsii lectin, having sequence 60% homologous to SEQ ID NO: 4 for the treatment of prevention of Parkinson's disease, Alzheimer's disease, Dementia and symptoms of dementia.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
A61P 25/00 - Médicaments pour le traitement des troubles du système nerveux
29.
LECTIN PROTEIN FOR TREATMENT AND PREVENTION OF NEURODEGENERATIVE DISEASES
Sclerotium rolfsiiSclerotium rolfsiiSclerotium rolfsii lectin, having sequence 60% homologous to SEQ ID NO: 4 for the treatment of prevention of Parkinson's disease, Alzheimer's disease, Dementia and symptoms of dementia.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
A61P 25/00 - Médicaments pour le traitement des troubles du système nerveux
30.
Novel Process for the Preparation of Filgotinib and Intermediates Thereof
The present invention relates to a novel process for the preparation of filgotinib or a pharmaceutically acceptable salt and intermediates thereof which avoid Suzuki coupling reaction.
C07D 213/75 - Radicaux amino ou imino, acylés par un acide carboxylique, par l'acide carbonique ou par leurs analogues du soufre ou de l'azote, p. ex. des carbamates
The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; wherein Q is a group of formula Q1 or Q2; wavy bond represents the points of attachment; wherein R1 is ?NRaRb; R2 is hydrogen or a C1-C10 alkyl group; Ra and Rb independently represent hydrogen or a C1-C10 alkyl group, and use of these compounds as kinase inhibitors and compositions comprising the compounds of the present invention.
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
11 is –NRaRb211010 alkyl group; Raand Rb11010 alkyl group, and use of these compounds as kinase inhibitors and compositions comprising the compounds of the present invention.
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
A61P 37/00 - Médicaments pour le traitement des troubles immunologiques ou allergiques
The present invention relates to a lectin for use in the treatment, reduction in progression and curing of inflammation in a subject in need thereof. Pharmaceutical compositions comprising said lectin are also described. The lectin may comprise an amino acid sequence having sequence of SEQ ID NO: 1 or at least 60% homology to SEQ ID NO: 1.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
A61P 19/02 - Médicaments pour le traitement des troubles du squelette des troubles articulaires, p. ex. arthrites, arthroses
34.
Process for the preparation of Rivaroxaban involving novel intermediate
The present invention relates to the novel key intermediate, 4-{4-[(SS)-(Aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]-phenyl}-morpholin-3-one perchlorate, m the synthesis of rivaroxaban. The invention further relates to the crystalline form of novel intermediate, the process to prepare the novel intermediate and method of preparing rivaroxaban using this novel intermediate. The invention provides an improved and efficient process for preparation of Rivaroxaban.
C07D 413/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
C07D 413/10 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant des cycles aromatiques
A61K 31/5377 - 1,4-Oxazines, p. ex. morpholine non condensées et contenant d'autres hétérocycles, p. ex. timolol
A recombinant lectin for use in a method of treatment of cancer by inhibiting angiogenesis in a subject. The treatment comprises administration of a therapeutically effective amount of the recombinant lectin.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
A recombinant lectin for use in a method of treatment of cancer by inhibiting angiogenesis in a subject. The treatment comprises administration of a therapeutically effective amount of the recombinant lectin.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
The present invention relates to the process to prepare recombinant lectin having amino acid sequence of SEQ ID NO:1, wherein the process comprises fed-batch fermentation of a clone in a host cell at specific feeding rate with carbon to Nitrogen ratio of 3:1 to 6:1. The invention also relates to the process of purification of recombinant lectin having amino acid sequence of SEQ ID NO: 1.
C12P 21/02 - Préparation de peptides ou de protéines comportant une séquence connue de plusieurs amino-acides, p. ex. glutathion
B01D 15/32 - Chromatographie en phase liée, p. ex. avec une phase normale liée, une phase inverse ou une interaction hydrophobe
B01D 15/36 - Adsorption sélective, p. ex. chromatographie caractérisée par le mécanisme de séparation impliquant une interaction ionique, p. ex. échange d'ions, paire d'ions, suppression d'ions ou exclusion d'ions
C07K 1/20 - Chromatographie de partage, de phase inverse ou d'interaction hydrophobe
C07K 1/34 - ExtractionSéparationPurification par filtration, ultrafiltration ou osmose inverse
C07K 1/36 - ExtractionSéparationPurification par une combinaison de plusieurs procédés de types différents
C07K 14/42 - Lectines, p. ex. concanavaline, phytohémagglutinine
C07K 14/47 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains provenant de vertébrés provenant de mammifères
A modified lectin protein is provided having at least one amino acid modification in an amino acid sequence of SEQ ID NO. 1 orin an amino acid sequence having at least 60% homology thereto. The amino acid modification is selected from one of more of the following: at least one amino acid modification in a carbohydrate binding site; at least one amino acid modification in the N-terminus; at least one amino acid modification at position 76; or at least one amino acid modification at position 44 or 89. The modified lectin protein does not consist of the amino acid sequence of any of SEQ ID NOs: 2 to 4.
The present invention relates to stable formulations of recombinant proteins. The invention specifically relates to the formulations of recombinant lectins derived from Sclerotium rolfsii lectin. The formulation comprises recombinant lectin derived from Sclerotium rolfsii lectin and a pharmaceutically acceptable excipient. The invention also relates to the stable liquid and/or lyophilized formulations comprising recombinant lectins derived from Sclerotium rolfsii lectin.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
A61K 47/18 - AminesAmidesUréesComposés d’ammonium quaternaireAcides aminésOligopeptides ayant jusqu’à cinq acides aminés
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61K 47/18 - AminesAmidesUréesComposés d’ammonium quaternaireAcides aminésOligopeptides ayant jusqu’à cinq acides aminés
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
41.
NOVEL PROCESS FOR THE PREPARATION OF FILGOTINIB AND INTERMEDIATES THEREOF
The present invention relates to a novel process for the preparation of filgotinib or a pharmaceutically acceptable salt and intermediates thereof which avoid Suzuki coupling reaction. (I)
The present disclosure provides an extended release composition of tofacitinib for oral administration, and methods of making the composition. The extended release composition employs a matrix drug core comprising tofacitinib or a pharmaceutically acceptable salt thereof and at least one release controlling polymer. The matrix drug core is surrounded by a soluble functional coating comprising at least one coating polymer and at least one pharmaceutically acceptable excipient.
A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
The present invention relates to a disintegrant free pharmaceutical composition comprising apremilast or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipients. Particularly the present invention relates to disintegrant free immediate release dosage form comprising apremilast or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipients. It further relates to process of preparing such composition and its use in psoriatic arthritis and psoriasis.
10 equal to or less than 5 μm and one or more and binders in an amount of 0.9% w/w or less, relative to the total weight of composition, where the composition is not free of binder and that the total amount of binder does not exceed 0.9% w/w relative to the total weight of the composition.
The invention relates to vortioxetine hydrobromide having particle size distribution of D98 100-200μ, D50 35-90μ and D5 7-30μ as well as to a stable, reproducible and bioequivalent pharmaceutical composition comprising vortioxetine hydrobromide having particle size distribution of D98 100-200μ, D50 35-90μ and D5 7-30μ and one or more pharmaceutically acceptable excipient. It is produced by wet granulation techniques.
An alternative and improved process for the preparation of Apremilast (Formula I) and Apremilast form B or a pharmaceutically acceptable salt thereof is provided. The novel process includes hydrogenation in acetone, Cyclization and acetylation followed by condensation in methyl isobutyl ketone (MIBK) and acetic acid mixture in specific volume ratios.
The present invention relates to the combination chemotherapy with recombinant lectin protein. The invention specifically relates to the cytotoxic effect of recombinant lectin protein having amino acid sequence of SEQ ID NO: 1 in combination with other therapeutic agents, wherein the other therapeutic agents are anti-cancer agents. The combinations are highly synergistic and efficacious against several cancers.
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
A61K 31/401 - ProlineSes dérivés, p. ex. captopril
A61K 31/513 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime ayant des groupes oxo liés directement à l'hétérocycle, p. ex. cytosine
The present invention relates to the combination chemotherapy with recombinant lectin protein. The invention specifically relates to the cytotoxic effect of recombinant lectin protein having amino acid sequence of SEQ ID NO: 1 in combination with other therapeutic agents, wherein the other therapeutic agents are anti-cancer agents. The combinations are highly synergistic and efficacious against several cancers.
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
A61K 31/401 - ProlineSes dérivés, p. ex. captopril
A61K 31/513 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime ayant des groupes oxo liés directement à l'hétérocycle, p. ex. cytosine
The present invention relates to the process to prepare recombinant lectin having amino acid sequence of SEQ ID NO:l, wherein the process comprises fed-batch fermentation of a clone in a host cell at specific feeding rate with carbon to Nitrogen ratio of 3:1 to 6:1. The invention also relates to the process of purification of recombinant lectin having amino acid sequence of SEQ ID NO: 1.
C07K 14/42 - Lectines, p. ex. concanavaline, phytohémagglutinine
C07K 14/47 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains provenant de vertébrés provenant de mammifères
C12P 21/02 - Préparation de peptides ou de protéines comportant une séquence connue de plusieurs amino-acides, p. ex. glutathion
The present invention relates to a lectin for use in the treatment, reduction in progression and curing of inflammation in a subject in need thereof. Pharmaceutical compositions comprising said lectin are also described. The lectin may comprise an amino acid sequence having sequence of SEQ ID NO: 1 or at least 60% homology to SEQ ID NO: 1.
A61K 38/16 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés
A61P 19/02 - Médicaments pour le traitement des troubles du squelette des troubles articulaires, p. ex. arthrites, arthroses
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
C07K 14/47 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains provenant de vertébrés provenant de mammifères
51.
AN IMPROVED PROCESS FOR THE PREPARATION OF RECOMBINANT LECTIN PROTEIN
The present invention relates to the process to prepare recombinant lectin having amino acid sequence of SEQ ID NO:l, wherein the process comprises fed-batch fermentation of a clone in a host cell at specific feeding rate with carbon to Nitrogen ratio of 3:1 to 6:1. The invention also relates to the process of purification of recombinant lectin having amino acid sequence of SEQ ID NO: 1.
C07K 14/42 - Lectines, p. ex. concanavaline, phytohémagglutinine
C07K 14/47 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains provenant de vertébrés provenant de mammifères
C12P 21/02 - Préparation de peptides ou de protéines comportant une séquence connue de plusieurs amino-acides, p. ex. glutathion
The present invention relates to a lectin for use in the treatment, reduction in progression and curing of inflammation in a subject in need thereof. Pharmaceutical compositions comprising said lectin are also described. The lectin may comprise an amino acid sequence having sequence of SEQ ID NO: 1 or at least 60% homology to SEQ ID NO: 1.
A61K 38/16 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés
C07K 14/47 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains provenant de vertébrés provenant de mammifères
A61P 19/02 - Médicaments pour le traitement des troubles du squelette des troubles articulaires, p. ex. arthrites, arthroses
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
A modified lectin protein is provided having at least one amino acid modification in an amino acid sequence of SEQ ID NO. 1 orin an amino acid sequence having at least 60% homologythereto. The amino acid modification is selected from one of more of the following: at least one amino acid modification in a carbohydrate binding site; at least one amino acid modification in the N-terminus;at least one amino acid modification at position 76; or at least one amino acid modification at position 44 or 89. The modified lectin protein does not consist of the amino acid sequence of any of SEQ ID NOs: 2 to 4.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
C07K 14/705 - RécepteursAntigènes de surface cellulaireDéterminants de surface cellulaire
A modified lectin protein is provided having at least one amino acid modification in an amino acid sequence of SEQ ID NO. 1 orin an amino acid sequence having at least 60% homologythereto. The amino acid modification is selected from one of more of the following: at least one amino acid modification in a carbohydrate binding site; at least one amino acid modification in the N-terminus;at least one amino acid modification at position 76; or at least one amino acid modification at position 44 or 89. The modified lectin protein does not consist of the amino acid sequence of any of SEQ ID NOs: 2 to 4.
C07K 14/705 - RécepteursAntigènes de surface cellulaireDéterminants de surface cellulaire
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
55.
LEADER SEQUENCE FOR HIGHER EXPRESSION OF RECOMBINANT PROTEINS
The present invention relates to the leader sequence for higher expression of recombinant proteins. The invention further relates to the process for preparation of insulin and insulin analogues using leader sequence. The leader peptides significantly increase the expression of pre-proinsulin. The present invention also relates to the protein sequences prepared by fusion of fragments with the leader sequences of the present invention. The invention is demonstrated by preparing and Insulin and its analogues using said leader sequences.
The present invention relates to the novel key intermediate, 4-{4-[(5S)-(Aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]-phenyl}-morpholin-3-one perchlorate, in the synthesis of rivaroxaban. The invention further relates to the crystalline form of novel intermediate, the process to prepare the novel intermediate and method of preparing rivaroxaban using this novel intermediate. The invention provides an improved and efficient process for preparation of Rivaroxaban.
C07D 413/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
C07D 413/10 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant des cycles aromatiques
57.
Process for preparation and purification of vortioxetine hydrobromide
The present invention is related to an improved process for the preparation and purification of crystalline Vortioxetine hydrobromide of Formula-I. The process according to present invention is operationally simple and suitable for industrial application which will avoid hazardous chemicals and eliminate column chromatography to get ICH quality of pharmaceutically acceptable active pharmaceutical ingredient having snow white appearance.
C07D 241/04 - Composés hétérocycliques contenant des cycles diazine-1,4 ou diazine-1,4 hydrogéné non condensés avec d'autres cycles ne comportant pas de liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques
A61K 31/496 - Pipérazines non condensées contenant d'autres hétérocycles, p. ex. rifampine, thiothixène ou sparfloxacine
90 particle size of more than 100 microns, preferably between 300 and 1000 microns, and more preferably between 350 and 800 microns, and further comprising one or more pharmaceutically acceptable excipients. The present disclosure further provides a process for preparation of a pharmaceutical composition comprising apixaban by wet granulation.
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
A61K 31/4545 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un cycle à six chaînons avec l'azote comme hétéro-atome du cycle, p. ex. pipampérone, anabasine
The present invention relates to an enzymatic process for the preparation of (R)- Sitagliptin. The process involves reductive amination of Pro-Sitagliptin to (R)- Sitagliptin using novel transaminase enzymes. The invention also relates to the Nucleotide sequences encoding novel transaminase enzymes and process to prepare transaminase enzymes.
The present invention relates to nucleotide sequence of SEQ ID 1 and SEQ ID 2 encoding recombinant 3-Quinuclidinone reductase and Glucose Dehydrogenase respectively. The invention further relates to the clone comprising the said nucleotide sequences and process to prepare 3-Quinuclidinone reductase and Glucose Dehydrogenase having amino acid sequence of SEQ ID 3 and SEQ ID 4, respectively.
C07D 413/04 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
The present invention relates to a disintegrant free pharmaceutical composition comprising apremilast or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipients. Particularly the present invention relates to disintegrant free immediate release dosage form comprising apremilast or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipients. It further relates to process of preparing such composition and its use in psoriatic arthritis and psoriasis.
The present invention relates to a disintegrant free pharmaceutical composition comprising apremilast or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipients. Particularly the present invention relates to disintegrant free immediate release dosage form comprising apremilast or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipients. It further relates to process of preparing such composition and its use in psoriatic arthritis and psoriasis.
Rhodotorula rubraRhodotorula rubra. The invention also relates to enzymatically produced (R)-3-quinuclidinol wherein the substrate loading capacity of the enzyme is not less than 100g/L.
The invention relates to a pharmaceutical composition comprising cinacalcet or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipient. The invention also relates to the pharmaceutical composition comprising cinacalcet or pharmaceutically acceptable salts thereof having a particle size distribution D 90 equal to or less than 20 µm, D 50 equal to or less than 10 µm, and D equal to or less than 5 µm and one or more and binders in an amount of 0.9% w/w or less, relative to the total weight of composition, wherein the composition is not free of binder and that the total amount of binder does not exceed 0.9%w/w relative to the total weight of the composition.
An alternative and improved process for the preparation of Apremilast (Formula I) and Apremilast form B or a pharmaceutically acceptable salt thereof is provided. The novel process includes hydrogenation in acetone, Cyclization and acetylation followed by condensation in methyl isobutyl ketone (MIBK) and acetic acid mixture in specific volume ratios.
C07D 209/48 - Iso-indolesIso-indoles hydrogénés avec des atomes d'oxygène en positions 1 et 3, p. ex. phtalimide
C07C 317/28 - SulfonesSulfoxydes ayant des groupes sulfone ou sulfoxyde et des atomes d'azote, ne faisant pas partie de groupes nitro ou nitroso, liés au même squelette carboné avec des groupes sulfone ou sulfoxyde liés à des atomes de carbone acycliques du squelette carboné
67.
AN IMPROVED PROCESS FOR PREPARATION AND PURIFICATION OF VORTIOXETINE HYDROBROMIDE
The present invention is related to an improved process for the preparation and purification of crystalline polymorph of Vortioxetine hydrobromide of Formula-I and Vortioxetine hydrochloride of Formula-Ia. The process according to present invention is operationally simple and suitable for industrial application which will avoid hazardous chemicals and eliminate column chromatography to get ICH quality of pharmaceutically acceptable active pharmaceutical ingredient having snow white appearance.
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
C07D 241/04 - Composés hétérocycliques contenant des cycles diazine-1,4 ou diazine-1,4 hydrogéné non condensés avec d'autres cycles ne comportant pas de liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques
C07D 295/096 - Composés hétérocycliques contenant des cycles polyméthylène imine d'au moins cinq chaînons, des cycles aza-3 bicyclo [3.2.2] nonane, piperazine, morpholine ou thiomorpholine, ne comportant que des atomes d'hydrogène liés directement aux atomes de carbone du cycle avec des radicaux hydrocarbonés substitués liés aux atomes d'azote du cycle substitués par des atomes d'oxygène ou de soufre liés par des liaisons simples avec les atomes d'azote du cycle et les atomes d'oxygène ou de soufre séparés par des carbocycles ou par des chaînes carbonées interrompues par des carbocycles
The present disclosure relates to a stable, reproducible and bioequivalent apixaban compositions, wherein the composition comprising apixaban having a D90 particle size of more than 100 microns, preferably between 300 and 1000 microns, and more preferably between 350 and 800 microns, and further comprising one or more pharmaceutically acceptable excipients. The present disclosure further provides a process for preparation of a pharmaceutical composition comprising apixaban by wet granulation.
A61K 31/4545 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un cycle à six chaînons avec l'azote comme hétéro-atome du cycle, p. ex. pipampérone, anabasine
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
The invention relates to vortioxetine hydrobromide having particle size distribution of D98 100-200μ, D50 35-90μ and D5 7-30μ as well as to a stable, reproducible and bioequivalent pharmaceutical composition comprising vortioxetine hydrobromide having particle size distribution of D98 100-200μ, D50 35-90μ and D5 7-30μ and one or more pharmaceutically acceptable excipient. It is produced by wet granulation techniques.
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
A61K 31/4418 - Pyridines non condenséesLeurs dérivés hydrogénés ayant un carbocycle lié directement à l'hétérocycle, p. ex. cyproheptadine
C07D 211/20 - Composés hétérocycliques contenant des cycles pyridiques hydrogénés, non condensés avec d'autres cycles avec uniquement des atomes d'hydrogène et de carbone liés directement à l'atome d'azote du cycle ne comportant pas de liaison double entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec des radicaux hydrocarbonés ou des radicaux hydrocarbonés substitués, liés directement aux atomes de carbone du cycle avec des radicaux hydrocarbonés substitués liés aux atomes de carbone du cycle avec des radicaux hydrocarbonés, substitués par des atomes d'oxygène ou de soufre liés par des liaisons simples
C07D 241/04 - Composés hétérocycliques contenant des cycles diazine-1,4 ou diazine-1,4 hydrogéné non condensés avec d'autres cycles ne comportant pas de liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques
C07D 295/08 - Composés hétérocycliques contenant des cycles polyméthylène imine d'au moins cinq chaînons, des cycles aza-3 bicyclo [3.2.2] nonane, piperazine, morpholine ou thiomorpholine, ne comportant que des atomes d'hydrogène liés directement aux atomes de carbone du cycle avec des radicaux hydrocarbonés substitués liés aux atomes d'azote du cycle substitués par des atomes d'oxygène ou de soufre liés par des liaisons simples
C07D 295/033 - Composés hétérocycliques contenant des cycles polyméthylène imine d'au moins cinq chaînons, des cycles aza-3 bicyclo [3.2.2] nonane, piperazine, morpholine ou thiomorpholine, ne comportant que des atomes d'hydrogène liés directement aux atomes de carbone du cycle contenant uniquement des atomes d'hydrogène et de carbone en plus des hétéro-éléments du cycle ne contenant qu'un hétérocycle avec les atomes d'azote du cycle liés directement à des carbocycles
C07D 295/096 - Composés hétérocycliques contenant des cycles polyméthylène imine d'au moins cinq chaînons, des cycles aza-3 bicyclo [3.2.2] nonane, piperazine, morpholine ou thiomorpholine, ne comportant que des atomes d'hydrogène liés directement aux atomes de carbone du cycle avec des radicaux hydrocarbonés substitués liés aux atomes d'azote du cycle substitués par des atomes d'oxygène ou de soufre liés par des liaisons simples avec les atomes d'azote du cycle et les atomes d'oxygène ou de soufre séparés par des carbocycles ou par des chaînes carbonées interrompues par des carbocycles
70.
AN IMPROVED PROCESS FOR THE PREPARATION OF RIVAROXABAN INVOLVING NOVEL INTERMEDIATE
The present invention relates to the novel key intermediate, 4-{4-[(5S)-(Aminomethyl)-2- oxo-l,3-oxazolidin-3-yl]-phenyl}-morpholin-3-one perchlorate, in the synthesis of rivaroxaban. The invention further relates to the crystalline form of novel intermediate, the process to prepare the novel intermediate and method of preparing rivaroxaban using this novel intermediate. The invention provides an improved and efficient process for preparation of Rivaroxaban.
C07D 413/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
71.
Process for the preparation of (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine
The present disclosure is related to an improved and efficient process for preparation of (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine which comprises:
(a) N-acylation of 3-Amino-4-methyl pyridine; (b) Quarternization of 3-Acetylamino-4-methyl pyridine using benzyl halide; (c) Partial reduction of quarternized 3-Acetylamino-4-methyl pyridine by Sodium borohydride in Methanol or water; (d) Hydrolysis of partially reduced product to 1-Benzyl-4-methylpiperidin-3-one in presence of acid; (e) Reductive amination of 1-Benzyl-4-methylpiperidin-3-one using Methanolic methylamine in presence of Titanium(IV) isopropoxide in Methanol; (f) Resolution of 1-Benzyl-4-methylpiperidin-3-yl)-methylamine using Ditoluoyl (L) tartaric acid to get (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine. The disclosure is also related to novel intermediates:
wherein R, R′ and X are as described in the specification.
C07D 211/72 - Composés hétérocycliques contenant des cycles pyridiques hydrogénés, non condensés avec d'autres cycles avec uniquement des atomes d'hydrogène et de carbone liés directement à l'atome d'azote du cycle comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des hétéro-atomes ou des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, liés directement aux atomes de carbone du cycle
C07D 213/75 - Radicaux amino ou imino, acylés par un acide carboxylique, par l'acide carbonique ou par leurs analogues du soufre ou de l'azote, p. ex. des carbamates
The present invention refers to novel process for the preparation of Apixaban. Further, the invention also related to a process for the preparation of intermediate of Apixaban from very basic and cheap row material i.e. Aniline which is widely commercially available. The present invention provides process for preparation of Apixaban using a different sequence of synthetic steps and does not involve use of Ullmann reaction.
The present invention relates to an improved process for the synthesis of (R)- Lacosamide in which free base of O-methyl-N-benzyl-D-Serinamide is not isolated before acylation. The process avoids the use of column chromatography and chiral resolution for the preparation of different stages of Lacosamide.
The present invention refers to novel process for the preparation of Apixaban. Further, the invention also related to a process for the preparation of intermediate of Apixaban from very basic and cheap row material i.e. Aniline which is widely commercially available. The present invention provides process for preparation of Apixaban using a different sequence of synthetic steps and does not involve use of Ullmann reaction.
The present invention relates to resinates of pharmaceutically acceptable salts of Tofacitinib such as Tofacitinib Citrate, fast disintegrating and or quick release pharmaceutical compositions comprising the said resinates and process for the preparation of resinates and compositions. The resin used to prepare the resinate is selected from copolymers of methacrylic acid and divinylbenzene, cross linked polymer of methacrylic acid and divinylbenzene, sulphonated copolymers of styrene and divinylbenzene. Ion exchange resin is contacted with the solution of Tofacitinib citrate under controlled pH in order to form the resinate. The resinate has versatile use in making of pharmaceutical preparations. Few such pharmaceutical preparations are Tablets, capsules, dry syrups, suspensions, lozenges, films.
The present invention relates to resinates of Tofacitinib. The invention also relates to taste masked, stable and readily dispersible resinates of Tofacitinib, rapidly disintegrating and or quick release taste masked pharmaceutical compositions comprising the said resinates and process for the preparation of resinates and compositions. In order to form the resinate, the resin is selected from copolymers of methacrylic acid and divinylbenzene, cross linked polymer of methacrylic acid and divinylbenzene, sulphonated copolymers of styrene and divinylbenzene. In order to form the resinate, Ion exchange resin is contacted with the solution of Tofacitinib prepared in nonaromatic solvent. The resinate is useful to formulate different pharmaceutical dosage forms such as Tablets, Capsule, drysyrups.
The present invention relates to a process for the preparation of Azilsartan Medoxomil Potassium. The invention further relates to novel highly crystalline polymorph of Azilsartan Medoxomil Potassium and composition comprising it. The invention provides thermostable highly crystalline polymorph of Azilsartan Medoxomil Potassium and process to produce a composition comprising the novel highly crystalline polymorph of Azilsartan Medoxomil Potassium.
C07D 413/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
The present invention relates to Orally Disintegrating Tablets (ODT) of Tofacitinib and its pharmaceutically acceptable salts and the process to produce the ODT. The invention further relates to ODTs comprising Tofacitinib and its pharmaceutically acceptable salts, at least one sweetening agent, at least one disintegrant and optionally other excipients. The weight of the Orally Disintegrating tablets is 200 mg or less. The invention further relates to Orally Disintegrating Tablets of Tofacitinib Citrate.
The present invention refers to novel process for the preparation of Apixaban. Further, the invention also related to a process for the preparation of intermediate of Apixaban from very basic and cheap row material i.e. Aniline which is widely commercially available. The present invention provides process for preparation of Apixaban using a different sequence of synthetic steps and does not involve use of Ullmann reaction.
The present invention relates to a process for the preparation of Azilsartan Medoxomil Potassium. The invention further relates to novel highly crystalline polymorph of Azilsartan Medoxomil Potassium and composition comprising it. The invention provides thermostable highly crystalline polymorph of Azilsartan Medoxomil Potassium and process to produce a composition comprising the novel highly crystalline polymorph of Azilsartan Medoxomil Potassium.
C07D 413/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
A61K 31/00 - Préparations médicinales contenant des ingrédients actifs organiques
A61K 31/395 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines
A61K 31/41 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec plusieurs hétéro-atomes cycliques, l'un au moins étant l'azote, p. ex. tétrazole
C07D 413/00 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle
The present invention relates to novel processes for the preparation of Ranolazine (I) and its acid addition salts and the novel process for the preparation of compound of formula (7).
C07D 295/15 - Composés hétérocycliques contenant des cycles polyméthylène imine d'au moins cinq chaînons, des cycles aza-3 bicyclo [3.2.2] nonane, piperazine, morpholine ou thiomorpholine, ne comportant que des atomes d'hydrogène liés directement aux atomes de carbone du cycle avec des radicaux hydrocarbonés substitués liés aux atomes d'azote du cycle substitués par des atomes de carbone comportant trois liaisons à des hétéro-atomes avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile avec les atomes d'azote du cycle et les atomes de carbone comportant trois liaisons à des hétéro-atomes liés à la même chaîne carbonée, qui n'est pas interrompue par des carbocycles à une chaîne acyclique saturée
C07D 303/23 - Éthers oxiranylméthyliques de composés comportant un groupe hydroxy lié à un cycle aromatique à six chaînons, le radical oxiranylméthylique ne comportant pas d'autre substituant, c.-à-d.
82.
AN IMPROVED PROCESS FOR THE PREPARATION OF PHARMACOPOEIAL GRADE INTERFERON ALPHA 2B
The present invention relates to a simple and scalable process for the production of pharmacopoeial grade Interferon alpha 2b by fed-batch fermentation followed by purification using chromatography techniques. The invention also relates to the recombinant expression of interferon alpha 2b in soluble form by fermentation to obtain high yields. The process involves clarification and chromatographic steps for the purification of Interferon alpha 2b.
(a) N-acylation of 3-Amino-4-methyl pyridine; (b) Quarternization of 3-Acetylamino-4-methyl pyridine using benzyl halide; (c) Partial reduction of quarternized 3-Acetylamino-4-methyl pyridine by Sodium borohydride in Methanol or water; (d) Hydrolysis of partially reduced product to 1-Benzyl-4-methylpiperidin-3-one in presence of acid; (e) Reductive amination of 1-Benzyl-4-methylpiperidin-3-one using Methanolic methylamine in presence of Titanium(IV) isopropoxide in Methanol; (f) Resolution of 1-Benzyl-4-methylpiperidin-3-yl)-methylamine using Ditoluoyl (L) tartaric acid to get (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine. The invention is also related to novel intermediates:
wherein R, R′ and X are as described in the specification.
C07D 213/75 - Radicaux amino ou imino, acylés par un acide carboxylique, par l'acide carbonique ou par leurs analogues du soufre ou de l'azote, p. ex. des carbamates
C07D 213/74 - Radicaux amino ou imino substitués par des radicaux hydrocarbonés ou par des radicaux hydrocarbonés substitués
C07D 211/72 - Composés hétérocycliques contenant des cycles pyridiques hydrogénés, non condensés avec d'autres cycles avec uniquement des atomes d'hydrogène et de carbone liés directement à l'atome d'azote du cycle comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des hétéro-atomes ou des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, liés directement aux atomes de carbone du cycle
84.
AN IMPROVED PROCESS FOR THE PREPARATION OF APIXABAN AND INTERMEDIATES THEREOF
The present invention refers to novel process for the preparation of Apixaban. Further, the invention also related to a process for the preparation of intermediate of Apixaban from very basic and cheap row material i.e. Aniline which is widely commercially available. The present invention provides process for preparation of Apixaban using a different sequence of synthetic steps and does not involve use of Ullmann reaction.
The present invention is related to an improved and efficient process for preparation of (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine which comprises: (a) N-acylation of 3-Amino-4-methyl pyridine; (b) Quarternization of 3-Acetylamino-4- methyl pyridine using benzyl halide; (c) Partial reduction of quarternized 3-Acetylamino- 4-methyl pyridine by Sodium borohydride in Methanol or water; (d) Hydrolysis of partially reduced product to 1-Benzyl-4-methylpiperidin-3-one in presence of acid; (e) Reductive animation of 1-Benzyl-4-methylpiperidin-3-one using Methanolic methylamine in presence of Titanium(IV) isopropoxide in Methanol; (f) Resolution of 1-Benzyl-4- methylpiperidin-3-yl)-methylamine using Ditoluoyl (L) tartaric acid to get (3R,4R)-(1- benzyl-4-methylpiperidin-3-yl)-methylamine. The invention is also related to novel intermediates.
The present invention provides a method for preparing a recombinant lectin expressed in a host cell such as E.coli or yeast, said method comprising the synthesis of a lectin gene based on amino acid sequence derived from the MALDI MS/MS of the Sclerotium rolfsii lectin (SEQ ID.1), a soil borne phytopathogenic fungus, and its cloning in the host cell.
C07K 14/37 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant de champignons
C07K 14/375 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant de champignons provenant de Basidiomycetes
87.
CANCER CELL BINDING RECOMBINANT LECTINS WITH ANTITUMOR ACTIVITY AND METHOD OF PREPARATION
The present invention discloses genes for new variants in E.coli that are more close to the wild type lectin sequence but still differ in surface charges. This recombinant version (exemplified Rec-2 and Rec-3) are cancer cell binding with anti tumor activity show blood group specificity similar to the native lectin but retains the stability and the solubility properties.
Derivatives of anacardic acid having antimicrobial properties and method for preparing said derivatives. The antimicrobial properties include bacteriostatic and bacteriocidal activity.
C07C 237/28 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle aromatique à six chaînons non condensé du squelette carboné
C07C 65/01 - Composés comportant des groupes carboxyle liés à des atomes de carbone de cycles aromatiques à six chaînons et contenant l'un des groupes OH, O-métal, —CHO, cétone, éther, des groupes , des groupes ou des groupes contenant des groupes hydroxyle ou O-métal
C07C 229/54 - Composés contenant des groupes amino et carboxyle liés au même squelette carboné ayant des groupes amino et carboxyle liés à des atomes de carbone de cycles aromatiques à six chaînons du même squelette carboné avec des groupes amino et carboxyle liés à des atomes de carbone du même cycle aromatique à six chaînons non condensé
A01N 37/18 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés organiques comportant un atome de carbone possédant trois liaisons à des hétéro-atomes, avec au plus deux liaisons à un halogène, p. ex. acides carboxyliques contenant le groupe —CO—N, p. ex. amides ou imides d'acide carboxyliqueLeurs thio-analogues
89.
A NOVEL PROCESS FOR THE PREPARATION OF 2-HALO-4-AMINOQUINAZOLINES
2-Halo-4-aminoquinazolines are produced by a one-step process involving intramolecular cyclization of appropriately substituted formamide derivatives in the presence of phosphorous oxyhalides. Exemplary of the process is the intramolecular cyclization of 3,4-dimethoxy-6-cyanoaniline-1-yl formamide in the presence of phosphorous oxychloride to 2-chloro-4-amino-6,7-dimethoxyquinazoline. These chemical compounds are utilized as intermediates in the preparation of some of the important antihypertensive agents e.g. 2-chloro-4-amino-6,7-dimethoxyquinazolines is used for the synthesis of alfuzosin hydrochloride.
Derivatives of anacardic acid having antimicrobial properties and method for preparing said derivatives. The antimicrobial properties include bacteriostatic and bacteriocidal activity.
A61K 31/496 - Pipérazines non condensées contenant d'autres hétérocycles, p. ex. rifampine, thiothixène ou sparfloxacine
C07D 403/12 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07D 403/00 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe
92.
IMPROVED MANUFACTURING PROCEDURE FOR THE PREPARATION OF POLYMORPHIC FORM II OF CIS-(1S)-N-METHYL-4-(3,4-DICHLOROPHENYL)-1,2,3,4-TETRAHYDRO-1-NAPTHLENEAMINE HYDROCHLORIDE (SERTRALINE HYDROCHLORIDE)
The present invention relates to the improved, scalable and efficient manufacturing procedure for the preparation of the antidepressant Cis-(1S)-N-Methyl-4-(3,4-Dichlorophenyl)-1,2,3,4-tetrahydro-1-napthaleneamine hydro chloride, Sertraline Hydrochloride polymorphic form II. The present invention further relates to the improved and modified procedures for preparing, separating and isolating the key intermediates involved in the preparationof Sertraline Hydrochloride polymorphic form II. The present invention also further relates to the use of novel reagents or a combination thereof and new methodologies to prepare some o'f the key intermediates involved in the preparation of Polymorphic Form II of Sertraline Hydrochloride.
C07C 209/26 - Préparation de composés contenant des groupes amino liés à un squelette carboné par alkylation réductive, avec des composés carbonylés, d'ammoniac, d'amines ou de composés ayant des groupes réductibles en groupes amino par réduction avec de l'hydrogène
C07C 209/28 - Préparation de composés contenant des groupes amino liés à un squelette carboné par alkylation réductive, avec des composés carbonylés, d'ammoniac, d'amines ou de composés ayant des groupes réductibles en groupes amino par réduction avec d'autres agents réducteurs
C07C 211/42 - Composés contenant des groupes amino liés à un squelette carboné ayant des groupes amino liés à des atomes de carbone de cycles autres que des cycles aromatiques à six chaînons d'un squelette carboné non saturé contenant des systèmes cycliques condensés avec des cycles aromatiques à six chaînons faisant partie des systèmes cycliques condensés
93.
AN IMPROVED PROCESS FOR THE MANUFACTURE OF LOSARTAN POTASSIUM
The present invention relates to an improved process for the manufacture of Losartan potassium. The process comprises of condensation of 2-butyl-4-chloro-5-formyl imidazole with 2-cyano-4-bromomethyl biphenyl in a biphasic solvent system under phase transfer catalysis followed by insitu reduction using sodium borohydride. The obtained product is converted to Losartan by treating with sodium azide and an amine salt. Losartan is then converted to its potassium salt by treating it with potassium hydroxide in alcohol.
C07D 403/10 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne carbonée contenant des cycles aromatiques
The present invention relates to a process for the preparation of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2, 3-dihydro-1H-pyrrolizin-5-yl acetic acid, in which the key intermediate, 5-Benzyl-3,3-dimethyl-3,4-dihydro-2H-pyrrole is obtained by the hydrogenation of 2,2-dimethyl-4-oxo-5-phenyl-nitropentane. The invention also relates to the preparation of the intermediates occurring in the above process.
C07C 205/45 - Composés contenant des groupes nitro liés à un squelette carboné le squelette carboné étant substitué de plus par au moins un atome d'oxygène lié par une liaison double, ne faisant pas partie d'un groupe —CHO
C07D 207/20 - Composés hétérocycliques contenant des cycles à cinq chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle avec uniquement des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec uniquement des atomes d'hydrogène, des radicaux hydrocarbonés ou des radicaux hydrocarbonés substitués, liés directement aux atomes de carbone du cycle
C07C 49/213 - Composés non saturés comportant des groupes cétone liés à des atomes de carbone acycliques contenant des cycles aromatiques à six chaînons
C07C 49/203 - Composés non saturés comportant des groupes cétone liés à des atomes de carbone acycliques avec uniquement des liaisons doubles carbone-carbone comme insaturation
95.
A PROCESS FOR THE PREPARATION OF EZETIMIBE VIA A NOVEL INTERMEDIATE
The present invention relates to a process for the preparation of Ezetimibe via a novel intermediate. Trans-3(R)-(3-⏧2-oxo-4(S)-(4-benzyloxyphenyl)-1-(4-fluorophenyl)-azetidinyl]propanoic acid is converted to trans-N-methoxy-N-methyl-3(R)-3-⏧2-oxo-4(S)-(4-benzyloxyphenyl)-1-(4-fluorophenyl)-azetidinyl]propanamide and the resultant intermediate is subjected to Grignard reaction to obtain trans-1-(4-fluorophenyl)-3(R)-⏧3-oxo-3-(4-fluorophenyl)propyl]-4(S)-(4-benzyloxyphenyl)-2-azetidinone. Reduction of trans-1-(4-JGiuorophenyl)-3(R)-⏧3-oxo-3-(4-fluorophenyl) propyl]-4(S)-(4-benzyloxyphenyl)-2-azetidinone, followed by debenzylation provides Ezetimibe. The invention also relates to the preparation of the intermediate occurring in the above process.
C07D 205/08 - Composés hétérocycliques comportant des cycles à quatre chaînons ne contenant qu'un atome d'azote comme unique hétéro-atome du cycle non condensés avec d'autres cycles comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec un atome d'oxygène lié directement en position 2, p. ex. bêta-lactames
96.
A NOVEL PROCESS FOR PREPARATION OF VENLAFAXINE HYDROCHLORIDE AND ITS INTERMEDIATES
A process for the preparation of 1-cyano-⏧(4-methoxyphenyl)methyl] cyclohexanol by reacting cyclohexanone with the carbanion of 4-methoxyphenyl acetonitrile in the presence of polyethylene glycol-400 (PEG-400) or Aliquate-336, as a phase transfer catalyst (PTC). The present invention also relates to an novel process for the preparation of 1-⏧2-amino-1-(4-methoxyphenyl)ethyl]cyclohexanol, using borane-dimethyl sulphide complex (BDMS) or AlCl3-NaBH4, in refluxing tetrahydrofuran. 1-⏧2-Amino-1-(4-methoxyphenyl)ethyl]cyclohexanol thus obtained was subjected to N,N-dimethylation using formic acid-formaldehyde in boiling 1,4-dioxane: water mixture to obtain 1-⏧2-(dimethylamino)-1-(4-methoxyphenyl)ethyl] cyclohexanol in high purity, which was treated with isopropanol saturated with HCl gas to get venlafaxine hydrochloride in high purity and high yield.
C07C 253/30 - Préparation de nitriles d'acides carboxyliques par des réactions n'impliquant pas la formation de groupes cyano
C07C 255/37 - Nitriles d'acides carboxyliques ayant des groupes cyano liés à des atomes de carbone acycliques ayant des groupes cyano liés à des atomes de carbone acycliques d'un squelette carboné contenant au moins un cycle aromatique à six chaînons le squelette carboné étant substitué de plus par des groupes hydroxy éthérifiés
C07C 209/28 - Préparation de composés contenant des groupes amino liés à un squelette carboné par alkylation réductive, avec des composés carbonylés, d'ammoniac, d'amines ou de composés ayant des groupes réductibles en groupes amino par réduction avec d'autres agents réducteurs
C07C 211/27 - Composés contenant des groupes amino liés à un squelette carboné ayant des groupes amino liés à des atomes de carbone acycliques d'un squelette carboné non saturé contenant au moins un cycle aromatique à six chaînons ayant des groupes amino reliés au cycle aromatique à six chaînons par l'intermédiaire de chaînes carbonées saturées
97.
A NOVEL PROCESS FOR PREPARATION OF ARIPIPRAZOLE AND ITS INTERMEDIATES
A process for the preparation of 7-hydroxy-3,4-dihydro carbostyril (II) by intramolecular Fridel-Craft alkylation of N-(3-methoxyphenyl)-3-chloropropionamide (I) in which an equivalent of N-(3-methoxyphenyl)-3-chloropropionamide (I) is contacted with a Lewis acid (e.g. aluminium chloride) in dimethyl acetamide (DMA), at an elevated temperature of from about 120°C to about 160°C, is provided. The process produces 7-hydroxy-3,4- dihydro carbostyril (II) in high yield and a high state of purity such that it may be used in subsequent .reaction towards the preparation of aripiprazole (IV). Thus 7-hydroxy-3,4- dihydro carbostyril (II) was treated with l-bromo-4-chlorobutane under phase transfer catalyst (PTC) conditions using solvents like acetone or n-butanol at temperature ranging 25°C to 45°C to afford 7-(4-chlorobutoxy)-3,4-dihydro carbostyril (III). The PTC conditions described in this patent afford 7-(4-chlorobutoxy)-3,4-dihydro carbostyril (III) in high purity and high yield with the corresponding dimmer formation is considerably low as compared with the other literature methods of preparing 7-(4-chlorobutoxy)-3,4- dihydro carbostyril (III). Compound (III) was treated with l-(2,3-dichlorophenyl)piperazine, at temperature ranging from 50°C to 100°C, and sodium iodide, potassium carbonate, dimethyl formamide (DMF) as a solvent to afford aripiprazole in high purity and high yield.
C07D 401/12 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
98.
AN IMPROVED PROCESS FOR PREPARATION OF LEFLUNOMIDE
This invention describes a process for the preparation of N-(4-trifluoromethyl)-5-methylisoxazole-4-carboxamide commonly known as leflunomide comprising : (a) reacting ethylaceto acetate, triethylorthoformate, and acetic anhydride with simultaneous distillation to form ethyl ethoxymethyleneacetoacetic ester; (b) reacting the ethyl ethoxymethyleneacetoacetic ester with aqueous hydroxylamine without using any external base and without any distillation to form ethyl-5-methylisoxazole-4-carboxylate; (c) reacting the ethyl-5-methylisoxazole-4-carboxylate with strong acid to form -5-methylisoxazole-4-carboxylic acid; (d) 5-methylisoxazole-4-carboxylic acid is reacted with thionyl chloride in presence of N, N-Dimethylformamide and equimolar of 4-trifluoromethylaniline without any external base to obtain highly pure Leflunomide.
The present invention provides a novel one-pot process for preparation of Pantoprazole sodium sesquihydrate Form-I in the pure form without isolating the pantoprazole base.
C07D 401/12 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
100.
A NOVEL PROCESS FOR THE SYNTHESIS OF LAMOTRIGINE AND ITS INTERMEDIATE
This invention discloses a process for the preparation of 3,5-Diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine of a formula (I), commonly known as Lamotrigine which comprises the step of reacting aminoguanidine bicarbonarte and 2,3- dichlorobenzocynide with a reagent prepared by dissolving phosphorus pentoxide and methane sulfonic acid, to produce a novel intermediate 2-(2,3-dichlorophenyl)-2-(aminoguanidine)-acetonitrile monomesylate which is further cyclized to lamotrigine without basification.
brevets
