The present invention provides to deuterated dydrogesterone of formulae (I), (II), (III), (IV) and (V). The invention further provides commercially viable process for preparation of deuterated Dydrogesterone. The invention specifically provides deuterated dydrogesterone with increased half-life period with therapeutic advantages.
C07J 7/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by a chain of two carbon atoms
A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
A61P 15/00 - Drugs for genital or sexual disordersContraceptives
The present invention provides a stable, liquid ready-to-use injectable pharmaceutical formulation comprising lurbinectedin. The invention further relates to a process for preparing such formulation.
The present invention relates to a ready-to-use solution of carmustine that does not require dissolution or dilution of the carmustine prior to addition to saline and dextrose parenteral solutions. In particular, the invention relates to a stable liquid pharmaceutical composition containing carmustine in the form of ready-to-use solution and method for preparing the same.
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/175 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine having the group , N—C(O)—N=N— or , e.g. carbonohydrazides, carbazones, semicarbazides, semicarbazonesThioanalogues thereof
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
The present invention relates to a composition comprising nitrosourea and pharmaceutically acceptable excipients. In particular, the present invention relates to novel drug delivery systems of carmustine such as nano-suspension and micro-emulsion and its use for the treatment of cancer by intravenous administration. Also provided are methods for preparation of such novel drug delivery systems.
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
The present invention relates to an improved kit for preparing injectable carmustine solutions, methods of preparing and administering such solutions, and methods of treatment with such solutions. The kit includes a product vial containing lyophilised carmustine and a diluent vial containing an ethanol-free non-aqueous diluent. Reconstitution of the lyophilised carmustine in the ethanol-free non-aqueous diluent results in a carmustine solution with improved solubility and stability.
The present invention relates to a ready-to-use solution of carmustine that does not require dissolution or dilution of the carmustine prior to addition to saline and dextrose parenteral solutions. In particular, the invention relates to a stable liquid pharmaceutical composition containing carmustine in the form of ready-to-use solution and method for preparing the same.
The present invention provides a process for preparation of isoproterenol hydrochloride (1a) comprising catalytic hydrogenation of 3′,4′-dihydroxy-2-(isopropylamino)-acetophenone hydrochloride (5a) in presence of an ion exchange resin, to provide isoproterenol hydrochloride (1a).
C07C 213/04 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reaction of ammonia or amines with olefin oxides or halohydrins
C07C 213/08 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
C07C 215/60 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by hydroxy groups with hydroxy groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain the chain having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
C07C 215/66 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with quaternised amino groups bound to the carbon skeleton
The present invention relates to a composition comprising nitrosourea and pharmaceutically acceptable excipients. In particular, the present invention relates to novel drug delivery systems of carmustine such as nano-suspension and micro-emulsion and its use for the treatment of cancer by intravenous administration. Also provided are methods for preparation of such novel drug delivery systems.
The present invention relates to a pharmaceutical lipid composition comprising nitrosoureas and process for its preparation. In particular, the compositions of present invention are useful in the treatment of brain cancers having improved physicochemical and pharmacokinetic characteristics.
A61K 31/175 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine having the group , N—C(O)—N=N— or , e.g. carbonohydrazides, carbazones, semicarbazides, semicarbazonesThioanalogues thereof
A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
A61K 9/19 - Particulate form, e.g. powders lyophilised
36 - Financial, insurance and real estate services
41 - Education, entertainment, sporting and cultural services
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
45 - Legal and security services; personal services for individuals.
Goods & Services
(1) Organization of exhibitions, trade fairs, seminar and other events for commercial or advertising purposes, all the aforesaid services being in the field of health care; Demonstration of goods; Dissemination of advertising matter; Presentation of goods on communication media, for retail purposes; Distribution of samples.
(2) Providing of training and education in pharmaceutical and medical fields including via the Internet, Audiovisual productions; Entertainment; Sporting and cultural activities; Organizing and arranging of workshops, forums, lectures, conferences, competitions and seminars; arranging of trade fairs, exhibitions and other events for educational purpose; publication of magazines, journals including journals online, books including electronic books, guides and databases in the field of medical and pharmaceutical.
(3) Chemical research; chemical analysis; biological and pharmaceutical research; hosting of computer sites; Bacteriological research; Biological research; Scientific and technological services and research and design relating thereto; Industrial analysis and research services; Design and development of computer hardware, software and databases.
(4) Medical services; Pharmacy advice; Dentistry; Healthcare services; veterinary services; veterinary assistance.
(5) Health Facilities; Welfare and Empowerment of Persons With Disability, Social Awareness; Exhibition for Cultural & Educational Purposes in the field of healthcare; Campaigning to spread social awareness; Conducting and Organizing workshops; Charity services.
05 - Pharmaceutical, veterinary and sanitary products
35 - Advertising and business services
41 - Education, entertainment, sporting and cultural services
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
(1) Pharmaceutical preparations for human purposes, namely, analgesics, antibiotics, anti-diabetics, antidiarrhea preparations, antibacterial handwashes, antibacterial skin soap hand-sanitizing preparations, anti-hypertensives, preparations for treating nausea and vertigo, cardio vascular agents, laxatives, central nervous system stimulants for respiratory purposes; anti-histamines, anti-inflammatory and anti-arthritic preparations, preparations for cancer, sarcoma, anti-diabetic preparations; preparations for the treatment of carpal tunnel syndrome, pharmaceutical preparations for the treatment of chronic pain, preparations for anti-parasitic. (1) Organization of exhibitions, trade fairs, workshops, forums, lectures, conferences, competitions for commercial and advertising purposes in the pharmaceutical and medical fields; Dissemination of advertising materials for others in the pharmaceutical and medical fields; Presenting the goods of others via the internet for retail purposes in the pharmaceutical and medical fields; Sample distribution for others of biotechnology products in the pharmaceutical and medical fields; Organization of seminars for commercial and advertising purposes in the pharmaceutical and medical fields; Charitable services for persons with disabilities, namely promoting public awareness of health and welfare; Providing business administration and management of health care facilities.
(2) Providing of training and education in pharmaceutical and medical fields via the Internet, and audiovisual productions, namely audio and video recordings and digital files; Organizing and arranging of workshops, forums, lectures, conferences, competitions and seminars in the pharmaceutical and medical fields; Arranging of exhibitions, trade fairs, workshops, forums, lectures, conferences, competitions and seminars for educational purposes in the pharmaceutical and medical fields; Publication of magazines, journals and journals online, books and electronic books, guides and electronic databases in the field of medical and pharmaceutical; Arranging and conducting exhibition for cultural & educational purposes in the pharmaceutical and medical fields.
(3) Chemical research; Chemical analysis; Hosting of computer sites; Bacteriological research; Research in the fields of biologic therapeutic preparations; Scientific research in the field of pharmacology, pharmaceuticals, and biochemistry; Design and development of computer hardware, software and databases.
(4) Medical services in the field of gynaecology, cardiology, pain and analgesics, HIV, anti-infectives, nephrology; Pharmacy advice; Dentistry; Healthcare services, namely medical screening services relating to cardiovascular disease; Healthcare services, namely medical ultrasound imaging services in the field of gynaecology, cardiology and nephrology; Veterinary services; Providing mental health rehabilitation facilities.
The invention relates to an improved method for the solution phase synthesis of Lanreotide acetate (1) comprising coupling of two suitably protected tetrapeptide fragments wherein the threonine hydroxyl is protected, to give an octapeptide, which on deprotection, oxidation, followed by treatment with acetic acid provides Lanreotide acetate (1) having desired purity.
The invention relates to improved method of synthesis for Treprostinil comprising condensation reaction of the carbonyl compound having allyl, alkyl, crotyl or MEM-protected phenolic hydroxyl group, compound (4) with a hydroxyl-protected alkynol (5) to give the condensation product, compound (6). Subjecting compound (6) to oxidation, reduction, hydroxyl protection and carbonylation, cyclization reactions gave the tricyclic derivative (10). Further reactions comprising reduction, hydrogenation and deprotection of the phenolic and side-chain hydroxyl groups, wherein the sequence and choice of reagents was governed by protecting groups, gave the triol intermediate, compound (14). Cyanoalkylation at phenolic hydroxyl functionality and further hydrolysis yielded the prostacyclin compound, Treprostinil (1) and its pharmaceutically acceptable salts, having desired purity.
C07C 51/08 - Preparation of carboxylic acids or their salts, halides, or anhydrides from nitriles
C07C 37/00 - Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring
C07C 45/64 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by introduction of functional groups containing oxygen only in singly bound form
C07C 253/00 - Preparation of carboxylic acid nitriles
C07C 253/30 - Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
C07B 51/00 - Introduction of protecting groups or activating groups, not provided for in groups
C07C 39/17 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring polycyclic with no unsaturation outside the aromatic rings containing other rings in addition to the six-membered aromatic rings
C07C 47/575 - Compounds having —CHO groups bound to carbon atoms of six-membered aromatic rings containing ether groups, groups, groups, or groups
C07C 59/72 - Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings and other rings
C07C 255/13 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and singly-bound oxygen atoms bound to the same saturated acyclic carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
14.
PARTICLE SIZE STABILIZATION OF PROTEIN BOUND PARTICLES AND METHODS THEREOF
The present invention relates to stable paclitaxel and albumin nanosuspension suitable for intravenous administration and method of preparation thereof.
The present invention provides a process for preparation of trientine dihydrochloride (1) comprising reaction of protected triethylene tetramine with hydrochloric acid in an aqueous system to yield the dihydrochloride salt wherein the formation of inorganic impurities and undesired salts is controlled significantly.
C07C 209/50 - Preparation of compounds containing amino groups bound to a carbon skeleton by reduction of carboxylic acids or esters thereof in presence of ammonia or amines, or by reduction of nitriles, carboxylic acid amides, imines or imino-ethers by reduction of carboxylic acid amides
16.
PROCESS FOR PREPARATION OF ISOPROTERENOL HYDROCHLORIDE
The present invention provides a process for preparation of isoproterenol hydrochloride (1a) comprising catalytic hydrogenation of 3',4'-dihydroxy-2-(isopropylamino)-acetophenone hydrochloride (5a) in presence of an ion exchange resin, to provide isoproterenol hydrochloride (1a).
C07C 213/00 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
C07C 213/10 - SeparationPurificationStabilisationUse of additives
C07C 215/60 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by hydroxy groups with hydroxy groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain the chain having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
C07C 215/66 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with quaternised amino groups bound to the carbon skeleton
The present invention relates to a stable liquid formulation of cabazitaxel. The formulation comprises cabazitaxel and at least one solubilizer. Typically, formulations are in the form of ready-to-use solutions or concentrates.
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
The present invention relates to a pharmaceutical lipid composition comprising nitrosoureas and process for its preparation. In particular, the compositions of present invention are useful in the treatment of brain cancers having improved physicochemical and pharmacokinetic characteristics.
A61K 31/175 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine having the group , N—C(O)—N=N— or , e.g. carbonohydrazides, carbazones, semicarbazides, semicarbazonesThioanalogues thereof
The invention relates to an improved method for a 5+3+2 solution phase syntheses of Icatibant acetate (1) comprising coupling of suitably protected peptide fragments which on deprotection followed by treatment with acetic acid provide Icatibant acetate (1) having desired purity.
The invention relates to an improved method for 4+4 solution phase synthesis of Lanreotide acetate (1) comprising coupling of two suitably protected tetrapeptide fragments which on deprotection, oxidation, followed by treatment with acetic acid to provide Lanreotide acetate (1) having desired purity.
The present invention relates to pharmaceutical compositions of Apixaban or pharmaceutically acceptable salts thereof and pharmaceutically acceptable excipients and process for its preparation. The compositions were prepared by conventional methods using pharmaceutically acceptable excipients. The impact of particle size on formulation dissolution parameters was also studied. The pharmaceutical compositions of present invention are particularly useful as a medicament, especially for the treatment or prevention of a thromboembolic disorders such as deep vein thrombosis, pulmonary embolism, non-valvular atrial fibrillation.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
Disclosed herein is an improved 4+4 solution phase synthesis of Lanreotide acetate. The process comprises coupling of two suitably protected tetrapeptide fragments which on deprotection, oxidation, followed by treatment with acetic acid provides Lanreotide acetate having desired purify.
Disclosed herein is an improved 4+4 solution phase synthesis of octreotide acetate. The process comprises coupling of two suitably protected tetrapeptide fragments which on deprotection, oxidation, and treatment with acetic acid provides octreotide acetate having desired purify.
Present invention relates to novel heterocyclic compounds as indoleamine 2,3- dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) modulators. Compounds of the present invention inhibit tryptophan degradation by modulating IDO and/or TDO. Formula (I) The invention further relates to the process of their preparation, pharmaceutical composition and their use in modulating the activity of indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3- dioxygenase (TDO). The compounds of the invention can be used alone or in combination for the treatment of conditions that benefits from the inhibition of tryptophan degradation.
Present invention relates to novel heterocyclic compounds as indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) modulators. Compounds of the present invention inhibit tryptophan degradation by modulating IDO and/or TDO. Formula (I) The invention further relates to the process of their preparation, pharmaceutical composition and their use in modulating the activity of indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3- dioxygenase (TDO). The compounds of the invention can be used alone or in combination for the treatment of conditions that benefits from the inhibition of tryptophan degradation.
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
Disclosed is an improved method of synthesis for Treprostinil comprising condensation reaction of compound (4) with a hydroxyl-protected alkynol (5) to give the condensation product, compound (6). Subjecting compound (6) to oxidation, reduction, hydroxyl protection and carbonylation, cyclization reactions gives the tricyclic derivative (10). Further reactions comprising reduction, hydrogenation and deprotection of the phenolic and side-chain hydroxyl groups, wherein the sequence and choice of reagents is governed by protecting groups, give the triol intermediate, compound (14). Cyanoalkylation at phenolic hydroxyl functionality and further hydrolysis yields the prostacyclin compound, Treprostinil (1) and its pharmaceutically acceptable salts with desired purity.
C07C 49/798 - Ketones containing a keto group bound to a six-membered aromatic ring having unsaturation outside an aromatic ring containing rings other than six-membered aromatic rings
C07C 39/12 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring polycyclic with no unsaturation outside the aromatic rings
C07C 69/76 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring
The present invention relates to pharmaceutical compositions of Teriflunomide or pharmaceutically acceptable salts thereof and method of preparation of such compositions. Typically, the composition according to present invention comprises about 1% w/w to about 30% w/w Teriflunomide, or a pharmaceutically acceptable salt thereof, about 0.1% w/w to about 0.8% w/w colloidal silicon dioxide, about 5% w/w to about 20% w/w disintegrant, about 0% w/w to about 40% w/w binder, about 0.1% w/w to about 2% w/w lubricant and the remaining percentage comprising diluents and optionally suitable agents to adjust the pH of the composition in the range of about 4.5 to 7.0.
The present invention relates to bulk sterilized parenteral suspension, formulations comprising water insoluble drugs suitable for parenteral use, Further, a process of preparation of such bulk sterilized suspension compositions employing conventional sterilization process under homogenization is also disclosed, The sterilization under homogenization is earned for prolonged period and the finally aseptically filled into suitable container closure systems. The bulk sterilized suspensions prepared by using the current invention exhibited good physical and chemical stability.
The present invention provides a process for preparation of trientine dihydrochloride (1) comprising reaction of protected triethylene tetramine with hydrochloric acid in an aqueous system to yield the dihydrochloride salt wherein the formation of inorganic impurities and undesired salts is controlled significantly.
C07C 209/44 - Preparation of compounds containing amino groups bound to a carbon skeleton by reduction of carboxylic acids or esters thereof in presence of ammonia or amines, or by reduction of nitriles, carboxylic acid amides, imines or imino-ethers
C07C 211/14 - Amines containing amino groups bound to at least two aminoalkyl groups, e.g. diethylenetriamines
C07C 209/00 - Preparation of compounds containing amino groups bound to a carbon skeleton
The present invention relates to a novel synthetic route for the preparation of raltegravir and pharmaceutically acceptable salts, starting from 2-amino-2-methylpropanenitrile and oxadiazole carbonyl chloride, through the formation of a pyrimidinone intermediate of formula (V).
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
A process for preparation of diethyl 2-aetamido-2-(4-octyl phenyl)ethyl malonate (III), a key intermediate of fingolimod hydrochloride comprising reaction of 2-(4-octylphenyl)ethyl iodide (IV) with diethyl acetamido malonate in presence of a base and an iodinating agent and in an organic solvent. The compound of formula (III) thus obtained provided fingolimod hydrochloride (Ia) having associated impurities below the regulatory limits.
C07C 213/02 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
C07C 215/28 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 213/00 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment of iron deficiency and anaemia due to iron deficiency, for human use; pharmaceutical vitamin preparations for human use, namely, Ferrous Ascorbate and Folic Acid; mineral supplements
The present invention relates to a stable liquid formulation of cabazitaxel. The formulation comprises cabazitaxel, and at least one solubilizer. Typically, formulations are in the form of ready-to-use solutions or concentrates.
The present invention relates to a stable ready-to-use injectable pharmaceutical formulation of bortezomib or pharmaceutically acceptable salts thereof. Methods of preparing such formulations are also provided.
The present invention provides a process for preparation of {(2E,4E,6E,8E)-9-(4-methoxy-2,3,6- trimethyl)phenyl-3,7-dimethyl-nona-2,4,6,8}tetraenoate, an acitretin intermediate of formula (VI) with trans isomer ≥97%, comprising of reacting 3-formyl-crotonic acid butyl ester of formula (V), substantially free of impurities, with 5-(4-methoxy-2,3,6-trimethylphenyl)-3- methyl-penta-2,4-diene-l-triphenyl phosphonium bromide of formula (IV) and isolating resultant compound of formula (VI), treating the filtrate with iodine for isomerization of the undesired cis intermediate and finally obtaining acitretin (I), with desired trans isomer ≥97%.
The present invention provides a pharmaceutical composition comprising Vitamin Kl and the process for preparation of the same. In particular, the present invention relates to stable injectable pharmaceutical compositions comprising a desired diastereomer of phytonadione in quantity not less than 50% of the total weight of active ingredient.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for human purposes, namely, analgesics, antibiotics, anti diabetics, anti diarrhea preparations, anti bacterial preparations, anti hypertensives, preparations for treating nausea and vertigo, cardio vascular agents, laxatives, central nervous system stimulants for respiratory purposes; anti-histamines, anti-inflammatory and anti-arthritic preparations, preparations for cancer, sarcoma, antidiabetic preparations; preparations for the treatment of carpal tunnel syndrome, pharmaceutical preparations for the treatment of chronic pain, preparations for antiparasitic.
The present invention relates to an improved solid formulation of (2S,3S)-2,3-Dihydroxy-4- methylsulfonyloxybutyl] methanesulfonate. The improved formulations are lyophilized pharmaceutical solid composition containing treosulfan for reconstitution with water to provide a solution for parenteral administration. The present invention also relates to Polymorphic Form I and II of treosulfan.
The present invention relates to a novel synthetic route for the preparation of fingolimod and its pharmaceutically acceptable salts. The synthetic strategy comprises reaction of 2-(4- octylphenyl)-acetaldehyde with nitro acetonide, and subsequent conversions of the resulting acetonide protected nitro-alcohpl intermediates of formulae (8), (9) and (10) to the penultimate acetonide protected amino intermediates of formula (11), which on deprotection with acid yields Fingolimod and its corresponding salts, having purity conforming to regulatory specification.
C07C 309/34 - Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of six-membered aromatic rings being part of condensed ring systems formed by two rings
A process for preparation of diethyl 2-acetamido-2-(4-octyl phenyl)ethyl malonate (III), a key intermediate of fingolimod hydrochloride comprising reaction of 2-(4- octylphenyl)ethyl iodide (IV) with diethyl acetamido malonate in presence of a base and an iodinating agent and in an organic solvent. The compound of formula (III) thus obtained provided fingolimod hydrochloride (la) having associated impurities below the regulatory limits.
C07C 213/02 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
C07C 215/30 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings containing hydroxy groups and carbon atoms of six-membered aromatic rings bound to the same carbon atom of the carbon skeleton
The present invention relates to a novel synthetic route for the preparation of raltegravir and pharmaceutically acceptable salts, starting from 2-amino-2-methylpropanenitrile and oxadiazole carbonyl chloride, through the formation of a pyrimidinone intermediate of formula (V).
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
43.
PYRIDONE DERIVATIVES AS ACID SECRETION INHIBITORS AND PROCESS FOR PREPARATION THEREOF
Provided are pyridine disulphide derivatives of Formula (I) and their preparation, pharmaceutical composition. The pyridine disulphide derivatives are useful in the treatment of gastrointestinal disorders. wherein, R1, R2 and R3 are independently alkyl, alkoxy, halogen, halogenated alkoxy, halogenated alkyl, hydrogen and could be same or different and X is CH or N. R1 is methyl, methoxy, fluorine, trifluoromefhyl, difluoromethoxy and hydrogen, R2 is methyl, methoxy and hydrogen, and R3 is methyl and hydrogen.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
The present invention relates to a stable injectable emulsion formulation of Propofol having uniform droplet size, which is obtained at a pH above 8.5 and by avoiding a rotary sterilizer.
41 - Education, entertainment, sporting and cultural services
45 - Legal and security services; personal services for individuals.
Goods & Services
Organization of exhibitions, trade fairs, seminar and other events for commercial or advertising purposes all the aforesaid services being in the field of health care; Demonstration of goods; Dissemination of advertising matter; Presentation of goods on communication media, for retail purposes; Distribution of samples. Providing of training and education in pharmaceutical and medical fields including via the Internet, Audiovisual productions; Entertainment; Sporting and cultural activities; Organizing and arranging of workshops, forums, lectures, conferences, competitions and seminars; arranging of trade fairs, exhibitions and other events for educational purpose; publication of magazines, journals including journals online, books including electronic books, guides and databases in the medical and pharmaceutical field; Exhibition for Cultural & Educational Purposes in the field of healthcare; Conducting and Organizing workshops; Provision of health club facilities. Welfare and Empowerment of Persons With Disability, Social Awareness; Campaigning to spread social awareness; Charity services.
The present invention relates to a novel synthetic route for the preparation of raltegravir and pharmaceutically acceptable salts, starting from 2-amino-2- methylpropanenitrile and oxadiazole carbonyl chloride, through the formation of a pyrimidinone intermediate of formula (V).
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
C07D 239/557 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms, e.g. orotic acid
C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
Provided is a pharmaceutical composition for oral administration comprising nisoldipine and one or more release controlling polymer, elected from various hydrophilic polymers or combinations thereof. Said polymer is present at a concentration of about 1% to about 60% by weight of the tablet, preferably from about 10% to about 40% by weight of the tablet. Said composition may also contain one or more adjuvant in combination with polymeric materials in order to modulate the release of nisoldipine.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
The present invention relates to pharmaceutical compositions comprising aliphatic amine polymer. The formulation, preferably a tablet, contains suitable excipients such as diluents along with the aliphatic amine polymer. The judicious selection of diluent in the pharmaceutical composition of the present invention, results in a formulation having desired characteristics.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical and medicinal preparations and products for human use; sanitary preparations; dietetic substances adapted for medical use, food for babies; plasters, materials for dressings; materials for stopping teeth, dental wax; disinfectants.
Provided is a process for the preparation of eptifibatide using a novel non-linear liquid phase peptide synthesis scheme. This invention makes use of combing precursor peptides synthesized separately in high purity and yield over presently known processes. The disclosed process has several advances over known processes like ease of scale-up and work-up as the process utilizes liquid phase peptide preparation chemistry.
C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
C07K 1/06 - General processes for the preparation of peptides using protecting groups or activating agents
C07K 1/02 - General processes for the preparation of peptides in solution
C07K 5/113 - Tetrapeptides the side chain of the first amino acid containing more carboxyl groups than amino groups, or derivatives thereof, e.g. Asp, Glu, Asn
C07K 5/09 - Tripeptides the side chain of the first amino acid containing more amino groups than carboxyl groups, or derivatives thereof, e.g. Lys, Arg
The present invention provides a convenient and industrially viable process for preparation of Zolmitriptan (I) having desired purity. The invention specifically relates to a method for isolating (S)-4-(4-hydrazinobenzyl)-l,3-oxazolidin-2-one hydrochloride (Ilia) of desired purity by separating the undesired inorganic side products such as stannous hydroxide by manipulation of pH at different stages and finally treating with Ν,Ν-dimethylamino butyraldehyde diethyl acetal in an acidic medium to provide Zolmitriptan (I) conforming to regulatory specifications.
C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
pharmaceutical preparations for human purposes, namely, [ analgesics, antibiotics, anti diabetics, anti diarrhea preparations, anti bacterial preparations, anti hypertensives, ] preparations for treating nausea and vertigo [, cardio vascular agents, laxatives, central nervous system stimulants for respiratory purposes; anti-histamines, anti-inflammatory and anti-arthritic preparations ]
53.
PROCESS FOR PREPARATION OF RILPIVIRINE INTERMEDIATE
Disclosed is process for the preparation of a key Rilpivirine intermediate namely, (E)-4-(2-cyanoethenyl)-2,6-dimethylphenylamine hydrochloride (II) by a process comprising reaction of the tetrafluoroborate salt of the diazonium ion of 2,6-dimethyl-4-amino-l-carboxybenzyl phenylamine (VI) with acrylonitrile in presence of palladium acetate, followed by treatment with an acid and its subsequent conversion to the hydrochloride salt (II), wherein the undesired Z isomer is less than 0.5% and provides Rilpivirine hydrochloride having Z isomer less than 0.1%.
C07C 255/34 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring with cyano groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by unsaturated carbon chains
C07C 253/30 - Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
C07D 239/04 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
54.
Process for the preparation of melphalan hydrochloride
The present invention provides a simple and efficient method for synthesis of 4-[bis(2-chloroethyl)-amino]-L-phenylalanine hydrochloride. The process involves the treatment of 4-[bis(2-chloroethyl)-amino]-L-phenylalanine free base with hydrochloric acid in water followed by isolation of 4-[bis(2-chloroethyl)-amino]-L-phenylalanine hydrochloride of desired purity.
C07C 229/00 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton
C07C 227/18 - Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions involving amino or carboxyl groups, e.g. hydrolysis of esters or amides, by formation of halides, salts or esters
55.
PROCESS FOR SYNTHESIS OF DIARYLPYRIMIDINE NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITOR
A method for synthesis of diarylpyrimidine non-nucleoside reverse transcriptase inhibitor such as etravirine is provided Typically, etravirine is synthesized by the steps of a Condensing 2,4,6-trichlorpyrimidine with 3,5-dimethyl-4-hydroxybenzonitrile to obtain compound (V), b Condensing compound (V) with 4-aminobenzonitrile to obtain compound (VI), c Ammonolysis of compound (VI) to get compound (IV), d Halogenation of compound (IV) to get etravirine.
A simple, cost-effective process for preparation of efavirenz of formula (I) comprising reacting a solution of 5-chloro-α-(cyclopropylethynyl)-2-amino-α-trifluoromethyl) benzene methanol of formula (II) in an organic solvent with triphosgene in the presence of an inorganic base at a temperature range -5 °C to 25 °C, adding water and isolating compound of formula (I).
C07D 265/18 - 1,3-OxazinesHydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in position 2
57.
Cost-effective process for preparation of manufacture of iron sucrose
The present invention relates to a new process for the preparation of sulfoxides, preferably stereoselective preparation of substituted or unsubstituted chiral sulfinyl derivatives 2-(2- pyridylmethyl) sulfinyl-l H-benzimidazole by oxidation with oxaziridine in presence of suitable solvent and base.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
The present invention relates to a stable pharmaceutical composition comprising therapeutically effective amounts of amlodipine or its pharmaceutically acceptable salt and benazepril or its pharmaceutically acceptable salt and at least one pharmaceutically acceptable carrier wherein the stability of the composition is achieved by an effective stabilizing amount of a buffering agent.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 31/4422 - 1,4-Dihydropyridines, e.g. nifedipine, nicardipine
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A unit dosage pharmaceutical preparation is disclosed. Said preparation comprises: a. functional coated composition of galanthamine or its salts; and b. uncoated/seal coated composition of galanthamine or its salts.
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
The present invention relates to an oral, stable pharmaceutical composition of angiotensin converting enzyme (ACE) inhibitor in combination with a diuretic, and to a process for preparation thereof.
The present invention relates to an improved, safe, commercially viable, cost effective and eco friendly process for the preparation of 4,1',6'-trichloro-4,1',6'-trideoxygalactosucrose (Sucralose). The invention is directed towards the convenient synthesis of 2,3,4,3',4'-penta-O-acetyl sucrose (4-PAS) from 6,1',6'-tri-O-trityl-penta-O-acetyl sucrose ('TRISPA').
C07H 5/02 - Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium to halogen
