Abstract

The present invention relates to a process for the preparation of Trisodium (4-{ [(1S.3R)- 1-([1,1'-biphenyl]-4-ylmethyl)-4-ethoxy-3-methyl-4-oxobutyl]amino}-4-oxo butanoate)-(N- pentanoyl-N-{[2'-(1H-tetrazol-1-id-5-yl)[1,1'-biphenyl]-4-yl]methyl}-L-valinate) represented by the following structural formula-1 :

IPC Classes  ?

• C07C 235/82 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring

Abstract

The present invention relates to an improved process for the preparation of (3R,4R)-4-methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl-amino)-ß-oxo-1-piperidine propanenitrile compound of formula-1 and its pharmaceutically acceptable salts. [Formula should be inserted here]

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

Abstract

The present invention relates to a novel polymorph of isobutyric acid 2-((R)-3-diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl) phenyl ester hydrochloride represented by the following structural formula-1a and process for its preparation.

IPC Classes  ?

• A61K 31/235 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
• C07C 213/06 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton from hydroxy amines by reactions involving the etherification or esterification of hydroxy groups

Abstract

The present invention relates to a process for the preparation of 2-(2-aminothiazol-4-yl)- N-[4-(2- {[(2R)-2-hydroxy-2-phenylethyl]amino} ethyl)phenyl]acetamide monohydrochloride compound of formula- la, its intermediates and polymorph thereof. [Formula should be inserted here]

IPC Classes  ?

• C07C 233/07 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
• C07D 277/36 - Sulfur atoms
• A61K 31/16 - Amides, e.g. hydroxamic acids

Abstract

The present invention provides a novel intermediate as well as novel polymorphs of l-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-l-yl)phenyl]-4,5,6,7-tetrahydro-lH- pyrazolo[3,4-c]pyridine-3-carboxamide compound represented by the following structural formula- 1 and processes for their preparation.

IPC Classes  ?

• C07D 471/02 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed system contains two hetero rings
• A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines

Abstract

The present invention relates to novel process for the preparation of (1S,3aR,6aS)-2- [(2S)-2-({(2S)-2-cyclohexyl-2-[(pyrazin-2-ylcarbonyl)amino]acetyl}amino)-3,3-dimethylbutanoyl]-N-[(3S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl]-3,3a,4,5,6,6a-hexahydro-1H- cyclopenta[c] pyrrole- 1-carboxamide compound represented by the following structural formula- 1 and intermediates thereof. The present invention also provides crystalline polymorphs of intermediates of compound of formula- 1.

IPC Classes  ?

• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone

Abstract

THE PRESENT INVENTION RELATES TO AN IMPROVED PROCESS FOR THE PREPARATION OF (1R,5S)-N-[3-AMINO-1-(CYCLOBUTYLMETHYL)-2,3-DIOXOPROPYL]-3-[2(S)-[[[(1,1-DIMETHYLETHYL)AMINO]CARBONYL] AMINO]-3,3-DIMETHYL-1-OXOBUTYL]-6,6-DIMETHYL-3-AZABICYCLO[3.1.0]HEXAN-2(S)-CARBOXAMIDE AND ITS INTERMEDIATES

IPC Classes  ?

• C07D 209/52 - Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
• C07C 233/08 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to acyclic carbon atoms of a saturated carbon skeleton containing rings
• C07K 5/08 - Tripeptides

Abstract

The present invention relates to an improved process for the preparation of antidepressant drug i.e., 5-[4-[4-(5-cyano-1H-indol-3-yl)butyl]-1-piperazinyl]-2-benzofuran carboxamide hydrochloride compound of formula- la represented by the following structural formula: (1a)

IPC Classes  ?

• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 209/10 - IndolesHydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin

Abstract

Provided processes for the preparation of (5-methyl-2-oxo-l,3-dioxol-4-yl)methyl 2-ethoxyl- 1 - { [2 '-(5-oxo-4,5 -dihydro- 1,2,4-oxadiazol-3 -yl)biphenyl-4-yl]methyl } - 1 H-benzimidazole-7 -carboxylate, its potassium salt and polymorphs thereof.

IPC Classes  ?

• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• A61K 31/4245 - Oxadiazoles
• A61P 9/12 - Antihypertensives

Abstract

Provided are novel salts of benzimidazole derivatives, preferably salts of benzimidazole derivatives which are useful intermediates in the synthesis of pure 1-methyl-2-[N-[4-(N-n-hexyloxycarbonylamidino)phenyl]aminomethyl]benzimidazol-5-yl-carboxylicacid-N -(2-pyridyl)-N-(2-ethoxycarbonylethyl)amide and its salts.

IPC Classes  ?

• C07D 277/64 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
• C07D 235/14 - Radicals substituted by nitrogen atoms
• C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
• C07D 495/04 - Ortho-condensed systems
• A61K 31/425 - Thiazoles

Abstract

The present invention provides a process for the preparation of (l S,3S,5S)-2-[(2S)-2- amino-2-(3 -hydroxyadamantan- l-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile and its pharmaceutically acceptable salts thereof, represented by the compound of formula- 1.

IPC Classes  ?

• C07C 29/147 - Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by reduction of an oxygen-containing functional group of C=O containing groups, e.g. —COOH of carboxylic acids or derivatives thereof
• C07C 35/52 - Alcohols with a condensed ring system
• C07D 213/00 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members

Abstract

The present invention relates to novel process for the preparation of 3-[(lR,2R)-3- (dimethylamino)-l-ethyl-2-methylpropyl]phenol and its pharmaceutically acceptable salts.

IPC Classes  ?

• 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 215/54 - 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 not further substituted by hydroxy groups linked by carbon chains having at least three carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
• C07C 217/72 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified 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 singly-bound oxygen atoms with singly-bound oxygen atoms and six-membered aromatic rings bound to the same carbon atom of the carbon chain linked by carbon chains having at least three carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
• A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine

Abstract

A process for the preparation of 4-[4-[4-[4-[[(3R,5R)-5-(2,4-difluorophenyl) tetrahydro-5-(lH-l,2,4-triazol-l-ylmefhyl) -3-furanyl]mefhoxy] phenyl] -1 -piperazinyl] phenyl]-2-[(lS,2S)-l-efhyl-2-hydroxypropyl]-2,4-dihydro-3H-l,2,4-triazol-3-one compound of formula- 1, its intermediates and polymorphs thereof.(I)

IPC Classes  ?

• C07D 295/135 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 307/16 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 407/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Abstract

Disclosed are processes for the preparation of 1-(3-hydroxypropyl)-5-[(2R)-2-({2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl} amino)propyl] -2,3-dihydro-lH-indole-7-carboxamide compound represented by the following structural formula-1 and it's pharmaceutical composition. (I)

IPC Classes  ?

• C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
• C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
• A61K 31/404 - Indoles, e.g. pindolol
• A61P 13/08 - Drugs for disorders of the urinary system of the prostate
• A61P 13/02 - Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
• A61P 13/00 - Drugs for disorders of the urinary system

Abstract

The present invention relates to novel and improved processes for the preparation of (r)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenylisobutyrate represented by the following structural formula-1 and its pharmaceutically acceptable salts thereof.

IPC Classes  ?

• C07C 219/28 - Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified 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 having amino groups bound to acyclic carbon atoms of the carbon skeleton
• C07C 213/10 - SeparationPurificationStabilisationUse of additives
• 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
• C07C 215/48 - 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 not further substituted by hydroxy groups
• C07C 29/12 - Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by hydrolysis of esters of mineral acids
• C07C 29/136 - Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by reduction of an oxygen-containing functional group of C=O containing groups, e.g. —COOH
• C07C 209/88 - Separation of optical isomers
• C07C 209/74 - Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton by halogenation, hydrohalogenation, dehalogenation, or dehydrohalogenation
• 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 213/02 - 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 213/06 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton from hydroxy amines by reactions involving the etherification or esterification of hydroxy groups
• 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
• A61K 31/222 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
• A61P 13/10 - Drugs for disorders of the urinary system of the bladder

Abstract

An dabigatran etexilate intermediate of Forumla-6a, and the use in the preparation of dabigatran etexilate thereof.

IPC Classes  ?

• C07D 401/02 - 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
• 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
• A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors

Abstract

An improved process for preparing (+)-[lR(S), 2S(R)]-2-(aminomethyl)-N, N- diethyl-l-phenylcyclopropane carboxamide hydrochloride compound of formula-la is provided.

IPC Classes  ?

• C07D 307/93 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
• C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
• C07C 237/24 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton

Abstract

A process for the preparation of N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide of Formula-1 is provided. The crystalline forms of its intermediates as well as the final compound are also provided.

IPC Classes  ?

• C07C 233/18 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
• C07C 231/06 - Preparation of carboxylic acid amides from nitriles by transformation of cyano groups into carboxamide groups
• C07C 211/25 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings other than six-membered aromatic rings

Abstract

Improved processes for preparation of asenapine by using specific intermediates and reaction conditions are provided. The intermediates for preparation of asenapine and the pharmaceutical composition comprising asenapine are also provided.

IPC Classes  ?

• C07D 491/044 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

Abstract

Disclosed are novel polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-iso-propyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl] (3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium.

IPC Classes  ?

• C07D 239/42 - One nitrogen atom
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• C07F 3/04 - Calcium compounds
• A61P 3/06 - Antihyperlipidemics

Abstract

The present invention relates to a process for the preparation of (2S,4S,5S,7S)-N-(2- Carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3-methoxy propoxy )phenyl]-octanamide compound of formula- 1 and its pharmaceutically acceptable salts thereof. Further, relates to the processes for the preparation of (R)-4-(2-(halomethyl)-3- methylbutyl)-l-methoxy-2-(3-methoxypropoxy) benzene and (R)-2-(4-methoxy-3-(3-methoxy propoxy) benzyl)-3-methyIbutan-l-ol useful intermediates in the synthesis of compound of formula- 1.

IPC Classes  ?

• C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
• C07C 247/12 - Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by carboxyl groups
• C07D 207/32 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
• C07D 303/40 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals by ester radicals

Abstract

Disclosed are novel and improved processes for the preparation of 2-[3-cyano-4-(2-methylpropoxy)phenyl]^l-methyl thiazole-5-carboxylic acid compound of Formula- 1 and pharmaceutically acceptable salts thereof. Novel processes for the preparation of crystalline forms of 2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methylthiazole-5-carboxylic acid compound of Formula-1 and its intermediates are also provided. (I)

IPC Classes  ?

• C07D 277/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
• A61K 31/426 - 1,3-Thiazoles
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents

Abstract

Processes for preparing (S)-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide and its intermediates are provided.

IPC Classes  ?

• C07D 223/22 - Dibenz [b, f] azepinesHydrogenated dibenz [b, f] azepines

Abstract

An improved process for the preparation of 11 -[(Z)-3-(dimethylamino)propylidene]-6,11-dihydrodibenzo[b,e]oxepin-2-acetic acid compound of formula-1 and pharmaceutically acceptable salts thereof are disclosed.

IPC Classes  ?

• C07D 313/12 - [b, e]-condensed
• C07F 9/54 - Quaternary phosphonium compounds

Abstract

Process for the preparation of DPP-IV inhibitors, such as 1-[[(3-hydroxy-1-adamantyl) amino] acetyl]-2-cyano-(S)-pyrrolidine are disclosed.

IPC Classes  ?

• C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07C 211/38 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton containing condensed ring systems

Abstract

Processes for preparing and purifying (R)-2-acetamido-N-benzyl-3-methoxy- propionamide of formula-1 and intermediates thereof are provided.

IPC Classes  ?

• C07C 237/06 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
• C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
• C07C 233/16 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
• C07C 229/22 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated the carbon skeleton being further substituted by oxygen atoms

Abstract

A pharmaceutical composition of prasugrel or its pharmaceutically acceptable salts, especially hydrochloride salts as well as process for their preparation are provided. The pharmaceutical composition comprises: a) prasugrel hydrochloride, b) a water insoluble dry binder, c) at least one diluent, d )at least one disintegrant and e) at least one lubricant. The pharmaceutical composition is optionally coated with a film. An improved process for preparing of prasugrel and its pharmaceutically acceptable salts, a process for purifying 5,6,7,7a-tetrahydro-4H-thieno[3,2-c]pyridine-2 -one hydrochloride compound, a process for preparing crystalline form-B2 of prasugrel hydrochloride and a process for preparing a-cyclopropylcarbonyl-2-fluorobenzyl bromide compound are provided.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems
• A61K 31/4365 - 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 having sulfur as a ring hetero atom, e.g. ticlopidine
• A61K 9/20 - Pills, lozenges or tablets
• A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

A solid pharmaceutical composition of moxifloxacin, its pharmaceutically acceptable salts and/or hydrates thereof as well as process for its preparation are disclosed. Furthermore, a stable aqueous formulation of moxifloxacin hydrochloride and process for its preparation are also disclosed. The pharmaceutical compositions disclosed herein can be used for the treatment and/or the prevention of bacterial infections in humans and/or animals.

IPC Classes  ?

• 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
• A61K 47/04 - Non-metalsCompounds thereof
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61K 9/08 - Solutions
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/28 - DrageesCoated pills or tablets
• A61P 31/04 - Antibacterial agents

Abstract

The present invention relates to an improved process for the preparation of amide intermediates useful in the preparation of cholesterol reducing agents.

IPC Classes  ?

• C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 239/12 - Nitrogen atoms not forming part of a nitro radical
• C07D 319/06 - 1,3-DioxanesHydrogenated 1,3-dioxanes not condensed with other rings

Abstract

The present invention relates to an improved process for the preparation of dihydroxy protected derivatives, which are important intermediates in the preparation of HMG-CoA reductase inhibitors.

IPC Classes  ?

• C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07C 49/12 - Ketones containing more than one keto group

Abstract

Processes for preparing pregabalin and its intermediate such as 3-(carbamoylmethyl)-5-methylhexanoic acid are provided. The process for preparing pregabalin mainly comprises reacting 3-(carbamoylmethyl)-5-methylhexanoic acid with (+)-phenyl ethyl amine, followed by reacting with bromine in the presence of base to obtain pregabalin.

IPC Classes  ?

• C07C 227/32 - Preparation of optical isomers by stereospecific synthesis
• C07C 229/08 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to hydrogen atoms
• C07C 233/05 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
• C07C 231/06 - Preparation of carboxylic acid amides from nitriles by transformation of cyano groups into carboxamide groups
• C07C 231/16 - Preparation of optical isomers
• C07C 211/01 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms

Abstract

Disclosed are improved processes for preparing prasugrel compound of formula-(1), its intermediates and pharmaceutically acceptable salts.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems
• A61K 31/4365 - 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 having sulfur as a ring hetero atom, e.g. ticlopidine
• A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors

Abstract

An improved process for the preparation of (±)-1-(1-Benzo[b]thien-2-ylethyl)-1-hydroxyurea compound of formula (I).

IPC Classes  ?

• C07D 333/58 - Radicals substituted by nitrogen atoms

Abstract

An improved process for preparing (S)-2-amino-4, 5, 6, 7-tetrahydro-6-(propylamino) benzothiazole (pramipexole) and its dihydrochloride monohydrate is provided. Pramipexole dihydrochloride is the compound represented by the following structural formula-1a.

IPC Classes  ?

• C07D 277/82 - Nitrogen atoms

Abstract

An improved process for preparing 4-(l, l-dimethylethyl)-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-[2, 2'-bipyπmidin]-4-yl] benzene sulfonamide monohydrate compound of formula-1 is disclosed

IPC Classes  ?

• C07D 239/52 - Two oxygen atoms
• C07D 239/69 - Benzenesulfonamido-pyrimidines
• C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 413/00 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms

Abstract

An improved process for preparing 4-[3, 5-bis (2-hydroxyphenyl)-l, 2, 4-tπazol-l -yl] benzoic acid of formula-1 and a process for its purification are provided The preparation process comprises reacting salicylic acid with salicylamide in the presence of a suitable base, in a suitable solvent and in the presence of thionyl chloride at reflux temperature, then reacting 2-(2-hydroxyphenyl)-benz[e][l,3]oxazin^-one with 4-hydrazinobenzoic acid in a suitable alcoholic solvent at reflux temperature to provide deferasirox.

IPC Classes  ?

• C07D 249/08 - 1,2,4-TriazolesHydrogenated 1,2,4-triazoles
• A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
• A61P 39/04 - Chelating agents

Abstract

The present invention relates to novel salts of ethyl (3R,4S,5R)- 4,5-imino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate and its use in the preparation of (3R,4R,5S)-4-(acetylamino)-5-amino-3-(1-ethyl propoxy)-1-cyclohexene-1-carboxylic acid ethyl ester and its pharmaceutically acceptable salts.

IPC Classes  ?

• C07D 203/26 - Heterocyclic compounds containing three-membered rings with one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
• C07D 203/02 - Preparation by ring-closure
• C07C 247/16 - Compounds containing azido groups with azido groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton

Abstract

Disclosed is an improved process for preparing (5-methyl-2-oxo-l,3-dioxolen-4-yl)methyl 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[4-[2-(tetrazol-5-yl)phenyl]phenyl]methylimidazole-5-carboxylate (formula-1, commonly known as "olmesartan medoxomil") through crystalline (5-methyl-2-oxo-1,3-dioxolen-4-yl) methyl 4-(1-hydroxy-1 -methylethyl)-2-propyl-1 -[4-[2-(trityltetrazol-5-yl)phenyl]phenyl]methylimidazole-5-carboxylate (commonly known as "trityl olmesartan medoxomil").

IPC Classes  ?

• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 233/90 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
• A61P 9/12 - Antihypertensives
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

Improved processes for the preparation of Sitagliptin compound of formula-1 and its intermediates are provided.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• C07D 277/36 - Sulfur atoms
• A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
• A61K 31/426 - 1,3-Thiazoles
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

A process for preparation of 1-[[[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl]sulfonyl]pyrrolidine of Formula (1), which is commonly known as Almotriptan, and its pharmaceutically acceptable salts is provided. The required purity of almotriptan malate free of impurities is attained in three different ways, including by preparing the acid addition salts of amino indole compound, by proceeding through the almotriptan succinate and by specific purification of almotriptan malate from a suitable solvent.

IPC Classes  ?

• C07D 209/16 - Tryptamines
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/40 - 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
• A61P 25/06 - Antimigraine agents

Abstract

An improved process for the preparation of proton pump inhibitors, such as 2-[(R)-[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole and pharmaceutically acceptable salts thereof is disclosed. The process involves protecting lansoprazole sulphide with D (+)-camphor sulphonyl chloride, followed by stereo selective oxidation using meta-chloroperbenzoic acid to obtain the camphor sulphonyl protected sulfoxide derivative, and stereo dexlansoprazole with high enantiomeric excess is prepared through deprotection of the camphor sulphonyl protected sulfoxide derivative.

IPC Classes  ?

• 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
• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof

Abstract

Processes for preparing pravastatin, intermediates and pharmaceutically acceptable salts thereof are provided Crystalline forms of pravastatin, intermediates and pharmaceutically acceptable salts thereof are also disclosed.

IPC Classes  ?

• C07D 215/12 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
• C07D 215/14 - Radicals substituted by oxygen atoms

Abstract

An improved process for the preparation of nebivolol and its pharmaceutically acceptable salts is disclosed Concretely, the process involves a) esterifying 6-fluoro-3,4-dihydro-2H-l-benzopyran-2-carboxylic acid to provide alkyl 6-fluoro-3,4-dihydro-2H-l-benzopyran-2-carboxylate, b) reducing the alkyl 6-fluoro-3,4-dihydro-2H-l-benzopyran-2-carboxylate to provide 6-fluoro-3,4-dihydro-2H-l-benzopyran-2-carboxaldehyde, which is subsequently converted to 6-fluoro-3,4-dihydro-2-oxiranyl-2H-l-benzopyran, c) reacting 6-fluoro-3,4-dihydro-2-oxiranyl-2H-l-benzopyran with benzyl amine in a suitable solvent followed by treatment with suitable organic acid, and recrystalhzing the obtained compound to provide the corresponding organic acid salt of benzyl protected nebivolol, d) debenzylating the benzyl protected nebivolol salt, followed by treatment with hydrochloric acid to provide nebivolol hydrochloride

IPC Classes  ?

• C07D 311/58 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulfur atoms in position 2 or 4
• C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 311/02 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
• C07D 407/02 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings
• C07D 407/00 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group

Abstract

The present invention relates to improved processes for the preparation of Endothelin receptor antagonists, their salts and intermediates.

IPC Classes  ?

• C07D 239/34 - One oxygen atom

Abstract

The present invention relates to a novel process for the preparation of paliperidone and its intermediates and also relates to an improved process for the preparation of paliperidone compound of formula (I).

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems

Abstract

The present invention relates to an improved process for the preparation of solifenacin compound of formula (1) and its succinate salt compound of formula (1a), comprising the condensation of (R)-3- quinuclidinol with (S)-ethyl- 1 -phenyl- 1,2,3,4-tetrahydro-2-isoquinoline carboxylate in presence of a suitable hydroxide base in a suitable solvent.

IPC Classes  ?

• C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems

Abstract

The present invention relates to an improved process for the preparation of aprepitant compound of formula- (I) as well as novel polymorphs of its intermediates.

IPC Classes  ?

• 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
• C07D 265/32 - 1,4-OxazinesHydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms

Abstract

The present invention relates to an improved and novel process for the preparation of bosentan compound of formula (1). The present invention also relates to a crystalline form of bosentan and its intermediates.

IPC Classes  ?

• 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

Abstract

The present invention relates to an improved process for the preparation of prasugrel compound of formula- 1 and its pharmaceutically acceptable salts thereof.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems
• C07C 22/08 - Cyclic compounds containing halogen atoms bound to an acyclic carbon atom having unsaturation in the rings containing six-membered aromatic rings containing fluorine
• C07C 25/13 - Monocyclic aromatic halogenated hydrocarbons containing fluorine

Abstract

The present invention provides an improved eco-friendly process for the preparation of memantine hydrochloride compound of formula (1). The present invention also provides one-pot process for the preparation of memantine hydrochloride compound of fomula (1) from 1,3 -dimethyl adamantane without isolating any intermediates.

IPC Classes  ?

• C07C 211/38 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton containing condensed ring systems
• C07C 209/62 - Preparation of compounds containing amino groups bound to a carbon skeleton by cleaving carbon-to-nitrogen, sulfur-to-nitrogen, or phosphorus-to-nitrogen bonds, e.g. hydrolysis of amides, N-dealkylation of amines or quaternary ammonium compounds

Abstract

The present invention relates to a novel process for the preparation of moxifloxacin hydrochloride compound of formula-1 through novel quinoline carboxamide intermediate compounds of general formula-2. The present invention provides the process for the preparation of novel quinoline carboxamide intermediate compounds of general formula-2. The present invention also relates to a novel process for the preparation of anhydrous form of moxifloxacin hydrochloride and a novel crystalline form of moxifloxacin.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• C07D 209/00 - Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom

Abstract

The present invention provides an improved process for the preparation of clopidogrel and its pharmaceutically acceptable salts, especially hydrogen chloride and hydrogen bromide by dissolving clopidogrel base in a suitable single or mixture of solvents followed by adding suitable acid and isolating the corresponding acid addition salts of clopidogrel compound of formula-1. Also provides an improved process for the preparation of clopidogrel hydrogen sulfate form-1; Formula (I).

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems

Abstract

The present invention related to an improved process for the preparation of Pantoprazole sodium sesquihydrate comprising the reaction of 5-difluoromethoxy-2-mercapto benzimidazole with 2-chloromethyl-3,4-dimethoxy pyridine hydrochloride in an aqueous alkali, which upon oxidation with sodium hypochlorite having pH of about 8.5-9.0 and assay of about 3.0-3.5 in chloro solvent followed by reaction with sodium hydroxide in acetone. The invention also relates to the process for the preparation of pantoprazole sodium sesquihydrate form-I.

IPC Classes  ?

• 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

Abstract

A process for the preparation of pure Duloxetine hydrochloride comprises the steps of : a) reacting 1-(thiophen-2-yl)ethanone with dimethylamine hydrochloride, b) purifying the component in a solvent, c) reducing the component with an alkali metal borohydride, d) resolving the compound with a chiral acid, and treating the obtained compound with weak inorganic base, e) reacting the compound to give Duloxetine oxalate salt and f) converting the Duloxetine salt into its hydrochloride salt. Further the purifications of the obtained compound and of two intermediate products are described.

IPC Classes  ?

• C07D 333/04 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulfur atom

Abstract

An improved process for the preparation of M&sgr;ntelukast and its pharmaceutically acceptable salts comprises of reacting (S) Benzenepropanol &agr; -⏧3-⏧2-(7-chloro2-quinolinyl) ethenyl]phenyl]-2-(l-hydroxy-1-methyl ethyl)-&agr;-methane sulfonate compound of formula (II) with l-(mercapto methyl) cyclo propane acetic acid or its ester or nitrile in presence of alkali or alkaline carbonates and/or alkali or alkaline earth metal alkoxide in a suitable polar aprotic solvent with or without combination of C1-C4 alcoholic solvents and then treating with organic amine in a suitable ester and/or acetone and/or aliphatic or aromatic hydrocarbon solvents, and converting the corresponding amine salt compound of montelukast into its sodium salt compound of formula (I) using sodium ion source in methanol, without converting into montelukast free acid.

IPC Classes  ?

• C07D 215/18 - Halogen atoms or nitro radicals

Abstract

An improved and industrial process for the preparation of Alfuzosin Hydrochloride and its novel polymorphs (Formula (I)).

IPC Classes  ?

• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links