C07D 207/27 - 2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
A61K 31/4015 - 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 having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
C07C 53/19 - Acids containing three or more carbon atoms
C07C 53/50 - Acyl halides containing halogen outside the carbonyl halide group of acids containing three or more carbon atoms
C07C 67/307 - Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by introduction of halogenPreparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by substitution of halogen atoms by other halogen atoms
C07C 69/63 - Halogen-containing esters of saturated acids
C07C 209/08 - Preparation of compounds containing amino groups bound to a carbon skeleton by substitution of functional groups by amino groups by substitution of halogen atoms with formation of amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
C07C 231/14 - Preparation of carboxylic acid amides by formation of carboxamide groups together with reactions not involving the carboxamide groups
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 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
Provided in the present application is a method for synthesizing deucravacitinib. The method comprises: subjecting the compound of formula (I) to chlorination and to electrophilic substitution with the compound of formula (VI) to synthesize the compound of formula (III); then carrying out an amine transesterification reaction on the compound of formula (III) and deuterated methylamine to synthesize the compound of formula (IV); and finally carrying out a coupling reaction on the compound of formula (VII) and the compound of formula (IV) to prepare compound (V). The method for synthesizing a heterocyclic drug intermediate has a simple process, convenient post-treatment, cheap and easily available starting materials, a stable isolated intermediate and easy industrial production.
A process of making Roxadustat of the following formula:
A process of making Roxadustat of the following formula:
A process of making Roxadustat of the following formula:
comprising converting a compound of formula VI:
A process of making Roxadustat of the following formula:
comprising converting a compound of formula VI:
A process of making Roxadustat of the following formula:
comprising converting a compound of formula VI:
to Roxadustat, wherein R is a C1-C20 alkyl group, and PG is a protective group.
The present application relates to crystalline form 04, crystalline form 06, crystalline form D-1, and crystalline form D-2 of an antidepressant drug SAGE-217 and a preparation method therefor and a pharmaceutical composition containing same. The crystalline form 04 has an XRPD pattern with characteristic peaks at 2theta values of 11.6±0.2°, 13.5±0.2°, 16.2±0.2°, 16.5±0.2°, and 23.2±0.2°; the crystalline form 06 has an XRPD pattern with characteristic peaks at 2theta values of 8.7±0.2°, 10.0±0.2°, 13.2±0.2°, 15.0±0.2°, 15.8±0.2°, and 17.3±0.2°; the crystalline form D-1 has an XRPD pattern with characteristic peaks at 2theta values of 7.2±0.2°, 8.6±0.2°, 13.3±0.2°, 19.6±0.2°, and 23.0±0.2°; and the crystalline form D-2 has an XRPD pattern with characteristic peaks at 2theta values of 7.3±0.2°, 8.6±0.2°, 13.4±0.2°, 19.7±0.2°, and 23.3±0.2°. The novel crystalline forms provided by the present application have good stability, and provide more choices for drug development.
C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
5.
Crystalline form of Di-p-toluoyl-L-tartrate of upadacitinib
The present application provides a upadacitinib salt compound and a preparation method therefor. The salt involved in the method in the present application has an easy preparation operation, a cheap raw material easy to get, and a good purification effect on upadacitinib, and is beneficial to industrial production.
C07C 65/21 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups
C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
7.
Synthesis methods for upadacitinib and intermediate thereof
The present disclosure relates to a JAK inhibitor upadacitinib intermediate and a preparation method therefor, and to a preparation method for a JAK inhibitor upadacitinib. The upadacitinib intermediate of the present application is as shown in Formula (II) or Formula (III),
1 is an open-chain or cyclic amine group. Compared with the prior art, the method for the synthesis of upadacitinib of the present application, significantly reduces cost, is environmentally-friendly. And the quality of the final product is well controlled.
C07D 207/08 - 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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
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
The present invention relates to new solid forms (including crystalline and amorphous solids) of relugolix, a compound applied as gonadotropin-releasing hormone (GnRH) receptor antagonist, and a preparation method therefor. The provided crystalline and amorphous solids have good stability and have great significance to purification of active pharmaceutical components and preparation process of medicines.
Disclosed are a synthetic scheme for a Relugolix intermediate and Relugolix. The synthetic scheme efficiently avoids the use of a highly toxic substance, i.e. methyl chloroformate or ethyl chloroformate, and uses other kinds of chloroformates that are low in toxicity and convenient to use. The synthetic scheme can reduce the usage risk in a raw material production process, and is easy to operate, safer in process, and beneficial to industrialized production.
C07D 333/38 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 409/12 - 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 chain containing hetero atoms as chain links
The present invention relates to a method for preparing the compound of formula IV, compound of formula XI, and acalabrutinib, a new generation of bruton tyrosine kinase (BTK) inhibitor.
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
C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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
The present application provides a upadacitinib salt compound and a preparation method therefor. The salt involved in the method in the present application has an easy preparation operation, a cheap raw material easy to get, and a good purification effect on upadacitinib, and is beneficial to industrial production.
The present application relates to crystal form 04, crystal form 06, crystal form D-1, and crystal form D-2 of an antidepressant drug SAGE-217 and a preparation method therefor and a pharmaceutical composition containing same. The XRPD of crystal form 04 has characteristic peaks at 2theta values of 11.6±0.2°, 13.5±0.2°, 16.2±0.2°, 16.5±0.2°, and 23.2±0.2°; the XRPD of crystal form 06 has characteristic peaks at 2theta values of 8.7±0.2°, 10.0±0.2°, 13.2±0.2°, 15.0±0.2°, 15.8±0.2°, and 17.3±0.2°; the XRPD of crystal form D-1 has characteristic peaks at 2theta values of 7.2±0.2°, 8.6±0.2°, 13.3±0.2°, 19.6±0.2°, and 23.0±0.2°; and the XRPD of crystal form D-2 has characteristic peaks at 2theta values of 7.3±0.2°, 8.6±0.2°, 13.4±0.2°, 19.7±0.2°, and 23.3±0.2°. The new crystal forms provided by the present application have good stability, and provide more choices for drug development.
C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
14.
SYNTHESIS METHODS FOR UPADACITINIB AND INTERMEDIATE THEREOF
11 is an open chain or cyclic amine group. Compared with the prior art, the method for synthesising upadacitinib, under the premise of ensuring the yield, significantly reduces costs, is environmentally friendly, and improves the quality of the final product.
C07D 207/04 - 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 no double bonds between ring members or between ring members and non-ring members
C07D 207/27 - 2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
A61K 31/4015 - 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 having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
C07C 53/19 - Acids containing three or more carbon atoms
C07C 53/50 - Acyl halides containing halogen outside the carbonyl halide group of acids containing three or more carbon atoms
C07C 67/307 - Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by introduction of halogenPreparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by substitution of halogen atoms by other halogen atoms
C07C 69/63 - Halogen-containing esters of saturated acids
C07C 209/08 - Preparation of compounds containing amino groups bound to a carbon skeleton by substitution of functional groups by amino groups by substitution of halogen atoms with formation of amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
C07C 231/14 - Preparation of carboxylic acid amides by formation of carboxamide groups together with reactions not involving the carboxamide groups
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 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
17.
VENETOCLAX CRYSTAL FORMS AND PREPARATION METHOD THEREFOR
Venetoclax crystal forms and a preparation method therefor, the structural formula thereof is represented by formula (I), and such crystal forms may be directly obtained from crystallization in a solvent.
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
Novel crystalline forms of trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl) propionate-(S)-3′-methyl-2′-(pentanoyl{2″-(tetrazol-5-ylate)biphenyl-4′-ylmethyl}amino)butyrate] hydrate, methods for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of angiotensin receptor 1 (AT1) blockage and neprilysin (NEP) inhibition, such as heart failure, are disclosed.
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
C07C 233/47 - 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 carboxyl groups 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
C07D 207/27 - 2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
A61K 31/4015 - 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 having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
C07C 53/19 - Acids containing three or more carbon atoms
C07C 53/50 - Acyl halides containing halogen outside the carbonyl halide group of acids containing three or more carbon atoms
C07C 67/307 - Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by introduction of halogenPreparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by substitution of halogen atoms by other halogen atoms
C07C 69/63 - Halogen-containing esters of saturated acids
C07C 209/08 - Preparation of compounds containing amino groups bound to a carbon skeleton by substitution of functional groups by amino groups by substitution of halogen atoms with formation of amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
C07C 231/14 - Preparation of carboxylic acid amides by formation of carboxamide groups together with reactions not involving the carboxamide groups
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 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
20.
Crystalline forms of trisodium supramolecular complex comprising valsartan and AHU-377 and methods thereof
Novel crystalline Forms of trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butyl carbamoyl) propionate-(S)-3′-methyl-T-(pentanoyl{2″-(tetrazol-5-ylate)biphenyl-4′-ylmethyl}amino)butyrate] hydrate, methods for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of angiotensin receptor 1 (AT1) blockage and neprilysin (NEP) inhibition, such as heart failure, are disclosed.
A ketolide antibiotics intermediate, a preparation method therefor, and application thereof in preparation of solithromycin. The ketolide antibiotics intermediate has a compound structural general formula as shown as follows, and can be prepared by using existing raw materials via several simple steps, the reaction operation is simple and convenient, the utilization rates of macrolides pregnant nucleus raw materials and side chain raw materials are high, and the yield is high. When the ketolide antibiotics intermediate is used for compounding of solithromycin, comprehensively compared with the prior art, the purity and the yield are greatly improved, and good practical value is obtained.
Crystalline Form I of ibrutinib, processes for its preparation, pharmaceutical compositions comprising the new Form, and use of Form I of ibrutinib for treating or delaying diseases or disorders related to activity of Bruton's tyrosine kinase (BTK) proteins are disclosed. The novel Form was characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. It can be readily prepared and is suitable for use in the preparation of solid dosage forms.
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 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
C07D 487/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups
A stereoselective process for providing a scalable synthesis of enantiomerically pure brivaracetam compound of formula XII, and related derivatives preparing formula XII, by screening for ligands with a higher affinity for LBS than levetiracetam; the process utilizing novel and inventive chiral compounds as starting material of the process.
A61K 31/4015 - 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 having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
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
A61K 31/4015 - 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 having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
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
Novel salts and cocrystals of lesinurad, processes for their preparation, pharmaceutical compositions comprising these new salt forms and co-crystals, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of uric acid transport 1 (URAT1) proteins are disclosed. These novel forms were characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. They can be readily prepared and are suitable for preparation of solid dosage forms owing to their ease of handling and superior pharmacological properties.
Disclosed are AHU-377 intermediates and a method for preparing AHU-377 and AHU-377 intermediates. The above-mentioned method for preparing AHU-377 uses a chiral glycidyl benzyl ether as the starting raw material. Intermediate compound (3) is produced by an addition reaction with a biphenyl Grignard reagent and a Mitsunobu reaction with a succimide or a phthalimide. Intermediate compound (4) is obtained after the benzyl protection has been removed. Intermediate compound (4) is oxidised to form an aldehyde, and then is reacted with a phosphorus ylide reagent to obtain target intermediate compound (8). Intermediate (9) is obtained under a selective catalytic hydrogenation condition. Target compound (10), i.e. AHU-377, is obtained by the hydrolysis of the single amide bond. The use of an expensive non-natural amino acid raw material tyrosine can be avoided in the method of the present application, and the method has a convenient operation and high safety.
C07C 233/47 - 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 carboxyl groups 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 231/08 - Preparation of carboxylic acid amides from amides by reaction at nitrogen atoms of carboxamide groups
C07C 43/178 - Unsaturated ethers containing hydroxy or O-metal groups
C07C 41/30 - Preparation of ethers by reactions not forming ether-oxygen bonds by increasing the number of carbon atoms, e.g. by oligomerisation
C07C 271/16 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
C07C 269/04 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups from amines with formation of carbamate groups
C07D 207/404 - 2,5-Pyrrolidine-diones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. succinimide
27.
SALTS AND CRYSTALLINE FORMS OF 6-ACETYL-8-CYCLOPENTYL-5-METHYL-2((5-(PIPERAZIN-1-YL)PYRIDIN-2-YL)AMINO)PYRIDO[2,3-D] PYRIMIDIN-7(8H)-ONE (PALBOCICLIB)
New salts and crystalline Forms of palbociclib, processes for their preparation, pharmaceutical compositions comprising the new salts or crystalline Forms, and use of the new salts and crystalline Forms of palbociclib for treating or delaying diseases or disorders related to activity of cyclin-dependent kinase (CDK) 4/6 are disclosed.
A novel crystalline Form of trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3- ethoxycarbonyl-1-butylcarbamoyl)propionate-(S)-3'-methyl-2'-(pentanoyl{2''-(tetrazol-5- ylate)biphenyl-4'-ylmethyl}amino)butyrate] hydrate, process for its preparation, pharmaceutical composition comprising the new form, and use of it for treating or delaying progression or onset of diseases or disorders related to activity of angiotensin receptor 1 (AT1) blockage and neprilysin (NEP) inhibition is disclosed. The novel form was characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques.
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
29.
CRYSTALLINE FORMS OF TRISODIUM SUPRAMOLECULAR COMPLEX COMPRISING VALSARTAN AND AHU-377 AND METHODS THEREOF
Novel crystalline Forms of trisodium [3-((1S,3R)-l-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butyl carbamoyl) propionate-(S)-3'-methyl-2'-(pentanoyl{2"-(tetrazol-5-ylate)biphenyl-4'-ylmethyl}amino)butyrate] hydrate, methods for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of angiotensin receptor 1 (AT1) blockage and neprilysin (NEP) inhibition, such as heart failure, are disclosed.
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
C07C 233/47 - 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 carboxyl groups 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
30.
CRYSTALLINE FORMS OF TRISODIUM SUPRAMOLECULAR COMPLEX COMPRISING VALSARTAN AND AHU-377 AND METHODS THEREOF
Novel crystalline Forms of trisodium [3-((1S,3R)-l-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butyl carbamoyl) propionate-(S)-3'-methyl-2'-(pentanoyl{2"-(tetrazol-5-ylate)biphenyl-4'-ylmethyl}amino)butyrate] hydrate, methods for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of angiotensin receptor 1 (AT1) blockage and neprilysin (NEP) inhibition, such as heart failure, are disclosed.
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
A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
C07C 233/47 - 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 carboxyl groups 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
The present invention relates to a method for preparing an aliphatic phosphate ester having protected hydroxyl with optical activity, which can efficiently synthesize the side chains or precursors of the drug, Treprostinil, for treating pulmonary arterial hypertension. It is a completely new synthetic route and synthetic strategy. The product precursor is obtained by the radical addition reaction of optical active alcohol with a double bond at its terminal, catalyzed by benzoyl peroxide, and the hydroxyl can further be protected by different strategies so as to prepare the target compound; the compound can also be obtained as follows: protecting the hydroxyl at first, and then an addition reaction on the double bond is carried out using a phosphate ester. The aliphatic phosphate ester ester having protected hydroxyl prepared by the present invention can be used for preparing the new drug, Treprostinil, for treating pulmonary arterial hypertension.
Novel salts and cocrystals of lesinurad, processes for their preparation, pharmaceutical compositions comprising these new salt forms and co-crystals, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of uric acid transport 1 (URAT1) proteins are disclosed. These novel forms were characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. They can be readily prepared and are suitable for preparation of solid dosage forms owing to their ease of handling and superior pharmacological properties.
Crystalline Form I of ibrutinib, processes for its preparation, pharmaceutical compositions comprising the new Form, and use of Form I of ibrutinib for treating or delaying diseases or disorders related to activity of Bruton's tyrosine kinase (BTK) proteins are disclosed. The novel Form was characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. It can be readily prepared and is suitable for use in the preparation of solid dosage forms.
Crystalline Form I of ibrutinib, processes for its preparation, pharmaceutical compositions comprising the new Form, and use of Form I of ibrutinib for treating or delaying diseases or disorders related to activity of Bruton's tyrosine kinase (BTK) proteins are disclosed. The novel Form was characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. It can be readily prepared and is suitable for use in the preparation of solid dosage forms.
Novel crystalline forms of lesinurad and its sodium salt, processes for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of uric acid transporter 1 (URAT1) proteins are disclosed. These novel forms were characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. They can be readily prepared and are suitable for preparation of solid dosage forms owing to their ease of handling and superior pharmacological properties.
Provided are a novel Lesinurad intermediate, providing a synthetic process more economical, more efficient, safer, more environmentally friendly, and suitable for large-scale industrial production for the preparation of Lesinurad. Also provided is a method for preparing the known Lesinurad intermediate and Lesinurad via the provided novel Lesinurad intermediate. Using the novel Lesinurad intermediate of the present invention to synthesize Lesinurad has the following advantages of using cheap and easily available required raw materials, avoiding the use of heavy metals and solvents harmful to the environment, easily separating and purifying the intermediate and the product with a simple operation, avoiding the use of the thiophosgene having high toxicity and difficulty of operation, and enabling the total yield of the reaction to reach a level equal to or higher than the prior art.
C07C 335/40 - Thioureas, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of thiourea or isothiourea groups further bound to other hetero atoms
37.
CARFILZOMIB INTERMEDIATE AND PREPARATION METHOD THEREFOR, AND PREPARATION METHOD FOR CARFILZOMIB
Disclosed is a new Carfilzomib intermediate and a preparation method therefor, and a preparation method for Carfilzomib using the intermediate. The Carfilzomib intermediate provided by the invention is easily separated from the isomers thereof, and can be prepared through an epoxidation reaction or a condensation reaction with high selectivity and yield.
C07K 5/117 - Tetrapeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp
C07D 303/36 - Compounds containing oxirane rings with hydrocarbon radicals, substituted by nitrogen atoms
C07C 271/22 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
patents
