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公开(公告)号：US20220009865A1
公开(公告)日：2022-01-13
申请号：US17293745
申请日：2019-11-11
申请人： Indena S.P.A.
IPC分类号： C07C37/16
摘要： A process for the synthesis of Cannabidiol of formula (1): (1) is herein disclosed. The process comprises contacting a solution [solution (S1)] of (+)-p-mentha-diene-3-ol of formula (4) (4) or an ester thereof and olivetol of formula (3): (3) with a solution [solution (S2)] of a non-supported Lewis acid in a continuous flow reactor and treatment of the resulting mixture with a basic solution. The process offers the advantage that it can be conveniently carried out on an industrial scale while avoiding the formation of abnormal CBD and THC (Δ9-tetrahydrocannabinol).
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公开(公告)号：US12077484B2
公开(公告)日：2024-09-03
申请号：US18320326
申请日：2023-05-19
申请人： Indena S.P.A.
IPC分类号： C07C227/20
CPC分类号： C07C227/20
摘要： The invention relates to a process for the preparation of Melphalan (4-[bis(2-chloroethyl)amino]-L-phenylalanine of formula (I)
said process comprising the reaction of a 4-amino-L-phenylalanine protected at the carboxy and amino aminoacidic groups with an agent able to convert the aromatic amino group into a group of formula: —N(CH2CH2OS(O)nO−)2, wherein n is 1 or 2 followed by conversion of the —N(CH2CH2OS(O)nO−)2 group into a —N(CH2CH2Cl)2 group.
The invention also provides novel intermediates useful for the preparation of Melphalan.-
公开(公告)号：US20230286901A1
公开(公告)日：2023-09-14
申请号：US18320326
申请日：2023-05-19
申请人： Indena S.P.A.
IPC分类号： C07C227/20
CPC分类号： C07C227/20
摘要： The invention relates to a process for the preparation of Melphalan (4-[bis(2-chloroethyl)amino]-L-phenylalanine of formula (I)
said process comprising the reaction of a 4-amino-L-phenylalanine protected at the carboxy and amino aminoacidic groups with an agent able to convert the aromatic amino group into a group of formula: —N(CH2CH2OS(O)nO−)2, wherein n is 1 or 2 followed by conversion of the —N(CH2CH2OS(O)nO−)2 group into a —N(CH2CH2Cl)2 group.
The invention also provides novel intermediates useful for the preparation of Melphalan.-
公开(公告)号：US20230094970A1
公开(公告)日：2023-03-30
申请号：US17757830
申请日：2020-12-21
申请人： Indena S.P.A.
IPC分类号： C07C227/20
摘要： The invention relates to a process for the preparation of Melphalan (4-[bis(2-5 chloroethyl)amino]-L-phenylalanine of formula (I) said process comprising the reaction of a 4-amino-L-phenylalanine protected at the carboxy and amino aminoacidic groups with an agent able to convert the aromatic amino group into a group of formula: —N(CH2CH2OS(O)nO—)2, wherein n is 1 or 2 followed by conversion of the →N(CH2CH2OS(O)nO—)2 group into a —N(CH2CH2Cl)2 group. The invention also provides novel intermediates useful for the preparation of Melphalan.
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公开(公告)号：US20190256473A1
公开(公告)日：2019-08-22
申请号：US16334027
申请日：2017-09-15
申请人： Indena S.P.A.
发明人： Nicola Sardone , Stefano Luca Giaffreda , Andrea Gambini , Alex Petrolati , Pietro Allegrini , Enrico Modena
IPC分类号： C07D215/48
摘要： The present invention provides novel crystalline forms of 4-[3-Chloro-4-(N′-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide methanesulfonate, as well as methods for their preparation.
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公开(公告)号：US20230398134A1
公开(公告)日：2023-12-14
申请号：US18252067
申请日：2021-11-12
申请人： INDENA S.P.A.
发明人： Pietro Allegrini , Massimo Ronchi , Antonella Riva
CPC分类号： A61K31/658 , A61K9/1652 , A61K9/10
摘要： The present invention relates to a composition comprising cannabidiol and at least two excipients, wherein at least one excipient is a lipid excipient and wherein at least one excipient is a hydrophilic excipient, and wherein the lipid excipient is present in an amount equal to or lower than 20% of the total weight of the composition; the invention also relates to the preparation process of the composition and to pharmaceutical or nutraceutical formulations containing it.
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公开(公告)号：US11787761B2
公开(公告)日：2023-10-17
申请号：US17757830
申请日：2020-12-21
申请人： Indena S.P.A.
IPC分类号： C07C227/20
CPC分类号： C07C227/20
摘要： The invention relates to a process for the preparation of Melphalan (4-[bis(2-5 chloroethyl)amino]-L-phenylalanine of formula (I) said process comprising the reaction of a 4-amino-L-phenylalanine protected at the carboxy and amino aminoacidic groups with an agent able to convert the aromatic amino group into a group of formula: —N(CH2CH2OS(O)nO—)2, wherein n is 1 or 2 followed by conversion of the →N(CH2CH2OS(O)nO—)2 group into a —N(CH2CH2Cl)2 group. The invention also provides novel intermediates useful for the preparation of Melphalan.
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公开(公告)号：US20230227873A1
公开(公告)日：2023-07-20
申请号：US18001741
申请日：2021-06-14
申请人： Indena S.P.A.
IPC分类号： C12P15/00 , C12N9/24 , C07C233/32
CPC分类号： C12P15/00 , C12N9/2402 , C12Y302/01021 , C07C233/32
摘要： The invention relates to a process for the preparation of colchicine 1 from colchicoside 2 which comprises enzymatic conversion of colchicoside 2 to 3-O-demethylcolchicine 3, wherein the enzyme used is a cellulase. According to another aspect of the invention, 3-O-demethylcolchicine 3 can be converted to colchicine 1 using an alkylating agent. The invention also relates to a process or enriching the colchicine 1 content of extracts from plants belonging to the Colchicaceae family containing colchicine 1, colchicoside 2 and 3-(9-demethyl colchicine 3, which comprises conversion by means of a colchicoside 2 cellulase to 3-O-demethylcolchicine 3, followed by conversion of 3-O-demethylcolchicine 3 to colchicine 1 using an alkylating agent.
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公开(公告)号：US20220387361A1
公开(公告)日：2022-12-08
申请号：US17755720
申请日：2020-10-30
申请人： Indena S.P.A.
发明人： Pietro Allegrini , Daniele Ciceri , Lorenzo Menna
摘要： The present invention relates to solid dispersions comprising a salt of ursolic acid with an alkali metal and a phospholipid and to oral dosage formulations containing them. The invention also relates to processes for preparing the solid dispersions and to the use of the solid dispersions and formulations for the prevention and/or treatment of a variety of pathological conditions in which hepatoprotective, antioxidant, anti-inflammatory, antiviral and cytotoxic activities are desired.
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公开(公告)号：US11214543B2
公开(公告)日：2022-01-04
申请号：US17273740
申请日：2019-09-03
申请人： Indena S.P.A.
发明人： Luca Senaldi , Pietro Allegrini , Daniele Ciceri , Anna Bernardi
IPC分类号： C07D215/233
摘要： The present invention relates to a process for the preparation of Lenvatinib of formula (I) from 4-amino-3-chloro-phenol and 4-chloro-7-methoxyquinoline-6-carboxamide.
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