Siegfried AG

Switzerland

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Date
2026 February 2
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IPC Class
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 6
C07D 489/08 - Oxygen atom 5
C07D 489/12 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms 4
A61K 31/465 - NicotineDerivatives thereof 3
A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine 3
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Status
Pending 2
Registered / In Force 32
Found results for  patents

1.

COMPOSITION COMPRISING NICOTINE, CORRESPONDING METHOD AND USE

      
Application Number EP2025071681
Publication Number 2026/027480
Status In Force
Filing Date 2025-07-28
Publication Date 2026-02-05
Owner
  • SIEGFRIED AG (Switzerland)
  • CONTRAF-NICOTEX-TOBACCO GMBH (Germany)
Inventor
  • Van Vegten, Cornelis
  • Artho, Nina

Abstract

The invention relates to a composition comprising or consisting of nicotine and water. The invention also relates to a method of preparing an article comprising the step of contacting nicotine and water to give a corresponding composition. The invention further relates to the use of a corresponding composition to stabilize nicotine. Moreover, the invention relates to the use of a corresponding composition as an intermediate product in the manufacture of an article.

IPC Classes  ?

  • A23G 4/06 - Chewing gum characterised by the composition
  • A24B 15/167 - Chemical features of tobacco products or tobacco substitutes of tobacco substitutes in liquid or vaporisable form, e.g. liquid compositions for electronic cigarettes
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/06 - OintmentsBases therefor
  • A61K 31/465 - NicotineDerivatives thereof
  • A61K 9/70 - Web, sheet or filament bases
  • A61K 9/68 - Medicinal preparations characterised by special physical form chewing gum type
  • A61K 47/02 - Inorganic compounds
  • A61K 31/00 - Medicinal preparations containing organic active ingredients
  • A24B 13/00 - Tobacco for pipes, for cigars, e.g. cigar inserts, or for cigarettesChewing tobaccoSnuff

2.

CRYSTALLINE NALOXONE-DIMETHYLFORMAMIDE SOLVATE, METHODS FOR ITS PREPARATION AND ITS USE AS A REAGENT IN A METHOD OF MAKING NALOXONE

      
Application Number EP2025071944
Publication Number 2026/027618
Status In Force
Filing Date 2025-07-30
Publication Date 2026-02-05
Owner SIEGFRIED AG (Switzerland)
Inventor Petzold, Daniel

Abstract

Described herein is a crystalline naloxone-dimethylformamide solvate and methods of making a first and a second amount thereof, as well as methods of making naloxone or a naloxone salt, involving said crystalline naloxone-dimethylformamide solvate. Further described herein is the use of dimethylformamide for preparing said crystalline naloxone-dimethylformamide solvate and the use of said crystalline naloxone-dimethylformamide solvate as a reagent for i.a. purifying naloxone. Moreover, it is described a crystalline naloxone, a use thereof and a method of making it, as well as a mixture comprising dimethylformamide and said crystalline naloxone-dimethylformamide solvate.

IPC Classes  ?

  • C07D 489/08 - Oxygen atom
  • C07C 233/03 - 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 hydrogen atoms
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61K 31/00 - Medicinal preparations containing organic active ingredients

3.

METHOD OF MAKING CHEMICAL COMPOUNDS USEFUL FOR THE SYNTHESIS OF BUPRENORPHINE

      
Application Number EP2025056192
Publication Number 2025/186408
Status In Force
Filing Date 2025-03-06
Publication Date 2025-09-11
Owner SIEGFRIED AG (Switzerland)
Inventor
  • Debnar, Thomas
  • Petzold, Daniel

Abstract

Described herein is a method of making chemical compounds useful in pharmaceutical syntheses, e.g. chemical compounds useful as intermediates in or final products of such syntheses, and in particular a method of making chemical compounds useful for the synthesis of buprenorphine, including buprenorphine. In one preferred variant, it is described herein a method of making buprenorphine from oripavine.

IPC Classes  ?

  • C07D 489/12 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms

4.

Chiral Synthesis of Nornicotine and Nicotine

      
Application Number 19029517
Status Pending
Filing Date 2025-01-17
First Publication Date 2025-05-22
Owner
  • SIEGFRIED AG (Switzerland)
  • CONTRAF-NICOTEX-TOBACCO GMBH (Germany)
Inventor
  • Straková, Karolína
  • Müller, Dominik Simon
  • Van Vegten, Cornelis Hendrik
  • Zeller, Florian Daniel
  • Debnar, Thomas

Abstract

The present invention relates to a method of producing nornicotine through enantioselective hydrosilylation of myosmine and a composition produced thereby, as well as a composition comprising nornicotine and a catalyst, wherein the catalyst is an organic chiral Lewis base, and a catalyst. The present invention also relates to a method of producing nicotine or a salt thereof from myosmine through enantioselective hydrosilylation of myosmine to nornicotine and further reacting the nornicotine to nicotine or a salt thereof, and a composition produced thereby, as well as a composition comprising nicotine, or a salt thereof, and a catalyst, wherein the catalyst.

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

5.

METHOD OF PURIFYING CANNABINOID COMPONENTS FROM PLANT EXTRACTS

      
Application Number EP2024053783
Publication Number 2024/193910
Status In Force
Filing Date 2024-02-15
Publication Date 2024-09-26
Owner
  • SIEGFRIED AG (Switzerland)
  • CONTRAF-NICOTEX-TOBACCO GMBH (Germany)
Inventor
  • Van Vegten, Cornelis Hendrik
  • Wirz, Yannick

Abstract

The invention provides a new and effective way to isolate and purify organic compounds from hemp and/or another plant from the Cannabaceae family and/or a part of the plant.

IPC Classes  ?

6.

PROCESS FOR THE SYNTHESIS OF 1,3-DIHYDRO-IMIDAZO[4,5-B]PYRIDIN-2-ONE AND/OR DERIVATIVES THEREOF

      
Application Number 18286964
Status Pending
Filing Date 2022-04-07
First Publication Date 2024-06-27
Owner SIEGFRIED AG (Switzerland)
Inventor
  • Weber, Beat Theodor
  • Huang, Fuping
  • Cheng, Mounuo
  • Cao, Chunli

Abstract

The present invention relates to a novel method of producing a compound of Formula (I) from a compound of formula (II) by a novel cyclisation process, as well as a method of producing an acid adduct of the compound of Formula (I) wherein L represents a leaving group, and R represents hydrogen, a substituted or unsubstituted linear, branched and/or cyclic alkyl group that may contain one or more hetero atoms in the linear, branched and/or cyclic alkyl chain, a substituted or unsubstituted aromatic or heteroaromatic group, a substituted or unsubstituted linear, branched and/or cyclic aralkyl or heteroaromatic alkyl group that may contain one or more hetero atoms in the linear, branched and/or cyclic alkanediyl chain, or a substituted or unsubstituted alkylaryl or alkyl heteroaromatic group with at least one linear, branched and/or cyclic alkyl residue that may contain one or more hetero atoms in the linear, branched and/or cyclic alkyl chain. The present invention relates to a novel method of producing a compound of Formula (I) from a compound of formula (II) by a novel cyclisation process, as well as a method of producing an acid adduct of the compound of Formula (I) wherein L represents a leaving group, and R represents hydrogen, a substituted or unsubstituted linear, branched and/or cyclic alkyl group that may contain one or more hetero atoms in the linear, branched and/or cyclic alkyl chain, a substituted or unsubstituted aromatic or heteroaromatic group, a substituted or unsubstituted linear, branched and/or cyclic aralkyl or heteroaromatic alkyl group that may contain one or more hetero atoms in the linear, branched and/or cyclic alkanediyl chain, or a substituted or unsubstituted alkylaryl or alkyl heteroaromatic group with at least one linear, branched and/or cyclic alkyl residue that may contain one or more hetero atoms in the linear, branched and/or cyclic alkyl chain.

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • B01J 27/055 - Sulfates with alkali metals, copper, gold or silver
  • B01J 27/122 - Halides of copper
  • B01J 31/02 - Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides

7.

CHIRAL SYNTHESIS OF NORNICOTINE AND NICOTINE

      
Application Number EP2023073883
Publication Number 2024/047152
Status In Force
Filing Date 2023-08-31
Publication Date 2024-03-07
Owner
  • SIEGFRIED AG (Switzerland)
  • CONTRAF-NICOTEX-TOBACCO GMBH (Germany)
Inventor
  • Straková, Karolína
  • Müller, Dominik Simon
  • Van Vegten, Cornelis Hendrik
  • Zeller, Florian Daniel
  • Debnar, Thomas

Abstract

The present invention relates to a method of producing nornicotine through enantioselective hydrosilylation of myosmine and a composition produced thereby, as well as a composition comprising nornicotine and a catalyst, wherein the catalyst is an organic chiral Lewis base, and a catalyst. The present invention also relates to a method of producing nicotine or a salt thereof from myosmine through enantioselective hydrosilylation of myosmine to nornicotine and further reacting the nornicotine to nicotine or a salt thereof, and a composition produced thereby, as well as a composition comprising nicotine, or a salt thereof, and a catalyst, wherein the catalyst is an organic chiral Lewis base.

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
  • C07D 401/06 - 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 carbon chain containing only aliphatic carbon atoms
  • C07D 403/06 - 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 only aliphatic carbon atoms

8.

PROCESS FOR THE SYNTHESIS OF 1,3-DIHYDRO-IMIDAZO[4,5-B]PYRIDIN-2-ONE AND/OR DERIVATIVES THEREOF

      
Application Number EP2022059248
Publication Number 2022/218811
Status In Force
Filing Date 2022-04-07
Publication Date 2022-10-20
Owner SIEGFRIED AG (Switzerland)
Inventor
  • Weber, Beat Theodor
  • Huang, Fuping
  • Cheng, Mounuo
  • Cao, Chunli

Abstract

The present invention relates to a novel method of producing a compound of Formula (I) from a compound of formula (II) by a novel cyclisation process, as well as a method of producing an acid adduct of the compound of Formula (I) wherein L represents a leaving group, and R represents hydrogen, a substituted or unsubstituted linear, branched and/or cyclic alkyl group that may contain one or more hetero atoms in the linear, branched and/or cyclic alkyl chain, a substituted or unsubstituted aromatic or heteroaromatic group, a substituted or unsubstituted linear, branched and/or cyclic aralkyl or heteroaromatic alkyl group that may contain one or more hetero atoms in the linear, branched and/or cyclic alkanediyl chain, or a substituted or unsubstituted alkylaryl or alkyl heteroaromatic group with at least one linear, branched and/or cyclic alkyl residue that may contain one or more hetero atoms in the linear, branched and/or cyclic alkyl chain.

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • B01J 23/00 - Catalysts comprising metals or metal oxides or hydroxides, not provided for in group

9.

Synthesis of mono-chlorinated acetophenone

      
Application Number 16954822
Grant Number 11104630
Status In Force
Filing Date 2018-12-14
First Publication Date 2021-04-15
Grant Date 2021-08-31
Owner SIEGFRIED AG (Switzerland)
Inventor
  • Ott-Dombrowski, Silvia
  • Rüter, Henning
  • Ulrich, Reto
  • Zumpe, Franz

Abstract

The present invention relates to the improved synthesis of chlorinated acetophenones (CAP) of formula (I). Particularly, the invention shows a way how to reduce the use of chlorinated solvents and the formation of chlorinated volatile by-products in the synthesis.

IPC Classes  ?

  • C07C 45/63 - 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 halogenPreparation 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 substitution of halogen atoms by other halogen atoms
  • 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 49/80 - Ketones containing a keto group bound to a six-membered aromatic ring containing halogen
  • 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

10.

Synthesis of noroxymorphone

      
Application Number 16769099
Grant Number 10927122
Status In Force
Filing Date 2018-11-29
First Publication Date 2020-12-10
Grant Date 2021-02-23
Owner SIEGFRIED AG (Switzerland)
Inventor
  • Santandrea, Ernesto
  • Weber, Beat Theodor
  • Boudier, Andreas
  • Geiseler, Oliver
  • Jeger, Patrick

Abstract

The present invention relates to the improved synthesis of noroxymorphone of formula (III). Particularly, the invention shows a way how to reduce the impurity level in the product avoiding lengthy purification steps.

IPC Classes  ?

11.

Enantiomeric separation of racemic nicotine by addition of an O,O″-disubstituted tartaric acid enantiomer

      
Application Number 16956964
Grant Number 11279685
Status In Force
Filing Date 2018-12-18
First Publication Date 2020-10-22
Grant Date 2022-03-22
Owner
  • SIEGFRIED AG (Switzerland)
  • CONTRAF-NICOTEX-TOBACCO GMBH (Germany)
Inventor
  • Weber, Beat Theodor
  • Pan, Ben

Abstract

The present invention relates to a method of separating racemic nicotine of Formula (1-a) as a mixture of the (R)- and (S)-enantiomers into the enantiomerically pure (S)- and (R)-nicotine represented by Formula (1-b) and (1-c), by adding a mixture of the L- and the D-enantiomer of a O,O′-disubstituted tartaric acid, wherein the molar ratio of the L- to the D-enantiomer is from 80:20 to 95:5, and obtaining the (S)-nicotine of formula (1-b), or by adding O,O′-dibenzoyl-D-tartaric acid and obtaining the (R)-nicotine of formula (1-c).

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

12.

Preparation of racemic nicotine by reaction of ethyl nicotinate with N-vinylpyrrolidone in the presence of an alcoholate base and subsequent process steps

      
Application Number 16957006
Grant Number 11407730
Status In Force
Filing Date 2018-12-18
First Publication Date 2020-10-22
Grant Date 2022-08-09
Owner
  • Siegfried AG (Switzerland)
  • Contraf-Nicotex-Tobacco GmbH (Germany)
Inventor
  • Weber, Beat Theodor
  • Lothschütz, Christian
  • Pan, Ben

Abstract

The present invention relates to a method of preparing racemic nicotine comprising: (i) reacting ethyl nicotinate and N-vinylpyrrolidone in the presence of an alcoholate base to 3-nicotinoyl-1-vinylpyrrolidin-2-one; (ii) reacting the 3-nicotinoyl-1-vinylpyrrolidin-2-one with an acid to myosmine; (iii) reducing the myosmine to nornicotine using a reducing agent; and (iv) methylating the nornicotine to obtain the racemic nicotine.

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

13.

PREPARATION OF RACEMIC NICOTINE BY REACTION OF ETHYL NICOTINATE WITH N-VINYLPYRROLIDONE IN THE PRESENCE OF AN ALCOHOLATE BASE AND SUBSEQUENT PROCESS STEPS

      
Application Number EP2018085437
Publication Number 2019/121644
Status In Force
Filing Date 2018-12-18
Publication Date 2019-06-27
Owner
  • SIEGFRIED AG (Switzerland)
  • CONTRAF-NICOTEX-TOBACCO GMBH (Germany)
Inventor
  • Weber, Beat
  • Lothschütz, Christian
  • Pan, Ben

Abstract

The present invention relates to a method of preparing racemic nicotine comprising: (i) reacting ethyl nicotinate and N-vinylpyrrolidone in the presence of an alcoholate base to 3-nicotinoyl-1-vinylpyrrolidin-2-one; (ii) reacting the 3-nicotinoyl-1-vinylpyrrolidin-2-one with an acid to myosmine; (iii) reducing the myosmine to nornicotine using a reducing agent; and (iv) methylating the nornicotine to obtain the racemic nicotine.

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
  • A61K 31/465 - NicotineDerivatives thereof
  • A61P 25/34 - Tobacco-abuse

14.

IMPROVED SYNTHESIS OF MONO-CHLORINATED ACETOPHENONE

      
Application Number EP2018084908
Publication Number 2019/121379
Status In Force
Filing Date 2018-12-14
Publication Date 2019-06-27
Owner SIEGFRIED AG (Switzerland)
Inventor
  • Ott-Dombrowski, Silvia
  • Rüter, Henning
  • Ulrich, Reto
  • Zumpe, Franz

Abstract

The present invention relates to the improved synthesis of chlorinated acetophenones (CAP) of formula (I). Particularly, the invention shows a way how to reduce the use of chlorinated solvents and the formation of chlorinated volatile by-products in the synthesis.

IPC Classes  ?

  • 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 45/63 - 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 halogenPreparation 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 substitution of halogen atoms by other halogen atoms
  • C07C 49/233 - Unsaturated compounds containing keto groups bound to acyclic carbon atoms containing halogen containing six-membered aromatic rings

15.

ENANTIOMERIC SEPARATION OF RACEMIC NICOTINE BY ADDITION OF AN O,O'-DISUBSTITUTED TARTARIC ACID ENANTIOMER

      
Application Number EP2018085444
Publication Number 2019/121649
Status In Force
Filing Date 2018-12-18
Publication Date 2019-06-27
Owner
  • SIEGFRIED AG (Switzerland)
  • CONTRAF-NICOTEX-TOBACCO GMBH (Germany)
Inventor
  • Weber, Beat
  • Pan, Ben

Abstract

The present invention relates to a method of separating racemic nicotine of Formula (l-a) as a mixture of the (R)- and (S)-enantiomers into the enantiomerically pure (S)- and (R)-nicotine represented by Formula (l-b) and (l-c), by adding a mixture of the L- and the D-enantiomer of a O,O'-disubstituted tartaric acid, wherein the molar ratio of the L- to the D-enantiomer is from 80:20 to 95:5, and obtaining the (S)-nicotine of formula (l-b), or by adding O,O'-dibenzoyl-D-tartaric acid and obtaining the (R)-nicotine of formula (l-c).

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
  • A61K 31/465 - NicotineDerivatives thereof
  • A61P 25/34 - Tobacco-abuse

16.

SYNTHESIS OF NOROXYMORPHONE

      
Application Number EP2018082986
Publication Number 2019/110413
Status In Force
Filing Date 2018-11-29
Publication Date 2019-06-13
Owner SIEGFRIED AG (Switzerland)
Inventor
  • Boudier, Andreas
  • Geiseler, Oliver
  • Jeger, Patrick
  • Weber, Beat
  • Santandrea, Ernesto

Abstract

The present invention relates to the improved synthesis of noroxymorphone of formula (III). Particularly, the invention shows a way how to reduce the impurity level in the product avoiding lengthy purification steps.

IPC Classes  ?

17.

Method of manufacturing stereoisomers of buprenorphine and analogues thereof

      
Application Number 15557311
Grant Number 10035807
Status In Force
Filing Date 2016-03-11
First Publication Date 2018-02-22
Grant Date 2018-07-31
Owner SIEGFRIED AG (Switzerland)
Inventor
  • Sahli, Stefan
  • Weber, Beat Theodor

Abstract

I represents hydrogen or a linear, branched and/or cyclic alkyl or alkenyl group having 1 to 10 carbon atoms; II are different from each other.

IPC Classes  ?

  • C07D 489/12 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms

18.

SUPPORTED METAL CATALYST FOR THE PRODUCTION OF HYDROCODONE AND HYDROMORPHONE

      
Application Number EP2017063808
Publication Number 2017/211879
Status In Force
Filing Date 2017-06-07
Publication Date 2017-12-14
Owner SIEGFRIED AG (Switzerland)
Inventor
  • Spälti, Michael
  • Weber, Beat

Abstract

The present invention relates to the process for the manufacture of hydrocodone or hydromorphone from their enol derivatives codeine and morphine respectively. Particularly, the invention discloses a metal catalyst that is used in low amount, leads to high yields and can easily be reused.

IPC Classes  ?

  • C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone

19.

Method of manufacturing buprenorphine and analogues thereof from oripavine

      
Application Number 15527540
Grant Number 10391091
Status In Force
Filing Date 2015-10-13
First Publication Date 2017-11-09
Grant Date 2019-08-27
Owner Siegfried AG (Switzerland)
Inventor
  • Weber, Beat Theodor
  • Roux, Lionel

Abstract

The invention relates to an improved method of preparing buprenorphine, a salt thereof, analogs of buprenorphine and their salts. In particular, the invention relates to a method of preparing buprenorphine and related products and salts in economic and ecologic ways having increased yields.

IPC Classes  ?

  • C07D 489/12 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine

20.

PROCESS FOR THE PREPARATION OF TRANS-4-AMINO-1-CYCLOHEXANECARBOXILIC ACID AND ITS DERIVATIVES

      
Application Number EP2017052361
Publication Number 2017/134212
Status In Force
Filing Date 2017-02-03
Publication Date 2017-08-10
Owner SIEGFRIED AG (Switzerland)
Inventor
  • Weber, Beat
  • Jacek, Olma
  • Brysz, Michal
  • Lukaszewicz, Ewa

Abstract

The present invention relates to a one-pot process for the preparation of trans-4-amino-l-cyclohexanecarboxylic acid derivatives where the trans ratio is more than 75% by reaction of a 4-aminobenzoic acid derivative using an appropriate catayst and an appropriate solvent or solvent mixture under basic conditions. The process uses low hydrogen pressure and is therefore suitable for industrial application.

IPC Classes  ?

  • C07C 227/32 - Preparation of optical isomers by stereospecific synthesis
  • C07C 229/48 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups and carboxyl groups bound to carbon atoms of the same non-condensed ring

21.

TILIDINE ISOMERIZATION AND CRYSTALLIZATION PROCESS

      
Application Number EP2016068534
Publication Number 2017/021445
Status In Force
Filing Date 2016-08-03
Publication Date 2017-02-09
Owner SIEGFRIED AG (Switzerland)
Inventor
  • Bahr, Nicolaus
  • Schäfer, Bernd
  • Siegel, Wolfgang

Abstract

Tilidine isomerization and crystallization process, comprising providing a reaction mixture comprising cis-tilidine, a dicarboxylic acid, water and an alcohol having 3 to 6 carbon atoms; maintaining the reaction mixture at a temperature T of from 80 °C to 150 °C at specific conditions of time and temperature; removing water from the reaction mixture and crystallizing a trans-tilidine dicarboxylic acid salt from the reaction mixture. The process allows for an efficient integration of isomerization and separation and yields trans-tilidine in a form that is essentially free of side products which are difficult to separate.

IPC Classes  ?

  • C07C 227/36 - Racemisation of optical isomers
  • C07C 229/48 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups and carboxyl groups bound to carbon atoms of the same non-condensed ring

22.

Mesoporous dosage forms for poorly soluble drugs

      
Application Number 15034055
Grant Number 10034883
Status In Force
Filing Date 2014-11-06
First Publication Date 2016-09-15
Grant Date 2018-07-31
Owner SIEGFRIED AG (Switzerland)
Inventor Prinderre, Pascal

Abstract

The present invention is directed to a new pharmaceutical dosage form comprising mesoporous particles loaded with a poorly soluble active pharmaceutical ingredient, the particles being at least partially, preferably homogeneously, covered with a polymer solid dispersion.

IPC Classes  ?

  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • A61K 9/14 - Particulate form, e.g. powders
  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid

23.

METHOD OF MANUFACTURING STEREOISOMERS OF BUPRENORPHINE AND ANALOGUES THEREOF

      
Application Number EP2016055249
Publication Number 2016/142506
Status In Force
Filing Date 2016-03-11
Publication Date 2016-09-15
Owner SIEGFRIED AG (Switzerland)
Inventor
  • Sahli, Stefan
  • Weber, Beat Theodor

Abstract

The present invention relates to a method of preparing a compound of Formula II-a' or Formula II-b', wherein RI represents hydrogen or a linear, branched and/or cyclic alkyl or alkenyl group having 1 to 10 carbon atoms; RII represents a linear, branched and/or cyclic alkyl or alkenyl group having 1 to 10 carbon atoms; RIII represents hydrogen or a linear, branched and/or cyclic alkyl or alkenyl group having 1 to 10 carbon atoms or a linear, branched and/or cyclic alkoxy group having 1 to 10 carbon atoms; RIV represents hydrogen or a linear, branched and/or cyclic alkyl group having 1 to 10 carbon atoms or an optionally substituted aryl or alkylaryl group having 6 to 40 carbon atom or acetyl or silyl or a protective group; and RV represents hydrogen or a methyl group; wherein RI and RII are differentfrom each other.

IPC Classes  ?

  • C07D 489/09 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems

24.

Synthesis of noroxymorphone from morphine

      
Application Number 14908064
Grant Number 09546177
Status In Force
Filing Date 2014-07-22
First Publication Date 2016-06-09
Grant Date 2017-01-17
Owner SIEGRIED AG (Switzerland)
Inventor
  • Weber, Beat Theodor
  • Hochstrasser, Lisa

Abstract

The present invention is directed to an improved process to convert morphine into noroxymorphone having economic and ecological advantages.

IPC Classes  ?

  • C07D 489/08 - Oxygen atom
  • C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone

25.

IMPROVED METHOD OF MANUFACTURING BUPRENORPHINE AND ANALOGUES THEREOF FROM ORIPAVINE

      
Application Number EP2015073646
Publication Number 2016/078833
Status In Force
Filing Date 2015-10-13
Publication Date 2016-05-26
Owner SIEGFRIED AG (Switzerland)
Inventor
  • Dr. Weber, Beat Theodor
  • Roux, Lionel

Abstract

The invention relates to an improved method of preparing buprenorphine, a salt thereof, analogues of buprenorphine and their salts. In particular, the invention relates to a method of preparing buprenorphine and related products and salts in economic and ecologic ways having increased yields.

IPC Classes  ?

  • C07D 489/12 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms
  • A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
  • A61P 25/36 - Opioid-abuse
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

26.

Oral pharmaceutical formulation

      
Application Number 14889009
Grant Number 10010510
Status In Force
Filing Date 2014-05-06
First Publication Date 2016-03-24
Grant Date 2018-07-03
Owner SIEGFRIED AG (Switzerland)
Inventor Prinderre, Pascal Christian

Abstract

Described herein are oral pharmaceutical formulations comprising a core component and a coating composition applied on the core component. Also described is a process for producing said oral pharmaceutical formulations.

IPC Classes  ?

  • A61K 9/50 - Microcapsules
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
  • A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
  • A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
  • A61K 31/404 - Indoles, e.g. pindolol
  • A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 31/155 - Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (HN=C(OH)NH2), isothiourea (HN=C(SH)—NH2)
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate

27.

MESOPOROUS DOSAGE FORMS FOR POORLY SOLUBLE DRUGS

      
Application Number EP2014073886
Publication Number 2015/067682
Status In Force
Filing Date 2014-11-06
Publication Date 2015-05-14
Owner SIEGFRIED AG (Switzerland)
Inventor Prinderre, Pascal

Abstract

The present invention is directed to a new pharmaceutical dosage form comprising mesoporous particles loaded with a poorly soluble active pharmaceutical ingredient, said particles being at least partially, preferably homogeneously, covered with a polymer solid dispersion.

IPC Classes  ?

  • A61K 9/14 - Particulate form, e.g. powders
  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets

28.

NOVEL SYNTHESIS OF NOROXYMORPHONE FROM MORPHINE

      
Application Number EP2014065703
Publication Number 2015/011131
Status In Force
Filing Date 2014-07-22
Publication Date 2015-01-29
Owner SIEGFRIED AG (Switzerland)
Inventor
  • Weber, Beat Theodor
  • Hochstrasser, Lisa

Abstract

The present invention is directed to an improved process to convert morphine into noroxymorphone comprising the step of reacting a compound of formula (Va) or (Vb) to a compound of formula (VIa) or (VIb), respectively characterized in that the reaction is carried out with hydrogen peroxide and an organic acid, wherein the organic acid and the hydrogen peroxide are mixed and allowed to react for a defined induction time prior to addition to the compound of formula (Va) or (Vb).

IPC Classes  ?

29.

ORAL PHARMACEUTICAL FORMULATION

      
Application Number EP2014059249
Publication Number 2014/180855
Status In Force
Filing Date 2014-05-06
Publication Date 2014-11-13
Owner SIEGFRIED AG (Switzerland)
Inventor Prinderre, Pascal Christian

Abstract

The present invention relates to oral pharmaceutical formulations comprising a core component and a coating composition applied on the core component. The present invention further is directed to a process for producing said oral pharmaceutical formulation.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 9/50 - Microcapsules

30.

METHOD FOR THE PREPARATION OF 1-ARYL-1-ALKYL-2-ALKYL-3-DIALKYLAMINOPROPANE COMPOUNDS

      
Application Number EP2013001761
Publication Number 2013/185928
Status In Force
Filing Date 2013-06-14
Publication Date 2013-12-19
Owner SIEGFRIED AG (Switzerland)
Inventor
  • Cyr, Patrick
  • Crump, Roger
  • Sahli, Stefan
  • Blum, Vinzenz

Abstract

The present invention refers to the preparation of 1-aryl-1-alkyl-2-alkyl-3-dialkylamino-propane compounds, such as tapentadol, using a diastereoselective Eschenmoser-Claisen or Ireland-Claisen rearrangement.

IPC Classes  ?

  • 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 217/62 - 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 not further substituted by singly-bound oxygen atoms 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 235/34 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms

31.

IMPROVED METHOD OF PREPARING OXYMORPHONE

      
Application Number US2013045198
Publication Number 2013/188418
Status In Force
Filing Date 2013-06-11
Publication Date 2013-12-19
Owner SIEGFRIED AG (Switzerland)
Inventor Sun, Jianguang

Abstract

The invention relates to an improved method of preparing oxymorphone or a salt thereof from oripavine. In particular, the invention relates to a method of preparing oxymorphone with a content of alpha-beta- unsaturated ketones (ABUK) < 10 ppm, wherein the content of 8,14-dihydroxydihydromorphinone in the prepared oxymorphone is > 10 ppm.

IPC Classes  ?

  • C07D 489/02 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone

32.

Preparation of low impurity opiates in a continuous flow reactor

      
Application Number 13582334
Grant Number 08921557
Status In Force
Filing Date 2011-03-21
First Publication Date 2013-02-07
Grant Date 2014-12-30
Owner Siegfried AG (Switzerland)
Inventor
  • Weber, Beat
  • Sahli, Stefan

Abstract

The present invention relates to a novel process for preparing opiates or salts thereof. More particularly, the present invention relates to oxidizing the starting material in a continuous flow reactor, followed by either an isolation of the intermediate, or a direct reduction reaction.

IPC Classes  ?

  • C07D 471/00 - 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
  • C07D 491/00 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or
  • C07D 498/00 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
  • C07D 513/00 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups , or
  • C07D 515/00 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups , or
  • C07D 489/00 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
  • C07D 489/08 - Oxygen atom

33.

PROCESS FOR THE PURIFICATION OF 2,6-DIISOPROPYL PHENOL

      
Application Number EP2012058177
Publication Number 2012/152665
Status In Force
Filing Date 2012-05-04
Publication Date 2012-11-15
Owner SIEGFRIED AG (Switzerland)
Inventor
  • Keller, Sarah
  • Schlegel, Jens

Abstract

The present invention relates to a novel process for purifying 2,6-diisopropy! phenol (propofol). More particularly, the present invention relates to chlorinating technical grade propofol into a 4-chloropropofol followed by hydrogenating said 4-chloropropofol into a pure propofol.

IPC Classes  ?

  • C07C 37/86 - SeparationPurificationStabilisationUse of additives by treatment giving rise to a chemical modification
  • C07C 39/06 - Alkylated phenols

34.

PREPARATION OF LOW IMPURITY OPIATES IN A CONTINUOUS FLOW REACTOR

      
Application Number EP2011054193
Publication Number 2011/117172
Status In Force
Filing Date 2011-03-21
Publication Date 2011-09-29
Owner SIEGFRIED AG (Switzerland)
Inventor
  • Weber, Beat
  • Sahli, Stefan

Abstract

The present invention relates to a novel process for preparing opiates or salts thereof. More particularly, the present invention relates to oxidizing the starting material in a continuous flow reactor, followed by either an isolation of the intermediate, or a direct reduction reaction.

IPC Classes  ?