BRPI0515470A - processos e intermediários para preparação de inibidores de cisteìna protease - Google Patents
processos e intermediários para preparação de inibidores de cisteìna proteaseInfo
- Publication number
- BRPI0515470A BRPI0515470A BRPI0515470-7A BRPI0515470A BRPI0515470A BR PI0515470 A BRPI0515470 A BR PI0515470A BR PI0515470 A BRPI0515470 A BR PI0515470A BR PI0515470 A BRPI0515470 A BR PI0515470A
- Authority
- BR
- Brazil
- Prior art keywords
- protease inhibitors
- processes
- intermediates
- preparation
- cysteine protease
- Prior art date
Links
- 239000002852 cysteine proteinase inhibitor Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000000543 intermediate Substances 0.000 title 1
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07C323/23—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
- C07C323/24—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
- C07C323/25—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/63—Esters of sulfonic acids
- C07C309/64—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
- C07C309/65—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C315/00—Preparation of sulfones; Preparation of sulfoxides
- C07C315/02—Preparation of sulfones; Preparation of sulfoxides by formation of sulfone or sulfoxide groups by oxidation of sulfides, or by formation of sulfone groups by oxidation of sulfoxides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C315/00—Preparation of sulfones; Preparation of sulfoxides
- C07C315/04—Preparation of sulfones; Preparation of sulfoxides by reactions not involving the formation of sulfone or sulfoxide groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
- C07C317/28—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
- C07C317/48—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C321/00—Thiols, sulfides, hydropolysulfides or polysulfides
- C07C321/12—Sulfides, hydropolysulfides, or polysulfides having thio groups bound to acyclic carbon atoms
- C07C321/16—Sulfides, hydropolysulfides, or polysulfides having thio groups bound to acyclic carbon atoms of a saturated carbon skeleton containing rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
- C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
- C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—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
- C07D213/02—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 having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—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 having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—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 having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
- C07D213/32—Sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—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
- C07D213/02—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 having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—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 having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—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 having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
- C07D213/32—Sulfur atoms
- C07D213/34—Sulfur atoms to which a second hetero atom is attached
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D309/14—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D335/00—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
- C07D335/02—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Enzymes And Modification Thereof (AREA)
- Heterocyclic Compounds Containing Sulfur Atoms (AREA)
- Pyridine Compounds (AREA)
- Pyrane Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US61080604P | 2004-09-17 | 2004-09-17 | |
| PCT/US2005/033051 WO2006034004A2 (en) | 2004-09-17 | 2005-09-16 | Processes and intermediates for preparing cysteine protease inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0515470A true BRPI0515470A (pt) | 2008-07-22 |
Family
ID=35899659
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0515470-7A BRPI0515470A (pt) | 2004-09-17 | 2005-09-16 | processos e intermediários para preparação de inibidores de cisteìna protease |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US7737300B2 (https=) |
| EP (1) | EP1799645A2 (https=) |
| JP (1) | JP2008513472A (https=) |
| KR (1) | KR20070061877A (https=) |
| CN (1) | CN101068783A (https=) |
| AU (1) | AU2005287046A1 (https=) |
| BR (1) | BRPI0515470A (https=) |
| CA (1) | CA2580065A1 (https=) |
| CR (1) | CR8993A (https=) |
| EC (1) | ECSP077321A (https=) |
| IL (1) | IL181792A0 (https=) |
| MX (1) | MX2007003118A (https=) |
| NO (1) | NO20071937L (https=) |
| WO (1) | WO2006034004A2 (https=) |
| ZA (1) | ZA200703102B (https=) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1663958T3 (da) | 2003-09-18 | 2015-04-07 | Virobay Inc | Haloalkylholdige forbindelser som cysteinproteasehæmmere |
| WO2006060810A1 (en) | 2004-12-02 | 2006-06-08 | Schering Aktiengesellschaft | Sulfonamide compounds as cysteine protease inhibitors |
| US7488848B2 (en) | 2005-03-21 | 2009-02-10 | Virobay, Inc. | Alpha ketoamide compounds as cysteine protease inhibitors |
| JP5215167B2 (ja) * | 2005-03-22 | 2013-06-19 | ビロベイ，インコーポレイティド | システインプロテアーゼ阻害剤としてのスルホニル基含有化合物 |
| EP2064178A4 (en) * | 2006-09-08 | 2011-10-05 | Merck Canada Inc | PRODRUGS OF INHIBITORS OF CATHEPSIN S |
| WO2008037072A1 (en) | 2006-09-25 | 2008-04-03 | Merck Frosst Canada Ltd. | Cathepsin b inhibitors |
| EP2079683B1 (en) | 2006-10-04 | 2015-01-21 | Virobay, Inc. | Di-fluoro containing compounds as cysteine protease inhibitors |
| US7893112B2 (en) | 2006-10-04 | 2011-02-22 | Virobay, Inc. | Di-fluoro containing compounds as cysteine protease inhibitors |
| CA2672494A1 (en) | 2006-12-14 | 2008-06-19 | Nps Pharmaceuticals, Inc. | Use of d-serine derivatives for the treatment of anxiety disorders |
| US8273913B2 (en) | 2007-04-02 | 2012-09-25 | Merck Canada Inc. | Amidation process for the preparation of cathepsin K inhibitors |
| CN105218565A (zh) | 2008-10-17 | 2016-01-06 | 泽农医药公司 | 螺羟吲哚化合物及其作为治疗剂的用途 |
| EP2445872A4 (en) * | 2009-06-22 | 2012-12-05 | Merck Canada Inc | CATHEPSIN CYSTEIN PROTEASE FOR THE TREATMENT OF VARIOUS DISEASES |
| US8324417B2 (en) | 2009-08-19 | 2012-12-04 | Virobay, Inc. | Process for the preparation of (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid and alkyl esters and acid salts thereof |
| WO2012119941A1 (en) | 2011-03-04 | 2012-09-13 | Prozymex A/S | Peptidyl nitrilcompounds as peptidase inhibitors |
| WO2012174552A2 (en) * | 2011-06-17 | 2012-12-20 | Virobay, Inc. | Cathepsin inhibitors for treating microglia-mediated neuron loss in the central nervous system |
| CN106478564B (zh) * | 2015-08-29 | 2021-11-12 | 广东东阳光药业有限公司 | 组织蛋白酶k抑制剂及其用途 |
| WO2017036357A1 (zh) * | 2015-08-29 | 2017-03-09 | 广东东阳光药业有限公司 | 组织蛋白酶k抑制剂及其用途 |
| AU2020250933A1 (en) | 2019-04-05 | 2021-10-28 | Centre Hospitalier Régional Et Universitaire De Brest | Protease-activated receptor-2 inhibitors for the treatment of sensory neuropathy induced by a marine neurotoxic poisoning |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TR200001189T2 (tr) * | 1997-11-05 | 2000-09-21 | Novartis Ag. | Dipeptid nitriller. |
| GB9723407D0 (en) * | 1997-11-05 | 1998-01-07 | Ciba Geigy Ag | Organic compounds |
| EP1155010A1 (en) * | 1999-02-20 | 2001-11-21 | AstraZeneca AB | Acetamido acetonitrile derivatives as inhibitors of cathepsin l and/or cathepsin s |
| AU2002340031A1 (en) * | 2001-10-02 | 2003-04-14 | Boehringer Ingelheim Pharmaceuticals, Inc. | Compounds useful as reversible inhibitors of cysteine proteases |
| US7375134B2 (en) * | 2002-03-05 | 2008-05-20 | Axys Pharmaceuticals, Inc. | Cathepsin cysteine protease inhibitors |
| DE60232547D1 (de) * | 2002-03-11 | 2009-07-16 | Kao Corp | Kosmetika |
-
2005
- 2005-09-16 JP JP2007532479A patent/JP2008513472A/ja active Pending
- 2005-09-16 KR KR1020077008584A patent/KR20070061877A/ko not_active Withdrawn
- 2005-09-16 BR BRPI0515470-7A patent/BRPI0515470A/pt not_active Application Discontinuation
- 2005-09-16 WO PCT/US2005/033051 patent/WO2006034004A2/en not_active Ceased
- 2005-09-16 MX MX2007003118A patent/MX2007003118A/es not_active Application Discontinuation
- 2005-09-16 AU AU2005287046A patent/AU2005287046A1/en not_active Abandoned
- 2005-09-16 US US11/662,933 patent/US7737300B2/en active Active
- 2005-09-16 CN CNA2005800389964A patent/CN101068783A/zh active Pending
- 2005-09-16 CA CA002580065A patent/CA2580065A1/en not_active Abandoned
- 2005-09-16 EP EP05796693A patent/EP1799645A2/en not_active Withdrawn
-
2007
- 2007-03-08 IL IL181792A patent/IL181792A0/en unknown
- 2007-03-15 EC EC2007007321A patent/ECSP077321A/es unknown
- 2007-03-15 CR CR8993A patent/CR8993A/es unknown
- 2007-04-16 NO NO20071937A patent/NO20071937L/no not_active Application Discontinuation
- 2007-04-16 ZA ZA200703102A patent/ZA200703102B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2006034004A3 (en) | 2006-11-23 |
| ECSP077321A (es) | 2007-04-26 |
| MX2007003118A (es) | 2007-05-24 |
| JP2008513472A (ja) | 2008-05-01 |
| US7737300B2 (en) | 2010-06-15 |
| NO20071937L (no) | 2007-06-15 |
| EP1799645A2 (en) | 2007-06-27 |
| CA2580065A1 (en) | 2006-03-30 |
| CR8993A (es) | 2007-10-04 |
| CN101068783A (zh) | 2007-11-07 |
| AU2005287046A1 (en) | 2006-03-30 |
| WO2006034004A2 (en) | 2006-03-30 |
| IL181792A0 (en) | 2007-07-04 |
| KR20070061877A (ko) | 2007-06-14 |
| ZA200703102B (en) | 2009-09-30 |
| US20080114175A1 (en) | 2008-05-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B25D | Requested change of name of applicant approved |
Owner name: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT (DE) Free format text: ALTERADO DE: SCHERING AKTIENGESELLSCHAFT |
|
| B11A | Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing | ||
| B11Y | Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette] |