CO2019009090A2 - Compuesto de prolinamida sustituida por fenildifluormetilo - Google Patents
Compuesto de prolinamida sustituida por fenildifluormetiloInfo
- Publication number
- CO2019009090A2 CO2019009090A2 CONC2019/0009090A CO2019009090A CO2019009090A2 CO 2019009090 A2 CO2019009090 A2 CO 2019009090A2 CO 2019009090 A CO2019009090 A CO 2019009090A CO 2019009090 A2 CO2019009090 A2 CO 2019009090A2
- Authority
- CO
- Colombia
- Prior art keywords
- present
- cathepsin
- compound
- phenyldifluoromethyl
- allergies
- Prior art date
Links
- 150000001875 compounds Chemical group 0.000 title abstract 3
- -1 phenyldifluoromethyl Chemical group 0.000 title abstract 3
- 230000002401 inhibitory effect Effects 0.000 abstract 3
- 201000000596 systemic lupus erythematosus Diseases 0.000 abstract 3
- 208000023275 Autoimmune disease Diseases 0.000 abstract 2
- 108090000613 Cathepsin S Proteins 0.000 abstract 2
- 102100035654 Cathepsin S Human genes 0.000 abstract 2
- 206010020751 Hypersensitivity Diseases 0.000 abstract 2
- 206010052779 Transplant rejections Diseases 0.000 abstract 2
- 230000007815 allergy Effects 0.000 abstract 2
- 210000000988 bone and bone Anatomy 0.000 abstract 2
- 210000001185 bone marrow Anatomy 0.000 abstract 2
- 210000000056 organ Anatomy 0.000 abstract 2
- 229940122805 Cathepsin S inhibitor Drugs 0.000 abstract 1
- 108010084457 Cathepsins Proteins 0.000 abstract 1
- 102000005600 Cathepsins Human genes 0.000 abstract 1
- 208000005777 Lupus Nephritis Diseases 0.000 abstract 1
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 201000008383 nephritis Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—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
- C07D207/04—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
- C07D207/10—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 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
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—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 aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Transplantation (AREA)
- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Pyrrole Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Problema Proporcionar un compuesto útil como inhibidor de la catepsina S. Medios para la solución Los presentes inventores han examinado un compuesto que tiene un efecto inhibidor de la catepsina S y puede utilizarse como un principio activo de una composición farmacéutica para prevenir y/o tratar enfermedades autoinmunes que incluyen lupus eritematoso sistémico (SLE) y nefritis lúpica, alergias, o rechazo de injertos de un órgano, médula ósea o tejido, y han hallado que un compuesto de prolinamida sustituida por fenildifluormetilo de la presente invención tiene el efecto inhibidor de la catepsina S, y de ese modo completa la presente invención. El compuesto de prolinamida sustituida por fenildifluormetilo de la presente invención tiene el efecto inhibidor de la catepsina S, y es útil como un agente para prevenir y/o tratar enfermedades autoinmunes que incluyen SLE y nefritis, alergias, o rechazo de injertos de un órgano, médula ósea o tejido.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2017010321 | 2017-01-24 | ||
| PCT/JP2018/001927 WO2018139438A1 (ja) | 2017-01-24 | 2018-01-23 | フェニルジフルオロメチル置換プロリンアミド化合物 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO2019009090A2 true CO2019009090A2 (es) | 2019-08-30 |
Family
ID=62979051
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CONC2019/0009090A CO2019009090A2 (es) | 2017-01-24 | 2019-08-22 | Compuesto de prolinamida sustituida por fenildifluormetilo |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | US10322997B2 (es) |
| EP (1) | EP3575284B1 (es) |
| JP (1) | JP7001068B2 (es) |
| KR (1) | KR102553613B1 (es) |
| CN (2) | CN111574422B (es) |
| AR (1) | AR110767A1 (es) |
| AU (1) | AU2018211735B2 (es) |
| BR (1) | BR112019014788A2 (es) |
| CA (1) | CA3050224A1 (es) |
| CO (1) | CO2019009090A2 (es) |
| CY (1) | CY1124906T1 (es) |
| DK (1) | DK3575284T3 (es) |
| ES (1) | ES2892400T3 (es) |
| HR (1) | HRP20211613T1 (es) |
| HU (1) | HUE056920T2 (es) |
| IL (1) | IL268060B (es) |
| JO (1) | JOP20190181B1 (es) |
| LT (1) | LT3575284T (es) |
| MA (1) | MA47380A (es) |
| MX (1) | MX2019008756A (es) |
| MY (1) | MY195587A (es) |
| PH (1) | PH12019501645A1 (es) |
| PL (1) | PL3575284T3 (es) |
| PT (1) | PT3575284T (es) |
| RS (1) | RS62477B1 (es) |
| SG (1) | SG11201906777TA (es) |
| SI (1) | SI3575284T1 (es) |
| TW (1) | TWI764976B (es) |
| UA (1) | UA124036C2 (es) |
| WO (1) | WO2018139438A1 (es) |
| ZA (1) | ZA201904741B (es) |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2477657C (en) * | 2002-03-05 | 2011-04-26 | Merck Frosst Canada & Co./Merck Frosst Canada & Cie | Cathepsin cysteine protease inhibitors |
| JP2010121918A (ja) | 2008-11-17 | 2010-06-03 | Hiroyoshi Asada | 鍋等の取っ手部分の焼き焦げ防止具。 |
| NZ595073A (en) * | 2009-04-20 | 2012-11-30 | Hoffmann La Roche | Proline derivatives as cathepsin inhibitors |
| US7893099B2 (en) * | 2009-06-11 | 2011-02-22 | Hoffman-La Roche Inc. | Cyclopentane derivatives |
| JP2012059507A (ja) | 2010-09-08 | 2012-03-22 | Panasonic Corp | 基板間接続コネクタ構造 |
| US8524710B2 (en) * | 2010-11-05 | 2013-09-03 | Hoffmann-La Roche Inc. | Pyrrolidine derivatives |
| DK2776392T3 (en) * | 2011-11-11 | 2016-07-04 | Hoffmann La Roche | PROCESS FOR THE PREPARATION OF 1-acyl-4-PHENYLSULFONYLPROLINAMID DERIVATIVES AND NEW INTERMEDIATE |
| CN104114549A (zh) * | 2012-02-17 | 2014-10-22 | 霍夫曼-拉罗奇有限公司 | 新型吡咯烷衍生物 |
| BR112015003217A2 (pt) * | 2012-08-21 | 2017-07-04 | Hoffmann La Roche | novos derivados de piridina. |
| US9458181B2 (en) * | 2013-10-08 | 2016-10-04 | Merck Sharp & Dohme Corp. | Cathepsin cysteine protease inhibitors |
| WO2015051479A1 (en) * | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Cathepsin cysteine protease inhibitors |
| MX2018009638A (es) | 2016-02-26 | 2018-09-11 | Hoffmann La Roche | Derivados novedosos de pirrolidina. |
-
2018
- 2018-01-23 WO PCT/JP2018/001927 patent/WO2018139438A1/ja active Application Filing
- 2018-01-23 JP JP2018564576A patent/JP7001068B2/ja active Active
- 2018-01-23 AU AU2018211735A patent/AU2018211735B2/en active Active
- 2018-01-23 HR HRP20211613TT patent/HRP20211613T1/hr unknown
- 2018-01-23 KR KR1020197021643A patent/KR102553613B1/ko active IP Right Grant
- 2018-01-23 UA UAA201908429A patent/UA124036C2/uk unknown
- 2018-01-23 CN CN202010529596.XA patent/CN111574422B/zh active Active
- 2018-01-23 HU HUE18744079A patent/HUE056920T2/hu unknown
- 2018-01-23 AR ARP180100143A patent/AR110767A1/es unknown
- 2018-01-23 BR BR112019014788-8A patent/BR112019014788A2/pt active Search and Examination
- 2018-01-23 SG SG11201906777TA patent/SG11201906777TA/en unknown
- 2018-01-23 ES ES18744079T patent/ES2892400T3/es active Active
- 2018-01-23 JO JOP/2019/0181A patent/JOP20190181B1/ar active
- 2018-01-23 PL PL18744079T patent/PL3575284T3/pl unknown
- 2018-01-23 TW TW107102307A patent/TWI764976B/zh active
- 2018-01-23 RS RS20211299A patent/RS62477B1/sr unknown
- 2018-01-23 DK DK18744079.7T patent/DK3575284T3/da active
- 2018-01-23 EP EP18744079.7A patent/EP3575284B1/en active Active
- 2018-01-23 MY MYPI2019004186A patent/MY195587A/en unknown
- 2018-01-23 CA CA3050224A patent/CA3050224A1/en active Pending
- 2018-01-23 SI SI201830429T patent/SI3575284T1/sl unknown
- 2018-01-23 MA MA047380A patent/MA47380A/fr unknown
- 2018-01-23 MX MX2019008756A patent/MX2019008756A/es unknown
- 2018-01-23 PT PT18744079T patent/PT3575284T/pt unknown
- 2018-01-23 LT LTEPPCT/JP2018/001927T patent/LT3575284T/lt unknown
- 2018-01-23 CN CN201880008062.3A patent/CN110248925B/zh active Active
- 2018-11-05 US US16/180,862 patent/US10322997B2/en active Active
-
2019
- 2019-04-25 US US16/394,571 patent/US10532979B2/en active Active
- 2019-07-15 IL IL268060A patent/IL268060B/en unknown
- 2019-07-15 PH PH12019501645A patent/PH12019501645A1/en unknown
- 2019-07-18 ZA ZA2019/04741A patent/ZA201904741B/en unknown
- 2019-08-22 CO CONC2019/0009090A patent/CO2019009090A2/es unknown
-
2021
- 2021-10-26 CY CY20211100928T patent/CY1124906T1/el unknown
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