EA201190267A1 - Способ получения ибодутанта (men15596) и родственных промежуточных соединений - Google Patents
Способ получения ибодутанта (men15596) и родственных промежуточных соединенийInfo
- Publication number
- EA201190267A1 EA201190267A1 EA201190267A EA201190267A EA201190267A1 EA 201190267 A1 EA201190267 A1 EA 201190267A1 EA 201190267 A EA201190267 A EA 201190267A EA 201190267 A EA201190267 A EA 201190267A EA 201190267 A1 EA201190267 A1 EA 201190267A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- ibodutant
- men15596
- obtaining
- intermediate compounds
- alpha
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- YQYSVMKCMIUCHY-WJOKGBTCSA-N 6-methyl-n-[1-[[(2r)-1-[[1-(oxan-4-ylmethyl)piperidin-4-yl]methylamino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]cyclopentyl]-1-benzothiophene-2-carboxamide Chemical compound S1C2=CC(C)=CC=C2C=C1C(=O)NC1(C(=O)N[C@H](CC=2C=CC=CC=2)C(=O)NCC2CCN(CC3CCOCC3)CC2)CCCC1 YQYSVMKCMIUCHY-WJOKGBTCSA-N 0.000 title abstract 2
- 229950007749 ibodutant Drugs 0.000 title abstract 2
- 108010091949 ibodutant Proteins 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- KQRBOHOKLNORTA-UHFFFAOYSA-N 6-methyl-1-benzothiophene-2-carboxylic acid Chemical compound CC1=CC=C2C=C(C(O)=O)SC2=C1 KQRBOHOKLNORTA-UHFFFAOYSA-N 0.000 abstract 2
- LTEKQAPRXFBRNN-UHFFFAOYSA-N piperidin-4-ylmethanamine Chemical compound NCC1CCNCC1 LTEKQAPRXFBRNN-UHFFFAOYSA-N 0.000 abstract 2
- SJHPCNCNNSSLPL-CSKARUKUSA-N (4e)-4-(ethoxymethylidene)-2-phenyl-1,3-oxazol-5-one Chemical compound O1C(=O)C(=C/OCC)\N=C1C1=CC=CC=C1 SJHPCNCNNSSLPL-CSKARUKUSA-N 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 239000003153 chemical reaction reagent Substances 0.000 abstract 1
- 230000007613 environmental effect Effects 0.000 abstract 1
- 238000007363 ring formation reaction Methods 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—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
- C07D409/12—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
-
- 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
- A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
-
- 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
- A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Compounds Of Unknown Constitution (AREA)
- Steroid Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Это изобретение относится к новому способу синтеза продукта ибодутанта, показанному на прилагаемой фигуре, состоящему из небольшого числа стадий с высоким выходом, включающему реагенты и растворители с низким воздействием на окружающую среду, характеризующемуся сочетанием двух составных частей, соединений (3) и (4), одно из которых, соединение (3), синтезируют путем сочетания 6-метил-2-бензо[b]тиофенкарбоновой кислоты (1) с 1-амино-альфа-альфа-циклопентанкарбоновой кислотой и последующей циклизации с оксазолоном, тогда как другое, соединение (4), получают из подходящего 4-аминометилпиперидина (2), функционализированного с высокой степенью селективности.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ITMI2009A000897A IT1394304B1 (it) | 2009-05-21 | 2009-05-21 | Processo per la preparazione di ibodutant (men15596) e relativi intermedi |
| PCT/EP2010/002884 WO2010133306A1 (en) | 2009-05-21 | 2010-05-11 | Process for the preparation of ibodutant (men15596) and related intermediates |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201190267A1 true EA201190267A1 (ru) | 2012-05-30 |
| EA019777B1 EA019777B1 (ru) | 2014-06-30 |
Family
ID=41264221
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201190267A EA019777B1 (ru) | 2009-05-21 | 2010-05-11 | Способ получения ибодутанта (men15596) и родственных промежуточных соединений |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US8431684B2 (ru) |
| EP (1) | EP2432778B1 (ru) |
| JP (1) | JP5645926B2 (ru) |
| KR (1) | KR101695346B1 (ru) |
| CN (1) | CN102428081B (ru) |
| AR (1) | AR076785A1 (ru) |
| AU (1) | AU2010251514B2 (ru) |
| BR (1) | BRPI1013073A2 (ru) |
| CA (1) | CA2762625A1 (ru) |
| CY (1) | CY1114079T1 (ru) |
| DK (1) | DK2432778T3 (ru) |
| EA (1) | EA019777B1 (ru) |
| EG (1) | EG27000A (ru) |
| ES (1) | ES2409705T3 (ru) |
| HR (1) | HRP20130380T1 (ru) |
| IL (1) | IL216400A (ru) |
| IT (1) | IT1394304B1 (ru) |
| MA (1) | MA33375B1 (ru) |
| MX (1) | MX2011012317A (ru) |
| NZ (1) | NZ596523A (ru) |
| PL (1) | PL2432778T3 (ru) |
| PT (1) | PT2432778E (ru) |
| SG (1) | SG176171A1 (ru) |
| SI (1) | SI2432778T1 (ru) |
| TW (1) | TWI424996B (ru) |
| UA (1) | UA105523C2 (ru) |
| WO (1) | WO2010133306A1 (ru) |
| ZA (1) | ZA201108483B (ru) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20240010642A1 (en) * | 2021-01-05 | 2024-01-11 | Southern Research Institute | Modulators of programmed death-ligand-1 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY130373A (en) * | 2001-10-29 | 2007-06-29 | Malesci Sas | Linear basic compounds having nk-2 antagonist activity and formulations thereof |
| ITFI20040221A1 (it) * | 2004-10-27 | 2005-01-27 | Guidotti & C Spa | Composizioni farmaceutiche a base di nk2 antagonisti per uso pediatrico |
| WO2007080884A1 (ja) * | 2006-01-11 | 2007-07-19 | Seikagaku Corporation | シクロアルキルカルボニルアミノ酸エステル誘導体及びその製造方法 |
-
2009
- 2009-05-21 IT ITMI2009A000897A patent/IT1394304B1/it active
-
2010
- 2010-05-11 EA EA201190267A patent/EA019777B1/ru not_active IP Right Cessation
- 2010-05-11 MX MX2011012317A patent/MX2011012317A/es active IP Right Grant
- 2010-05-11 EP EP10721687A patent/EP2432778B1/en active Active
- 2010-05-11 CN CN201080021722.5A patent/CN102428081B/zh not_active Expired - Fee Related
- 2010-05-11 BR BRPI1013073A patent/BRPI1013073A2/pt not_active IP Right Cessation
- 2010-05-11 UA UAA201113614A patent/UA105523C2/ru unknown
- 2010-05-11 WO PCT/EP2010/002884 patent/WO2010133306A1/en not_active Ceased
- 2010-05-11 CA CA2762625A patent/CA2762625A1/en not_active Abandoned
- 2010-05-11 MA MA34472A patent/MA33375B1/fr unknown
- 2010-05-11 ES ES10721687T patent/ES2409705T3/es active Active
- 2010-05-11 US US13/321,501 patent/US8431684B2/en not_active Expired - Fee Related
- 2010-05-11 HR HRP20130380AT patent/HRP20130380T1/hr unknown
- 2010-05-11 SI SI201030192T patent/SI2432778T1/sl unknown
- 2010-05-11 DK DK10721687.1T patent/DK2432778T3/da active
- 2010-05-11 SG SG2011085545A patent/SG176171A1/en unknown
- 2010-05-11 NZ NZ596523A patent/NZ596523A/xx not_active IP Right Cessation
- 2010-05-11 KR KR1020117027585A patent/KR101695346B1/ko not_active Expired - Fee Related
- 2010-05-11 PL PL10721687T patent/PL2432778T3/pl unknown
- 2010-05-11 AU AU2010251514A patent/AU2010251514B2/en not_active Ceased
- 2010-05-11 JP JP2012511171A patent/JP5645926B2/ja not_active Expired - Fee Related
- 2010-05-11 PT PT107216871T patent/PT2432778E/pt unknown
- 2010-05-20 AR ARP100101759A patent/AR076785A1/es unknown
- 2010-05-20 TW TW099116060A patent/TWI424996B/zh not_active IP Right Cessation
-
2011
- 2011-11-17 IL IL216400A patent/IL216400A/en not_active IP Right Cessation
- 2011-11-17 EG EG2011111951A patent/EG27000A/xx active
- 2011-11-18 ZA ZA2011/08483A patent/ZA201108483B/en unknown
-
2013
- 2013-05-16 CY CY20131100392T patent/CY1114079T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM RU |