PE20190609A1 - DERIVADOS DE CROMANO, ISOCROMANO Y DIHIDROISOBENZOFURANOS COMO MODULADORES ALOSTERICOS NEGATIVOS DE mGluR2, COMPOSICIONES Y SU USO - Google Patents
DERIVADOS DE CROMANO, ISOCROMANO Y DIHIDROISOBENZOFURANOS COMO MODULADORES ALOSTERICOS NEGATIVOS DE mGluR2, COMPOSICIONES Y SU USOInfo
- Publication number
- PE20190609A1 PE20190609A1 PE2019000706A PE2019000706A PE20190609A1 PE 20190609 A1 PE20190609 A1 PE 20190609A1 PE 2019000706 A PE2019000706 A PE 2019000706A PE 2019000706 A PE2019000706 A PE 2019000706A PE 20190609 A1 PE20190609 A1 PE 20190609A1
- Authority
- PE
- Peru
- Prior art keywords
- mglur2
- ring
- negative allosteric
- isocromano
- dihydroisobenzofuranos
- Prior art date
Links
Classifications
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- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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- 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
- A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
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- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
- C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
- C07D221/22—Bridged ring systems
- C07D221/24—Camphidines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—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 C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—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 C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—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 C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—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 C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
- C07D491/18—Bridged systems
-
- 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
- A61K31/01—Hydrocarbons
- A61K31/015—Hydrocarbons carbocyclic
-
- 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
- A61K31/02—Halogenated hydrocarbons
- A61K31/025—Halogenated hydrocarbons carbocyclic
- A61K31/03—Halogenated hydrocarbons carbocyclic aromatic
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Anesthesiology (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
Se refiere a ciertos compuestos de cromano, isocromano y dihidroisobenzofurano sustituidos de Formula (I) o su sal farmaceuticamente aceptable, en la que: el anillo A es (II), (III), (IV) o (V); R2 es H, ciclopropilo, entre otros; R2A, R3 y R3A son H o metilo; el anillo B es fenilo, heteroarilo, entre otros; n es 0, 1, 2 o 3 (si no supera el numero maximo de atomos de H sustituibles en el anillo B); y R1 es halogeno, -CN, entre otros. Tambien se refiere a una composicion farmaceutica y a metodos de preparacion. La presente invencion es util como inhibidor o modulador alosterico negativo (NAM) del receptor metabotropico de glutamato 2 (mGluR2) para el tratamiento de enfermedades o trastornos en los que esta implicado dicho receptor, como Alzheimer, deterioro cognitivo, esquizofrenia y otros trastornos del estado de animo, del dolor y del sueno.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662400150P | 2016-09-27 | 2016-09-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20190609A1 true PE20190609A1 (es) | 2019-04-23 |
Family
ID=60043302
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2019000706A PE20190609A1 (es) | 2016-09-27 | 2017-09-25 | DERIVADOS DE CROMANO, ISOCROMANO Y DIHIDROISOBENZOFURANOS COMO MODULADORES ALOSTERICOS NEGATIVOS DE mGluR2, COMPOSICIONES Y SU USO |
Country Status (39)
| Country | Link |
|---|---|
| US (4) | US10335399B2 (es) |
| EP (1) | EP3519416B1 (es) |
| JP (3) | JP6681517B2 (es) |
| KR (1) | KR102296043B1 (es) |
| CN (1) | CN109983022B (es) |
| AR (1) | AR109714A1 (es) |
| AU (2) | AU2017334870C1 (es) |
| CA (1) | CA3037537C (es) |
| CL (1) | CL2019000778A1 (es) |
| CO (1) | CO2019002673A2 (es) |
| CR (1) | CR20190147A (es) |
| CY (1) | CY1124346T1 (es) |
| DK (1) | DK3519416T3 (es) |
| DO (1) | DOP2019000076A (es) |
| EA (1) | EA038627B1 (es) |
| EC (1) | ECSP19020742A (es) |
| ES (1) | ES2868973T3 (es) |
| GE (2) | GEP20217266B (es) |
| HR (1) | HRP20210793T1 (es) |
| HU (1) | HUE054898T2 (es) |
| IL (1) | IL265366B (es) |
| JO (1) | JOP20190058B1 (es) |
| LT (1) | LT3519416T (es) |
| MA (1) | MA46342B1 (es) |
| MD (1) | MD3519416T2 (es) |
| MX (1) | MX2019003492A (es) |
| MY (1) | MY196807A (es) |
| NI (1) | NI201900025A (es) |
| PE (1) | PE20190609A1 (es) |
| PH (1) | PH12019500597A1 (es) |
| PL (1) | PL3519416T3 (es) |
| PT (1) | PT3519416T (es) |
| RS (1) | RS61890B1 (es) |
| SI (1) | SI3519416T1 (es) |
| TN (2) | TN2020000161A1 (es) |
| TW (1) | TWI764934B (es) |
| UA (1) | UA123687C2 (es) |
| WO (1) | WO2018063955A1 (es) |
| ZA (1) | ZA201901701B (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LT3519416T (lt) * | 2016-09-27 | 2021-06-10 | Merck Sharp & Dohme Corp. | Chromano, izochromano ir dihidroizobenzofurano dariniai, kaip mglur2 neigiami alosteriniai moduliatoriai, kompozicijos ir jų panaudojimas |
| SG11202006296YA (en) | 2018-01-19 | 2020-08-28 | Cytokinetics Inc | Dihydrobenzofuran and inden analogs as cardiac sarcomere inhibitors |
| EP3814342B1 (en) | 2018-06-26 | 2022-07-27 | Cytokinetics, Inc. | Cardiac sarcomere inhibitors |
| JP7291426B2 (ja) * | 2019-03-01 | 2023-06-15 | 山東亨利醫藥科技有限責任公司 | 縮合三環式化合物を調製するための方法、及びその中間体 |
| MX2023010125A (es) | 2021-03-04 | 2023-09-11 | Cytokinetics Inc | Inhibidores del sarcomero cardiaco. |
| WO2023278729A1 (en) * | 2021-06-30 | 2023-01-05 | The General Hospital Corporation | Chromane imaging ligands |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5552437A (en) | 1994-10-27 | 1996-09-03 | Merck Frosst Canada, Inc. | Bisarylcarbinol derivatives as inhibitors of leukotriene biosynthesis |
| US5576338A (en) | 1995-02-15 | 1996-11-19 | Merck Frosst Canada, Inc. | Bis (biaryl) compounds as inhibitors of leukotriene biosynthesis |
| WO2005014543A1 (ja) | 2003-08-06 | 2005-02-17 | Japan Tobacco Inc. | 縮合環化合物及びそのｈｃｖポリメラーゼ阻害剤としての利用 |
| AU2006299671A1 (en) | 2005-10-05 | 2007-04-12 | Merck Frosst Canada Ltd | Substituted quinolines as inhibitors of leukotriene biosynthesis |
| AR065093A1 (es) | 2007-02-05 | 2009-05-13 | Merck Frosst Canada Ltd | Compuestos farmacéuticos inhibidores de la biosintesis de leucotrienos |
| PE20110368A1 (es) | 2008-08-18 | 2011-06-13 | Univ Yale | Moduladores de mif |
| KR101753826B1 (ko) * | 2009-05-12 | 2017-07-04 | 얀센 파마슈티칼즈, 인코포레이티드 | 1,２,４―트리아졸로［４,３―ａ］피리딘 유도체 및 신경정신 질환의 치료 또는 예방을 위한 이들의 용도 |
| US8772301B2 (en) | 2009-12-18 | 2014-07-08 | Sunovion Pharmaceuticals, Inc. | Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof |
| KR20140088887A (ko) * | 2011-11-03 | 2014-07-11 | 머크 샤프 앤드 돔 코포레이션 | mGluR2-음성 알로스테릭 조절제로서의 퀴놀린 카르복스아미드 및 퀴놀린 카르보니트릴 유도체, 조성물, 및 그의 용도 |
| JO3368B1 (ar) | 2013-06-04 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2 |
| WO2016029454A1 (en) | 2014-08-29 | 2016-03-03 | Merck Sharp & Dohme Corp. | TETRAHYDRONAPHTHYRIDINE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE |
| US9382208B1 (en) | 2015-01-26 | 2016-07-05 | Vanderbilt University | Negative allosteric modulators of metabotropic glutamate receptor 2 |
| US10538491B2 (en) | 2015-03-16 | 2020-01-21 | Vanderbilt University | 4,5-substituted picolinamide and picolinonitrile metabotropic glutamate receptor 2 negative allosteric modulators |
| JP6471614B2 (ja) | 2015-05-29 | 2019-02-20 | 株式会社リコー | 通信端末、通信システム、通信制御方法、及びプログラム |
| JP2018154554A (ja) | 2015-07-29 | 2018-10-04 | 大日本住友製薬株式会社 | 新規リンカー部位を持つ縮合ピラゾール誘導体およびその医薬用途 |
| LT3519416T (lt) * | 2016-09-27 | 2021-06-10 | Merck Sharp & Dohme Corp. | Chromano, izochromano ir dihidroizobenzofurano dariniai, kaip mglur2 neigiami alosteriniai moduliatoriai, kompozicijos ir jų panaudojimas |
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2017
- 2017-09-25 LT LTEP17781253.4T patent/LT3519416T/lt unknown
- 2017-09-25 SI SI201730727T patent/SI3519416T1/sl unknown
- 2017-09-25 DK DK17781253.4T patent/DK3519416T3/da active
- 2017-09-25 MY MYPI2019001659A patent/MY196807A/en unknown
- 2017-09-25 TW TW106132824A patent/TWI764934B/zh active
- 2017-09-25 CR CR20190147A patent/CR20190147A/es unknown
- 2017-09-25 GE GEAP201715056A patent/GEP20217266B/en unknown
- 2017-09-25 EA EA201990818A patent/EA038627B1/ru unknown
- 2017-09-25 PL PL17781253T patent/PL3519416T3/pl unknown
- 2017-09-25 US US15/713,769 patent/US10335399B2/en active Active
- 2017-09-25 PE PE2019000706A patent/PE20190609A1/es unknown
- 2017-09-25 MA MA46342A patent/MA46342B1/fr unknown
- 2017-09-25 KR KR1020197011789A patent/KR102296043B1/ko active IP Right Grant
- 2017-09-25 MX MX2019003492A patent/MX2019003492A/es unknown
- 2017-09-25 MD MDE20190867T patent/MD3519416T2/ro unknown
- 2017-09-25 CA CA3037537A patent/CA3037537C/en active Active
- 2017-09-25 AR ARP170102642A patent/AR109714A1/es active IP Right Grant
- 2017-09-25 TN TNP/2020/000161A patent/TN2020000161A1/en unknown
- 2017-09-25 CN CN201780071759.0A patent/CN109983022B/zh active Active
- 2017-09-25 HU HUE17781253A patent/HUE054898T2/hu unknown
- 2017-09-25 AU AU2017334870A patent/AU2017334870C1/en active Active
- 2017-09-25 UA UAA201904545A patent/UA123687C2/uk unknown
- 2017-09-25 EP EP17781253.4A patent/EP3519416B1/en active Active
- 2017-09-25 GE GEAP201715310A patent/GEP20217279B/en unknown
- 2017-09-25 WO PCT/US2017/053155 patent/WO2018063955A1/en active Application Filing
- 2017-09-25 PT PT177812534T patent/PT3519416T/pt unknown
- 2017-09-25 TN TNP/2020/000160A patent/TN2020000160A1/en unknown
- 2017-09-25 JO JOP/2019/0058A patent/JOP20190058B1/ar active
- 2017-09-25 JP JP2019516203A patent/JP6681517B2/ja active Active
- 2017-09-25 RS RS20210649A patent/RS61890B1/sr unknown
- 2017-09-25 ES ES17781253T patent/ES2868973T3/es active Active
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2019
- 2019-03-13 IL IL265366A patent/IL265366B/en unknown
- 2019-03-19 ZA ZA2019/01701A patent/ZA201901701B/en unknown
- 2019-03-19 PH PH12019500597A patent/PH12019500597A1/en unknown
- 2019-03-20 NI NI201900025A patent/NI201900025A/es unknown
- 2019-03-22 CO CONC2019/0002673A patent/CO2019002673A2/es unknown
- 2019-03-25 CL CL2019000778A patent/CL2019000778A1/es unknown
- 2019-03-26 DO DO2019000076A patent/DOP2019000076A/es unknown
- 2019-03-28 EC ECSENADI201920742A patent/ECSP19020742A/es unknown
- 2019-04-23 US US16/392,131 patent/US10806724B2/en active Active
- 2019-09-30 JP JP2019178232A patent/JP6945605B2/ja active Active
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2020
- 2020-03-23 JP JP2020051049A patent/JP6992109B2/ja active Active
- 2020-09-25 US US17/032,626 patent/US20210015800A1/en not_active Abandoned
- 2020-11-16 AU AU2020270468A patent/AU2020270468B2/en active Active
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2021
- 2021-05-17 HR HRP20210793TT patent/HRP20210793T1/hr unknown
- 2021-05-31 CY CY20211100468T patent/CY1124346T1/el unknown
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2022
- 2022-03-15 US US17/695,262 patent/US20220218676A1/en active Pending
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