HRP20201615T1 - Derivati etinila - Google Patents
Derivati etinila Download PDFInfo
- Publication number
- HRP20201615T1 HRP20201615T1 HRP20201615TT HRP20201615T HRP20201615T1 HR P20201615 T1 HRP20201615 T1 HR P20201615T1 HR P20201615T T HRP20201615T T HR P20201615TT HR P20201615 T HRP20201615 T HR P20201615T HR P20201615 T1 HRP20201615 T1 HR P20201615T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound
- formula
- pharmaceutically acceptable
- image
- formulas
- Prior art date
Links
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 3
- 238000000034 method Methods 0.000 claims 2
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 206010003805 Autism Diseases 0.000 claims 1
- 208000020706 Autistic disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 206010047700 Vomiting Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 230000029936 alkylation Effects 0.000 claims 1
- 238000005804 alkylation reaction Methods 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- HVTICUPFWKNHNG-UHFFFAOYSA-N iodoethane Chemical compound CCI HVTICUPFWKNHNG-UHFFFAOYSA-N 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000003287 optical effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 238000000926 separation method Methods 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 230000008673 vomiting Effects 0.000 claims 1
Classifications
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/527—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/09—Geometrical isomers
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychology (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Toxicology (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (5)
1. Spoj, naznačen time, da je predstavljen formulama IA i IB
[image]
ili njegova farmaceutski prihvatljiva sol ili kiselinska adicijska sol, racemična smjesa, ili njezin odgovarajući enantiomer i/ili optički izomer i/ili stereoizomer.
2. Postupak proizvodnje spoja formule IA ili IB prema patentnom zahtjevu 1, naznačen time, da se taj postupak sastoji od
alkiliranja spoja formule
[image]
s etil-jodidom i razdvajanja izomera na spoj formula
[image]
ili, po želji, pretvaranja dobivenih spojeva u njihove farmaceutski prihvatljive soli.
3. Spoj formule IA ili IB prema patentnom zahtjevu 1, naznačen time, da je za upotrebu u vidu terapeutski aktivnih tvari.
4. Spoj formule IA ili IB prema patentnom zahtjevu 1, naznačen time, da je za upotrebu u liječenju Parkinsonove bolesti, anksioznosti, povraćanja, opsesivno-kompulzivnog poremećaja, autizma, raka, depresije i dijabetesa tipa 2.
5. Farmaceutski pripravak, naznačen time, da sadrži spoj formule IA ili IB prema patentnom zahtjevu 1 i farmaceutski prihvatljive pomoćne tvari.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16179837 | 2016-07-18 | ||
| EP17742971.9A EP3484889B1 (en) | 2016-07-18 | 2017-07-12 | Ethynyl derivatives |
| PCT/EP2017/067495 WO2018015235A1 (en) | 2016-07-18 | 2017-07-12 | Ethynyl derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20201615T1 true HRP20201615T1 (hr) | 2020-12-11 |
Family
ID=56418435
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20201615TT HRP20201615T1 (hr) | 2016-07-18 | 2020-10-08 | Derivati etinila |
Country Status (31)
| Country | Link |
|---|---|
| US (3) | US20190144458A1 (hr) |
| EP (1) | EP3484889B1 (hr) |
| JP (1) | JP6936305B2 (hr) |
| KR (1) | KR20190026805A (hr) |
| CN (1) | CN109476671B (hr) |
| AR (1) | AR109075A1 (hr) |
| AU (1) | AU2017299083B2 (hr) |
| BR (1) | BR112019000314A2 (hr) |
| CA (1) | CA3030788A1 (hr) |
| CL (1) | CL2019000045A1 (hr) |
| CO (1) | CO2018013824A2 (hr) |
| CR (1) | CR20190014A (hr) |
| DK (1) | DK3484889T3 (hr) |
| ES (1) | ES2826389T3 (hr) |
| HR (1) | HRP20201615T1 (hr) |
| HU (1) | HUE051006T2 (hr) |
| IL (1) | IL263884A (hr) |
| LT (1) | LT3484889T (hr) |
| MA (1) | MA45665B1 (hr) |
| MX (1) | MX2019000442A (hr) |
| PE (1) | PE20190382A1 (hr) |
| PH (1) | PH12019500119A1 (hr) |
| PL (1) | PL3484889T3 (hr) |
| PT (1) | PT3484889T (hr) |
| RS (1) | RS60908B1 (hr) |
| RU (1) | RU2745068C2 (hr) |
| SG (1) | SG11201811829QA (hr) |
| SI (1) | SI3484889T1 (hr) |
| TW (1) | TWI729169B (hr) |
| WO (1) | WO2018015235A1 (hr) |
| ZA (1) | ZA201900113B (hr) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MA42442B1 (fr) | 2015-07-15 | 2019-07-31 | Hoffmann La Roche | Dérivés d'éthynyle comme modulateurs du récepteur métabotropique au glutamate |
| CN110183456A (zh) * | 2019-07-11 | 2019-08-30 | 河南师范大学 | 一种2-芳基吲唑琥珀酰亚胺螺环化合物的合成方法 |
| US11515154B2 (en) * | 2020-10-27 | 2022-11-29 | Applied Materials, Inc. | Selective deposition of a passivation film |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003298889A1 (en) * | 2002-12-04 | 2004-06-23 | Merck & Co., Inc. | Spirocyclic ureas, compositions containing such compounds and methods of use |
| WO2006125784A1 (en) | 2005-05-24 | 2006-11-30 | Laboratoires Serono S.A. | Tricyclic spiro derivatives as crth2 modulators |
| ATE540932T1 (de) | 2006-08-31 | 2012-01-15 | Schering Corp | Hydantoin-derivate als antibakterielle wirkstoffe |
| EA200971143A1 (ru) | 2007-06-03 | 2010-06-30 | Вандербилт Юниверсити | Бензамидные mglur5 позитивные аллостерические модуляторы и способы их получения и применения |
| US8779157B2 (en) | 2009-09-04 | 2014-07-15 | Vanderbilt University | MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| US8389536B2 (en) | 2009-10-27 | 2013-03-05 | Hoffmann-La Roche Inc. | Positive allosteric modulators (PAM) |
| US8759377B2 (en) | 2009-11-23 | 2014-06-24 | Vanderbilt University | Substituted dioxopiperidines and dioxopyrrolidines as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| US8586581B2 (en) * | 2009-12-17 | 2013-11-19 | Hoffmann-La Roche Inc | Ethynyl compounds useful for treatment of CNS disorders |
| US8420661B2 (en) | 2010-04-13 | 2013-04-16 | Hoffmann-La Roche Inc. | Arylethynyl derivatives |
| US8772300B2 (en) | 2011-04-19 | 2014-07-08 | Hoffmann-La Roche Inc. | Phenyl or pyridinyl-ethynyl derivatives |
| DK2702051T3 (en) | 2011-04-26 | 2015-03-16 | Hoffmann La Roche | Ethynyl derivatives AS POSITIVE allosteric modulators mGluR5 |
| US10533000B2 (en) | 2011-05-26 | 2020-01-14 | Sunovion Pharmaceuticals, Inc. | Metabotrophic glutamate receptor 5 modulators and methods of use thereof |
| WO2013006738A1 (en) * | 2011-07-06 | 2013-01-10 | Gilead Sciences, Inc. | Compounds for the treatment of hiv |
| US20130123254A1 (en) | 2011-09-30 | 2013-05-16 | Barbara Biemans | Pharmaceutically acceptable mglur5 positive allosteric modulators and their methods of identification |
| UA110862C2 (uk) | 2011-10-07 | 2016-02-25 | Ф. Хоффманн-Ля Рош Аг | Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5 |
| JP5989253B2 (ja) | 2012-10-18 | 2016-09-07 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | ｍＧｌｕＲ５受容体活性のモジュレータとしてのエチニル誘導体 |
| AU2013331782B2 (en) | 2012-10-18 | 2017-03-09 | F. Hoffmann-La Roche Ag | Ethynyl derivatives as modulators of mGluR5 receptor activity |
| CN105121424B (zh) | 2013-02-18 | 2019-01-22 | 华领医药技术（上海）有限公司 | mGluR调节剂 |
| UY35400A (es) | 2013-03-15 | 2014-10-31 | Novartis Ag | Compuestos y composiciones para el tratamiento de enfermedades parasitarias |
| 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 |
| AU2014327504B2 (en) * | 2013-09-25 | 2018-01-04 | F. Hoffmann-La Roche Ag | Ethynyl derivatives |
| TWI649310B (zh) | 2014-01-10 | 2019-02-01 | 赫孚孟拉羅股份公司 | 乙炔基衍生物 |
| CN104860941B (zh) | 2014-02-25 | 2017-03-22 | 上海海雁医药科技有限公司 | 2,4‑二取代苯‑1,5‑二胺衍生物及其应用以及由其制备的药物组合物和药用组合物 |
| HUE041392T2 (hu) | 2014-02-25 | 2019-05-28 | Hoffmann La Roche | Etinil származékok |
| WO2016146600A1 (en) | 2015-03-19 | 2016-09-22 | F. Hoffmann-La Roche Ag | 3-(4-ethynylphenyl)hexahydropyrimidin-2,4-dione derivatives as modulators of mglur4 |
| MA42442B1 (fr) * | 2015-07-15 | 2019-07-31 | Hoffmann La Roche | Dérivés d'éthynyle comme modulateurs du récepteur métabotropique au glutamate |
| US10391998B2 (en) | 2016-11-16 | 2019-08-27 | Ford Global Technologies, Llc | Vehicle systems and methods for reducing electrified vehicle noise, vibration, and harshness |
-
2017
- 2017-07-12 RU RU2019102757A patent/RU2745068C2/ru active
- 2017-07-12 MA MA45665A patent/MA45665B1/fr unknown
- 2017-07-12 PL PL17742971T patent/PL3484889T3/pl unknown
- 2017-07-12 KR KR1020197003025A patent/KR20190026805A/ko active IP Right Grant
- 2017-07-12 PE PE2018003348A patent/PE20190382A1/es unknown
- 2017-07-12 EP EP17742971.9A patent/EP3484889B1/en active Active
- 2017-07-12 WO PCT/EP2017/067495 patent/WO2018015235A1/en unknown
- 2017-07-12 MX MX2019000442A patent/MX2019000442A/es active IP Right Grant
- 2017-07-12 JP JP2019502162A patent/JP6936305B2/ja active Active
- 2017-07-12 RS RS20201217A patent/RS60908B1/sr unknown
- 2017-07-12 SI SI201730468T patent/SI3484889T1/sl unknown
- 2017-07-12 DK DK17742971.9T patent/DK3484889T3/da active
- 2017-07-12 HU HUE17742971A patent/HUE051006T2/hu unknown
- 2017-07-12 LT LTEP17742971.9T patent/LT3484889T/lt unknown
- 2017-07-12 CR CR20190014A patent/CR20190014A/es unknown
- 2017-07-12 PT PT177429719T patent/PT3484889T/pt unknown
- 2017-07-12 CA CA3030788A patent/CA3030788A1/en not_active Abandoned
- 2017-07-12 CN CN201780044455.5A patent/CN109476671B/zh active Active
- 2017-07-12 BR BR112019000314-2A patent/BR112019000314A2/pt not_active IP Right Cessation
- 2017-07-12 AU AU2017299083A patent/AU2017299083B2/en not_active Ceased
- 2017-07-12 ES ES17742971T patent/ES2826389T3/es active Active
- 2017-07-12 SG SG11201811829QA patent/SG11201811829QA/en unknown
- 2017-07-17 TW TW106123741A patent/TWI729169B/zh not_active IP Right Cessation
- 2017-07-17 AR ARP170101987A patent/AR109075A1/es unknown
-
2018
- 2018-12-19 CO CONC2018/0013824A patent/CO2018013824A2/es unknown
- 2018-12-20 IL IL263884A patent/IL263884A/en active IP Right Grant
-
2019
- 2019-01-07 CL CL2019000045A patent/CL2019000045A1/es unknown
- 2019-01-08 ZA ZA2019/00113A patent/ZA201900113B/en unknown
- 2019-01-16 PH PH12019500119A patent/PH12019500119A1/en unknown
- 2019-01-17 US US16/250,278 patent/US20190144458A1/en not_active Abandoned
-
2020
- 2020-05-01 US US16/865,233 patent/US11242349B2/en active Active
- 2020-10-08 HR HRP20201615TT patent/HRP20201615T1/hr unknown
-
2022
- 2022-01-04 US US17/568,530 patent/US20220127275A1/en active Pending
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HRP20201615T1 (hr) | Derivati etinila | |
| PH12018500106A1 (en) | Ethynyl derivatives as metabotropic glutamate receptor modulators | |
| JP2013032389A5 (hr) | ||
| RU2018114447A (ru) | Введение дейтерированных усилителей cftr | |
| EA201592144A1 (ru) | Производное фенола, способ его получения и его применение в медицине | |
| WO2013061205A3 (en) | (4 - phenylimidazol - 2 - yl) ethylamine derivatives usful as sodium channel modulators | |
| MX343788B (es) | Derivados de heteroarilo como moduladores de nachr alfa 7. | |
| EA201071298A1 (ru) | Соединение 3-аминокарбазола, фармацевтическая композиция, его содержащая, и способ их получения | |
| IN2014CN00989A (hr) | ||
| UA109698C2 (xx) | Похідні азаіндазолу або діазаіндазолу як медикамент | |
| MA37866A1 (fr) | Dérivés de type aza-indazole ou diaza-indazole pour le traitement de la douleur | |
| EA201490569A1 (ru) | Полиморфная форма гидрохлорида придопидина | |
| JP2016510326A5 (hr) | ||
| MX2021010046A (es) | Nueva composicion terapeutica que contiene ingrediente activo de apomorfinas. | |
| EA201491818A1 (ru) | Способ получения оптически чистых и необязательно замещенных производных 2-(1-гидроксиалкил)хромен-4-она и их применение при получении лекарственных препаратов | |
| HRP20201187T1 (hr) | Derivat triazolopirazinona koristan kao inhibitor ljudskog pde1 | |
| WO2015009731A3 (en) | Azacyclic constrained analogs of fty720 | |
| AR075626A1 (es) | Metodos para administrar (4ar,10ar)-1-n- propil-1,2,3,4,4a,5,10,10a- octahidro -benzo (g) quinolin-6,7-diol y sus composiciones farmaceuticas. uso. | |
| MX2021003670A (es) | Derivados biciclicos como moduladores del receptor gabaa a5. | |
| BR112016017816A8 (pt) | derivados de etinila, seus usos, e composição farmacêutica | |
| HRP20161692T1 (hr) | Ariletinil pirimidini | |
| WO2015138276A3 (en) | Retinoic acid receptor-related orphan receptor modulators and uses thereof | |
| EA201590676A1 (ru) | Производные этинила в качестве модуляторов активности рецептора mglur5 | |
| HRP20150387T1 (hr) | Sol kolina i trometamina od likofelona | |
| MY170152A (en) | Ethynyl derivative as modulators of mglur5 receptor activity |