PE20220253A1 - Benzamidas sustituidas con 1,3-tiazol-2-ilo - Google Patents
Benzamidas sustituidas con 1,3-tiazol-2-iloInfo
- Publication number
- PE20220253A1 PE20220253A1 PE2021001723A PE2021001723A PE20220253A1 PE 20220253 A1 PE20220253 A1 PE 20220253A1 PE 2021001723 A PE2021001723 A PE 2021001723A PE 2021001723 A PE2021001723 A PE 2021001723A PE 20220253 A1 PE20220253 A1 PE 20220253A1
- Authority
- PE
- Peru
- Prior art keywords
- thiazol
- ethyl
- methylmorpholin
- benzamide
- trifluoromethyl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/433—Thidiazoles
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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
- A61K31/44—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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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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
- A61K31/495—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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- 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
-
- 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
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- 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
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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
- A61P25/28—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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/582—Recycling of unreacted starting or intermediate materials
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- AIDS & HIV (AREA)
- Psychology (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
Abstract
La presente invencion se refiere a un compuesto derivado de benzamidas sustituidas con 1,3-tiazol-2-ilo de formula I o un enantiomero, diastereomero, racemato, hidrato, solvato o una sal del este, donde: R1 es alquilo C1-C4; R2 es -(CH2)q-morfolinilo sustituido con Rc; R3 es alquilo C1-C4; Rc es metilo; A es CF3-pirimidinilo; q es 1. Tambien se refiere a una composicion farmaceutica. Son compuestos especificos: 3-(5-etil-1,3-tiazol-2-il)-5-{[(2R)-4-metilmorfolin-2-il]metoxi}-N-{(1R)-1-[2-(trifluorometil)pirimidin-5-il]etil}benzamida, 3-{[(2R)-4-metilmorfolin-2-il]metoxi}-5-(5-metil-1,3-tiazol-2-il)-N-{(1R)-1-[2-(trifluorometil)pirimidin-5-il]etil}benzamida, 3-(5-etil-1,3-tiazol-2-il)-5-{[(2R)-4-metilmorfolin-2-il]metoxi}-N-{(1R)-1-[6-(trifluorometil)piridazin-3-il]etil}benzamida. Dichos compuestos son inhibidores del receptor P2X3, siendo utiles en el tratamiento de un trastorno neurogenico.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14196954 | 2014-12-09 | ||
| PCT/EP2015/078765 WO2016091776A1 (en) | 2014-12-09 | 2015-12-07 | 1,3-thiazol-2-yl substituted benzamides |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20220253A1 true PE20220253A1 (es) | 2022-02-16 |
Family
ID=52015966
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021001723A PE20220253A1 (es) | 2014-12-09 | 2015-12-07 | Benzamidas sustituidas con 1,3-tiazol-2-ilo |
| PE2017000984A PE20180227A1 (es) | 2014-12-09 | 2015-12-07 | Benzamidas sustituidas con 1,3-tiazol-2-ilo |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2017000984A PE20180227A1 (es) | 2014-12-09 | 2015-12-07 | Benzamidas sustituidas con 1,3-tiazol-2-ilo |
Country Status (42)
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6544665B2 (ja) | 2014-12-09 | 2019-07-17 | バイエル アクチェンゲゼルシャフトＢａｙｅｒ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | １，３−チアゾール−２−イル置換ベンズアミド |
| TWI794171B (zh) | 2016-05-11 | 2023-03-01 | 美商滬亞生物國際有限公司 | Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療 |
| TWI808055B (zh) | 2016-05-11 | 2023-07-11 | 美商滬亞生物國際有限公司 | Hdac 抑制劑與 pd-1 抑制劑之組合治療 |
| CN106588785A (zh) * | 2016-12-02 | 2017-04-26 | 山东吉田香料股份有限公司 | 一种乙酰基吡嗪的制备方法 |
| US10111883B1 (en) * | 2017-09-18 | 2018-10-30 | Bellus Health Cough Inc. | Selective P2X3 modulators |
| HU231206B1 (hu) | 2017-12-15 | 2021-10-28 | Richter Gedeon Nyrt. | Triazolobenzazepinek |
| KR20210009341A (ko) | 2018-05-15 | 2021-01-26 | 바이엘 악티엔게젤샤프트 | 신경 섬유 감작과 연관된 질환의 치료를 위한 1,3-티아졸-2-일 치환된 벤즈아미드 |
| MA52616A (fr) | 2018-05-15 | 2021-03-24 | Bayer Ag | Benzamides à substitution 1,3-thiazol-2-yl pour le traitement de maladies associées à la sensibilisation de fibres nerveuses |
| WO2020071530A1 (ja) | 2018-10-05 | 2020-04-09 | 塩野義製薬株式会社 | 慢性咳嗽治療用医薬 |
| WO2020074962A1 (en) * | 2018-10-10 | 2020-04-16 | Bellus Health Cough Inc. | Treatment of pruritus with p2x3 antagonists |
| CN113727716A (zh) * | 2019-02-25 | 2021-11-30 | 贝卢斯医疗咳嗽病公司 | 采用p2x3调节剂的治疗 |
| PE20220171A1 (es) * | 2019-04-05 | 2022-01-28 | Syngenta Crop Protection Ag | Compuestos de diazina-amida activos como pesticidas |
| US20220169629A1 (en) * | 2019-04-11 | 2022-06-02 | Syngenta Crop Protection Ag | Pesticidally active diazine-amide compounds |
| WO2020239953A1 (en) | 2019-05-31 | 2020-12-03 | Chiesi Farmaceutici S.P.A. | Pyridopyrimidines derivatives as p2x3 inhibitors |
| GEP20257823B (en) | 2019-05-31 | 2025-11-10 | Chiesi Farm Spa | Amino quinazoline derivatives as p2x3 inhibitors |
| EP3757103A1 (en) | 2019-06-27 | 2020-12-30 | Bayer AG | Analogues of 3-(5-methyl-1,3-thiazol-2-yl)-n-{(1r)-1-[2-(trifluoro-methyl)pyrimidin-5-yl]ethyl}benzamide for the treatment of neurogenic diseases |
| CN113082023B (zh) * | 2019-12-23 | 2024-03-01 | 武汉朗来科技发展有限公司 | P2x3抑制剂和p2x4抑制剂的药物组合及其应用 |
| CN114072399B (zh) * | 2020-05-25 | 2024-11-29 | 中国医药研究开发中心有限公司 | 芳甲酰胺类化合物及其制备方法和医药用途 |
| WO2022063205A1 (zh) * | 2020-09-24 | 2022-03-31 | 中国医药研究开发中心有限公司 | 芳基甲酰胺类化合物及其制备方法和医药用途 |
| IL301667A (en) * | 2020-09-30 | 2023-05-01 | Humanwell Healthcare Group Co Ltd | Benzamide compound and use thereof |
| CN116601149A (zh) | 2020-11-27 | 2023-08-15 | 奇斯药制品公司 | 作为p2x3抑制剂的氨基喹唑啉衍生物 |
| AU2021386684A1 (en) | 2020-11-27 | 2023-05-25 | Chiesi Farmaceutici S.P.A. | (aza)quinoline 4-amines derivatives as p2x3 inhibitors |
| KR20230113289A (ko) | 2020-11-27 | 2023-07-28 | 키에시 파르마슈티시 엣스. 피. 에이. | P2x3 억제제로서 프탈라진 유도체 |
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| WO2022253943A1 (en) | 2021-06-04 | 2022-12-08 | Bayer Aktiengesellschaft | Crystalline forms of 3-(5-methyl-1,3-thiazol-2-yl)-5-[(3r)-tetrahydrofuran-3-yloxy]-n-{(1r)-1-[2-(trifluoro-methyl)pyrimidin-5-yl]ethyl}-benzamide |
| WO2022253945A1 (en) | 2021-06-04 | 2022-12-08 | Bayer Aktiengesellschaft | Pharmaceutical dosage forms comprising 3-(5-methyl-1,3-thiazol-2-yl)-5-[(3r)-tetrahydrofuran-3-yloxy]-n-{(1r)-1-[2-(trifluoromethyl)pyrimidin-5-yl]ethyl}-benzamide |
| CN116396285A (zh) * | 2022-01-04 | 2023-07-07 | 上海华汇拓医药科技有限公司 | 氘代四氢呋喃类化合物制备及其应用 |
| US12024285B1 (en) | 2022-03-10 | 2024-07-02 | Skypad Tech, Inc. | Modular mobility system including thrusters movably connected to a support structure |
| WO2023185931A1 (zh) * | 2022-03-29 | 2023-10-05 | 人福医药集团股份公司 | 一种p2x3抑制剂化合物及其盐、多晶型和用途 |
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