JP6814814B2 - Ｔａａｒのアゴニストとしての活性を有する５−エチル−４−メチル−ピラゾール−３−カルボキサミド誘導体 - Google Patents
Ｔａａｒのアゴニストとしての活性を有する５−エチル−４−メチル−ピラゾール−３−カルボキサミド誘導体 Download PDFInfo
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- JP6814814B2 JP6814814B2 JP2018545336A JP2018545336A JP6814814B2 JP 6814814 B2 JP6814814 B2 JP 6814814B2 JP 2018545336 A JP2018545336 A JP 2018545336A JP 2018545336 A JP2018545336 A JP 2018545336A JP 6814814 B2 JP6814814 B2 JP 6814814B2
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- IIBXKZGDWYLRKI-VWOUQIAPSA-N CC/C(/N)=C(\C)/C(C(Nc1ccc([C@@H]2OCCNC2)cc1)=O)=N Chemical compound CC/C(/N)=C(\C)/C(C(Nc1ccc([C@@H]2OCCNC2)cc1)=O)=N IIBXKZGDWYLRKI-VWOUQIAPSA-N 0.000 description 1
- UTHLHTHTBNRBHX-NNJIEVJOSA-N CC1([C@@H]2OCCNC2)C=CC(NC(c(cn2)ccc2OCC(F)(F)F)=O)=CC1 Chemical compound CC1([C@@H]2OCCNC2)C=CC(NC(c(cn2)ccc2OCC(F)(F)F)=O)=CC1 UTHLHTHTBNRBHX-NNJIEVJOSA-N 0.000 description 1
- 0 CCC(N)=C(C)C(C(Nc1ccc([C@@]2OCCN(*)C2)cc1)=O)=[N+] Chemical compound CCC(N)=C(C)C(C(Nc1ccc([C@@]2OCCN(*)C2)cc1)=O)=[N+] 0.000 description 1
- XHHXGKRFUPEPFM-OAHLLOKOSA-N CCc1c(C)c(C(Nc2ccc([C@@H]3OCCNC3)cc2)=O)n[nH]1 Chemical compound CCc1c(C)c(C(Nc2ccc([C@@H]3OCCNC3)cc2)=O)n[nH]1 XHHXGKRFUPEPFM-OAHLLOKOSA-N 0.000 description 1
- JEQFKXKYXLHVQE-CQSZACIVSA-N Cc1nc(C(Nc2ccc([C@@H]3OCCNC3)cc2)=O)c[s]1 Chemical compound Cc1nc(C(Nc2ccc([C@@H]3OCCNC3)cc2)=O)c[s]1 JEQFKXKYXLHVQE-CQSZACIVSA-N 0.000 description 1
- QZQLOJFUTYSQRK-CQSZACIVSA-N O=C(c(cn1)ccc1Cl)Nc1ccc([C@@H]2OCCNC2)cc1 Chemical compound O=C(c(cn1)ccc1Cl)Nc1ccc([C@@H]2OCCNC2)cc1 QZQLOJFUTYSQRK-CQSZACIVSA-N 0.000 description 1
- FMARCCRRUGZDDU-GOSISDBHSA-N O=C(c1c[s]c(-c2ccccc2)n1)Nc1ccc([C@@H]2OCCNC2)cc1 Chemical compound O=C(c1c[s]c(-c2ccccc2)n1)Nc1ccc([C@@H]2OCCNC2)cc1 FMARCCRRUGZDDU-GOSISDBHSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and 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
- A61K31/535—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/282—Organic compounds, e.g. fats
- A61K9/2826—Sugars or sugar alcohols, e.g. sucrose; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
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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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
-
- 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
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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- 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
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- 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
- A61P3/04—Anorexiants; Antiobesity agents
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- 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
- A61P3/06—Antihyperlipidemics
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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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
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Child & Adolescent Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Addiction (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16160790.8 | 2016-03-17 | ||
| EP16160790 | 2016-03-17 | ||
| PCT/EP2017/055885 WO2017157873A1 (en) | 2016-03-17 | 2017-03-14 | 5-ethyl-4-methyl-pyrazole-3-carboxamide derivative having activity as agonist of taar |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019512469A JP2019512469A (ja) | 2019-05-16 |
| JP2019512469A5 JP2019512469A5 (cg-RX-API-DMAC7.html) | 2020-12-24 |
| JP6814814B2 true JP6814814B2 (ja) | 2021-01-20 |
Family
ID=55542549
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018545336A Active JP6814814B2 (ja) | 2016-03-17 | 2017-03-14 | Ｔａａｒのアゴニストとしての活性を有する５−エチル−４−メチル−ピラゾール−３−カルボキサミド誘導体 |
Country Status (33)
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112022000181A2 (pt) | 2019-07-11 | 2022-02-22 | Hoffmann La Roche | Processo para a preparação de derivados de pirazol substituídos |
| JP2023517729A (ja) | 2020-03-19 | 2023-04-26 | エフ． ホフマン－ラ ロシュ アーゲー | Ｔａａｒ１アゴニストの塩形態および結晶形態 |
| WO2023079128A1 (en) | 2021-11-08 | 2023-05-11 | F. Hoffmann-La Roche Ag | Catalytic hydrogenation of aromatic nitro compounds |
| CN114288304A (zh) * | 2021-12-31 | 2022-04-08 | 江苏海洋大学 | 一种抗精神分裂症组合物及其应用 |
| AR129909A1 (es) | 2022-07-15 | 2024-10-09 | Hoffmann La Roche | Cetorreductasa mutante con mayor actividad de cetorreductasa así como métodos y usos de esta |
| CN119654138A (zh) | 2022-08-12 | 2025-03-18 | 豪夫迈·罗氏有限公司 | 包含5-乙基-4-甲基-n-[4-[(2s)吗啉-2-基]苯基]-1h-吡唑-3-甲酰胺的药物组合物 |
| EP4568654A1 (en) * | 2022-08-12 | 2025-06-18 | F. Hoffmann-La Roche AG | Use of co-processed excipients in continuous manufacturing of solid dosage forms |
| TW202440563A (zh) * | 2022-11-28 | 2024-10-16 | 美商住友製藥美國公司 | 2-苯基嗎啉與2-苯基(硫代)嗎啉化合物及其用途 |
| WO2024222860A1 (zh) * | 2023-04-28 | 2024-10-31 | 江苏豪森药业集团有限公司 | 一种吗啉杂环类化合物的盐及其制备方法和应用 |
| WO2024258900A2 (en) * | 2023-06-13 | 2024-12-19 | University Of Georgia Research Foundation, Inc. | Plasmodium falciparum blood stage inhibitors |
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| US2731471A (en) | 1956-01-17 | Nxg hi | ||
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| DE842065C (de) | 1950-07-30 | 1952-06-23 | Bayer Ag | Verfahren zur Herstellung stickstoffhaltiger heterocyclischer Verbindungen |
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| FR1355049A (fr) | 1962-04-12 | 1964-03-13 | Merck Ag E | Agent pour le traitement préalable de la peau en vue du rasage |
| DE1150180B (de) | 1962-04-12 | 1963-06-12 | Merck Ag E | Mittel zur Vorbehandlung der Haut fuer die Rasur |
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