UA113776C2 - Похідні піразолкарбоксаміду як модулятори рецепторів слідових амінів (taar) для застосування при лікуванні різних розладів, таких як депресія, діабет та хвороба паркінсона - Google Patents
Похідні піразолкарбоксаміду як модулятори рецепторів слідових амінів (taar) для застосування при лікуванні різних розладів, таких як депресія, діабет та хвороба паркінсонаInfo
- Publication number
- UA113776C2 UA113776C2 UAA201503288A UAA201503288A UA113776C2 UA 113776 C2 UA113776 C2 UA 113776C2 UA A201503288 A UAA201503288 A UA A201503288A UA A201503288 A UAA201503288 A UA A201503288A UA 113776 C2 UA113776 C2 UA 113776C2
- Authority
- UA
- Ukraine
- Prior art keywords
- substituted
- lower alkyl
- disorders
- halogen atom
- alkoxy
- Prior art date
Links
- 102000011829 Trace amine associated receptor Human genes 0.000 title abstract 3
- 108050002178 Trace amine associated receptor Proteins 0.000 title abstract 3
- BNYCHCAYYYRJSH-UHFFFAOYSA-N 1h-pyrazole-5-carboxamide Chemical class NC(=O)C1=CC=NN1 BNYCHCAYYYRJSH-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 15
- 125000003545 alkoxy group Chemical group 0.000 abstract 10
- 125000005843 halogen group Chemical group 0.000 abstract 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 4
- 208000035475 disorder Diseases 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 206010012601 diabetes mellitus Diseases 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- -1 substituted alkoxy halogen Chemical class 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 abstract 1
- 208000020925 Bipolar disease Diseases 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 208000017164 Chronobiology disease Diseases 0.000 abstract 1
- 208000032928 Dyslipidaemia Diseases 0.000 abstract 1
- 208000030814 Eating disease Diseases 0.000 abstract 1
- 208000019454 Feeding and Eating disease Diseases 0.000 abstract 1
- 208000017170 Lipid metabolism disease Diseases 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 208000028017 Psychotic disease Diseases 0.000 abstract 1
- 208000027520 Somatoform disease Diseases 0.000 abstract 1
- 238000010521 absorption reaction Methods 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 150000001412 amines Chemical class 0.000 abstract 1
- 230000036760 body temperature Effects 0.000 abstract 1
- 230000027288 circadian rhythm Effects 0.000 abstract 1
- WJJMNDUMQPNECX-UHFFFAOYSA-N dipicolinic acid Chemical group OC(=O)C1=CC=CC(C(O)=O)=N1 WJJMNDUMQPNECX-UHFFFAOYSA-N 0.000 abstract 1
- 235000014632 disordered eating Nutrition 0.000 abstract 1
- 230000004064 dysfunction Effects 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 230000013632 homeostatic process Effects 0.000 abstract 1
- 208000030159 metabolic disease Diseases 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 208000027753 pain disease Diseases 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 230000007958 sleep Effects 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 125000005415 substituted alkoxy group Chemical group 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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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
- A61P25/14—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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
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- A—HUMAN NECESSITIES
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- A61P25/24—Antidepressants
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- A—HUMAN NECESSITIES
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- 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
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- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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- A—HUMAN NECESSITIES
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- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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
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- 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
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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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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- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Psychiatry (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Addiction (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Child & Adolescent Psychology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Anesthesiology (AREA)
- Hospice & Palliative Care (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Epidemiology (AREA)
Abstract
Даний винахід належить до сполук формули, (I)деRявляє собою феніл, необов'язково заміщений атомом галогену, нижчим алкілом, нижчим циклоалкілом, нижчим алкокси, ціано, нижчим алкілом, заміщеним атомом галогену, нижчим алкілом, заміщеним гідрокси, нижчим алкокси, заміщеним атомом галогену, або нижчим алкокси, заміщеним гідрокси; або являє собою піридин-2, -3 або -4-іл, необов'язково заміщений атомом галогену, нижчим алкілом, нижчим циклоалкілом, ціано, нижчим алкілом, заміщеним атомом галогену, нижчим алкілом, заміщеним гідрокси, нижчим алкокси, нижчим алкокси, заміщеним атомом галогену, або нижчим алкокси, заміщеним гідроксилом; або являє собою піримідин-2, -4 або -5-іл, необов'язково заміщений атомом галогену, нижчим алкілом, нижчим циклоалкілом, нижчим алкілом, заміщеним гідрокси, або нижчим алкілом, заміщеним атомом галогену; або являє собою піразин-2-іл, необов'язково заміщений атомом галогену, нижчим алкілом, нижчим циклоалкілом, нижчим алкілом, заміщеним атомом галогену, нижчим алкілом, заміщеним гідрокси або ціано; або являє собою 2,2-дифторбензо[d][1,3]діоксол-5-іл, або являє собою тіазоліл, необов'язково заміщений нижчим алкілом, заміщеним атомом галогену;Rявляє собою атом водню або нижчий алкіл;Rявляє собою атом водню, аміно або нижчий алкіл;Z являє собою зв'язок -СН- або -О-;або до їх фармацевтично прийнятних солей приєднання кислоти.В даний час виявлено, що сполуки формули І мають високу спорідненість до рецепторів, асоційованих із слідовими амінами (TAAR; від англ. "trace amine associated receptors"), зокрема до ТААR1.Ці сполуки можна застосовувати для лікування депресії, тривожних розладів, біполярного розладу, синдрому дефіциту уваги і гіперактивності (СДУГ), розладів, обумовлених стресом, психотичних розладів, таких як шизофренія, неврологічних розладів, таких як хвороба Паркінсона, нейродегенеративих розладів, таких як хвороба Альцгеймера, епілепсії, мігрені, гіпертензії, зловживання речовинами і метаболічних розладів, таких як порушення харчування, діабет, ускладнення діабету, ожиріння, дисліпідемія, порушень поглинання енергії та асиміляції, розладів і дисфункції гомеостазу температури тіла, розладів сну і циркадного ритму та серцево-судинних розладів.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12184360 | 2012-09-14 | ||
| PCT/EP2013/068769 WO2014041007A1 (en) | 2012-09-14 | 2013-09-11 | Pyrazole carboxamide derivatives as taar modulators for use in the treatment of several disorders, such as depression, diabetes and parkinson's disease |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UA113776C2 true UA113776C2 (xx) | 2017-03-10 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UAA201503288A UA113776C2 (xx) | 2012-09-14 | 2013-09-11 | Похідні піразолкарбоксаміду як модулятори рецепторів слідових амінів (taar) для застосування при лікуванні різних розладів, таких як депресія, діабет та хвороба паркінсона |
Country Status (35)
| Country | Link |
|---|---|
| US (1) | US9487501B2 (uk) |
| EP (1) | EP2895477B1 (uk) |
| JP (2) | JP2015531782A (uk) |
| KR (1) | KR101706486B1 (uk) |
| CN (2) | CN104619700A (uk) |
| AR (1) | AR092537A1 (uk) |
| AU (1) | AU2013314388B2 (uk) |
| BR (1) | BR112015004511B1 (uk) |
| CA (1) | CA2882821C (uk) |
| CL (1) | CL2015000580A1 (uk) |
| CR (1) | CR20150087A (uk) |
| DK (1) | DK2895477T3 (uk) |
| EA (1) | EA026062B1 (uk) |
| ES (1) | ES2654653T3 (uk) |
| HK (2) | HK1206720A1 (uk) |
| HR (1) | HRP20171981T1 (uk) |
| HU (1) | HUE037689T2 (uk) |
| IL (1) | IL237332B (uk) |
| LT (1) | LT2895477T (uk) |
| MA (1) | MA37944B2 (uk) |
| MX (1) | MX363362B (uk) |
| MY (1) | MY178667A (uk) |
| NO (1) | NO2895477T3 (uk) |
| NZ (1) | NZ705154A (uk) |
| PE (1) | PE20150735A1 (uk) |
| PH (1) | PH12015500489A1 (uk) |
| PL (1) | PL2895477T3 (uk) |
| PT (1) | PT2895477T (uk) |
| RS (1) | RS56747B1 (uk) |
| SG (1) | SG11201501958QA (uk) |
| SI (1) | SI2895477T1 (uk) |
| TW (1) | TWI610926B (uk) |
| UA (1) | UA113776C2 (uk) |
| WO (1) | WO2014041007A1 (uk) |
| ZA (1) | ZA201501126B (uk) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6383860B2 (ja) * | 2014-07-30 | 2018-08-29 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | Ｔａａｒ調節因子としての６−アミノ−５，６，７，８−テトラヒドロナフタレン−２−イル又は３−アミノクロマン−７−イル誘導体 |
| BR112018015389B1 (pt) | 2016-03-17 | 2023-12-19 | F. Hoffmann-La Roche Ag | Derivado de 5-etil-4-metil-pirazol-3-carboxamida, seu processo de fabricação, preparação farmacêutica oral e uso |
| CN110291084A (zh) | 2016-12-15 | 2019-09-27 | 加利福尼亚大学董事会 | 用于治疗癌症的组合物和方法 |
| SG11202110401WA (en) | 2019-04-09 | 2021-10-28 | Hoffmann La Roche | Hexahydro-1h-pyrazino[1,2-a]pyrazine compounds for the treatment of autoimmune disease |
| WO2022262855A1 (zh) * | 2021-06-18 | 2022-12-22 | 上海拓界生物医药科技有限公司 | 一种malt1抑制剂及其制备方法和用途 |
| CN116236478A (zh) * | 2022-12-27 | 2023-06-09 | 浙江大学 | 芳香杂环甲酰胺类化合物的应用 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| GB9425211D0 (en) | 1994-12-14 | 1995-02-15 | Ucb Sa | Substituted 1H-imidazoles |
| GB9520150D0 (en) | 1995-10-03 | 1995-12-06 | Orion Yhtymae Oy | New imidazole derivatives |
| US6841684B2 (en) | 1997-12-04 | 2005-01-11 | Allergan, Inc. | Imidiazoles having reduced side effects |
| EP2121641B1 (en) | 2007-02-15 | 2014-09-24 | F. Hoffmann-La Roche AG | 2-aminooxazolines as taar1 ligands |
| US9452980B2 (en) * | 2009-12-22 | 2016-09-27 | Hoffmann-La Roche Inc. | Substituted benzamides |
| WO2012063896A1 (ja) * | 2010-11-11 | 2012-05-18 | 第一三共株式会社 | 新規ピラゾールアミド誘導体 |
| US9073911B2 (en) * | 2011-06-09 | 2015-07-07 | Hoffmann-La Roche Inc. | Pyrazole derivatives |
| US9029370B2 (en) * | 2011-06-10 | 2015-05-12 | Hoffmann-La Roche Inc. | Substituted benzamide derivatives |
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