RU2018134262A - Производное 5-этил-4-метил-пиразол-3-карбоксамида, обладающее активностью агониста taar - Google Patents
Производное 5-этил-4-метил-пиразол-3-карбоксамида, обладающее активностью агониста taar Download PDFInfo
- Publication number
- RU2018134262A RU2018134262A RU2018134262A RU2018134262A RU2018134262A RU 2018134262 A RU2018134262 A RU 2018134262A RU 2018134262 A RU2018134262 A RU 2018134262A RU 2018134262 A RU2018134262 A RU 2018134262A RU 2018134262 A RU2018134262 A RU 2018134262A
- Authority
- RU
- Russia
- Prior art keywords
- disorders
- formula
- paragraphs
- disease
- compound
- Prior art date
Links
- SONZLIIHTSKJMC-UHFFFAOYSA-N 5-ethyl-4-methyl-1h-pyrazole-3-carboxamide Chemical class CCC=1NN=C(C(N)=O)C=1C SONZLIIHTSKJMC-UHFFFAOYSA-N 0.000 title 1
- 102000011829 Trace amine associated receptor Human genes 0.000 title 1
- 108050002178 Trace amine associated receptor Proteins 0.000 title 1
- 239000000556 agonist Substances 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
- 208000035475 disorder Diseases 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 11
- 208000020925 Bipolar disease Diseases 0.000 claims 5
- 201000000980 schizophrenia Diseases 0.000 claims 4
- 208000024827 Alzheimer disease Diseases 0.000 claims 3
- 208000019901 Anxiety disease Diseases 0.000 claims 3
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 3
- 206010012335 Dependence Diseases 0.000 claims 3
- 208000002249 Diabetes Complications Diseases 0.000 claims 3
- 206010012655 Diabetic complications Diseases 0.000 claims 3
- 208000032928 Dyslipidaemia Diseases 0.000 claims 3
- 208000030814 Eating disease Diseases 0.000 claims 3
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 3
- 206010020772 Hypertension Diseases 0.000 claims 3
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 3
- 208000019695 Migraine disease Diseases 0.000 claims 3
- 208000008589 Obesity Diseases 0.000 claims 3
- 208000018737 Parkinson disease Diseases 0.000 claims 3
- 238000010521 absorption reaction Methods 0.000 claims 3
- 230000009045 body homeostasis Effects 0.000 claims 3
- 206010012601 diabetes mellitus Diseases 0.000 claims 3
- 235000014632 disordered eating Nutrition 0.000 claims 3
- 206010015037 epilepsy Diseases 0.000 claims 3
- 206010027599 migraine Diseases 0.000 claims 3
- 235000020824 obesity Nutrition 0.000 claims 3
- 208000019116 sleep disease Diseases 0.000 claims 3
- 201000009032 substance abuse Diseases 0.000 claims 3
- 231100000736 substance abuse Toxicity 0.000 claims 3
- 208000011117 substance-related disease Diseases 0.000 claims 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 208000017164 Chronobiology disease Diseases 0.000 claims 2
- 208000020401 Depressive disease Diseases 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- XHHXGKRFUPEPFM-OAHLLOKOSA-N 5-ethyl-4-methyl-N-[4-[(2S)-morpholin-2-yl]phenyl]-1H-pyrazole-3-carboxamide Chemical compound C(C)C1=C(C(=NN1)C(=O)NC1=CC=C(C=C1)[C@H]1CNCCO1)C XHHXGKRFUPEPFM-OAHLLOKOSA-N 0.000 claims 1
- 208000013200 Stress disease Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 230000006399 behavior Effects 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 208000028683 bipolar I disease Diseases 0.000 claims 1
- 208000025307 bipolar depression Diseases 0.000 claims 1
- 238000003776 cleavage reaction Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 150000002780 morpholines Chemical class 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000033764 rhythmic process Effects 0.000 claims 1
- 230000007017 scission Effects 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
Classifications
-
- 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
-
- 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
- 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
- A61P25/06—Antimigraine agents
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (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)
Claims (17)
1. Морфолиновое производное формулы
и его фармацевтически приемлемая соль присоединения кислоты.
2. Соединение формулы I, которое представляет собой 5-этил-4-метил-N-[4-[(2S)морфолин-2-ил]фенил]-1Н-пиразол-3-карбоксамид.
3. Способ получения соединения формулы I согласно пп. 1 и 2, включающий
а) отщепление N-защитной группы (PG) у соединений формулы
с образованием соединения формулы
где PG является N-защитной группой, выбранной из -С(O)O-трет-бутила (ВОС), и,
при желании, превращение полученных соединений в фармацевтически приемлемые соли присоединения кислоты.
4. Соединение формулы I согласно пп. 1 и 2 для применения в качестве терапевтически активного вещества.
5. Соединение формулы I по пп. 1 и 2 для применения в лечении депрессии, тревожных расстройств, биполярного расстройства, синдрома гиперактивности с дефицитом внимания (СГДВ), связанных со стрессом расстройств, шизофрении, болезни Паркинсона, болезни Альцгеймера, эпилепсии, мигрени, гипертензии, злоупотребления веществами, аддикции, нарушений пищевого поведения, диабета, диабетических осложнений, ожирения, дислипидемии, нарушений поглощения энергии и ассимиляции, расстройств и нарушения гомеостаза температуры тела, расстройств сна и циркадного ритма и сердечно-сосудистых расстройств.
6. Соединение формулы I согласно пп. 1 и 2 для применения в лечении шизофрении, биполярного расстройства или депрессии.
7. Фармацевтическая композиция, содержащая соединение формулы I согласно пп. 1 или 2 и фармацевтически приемлемые эксципиенты.
8. Применение соединения формулы I согласно пп. 1 или 2 для изготовления лекарственного средства для лечения депрессии, тревожных расстройств, биполярного расстройства, синдрома гиперактивности с дефицитом внимания (СГДВ), связанных со стрессом расстройств, шизофрении, болезни Паркинсона, болезни Альцгеймера, эпилепсии, мигрени, гипертензии, злоупотребления веществами, аддикции, нарушений пищевого поведения, диабета, диабетических осложнений, ожирения, дислипидемии, нарушений поглощения энергии и ассимиляции, расстройств и нарушения гомеостаза температуры тела, расстройств сна и циркадного ритма и сердечно-сосудистых расстройств.
9. Способ лечения депрессии, тревожных расстройств, биполярного расстройства, синдрома гиперактивности с дефицитом внимания (СГДВ), связанных со стрессом расстройств, шизофрении, болезни Паркинсона, болезни Альцгеймера, эпилепсии, мигрени, гипертензии, злоупотребления веществами, аддикции, нарушений пищевого поведения, диабета, диабетических осложнений, ожирения, дислипидемии, нарушений поглощения энергии и ассимиляции, расстройств и нарушения гомеостаза температуры тела, расстройств сна и циркадного ритма и сердечно-сосудистых расстройств, включающий введение эффективного количества соединения формулы I согласно пп. 1 или 2.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16160790 | 2016-03-17 | ||
| EP16160790.8 | 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 |
|---|---|
| RU2018134262A true RU2018134262A (ru) | 2020-04-17 |
| RU2018134262A3 RU2018134262A3 (ru) | 2020-04-17 |
| RU2731095C2 RU2731095C2 (ru) | 2020-08-28 |
Family
ID=55542549
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2018134262A RU2731095C2 (ru) | 2016-03-17 | 2017-03-14 | Производное 5-этил-4-метил-пиразол-3-карбоксамида, обладающее активностью агониста taar |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US10508107B2 (ru) |
| EP (2) | EP3430010B1 (ru) |
| JP (1) | JP6814814B2 (ru) |
| KR (2) | KR102537050B1 (ru) |
| CN (1) | CN108713019B (ru) |
| AR (1) | AR107878A1 (ru) |
| AU (1) | AU2017234042B2 (ru) |
| BR (1) | BR112018015389B1 (ru) |
| CA (1) | CA3013696C (ru) |
| CL (1) | CL2018002583A1 (ru) |
| CO (1) | CO2018007515A2 (ru) |
| CR (1) | CR20180443A (ru) |
| DK (1) | DK3430010T3 (ru) |
| ES (1) | ES2819830T3 (ru) |
| HR (1) | HRP20201405T1 (ru) |
| HU (1) | HUE050986T2 (ru) |
| IL (1) | IL260473B (ru) |
| LT (1) | LT3430010T (ru) |
| MA (2) | MA53755A (ru) |
| MX (1) | MX377836B (ru) |
| MY (1) | MY195528A (ru) |
| PE (1) | PE20181446A1 (ru) |
| PH (1) | PH12018501588A1 (ru) |
| PL (1) | PL3430010T3 (ru) |
| PT (1) | PT3430010T (ru) |
| RS (1) | RS60825B1 (ru) |
| RU (1) | RU2731095C2 (ru) |
| SG (2) | SG10201913878YA (ru) |
| SI (1) | SI3430010T1 (ru) |
| TW (1) | TWI634117B (ru) |
| UA (1) | UA122881C2 (ru) |
| WO (1) | WO2017157873A1 (ru) |
| ZA (1) | ZA201804943B (ru) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2020310539A1 (en) * | 2019-07-11 | 2022-01-06 | F. Hoffmann-La Roche Ag | Process for the preparation of substituted pyrazole derivatives |
| KR20220155575A (ko) * | 2020-03-19 | 2022-11-23 | 에프. 호프만-라 로슈 아게 | Taar1 작용제의 염 및 결정질 형태 |
| AR127592A1 (es) | 2021-11-08 | 2024-02-07 | Hoffmann La Roche | Hidrogenación catalítica de nitrocompuestos aromáticos |
| 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 |
| 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 |
| JP2025526086A (ja) | 2022-08-12 | 2025-08-07 | エフ． ホフマン－ラ ロシュ アーゲー | ５－エチル－４－メチル－ｎ－［４－［（２ｓ）モルホリン－２－イル］フェニル］－１ｈ－ピラゾール－３－カルボキサミドを含む医薬組成物 |
| WO2024118488A1 (en) * | 2022-11-28 | 2024-06-06 | Sumitomo Pharma America, Inc. | 2-phenylmorpholine and 2-phenyl(thio)morpholine compounds and uses thereof |
| CN121311474A (zh) * | 2023-04-28 | 2026-01-09 | 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 |
| AU2024305453A1 (en) * | 2023-06-13 | 2026-01-08 | Northeastern University | Plasmodium falciparum blood stage inhibitors |
Family Cites Families (180)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2731471A (en) | 1956-01-17 | Nxg hi | ||
| FR6551E (fr) | 1905-07-27 | 1906-12-17 | Carlo Chiesa | Séchoir à tambour rotatif, démontable et transportable, et fonctionnant à ciel ouvert, pour cocons, céréales, etc. |
| US2161938A (en) | 1934-07-31 | 1939-06-13 | Soc Of Chemical Ind | Imidazolines |
| US2457047A (en) | 1946-02-13 | 1948-12-21 | Monsanto Chemicals | 2-(2'-thenyl)-4, 5-dihydroimidazoles and process for making the same |
| DE842065C (de) | 1950-07-30 | 1952-06-23 | Bayer Ag | Verfahren zur Herstellung stickstoffhaltiger heterocyclischer Verbindungen |
| US2778836A (en) | 1954-04-02 | 1957-01-22 | Union Chimique Belge Sa | Substituted 2-methyl-delta2 imidazolines |
| US2744910A (en) | 1955-06-27 | 1956-05-08 | Bristol Lab Inc | 2-(ortho-benzylbenzyl)-imidazoline and acid addition salts |
| US2744909A (en) | 1955-06-27 | 1956-05-08 | Bristol Lab Inc | 2-(ortho-phenylbenzyl) imidazoline and acid addition salts |
| US2919274A (en) | 1957-09-17 | 1959-12-29 | Sahyun Melville | Amidines |
| GB877306A (en) | 1958-04-21 | 1961-09-13 | Pfizer & Co C | Halogenated derivatives of tetrahydro-1-naphthyl cyclic amidines |
| DE1083803B (de) | 1958-05-30 | 1960-06-23 | Bayer Ag | Verfahren zur Herstellung von Derivaten der Anthranil-N-carbonsaeure |
| DE1121054B (de) | 1960-11-23 | 1962-01-04 | Merck Ag E | Verfahren zur Herstellung eines neuen Imidazolinderivates und dessen Saeureadditionssalzen |
| US3190802A (en) | 1961-10-09 | 1965-06-22 | Boehringer Sohn Ingelheim | Shaving composition and method of using same |
| 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 |
| US3459763A (en) | 1966-01-25 | 1969-08-05 | Geigy Chem Corp | Certain amino imidazole derivatives |
| ES323985A1 (es) | 1966-02-26 | 1966-12-16 | Blade Pique Juan | Procedimiento para la obtenciën de derivados del imidazol |
| FI48082C (fi) | 1966-08-05 | 1974-06-10 | Boehringer Sohn Ingelheim | Menetelmä uusien verenpainetta alentavien 2-aryylihydratsino-imidatsol iinien-(2) valmistamiseksi |
| US3377247A (en) | 1967-04-28 | 1968-04-09 | Dow Chemical Co | Antidepressant method |
| US3586695A (en) | 1968-01-26 | 1971-06-22 | Dow Chemical Co | Substituted imidazolinyl indoles |
| US3577415A (en) | 1968-12-23 | 1971-05-04 | Robins Co Inc A H | 1-substituted-3-substituted phenoxypyrrolidines |
| US3577428A (en) | 1969-04-14 | 1971-05-04 | Colgate Palmolive Co | 2-amino-4-aryloxyalkyl-4-alkyl-2-oxazolines |
| BE754935A (fr) | 1969-08-13 | 1971-02-17 | Hoechst Ag | 2-(thienyl-3'-amino)-1,3-diazacycloalcenes et leur preparation |
| US3622579A (en) | 1969-08-28 | 1971-11-23 | Boehringer Sohn Ingelheim | Derivatives of 2-anilino-1,3-diazacyclopentene-(2) |
| US3818094A (en) | 1969-08-28 | 1974-06-18 | Boehringer Sohn Ingelheim | Hypotensive pharmaceutical compositions containing certain 2-anilino-1,3-diazacyclopentenes-(2) |
| US3660423A (en) | 1970-02-13 | 1972-05-02 | Dow Chemical Co | 2-(substituted benzyl)methyl-2-imidazolines |
| GB1333471A (en) | 1971-01-27 | 1973-10-10 | Labaz | Imidazoline derivatives and process for preparing the same |
| DE2123246C2 (de) | 1971-05-11 | 1982-11-25 | Basf Ag, 6700 Ludwigshafen | 6-[p-(β-Phenyläthylaminoacetylamino)-phenyl]-4,5-dihydropyridazon-(3) |
| DE2123243A1 (de) | 1971-05-11 | 1972-11-16 | Hupfauf, Lorenz, 8510 Fürth | Verfahren und Vorrichtung zum Schneiden oder Falten von Bahnen aus Papier-, Zellstoff od. dgl |
| DE2253555A1 (de) | 1972-11-02 | 1974-05-09 | Hoechst Ag | Oxazolo-pyrimidine und verfahren zu ihrer herstellung |
| US3981814A (en) | 1973-09-18 | 1976-09-21 | Givaudan Corporation | Bacteriostatic substituted benzanilide compositions and methods for their use |
| CH609558A5 (en) | 1973-09-18 | 1979-03-15 | Givaudan & Cie Sa | Antibacterial composition |
| US4125620A (en) | 1974-10-01 | 1978-11-14 | Boehringer Ingelheim Gmbh | 2-[(2',6'-Disubstituted-phenyl)-imino]-imidazolidines and salts thereof |
| DE2446758C3 (de) | 1974-10-01 | 1979-01-04 | C.H. Boehringer Sohn, 6507 Ingelheim | 2-(2-Fluor-6-trifluormethylphenylimino)-imidazolidin, dessen Säureadditionssalze, Verfahren zur Herstellung dieser Verbindungen und deren Verwendung bei der Bekämpfung der Hypertonie |
| US3992403A (en) | 1975-05-30 | 1976-11-16 | Schering Corporation | 2-Imidazolines and their use as hypoglycemic agents |
| GB1538097A (en) | 1976-01-26 | 1979-01-10 | Lafon Labor | Substituted phenyl-amidines |
| DE2849537C2 (de) | 1978-11-15 | 1983-03-17 | Beiersdorf Ag, 2000 Hamburg | Substituierte 5-(2-Imidazolin-2-yl)-aminopyrimidine, Verfahren zu deren Herstellung und diese enthaltende Arzneimittel |
| US4323570A (en) | 1978-11-15 | 1982-04-06 | Beiersdorf Aktiengesellschaft | Substituted aminopyrimidines |
| AU518569B2 (en) | 1979-08-07 | 1981-10-08 | Farmos-Yhtyma Oy | 4-benzyl- and 4-benzoyl imidazole derivatives |
| US4311840A (en) | 1980-11-13 | 1982-01-19 | E. R. Squibb & Sons, Inc. | 2,3,6,7-Tetrahydro-2-thioxo-4H-oxazolo[3,2-a]-1,3,5 triazin-4-ones |
| US4735959A (en) | 1981-01-10 | 1988-04-05 | Dr. Karl Thomae Gmbh | Carboxylic acid amides and pharmaceutical compositions containing them |
| DE3133887A1 (de) | 1981-08-27 | 1983-03-10 | Bayer Ag, 5090 Leverkusen | 2-arylhydrazino-2-imidazoline, deren acylderivate, verfahren zu ihrer herstellung und ihre verwendung zur bekaempfung von endo- und ektoparasiten |
| ES8405770A1 (es) | 1982-01-27 | 1984-06-16 | Pfizer | Un procedimiento para la preparacion de una composicion ectoparasiticida, especialmente acaricida, o antihelmintica. |
| DE3302021A1 (de) | 1983-01-22 | 1984-07-26 | Basf Ag, 6700 Ludwigshafen | 6-aryl-4,5-dihydro-3(2h)-pyridazinone, ihre herstellung und verwendung |
| US4540705A (en) | 1983-03-14 | 1985-09-10 | Sterling Drug Inc. | Antidepressant imidazolines and related compounds |
| DE3583900D1 (de) | 1984-06-06 | 1991-10-02 | Abbott Lab | Adrenergische verbindungen. |
| DK302185A (da) | 1984-07-05 | 1986-01-06 | Rolland Sa A | 2-amino-oxazoliner samt fremgangsmaade til deres fremstilling |
| JPS61233678A (ja) | 1985-04-09 | 1986-10-17 | Maruko Seiyaku Kk | ベンジルピペラジン誘導体 |
| US4665095A (en) | 1985-12-11 | 1987-05-12 | Abbott Laboratories | Use of 2-[(3,5-dihalo-4-aminobenzyl)]imidazolines to stimulate alpha-1 adrenergic receptors and to treat nasal congestion |
| GB2215206B (en) | 1988-02-29 | 1991-07-03 | Farmos Oy | 4-substituted imidazole derivatives useful in perioperative care |
| DE3830054A1 (de) | 1988-09-03 | 1990-03-15 | Boehringer Mannheim Gmbh | Phenylamide - verfahren zu ihrer herstellung sowie diese verbindungen enthaltende arzneimittel |
| FR2645860B1 (fr) | 1989-04-14 | 1991-07-26 | Sarget Lab | Nouvelles aryloxymethyl-5 amino-2 oxazolines, syntheses et applications therapeutiques |
| FI894911A0 (fi) | 1989-10-17 | 1989-10-17 | Farmos Oy | En terapeutiskt vaerdefull foerening. |
| DE69127002T2 (de) | 1990-01-31 | 1997-11-20 | Fuji Photo Film Co Ltd | Farbphotographisches Silberhalogenidmaterial |
| CA2211325C (en) | 1993-10-13 | 2006-08-15 | H. Joseph Horacek | Extended release clonidine formulation |
| EP0661266A1 (en) | 1993-12-27 | 1995-07-05 | Toa Eiyo Ltd. | Substituted cyclic amine compounds as 5HT2 antagonists |
| GB9425211D0 (en) | 1994-12-14 | 1995-02-15 | Ucb Sa | Substituted 1H-imidazoles |
| DE19514579A1 (de) | 1995-04-20 | 1996-10-24 | Boehringer Ingelheim Kg | Verwendung von alpha¶1¶¶L¶-Agonisten zur Behandlung der Harninkontinenz |
| US5610174A (en) | 1995-06-02 | 1997-03-11 | Synaptic Pharmaceutical Corporation | Use of α1A -selective adrenoceptor agonists for the treatment of urinary incontinence |
| DE69612698T2 (de) | 1995-06-09 | 2001-12-06 | F. Hoffmann-La Roche Ag, Basel | Pyrimidindion-, Pyrimidintrion-, Triazindion-Derivate als alpha-1-adrenergische Rezeptorantagonisten |
| GB9520150D0 (en) | 1995-10-03 | 1995-12-06 | Orion Yhtymae Oy | New imidazole derivatives |
| SK20199A3 (en) | 1996-08-15 | 2000-03-13 | Schering Corp | Ether muscarinic antagonists |
| US5969137A (en) | 1996-09-19 | 1999-10-19 | Virginia Commonwealth University | Benzylamidine derivatives with serotonin receptor binding activity |
| GB9625145D0 (en) | 1996-12-03 | 1997-01-22 | Smithkline Beecham Plc | Novel compounds |
| ZA981029B (en) | 1997-02-11 | 1999-08-10 | Lilly Co Eli | Pharmaceutical agents. |
| US5866579A (en) | 1997-04-11 | 1999-02-02 | Synaptic Pharmaceutical Corporation | Imidazole and imidazoline derivatives and uses thereof |
| AR016817A1 (es) | 1997-08-14 | 2001-08-01 | Smithkline Beecham Plc | Derivados de fenilurea o feniltiourea, procedimiento para su preparacion, coleccion de compuestos, compuestos intermediarios, composicion farmaceutica,metodo de tratamiento y uso de dichos compuestos para la manufactura de un medicamento |
| US6184242B1 (en) | 1997-09-04 | 2001-02-06 | Syntex Usa (Llc) | 2-(substituted-phenyl)amino-imidazoline derivatives |
| PL341009A1 (en) | 1997-12-04 | 2001-03-12 | Allergan Sales | Substitute derivatives of imidazole exhibiting agonist-like activity in respect to adrenergic alpha 2b or 2b/2c receptors |
| US6841684B2 (en) | 1997-12-04 | 2005-01-11 | Allergan, Inc. | Imidiazoles having reduced side effects |
| CA2315226A1 (en) | 1997-12-19 | 1999-07-01 | Eli Lilly And Company | Hypoglycemic imidazoline compounds |
| CA2328973A1 (en) | 1998-04-23 | 1999-10-28 | Akio Ojida | Naphthalene derivatives, their production and use |
| DE19826517B4 (de) | 1998-06-15 | 2006-03-23 | Baxter Healthcare S.A. | Verfahren zur Herstellung von Filmtabletten mit Cyclophosphamid als Wirkstoff und daraus hergestellte Cyclophosphamid-Filmtablette |
| ES2150378B1 (es) | 1998-08-07 | 2001-07-01 | Esteve Labor Dr | Empleo de derivados de aril(o heteroaril)azolilcarbinoles en la elaboracion de un medicamento para el tratamiento de los trastornos mediados por un exceso de substancia p. |
| CA2246027A1 (en) | 1998-08-27 | 2000-02-27 | Virginia Commonwealth University | Benzylamidine derivatives with serotonin receptor binding activity |
| JP4689042B2 (ja) | 1998-11-04 | 2011-05-25 | 明治製菓株式会社 | ピコリン酸アミド誘導体、それを有効成分として含有する有害生物防除剤 |
| GB9826412D0 (en) | 1998-12-03 | 1999-01-27 | Glaxo Group Ltd | Chemical compounds |
| US6331541B1 (en) | 1998-12-18 | 2001-12-18 | Soo S. Ko | N-ureidoalkyl-piperidines as modulators of chemokine receptor activity |
| EP1161240B1 (en) | 1998-12-18 | 2005-08-17 | Bristol-Myers Squibb Pharma Company | N-ureidoalkyl-piperidines as modulators of chemokine receptor activity |
| US6777428B1 (en) | 1999-02-10 | 2004-08-17 | Eli Lilly And Company | 5-HT1f agonist |
| CA2361819A1 (en) | 1999-03-17 | 2000-09-21 | Astrazeneca Ab | Amide derivatives |
| ATE306481T1 (de) | 1999-05-12 | 2005-10-15 | Ortho Mcneil Pharm Inc | Pyrazolecarboxamide zur behandlung von fettleibigkeit und anderen erkrankungen |
| US6355660B1 (en) | 1999-07-20 | 2002-03-12 | Dow Agrosciences Llc | Fungicidal heterocyclic aromatic amides and their compositions, methods of use and preparation |
| PE20010781A1 (es) | 1999-10-22 | 2001-08-08 | Takeda Chemical Industries Ltd | Compuestos 1-(1h-imidazol-4-il)-1-(naftil-2-sustituido)etanol, su produccion y utilizacion |
| JP2001151742A (ja) | 1999-11-26 | 2001-06-05 | Mitsui Chemicals Inc | アニリド誘導体及びそれを含有する抗不整脈剤 |
| FR2802533B1 (fr) | 1999-12-17 | 2002-02-15 | Sanofi Synthelabo | Phenoxypropanolamines, leur preparation et leur application en therapeutique |
| JP2001302643A (ja) | 2000-04-21 | 2001-10-31 | Suntory Ltd | 環状アミジン化合物 |
| JO2654B1 (en) | 2000-09-04 | 2012-06-17 | شركة جانسين فارماسوتيكا ان. في | Multiple aryl caroxa amides are useful as lipid - lowering agents |
| CA2422288A1 (en) | 2000-09-12 | 2002-03-21 | Oregon Health & Science University | Novel mammalian receptor genes and uses |
| EP1339694B1 (en) | 2000-11-14 | 2005-09-21 | F. Hoffmann-La Roche Ag | Substituted 2-phenylaminoimidazoline phenyl ketone derivatives as ip antagonists |
| US7141590B2 (en) | 2000-12-29 | 2006-11-28 | Ucb Sa | Pharmaceutical uses and synthesis of nicotinanilide-N-oxides |
| CA2435829A1 (en) | 2001-01-25 | 2002-08-01 | Guilford Pharmaceuticals Inc. | Trisubstituted carbocyclic cyclophilin binding compounds and their use |
| US7429593B2 (en) | 2001-09-14 | 2008-09-30 | Shionogi & Co., Ltd. | Utilities of amide compounds |
| IL147921A0 (en) | 2002-01-31 | 2002-08-14 | Abdulrazik Mohammad | A method for treating central nervous system disorders by ocular dosing |
| US7662826B2 (en) | 2002-04-23 | 2010-02-16 | Shionogi & Co., Ltd. | Pyrazolo [1,5-a] pyrimidine derivative and nad (p) h oxidase inhibitor containing the same |
| TW200930291A (en) | 2002-04-29 | 2009-07-16 | Bayer Cropscience Ag | Pesticidal heterocycles |
| US7202244B2 (en) | 2002-05-29 | 2007-04-10 | Millennium Pharmaceuticals, Inc. | Chk-1 inhibitors |
| UA77536C2 (en) | 2002-07-03 | 2006-12-15 | Lundbeck & Co As H | Secondary aminoaniline piperidines as mch1 antagonists and their use |
| KR100492252B1 (ko) | 2002-08-09 | 2005-05-30 | 한국화학연구원 | 이미다졸을 포함하는 이차아민으로 치환된 벤조피란유도체 및 그의 제조방법 |
| US7351719B2 (en) | 2002-10-31 | 2008-04-01 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Amide compounds having MCH-antagonistic activity and medicaments comprising these compounds |
| DE10250743A1 (de) | 2002-10-31 | 2004-05-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Amid-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel |
| US20060100245A1 (en) | 2002-12-19 | 2006-05-11 | Neurogen Corporation | Substituted biphenyl-4-carboxylic acid arylamide analogues |
| US6933311B2 (en) | 2003-02-11 | 2005-08-23 | Abbott Laboratories | Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor |
| DE10306250A1 (de) | 2003-02-14 | 2004-09-09 | Aventis Pharma Deutschland Gmbh | Substituierte N-Arylheterozyklen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| EP2415760A3 (en) | 2003-02-20 | 2012-02-22 | Encysive Pharmaceuticals, Inc. | CCR-9 antagonists |
| JP2006523692A (ja) | 2003-04-18 | 2006-10-19 | イーライ リリー アンド カンパニー | ５−ｈｔ１ｆ作用薬としての（ピペリジニルオキシ）フェニル、（ピペリジニルオキシ）ピリジニル、（ピペリジニルスルファニル）フェニル、および（ピペリジニルスルファニル）ピリジニル化合物 |
| WO2005014554A1 (en) | 2003-08-08 | 2005-02-17 | Astex Therapeutics Limited | 1h-indazole-3-carboxamide compounds as mapkap kinase modulators |
| MXPA06003951A (es) | 2003-10-07 | 2006-06-27 | Renovis Inc | Derivados de amida como ligandos del canal de ion y composiciones farmaceuticas y sus metodos de uso. |
| CA2541299A1 (en) | 2003-10-07 | 2005-04-14 | Renovis, Inc. | Amide compounds as ion channel ligands and uses thereof |
| JP4490434B2 (ja) | 2003-10-23 | 2010-06-23 | エフ．ホフマン−ラ ロシュ アーゲー | 神経及び神経精神疾患の処置においてＧｌｙＴ−１阻害剤として使用するためのトリアザ−スピロピペリジン誘導体 |
| KR101122708B1 (ko) | 2003-12-26 | 2012-03-26 | 마사토시 하기와라 | Ｓｒ 단백질 인산화 제어 방법, 및 유효성분으로서 ｓｒ 단백질 활성 제어제를 함유하는 항바이러스제 |
| US8404747B2 (en) | 2004-03-05 | 2013-03-26 | The General Hospital Corporation | Compositions and methods for modulating interaction between polypeptides |
| BRPI0510453A (pt) | 2004-04-30 | 2007-10-30 | Warner Lambert Co | composto substituìdos com morfolina para o tratamento de distúrbios do sistema nervoso central |
| SI1761520T1 (sl) | 2004-06-23 | 2008-10-31 | Lilly Co Eli | Inhibitorji kinaze |
| US20070249620A1 (en) | 2004-07-02 | 2007-10-25 | Hitoshi Kurata | Urea Derivative |
| WO2006018662A2 (en) | 2004-08-16 | 2006-02-23 | Prosidion Limited | Aryl urea derivatives for treating obesity |
| DE102004039789A1 (de) | 2004-08-16 | 2006-03-02 | Sanofi-Aventis Deutschland Gmbh | Arylsubstituierte polycyclische Amine, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| WO2006051851A1 (ja) | 2004-11-10 | 2006-05-18 | Wakamoto Pharmaceutical Co., Ltd. | ２，３，４，５－テトラヒドロ－１ｈ－１，５－ベンゾジアゼピン誘導体、及び、医薬組成物 |
| US20060111392A1 (en) | 2004-11-23 | 2006-05-25 | Wood Michael R | Substituted biaryl-carboxylate derivatives |
| WO2006070878A1 (ja) | 2004-12-28 | 2006-07-06 | Astellas Pharma Inc. | カルボン酸誘導体またはその塩 |
| GB0611907D0 (en) | 2006-06-15 | 2006-07-26 | Glaxo Group Ltd | Compounds |
| JP5475234B2 (ja) | 2005-01-21 | 2014-04-16 | アステックス・セラピューティクス・リミテッド | 医薬化合物 |
| AR054425A1 (es) | 2005-01-21 | 2007-06-27 | Astex Therapeutics Ltd | Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico. |
| RU2007131101A (ru) | 2005-01-21 | 2009-02-27 | Астекс Терапьютикс Лимитед (Gb) | Комбинации пиразольных ингибиторов киназы и других средств против злокачественных новообразований |
| WO2006107923A1 (en) | 2005-04-05 | 2006-10-12 | Boehringer Ingelheim International Gmbh | Substituted benzylimidazoles useful for the treatment of inflammatory diseases |
| US20090209422A1 (en) | 2005-05-03 | 2009-08-20 | Bayer Cropscience Ag | Insecticidal Substituted Aminoalkyl Heterocyclic and Heteroaryl Derivatives |
| WO2007003967A2 (en) | 2005-07-06 | 2007-01-11 | Cambridge Semiconductor Limited | Switch mode power supply control systems |
| JP2007051121A (ja) | 2005-07-22 | 2007-03-01 | Taiho Yakuhin Kogyo Kk | プロスタグランジンｄ合成酵素を阻害するピリミジン化合物 |
| US20100152188A1 (en) | 2005-08-05 | 2010-06-17 | Akella Satya Surya Visweswara Srinivas | Novel Heterocyclic Compounds |
| BRPI0615307A2 (pt) | 2005-08-25 | 2009-08-04 | Schering Corp | agonistas de adrenorreceptor alfa2c |
| PL1940786T3 (pl) | 2005-09-16 | 2010-12-31 | Arrow Therapeutics Ltd | Pochodne bifenylowe i ich zastosowanie w leczeniu zapalenia wątroby typu C |
| CN101355939A (zh) | 2005-10-06 | 2009-01-28 | 马萨诸塞大学 | 用于抑制hiv复制的新物质的组合物和合成 |
| US20070197529A1 (en) | 2005-12-01 | 2007-08-23 | Viviana Braude | Isolated desfluoro-linezolid, preparation thereof and its use as a reference marker and standard |
| JP2007191471A (ja) | 2005-12-21 | 2007-08-02 | Sankyo Co Ltd | ウレア誘導体を含有する医薬 |
| US20070254894A1 (en) | 2006-01-10 | 2007-11-01 | Kane John L Jr | Novel small molecules with selective cytotoxicity against human microvascular endothelial cell proliferation |
| KR101079914B1 (ko) | 2006-01-27 | 2011-11-04 | 에프. 호프만-라 로슈 아게 | 중추신경계 장애를 위한 4-이미다졸 유도체의 용도 |
| JP5182088B2 (ja) | 2006-04-19 | 2013-04-10 | アステラス製薬株式会社 | アゾールカルボキサミド誘導体 |
| ATE465150T1 (de) | 2006-06-28 | 2010-05-15 | Glaxo Group Ltd | Für die behandlung von durch den gpr38-rezeptor vermittelten krankheiten geeignete piperazinylderivate |
| CA2666762C (en) | 2006-10-19 | 2014-12-30 | F. Hoffmann-La Roche Ag | Aminomethyl-4-imidazoles |
| KR20090075873A (ko) | 2006-10-31 | 2009-07-09 | 쉐링 코포레이션 | 아닐리노피페라진 유도체 및 이의 사용방법 |
| WO2008054749A1 (en) | 2006-10-31 | 2008-05-08 | Schering Corporation | 2-aminothiazole-4-carboxylic amides as protein kinase inhibitors |
| EP2077839A2 (en) | 2006-11-03 | 2009-07-15 | Arete Therapeutics, INC. | Soluble epoxide hydrolase inhibitors for the treatment of rheumatoid arthritis |
| JP2008179624A (ja) | 2006-12-26 | 2008-08-07 | Santen Pharmaceut Co Ltd | ウレア構造を有する新規ｎ−（２−アミノフェニル）ベンズアミド誘導体 |
| WO2008092785A1 (en) | 2007-02-02 | 2008-08-07 | F. Hoffmann-La Roche Ag | Novel 2-aminooxazolines as taar1 ligands for cns disorders |
| KR101222412B1 (ko) | 2007-02-15 | 2013-01-15 | 에프. 호프만-라 로슈 아게 | Ｔａａｒ1 리간드로서의 2-아미노옥사졸린 |
| CN101835757B (zh) | 2007-05-22 | 2014-03-05 | 玛德瑞哥制药公司 | 二酰甘油酰基转移酶抑制剂 |
| US8058299B2 (en) | 2007-05-22 | 2011-11-15 | Via Pharmaceuticals, Inc. | Diacylglycerol acyltransferase inhibitors |
| WO2008153959A1 (en) | 2007-06-07 | 2008-12-18 | Intra-Cellular Therapies, Inc. | Novel heterocycle compounds and uses thereof |
| JO2972B1 (en) | 2007-06-08 | 2016-03-15 | جانسين فارماسوتيكا ان. في | Piperidine / piperazine derivatives |
| AU2008258487B2 (en) | 2007-06-08 | 2012-11-15 | Janssen Pharmaceutica N.V. | Piperidine/piperazine derivatives |
| BRPI0815038A2 (pt) | 2007-08-02 | 2015-03-17 | Hoffmann La Roche | Uso de derivados de benzamida para o tratamento de transtornos do cns |
| KR101167773B1 (ko) | 2007-08-03 | 2012-07-24 | 에프. 호프만-라 로슈 아게 | Ｔａａｒ１ 리간드로서의 피리딘카복스아마이드 및 벤즈아마이드 유도체 |
| JP2009094891A (ja) | 2007-10-10 | 2009-04-30 | Toshiba Corp | 半導体集積回路装置及びパターン検出方法 |
| US8093428B2 (en) | 2007-10-26 | 2012-01-10 | Janssen Pharmaceutica N.V. | Synthesis of quaternary salt compounds |
| CN101434570B (zh) | 2007-11-16 | 2011-02-02 | 上海医药工业研究院 | 吡咯烷衍生物及其制备方法和应用 |
| US8642660B2 (en) | 2007-12-21 | 2014-02-04 | The University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| US8242153B2 (en) | 2008-07-24 | 2012-08-14 | Hoffmann-La Roche Inc. | 4,5-dihydro-oxazol-2YL derivatives |
| CN102083805A (zh) | 2008-07-24 | 2011-06-01 | 弗·哈夫曼-拉罗切有限公司 | 4,5-二氢-唑-2-基衍生物 |
| EP2351744B1 (en) | 2008-10-17 | 2015-01-07 | Shionogi & Co., Ltd. | Acetic acid amide derivative having inhibitory activity on vascular endothelial lipase |
| ES2432070T3 (es) | 2009-02-24 | 2013-11-29 | Respiratorius Ab | Diazaheteroarilos broncodilatadores novedosos |
| WO2010111711A2 (en) | 2009-03-27 | 2010-09-30 | Zacharon Pharmaceuticals, Inc. | Ganglioside biosynthesis modulators |
| JP5381257B2 (ja) | 2009-04-09 | 2014-01-08 | ユニマテック株式会社 | 含フッ素ボロン酸エステル化合物の製造方法 |
| WO2010118347A2 (en) | 2009-04-10 | 2010-10-14 | Zacharon Pharmaceuticals, Inc. | O-linked glycan biosynthesis modulators |
| US20100311798A1 (en) | 2009-06-05 | 2010-12-09 | Decoret Guillaume | 2-aminooxazolines as taar1 ligands |
| US20120040950A1 (en) | 2009-12-22 | 2012-02-16 | Vertex Pharmaceuticals Incorporated | Isoindolinone inhibitors of phosphatidylinositol 3-kinase |
| US8440693B2 (en) | 2009-12-22 | 2013-05-14 | Novartis Ag | Substituted isoquinolinones and quinazolinones |
| SG181891A1 (en) | 2009-12-22 | 2012-07-30 | Celgene Corp | (methylsulfonyl) ethyl benzene isoindoline derivatives and their therapeutical uses |
| US9452980B2 (en) | 2009-12-22 | 2016-09-27 | Hoffmann-La Roche Inc. | Substituted benzamides |
| 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 |
| DE102011112317B3 (de) | 2011-09-02 | 2013-02-28 | Mühlbauer Ag | Wendevorrichtung für Identifikationsgegenstände |
| AU2013208104B2 (en) | 2012-01-09 | 2017-11-23 | X-Chem, Inc. | Benzhydrol-pyrazole derivatives having kinase inhibitory activity and uses thereof |
| BR112015004511B1 (pt) * | 2012-09-14 | 2022-08-02 | F. Hoffmann-La Roche Ag | Derivados de pirazol carboxamida como moduladores de taar para uso no tratamento de diversas desordens, tais como depressão, diabetes e doença de parkinson |
| MX361761B (es) * | 2012-09-17 | 2018-12-17 | Hoffmann La Roche | Derivados de triazol carboxamida. |
| CN104109165A (zh) | 2013-04-19 | 2014-10-22 | 四川海思科制药有限公司 | 4,5-二氢-吡唑并[3,4-c]吡啶-2-酮衍生物、其制备方法以及应用 |
| WO2015165085A1 (en) * | 2014-04-30 | 2015-11-05 | F.Hoffmann-La Roche Ag | Morpholin-pyridine derivatives |
| LT3149002T (lt) | 2014-05-28 | 2018-07-10 | F. Hoffmann-La Roche Ag | 5-oksa-2-azabiciklo[2.2.2]oktan-4-ilo ir 5-oksa-2-azabiciklo[2.2.1]heptan-4-ilo dariniai kaip taar1 moduliatoriai |
| WO2016015333A1 (en) * | 2014-08-01 | 2016-02-04 | F.Hoffmann-La Roche Ag | 2-oxa-5-azabicyclo [2.2.1] heptan-3-yl derivatives |
| WO2016030310A1 (en) | 2014-08-27 | 2016-03-03 | F. Hoffmann-La Roche Ag | Substituted azetidine derivatives as taar ligands |
| WO2018129524A1 (en) | 2017-01-09 | 2018-07-12 | Lentigen Technology, Inc. | Compositions and methods for treating cancer with anti-mesothelin immunotherapy |
-
2017
- 2017-03-14 RS RS20201094A patent/RS60825B1/sr unknown
- 2017-03-14 PL PL17710286T patent/PL3430010T3/pl unknown
- 2017-03-14 MX MX2018010622A patent/MX377836B/es unknown
- 2017-03-14 SI SI201730407T patent/SI3430010T1/sl unknown
- 2017-03-14 MA MA053755A patent/MA53755A/fr unknown
- 2017-03-14 EP EP17710286.0A patent/EP3430010B1/en active Active
- 2017-03-14 MY MYPI2018001546A patent/MY195528A/en unknown
- 2017-03-14 HR HRP20201405TT patent/HRP20201405T1/hr unknown
- 2017-03-14 KR KR1020227021732A patent/KR102537050B1/ko active Active
- 2017-03-14 CR CR20180443A patent/CR20180443A/es unknown
- 2017-03-14 RU RU2018134262A patent/RU2731095C2/ru active
- 2017-03-14 PE PE2018001346A patent/PE20181446A1/es unknown
- 2017-03-14 UA UAA201809608A patent/UA122881C2/uk unknown
- 2017-03-14 EP EP20184122.8A patent/EP3757102A1/en active Pending
- 2017-03-14 LT LTEP17710286.0T patent/LT3430010T/lt unknown
- 2017-03-14 SG SG10201913878YA patent/SG10201913878YA/en unknown
- 2017-03-14 MA MA43706A patent/MA43706B1/fr unknown
- 2017-03-14 ES ES17710286T patent/ES2819830T3/es active Active
- 2017-03-14 SG SG11201807516UA patent/SG11201807516UA/en unknown
- 2017-03-14 DK DK17710286.0T patent/DK3430010T3/da active
- 2017-03-14 JP JP2018545336A patent/JP6814814B2/ja active Active
- 2017-03-14 BR BR112018015389-3A patent/BR112018015389B1/pt active IP Right Grant
- 2017-03-14 AU AU2017234042A patent/AU2017234042B2/en active Active
- 2017-03-14 WO PCT/EP2017/055885 patent/WO2017157873A1/en not_active Ceased
- 2017-03-14 PT PT177102860T patent/PT3430010T/pt unknown
- 2017-03-14 HU HUE17710286A patent/HUE050986T2/hu unknown
- 2017-03-14 KR KR1020187026570A patent/KR102415797B1/ko active Active
- 2017-03-14 CN CN201780014687.6A patent/CN108713019B/zh active Active
- 2017-03-14 CA CA3013696A patent/CA3013696C/en active Active
- 2017-03-15 AR ARP170100637A patent/AR107878A1/es not_active Application Discontinuation
- 2017-03-16 TW TW106108638A patent/TWI634117B/zh active
-
2018
- 2018-07-08 IL IL260473A patent/IL260473B/en active IP Right Grant
- 2018-07-17 CO CONC2018/0007515A patent/CO2018007515A2/es unknown
- 2018-07-23 ZA ZA2018/04943A patent/ZA201804943B/en unknown
- 2018-07-25 PH PH12018501588A patent/PH12018501588A1/en unknown
- 2018-09-10 CL CL2018002583A patent/CL2018002583A1/es unknown
- 2018-09-13 US US16/130,881 patent/US10508107B2/en active Active
-
2020
- 2020-06-11 US US16/898,827 patent/US11312711B2/en active Active
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2018134262A (ru) | Производное 5-этил-4-метил-пиразол-3-карбоксамида, обладающее активностью агониста taar | |
| RU2462456C2 (ru) | Производные пиразола в качестве ингибиторов 11-бета-hsd1 | |
| JP6453931B2 (ja) | 抗コネクシン剤としてのフレカイニドの使用、及び向精神薬の効果を増強する方法 | |
| RU2011123371A (ru) | Кристаллические формы гидрохлорида финголимода | |
| RU2015111836A (ru) | Производные триазолкарбоксамида | |
| JP2019512469A5 (ru) | ||
| BR112013024312A2 (pt) | derivados de amina heterocíclica | |
| RU2011123365A (ru) | Соли финголимода | |
| TW200833685A (en) | Aminomethyl-4-imidazoles | |
| JP2010535172A (ja) | Ｃｎｓ障害の処置のためのベンズアミド誘導体の使用 | |
| RU2012129737A (ru) | Замещенные бензамидные производные | |
| JP2012508215A5 (ru) | ||
| CO6331336A2 (es) | Derivados de 4,5-dihidro-oxazol-2-ilo | |
| BRPI0905849A2 (pt) | Composto, composição farmacêutica e método | |
| JP2013536181A (ja) | 非定型抗精神病薬及びｔａａｒ１アゴニストを含む組合せ | |
| WO2009003868A3 (en) | 2 -imidazolines having a good affinity to the trace amine associated receptors (taars) | |
| MX2009003887A (es) | Aminometil-2-imidazoles con afinidad con los receptores asociados a trazas de amina. | |
| BR112014006763A2 (pt) | n-(3-(2-amino-6,6-difluoro-4,4a,5,6,7,7a-hexa-hidro-ciclopenta[e][1,3]oxazin-4-il)-fenil)-amidas como inibidores de bace1 | |
| JP5423905B2 (ja) | 新規化合物及びその医薬用途 | |
| RU2009122665A (ru) | 4-имидазолины в качестве лигандов taar | |
| JP2014518552A5 (ru) | ||
| EA200801488A1 (ru) | Замещенные фенетиламины, обладающие серотонинергической и/или норэпинефринергической активностью | |
| JP6605447B2 (ja) | ジスキネジアおよび関連障害を治療する方法 | |
| AR092537A1 (es) | Derivados de pirazol-carboxamida | |
| CN1638756A (zh) | 左旋(r)班布特罗及其药物用途 |