MX2013011781A - Derivados de pirrolotriazinona como inhibidores de pi3k. - Google Patents
Derivados de pirrolotriazinona como inhibidores de pi3k.Info
- Publication number
- MX2013011781A MX2013011781A MX2013011781A MX2013011781A MX2013011781A MX 2013011781 A MX2013011781 A MX 2013011781A MX 2013011781 A MX2013011781 A MX 2013011781A MX 2013011781 A MX2013011781 A MX 2013011781A MX 2013011781 A MX2013011781 A MX 2013011781A
- Authority
- MX
- Mexico
- Prior art keywords
- derivatives
- pirrolotriazinona
- pi3k inhibitors
- inhibitors
- formula
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- 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
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- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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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
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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
- A61P3/08—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
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- A61P31/12—Antivirals
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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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
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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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- A61P7/06—Antianaemics
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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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Endocrinology (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Dermatology (AREA)
- Obesity (AREA)
- Oncology (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Otolaryngology (AREA)
- Transplantation (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Vascular Medicine (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
Abstract
(Ver Formula) Se describen nuevos derivados de pirrolotriazinona que tienen la estructura química de fórmula (I); así como un procedimiento para su preparación, composiciones farmacéuticas que los contienen y su uso en terapia como inhibidores de Fosfoinositido 3-quinasas (PI3Ks).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11382124A EP2518070A1 (en) | 2011-04-29 | 2011-04-29 | Pyrrolotriazinone derivatives as PI3K inhibitors |
| US201161502550P | 2011-06-29 | 2011-06-29 | |
| PCT/EP2012/057671 WO2012146666A1 (en) | 2011-04-29 | 2012-04-26 | Pyrrolotriazinone derivatives as pi3k inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2013011781A true MX2013011781A (es) | 2013-11-01 |
| MX336214B MX336214B (es) | 2016-01-12 |
Family
ID=44484054
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2013011781A MX336214B (es) | 2011-04-29 | 2012-04-26 | Derivados de pirrolotriazinona como inhibidores de pi3k. |
Country Status (36)
| Country | Link |
|---|---|
| US (1) | US9340547B2 (es) |
| EP (2) | EP2518070A1 (es) |
| JP (1) | JP5903160B2 (es) |
| KR (1) | KR20140021622A (es) |
| CN (1) | CN103649089B (es) |
| AR (1) | AR086144A1 (es) |
| AU (1) | AU2012247491B2 (es) |
| BR (1) | BR112013023876A2 (es) |
| CA (1) | CA2826197A1 (es) |
| CL (1) | CL2013003073A1 (es) |
| CO (1) | CO6801747A2 (es) |
| CR (1) | CR20130543A (es) |
| CY (1) | CY1116871T1 (es) |
| DK (1) | DK2702061T3 (es) |
| EA (1) | EA024350B1 (es) |
| ES (1) | ES2545853T3 (es) |
| GT (1) | GT201300266A (es) |
| HR (1) | HRP20151153T1 (es) |
| HU (1) | HUE026041T2 (es) |
| IL (1) | IL227764A (es) |
| ME (1) | ME02210B (es) |
| MX (1) | MX336214B (es) |
| MY (1) | MY171553A (es) |
| PE (1) | PE20141193A1 (es) |
| PH (1) | PH12013502059A1 (es) |
| PL (1) | PL2702061T3 (es) |
| PT (1) | PT2702061E (es) |
| RS (1) | RS54270B1 (es) |
| SG (1) | SG194084A1 (es) |
| SI (1) | SI2702061T1 (es) |
| SM (1) | SMT201500270B (es) |
| TW (2) | TWI535720B (es) |
| UA (1) | UA111197C2 (es) |
| UY (1) | UY34051A (es) |
| WO (1) | WO2012146666A1 (es) |
| ZA (1) | ZA201305612B (es) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2518070A1 (en) | 2011-04-29 | 2012-10-31 | Almirall, S.A. | Pyrrolotriazinone derivatives as PI3K inhibitors |
| DK2790705T3 (en) | 2011-12-15 | 2018-03-12 | Novartis Ag | Use of inhibitors of the activity or function of PI3K |
| WO2014015523A1 (en) * | 2012-07-27 | 2014-01-30 | Hutchison Medipharma Limited | Novel heteroaryl and heterocycle compounds, compositions and methods |
| EP2909207A1 (en) * | 2012-10-16 | 2015-08-26 | Almirall S.A. | Pyrrolotriazinone derivatives as pi3k inhibitors |
| JP6434416B2 (ja) | 2012-11-08 | 2018-12-05 | ライゼン・ファーマシューティカルズ・エスアー | PDE4阻害剤とPI3δ阻害剤または二重PI3δ−γキナーゼ阻害剤とを含有する薬学的組成物 |
| RU2661896C2 (ru) * | 2012-11-16 | 2018-07-23 | Мерк Шарп И Доум Корп. | Пуриновые ингибиторы фосфатидилинозитол-3-киназы дельта человека |
| WO2014082230A1 (zh) * | 2012-11-28 | 2014-06-05 | 上海希迈医药科技有限公司 | 吡咯并三嗪类衍生物、其制备方法及其在医药上的应用 |
| WO2014087208A2 (en) * | 2012-12-06 | 2014-06-12 | Enaltec Labs Pvt. Ltd. | A process of preparing alcaftadine |
| ES2677919T3 (es) | 2012-12-21 | 2018-08-07 | Gilead Calistoga Llc | Aminoalquil-quinazolonas sustituidas con pirimidina como inhibidores de la fosfatidilinositol 3-quinasa |
| BR112015014592A2 (pt) | 2012-12-21 | 2017-07-11 | Gilead Calistoga Llc | composto, composição farmacêutica, e, método para o tratamento de um humano |
| AR094797A1 (es) * | 2013-02-15 | 2015-08-26 | Almirall Sa | Derivados de pirrolotriazina como inhibidores de pi3k |
| KR101709436B1 (ko) | 2013-06-14 | 2017-02-22 | 길리애드 사이언시즈, 인코포레이티드 | 포스파티딜이노시톨 3-키나제 억제제 |
| EP3033340B1 (en) * | 2013-08-13 | 2019-12-04 | The Regents of The University of California | Deoxycytidine kinase inhibitors |
| GB201402431D0 (en) | 2014-02-12 | 2014-03-26 | Karus Therapeutics Ltd | Compounds |
| EA202191009A1 (ru) * | 2014-04-08 | 2021-08-31 | Инсайт Корпорейшн | Лечение b-клеточных злокачественных новообразований с применением комбинации ингибиторов jak и pi3k |
| US20170158699A1 (en) * | 2014-05-27 | 2017-06-08 | Almirall, S.A. | Addition salts of (s)-2-(1-(6-amino-5-cyanopyrimidin-4-ylamino)ethyl)-4-oxo-3-phenyl-3,4-dihydropyrrolo[1,2-f][1,2,4]triazine-5-carbonitrile |
| SG11201609527PA (en) | 2014-06-13 | 2016-12-29 | Gilead Sciences Inc | Quinazolinone derivatives as phosphatidylinositol 3-kinase inhibitors |
| WO2015191754A2 (en) * | 2014-06-13 | 2015-12-17 | Gilead Sciences, Inc. | Phosphatidylinositol 3-kinase inhibitors |
| WO2015191726A1 (en) | 2014-06-13 | 2015-12-17 | Gilead Sciences, Inc. | Phosphatidylinositol 3-kinase inhibitors |
| JP6291601B2 (ja) | 2014-07-04 | 2018-03-14 | ルピン・リミテッド | Pi3k阻害剤としてのキノリジノン誘導体 |
| WO2016054491A1 (en) | 2014-10-03 | 2016-04-07 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| CA2966252C (en) | 2014-11-01 | 2023-10-24 | Shanghai Institute Of Materia Medica Chinese Academy Of Sciences | Phosphoinositide 3-kinase inhibitors |
| EP3225618B1 (en) | 2014-11-26 | 2020-05-06 | Takeda Pharmaceutical Company Limited | Bicyclic compound |
| CN105712998B (zh) * | 2014-12-05 | 2019-12-13 | 上海润诺生物科技有限公司 | 氮杂吲哚类衍生物、其制备方法及其在医药上的应用 |
| GB201514760D0 (en) | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Compounds and method of use |
| GB201514758D0 (en) * | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Formulation |
| WO2017160930A1 (en) * | 2016-03-16 | 2017-09-21 | Kalyra Pharmaceuticals, Inc. | Analgesic compounds |
| WO2017214269A1 (en) | 2016-06-08 | 2017-12-14 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| JP7098630B2 (ja) | 2017-01-10 | 2022-07-11 | バイエル・アクチエンゲゼルシヤフト | 有害生物防除剤としてのヘテロサイクレン誘導体 |
| US20210161870A1 (en) | 2017-06-07 | 2021-06-03 | Arcutis Biotherapeutics, Inc. | Roflumilast formulations with an improved pharmacokinetic profile |
| US12042487B2 (en) | 2018-11-16 | 2024-07-23 | Arcutis Biotherapeutics, Inc. | Method for reducing side effects from administration of phosphodiesterase-4 inhibitors |
| US11129818B2 (en) | 2017-06-07 | 2021-09-28 | Arcutis Biotherapeutics, Inc. | Topical roflumilast formulation having improved delivery and plasma half life |
| US9895359B1 (en) | 2017-06-07 | 2018-02-20 | Arcutis, Inc. | Inhibition of crystal growth of roflumilast |
| US12011437B1 (en) | 2017-06-07 | 2024-06-18 | Arcutis Biotherapeutics, Inc. | Roflumilast formulations with an improved pharmacokinetic profile |
| US20200155524A1 (en) | 2018-11-16 | 2020-05-21 | Arcutis, Inc. | Method for reducing side effects from administration of phosphodiesterase-4 inhibitors |
| CN107383004B (zh) * | 2017-07-05 | 2020-04-17 | 浙江大学 | 2-氨基咪唑并吡啶类衍生物及制备和应用 |
| EP3672597A4 (en) * | 2017-08-21 | 2021-09-22 | Navigen, Inc. | ARF6 INHIBITORS AND RELATED PROCEDURES |
| CN111212839A (zh) * | 2017-09-15 | 2020-05-29 | 艾杜罗生物科技公司 | 吡唑并嘧啶酮化合物及其用途 |
| US11534493B2 (en) | 2017-09-22 | 2022-12-27 | Arcutis Biotherapeutics, Inc. | Pharmaceutical compositions of roflumilast in aqueous blends of water-miscible, pharmaceutically acceptable solvents |
| WO2019236374A2 (en) | 2018-06-04 | 2019-12-12 | Arcutis, Inc. | Method and formulation for improving roflumilast skin penetration lag time |
| JP2021528479A (ja) * | 2018-07-06 | 2021-10-21 | レオ ファーマ アクティーゼルスカブ | ヤヌスキナーゼ阻害剤としての新規アミノ−イミダゾピリミジン誘導体およびその製薬学的用途 |
| JP2022541954A (ja) * | 2019-07-17 | 2022-09-28 | 小野薬品工業株式会社 | Kdm5阻害活性を有する化合物およびその医薬用途 |
| CN111346095B (zh) * | 2020-03-14 | 2021-06-08 | 温州医科大学附属第二医院、温州医科大学附属育英儿童医院 | 用于治疗神经外科术后头痛的药物制剂 |
| CA3178569A1 (en) * | 2020-05-16 | 2021-11-25 | Zuwen ZHOU | Compounds as protein kinase inhibitors |
| CN116963717A (zh) | 2020-12-04 | 2023-10-27 | 阿尔库缇斯生物疗法股份有限公司 | 具有抗真菌性能的局部用罗氟司特制剂 |
| EP4456870A1 (en) | 2021-12-28 | 2024-11-06 | Arcutis Biotherapeutics, Inc. | Topical roflumilast aerosol foams |
| JP2025530005A (ja) | 2022-09-15 | 2025-09-09 | アーキュティス・バイオセラピューティクス・インコーポレーテッド | ロフルミラスト及び大量のロフルミラストを溶解可能な溶媒の医薬組成物 |
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| IT7920688U1 (it) | 1979-02-05 | 1980-08-05 | Chiesi Paolo | Inalatore per sostanze medicamentose pulverulente, con combinata funzione di dosatore |
| US5200416A (en) * | 1980-05-12 | 1993-04-06 | Usv Pharmaceutical Corporation | Cyclic amides |
| EP0069715B1 (en) | 1981-07-08 | 1986-11-05 | Aktiebolaget Draco | Powder inhalator |
| US4570630A (en) | 1983-08-03 | 1986-02-18 | Miles Laboratories, Inc. | Medicament inhalation device |
| FI69963C (fi) | 1984-10-04 | 1986-09-12 | Orion Yhtymae Oy | Doseringsanordning |
| DE3927170A1 (de) | 1989-08-17 | 1991-02-21 | Boehringer Ingelheim Kg | Inhalator |
| IT1237118B (it) | 1989-10-27 | 1993-05-18 | Miat Spa | Inalatore multidose per farmaci in polvere. |
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