BRPI0911243B8 - derivados de benzofurano, benzotiofeno, benzotiazol, e composição farmacêutica - Google Patents
derivados de benzofurano, benzotiofeno, benzotiazol, e composição farmacêuticaInfo
- Publication number
- BRPI0911243B8 BRPI0911243B8 BRPI0911243A BRPI0911243A BRPI0911243B8 BR PI0911243 B8 BRPI0911243 B8 BR PI0911243B8 BR PI0911243 A BRPI0911243 A BR PI0911243A BR PI0911243 A BRPI0911243 A BR PI0911243A BR PI0911243 B8 BRPI0911243 B8 BR PI0911243B8
- Authority
- BR
- Brazil
- Prior art keywords
- benzothiophene
- benzothiazole
- pharmaceutical composition
- benzofuran derivatives
- formula
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
-
- 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
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- 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
- A61P17/18—Antioxidants, e.g. antiradicals
-
- 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
- C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
- C07D307/84—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D307/85—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Dermatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Biochemistry (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Child & Adolescent Psychology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
derivados de benzofurano, benzotiofeno, benzotiazol como moduladores de fxr. a presente invenção refere-se aos compostos de fórmula (i) (i) em que os substituintes são tais como definidos nas reivindicações, incluindo composições farmacêuticas dos mesmos e quanto ao seu emprego no tratamento e/ou prevenção e/ou melhora de um ou mais sintomas de doença ou distúrbios relacionados à atividade de fxr. a invenção também é direcionada à intermediários e a um método de preparação de compostos de fórmula (i).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08300183.4 | 2008-04-18 | ||
| EP08300183A EP2110374A1 (en) | 2008-04-18 | 2008-04-18 | Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators |
| PCT/EP2009/002297 WO2009127321A1 (en) | 2008-04-18 | 2009-03-30 | Benzofurane, benzothiophene, benzothiazol derivatives as fxr modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BRPI0911243A2 BRPI0911243A2 (pt) | 2015-10-06 |
| BRPI0911243B1 BRPI0911243B1 (pt) | 2019-10-08 |
| BRPI0911243B8 true BRPI0911243B8 (pt) | 2021-05-25 |
Family
ID=39769187
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0911243A BRPI0911243B8 (pt) | 2008-04-18 | 2009-03-30 | derivados de benzofurano, benzotiofeno, benzotiazol, e composição farmacêutica |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US8575161B2 (pt) |
| EP (2) | EP2110374A1 (pt) |
| JP (2) | JP5616326B2 (pt) |
| KR (1) | KR101662853B1 (pt) |
| CN (1) | CN101990535B (pt) |
| AR (1) | AR071207A1 (pt) |
| AU (1) | AU2009238015B2 (pt) |
| BR (1) | BRPI0911243B8 (pt) |
| CA (1) | CA2721591C (pt) |
| CO (1) | CO6311099A2 (pt) |
| CY (1) | CY1116333T1 (pt) |
| DK (1) | DK2262785T3 (pt) |
| EA (1) | EA020454B1 (pt) |
| EC (1) | ECSP10010615A (pt) |
| ES (1) | ES2531006T3 (pt) |
| HR (1) | HRP20150319T1 (pt) |
| IL (1) | IL208322A (pt) |
| MX (1) | MX2010011292A (pt) |
| MY (1) | MY156530A (pt) |
| NZ (1) | NZ589327A (pt) |
| PL (1) | PL2262785T3 (pt) |
| PT (1) | PT2262785E (pt) |
| SI (1) | SI2262785T1 (pt) |
| UA (1) | UA104140C2 (pt) |
| WO (1) | WO2009127321A1 (pt) |
| ZA (1) | ZA201008243B (pt) |
Families Citing this family (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3205644A1 (en) | 2005-12-29 | 2017-08-16 | Celtaxsys Inc. | Diamine derivatives as inhibitors of leukotriene a4 hydrolase |
| EP2110374A1 (en) * | 2008-04-18 | 2009-10-21 | Merck Sante | Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators |
| KR20110128913A (ko) * | 2009-03-10 | 2011-11-30 | 다케다 야쿠힌 고교 가부시키가이샤 | 벤조푸란 유도체 |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| EP2566862B1 (en) | 2010-05-06 | 2015-09-16 | Bristol-Myers Squibb Company | Benzofuranyl analogues as gpr119 modulators |
| CN102971311B (zh) | 2010-05-06 | 2015-07-08 | 百时美施贵宝公司 | 作为gpr119调节剂的二环杂芳基化合物 |
| TW201204733A (en) | 2010-06-25 | 2012-02-01 | Kowa Co | Novel condensed pyridine or condensed pyrimidine derivative, and medicinal agent comprising same |
| WO2012087833A1 (en) | 2010-12-22 | 2012-06-28 | Abbott Laboratories | Hepatitis c inhibitors and uses thereof |
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| WO2013037482A1 (en) | 2011-09-15 | 2013-03-21 | Phenex Pharmaceuticals Ag | Farnesoid x receptor agonists for cancer treatment and prevention |
| WO2014006637A2 (en) * | 2012-07-02 | 2014-01-09 | Symed Labs Limited | Improved process for preparing benzofuran-2-carboxamide derivatives |
| CN102993186B (zh) * | 2012-12-20 | 2015-11-18 | 北京海步国际医药科技发展有限公司 | 一种新型的哌嗪衍生物 |
| AU2014249168B2 (en) | 2013-03-12 | 2018-07-12 | Celltaxis, Llc | Methods of inhibiting leukotriene A4 hydrolase |
| AU2014240042C1 (en) | 2013-03-14 | 2019-09-05 | Celltaxis, Llc | Inhibitors of leukotriene A4 hydrolase |
| MX2015011678A (es) | 2013-03-14 | 2016-07-08 | Celtaxsys Inc | Inhibidores de leucotrieno a4 hidrolasa. |
| EP2968265A4 (en) | 2013-03-14 | 2016-12-28 | Celtaxsys Inc | INHIBITORS OF THE LEUKOTRIEN A4 HYDROLASE |
| MX377523B (es) * | 2013-09-11 | 2025-03-10 | Inst Nat Sante Rech Med | Metodos y composiciones farmaceuticas para el tratamiento de la infeccion por el virus de la hepatitis b. |
| ES2905872T3 (es) | 2015-02-06 | 2022-04-12 | Intercept Pharmaceuticals Inc | Composiciones farmacéuticas para terapia combinada |
| RU2712099C2 (ru) | 2015-03-31 | 2020-01-24 | Энанта Фармасьютикалс, Инк. | Производные желчных кислот в качестве агонистов fxr/tgr5 и способы их применения |
| CN107613986A (zh) | 2015-04-07 | 2018-01-19 | 英特塞普特医药品公司 | 用于组合疗法的药物组合物 |
| CN104926804B (zh) * | 2015-06-04 | 2019-01-25 | 天津渤海职业技术学院 | 一类具有抗肿瘤作用的化合物、其制备方法和用途 |
| CA2968836C (en) | 2016-06-13 | 2025-09-02 | Gilead Sciences, Inc. | FXR MODULATING COMPOUNDS (NR1H4) |
| NZ748641A (en) | 2016-06-13 | 2020-04-24 | Gilead Sciences Inc | Fxr (nr1h4) modulating compounds |
| CA3039124A1 (en) * | 2016-10-04 | 2018-04-12 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as fxr agonists and methods of use thereof |
| CN108017636A (zh) * | 2016-11-04 | 2018-05-11 | 合帕吉恩治疗公司 | 作为fxr调节剂的含氮杂环化合物 |
| ES2982801T3 (es) | 2017-03-28 | 2024-10-17 | Gilead Sciences Inc | Combinaciones terapéuticas para el tratamiento de las enfermedades hepáticas |
| JP2020515564A (ja) | 2017-03-30 | 2020-05-28 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | エピソーマルウイルスの持続性及び発現を低下させるための方法及び医薬組成物 |
| EP3801559B1 (en) | 2018-05-31 | 2025-01-01 | Celltaxis, LLC | Method of reducing pulmonary exacerbations in respiratory disease patients |
| KR102692309B1 (ko) | 2019-01-15 | 2024-08-07 | 길리애드 사이언시즈, 인코포레이티드 | Fxr (nr1h4) 조정 화합물 |
| WO2020172075A1 (en) | 2019-02-19 | 2020-08-27 | Gilead Sciences, Inc. | Solid forms of fxr agonists |
| WO2020231917A1 (en) | 2019-05-13 | 2020-11-19 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| US20220226350A1 (en) | 2019-05-30 | 2022-07-21 | Intercept Pharmaceuticals, Inc. | Pharmaceutical compositions comprising a fxr agonist and a fibrate for use in the treatment of cholestatic liver disease |
| WO2021009332A1 (en) | 2019-07-18 | 2021-01-21 | Enyo Pharma | Method for decreasing adverse-effects of interferon |
| IL293892A (en) | 2020-01-15 | 2022-08-01 | Inserm Institut National De La Sant? Et De La Rech M?Dicale | Use of fxr agonists for treating an infection by hepatitis d virus |
| CA3201686A1 (en) * | 2021-01-14 | 2022-07-21 | Fabiola Terzi | Method for treating chronic kidney diseases |
| CN116685321A (zh) * | 2021-01-14 | 2023-09-01 | 埃尼奥制药公司 | 治疗慢性肾病的方法 |
| MX2023008365A (es) | 2021-01-14 | 2023-10-04 | Enyo Pharma | Efecto sinérgico de un agonista de fxr e ifn para el tratamiento de infección por hbv. |
| EP4324825A4 (en) * | 2021-04-16 | 2025-08-27 | Beijing Best Pathway Man Consulting Center Limited Partnership | FXR REGULATOR, ITS PREPARATION METHOD, PHARMACEUTICAL COMPOSITION THEREOF AND ITS USE |
| TW202308629A (zh) | 2021-04-28 | 2023-03-01 | 法商Enyo製藥公司 | 使用fxr激動劑作為組合治療以增強tlr3激動劑之療效 |
| CN113214200B (zh) * | 2021-05-26 | 2022-03-29 | 神隆医药(常熟)有限公司 | 一种以铜催化偶联反应制备维拉佐酮中间体的方法 |
| TW202317546A (zh) | 2021-07-09 | 2023-05-01 | 美商普萊克斯姆公司 | 調節ikzf2之芳基化合物及醫藥組合物 |
| TW202329937A (zh) | 2021-12-03 | 2023-08-01 | 美商英塞特公司 | 雙環胺ck12抑制劑 |
| US12084453B2 (en) | 2021-12-10 | 2024-09-10 | Incyte Corporation | Bicyclic amines as CDK12 inhibitors |
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| EP4743449A1 (en) | 2023-07-13 | 2026-05-20 | ENYO Pharma | L-ARGININE SALT OF 4-CHLORO-5-[4-(2,6-DICHLOROPHENYL)SULFONYLPIPERAZIN-1-YL]-1-BENZOFURAN-2-CARBOXYLIC ACID AND VARIOUS FORMS THEREIN |
| CN121646582A (zh) | 2023-07-13 | 2026-03-10 | 恩佑制药 | 4-氯-5-[4-(2,6-二氯苯基)磺酰基哌嗪-1-基]-1-苯并呋喃-2-甲酸的氨丁三醇盐及其各种形式 |
| JP2026524534A (ja) | 2023-07-13 | 2026-07-22 | ウエヌイグレックオ・ファーマ | 4-クロロ-5-[4-(2,6-ジクロロフェニル)スルホニルピペラジン-1-イル]-1-ベンゾフラン-2-カルボン酸のl-リジン塩及びそのさまざまな形態 |
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2008
- 2008-04-18 EP EP08300183A patent/EP2110374A1/en not_active Withdrawn
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