MX369576B - Imidazoles 2-piridilo sustituidos como inhibidores de alk5 y/o alk4. - Google Patents
Imidazoles 2-piridilo sustituidos como inhibidores de alk5 y/o alk4.Info
- Publication number
- MX369576B MX369576B MX2014000309A MX2014000309A MX369576B MX 369576 B MX369576 B MX 369576B MX 2014000309 A MX2014000309 A MX 2014000309A MX 2014000309 A MX2014000309 A MX 2014000309A MX 369576 B MX369576 B MX 369576B
- Authority
- MX
- Mexico
- Prior art keywords
- alk5
- pyridyl substituted
- alk4
- substituted imidazoles
- receptor
- Prior art date
Links
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 title abstract 3
- 150000002460 imidazoles Chemical class 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title 1
- 101000799189 Homo sapiens Activin receptor type-1B Proteins 0.000 abstract 2
- 102000004887 Transforming Growth Factor beta Human genes 0.000 abstract 2
- 108090001012 Transforming Growth Factor beta Proteins 0.000 abstract 2
- 108020003175 receptors Proteins 0.000 abstract 2
- ZRKFYGHZFMAOKI-QMGMOQQFSA-N tgfbeta Chemical compound C([C@H](NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCSC)C(C)C)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(O)=O)C1=CC=C(O)C=C1 ZRKFYGHZFMAOKI-QMGMOQQFSA-N 0.000 abstract 2
- 102100034134 Activin receptor type-1B Human genes 0.000 abstract 1
- 102000005606 Activins Human genes 0.000 abstract 1
- 108010059616 Activins Proteins 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 239000000488 activin Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- 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
-
- 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
- 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
- A61P11/08—Bronchodilators
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic 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
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
-
- 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
-
- 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
-
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Cardiology (AREA)
- Neurology (AREA)
- Heart & Thoracic Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Ophthalmology & Optometry (AREA)
- Oncology (AREA)
- Psychiatry (AREA)
- Gynecology & Obstetrics (AREA)
- Gastroenterology & Hepatology (AREA)
- Obesity (AREA)
- Vascular Medicine (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente invención proporciona un derivado imidazol 2-piridilo sustituido novedoso, o una sal o solvato farmacéuticamente aceptable del mismo, el cual inhibe selectivamente el receptor (ALK5) de tipo I del factor de crecimiento transformante ß (TGF-ß) y/o el receptor (ALK4) de tipo I de activina; una composición farmacéutica que comprende lo mismo como un ingrediente activo; y un uso del derivado imidazol 2-piridilo sustituido para la fabricación de un medicamento para prevenir o tratar una enfermedad mediada por los receptores ALK5 y/o ALK4 en un mamífero.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161507305P | 2011-07-13 | 2011-07-13 | |
| PCT/KR2012/005617 WO2013009140A2 (en) | 2011-07-13 | 2012-07-13 | 2-pyridyl substituted imidazoles as alk5 and/or alk4 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2014000309A MX2014000309A (es) | 2014-02-27 |
| MX369576B true MX369576B (es) | 2019-11-13 |
Family
ID=47506748
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2014000309A MX369576B (es) | 2011-07-13 | 2012-07-13 | Imidazoles 2-piridilo sustituidos como inhibidores de alk5 y/o alk4. |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US10155763B2 (es) |
| EP (1) | EP2731949B1 (es) |
| JP (1) | JP6094975B2 (es) |
| KR (1) | KR101938368B1 (es) |
| CN (1) | CN103764655B (es) |
| AU (1) | AU2012281281B2 (es) |
| BR (1) | BR112014000774B1 (es) |
| CA (1) | CA2841252C (es) |
| DK (1) | DK2731949T3 (es) |
| ES (1) | ES2671581T3 (es) |
| MX (1) | MX369576B (es) |
| NO (1) | NO2861601T3 (es) |
| PL (1) | PL2731949T3 (es) |
| PT (1) | PT2731949T (es) |
| RU (1) | RU2612958C2 (es) |
| TR (1) | TR201808033T4 (es) |
| WO (1) | WO2013009140A2 (es) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015157093A1 (en) * | 2014-04-08 | 2015-10-15 | Rigel Pharmaceuticals, Inc. | 2,3-disubstituted pyridine compounds as tgf-beta inhibitors and methods of use |
| WO2016081364A1 (en) * | 2014-11-21 | 2016-05-26 | Rigel Pharmaceuticals, Inc. | Fused imidazole derivatives as tgf-beta inhibitors |
| US10071079B2 (en) | 2016-06-29 | 2018-09-11 | Bristol-Myers Squibb Company | [1,2,4]triazolo[1,5-a]pyridinyl substituted indole compounds |
| CA3035115C (en) | 2016-07-29 | 2021-10-26 | Shanghai Yingli Pharmaceutical Co., Ltd | Nitrogenous heterocyclic aromatic compound, preparation method therefor, pharmaceutical composition thereof, and application thereof |
| US10906905B2 (en) | 2016-10-14 | 2021-02-02 | Jiangsu Hengrui Medicine Co., Ltd. | Five-membered heteroaryl ring bridged ring derivative, preparation method therefor and medical use thereof |
| WO2018086609A1 (zh) | 2016-11-14 | 2018-05-17 | 江苏恒瑞医药股份有限公司 | 3,4-二吡啶基吡唑类衍生物、其制备方法及其在医药上的应用 |
| CN109983015B (zh) * | 2017-03-22 | 2021-09-03 | 江苏恒瑞医药股份有限公司 | 6-吡唑-[1,2,4]三唑并[4,3-a]吡啶-3-酰胺类衍生物、其制备方法及其在医药上的应用 |
| EP3600294B1 (en) | 2017-03-23 | 2025-09-03 | Clavius Pharmaceuticals, LLC | Tri-substituted imidazoles for the inhibition of tgf beta and methods of treatment |
| GB201718285D0 (en) | 2017-11-03 | 2017-12-20 | Discuva Ltd | Antibacterial Compounds |
| CA3103995A1 (en) | 2018-07-26 | 2020-01-30 | Sumitomo Dainippon Pharma Oncology, Inc. | Methods for treating diseases associated with abnormal acvr1 expression and acvr1 inhibitors for use in the same |
| JP7147048B2 (ja) * | 2018-08-22 | 2022-10-04 | クラヴィウス ファーマシューティカルズ,エルエルシー | Tgf-ベータを阻害するための置換イミダゾールおよび処置方法 |
| CN113195467A (zh) | 2018-12-11 | 2021-07-30 | 施万生物制药研发Ip有限责任公司 | 适用作alk5抑制剂的萘啶和喹啉衍生物 |
| JP2022517951A (ja) * | 2019-01-10 | 2022-03-11 | スミトモ ダイニッポン ファーマ オンコロジー, インコーポレイテッド | 骨髄異形成症候群を処置するためのalk5阻害剤 |
| CN110563735B (zh) * | 2019-09-27 | 2022-03-29 | 江苏好收成韦恩农化股份有限公司 | 制备双氟磺草胺的方法 |
| EP4061809A1 (en) | 2019-11-22 | 2022-09-28 | Theravance Biopharma R&D IP, LLC | Substituted 1,5-naphthyridines or quinolines as alk5 inhibitors |
| EP4065572A1 (en) * | 2019-11-28 | 2022-10-05 | Origo Biopharma, S.L. | Benzylamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5 |
| US20230090552A1 (en) | 2020-01-08 | 2023-03-23 | Synthis Therapeutics, Inc. | Alk5 inhibitor conjugates and uses thereof |
| JP2023530734A (ja) * | 2020-06-18 | 2023-07-19 | ザ ボード オブ トラスティーズ オブ ザ レランド スタンフォード ジュニア ユニバーシティー | アイソフォーム特異的アルデヒドデヒドロゲナーゼ阻害剤 |
| KR20230051500A (ko) | 2020-07-15 | 2023-04-18 | 키에시 파르마슈티시 엣스. 피. 에이. | Alk5 억제제로서 피리다진일 아미노 유도체 |
| US20240116947A1 (en) | 2020-07-15 | 2024-04-11 | Chiesi Farmaceutici S.P.A. | Pyrido oxazine derivatives as alk5 inhibitors |
| ES2984546T3 (es) | 2020-07-15 | 2024-10-29 | Chiesi Farm Spa | Derivados de amino pirido-oxazina como inhibidores de ALK5 |
| EP3978487A1 (en) * | 2020-09-30 | 2022-04-06 | Origo Biopharma, S.L. | 2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-acetamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5 |
| EP4267584A1 (en) | 2020-12-23 | 2023-11-01 | Chiesi Farmaceutici S.p.A. | Pyrido oxazine derivatives as alk5 inhibitors |
| CN112759592A (zh) * | 2021-02-01 | 2021-05-07 | 无锡鸣鹭医药科技有限公司 | 一种6-碘[1,2,3]三唑并[1,5-a]吡啶的合成方法 |
| US20240342166A1 (en) | 2021-07-28 | 2024-10-17 | Tiumbio Co., Ltd. | Pharmaceutical composition for preventing or treating tumor, and use thereof |
| EP4514802A1 (en) | 2022-04-27 | 2025-03-05 | Chiesi Farmaceutici S.p.A. | Imidazole derivatives as alk5 inhibitors |
| US20250368650A1 (en) | 2022-06-22 | 2025-12-04 | Chiesi Farmaceutici S.P.A. | 5-(4-fluorophenyl)-2,3-dihydro-1h-imidazo[1,2-a]imidazole derivatives as alk inhibitors for the treatment of fibrosis |
| EP4651877A1 (en) * | 2023-01-17 | 2025-11-26 | Baylor College of Medicine | Inhibitors of activin receptor type 1 (acvr1) and activin receptor like type 1 (acvrl1), and methods using same |
| CN121712526A (zh) | 2023-06-13 | 2026-03-20 | 辛瑟斯治疗股份有限公司 | 抗cd5抗体及其用途 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4175127A (en) * | 1978-09-27 | 1979-11-20 | Smithkline Corporation | Pyridyl substituted 2,3-dihydroimidazo[2,1-b]thiazoles |
| CN86108538A (zh) * | 1985-12-12 | 1987-07-29 | 史密丝克莱恩贝克曼公司 | 5-脂肪氧合酶途径的抑制 |
| US4719218A (en) * | 1985-12-12 | 1988-01-12 | Smithkline Beckman Corporation | Pyrrolo[1,2-a]imidazole and pyrrolo[1,2-a]pyridine derivatives and their use as 5-lipoxygenase pathway inhibitor |
| ZW24186A1 (en) * | 1985-12-12 | 1987-07-08 | Smithkline Beckman Corp | Inhibition of the 5-lipoxygenase pathway |
| KR920702606A (ko) * | 1989-06-13 | 1992-10-06 | 스튜어트 알. 슈터 | 모노킨(Monokine)의 활성저해 |
| JPH04273877A (ja) * | 1991-02-28 | 1992-09-30 | Sumitomo Pharmaceut Co Ltd | 新規なイミダゾール誘導体 |
| DE60001229T2 (de) | 1999-04-09 | 2003-10-30 | Smithkline Beecham Corp., Philadelphia | Triarylimidazole |
| US6492408B1 (en) * | 1999-07-21 | 2002-12-10 | Boehringer Ingelheim Pharmaceuticals, Inc. | Small molecules useful in the treatment of inflammatory disease |
| CO5271680A1 (es) | 2000-02-21 | 2003-04-30 | Smithkline Beecham Corp | Compuestos |
| GB0007405D0 (en) | 2000-03-27 | 2000-05-17 | Smithkline Beecham Corp | Compounds |
| GB0100762D0 (en) | 2001-01-11 | 2001-02-21 | Smithkline Beecham Plc | Novel use |
| GB0108770D0 (en) * | 2001-04-06 | 2001-05-30 | Eisai London Res Lab Ltd | Inhibitors |
| AR039241A1 (es) | 2002-04-04 | 2005-02-16 | Biogen Inc | Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos |
| EP1539749A4 (en) * | 2002-09-13 | 2007-06-13 | Merck & Co Inc | BY CONDENSED HETEROBICYCLOGRUPPEN SUBSTITUTED PHENYL COMPOUNDS AS METOBOTROPE GLUTAMATE-5 MODULATORS |
| WO2004050659A1 (en) * | 2002-11-27 | 2004-06-17 | Eli Lilly And Company | Novel compounds as pharmaceutical agents |
| PA8595001A1 (es) * | 2003-03-04 | 2004-09-28 | Pfizer Prod Inc | Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf) |
| US20080319012A1 (en) * | 2004-04-21 | 2008-12-25 | In2Gen Co., Ltd. | 2-Pyridyl substituted imidazoles as ALK5 and/or ALK4 inhibitors |
| EP1910370B1 (en) * | 2005-07-22 | 2015-04-22 | Eli Lilly And Company | A pyridin quinolin substituted pyrrolo [1,2-b] pyrazole monohydrate as tgf-beta inhibitor |
-
2012
- 2012-07-13 TR TR2018/08033T patent/TR201808033T4/tr unknown
- 2012-07-13 CA CA2841252A patent/CA2841252C/en active Active
- 2012-07-13 PL PL12811865T patent/PL2731949T3/pl unknown
- 2012-07-13 CN CN201280034416.4A patent/CN103764655B/zh active Active
- 2012-07-13 BR BR112014000774-8A patent/BR112014000774B1/pt active IP Right Grant
- 2012-07-13 DK DK12811865.0T patent/DK2731949T3/en active
- 2012-07-13 RU RU2014105169A patent/RU2612958C2/ru active
- 2012-07-13 MX MX2014000309A patent/MX369576B/es active IP Right Grant
- 2012-07-13 PT PT128118650T patent/PT2731949T/pt unknown
- 2012-07-13 WO PCT/KR2012/005617 patent/WO2013009140A2/en not_active Ceased
- 2012-07-13 EP EP12811865.0A patent/EP2731949B1/en active Active
- 2012-07-13 AU AU2012281281A patent/AU2012281281B2/en active Active
- 2012-07-13 US US13/548,785 patent/US10155763B2/en active Active
- 2012-07-13 JP JP2014520137A patent/JP6094975B2/ja active Active
- 2012-07-13 ES ES12811865.0T patent/ES2671581T3/es active Active
- 2012-07-13 KR KR1020147003555A patent/KR101938368B1/ko active Active
-
2013
- 2013-06-07 NO NO13729240A patent/NO2861601T3/no unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR20140050048A (ko) | 2014-04-28 |
| AU2012281281B2 (en) | 2017-06-01 |
| PT2731949T (pt) | 2018-06-15 |
| EP2731949A4 (en) | 2014-12-17 |
| RU2612958C2 (ru) | 2017-03-14 |
| ES2671581T3 (es) | 2018-06-07 |
| WO2013009140A2 (en) | 2013-01-17 |
| BR112014000774A8 (pt) | 2017-10-10 |
| WO2013009140A3 (en) | 2013-04-11 |
| CN103764655A (zh) | 2014-04-30 |
| KR101938368B1 (ko) | 2019-01-14 |
| RU2014105169A (ru) | 2015-08-20 |
| BR112014000774B1 (pt) | 2022-03-29 |
| CA2841252C (en) | 2019-02-26 |
| TR201808033T4 (tr) | 2018-06-21 |
| US10155763B2 (en) | 2018-12-18 |
| NO2861601T3 (es) | 2018-07-07 |
| BR112014000774A2 (pt) | 2016-08-23 |
| PL2731949T3 (pl) | 2018-10-31 |
| US20130018052A1 (en) | 2013-01-17 |
| JP6094975B2 (ja) | 2017-03-15 |
| DK2731949T3 (en) | 2018-06-14 |
| EP2731949A2 (en) | 2014-05-21 |
| CA2841252A1 (en) | 2013-01-17 |
| AU2012281281A1 (en) | 2014-03-06 |
| EP2731949B1 (en) | 2018-04-04 |
| CN103764655B (zh) | 2017-04-12 |
| MX2014000309A (es) | 2014-02-27 |
| JP2014520846A (ja) | 2014-08-25 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| MX369576B (es) | Imidazoles 2-piridilo sustituidos como inhibidores de alk5 y/o alk4. | |
| PH12018501807A1 (en) | Pyrazolopyrrolidine derivatives and their use in the treatment of diseas | |
| PH12012502512A1 (en) | 2-pyridyl substituted imidazoles as therapeutic alk5 and/or alk4 inhibitors | |
| PH12016500756A1 (en) | Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors | |
| MX2015016344A (es) | Derivados de imidazo-pirrolidinona y su uso en el tratamiento de enfermedades. | |
| CY1116328T1 (el) | Παραγωγα 4 - αμινοπυριμιδινης και η χρηση τους ως ανταγωνιστων α2α υποδοχεων αδενοσινης | |
| PH12012501800A1 (en) | 2,3 dihydro- 1h - inden- 1 - yl -2,7 -diazaspirol [ 3.5 ] nonane derivatives and their use as antagonists or inverse agonists of the ghrelin receptor | |
| MX2015008975A (es) | Analogos de tiadiazol y metodos para el tratamiento de afecciones relacionadas con deficiencia del gen de supervivencia de las neuronas motoras (smn). | |
| EA033689B9 (ru) | Ингибиторы g12c kras | |
| JO3425B1 (ar) | مشتقات البابيريدينيل-اندول واستخدامها كعامل متمم لمثبطات b | |
| MX2015016421A (es) | Derivados de pirazolo-pirrolidin-4-ona como inhibidores de bet y su uso en el tratamiento de enfermedades. | |
| MX2016006667A (es) | Derivados de pirrolo-pirrolona y su uso como inhibidores. | |
| JO3078B1 (ar) | مورفولينوثيازولات بصفتها منظمات الوستيرية نوع الفا 7 موجبة | |
| MX2017012295A (es) | Derivados formilados n-heterociclicos como inhibidores de fgfr4. | |
| ZA202002762B (en) | Benzimidazole derivatives and their uses | |
| PH12016502246A1 (en) | Carboxamide derivatives | |
| MY161236A (en) | (pyridin-4-yl)benzylamides as allosteric modulators of alpha 7 nachr | |
| MX2016014946A (es) | Derivados de carboxamida. | |
| MY162554A (en) | Novel benzamide derivatives | |
| JOP20200127A1 (ar) | مشتقات بيريدينون واستخدامها كمثبطات alk-2 انتقائية | |
| PH12019500327A1 (en) | Indazole compounds for use in tendon and/or ligament injuries | |
| MX2012008611A (es) | Sales farmaceuticas aceptables de derivados heterociclicos pirrolo-nitrogenosos, su metodo de preparacion y uso medico. | |
| MX2014014813A (es) | Uso de agonistas o antagonistas inversos para el receptor de grelina para tratar trastornos del sueño. | |
| PH12016502247A1 (en) | Carboxamide derivatives |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| GB | Transfer or rights |
Owner name: TIUMBIO CO., LTD. |
|
| FG | Grant or registration |