CA2853970A1 - Alkylated piperazine compounds as inhibitors of btk activity - Google Patents
Alkylated piperazine compounds as inhibitors of btk activity Download PDFInfo
- Publication number
- CA2853970A1 CA2853970A1 CA2853970A CA2853970A CA2853970A1 CA 2853970 A1 CA2853970 A1 CA 2853970A1 CA 2853970 A CA2853970 A CA 2853970A CA 2853970 A CA2853970 A CA 2853970A CA 2853970 A1 CA2853970 A1 CA 2853970A1
- Authority
- CA
- Canada
- Prior art keywords
- mmol
- compound
- oxo
- pyridin
- mixture
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- 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
- C07D405/14—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 three or more hetero rings
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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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
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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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
- A61K31/535—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
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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- 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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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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- A—HUMAN NECESSITIES
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed systems
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Oncology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Biomedical Technology (AREA)
- Ophthalmology & Optometry (AREA)
- Obesity (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Vascular Medicine (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161555395P | 2011-11-03 | 2011-11-03 | |
| US61/555,395 | 2011-11-03 | ||
| PCT/US2012/063198 WO2013067277A1 (en) | 2011-11-03 | 2012-11-02 | Alkylated piperazine compounds as inhibitors of btk activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2853970A1 true CA2853970A1 (en) | 2013-05-10 |
Family
ID=47146780
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2853970A Abandoned CA2853970A1 (en) | 2011-11-03 | 2012-11-02 | Alkylated piperazine compounds as inhibitors of btk activity |
Country Status (23)
| Country | Link |
|---|---|
| US (3) | US8729072B2 (enExample) |
| EP (1) | EP2773639B1 (enExample) |
| JP (2) | JP5976828B2 (enExample) |
| KR (1) | KR101716011B1 (enExample) |
| CN (1) | CN104024255B (enExample) |
| AR (1) | AR088642A1 (enExample) |
| AU (1) | AU2012332368A1 (enExample) |
| BR (1) | BR112014010439A2 (enExample) |
| CA (1) | CA2853970A1 (enExample) |
| CL (1) | CL2014001158A1 (enExample) |
| CO (1) | CO6950475A2 (enExample) |
| CR (1) | CR20140187A (enExample) |
| EA (1) | EA027561B1 (enExample) |
| IL (1) | IL232280A0 (enExample) |
| IN (1) | IN2014CN03265A (enExample) |
| MA (1) | MA35725B1 (enExample) |
| MX (1) | MX2014005289A (enExample) |
| PE (1) | PE20141686A1 (enExample) |
| PH (1) | PH12014500966A1 (enExample) |
| SG (1) | SG11201401993RA (enExample) |
| TW (1) | TW201326171A (enExample) |
| WO (1) | WO2013067277A1 (enExample) |
| ZA (1) | ZA201403158B (enExample) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013021374A2 (en) | 2011-08-05 | 2013-02-14 | Mitraltech Ltd. | Techniques for percutaneous mitral valve replacement and sealing |
| BR112014010439A2 (pt) * | 2011-11-03 | 2017-04-18 | F Hoffmann - La Roche Ag | compostos, composição farmacêutica, processo de produção, método de tratamento de uma doença ou distúrbio, métodos, kit e uso de uma composição farmacêutica |
| UA111756C2 (uk) * | 2011-11-03 | 2016-06-10 | Ф. Хоффманн-Ля Рош Аг | Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона |
| WO2015000949A1 (en) | 2013-07-03 | 2015-01-08 | F. Hoffmann-La Roche Ag | Heteroaryl pyridone and aza-pyridone amide compounds |
| EP3077384B1 (en) | 2013-12-05 | 2017-09-06 | F. Hoffmann-La Roche AG | Heteroaryl pyridone and aza-pyridone compounds with electrophilic functionality |
| JP6879740B2 (ja) | 2013-12-13 | 2021-06-02 | ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド | リンパ形質細胞性リンパ腫を処置する方法 |
| US9908872B2 (en) | 2013-12-13 | 2018-03-06 | Dana-Farber Cancer Institute, Inc. | Methods to treat lymphoplasmacytic lymphoma |
| WO2015151006A1 (en) | 2014-03-29 | 2015-10-08 | Lupin Limited | Substituted purine compounds as btk inhibitors |
| CA2946538A1 (en) | 2014-04-04 | 2015-10-08 | Del Mar Pharmaceuticals | Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer |
| WO2015170266A1 (en) | 2014-05-07 | 2015-11-12 | Lupin Limited | Substituted pyrimidine compounds as btk inhibitors |
| CN106922146B (zh) | 2014-10-02 | 2020-05-26 | 豪夫迈·罗氏有限公司 | 用于治疗由布鲁顿酪氨酸激酶(btk)介导的疾病的吡唑甲酰胺化合物 |
| JP6788583B2 (ja) | 2014-10-22 | 2020-11-25 | ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド | 増殖性疾患を処置するためのチアゾリル含有化合物 |
| WO2016066490A1 (en) | 2014-10-27 | 2016-05-06 | F. Hoffmann-La Roche Ag | Process for making tricyclic lactam compounds |
| CN105837576B (zh) | 2015-01-14 | 2019-03-26 | 湖北生物医药产业技术研究院有限公司 | Btk抑制剂 |
| MX384444B (es) * | 2015-03-10 | 2025-03-14 | Aurigene Discovery Tech Ltd | Compuestos de 1,2,4-oxadiazol y tiadiazol como inmunomoduladores |
| BR112018069530B1 (pt) | 2016-02-29 | 2021-02-17 | F. Hoffmann-La Roche Ag | composições de forma de dosagem que compreendem um inibidor da tirosina quinase de bruton |
| EP3548046A2 (en) | 2016-12-03 | 2019-10-09 | Juno Therapeutics, Inc. | Methods and compositions for use of therapeutic t cells in combination with kinase inhibitors |
| AU2017376580B2 (en) * | 2016-12-15 | 2020-08-13 | F. Hoffmann-La Roche Ag | Process for preparing BTK inhibitors |
| CN107445981B (zh) * | 2017-08-25 | 2018-06-22 | 牡丹江医学院 | 一种用于防治宫颈炎的活性化合物 |
| EP3930717A1 (en) | 2019-02-25 | 2022-01-05 | Guangzhou Lupeng Pharmaceutical Company Ltd. | Inhibitor of btk and mutants thereof |
| BR112021018168B1 (pt) | 2019-03-21 | 2023-11-28 | Onxeo | Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer |
| WO2021066958A1 (en) | 2019-10-05 | 2021-04-08 | Newave Pharmaceutical Inc. | Inhibitor of btk and mutants thereof |
| CA3159348A1 (en) | 2019-11-08 | 2021-05-14 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| WO2021164735A1 (en) | 2020-02-20 | 2021-08-26 | Hutchison Medipharma Limited | Heteroaryl heterocyclic compounds and uses thereof |
| CA3175788A1 (en) * | 2020-04-22 | 2021-10-28 | Claire LANGRISH | Treatment of acute respiratory distress syndrome and other disorders involving cytokine storm using btk inhibitors |
| US20230348471A1 (en) * | 2020-06-18 | 2023-11-02 | Shanghai Synergy Pharmaceutical Sciences Co., Ltd. | Bruton's tyrosine kinase inhibitor and preparation method therefor |
| EP4214206A4 (en) | 2020-09-21 | 2024-10-09 | Hutchison Medipharma Limited | HETEROCYCLIC HETEROARYL COMPOUNDS AND USES THEREOF |
| WO2022094172A2 (en) | 2020-10-30 | 2022-05-05 | Newave Pharmaceutical Inc. | Inhibitors of btk |
| US20240058457A1 (en) | 2020-12-20 | 2024-02-22 | Newave Pharmaceutical Inc. | Btk degrader |
| US20250154155A1 (en) * | 2022-01-28 | 2025-05-15 | Hutchmed Limited | Synthetic method of 7,8-dihydro-2h-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6h)-one compounds |
| CN119080748A (zh) * | 2024-08-29 | 2024-12-06 | 中南大学 | 一种靶向brd7抑瘤蛋白的增稳剂及其在制备治疗实体肿瘤药物中的应用 |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
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