SG11201806438UA - Fused Pyrazole Derivatives, Preparation Method Thereof, And Use Thereof In Treatment Of Cancers, Inflammation And Immune Diseases - Google Patents
Fused Pyrazole Derivatives, Preparation Method Thereof, And Use Thereof In Treatment Of Cancers, Inflammation And Immune DiseasesInfo
- Publication number
- SG11201806438UA SG11201806438UA SG11201806438UA SG11201806438UA SG11201806438UA SG 11201806438U A SG11201806438U A SG 11201806438UA SG 11201806438U A SG11201806438U A SG 11201806438UA SG 11201806438U A SG11201806438U A SG 11201806438UA SG 11201806438U A SG11201806438U A SG 11201806438UA
- Authority
- SG
- Singapore
- Prior art keywords
- preparation
- same
- cancers
- inflammation
- treatment
- Prior art date
Links
Classifications
-
- 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
- C07D471/22—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 systems contains four or more hetero 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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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]
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
The present invention relates to pyrazole fused-ring derivatives, their preparation methods, and use thereof in medicine. In particular, the present invention relates to a novel derivative 5 represented by formula (I), and a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising the same and a method for preparing the same. The present invention also relates to use of the derivatives and the pharmaceutically acceptable salt thereof or the pharmaceutical composition comprising the same in the preparation of therapeutic agents, in particular Bruton tyrosine kinase inhibitors, and preparing a medicament for treating and/or 10 preventing tumors and inflammatory associated diseases. The substituents on formula (I) are defined same as in the specification. B i- `B- Li ., P -----L , A3 R 4 N, 1 A v \ A .1 \"-A2 - --L2 - - ^ . R2 (I) 15
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610066886.9A CN107021963A (en) | 2016-01-29 | 2016-01-29 | Pyrazole fused ring analog derivative, its preparation method and its application in treating cancer, inflammation and immunity disease |
| PCT/CN2016/112625 WO2017128917A1 (en) | 2016-01-29 | 2016-12-28 | Parazole condensed-ring derivatives and preparation method thereof and application thereof in treatment of cancers, inflammation and immune diseases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201806438UA true SG11201806438UA (en) | 2018-08-30 |
Family
ID=59397319
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201806438UA SG11201806438UA (en) | 2016-01-29 | 2016-12-28 | Fused Pyrazole Derivatives, Preparation Method Thereof, And Use Thereof In Treatment Of Cancers, Inflammation And Immune Diseases |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US10336755B2 (en) |
| EP (1) | EP3409672B1 (en) |
| JP (1) | JP7043409B2 (en) |
| KR (1) | KR20180104132A (en) |
| CN (2) | CN107021963A (en) |
| AU (1) | AU2016389434B2 (en) |
| CA (1) | CA3012882A1 (en) |
| CY (1) | CY1124970T1 (en) |
| DK (1) | DK3409672T3 (en) |
| ES (1) | ES2902128T3 (en) |
| HK (1) | HK1256798A1 (en) |
| HR (1) | HRP20212020T1 (en) |
| HU (1) | HUE057319T2 (en) |
| LT (1) | LT3409672T (en) |
| PL (1) | PL3409672T3 (en) |
| PT (1) | PT3409672T (en) |
| RS (1) | RS62768B1 (en) |
| SG (1) | SG11201806438UA (en) |
| SI (1) | SI3409672T1 (en) |
| WO (1) | WO2017128917A1 (en) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI795381B (en) | 2016-12-21 | 2023-03-11 | 比利時商健生藥品公司 | Pyrazole derivatives as malt1 inhibitors |
| CA3077238C (en) * | 2017-09-28 | 2022-04-12 | Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | 4,6,7-trisubstituted 1,2-dihydropyrrolo[3,4-c]pyridin/pyrimidin-3-one derivatives and uses thereof |
| CN112955444B (en) * | 2019-01-22 | 2023-12-12 | 江苏恒瑞医药股份有限公司 | Novel small molecule CD73 inhibitor, preparation method thereof and application thereof in medicine |
| WO2020187267A1 (en) * | 2019-03-18 | 2020-09-24 | 上海海雁医药科技有限公司 | Btk inhibitor, pharmaceutically acceptable salt, polymorph and application thereof |
| CN114364798A (en) | 2019-03-21 | 2022-04-15 | 欧恩科斯欧公司 | Combination of Dbait molecules with kinase inhibitors for the treatment of cancer |
| JP7554768B2 (en) * | 2019-04-11 | 2024-09-20 | ヤンセン ファーマシューティカ エヌ．ベー． | Urea Derivatives as MALT1 Inhibitors |
| US20220401436A1 (en) | 2019-11-08 | 2022-12-22 | INSERM (Institute National de la Santé et de la Recherche Médicale) | 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 |
| JP2023535279A (en) | 2020-06-22 | 2023-08-17 | コーセプト セラピューティクス， インコーポレイテッド | Quaternary indazole glucocorticoid receptor antagonist |
| WO2022048551A1 (en) * | 2020-09-01 | 2022-03-10 | 上海海雁医药科技有限公司 | Polymorph of bruton's tyrosine kinase inhibitor, and preparation method therefor and use thereof |
| US12098141B2 (en) | 2021-12-21 | 2024-09-24 | Corcept Therapeutics Incorporated | Bicyclic indazole glucocorticoid receptor antagonists |
| IL313663A (en) | 2021-12-21 | 2024-08-01 | Corcept Therapeutics Inc | Piperazine indazole glucocorticoid receptor antagonists |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0100624D0 (en) | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical compounds VII |
| AU2005323311A1 (en) | 2004-11-23 | 2006-07-13 | Venkateswara Rao Batchu | Novel bicyclic heterocyclic compounds, process for their preparation and compositions containing them |
| US20090234117A1 (en) | 2005-05-27 | 2009-09-17 | Toshihiko Kashiwagi | Pyrazolopyrimidine Derivative |
| CN101421269A (en) | 2006-01-13 | 2009-04-29 | 环状药物公司 | Inhibitors of tyrosine kinases and uses thereof |
| CA2644910C (en) | 2006-03-31 | 2014-01-28 | Abbott Laboratories | Indazole compounds |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| EP2424368B1 (en) | 2009-04-29 | 2014-12-31 | Locus Pharmaceuticals, Inc. | Pyrrolotriazine compounds |
| EP2464647B1 (en) | 2009-08-11 | 2016-09-21 | Bristol-Myers Squibb Company | Azaindazoles as btk kinase modulators and use thereof |
| BR112012011147A2 (en) * | 2009-11-12 | 2021-09-08 | F.Hoffmann-La Roche Ag | COMPOUND, PHARMACEUTICAL COMPOSITION AND USE OF A COMPOUND. |
| US8703767B2 (en) | 2011-04-01 | 2014-04-22 | University Of Utah Research Foundation | Substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase BTK inhibitors |
| US8962831B2 (en) | 2011-05-17 | 2015-02-24 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| AU2012285988B2 (en) | 2011-07-19 | 2017-05-25 | Merck Sharp & Dohme B.V. | 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides Btk-inhibitors |
| CN103073508B (en) | 2011-10-25 | 2016-06-01 | 北京大学深圳研究生院 | The method of inhibitors of kinases and treatment relevant disease |
| RU2615999C2 (en) | 2011-11-29 | 2017-04-12 | Оно Фармасьютикал Ко., Лтд. | Hydrochloride of derivative purinona |
| JP5985658B2 (en) | 2012-01-31 | 2016-09-06 | ナンジン アルゲン ファルマ カンパニー リミテッドＮａｎｊｉｎｇ Ａｌｌｇｅｎ Ｐｈａｒｍａ Ｃｏ． Ｌｔｄ． | Cyclic molecules as breton tyrosine kinase inhibitors |
| KR20130091464A (en) | 2012-02-08 | 2013-08-19 | 한미약품 주식회사 | Triazolopyridine derivatives as a tyrosine kinase inhibitor |
| US20150291554A1 (en) | 2012-11-02 | 2015-10-15 | Pfizer Inc. | Bruton's Tyrosine Kinase Inhibitors |
| WO2014125410A1 (en) | 2013-02-12 | 2014-08-21 | Aurigene Discovery Technologies Limited | N-substituted heterocyclic derivatives as kinase inhibitors |
| CN103113375B (en) | 2013-02-21 | 2017-09-15 | 南京勇山生物科技有限公司 | Pyrazole simultaneously [3,4 d] pyrimidines and preparation method thereof |
| US9242969B2 (en) | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
| ES2619125T3 (en) | 2013-04-25 | 2017-06-23 | Beigene, Ltd. | Heterocyclic compounds fused as protein kinase inhibitors |
| US9662311B2 (en) | 2013-06-21 | 2017-05-30 | Zenith Epigenetics Ltd. | Substituted bicyclic compounds as bromodomain inhibitors |
| CN105814057B (en) | 2013-07-31 | 2019-05-03 | 默克专利有限公司 | Pyrimidine, pyridine and pyrazine as BTK inhibitor and application thereof |
| TN2016000094A1 (en) | 2013-09-30 | 2017-07-05 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase. |
-
2016
- 2016-01-29 CN CN201610066886.9A patent/CN107021963A/en not_active Withdrawn
- 2016-12-28 US US16/073,607 patent/US10336755B2/en active Active
- 2016-12-28 CA CA3012882A patent/CA3012882A1/en not_active Abandoned
- 2016-12-28 PT PT168877884T patent/PT3409672T/en unknown
- 2016-12-28 SG SG11201806438UA patent/SG11201806438UA/en unknown
- 2016-12-28 DK DK16887788.4T patent/DK3409672T3/en active
- 2016-12-28 KR KR1020187024923A patent/KR20180104132A/en not_active Application Discontinuation
- 2016-12-28 EP EP16887788.4A patent/EP3409672B1/en active Active
- 2016-12-28 CN CN201680080472.XA patent/CN108602818B/en active Active
- 2016-12-28 JP JP2018539817A patent/JP7043409B2/en active Active
- 2016-12-28 SI SI201631429T patent/SI3409672T1/en unknown
- 2016-12-28 HU HUE16887788A patent/HUE057319T2/en unknown
- 2016-12-28 PL PL16887788T patent/PL3409672T3/en unknown
- 2016-12-28 ES ES16887788T patent/ES2902128T3/en active Active
- 2016-12-28 HR HRP20212020TT patent/HRP20212020T1/en unknown
- 2016-12-28 WO PCT/CN2016/112625 patent/WO2017128917A1/en active Application Filing
- 2016-12-28 LT LTEPPCT/CN2016/112625T patent/LT3409672T/en unknown
- 2016-12-28 AU AU2016389434A patent/AU2016389434B2/en not_active Ceased
- 2016-12-28 RS RS20211556A patent/RS62768B1/en unknown
-
2018
- 2018-12-11 HK HK18115881.0A patent/HK1256798A1/en unknown
-
2021
- 2021-12-30 CY CY20211101138T patent/CY1124970T1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| NZ744870A (en) | 2022-03-25 |
| ES2902128T3 (en) | 2022-03-25 |
| HK1256798A1 (en) | 2019-10-04 |
| WO2017128917A1 (en) | 2017-08-03 |
| SI3409672T1 (en) | 2022-03-31 |
| WO2017128917A8 (en) | 2017-09-14 |
| CA3012882A1 (en) | 2017-08-03 |
| CN107021963A (en) | 2017-08-08 |
| EP3409672A4 (en) | 2019-07-10 |
| CY1124970T1 (en) | 2023-01-05 |
| JP2019503393A (en) | 2019-02-07 |
| KR20180104132A (en) | 2018-09-19 |
| AU2016389434A1 (en) | 2018-08-23 |
| CN108602818A (en) | 2018-09-28 |
| HUE057319T2 (en) | 2022-04-28 |
| JP7043409B2 (en) | 2022-03-29 |
| PT3409672T (en) | 2022-01-05 |
| RS62768B1 (en) | 2022-01-31 |
| EP3409672B1 (en) | 2021-12-08 |
| US20190016721A1 (en) | 2019-01-17 |
| DK3409672T3 (en) | 2022-01-10 |
| HRP20212020T1 (en) | 2022-04-01 |
| AU2016389434B2 (en) | 2021-03-11 |
| EP3409672A1 (en) | 2018-12-05 |
| PL3409672T3 (en) | 2022-02-21 |
| CN108602818B (en) | 2021-12-21 |
| US10336755B2 (en) | 2019-07-02 |
| LT3409672T (en) | 2022-01-10 |
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