KR101716011B1 - Btk 활성의 억제제인 알킬화된 피페라진 화합물 - Google Patents
Btk 활성의 억제제인 알킬화된 피페라진 화합물 Download PDFInfo
- Publication number
- KR101716011B1 KR101716011B1 KR1020147014782A KR20147014782A KR101716011B1 KR 101716011 B1 KR101716011 B1 KR 101716011B1 KR 1020147014782 A KR1020147014782 A KR 1020147014782A KR 20147014782 A KR20147014782 A KR 20147014782A KR 101716011 B1 KR101716011 B1 KR 101716011B1
- Authority
- KR
- South Korea
- Prior art keywords
- mmol
- fluoro
- methyl
- phenyl
- pyridin
- 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.)
- Expired - Fee Related
Links
- 0 CC=C(N)N=CC(N1CCN(*)CC1)=* Chemical compound CC=C(N)N=CC(N1CCN(*)CC1)=* 0.000 description 3
- IYFYLBRGTQCCGW-UHFFFAOYSA-N CC1(C)OB(c2cc(F)cc(N(C3=O)N=Cc4c3[s]c3c4CCCC3)c2COC(C)=O)OC1(C)C Chemical compound CC1(C)OB(c2cc(F)cc(N(C3=O)N=Cc4c3[s]c3c4CCCC3)c2COC(C)=O)OC1(C)C IYFYLBRGTQCCGW-UHFFFAOYSA-N 0.000 description 1
- LCKGWMCJLOFBAO-UHFFFAOYSA-N CCC(CN(CC1)C2COC2)N1c1ccc(NC2=CC(c3cc(F)cc(N(CCc4c5cc6[n]4CCCC6)C5=O)c3COC(C)=O)=CN(C)C2=O)nc1 Chemical compound CCC(CN(CC1)C2COC2)N1c1ccc(NC2=CC(c3cc(F)cc(N(CCc4c5cc6[n]4CCCC6)C5=O)c3COC(C)=O)=CN(C)C2=O)nc1 LCKGWMCJLOFBAO-UHFFFAOYSA-N 0.000 description 1
- GYPZSDXMAZSJRF-OYRHEFFESA-N CCOC([C@@H](CN(C1)S(c2ccccc2)(=O)=O)N(Cc2ccccc2)[C@@H]1C(OCC)=O)=O Chemical compound CCOC([C@@H](CN(C1)S(c2ccccc2)(=O)=O)N(Cc2ccccc2)[C@@H]1C(OCC)=O)=O GYPZSDXMAZSJRF-OYRHEFFESA-N 0.000 description 1
- VGRKPWHLVRPNAO-CYBMUJFWSA-N C[C@H](CN(CC1)C2COC2)N1c1ccc(NC2=CC(Br)=CN(C)C2=O)nc1 Chemical compound C[C@H](CN(CC1)C2COC2)N1c1ccc(NC2=CC(Br)=CN(C)C2=O)nc1 VGRKPWHLVRPNAO-CYBMUJFWSA-N 0.000 description 1
- SHEGBLQFOSBVPT-JOCHJYFZSA-N C[C@H](CN(CC1)C2COC2)N1c1ccc(NC2=CC(c3cc(F)cc(N(C4=O)N=Cc5c4[s]c4c5CCCC4)c3COC(C)=O)=CN(C)C2=O)nc1 Chemical compound C[C@H](CN(CC1)C2COC2)N1c1ccc(NC2=CC(c3cc(F)cc(N(C4=O)N=Cc5c4[s]c4c5CCCC4)c3COC(C)=O)=CN(C)C2=O)nc1 SHEGBLQFOSBVPT-JOCHJYFZSA-N 0.000 description 1
- YVIXIVOKRYMFMD-NWDGAFQWSA-N C[C@H](CN([C@@H](C)C1)c(cn2)ccc2[N+]([O-])=O)N1C(OC(C)(C)C)=O Chemical compound C[C@H](CN([C@@H](C)C1)c(cn2)ccc2[N+]([O-])=O)N1C(OC(C)(C)C)=O YVIXIVOKRYMFMD-NWDGAFQWSA-N 0.000 description 1
- FYYRXKIAVBUGCF-LOSJGSFVSA-N C[C@H](CN([C@@H](C)C1)c2ccc(NC3=CC(c4cc(F)cc(N(CC[n]5c6cc7c5CCCC7)C6=O)c4COC(C)=O)=CN(C)C3=O)nc2)N1C1COC1 Chemical compound C[C@H](CN([C@@H](C)C1)c2ccc(NC3=CC(c4cc(F)cc(N(CC[n]5c6cc7c5CCCC7)C6=O)c4COC(C)=O)=CN(C)C3=O)nc2)N1C1COC1 FYYRXKIAVBUGCF-LOSJGSFVSA-N 0.000 description 1
Images
Classifications
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
- A61P11/06—Antiasthmatics
-
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- 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
- 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
- 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
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
-
- 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
- A61P37/02—Immunomodulators
-
- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- 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
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic 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
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Transplantation (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Communicable Diseases (AREA)
- Ophthalmology & Optometry (AREA)
- Obesity (AREA)
- Virology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Vascular Medicine (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (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 (2)
| Publication Number | Publication Date |
|---|---|
| KR20140090227A KR20140090227A (ko) | 2014-07-16 |
| KR101716011B1 true KR101716011B1 (ko) | 2017-03-13 |
Family
ID=47146780
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020147014782A Expired - Fee Related KR101716011B1 (ko) | 2011-11-03 | 2012-11-02 | Btk 활성의 억제제인 알킬화된 피페라진 화합물 |
Country Status (23)
| Country | Link |
|---|---|
| US (3) | US8729072B2 (https=) |
| EP (1) | EP2773639B1 (https=) |
| JP (2) | JP5976828B2 (https=) |
| KR (1) | KR101716011B1 (https=) |
| CN (1) | CN104024255B (https=) |
| AR (1) | AR088642A1 (https=) |
| AU (1) | AU2012332368A1 (https=) |
| BR (1) | BR112014010439A2 (https=) |
| CA (1) | CA2853970A1 (https=) |
| CL (1) | CL2014001158A1 (https=) |
| CO (1) | CO6950475A2 (https=) |
| CR (1) | CR20140187A (https=) |
| EA (1) | EA027561B1 (https=) |
| IL (1) | IL232280A0 (https=) |
| IN (1) | IN2014CN03265A (https=) |
| MA (1) | MA35725B1 (https=) |
| MX (1) | MX2014005289A (https=) |
| PE (1) | PE20141686A1 (https=) |
| PH (1) | PH12014500966A1 (https=) |
| SG (1) | SG11201401993RA (https=) |
| TW (1) | TW201326171A (https=) |
| WO (1) | WO2013067277A1 (https=) |
| ZA (1) | ZA201403158B (https=) |
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 |
| MX2014005289A (es) * | 2011-11-03 | 2014-05-30 | Hoffmann La Roche | Compuestos de piperazina alquilados. |
| UA111756C2 (uk) | 2011-11-03 | 2016-06-10 | Ф. Хоффманн-Ля Рош Аг | Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона |
| RU2016101548A (ru) | 2013-07-03 | 2017-08-08 | Ф. Хоффманн-Ля Рош Аг | Соединения амидов гетероарилпиридона и азапиридона |
| WO2015082583A1 (en) | 2013-12-05 | 2015-06-11 | F. Hoffmann-La Roche Ag | Heteroaryl pyridone and aza-pyridone compounds with electrophilic functionality |
| EP3079682A4 (en) | 2013-12-13 | 2017-08-30 | Dana-Farber Cancer Institute, Inc. | Methods to treat lymphoplasmacytic lymphoma |
| US9856223B2 (en) | 2013-12-13 | 2018-01-02 | 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 |
| KR102359214B1 (ko) | 2014-04-04 | 2022-02-07 | 델 마 파마슈티컬스 | 폐의 비소세포 암종 및 난소암을 치료하기 위한 디안하이드로갈락티톨 및 이의 유사체 또는 유도체 |
| WO2015170266A1 (en) | 2014-05-07 | 2015-11-12 | Lupin Limited | Substituted pyrimidine compounds as btk inhibitors |
| JP6507234B2 (ja) * | 2014-10-02 | 2019-04-24 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | ブルトンチロシンキナーゼ(btk)によって介入される障害の処置における使用のためのピラゾールカルボキサミド化合物 |
| US10112957B2 (en) | 2014-10-22 | 2018-10-30 | Dana-Farber Cancer Institute, Inc. | Thiazolyl-containing compounds for treating proliferative diseases |
| EP3212645B1 (en) | 2014-10-27 | 2018-11-28 | 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 |
| NZ734650A (en) * | 2015-03-10 | 2023-07-28 | Aurigene Oncology Ltd | 1,2,4-oxadiazole and thiadiazole compounds as immunomodulators |
| EP4049660B1 (en) | 2016-02-29 | 2025-02-19 | F. Hoffmann-La Roche AG | Dosage form compositions comprising an inhibitor of bruton's tyrosine kinase |
| MA46995A (fr) | 2016-12-03 | 2019-10-09 | Acerta Pharma Bv | Méthodes et compositions pour l'utilisation de lymphocytes t thérapeutiques en association avec des inhibiteurs de kinase |
| SG10202009148XA (en) * | 2016-12-15 | 2020-10-29 | Hoffmann La Roche | 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 |
| US20220143049A1 (en) | 2019-03-21 | 2022-05-12 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| WO2021066958A1 (en) | 2019-10-05 | 2021-04-08 | Newave Pharmaceutical Inc. | Inhibitor of btk and mutants thereof |
| EP4054579A1 (en) | 2019-11-08 | 2022-09-14 | Institut National de la Santé et de la Recherche Médicale (INSERM) | 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 |
| CA3171012A1 (en) | 2020-02-20 | 2021-08-26 | Hutchison Medipharma Limited | Heteroaryl heterocyclic compounds and uses thereof |
| IL297316A (en) * | 2020-04-22 | 2022-12-01 | Principia Biopharma Inc | Treatment of acute respiratory distress syndrome and other disorders involving cytokine storm using btk inhibitors |
| CN115715291B (zh) * | 2020-06-18 | 2025-04-29 | 上海华汇拓医药科技有限公司 | 布鲁顿酪氨酸激酶抑制剂及其制备方法 |
| CA3195525A1 (en) | 2020-09-21 | 2022-03-24 | Hutchison Medipharma Limited | Heteroaryl heterocyclic compounds and uses thereof |
| US20230382900A1 (en) | 2020-10-30 | 2023-11-30 | Newave Pharmaceutical Inc. | Inhibitors of btk |
| WO2022133184A1 (en) | 2020-12-20 | 2022-06-23 | Newave Pharmaceutical Inc. | Btk degrader |
| EP4471012A4 (en) * | 2022-01-28 | 2026-01-21 | Hutchmed Ltd | PROCESS FOR THE SYNTHESIS OF A 7,8-DIHYDRO-2H-CYCLOPENTAPYRROLOPYRAZINONE COMPOUND |
| 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 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010122038A1 (en) | 2009-04-24 | 2010-10-28 | F. Hoffmann-La Roche Ag | Inhibitors of bruton's tyrosine kinase |
| WO2010126960A1 (en) | 2009-04-29 | 2010-11-04 | Locus Pharmaceuticals, Inc. | Pyrrolotriazine compounds |
| WO2011140488A1 (en) | 2010-05-07 | 2011-11-10 | Gilead Connecticut, Inc. | Pyridone and aza-pyridone compounds and methods of use |
| WO2012031004A1 (en) | 2010-09-01 | 2012-03-08 | Gilead Connecticut, Inc. | Pyridinones/pyrazinones, method of making, and method of use thereof |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| US5583024A (en) | 1985-12-02 | 1996-12-10 | The Regents Of The University Of California | Recombinant expression of Coleoptera luciferase |
| US5543523A (en) | 1994-11-15 | 1996-08-06 | Regents Of The University Of Minnesota | Method and intermediates for the synthesis of korupensamines |
| JPH08336393A (ja) | 1995-04-13 | 1996-12-24 | Mitsubishi Chem Corp | 光学活性なγ−置換−β−ヒドロキシ酪酸エステルの製造法 |
| US6602677B1 (en) | 1997-09-19 | 2003-08-05 | Promega Corporation | Thermostable luciferases and methods of production |
| WO2003006151A1 (en) | 2001-07-12 | 2003-01-23 | Avecia Limited | Microencapsulated catalyst, methods of preparation and methods of use thereof |
| US7405295B2 (en) | 2003-06-04 | 2008-07-29 | Cgi Pharmaceuticals, Inc. | Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds |
| US7393848B2 (en) | 2003-06-30 | 2008-07-01 | Cgi Pharmaceuticals, Inc. | Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of Bruton's tyrosine kinase by such compounds |
| CA2587192A1 (en) | 2004-11-10 | 2006-05-18 | Cgi Pharmaceuticals, Inc. | Imidazo[1 , 2-a] pyrazin-8-ylamines useful as modulators of kinase activity |
| CA2601628C (en) | 2005-03-10 | 2014-05-13 | Cgi Pharmaceuticals, Inc. | Certain substituted amides, method of making, and method of use thereof |
| HRP20110498T1 (hr) | 2005-10-07 | 2011-08-31 | Exelixis | Azetidini kao inhibitori mek za liječenje proliferativnih bolesti |
| US7838523B2 (en) | 2006-09-11 | 2010-11-23 | Cgi Pharmaceuticals, Inc. | Certain substituted amides, method of making, and method of use thereof |
| AR063706A1 (es) | 2006-09-11 | 2009-02-11 | Cgi Pharmaceuticals Inc | Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden. |
| AR063946A1 (es) | 2006-09-11 | 2009-03-04 | Cgi Pharmaceuticals Inc | Determinadas pirimidinas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden. |
| CL2008002793A1 (es) * | 2007-09-20 | 2009-09-04 | Cgi Pharmaceuticals Inc | Compuestos derivados de amidas sustituidas, inhibidores de la actividad de btk; composicion farmaceutica que los comprende; utiles en el tratamiento del cancer, trastornos oseos, enfermedades autoinmunes, entre otras |
| US8426441B2 (en) | 2007-12-14 | 2013-04-23 | Roche Palo Alto Llc | Inhibitors of bruton's tyrosine kinase |
| US7683064B2 (en) | 2008-02-05 | 2010-03-23 | Roche Palo Alto Llc | Inhibitors of Bruton's tyrosine kinase |
| US8426424B2 (en) | 2008-05-06 | 2013-04-23 | Cgi Pharmaceuticals, Inc. | Certain substituted amides, method of making, and method of use thereof |
| ES2552320T3 (es) | 2008-06-24 | 2015-11-27 | F. Hoffmann-La Roche Ag | Nuevas piridín-2-onas y piridazín-3-onas sustituidas |
| BRPI0913879A2 (pt) * | 2008-07-02 | 2019-09-24 | Hoffmann La Roche | fenilpirazinonas como inibidores de quinase |
| CA2726460C (en) | 2008-07-15 | 2017-02-21 | F. Hoffmann-La Roche Ag | Novel phenyl-imidazopyridines and pyridazines |
| WO2010056875A1 (en) | 2008-11-12 | 2010-05-20 | Cgi Pharmaceuticals, Inc. | Pyridazinones and their use as btk inhibitors |
| US8299077B2 (en) * | 2009-03-02 | 2012-10-30 | Roche Palo Alto Llc | Inhibitors of Bruton's tyrosine kinase |
| PT2473049T (pt) * | 2009-09-04 | 2019-03-04 | Sunesis Pharmaceuticals Inc | Inibidores de tirosina quinase de bruton |
| AR082590A1 (es) | 2010-08-12 | 2012-12-19 | Hoffmann La Roche | Inhibidores de la tirosina-quinasa de bruton |
| BR112013007499A2 (pt) | 2010-09-01 | 2016-07-12 | Genentech Inc | piridazinonas - métodos de criação e usos |
| CN103582637B (zh) | 2011-05-17 | 2015-08-12 | 弗·哈夫曼-拉罗切有限公司 | 酪氨酸激酶抑制剂 |
| CN103748088A (zh) | 2011-08-17 | 2014-04-23 | 弗·哈夫曼-拉罗切有限公司 | 酪氨酸激酶抑制剂 |
| UA111756C2 (uk) * | 2011-11-03 | 2016-06-10 | Ф. Хоффманн-Ля Рош Аг | Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона |
| MX2014005289A (es) * | 2011-11-03 | 2014-05-30 | Hoffmann La Roche | Compuestos de piperazina alquilados. |
-
2012
- 2012-11-02 MX MX2014005289A patent/MX2014005289A/es active IP Right Grant
- 2012-11-02 JP JP2014541115A patent/JP5976828B2/ja not_active Expired - Fee Related
- 2012-11-02 PE PE2014000639A patent/PE20141686A1/es not_active Application Discontinuation
- 2012-11-02 BR BR112014010439A patent/BR112014010439A2/pt not_active Application Discontinuation
- 2012-11-02 WO PCT/US2012/063198 patent/WO2013067277A1/en not_active Ceased
- 2012-11-02 IN IN3265CHN2014 patent/IN2014CN03265A/en unknown
- 2012-11-02 SG SG11201401993RA patent/SG11201401993RA/en unknown
- 2012-11-02 PH PH1/2014/500966A patent/PH12014500966A1/en unknown
- 2012-11-02 US US13/667,114 patent/US8729072B2/en active Active
- 2012-11-02 EA EA201490859A patent/EA027561B1/ru not_active IP Right Cessation
- 2012-11-02 KR KR1020147014782A patent/KR101716011B1/ko not_active Expired - Fee Related
- 2012-11-02 TW TW101140859A patent/TW201326171A/zh unknown
- 2012-11-02 AR ARP120104129A patent/AR088642A1/es unknown
- 2012-11-02 CA CA2853970A patent/CA2853970A1/en not_active Abandoned
- 2012-11-02 CN CN201280065838.8A patent/CN104024255B/zh not_active Expired - Fee Related
- 2012-11-02 AU AU2012332368A patent/AU2012332368A1/en not_active Abandoned
- 2012-11-02 EP EP12783838.1A patent/EP2773639B1/en not_active Not-in-force
-
2014
- 2014-04-07 US US14/246,471 patent/US8946213B2/en active Active
- 2014-04-24 CR CR20140187A patent/CR20140187A/es unknown
- 2014-04-28 IL IL232280A patent/IL232280A0/en unknown
- 2014-04-30 ZA ZA2014/03158A patent/ZA201403158B/en unknown
- 2014-04-30 CO CO14093206A patent/CO6950475A2/es active IP Right Grant
- 2014-05-02 CL CL2014001158A patent/CL2014001158A1/es unknown
- 2014-06-06 MA MA37107A patent/MA35725B1/fr unknown
- 2014-12-11 US US14/566,920 patent/US9115152B2/en active Active
-
2015
- 2015-08-24 JP JP2015165095A patent/JP2016028045A/ja not_active Withdrawn
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010122038A1 (en) | 2009-04-24 | 2010-10-28 | F. Hoffmann-La Roche Ag | Inhibitors of bruton's tyrosine kinase |
| WO2010126960A1 (en) | 2009-04-29 | 2010-11-04 | Locus Pharmaceuticals, Inc. | Pyrrolotriazine compounds |
| WO2011140488A1 (en) | 2010-05-07 | 2011-11-10 | Gilead Connecticut, Inc. | Pyridone and aza-pyridone compounds and methods of use |
| WO2012031004A1 (en) | 2010-09-01 | 2012-03-08 | Gilead Connecticut, Inc. | Pyridinones/pyrazinones, method of making, and method of use thereof |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| KR101716011B1 (ko) | Btk 활성의 억제제인 알킬화된 피페라진 화합물 | |
| KR101696525B1 (ko) | Btk 활성 억제제로서의 8-플루오로프탈라진-1(2h)-온 화합물 | |
| KR101815360B1 (ko) | 헤테로아릴 피리돈 및 아자-피리돈 아마이드 화합물 | |
| KR20140096100A (ko) | 이환 피페라진 화합물 | |
| KR101659193B1 (ko) | Btk 활성의 억제제로서의 헤테로아릴 피리돈 및 아자-피리돈 화합물 | |
| KR101813830B1 (ko) | 친전자성 작용기를 갖는 헤테로아릴 피리돈 및 아자-피리돈 화합물 | |
| KR101864908B1 (ko) | 피리다지논, 그의 제조 방법 및 사용 방법 | |
| JP6507234B2 (ja) | ブルトンチロシンキナーゼ(btk)によって介入される障害の処置における使用のためのピラゾールカルボキサミド化合物 | |
| HUE025173T2 (hu) | Heteroaril-szubsztituált pirrollo[2,3-b]piridinek és pirrolo[2,3-b]pirimidinek mint Janus-kináz inhibitorok | |
| KR20140032383A (ko) | Pi3k p110 델타에 대하여 선택적인 벤즈옥사제핀 화합물 및 이의 사용 방법 | |
| HK1197401B (en) | Alkylated piperazine compounds as inhibitors of btk activity | |
| HK1197401A (en) | Alkylated piperazine compounds as inhibitors of btk activity | |
| HK1201268B (zh) | 二环哌嗪化合物 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A201 | Request for examination | ||
| E13-X000 | Pre-grant limitation requested |
St.27 status event code: A-2-3-E10-E13-lim-X000 |
|
| P11-X000 | Amendment of application requested |
St.27 status event code: A-2-2-P10-P11-nap-X000 |
|
| P13-X000 | Application amended |
St.27 status event code: A-2-2-P10-P13-nap-X000 |
|
| PA0105 | International application |
St.27 status event code: A-0-1-A10-A15-nap-PA0105 |
|
| PA0201 | Request for examination |
St.27 status event code: A-1-2-D10-D11-exm-PA0201 |
|
| PG1501 | Laying open of application |
St.27 status event code: A-1-1-Q10-Q12-nap-PG1501 |
|
| E902 | Notification of reason for refusal | ||
| PE0902 | Notice of grounds for rejection |
St.27 status event code: A-1-2-D10-D21-exm-PE0902 |
|
| T11-X000 | Administrative time limit extension requested |
St.27 status event code: U-3-3-T10-T11-oth-X000 |
|
| T11-X000 | Administrative time limit extension requested |
St.27 status event code: U-3-3-T10-T11-oth-X000 |
|
| E13-X000 | Pre-grant limitation requested |
St.27 status event code: A-2-3-E10-E13-lim-X000 |
|
| P11-X000 | Amendment of application requested |
St.27 status event code: A-2-2-P10-P11-nap-X000 |
|
| P13-X000 | Application amended |
St.27 status event code: A-2-2-P10-P13-nap-X000 |
|
| E902 | Notification of reason for refusal | ||
| PE0902 | Notice of grounds for rejection |
St.27 status event code: A-1-2-D10-D21-exm-PE0902 |
|
| P11-X000 | Amendment of application requested |
St.27 status event code: A-2-2-P10-P11-nap-X000 |
|
| P13-X000 | Application amended |
St.27 status event code: A-2-2-P10-P13-nap-X000 |
|
| E902 | Notification of reason for refusal | ||
| PE0902 | Notice of grounds for rejection |
St.27 status event code: A-1-2-D10-D21-exm-PE0902 |
|
| E13-X000 | Pre-grant limitation requested |
St.27 status event code: A-2-3-E10-E13-lim-X000 |
|
| P11-X000 | Amendment of application requested |
St.27 status event code: A-2-2-P10-P11-nap-X000 |
|
| P13-X000 | Application amended |
St.27 status event code: A-2-2-P10-P13-nap-X000 |
|
| E701 | Decision to grant or registration of patent right | ||
| PE0701 | Decision of registration |
St.27 status event code: A-1-2-D10-D22-exm-PE0701 |
|
| GRNT | Written decision to grant | ||
| PR0701 | Registration of establishment |
St.27 status event code: A-2-4-F10-F11-exm-PR0701 |
|
| PR1002 | Payment of registration fee |
St.27 status event code: A-2-2-U10-U12-oth-PR1002 Fee payment year number: 1 |
|
| PG1601 | Publication of registration |
St.27 status event code: A-4-4-Q10-Q13-nap-PG1601 |
|
| PC1903 | Unpaid annual fee |
St.27 status event code: A-4-4-U10-U13-oth-PC1903 Not in force date: 20200308 Payment event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE |
|
| PC1903 | Unpaid annual fee |
St.27 status event code: N-4-6-H10-H13-oth-PC1903 Ip right cessation event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE Not in force date: 20200308 |
|
| R18-X000 | Changes to party contact information recorded |
St.27 status event code: A-5-5-R10-R18-oth-X000 |