BR112017003800A2 - composto de pirazolotiazol e medicamento - Google Patents
composto de pirazolotiazol e medicamentoInfo
- Publication number
- BR112017003800A2 BR112017003800A2 BR112017003800A BR112017003800A BR112017003800A2 BR 112017003800 A2 BR112017003800 A2 BR 112017003800A2 BR 112017003800 A BR112017003800 A BR 112017003800A BR 112017003800 A BR112017003800 A BR 112017003800A BR 112017003800 A2 BR112017003800 A2 BR 112017003800A2
- Authority
- BR
- Brazil
- Prior art keywords
- effect
- jak1
- present
- compounds
- inhibitory activity
- Prior art date
Links
- 239000003814 drug Substances 0.000 title 1
- -1 pyrazolothiazole compound Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 230000002401 inhibitory effect Effects 0.000 abstract 3
- 101150079478 jak1 gene Proteins 0.000 abstract 3
- VHHWHDFVZGPKRT-UHFFFAOYSA-N 5h-pyrazolo[3,4-d][1,3]thiazole Chemical class N1=NC2=NCSC2=C1 VHHWHDFVZGPKRT-UHFFFAOYSA-N 0.000 abstract 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 abstract 1
- 208000000592 Nasal Polyps Diseases 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 206010047115 Vasculitis Diseases 0.000 abstract 1
- 230000003110 anti-inflammatory effect Effects 0.000 abstract 1
- 230000001028 anti-proliverative effect Effects 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 230000002327 eosinophilic effect Effects 0.000 abstract 1
- 230000001506 immunosuppresive effect Effects 0.000 abstract 1
- 208000030603 inherited susceptibility to asthma Diseases 0.000 abstract 1
- 208000016366 nasal cavity polyp Diseases 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000009890 sinusitis Diseases 0.000 abstract 1
Classifications
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
- A61K31/095—Sulfur, selenium, or tellurium compounds, e.g. thiols
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
-
- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/25—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids with polyoxyalkylated alcohols, e.g. esters of polyethylene glycol
-
- 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
- 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
-
- 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
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (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)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Transplantation (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
a invenção refere-se a um composto tendo um excepcional efeito inibidor de jak1. exemplos da presente invenção incluem os compostos de pirazolotiazol representado por fórmula geral [i], e sais farmaceuticamente aceitáveis do mesmo. os compostos da presente invenção têm atividade inibidora de jak1. dada esta atividade inibido-ra de jak1, os compostos da presente invenção da mesma forma têm efeito imunossupressor (contra, por exemplo, artrite reumatoide, doen-ça intestinal inflamatória, psoríase e vasculite), um efeito anti-inflamatório (contra, por exemplo, asma brônquica, doença pulmonar obstrutiva crônica, sinusite eosinofílica, pólipo nasal) um efeito antipro-liferativo, e similares.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2014177969 | 2014-09-02 | ||
JP2014-177969 | 2014-09-02 | ||
PCT/JP2015/074935 WO2016035814A1 (ja) | 2014-09-02 | 2015-09-02 | ピラゾロチアゾール化合物および医薬 |
Publications (2)
Publication Number | Publication Date |
---|---|
BR112017003800A2 true BR112017003800A2 (pt) | 2017-11-28 |
BR112017003800B1 BR112017003800B1 (pt) | 2022-09-13 |
Family
ID=55439874
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112017003800-5A BR112017003800B1 (pt) | 2014-09-02 | 2015-09-02 | Composto de pirazolotiazol e composição farmacêutica com efeito inibidor de jak1 |
Country Status (33)
Country | Link |
---|---|
US (2) | US9937176B2 (pt) |
EP (1) | EP3190116B1 (pt) |
JP (1) | JP6558372B2 (pt) |
KR (1) | KR102294330B1 (pt) |
CN (1) | CN107108653B (pt) |
AU (1) | AU2015312886B2 (pt) |
BR (1) | BR112017003800B1 (pt) |
CA (1) | CA2959721C (pt) |
CL (1) | CL2017000478A1 (pt) |
CO (1) | CO2017002982A2 (pt) |
CY (1) | CY1123320T1 (pt) |
DK (1) | DK3190116T3 (pt) |
ES (1) | ES2827243T3 (pt) |
HR (1) | HRP20201382T1 (pt) |
HU (1) | HUE050565T2 (pt) |
IL (1) | IL250729B (pt) |
LT (1) | LT3190116T (pt) |
MA (1) | MA40605B1 (pt) |
MX (1) | MX2017002488A (pt) |
MY (1) | MY181814A (pt) |
NZ (1) | NZ729494A (pt) |
PE (1) | PE20170668A1 (pt) |
PH (1) | PH12017500383B1 (pt) |
PL (1) | PL3190116T3 (pt) |
PT (1) | PT3190116T (pt) |
RS (1) | RS60798B1 (pt) |
RU (1) | RU2688660C2 (pt) |
SG (2) | SG10201901676UA (pt) |
SI (1) | SI3190116T1 (pt) |
TW (1) | TWI679205B (pt) |
UA (1) | UA121869C2 (pt) |
WO (1) | WO2016035814A1 (pt) |
ZA (1) | ZA201701492B (pt) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TWI679205B (zh) * | 2014-09-02 | 2019-12-11 | 日商日本新藥股份有限公司 | 吡唑并噻唑化合物及醫藥 |
TWI712604B (zh) * | 2016-03-01 | 2020-12-11 | 日商日本新藥股份有限公司 | 具jak抑制作用之化合物之結晶 |
CN110709346B (zh) | 2017-06-09 | 2020-12-22 | 三菱电机株式会社 | 乘客输送机 |
JP2023508952A (ja) * | 2019-12-23 | 2023-03-06 | エスアールアイ インターナショナル | リポキシゲナーゼ阻害剤 |
Family Cites Families (27)
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DE3600390A1 (de) | 1986-01-09 | 1987-07-16 | Hoechst Ag | Diarylalkyl-substituierte alkylamine, verfahren zu ihrer herstellung, ihre verwendung sowie sie enthaltende arzneimittel |
PH25866A (en) * | 1986-03-20 | 1991-12-02 | Takeda Chemical Industries Ltd | Sulfonylurea compounds and their herbicides |
US5082847A (en) | 1990-07-18 | 1992-01-21 | Syntex (U.S.A.) Inc. | Carbostyril compounds connected via an oxyalkyl group with a piperidine ring and having pharmaceutical utility |
GB0216383D0 (en) | 2002-07-13 | 2002-08-21 | Astrazeneca Ab | Compounds |
CN100465173C (zh) | 2004-01-12 | 2009-03-04 | 西托匹亚研究有限公司 | 选择性激酶抑制剂 |
MXPA06012510A (es) | 2004-04-28 | 2006-12-15 | Pfizer | Derivados de 3-heterociclil-4-fenil-triazol como inhibidores del receptor de vasopresina via. |
SG151327A1 (en) * | 2005-09-30 | 2009-04-30 | Vertex Pharmaceuticals Incopor | Deazapurines useful as inhibitors of janus kinases |
US7528143B2 (en) * | 2005-11-01 | 2009-05-05 | Targegen, Inc. | Bi-aryl meta-pyrimidine inhibitors of kinases |
RU2453548C2 (ru) | 2006-01-17 | 2012-06-20 | Вертекс Фармасьютикалз Инкорпорейтед | Азаиндолы, полезные в качестве ингибиторов янус-киназ |
JP5275371B2 (ja) | 2008-03-11 | 2013-08-28 | インサイト・コーポレイション | Jak阻害剤としてのアゼチジン誘導体およびシクロブタン誘導体 |
CA2721670C (en) * | 2008-04-15 | 2013-09-10 | Eisai R&D Management Co., Ltd. | 3-phenylpyrazolo[5,1-b]thiazole compound |
JO3041B1 (ar) | 2008-07-25 | 2016-09-05 | Galapagos Nv | مركبات جديدة مفيدة لمعالجة الأمراض التنكسية والالتهابية |
JP5490137B2 (ja) * | 2008-12-19 | 2014-05-14 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | プロテインキナーゼ阻害薬としての二環式ピラゾール |
TWI462920B (zh) | 2009-06-26 | 2014-12-01 | 葛萊伯格有限公司 | 用於治療退化性及發炎疾病之新穎化合物 |
ES2461967T3 (es) | 2009-12-18 | 2014-05-21 | Pfizer Inc. | Compuestos de pirrolo[2,3-d]pirimidina |
TW201124078A (en) | 2009-12-22 | 2011-07-16 | Du Pont | Fungicidal 2-(bicyclic aryloxy) carboxamides |
EP2338888A1 (en) | 2009-12-24 | 2011-06-29 | Almirall, S.A. | Imidazopyridine derivatives as JAK inhibitors |
JP2011136925A (ja) | 2009-12-28 | 2011-07-14 | Dainippon Sumitomo Pharma Co Ltd | 含窒素二環性化合物 |
TW201129565A (en) | 2010-01-12 | 2011-09-01 | Hoffmann La Roche | Tricyclic heterocyclic compounds, compositions and methods of use thereof |
UY33213A (es) | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
CA2801032A1 (en) | 2010-07-12 | 2012-01-19 | Pfizer Limited | N-sulfonylbenzamide derivatives useful as voltage gated sodium channel inhibitors |
WO2012022045A1 (en) | 2010-08-20 | 2012-02-23 | Hutchison Medipharma Limited | Pyrrolopyrimidine compounds and uses thereof |
CA2812088A1 (en) | 2010-09-14 | 2012-03-22 | Exelixis, Inc. | Phtalazine derivatives as jak1 inhibitors |
WO2012054364A2 (en) | 2010-10-22 | 2012-04-26 | Merck Sharp & Dohme Corp. | Bicyclic diamines as janus kinase inhibitors |
WO2012085176A1 (en) | 2010-12-23 | 2012-06-28 | F. Hoffmann-La Roche Ag | Tricyclic pyrazinone compounds, compositions and methods of use thereof as janus kinase inhibitors |
WO2013025628A1 (en) * | 2011-08-15 | 2013-02-21 | Ligand Pharmaceuticals Incorporated | Janus kinase inhibitor compounds and methods |
TWI679205B (zh) * | 2014-09-02 | 2019-12-11 | 日商日本新藥股份有限公司 | 吡唑并噻唑化合物及醫藥 |
-
2015
- 2015-09-01 TW TW104128865A patent/TWI679205B/zh active
- 2015-09-02 HU HUE15838466A patent/HUE050565T2/hu unknown
- 2015-09-02 BR BR112017003800-5A patent/BR112017003800B1/pt active IP Right Grant
- 2015-09-02 LT LTEP15838466.9T patent/LT3190116T/lt unknown
- 2015-09-02 RU RU2017110535A patent/RU2688660C2/ru active
- 2015-09-02 UA UAA201702990A patent/UA121869C2/uk unknown
- 2015-09-02 MX MX2017002488A patent/MX2017002488A/es unknown
- 2015-09-02 SI SI201531340T patent/SI3190116T1/sl unknown
- 2015-09-02 PL PL15838466T patent/PL3190116T3/pl unknown
- 2015-09-02 PE PE2017000370A patent/PE20170668A1/es unknown
- 2015-09-02 CN CN201580058944.7A patent/CN107108653B/zh active Active
- 2015-09-02 KR KR1020177008967A patent/KR102294330B1/ko active IP Right Grant
- 2015-09-02 DK DK15838466.9T patent/DK3190116T3/da active
- 2015-09-02 MY MYPI2017700677A patent/MY181814A/en unknown
- 2015-09-02 NZ NZ729494A patent/NZ729494A/en unknown
- 2015-09-02 JP JP2016546669A patent/JP6558372B2/ja active Active
- 2015-09-02 ES ES15838466T patent/ES2827243T3/es active Active
- 2015-09-02 RS RS20201081A patent/RS60798B1/sr unknown
- 2015-09-02 PT PT158384669T patent/PT3190116T/pt unknown
- 2015-09-02 SG SG10201901676UA patent/SG10201901676UA/en unknown
- 2015-09-02 AU AU2015312886A patent/AU2015312886B2/en active Active
- 2015-09-02 EP EP15838466.9A patent/EP3190116B1/en active Active
- 2015-09-02 MA MA40605A patent/MA40605B1/fr unknown
- 2015-09-02 US US15/505,767 patent/US9937176B2/en active Active
- 2015-09-02 CA CA2959721A patent/CA2959721C/en active Active
- 2015-09-02 SG SG11201701447UA patent/SG11201701447UA/en unknown
- 2015-09-02 WO PCT/JP2015/074935 patent/WO2016035814A1/ja active Application Filing
-
2017
- 2017-02-23 IL IL250729A patent/IL250729B/en active IP Right Grant
- 2017-02-28 ZA ZA2017/01492A patent/ZA201701492B/en unknown
- 2017-02-28 CL CL2017000478A patent/CL2017000478A1/es unknown
- 2017-03-01 PH PH12017500383A patent/PH12017500383B1/en unknown
- 2017-03-27 CO CONC2017/0002982A patent/CO2017002982A2/es unknown
- 2017-12-04 US US15/830,181 patent/US9999622B2/en active Active
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2020
- 2020-08-31 HR HRP20201382TT patent/HRP20201382T1/hr unknown
- 2020-09-04 CY CY20201100832T patent/CY1123320T1/el unknown
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