BR112016016732A8 - derivados de benzimidazol, seus usos, e composições farmacêuticas para tratamento de distúrbios inflamatórios - Google Patents
derivados de benzimidazol, seus usos, e composições farmacêuticas para tratamento de distúrbios inflamatórios Download PDFInfo
- Publication number
- BR112016016732A8 BR112016016732A8 BR112016016732A BR112016016732A BR112016016732A8 BR 112016016732 A8 BR112016016732 A8 BR 112016016732A8 BR 112016016732 A BR112016016732 A BR 112016016732A BR 112016016732 A BR112016016732 A BR 112016016732A BR 112016016732 A8 BR112016016732 A8 BR 112016016732A8
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- BR
- Brazil
- Prior art keywords
- diseases
- treatment
- pharmaceutical compositions
- inflammatory disorders
- benzimidazole derivatives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D235/08—Radicals containing only hydrogen and carbon atoms
-
- 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
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
- A61K31/535—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
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- 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
- 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
- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
-
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Abstract
a presente invenção refere-se a compostos de acordo com a fórmula (i), em que cy, r1, l1, r3, r4, r5, la, e ra são como definidos neste documento. divulgam-se novos benzimidazóis de acordo com a fórmula (i), capazes de inibir a jak, estes compostos podem ser preparados como uma composição farmacêutica, e podem ser usados para a prevenção e o tratamento de uma variedade de condições em mamíferos, incluindo os seres humanos, incluindo, a título de exemplo não limitativo, as doenças alérgicas, as doenças inflamatórias, as doenças autoimunes, as doenças proliferativas, a rejeição ao transplante, as doenças envolvendo a deficiência da renovação da cartilagem, as malformações congênitas da cartilagem, e/ou as doenças associadas com a hipersecreção de il6 ou a hipersecreção de interferons.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB1401086.2 | 2014-01-23 | ||
GBGB1401086.2A GB201401086D0 (en) | 2014-01-23 | 2014-01-23 | Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders |
PCT/EP2015/050850 WO2015110378A1 (en) | 2014-01-23 | 2015-01-19 | Benzimidazole derivatives and pharmaceutical compositions thereof for the treatment of inflammatory disorders |
Publications (2)
Publication Number | Publication Date |
---|---|
BR112016016732A8 true BR112016016732A8 (pt) | 2020-06-16 |
BR112016016732B1 BR112016016732B1 (pt) | 2023-04-18 |
Family
ID=50287405
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112016016732-5A BR112016016732B1 (pt) | 2014-01-23 | 2015-01-19 | Derivados de benzimidazol, seus usos, e composições farmacêuticas para tratamento de distúrbios inflamatórios |
Country Status (27)
Country | Link |
---|---|
US (3) | US9440929B2 (pt) |
EP (2) | EP3097083B1 (pt) |
JP (1) | JP6472454B2 (pt) |
CN (1) | CN106132934B (pt) |
AR (1) | AR099160A1 (pt) |
AU (1) | AU2015208269B2 (pt) |
BR (1) | BR112016016732B1 (pt) |
CA (1) | CA2941474A1 (pt) |
CY (1) | CY1120679T1 (pt) |
DK (1) | DK3097083T3 (pt) |
EA (1) | EA029827B1 (pt) |
ES (1) | ES2693019T3 (pt) |
GB (1) | GB201401086D0 (pt) |
HR (1) | HRP20181332T1 (pt) |
HU (1) | HUE039450T2 (pt) |
IL (1) | IL246823B (pt) |
LT (1) | LT3097083T (pt) |
MX (1) | MX370546B (pt) |
MY (1) | MY180363A (pt) |
NZ (1) | NZ723313A (pt) |
PH (1) | PH12016501677B1 (pt) |
PL (1) | PL3097083T3 (pt) |
PT (1) | PT3097083T (pt) |
SG (1) | SG11201606971XA (pt) |
SI (1) | SI3097083T1 (pt) |
TW (1) | TWI689496B (pt) |
WO (1) | WO2015110378A1 (pt) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AR105400A1 (es) * | 2015-08-04 | 2017-09-27 | Lilly Co Eli | Inhibidores de jak1 |
BR112018075086B1 (pt) * | 2016-07-14 | 2024-02-27 | Eli Lilly And Company | Derivados de pirazolilaminobenzimidazol, seu uso, e composição farmacêutica |
GB201717260D0 (en) | 2017-10-20 | 2017-12-06 | Galapagos Nv | Novel compounds and pharma ceutical compositions thereof for the treatment of inflammatory disorders |
CN108355618B (zh) * | 2018-02-27 | 2020-09-08 | 江南大学 | 牛来源透明质酸酶亲和介质及其吸附方法 |
CN108776121B (zh) * | 2018-04-08 | 2021-07-30 | 广州卡马生物科技有限公司 | 一种基于荧光猝灭原理对药材中抗氧剂的高通量筛选方法 |
CN115215838A (zh) * | 2018-09-18 | 2022-10-21 | 拓臻股份有限公司 | 用于治疗特定白血病的化合物 |
WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
GB201904373D0 (en) * | 2019-03-29 | 2019-05-15 | Galapagos Nv | Novel compounds and pharamaceutical compositions thereof for the treatment of inflammatory disorders |
CN114671858B (zh) * | 2022-03-07 | 2023-08-08 | 华中师范大学 | 一种苯并咪唑系化合物及其制备方法与应用 |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2386856B1 (en) | 2004-06-21 | 2013-07-24 | Galapagos N.V. | Methods and means for treatment of osteoarthritis |
EP2226315A4 (en) * | 2007-12-28 | 2012-01-25 | Carna Biosciences Inc | 2-AMINOQUINAZOLINE DERIVATIVE |
EP2271631B1 (en) * | 2008-04-22 | 2018-07-04 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
WO2012044090A2 (ko) | 2010-09-29 | 2012-04-05 | 크리스탈지노믹스(주) | 단백질 키나제 억제 활성을 갖는 신규한 아미노퀴나졸린 화합물 |
UY34616A (es) * | 2012-02-10 | 2013-09-30 | Galapagos Nv | Nuevo compuesto útil para el tratamiento de enfermedades degenerativas e inflamatorias. |
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2014
- 2014-01-23 GB GBGB1401086.2A patent/GB201401086D0/en not_active Ceased
-
2015
- 2015-01-19 AU AU2015208269A patent/AU2015208269B2/en active Active
- 2015-01-19 CN CN201580015662.9A patent/CN106132934B/zh active Active
- 2015-01-19 MX MX2016009442A patent/MX370546B/es active IP Right Grant
- 2015-01-19 JP JP2016548110A patent/JP6472454B2/ja active Active
- 2015-01-19 MY MYPI2016702630A patent/MY180363A/en unknown
- 2015-01-19 ES ES15701945.6T patent/ES2693019T3/es active Active
- 2015-01-19 HU HUE15701945A patent/HUE039450T2/hu unknown
- 2015-01-19 SG SG11201606971XA patent/SG11201606971XA/en unknown
- 2015-01-19 DK DK15701945.6T patent/DK3097083T3/en active
- 2015-01-19 BR BR112016016732-5A patent/BR112016016732B1/pt active IP Right Grant
- 2015-01-19 EP EP15701945.6A patent/EP3097083B1/en active Active
- 2015-01-19 US US14/599,644 patent/US9440929B2/en active Active
- 2015-01-19 EP EP18177201.3A patent/EP3395802A1/en not_active Withdrawn
- 2015-01-19 EA EA201691468A patent/EA029827B1/ru not_active IP Right Cessation
- 2015-01-19 SI SI201530383T patent/SI3097083T1/sl unknown
- 2015-01-19 PT PT15701945T patent/PT3097083T/pt unknown
- 2015-01-19 WO PCT/EP2015/050850 patent/WO2015110378A1/en active Application Filing
- 2015-01-19 NZ NZ72331315A patent/NZ723313A/en unknown
- 2015-01-19 CA CA2941474A patent/CA2941474A1/en not_active Abandoned
- 2015-01-19 LT LTEP15701945.6T patent/LT3097083T/lt unknown
- 2015-01-19 PL PL15701945T patent/PL3097083T3/pl unknown
- 2015-01-22 AR ARP150100176A patent/AR099160A1/es unknown
- 2015-01-22 TW TW104102159A patent/TWI689496B/zh active
-
2016
- 2016-07-18 IL IL246823A patent/IL246823B/en active IP Right Grant
- 2016-08-23 PH PH12016501677A patent/PH12016501677B1/en unknown
- 2016-09-12 US US15/262,097 patent/US10179771B2/en active Active
-
2018
- 2018-08-22 HR HRP20181332TT patent/HRP20181332T1/hr unknown
- 2018-08-23 US US16/110,353 patent/US20190152922A1/en not_active Abandoned
- 2018-09-11 CY CY181100950T patent/CY1120679T1/el unknown
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B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] | ||
B06U | Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette] | ||
B06A | Patent application procedure suspended [chapter 6.1 patent gazette] | ||
B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
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