WO2016198698A3 - P38 inhibitors for the treatment and prophylaxis of liver cancer - Google Patents
P38 inhibitors for the treatment and prophylaxis of liver cancer Download PDFInfo
- Publication number
- WO2016198698A3 WO2016198698A3 PCT/EP2016/063532 EP2016063532W WO2016198698A3 WO 2016198698 A3 WO2016198698 A3 WO 2016198698A3 EP 2016063532 W EP2016063532 W EP 2016063532W WO 2016198698 A3 WO2016198698 A3 WO 2016198698A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- liver cancer
- treatment
- prophylaxis
- inhibitors
- present
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
- A61K31/175—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine having the group, >N—C(O)—N=N— or, e.g. carbonohydrazides, carbazones, semicarbazides, semicarbazones; Thioanalogues thereof
-
- 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
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
-
- 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
-
- 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
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7088—Compounds having three or more nucleosides or nucleotides
- A61K31/713—Double-stranded nucleic acids or oligonucleotides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/10—Peptides having 12 to 20 amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/43—Enzymes; Proenzymes; Derivatives thereof
- A61K38/45—Transferases (2)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/36—Radicals substituted by singly-bound nitrogen atoms
- C07D213/40—Acylated substituent nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/20—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Y—ENZYMES
- C12Y207/00—Transferases transferring phosphorus-containing groups (2.7)
- C12Y207/11—Protein-serine/threonine kinases (2.7.11)
- C12Y207/11024—Mitogen-activated protein kinase (2.7.11.24), i.e. MAPK or MAPK2 or c-Jun N-terminal kinase
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP15382308 | 2015-06-12 | ||
EP15382308.3 | 2015-06-12 |
Publications (3)
Publication Number | Publication Date |
---|---|
WO2016198698A2 WO2016198698A2 (en) | 2016-12-15 |
WO2016198698A8 WO2016198698A8 (en) | 2017-02-16 |
WO2016198698A3 true WO2016198698A3 (en) | 2017-03-16 |
Family
ID=53476803
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/EP2016/063532 WO2016198698A2 (en) | 2015-06-12 | 2016-06-13 | P38 inhibitors for the treatment and prophylaxis of liver cancer |
Country Status (1)
Country | Link |
---|---|
WO (1) | WO2016198698A2 (en) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2018132372A1 (en) * | 2017-01-10 | 2018-07-19 | Sanford Burnham Prebys Medical Discovery Institute | Small molecule activators of nicotinamide phosphoribosyltransferase (nampt) and uses thereof |
WO2018183559A1 (en) * | 2017-03-28 | 2018-10-04 | The General Hospital Corporation | Combination therapy against chemoresistance in leukemia |
AU2018346709A1 (en) | 2017-10-05 | 2020-04-16 | Fulcrum Therapeutics, Inc. | Use of p38 inhibitors to reduce expression of DUX4 |
US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
CN112654608B (en) | 2018-07-05 | 2024-05-07 | 桑福德伯纳姆普利斯医学发现研究所 | Fused ring compound having urea structure |
IT202200000314A1 (en) * | 2022-01-11 | 2023-07-11 | Universita’ Degli Studi Di Parma | COMPOUND AND COMPOSITION FOR THE METABOLIC AND FUNCTIONAL RESTORATION OF NK LYMPHOCYTES IN HEPATOCARCINOMA AND RELATED METHOD |
Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2005040758A2 (en) * | 2003-10-24 | 2005-05-06 | Intermune, Inc. | Use of pirfenidone in therapeutic regimens |
WO2005063715A1 (en) * | 2003-12-18 | 2005-07-14 | Boehringer Ingelheim Pharmaceuticals, Inc. | Polymorph of birb 796, a p38map kinase inhibitor |
CN101652138B (en) * | 2007-09-19 | 2011-07-06 | 中南大学 | New medicine use of 1-substituted aryl -2(1H)-pyridone |
EP2653555A1 (en) * | 2012-04-19 | 2013-10-23 | Fundacion Centro Nacional De Investigaciones Cardiovasculares Carlos III (CINC) | P38 MAPK gamma and delta for use as biomarkers of NAFLD |
CN103550242A (en) * | 2013-11-22 | 2014-02-05 | 四川国康药业有限公司 | Pharmaceutical composition for treating hepatic fibrosis and preparation method thereof |
EP2727596A1 (en) * | 2012-10-30 | 2014-05-07 | Fundación Centro Nacional de Investigaciones Cardiovasculares Carlos III (CNIC) | eEF2/eEF2K as therapeutic target for treating TNF-alpha-related diseases |
-
2016
- 2016-06-13 WO PCT/EP2016/063532 patent/WO2016198698A2/en active Application Filing
Patent Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2005040758A2 (en) * | 2003-10-24 | 2005-05-06 | Intermune, Inc. | Use of pirfenidone in therapeutic regimens |
WO2005063715A1 (en) * | 2003-12-18 | 2005-07-14 | Boehringer Ingelheim Pharmaceuticals, Inc. | Polymorph of birb 796, a p38map kinase inhibitor |
CN101652138B (en) * | 2007-09-19 | 2011-07-06 | 中南大学 | New medicine use of 1-substituted aryl -2(1H)-pyridone |
EP2653555A1 (en) * | 2012-04-19 | 2013-10-23 | Fundacion Centro Nacional De Investigaciones Cardiovasculares Carlos III (CINC) | P38 MAPK gamma and delta for use as biomarkers of NAFLD |
EP2727596A1 (en) * | 2012-10-30 | 2014-05-07 | Fundación Centro Nacional de Investigaciones Cardiovasculares Carlos III (CNIC) | eEF2/eEF2K as therapeutic target for treating TNF-alpha-related diseases |
CN103550242A (en) * | 2013-11-22 | 2014-02-05 | 四川国康药业有限公司 | Pharmaceutical composition for treating hepatic fibrosis and preparation method thereof |
Non-Patent Citations (6)
Title |
---|
A. BUDHU ET AL: "The role of cytokines in hepatocellular carcinoma", JOURNAL OF LEUKOCYTE BIOLOGY, vol. 80, no. 6, 18 August 2006 (2006-08-18), US, pages 1197 - 1213, XP055227184, ISSN: 0741-5400, DOI: 10.1189/jlb.0506297 * |
ANONYMOUS: "Useful new molecules for the treatment of liver cancer.", 21 October 2015 (2015-10-21), XP055303285, Retrieved from the Internet <URL:https://www.cnic.es/sites/default/files/ot44.en.pdf> [retrieved on 20160916] * |
MARCIA GOETTERT ET AL: "Development of a p38 mitogen activated protein kinase ELISA assay for the quantitative determination of inhibitor activity", JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, NEW YORK, NY, US, vol. 66, 6 March 2012 (2012-03-06), pages 349 - 351, XP028490226, ISSN: 0731-7085, [retrieved on 20120315], DOI: 10.1016/J.JPBA.2012.03.008 * |
TATIANA EFIMOVA: "p38[delta] mitogen-activated protein kinase regulates skin homeostasis and tumorigenesis", CELL CYCLE, vol. 9, no. 3, 1 February 2010 (2010-02-01), pages 498 - 505, XP055227163, ISSN: 1538-4101, DOI: 10.4161/cc.9.3.10541 * |
Y.-S. KEUM: "Mechanism of Action of Sulforaphane: Inhibition of p38 Mitogen-Activated Protein Kinase Isoforms Contributing to the Induction of Antioxidant Response Element-Mediated Heme Oxygenase-1 in Human Hepatoma HepG2 Cells", CANCER RESEARCH, vol. 66, no. 17, 1 September 2006 (2006-09-01), US, pages 8804 - 8813, XP055227130, ISSN: 0008-5472, DOI: 10.1158/0008-5472.CAN-05-3513 * |
YVONNE KUMA ET AL: "BIRB796 Inhibits All p38 MAPK Isoforms in Vitro and in Vivo", JOURNAL OF BIOLOGICAL CHEMISTRY, AMERICAN SOCIETY FOR BIOCHEMISTRY AND MOLECULAR BIOLOGY, US, vol. 280, no. 20, 20 May 2005 (2005-05-20), pages 19472 - 19479, XP007913553, ISSN: 0021-9258, [retrieved on 20050508], DOI: 10.1074/JBC.M414221200 * |
Also Published As
Publication number | Publication date |
---|---|
WO2016198698A8 (en) | 2017-02-16 |
WO2016198698A2 (en) | 2016-12-15 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
PH12020550622A1 (en) | Kras g12c inhibitors | |
MX2018013983A (en) | Kras g12c inhibitors. | |
PH12018500899A1 (en) | Compositions and methods for inhibiting arginase activity | |
PH12018500792A1 (en) | Benzolactam compounds as protein kinase inhibitors | |
PH12018501151A1 (en) | Tank-binding kinase inhibitor compounds | |
NZ729005A (en) | Aminopyrimidinyl compounds as jak inhibitors | |
MX2018008052A (en) | Lsd1 inhibitors. | |
PH12016501578A1 (en) | Pharmaceutical compounds | |
WO2016198698A3 (en) | P38 inhibitors for the treatment and prophylaxis of liver cancer | |
IL268625A (en) | Amino pyrimidine compounds useful as ssao inhibitors | |
MX2019007243A (en) | Ectonucleotidase inhibitors and methods of use thereof. | |
MX2016015565A (en) | Certain protein kinase inhibitors. | |
WO2015120062A3 (en) | Therapeutic compounds and compositions | |
PH12017500881A1 (en) | Aurora a kinase inhibitor | |
EP3103802A4 (en) | Novel pyrrolopyrimidine compound or salt thereof, pharmaceutical composition containing same, especially agent for prevention and/or treatment of tumors etc based on nae inhibitory effect | |
EP3273983A4 (en) | Novel cytotoxic agents that preferentially target leukemia inhibitory factor (lif) for the treatment of malignancies and as new contraceptive agents | |
TN2018000057A1 (en) | Compounds useful for inhibiting ror-gamma-t. | |
PH12016501838A1 (en) | Compounds and their methods of use | |
GB2579480B (en) | Composition for preventing or treating cancer containing Triazolopyridine-based derivative as active ingredient | |
MX2019005294A (en) | Inhibitors of mtor-deptor interactions and methods of use thereof. | |
EP3360581A4 (en) | Pharmaceutical composition for preventing or treating cancer comprising inhibitor of plrg1 (pleiotropic regulator 1) as active ingredient | |
GB202001368D0 (en) | Pharmaceutical composition for preventing or treating cancer containign recepto tyrosine kinase inhibitor as active ingredient |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
121 | Ep: the epo has been informed by wipo that ep was designated in this application |
Ref document number: 16730791 Country of ref document: EP Kind code of ref document: A2 |
|
WPC | Withdrawal of priority claims after completion of the technical preparations for international publication |
Ref document number: 15382308.3 Country of ref document: EP Date of ref document: 20171102 Free format text: WITHDRAWN AFTER TECHNICAL PREPARATION FINISHED |
|
NENP | Non-entry into the national phase |
Ref country code: DE |
|
122 | Ep: pct application non-entry in european phase |
Ref document number: 16730791 Country of ref document: EP Kind code of ref document: A2 |