CA2798698A1 - Methods and compositions for inhibition of the transitional endoplasmic reticulum atpase - Google Patents
Methods and compositions for inhibition of the transitional endoplasmic reticulum atpase Download PDFInfo
- Publication number
- CA2798698A1 CA2798698A1 CA2798698A CA2798698A CA2798698A1 CA 2798698 A1 CA2798698 A1 CA 2798698A1 CA 2798698 A CA2798698 A CA 2798698A CA 2798698 A CA2798698 A CA 2798698A CA 2798698 A1 CA2798698 A1 CA 2798698A1
- Authority
- CA
- Canada
- Prior art keywords
- formula
- compound
- groups listed
- methyl
- hydrogen
- 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.)
- Abandoned
Links
- 239000000203 mixture Substances 0.000 title claims abstract 16
- 238000000034 method Methods 0.000 title claims abstract 7
- 101710132062 Transitional endoplasmic reticulum ATPase Proteins 0.000 title claims 12
- 102100026145 Transitional endoplasmic reticulum ATPase Human genes 0.000 title 1
- 230000005764 inhibitory process Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 29
- 230000015556 catabolic process Effects 0.000 claims abstract 9
- 238000006731 degradation reaction Methods 0.000 claims abstract 9
- 230000001419 dependent effect Effects 0.000 claims abstract 9
- 108010045304 p97 ATPase Proteins 0.000 claims abstract 9
- 239000000758 substrate Substances 0.000 claims abstract 9
- 239000003112 inhibitor Substances 0.000 claims abstract 3
- 230000002401 inhibitory effect Effects 0.000 claims abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 24
- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 239000001257 hydrogen Substances 0.000 claims 20
- 229910052801 chlorine Inorganic materials 0.000 claims 18
- 239000000460 chlorine Substances 0.000 claims 18
- 150000002431 hydrogen Chemical group 0.000 claims 18
- 229910052794 bromium Inorganic materials 0.000 claims 16
- 229910052731 fluorine Inorganic materials 0.000 claims 16
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 16
- 125000000217 alkyl group Chemical group 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 12
- 102100037364 Craniofacial development protein 1 Human genes 0.000 claims 11
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 10
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 10
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 10
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical group BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 10
- 230000000694 effects Effects 0.000 claims 10
- 239000011737 fluorine Chemical group 0.000 claims 10
- 229910052760 oxygen Inorganic materials 0.000 claims 10
- -1 analog Chemical class 0.000 claims 6
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 6
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 6
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 4
- 230000007423 decrease Effects 0.000 claims 4
- 230000003247 decreasing effect Effects 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 210000005260 human cell Anatomy 0.000 claims 4
- 239000001301 oxygen Substances 0.000 claims 4
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 2
- 125000004103 aminoalkyl group Chemical group 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 239000000243 solution Substances 0.000 claims 2
- 239000012085 test solution Substances 0.000 claims 2
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
- C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
- C12Q1/42—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving phosphatase
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
- C12Q1/48—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
- C12Q1/485—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2500/00—Screening for compounds of potential therapeutic value
- G01N2500/02—Screening involving studying the effect of compounds C on the interaction between interacting molecules A and B (e.g. A = enzyme and B = substrate for A, or A = receptor and B = ligand for the receptor)
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Zoology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Wood Science & Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- General Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Immunology (AREA)
- Microbiology (AREA)
- Molecular Biology (AREA)
- Analytical Chemistry (AREA)
- Physics & Mathematics (AREA)
- Biophysics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33266710P | 2010-05-07 | 2010-05-07 | |
| US61/332,667 | 2010-05-07 | ||
| PCT/US2011/035654 WO2011140527A2 (en) | 2010-05-07 | 2011-05-06 | Methods and compositions for inhibition of the transitional endoplasmic reticulum atpase |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2798698A1 true CA2798698A1 (en) | 2011-11-10 |
Family
ID=44904519
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2798698A Abandoned CA2798698A1 (en) | 2010-05-07 | 2011-05-06 | Methods and compositions for inhibition of the transitional endoplasmic reticulum atpase |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US8865708B2 (https=) |
| EP (1) | EP2566480A4 (https=) |
| JP (1) | JP2013530942A (https=) |
| KR (1) | KR20130128308A (https=) |
| CN (1) | CN103068393A (https=) |
| AU (1) | AU2011249859B2 (https=) |
| CA (1) | CA2798698A1 (https=) |
| WO (1) | WO2011140527A2 (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8865708B2 (en) | 2010-05-07 | 2014-10-21 | California Institute Of Technology | Methods and compositions for inhibition of the transitional endoplasmic reticulum ATPase |
| US8906918B1 (en) * | 2012-03-23 | 2014-12-09 | University Of South Florida (A Florida Non-Profit Corporation) | Compositions, methods of use, and methods of treatment |
| US9062026B2 (en) | 2012-07-20 | 2015-06-23 | Cleave Biosciences, Inc. | Fused pyrimidines and substituted quinazolines as inhibitors of p97 |
| CA2896731A1 (en) | 2012-12-28 | 2014-07-03 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof |
| US10479777B2 (en) | 2013-07-16 | 2019-11-19 | Basf Se | Herbicidal azines |
| DE102013110714A1 (de) * | 2013-09-27 | 2015-04-02 | Eberhard Karls Universität Tübingen Medizinische Fakultät | Prophylaxe und Behandlung einer nicht auf einer Proteinfaltungsstörung beruhenden neurodegenerativen Erkrankung |
| CN105828823B (zh) * | 2013-10-18 | 2019-06-14 | 美国印第安纳大学研究和技术公司 | 乙型肝炎病毒组装效应物 |
| TW201605832A (zh) | 2013-12-10 | 2016-02-16 | 克立弗生物科學公司 | 作為ｐ９７錯合物之抑制劑之單環嘧啶／吡啶化合物 |
| AU2015206292B2 (en) | 2014-01-20 | 2018-02-15 | Cleave Biosciences, Inc. | Fused pyrimidines as inhibitors of p97 complex |
| CN106458937A (zh) | 2014-04-11 | 2017-02-22 | 巴斯夫欧洲公司 | 作为除草剂的二氨基三嗪衍生物 |
| US10029992B2 (en) | 2014-04-23 | 2018-07-24 | Basf Se | Diaminotriazine compounds and their use as herbicides |
| CR20160545A (es) | 2014-04-23 | 2017-03-31 | Basf Se | Compuestos de diaminotriazina como herbicidas |
| AU2016249021A1 (en) | 2015-04-17 | 2017-10-19 | Assembly Biosciences, Inc. | Hepatitis B viral assembly effectors |
| CN106518849B (zh) * | 2016-10-27 | 2019-08-16 | 上海人类基因组研究中心 | 喹唑啉类化合物及其制备方法和用途 |
| CN113727758A (zh) * | 2019-03-01 | 2021-11-30 | 锐新医药公司 | 双环杂环基化合物及其用途 |
| AU2023377192A1 (en) * | 2022-11-07 | 2025-05-22 | Kyoto University | Nitrogen-containing heterocyclic compound |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CZ387292A3 (en) | 1991-02-20 | 1994-04-13 | Pfizer | 2,4-diaminoquinazoline derivatives, process of their preparation and use as substances for increasing anti-tumorous activity |
| AU2002361846A1 (en) | 2001-12-21 | 2003-07-15 | Bayer Pharmaceuticals Corporation | Quinazoline and quinoline derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents |
| AU2003255482A1 (en) | 2002-10-02 | 2004-04-23 | Merck Patent Gmbh | Use of 4 amino-quinazolines as anti cancer agents |
| CN101031551A (zh) * | 2004-07-06 | 2007-09-05 | 安吉永生物制药公司 | 针对癌症治疗的肝细胞生长因子/c－met活性的喹唑啉调节剂 |
| WO2006105056A2 (en) * | 2005-03-28 | 2006-10-05 | Fmc Corporation | Insecticidal 2,4-diaminoquinazolines and related derivatives |
| WO2007041282A2 (en) * | 2005-09-29 | 2007-04-12 | The Johns Hopkins University | Methods and compositions for treatment of cystic fibrosis |
| US20090209536A1 (en) * | 2007-06-17 | 2009-08-20 | Kalypsys, Inc. | Aminoquinazoline cannabinoid receptor modulators for treatment of disease |
| US20100317607A1 (en) * | 2007-06-27 | 2010-12-16 | Infectious Disease Research Institute | Use of compounds for preparing anti-tuberculosis agents |
| US8637560B2 (en) | 2007-07-18 | 2014-01-28 | The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | Imidazolidinone compounds, methods to inhibit deubiquitination and methods of treatment |
| US9089572B2 (en) * | 2008-01-17 | 2015-07-28 | California Institute Of Technology | Inhibitors of p97 |
| WO2010003908A1 (en) | 2008-07-08 | 2010-01-14 | Jakobsson, Andreas | Screening assay for compounds targeting the p97 aaa-atpase complex in the ubiquitin proteasome system. |
| US8865708B2 (en) | 2010-05-07 | 2014-10-21 | California Institute Of Technology | Methods and compositions for inhibition of the transitional endoplasmic reticulum ATPase |
-
2011
- 2011-05-06 US US13/103,003 patent/US8865708B2/en not_active Expired - Fee Related
- 2011-05-06 EP EP20110778469 patent/EP2566480A4/en not_active Withdrawn
- 2011-05-06 WO PCT/US2011/035654 patent/WO2011140527A2/en not_active Ceased
- 2011-05-06 AU AU2011249859A patent/AU2011249859B2/en not_active Ceased
- 2011-05-06 JP JP2013510192A patent/JP2013530942A/ja active Pending
- 2011-05-06 KR KR1020127032164A patent/KR20130128308A/ko not_active Withdrawn
- 2011-05-06 CN CN201180026946XA patent/CN103068393A/zh active Pending
- 2011-05-06 CA CA2798698A patent/CA2798698A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| KR20130128308A (ko) | 2013-11-26 |
| CN103068393A (zh) | 2013-04-24 |
| WO2011140527A3 (en) | 2012-03-29 |
| JP2013530942A (ja) | 2013-08-01 |
| AU2011249859B2 (en) | 2014-07-03 |
| EP2566480A2 (en) | 2013-03-13 |
| AU2011249859A1 (en) | 2012-12-20 |
| EP2566480A4 (en) | 2014-03-19 |
| WO2011140527A2 (en) | 2011-11-10 |
| US8865708B2 (en) | 2014-10-21 |
| US20110288082A1 (en) | 2011-11-24 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |
Effective date: 20170510 |