HRP20160545T1 - Inhibitor fosfoinozitid 3-kinaze sa dijelom koji veže cink - Google Patents
Inhibitor fosfoinozitid 3-kinaze sa dijelom koji veže cink Download PDFInfo
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- HRP20160545T1 HRP20160545T1 HRP20160545TT HRP20160545T HRP20160545T1 HR P20160545 T1 HRP20160545 T1 HR P20160545T1 HR P20160545T T HRP20160545T T HR P20160545TT HR P20160545 T HRP20160545 T HR P20160545T HR P20160545 T1 HRP20160545 T1 HR P20160545T1
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- Prior art keywords
- cancer
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- compound according
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- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 title 1
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 title 1
- 230000004572 zinc-binding Effects 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 14
- 201000010099 disease Diseases 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 9
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 claims 6
- 108091007960 PI3Ks Proteins 0.000 claims 6
- 230000001404 mediated effect Effects 0.000 claims 6
- 239000000825 pharmaceutical preparation Substances 0.000 claims 5
- 102000003964 Histone deacetylase Human genes 0.000 claims 4
- 108090000353 Histone deacetylase Proteins 0.000 claims 4
- 239000004480 active ingredient Substances 0.000 claims 4
- 208000035269 cancer or benign tumor Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 4
- 208000014829 head and neck neoplasm Diseases 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 206010003571 Astrocytoma Diseases 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 208000017604 Hodgkin disease Diseases 0.000 claims 2
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 2
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 208000026037 malignant tumor of neck Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 208000003154 papilloma Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 201000002510 thyroid cancer Diseases 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 125000006686 (C1-C24) alkyl group Chemical group 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
Classifications
-
- 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
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4365—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
-
- 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
- A61K31/33—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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- 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
- C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
- C07D213/30—Oxygen atoms
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (15)
1. Spoj s formulom I:
[image]
ili njegova farmaceutski prihvatljiva sol, naznačen time da R je vodik ili acil skupina.
2. Spoj prema zahtjevu 1 naznačen time da R je R1C(O)-, naznačen time da R1 je supstituirani ili nesupstituirani C1-C24-alkil; supstituirani ili nesupstituirani C2-C24-alkenil; supstituirani ili nesupstituirani C2-C24-alkinil; supstituirani ili nesupstituirani aril; ili supstituirani ili nesupstituirani heteroaril.
3. Spoj prema zahtjevu 2 naznačen time da R1 je supstituirani ili nesupstituirani C1-C6-alkil ili supstituirani ili nesupstituirani C2-C6 alkenil.
4. Spoj prema zahtjevu 1 naznačen time da R je H ili acetil.
5. Spoj prema zahtjevu 1 naznačen time da je prikazan s formulom:
[image]
ili njegova farmaceutski prihvatljiva sol.
6. Farmaceutski pripravak naznačen time da sadrži kao aktivni sastojak spoj prema zahtjevu 1 i farmaceutski prihvatljiv nosač.
7. Farmaceutski pripravak za oralnu primjenu naznačen time da sadrži kao aktivni sastojak spoj prema zahtjevu 1 i farmaceutski prihvatljiv nosač.
8. Farmaceutski pripravak naznačen time da sadrži kao aktivni sastojak spoj prema zahtjevu 5 i farmaceutski prihvatljiv nosač.
9. Farmaceutski pripravak za oralnu primjenu naznačen time da sadrži kao aktivni sastojak spoj prema zahtjevu 5 i farmaceutski prihvatljiv nosač.
10. Farmaceutski pripravak prema zahtjevu 6 naznačen time da je za uporabu za liječenje bolesti ili poremećaja posredovanih s PI3K kod subjekta kojemu je to potrebno.
11. Pripravak za uporabu prema zahtjevu 10, naznačen time da navedena bolest ili poremećaj povezan s PI3K je poremećaj proliferacije stanice, poželjno gdje je poremećaj proliferacije stanice rak, kao što je papilom, blastogliom, Kapozijev sarkom, melanom, karcinom ne-malih stanica pluća, rak jajnika, rak prostate, karcinom skvamoznih stanica, astrocitom, rak glave, rak vrata, rak mokraćnog mjehura, rak dojke, rak pluća, kolorektalni rak, rak tiroidne žlijezde, rak gušterače, rak želuca, hepatocelularni karcinom, leukemija, limfom, Hodgkinova bolest i Burkittova bolest.
12. Farmaceutski pripravak prema zahtjevu 6 naznačen time da je za uporabu za liječenje bolesti posredovane s HDAC ili za uporabu za liječenje bolesti koja je posredovana s oboje PI3K i HDAC.
13. Farmaceutski pripravak prema zahtjevu 8 naznačen time da je za uporabu za liječenje bolesti ili poremećaja posredovanih s PI3K kod subjekta kojemu je to potrebno.
14. Pripravak za uporabu prema zahtjevu 13 naznačen time da navedena bolest ili poremećaj povezan s PI3K je poremećaj proliferacije stanice, poželjno gdje je poremećaj proliferacije stanice rak, kao što je papilom, blastogliom, Kapozijev sarkom, melanom, karcinom ne-malih stanica pluća, rak jajnika, rak prostate, karcinom skvamoznih stanica, astrocitom, rak glave, rak vrata, rak mokraćnog mjehura, rak dojke, rak pluća, kolorektalni rak, rak tiroidne žlijezde, rak gušterače, rak želuca, hepatocelularni karcinom, leukemija, limfom, Hodgkinova bolest i Burkittova bolest.
15. Farmaceutski pripravak prema zahtjevu 8 naznačen time da je za uporabu za liječenje bolesti posredovane s HDAC, ili za uporabu za liječenje bolesti koja je posredovana s oboje PI3K i HDAC.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161470849P | 2011-04-01 | 2011-04-01 | |
| US201161559489P | 2011-11-14 | 2011-11-14 | |
| EP12764605.7A EP2694075B1 (en) | 2011-04-01 | 2012-03-30 | Phosphoinositide 3-kinase inhibitor with a zinc binding moiety |
| PCT/US2012/031361 WO2012135571A1 (en) | 2011-04-01 | 2012-03-30 | Phosphoinositide 3-kinase inhibitor with a zinc binding moiety |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20160545T1 true HRP20160545T1 (hr) | 2016-06-17 |
Family
ID=46931927
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20160545TT HRP20160545T1 (hr) | 2011-04-01 | 2016-05-20 | Inhibitor fosfoinozitid 3-kinaze sa dijelom koji veže cink |
| HRP20191091TT HRP20191091T1 (hr) | 2011-04-01 | 2019-06-17 | Inhibitor fosfoinozitid-3-kinaze s ostatkom koji se veže na cink |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20191091TT HRP20191091T1 (hr) | 2011-04-01 | 2019-06-17 | Inhibitor fosfoinozitid-3-kinaze s ostatkom koji se veže na cink |
Country Status (30)
| Country | Link |
|---|---|
| US (7) | US8710219B2 (hr) |
| EP (2) | EP3111938B1 (hr) |
| JP (3) | JP6242331B2 (hr) |
| KR (2) | KR20180108848A (hr) |
| CN (2) | CN103582483B (hr) |
| AU (1) | AU2012236367B2 (hr) |
| BR (1) | BR112013025340B1 (hr) |
| CA (1) | CA2830822C (hr) |
| CL (1) | CL2013002823A1 (hr) |
| CY (2) | CY1117785T1 (hr) |
| DK (2) | DK3111938T3 (hr) |
| EA (1) | EA022434B9 (hr) |
| ES (2) | ES2733128T3 (hr) |
| HK (1) | HK1194969A1 (hr) |
| HR (2) | HRP20160545T1 (hr) |
| HU (2) | HUE045041T2 (hr) |
| IL (2) | IL228588A (hr) |
| LT (1) | LT3111938T (hr) |
| ME (2) | ME02451B (hr) |
| MX (1) | MX340577B (hr) |
| PE (1) | PE20141382A1 (hr) |
| PL (2) | PL2694075T3 (hr) |
| PT (2) | PT3111938T (hr) |
| RS (2) | RS54903B1 (hr) |
| SG (2) | SG10201602569RA (hr) |
| SI (2) | SI3111938T1 (hr) |
| SM (1) | SMT201600179B (hr) |
| TW (1) | TWI571469B (hr) |
| WO (1) | WO2012135571A1 (hr) |
| ZA (2) | ZA201307082B (hr) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA024252B1 (ru) | 2009-01-08 | 2016-08-31 | Кьюрис, Инк. | Ингибиторы фосфоинозитид-3-киназ с цинксвязывающей группой |
| AU2012236367B2 (en) * | 2011-04-01 | 2014-10-09 | Curis, Inc. | Phosphoinositide 3-kinase inhibitor with a zinc binding moiety |
| SG10201510307WA (en) | 2011-11-14 | 2016-01-28 | Cephalon Inc | Uracil derivatives as axl and c-met kinase inhibitors |
| CN104725301A (zh) * | 2013-12-20 | 2015-06-24 | 北京蓝贝望生物医药科技股份有限公司 | 一种1,2-二氢吡啶-2-酮衍生物的制备方法 |
| ES2833473T3 (es) * | 2015-04-21 | 2021-06-15 | Chengdu Zenitar Biomedical Tech Co Ltd | Derivados de purinil-N-hidroxil pirimidin formamida, método de preparación y uso de los mismos |
| WO2018015895A1 (en) * | 2016-07-19 | 2018-01-25 | National Institute Of Plant Genome Research | Novel protein against fungal pathogens |
| AU2017355385A1 (en) * | 2016-11-02 | 2019-05-30 | Curis, Inc. | Combination therapy with a phosphoinositide 3-kinase inhibitor with a zinc binding moiety |
| AU2018360845B2 (en) * | 2017-11-06 | 2024-05-02 | Cold Spring Harbor Laboratory | Method and compositions for forming a copper-containing complex and uses thereof |
| KR20210087438A (ko) | 2018-09-11 | 2021-07-12 | 쿠리스 인코퍼레이션 | 아연 결합 모이어티를 가진 포스포이노시티드 3-키나제 저해제를 이용한 병용 요법 |
| WO2023212574A1 (en) * | 2022-04-26 | 2023-11-02 | Olivia Szu Hsieh Lee Nakaya | Compositions and methods for modulating rhythmic activity of pacemaker cardiomyocytes |
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