HRP20161654T1 - Kristalinični tripeptid epoksi ketoni-inhibitori proteaze - Google Patents
Kristalinični tripeptid epoksi ketoni-inhibitori proteaze Download PDFInfo
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- HRP20161654T1 HRP20161654T1 HRP20161654TT HRP20161654T HRP20161654T1 HR P20161654 T1 HRP20161654 T1 HR P20161654T1 HR P20161654T T HRP20161654T T HR P20161654TT HR P20161654 T HRP20161654 T HR P20161654T HR P20161654 T1 HRP20161654 T1 HR P20161654T1
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- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 title 1
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 title 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 29
- 239000000203 mixture Substances 0.000 claims 7
- 208000034578 Multiple myelomas Diseases 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 239000000126 substance Substances 0.000 claims 3
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 206010065687 Bone loss Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims 2
- 210000000481 breast Anatomy 0.000 claims 2
- 239000002775 capsule Substances 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000008187 granular material Substances 0.000 claims 2
- 208000028867 ischemia Diseases 0.000 claims 2
- 210000003734 kidney Anatomy 0.000 claims 2
- 239000000843 powder Substances 0.000 claims 2
- 239000003826 tablet Substances 0.000 claims 2
- 238000002054 transplantation Methods 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 1
- 208000026305 Myelodysplastic-Myeloproliferative disease Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000007452 Plasmacytoma Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 230000030741 antigen processing and presentation Effects 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 238000000113 differential scanning calorimetry Methods 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000004696 endometrium Anatomy 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 210000001508 eye Anatomy 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 201000009277 hairy cell leukemia Diseases 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 230000002489 hematologic effect Effects 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 210000000867 larynx Anatomy 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 210000001165 lymph node Anatomy 0.000 claims 1
- 210000004698 lymphocyte Anatomy 0.000 claims 1
- 201000007919 lymphoplasmacytic lymphoma Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 210000000214 mouth Anatomy 0.000 claims 1
- 210000003739 neck Anatomy 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 210000000664 rectum Anatomy 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 235000020357 syrup Nutrition 0.000 claims 1
- 239000006188 syrup Substances 0.000 claims 1
- 210000001550 testis Anatomy 0.000 claims 1
- 238000002411 thermogravimetry Methods 0.000 claims 1
- 238000001757 thermogravimetry curve Methods 0.000 claims 1
- 210000004291 uterus Anatomy 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
-
- 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
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P31/12—Antivirals
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P35/02—Antineoplastic agents specific for leukemia
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- A61P37/02—Immunomodulators
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- A—HUMAN NECESSITIES
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- A61P37/00—Drugs for immunological or allergic disorders
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- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or 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
- C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
- C07K1/02—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length in solution
- C07K1/026—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length in solution by fragment condensation in solution
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Communicable Diseases (AREA)
- Analytical Chemistry (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Virology (AREA)
- Urology & Nephrology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Tropical Medicine & Parasitology (AREA)
Claims (29)
1. Farmaceutski sastav sadrži (a) farmaceutski prihvatljivi nosač i (b) kristaliničnu tvar koja ima strukturnu formulu (II)
[image]
2. Farmaceutski sastav iz patentnog zahtjeva 1, pri čemu se sastav može primjenjivati oralnim putem.
3. Farmaceutski sastav iz patentnog zahtjeva 2, pri čemu je sastav koji se može primjenjivati oralno odabran iz grupe koja se sastoji od tableta, kapsula, granula, praška i sirupa.
4. Farmaceutski sastav iz patentnog zahtjeva 3, pri čemu je sastav koji se može primjenjivati oralno tableta.
5. Farmaceutski sastav iz patentnog zahtjeva 3, pri čemu je sastav koji se može primjenjivati oralno kapsula.
6. Farmaceutski sastav iz patentnog zahtjeva 3, pri čemu je sastav koji se može primjenjivati oralno granula.
7. Farmaceutski sastav iz patentnog zahtjeva 3, pri čemu je sastav koji se može primjenjivati oralno prašak.
8. Farmaceutski sastav iz patentnog zahtjeva 1, pri čemu se sastav može primjenjivati parenteralnim putem.
9. Farmaceutski sastav iz bilo kojeg od patentnih zahtjeva 1 do 8 pri čemu kristalinična tvar prikazuje termogram dobiven diferencijalnim kalorimetrijskim pregledom (DSC) koji je karakteriziran oštrim endotermičkim pikom na 147°C.
10. Farmaceutski sastav iz bilo kojeg od patentnih zahtjeva 1 do 9 pri čemu kristalinična tvar formule (II) prikazuje od 0.0 do 0.3% gubitka mase u rasponu temperature od 25°C do 125°C u termogravimetrijskim analizama.
11. Farmaceutski sastav iz bilo kojeg od patentnih zahtjeva 1 do 10 za uporabu u liječenju raka.
12. Farmaceutski sastav za uporabu iz patentnog zahtjeva 11, pri čemu je rak rak mjehura, krvi, kostiju, mozga, dojke, cerviksa, prsiju, debelog crijeva, endometrija, jednjaka, oka, glave, bubrega, jetre, pluća, limfnih čvorova, usta, vrata, jajnika, gušterače, prostate, rektuma, bubrega, kože, želuca, testisa, grkljana ili maternice.
13. Farmaceutski sastav iz bilo kojeg od patentnih zahtjeva 1 do 10 za uporabu u liječenju leukemije, akutne limfocitne leukemije (ALL), akutne mijeloične leukemije (AML), kronične limfocitne leukemije (CLL), kronične mijeloične leukemije (CML), leukemije vlasastih stanica, limfoma malih limfocita, limfoplazmacitnog limfoma, mijeloma plazma stanica, plazmacitoma ili multiplog mijeloma.
14. Farmaceutski sastav iz bilo kojeg od patentnih zahtjeva 1 do 10 za uporabu u liječenju multiplog mijeloma.
15. Farmaceutski sastav iz bilo kojeg od patentnih zahtjeva 1 do 10 za uporabu u liječenju Waldenstromove makroglobulinemije.
16. Farmaceutski sastav iz bilo kojeg od patentnih zahtjeva 1 do 10 za uporabu u liječenju raka odabranog između hematološkog raka, Waldenstromove makroglobulinemije, multiplog mijeloma, difuznog limfoma B stanica, limfoma plaštenih stanica, raka gušterače i raka pluća.
17. Farmaceutski sastav iz bilo kojeg od patentnih zahtjeva 1 do 10 za uporabu u liječenju mijelodisplastičnog sindroma ili mijeloproliferativne bolesti.
18. Farmaceutski sastav iz bilo kojeg od patentnih zahtjeva 1 do 10 za uporabu u liječenju autoimune bolesti.
19. Farmaceutski sastav za uporabu u liječenju iz patentnog zahtjeva 18 pri čemu je autoimuna bolest odabrana iz grupe koja se sastoji od lupusa, reumatoidnog artritisa i prezentacije antigena.
20. Farmaceutski sastav iz bilo kojeg od patentnih zahtjeva 1 do 10 za uporabu u liječenju stanja uzrokovanog presatkom ili transplantacijom.
21. Farmaceutski sastav za uporabu u liječenju iz patentnog zahtjeva 20 pri čemu je presatkom ili transplantacijom uzrokovano stanje bolest presatka protiv primatelja.
22. Farmaceutski sastav iz bilo kojeg od patentnih zahtjeva 1 do 10 za uporabu u liječenju neurodegenerativne bolesti.
23. Farmaceutski sastav iz bilo kojeg od patentnih zahtjeva 1 do 10 za uporabu u liječenju upale.
24. Farmaceutski sastav iz bilo kojeg od patentnih zahtjeva 1 do 10 za uporabu u liječenju stanja povezanog s fibrozom.
25. Farmaceutski sastav iz bilo kojeg od patentnih zahtjeva 1 do 10 za uporabu u liječenju stanja povezanog s ishemijom.
26. Farmaceutski sastav za uporabu u liječenju iz patentnog zahtjeva 25 pri čemu je stanje povezano s ishemijom zatajenje srca.
27. Farmaceutski sastav iz bilo kojeg od patentnih zahtjeva 1 do 10 za uporabu u liječenju infekcije.
28. Farmaceutski sastav iz bilo kojeg od patentnih zahtjeva 1 do 10 za uporabu u liječenju bolesti povezane s gubitkom kostiju.
29. Farmaceutski sastav za uporabu u liječenju iz patentnog zahtjeva 28 pri čemu je stanje povezano s gubitkom kostiju osteoporoza.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16219609P | 2009-03-20 | 2009-03-20 | |
| US18056109P | 2009-05-22 | 2009-05-22 | |
| EP14178725.9A EP2813241B1 (en) | 2009-03-20 | 2010-03-22 | Crystalline tripeptide epoxy ketone protease inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20161654T1 true HRP20161654T1 (hr) | 2017-01-27 |
Family
ID=42738216
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20150014AT HRP20150014T1 (hr) | 2009-03-20 | 2015-01-08 | Inhibitori proteaze kristalnih tripeptida epoksidketona |
| HRP20161654TT HRP20161654T1 (hr) | 2009-03-20 | 2016-12-06 | Kristalinični tripeptid epoksi ketoni-inhibitori proteaze |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20150014AT HRP20150014T1 (hr) | 2009-03-20 | 2015-01-08 | Inhibitori proteaze kristalnih tripeptida epoksidketona |
Country Status (45)
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1948678T3 (da) | 2005-11-09 | 2013-06-24 | Onyx Therapeutics Inc | Forbindelser til enzyminhibering |
| UA101303C2 (uk) | 2006-06-19 | 2013-03-25 | Протеолікс, Інк. | Сполуки для інгібування ферменту протеасоми |
| DK2207791T4 (da) | 2007-10-04 | 2019-10-07 | Onyx Therapeutics Inc | Krystallinske peptidepoxyketon-proteasehæmmere og syntese af aminosyreketoepoxider |
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