HRP20171754T1 - Soli i kristalni oblici agensa za induciranje apopotoze - Google Patents
Soli i kristalni oblici agensa za induciranje apopotoze Download PDFInfo
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- HRP20171754T1 HRP20171754T1 HRP20171754TT HRP20171754T HRP20171754T1 HR P20171754 T1 HRP20171754 T1 HR P20171754T1 HR P20171754T T HRP20171754T T HR P20171754TT HR P20171754 T HRP20171754 T HR P20171754T HR P20171754 T1 HRP20171754 T1 HR P20171754T1
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- 230000006907 apoptotic process Effects 0.000 title 1
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- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
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- DKAGJZJALZXOOV-UHFFFAOYSA-N hydrate;hydrochloride Chemical compound O.Cl DKAGJZJALZXOOV-UHFFFAOYSA-N 0.000 claims 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—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
- A61K31/437—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 containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- 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
- A61K31/4375—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 containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- 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
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- 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
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- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (35)
1. Spoj, naznačen time, da mu je sistemski naziv 4-(4-{[2-(4-klorfenil)-4,4-dimetilcikloheks-1-en-1-il]metil} piperazin-1-il)-N-({3-nitro-4-[(tetrahidro-2H-piran-4-ilmetil)amino]fenil}sulfonil)-2- (1H-pirolo [2,3-b] piridin- 5-iloksi)benzamid (Spoj 1) ili njegove soli u kristalnom obliku.
2. Spoj u skladu s patentnim zahtjevom 1, pri čemu je kristalni oblik slobodna baza anhidrata Spoja 1, naznačen time, da ga karakterizira rendgenski difraktogram praha koji ima najmanje jedan pik odabran od sljedećih vrijednosti: 6.3, 7.1, 9.0, 9.5, 12.5, 14.5, 14.7, 15.9, 16.9 i 18.9 stupnjeva 2θ (uzorak A), pri čemu je svaki vrh ± 0.2 stupnjeva 2θ, izmjereno pri približno 25 °C uz Cu Kα zračenje na 1,54178 Å.
3. Spoj u skladu s patentnim zahtjevom 1, pri čemu je kristalni oblik slobodna baza anhidrata Spoja 1, naznačen time, da ga karakterizira rendgenski difraktogram praha koji ima najmanje jedan pik odabran od sljedećih vrijednosti: 5.8, 7.7, 8.3, 9.9, 13.0, 13.3, 14.2, 15.3, 16.6, 17.9, 18.3, 19.8, 20.7, 21.2, 21.9, 22.5, 23.6 i 24.1 stupnjeva 2θ (uzorak B), pri čemu je svaki vrh ± 0.2 stupnjeva 2θ, izmjereno pri približno 25 °C uz Cu Kα zračenje na 1,54178 Å.
4. Spoj u skladu s patentnim zahtjevom 1, pri čemu je kristalni oblik slobodna baza hidrata Spoja 1, naznačen time, da ga karakterizira rendgenski difraktogram praha koji ima najmanje jedan pik odabran od sljedećih vrijednosti: 5.8, 7.6, 7.9, 10.7, 11.7, 14.0, 15.3 15.8, 17.4, 18.3, 19.9, 20.4, 20.7, 22.5, 24.9, 25.8 i 26.7 stupnjeva 2θ (uzorak C), pri čemu je svaki vrh ± 0.2 stupnjeva 2θ, izmjereno pri približno 25 °C uz Cu Kα zračenje na 1,54178 Å .
5. Spoj u skladu s patentnim zahtjevom 1, pri čemu je kristalni oblik slobodna baza hidrata Spoja 1, naznačen time, da ga karakterizira rendgenski difraktogram praha koji ima najmanje jedan pik odabran sljedećih vrijednosti: 3.3, 6.4, 7.1, 7.3, 10.1, 11.4, 13.2, 14.4, 14.6, 15.1, 15.8, 16.2, 17.2, 17.6, 18.0, 18.6, 19.0, 19.5, 19.8, 20.2, 20.7, 21.0, 22.5, 23.0, 26.0, 28.9 i 29.2 stupnjeva 2θ (uzorak D), pri čemu je svaki vrh ± 0.2 stupnjeva 2θ, izmjereno pri približno 25 °C uz Cu Kα zračenje na 1,54178 Å.
6. Spoj u skladu s patentnim zahtjevom 1, pri čemu je kristalni oblik slobodna baza diklormetanskog solvata Spoja 1, naznačen time, da ga karakterizira rendgenski difraktogram praha koji ima najmanje jedan pik odabran od sljedećih vrijednosti: 5.9, 7.1, 9.6, 10.0, 10.7, 11.1, 13.2, 14.8 i 18.2 stupnjeva 2θ, pri čemu je svaki vrh ± 0.2 stupnjeva 2θ(uzorak E), izmjereno pri približno 25 °C uz Cu Kα zračenje na 1,54178 Å .
7. Spoj u skladu s patentnim zahtjevom 1, pri čemu je kristalni oblik slobodna baza diklormetanskog solvata Spoja 1, naznačen time, da je karakteriziran tipom monoklinskih rešetaka i prostornom skupinom P21/n koja ima duljine jediničnih stanica za tri osi od oko (a) 13.873 Å, (b), 12.349 Å, (c) 29.996 Å i tri kuta jedinične ćelija od oko (α) 90.00°, (β) 92.259° i (γ) 90.00°.
8. Spoj u skladu s patentnim zahtjevom 1, pri čemu je kristalni oblik slobodna baza etil-acetatnog solvata spoja 1, naznačen time, da ga karakterizira rendgenski difraktogram praha koji ima najmanje jedan pik odabran od sljedećih vrijednosti: 5.8, 7.1, 9.5, 9.9, 10.6, 11.6, 13.1, 13.8, 14.8, 16.0, 17.9, 20.2, 21.2, 23.2, 24.4 i 26.4 stupnjeva 2θ (uzorak F), pri čemu je svaki vrh ± 0.2 stupnjeva 2θ, izmjereno pri približno 25 °C uz Cu Ka zračenje na 1,54178 Å.
9. Spoj u skladu s patentnim zahtjevom 1, pri čemu je kristalni oblik slobodna baza etil-acetatnog solvata spoja 1, naznačen time, da ga karakterizira rendgenski difraktogram praha koji ima najmanje jedan pik odabran od sljedećih vrijednosti: 3.3, 6.5, 7.0, 7.3, 9.2, 9.7, 11.2, 11.4, 11.9, 12.9, 14.4, 14.9, 15.8, 16.2, 17.2, 17.4, 17.8, 18.5, 18.9, 19.4, 20.1, 20.7, 20.9, 22.0, 22.7, 23.4, 23.8, 24.7, 25.9, 27.0 i 28.9 stupnjeva 2θ (uzorak G), pri čemu je svaki vrh ± 0.2 stupnjeva 2θ, izmjereno pri približno 25 °C uz zračenje na 1,54178 Å.
10. Spoj u skladu s patentnim zahtjevom 1, pri čemu je kristalni oblik slobodna baza acetonitrilnog solvata Spoja 1, naznačen time, da ga karakterizira rendgenski difraktogram praha koji ima najmanje jedan pik odabran od sljedećih vrijednosti: 5.8, 7.4, 7.6, 10.2, 13.0, 13.6, 14.9, 16.4, 17.0, 17.5, 18.2, 19.4, 19.7, 20.4, 21.0, 21.2, 21.8, 22.4, 22.9, 24.2, 24.3, 26.1 i 29.2 stupnjeva 2θ (uzorak H), pri čemu je svaki vrh ± 0.2 stupnjeva 2θ, izmjereno pri približno 25 °C uz zračenje na 1,54178 Å.
11. Spoj u skladu s patentnim zahtjevom 1, pri čemu je kristalni oblik slobodna baza acetonitrilnog solvata Spoja 1, naznačen time, da je karakteriziran tipom triklinskih rešetaka i prostornom skupinom Pl koja ima duljine jediničnih stanica za tri osi od oko (a) 12.836 Å, (b) 13.144 Å, (c) 15.411 Å i tri kuta jedinične ćelija od oko (α) 92.746°, (β) 95.941° i (γ) 113.833°.
12. Spoj u skladu s patentnim zahtjevom 1, pri čemu je kristalni oblik slobodna baza acetonitrilnog solvata Spoja 1, naznačen time, da ga karakterizira rendgenski difraktogram praha koji ima najmanje jedan pik odabran između sljedećih vrijednosti: 6.4, 6.9, 7.7, 8.8, 9.4, 11.1, 12.3, 12.8, 16.5, 17.0, 17.4, 18.3, 18.6, 19.0, 19.2, 20.3, 21.6, 22.3, 22.9 i 23.7 stupnjeva 2θ (uzorak I), pri čemu je svaki vrh ± 0.2 stupnjeva 2θ, izmjereno pri približno 25 °C uz zračenje na 1,54178 Å.
13. Spoj u skladu s patentnim zahtjevom 1, pri čemu je kristalni oblik slobodna baza acetonskog solvata Spoja 1, naznačen time, da ga karakterizira rendgenski difraktogram praha koji ima najmanje jedan pik odabran između sljedećih vrijednosti: 6.0, 6.8, 8.0, 9.0, 9.7, 11.2, 11.9, 12.6, 14.7, 15.0, 15.2, 15.8, 16.4, 16.6, 17.6, 17.8, 17.9, 18.7, 20.2, 20.8, 21.6, 22.2, 22.6, 23.3, 23.8, 24.0, 24.4, 26.8, 27.1, 28.0 i 28.2 stupnjeva 2θ (uzorak J), pri čemu je svaki vrh ± 0.2 stupnjeva 2θ, izmjereno pri približno 25 °C uz zračenje na 1,54178 Å.
14. Spoj u skladu s patentnim zahtjevom 1, pri čemu je kristalni oblik hidroklorid Spoja 1, naznačen time, da ga karakterizira rendgenski difraktogram praha koji ima najmanje jedan pik odabran između sljedećih vrijednosti: 5.1, 5.9, 7.7, 9.9, 10.2, 10.8, 13.6, 14.0, 15.4, 15.9, 16.2, 17.6, 18.3, 18.7, 19.7, 19.9, 20.1, 20.4,
20.7, 20.9, 22.9, i 26.2 stupnjeva 2θ (uzorak K), pri čemu je svaki vrh ± 0.2 stupnjeva 2θ, izmjereno pri približno 25 °C uz Cu Ka zračenje na 1,54178 Å.
15. Spoj u skladu s patentnim zahtjevom 1, pri čemu je kristalni oblik hidroklorid Spoja 1, naznačen time, da je karakteriziran tipom triklinskih rešetaka i prostornom skupinom Pl koja ima duljine jediničnih stanica za tri osi od oko (a) 10.804 Å, (b) 12.372 Å, (c) 19.333 Å i tri kuta jedinične ćelija od oko (α) 76.540°, (β) 87.159° i (γ) 70.074°.
16. Spoj u skladu s patentnim zahtjevom 1, pri čemu je kristalni oblik hidroklorid hidrat Spoja 1, naznačen time, da ga karakterizira rendgenski difraktogram praha koji ima barem jedan pik odabran između sljedećih vrijednosti: 4.6, 8.7, 9.6, 9.9, 12.3, 14.9, 15.7, 17.6, 18.1, 18.4, 19.3, 19.6, 21.0, 23.3, 23.9, 24.8, 26.5, 27.2, 27.4, 29.0 i 30.1 stupnjeva 2θ (uzorak L), pri čemu je svaki vrh ± 0.2 stupnjeva 2θ, izmjereno pri približno 25 °C uz Cu Ka zračenje na 1,54178 Å.
17. Spoj u skladu s patentnim zahtjevom 1, pri čemu je kristalni oblik sulfat Spoja 1, naznačen time, da ga karakterizira rendgenski difraktogram praha koji ima najmanje jedan pik odabran između sljedećih vrijednosti: 4.8, 7.7, 8.3, 9.7, 10.2, 12.0, 12.6, 14.5, 15.4, 17.4, 17.9, 18.4, 19.1, 19.5, 21.0, 22.4, 23.3, 23.9, 25.1 i 26.8 stupnjeva 2θ (uzorak M), pri čemu je svaki vrh ± 0.2 stupnjeva 2θ, izmjereno pri približno 25 °C uz Cu Ka zračenje na 1,54178 θ.
18. Farmaceutski pripravak, naznačen time, da sadržava spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1 do 17 i jedan ili više farmaceutski prihvatljivih pomoćnih tvari.
19. Postupak za pripravu farmaceutske otopine Spoja 1 ili njegove soli, naznačen time, da obuhvaća otapanje spoja ili soli iz bilo kojeg od patentnih zahtjeva 1 do 17 u farmaceutski prihvatljivom otapalu ili smjesi otapala.
20. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1 do 17, ili farmaceutski pripravak koji sadržava spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1 do 17 i jedan ili više farmaceutski prihvatljivih pomoćnih tvari, namijenjen upotrebi u postupku liječenja bolesti, naznačen time, da je riječ o apoptoznoj disfunkciji i / ili prekomjernoj ekspresiji proteina iz obitelji anti-apoptotičnog Bcl-2 pri čemu je bolest neoplastična, imuna ili autoimuna bolest.
21. Spoj ili sol ili farmaceutski pripravak za uporabu u skladu s patentnim zahtjevom 20, naznačen time, da navedeni postupak obuhvaća davanje navedenog spoja ili soli ili farmaceutskog pripravka oralnim, parenteralnim, sublingvalnim, bukalnim,
intranazalnim, plućnim, topikalnim, transdermalnim, intradermalnim, okularnim, otičnim, rektalnim, vaginalnim, intragastričnim, intrakranijskim, intrasinovialnim ili intraartikularnim putem.
22. Spoj, sol ili farmaceutski pripravak za uporabu u skladu s patentnim zahtjevom 20, naznačen time, da je neoplastična bolest odabrana iz skupine koju čine rak, mezoteliom, rak mjehura, rak gušterače, rak kože, rak glave ili vrata, kožni ili intraokularni melanom, rak jajnika, rak dojke, rak maternice, rak jajovoda, karcinom endometrija, karcinom cerviksa, karcinom vagine, karcinom vulve, karcinom kostiju, rak debelog crijeva, rak rektuma, rak analnog područja, rak želuca, gastrointestinalni karcinom, rak želuca, rak debelog crijeva, rak dvanaestpalčanog crijeva, kronična limfocitna leukemija, rak jednjaka, rak tankog crijeva, rak endokrinog sustava, rak štitne žlijezde, rak paratiroidne žlijezde, rak nadbubrežne žlijezde, sarkom mekog tkiva, rak mokraćovoda, karcinom penisa, rak testisa, hepatocelularni karcinom, rak jetre, rak žučnog kanala, primarni ili sekundarni tumor središnjeg živčanog sustava, primarni ili sekundarni tumor mozga, Hodgkinova bolest, kronična ili akutna leukemija, kronična mijeloična leukemija, limfocitni limfom, limfoblastična leukemija, folikularni limfom, limfoidni maligni tumor T-stanica ili B-stanica, melanom, multipli mijelom, oralni karcinom, rak pluća ne-malih stanica, rak prostate, rak pluća malih stanica, rak bubrega i / ili uretre, karcinom bubrežnih stanica, karcinom bubrežne zdjelice, neoplazam središnjeg živčanog sustava, primarni limfom središnjeg živčanog sustava, ne-Hodgkinov limfom, tumor kralježnične moždine, gliom moždanog stabla, adenom hipofize, adrenokortikalni tumor, rak žučnog mjehura, rak slezene, kolangiokarcinom, fibrosarkom, neuroblastom, retinoblastom i njihove kombinacije.
23. Spoj ili sol ili farmaceutski pripravak za uporabu u skladu s patentnim zahtjevom 20, naznačen time, da bolest je limfoidni maligni tumor.
24. Spoj ili sol ili farmaceutski pripravak za uporabu u skladu s patentnim zahtjevom 23, naznačen time, da je limfoidni maligni tumor (maligni tumor) ne-Hodgkinov limfom, kronična limfoidna leukemija ili akutna limfocitna leukemija.
25. Spoj, sol ili farmaceutski pripravak za uporabu u skladu s patentnim zahtjevom 20, naznačen time, da navedeni postupak obuhvaća davanje navedenog spoja ili soli ili farmaceutskog pripravka oralno u dozi od oko 50 do oko 1000 mg spoja 1 ili njegove soli po danu uz prosječni interval liječenja od oko 3 sata do oko 7 dana.
26. Spoj, sol ili farmaceutski pripravak za uporabu u skladu s patentnim zahtjevom 20, naznačen time, da navedeni postupak obuhvaća davanje navedenog spoja ili soli ili farmaceutskog pripravka oralno jednom dnevno u dozi od oko 200 do oko 400 mg ekvivalenta slobodne baze Spoja 1 po danu.
27. Disperzija spoja ili soli u skladu s bilo kojim od patentnih zahtjeva 1 do 17, namijenjena upotrebi u postupku liječenja bolesti, naznačena time, da je riječ o apoptoznoj disfunkciji i/ili prekomjernoj ekspresiji proteina iz obitelji anti-apoptotičnog Bcl-2 pri čemu je bolest neoplastična, imuna ili autoimuna bolest.
28. Disperzija za uporabu u skladu s patentnim zahtjevom 27, naznačena time, da navedeni postupak obuhvaća primjenu navedene disperzije oralnim, parenteralnim, sublingvalnim, bukalnim, intranazalnim, plućnim, topikalnim, transdermalnim, intradermalnim, okularnim, otičnim, rektalnim, vaginalnim, intragastričnim, intrakranijalnim, intrasinovijalnom ili intraartikularnim putem.
29. Disperzija za uporabu u skladu s patentnim zahtjevom 27, naznačena time, da je neoplastična bolest odabrana iz skupine koju čine rak, mezoteliom, rak mjehura, rak gušterače, rak kože, rak glave ili vrata, kožni ili intraokularni melanom, rak jajnika, rak dojke, rak maternice, rak jajovoda, karcinom endometrija, karcinom cerviksa, karcinom vagine, karcinom vulve, karcinom kostiju, rak debelog crijeva, rak rektuma, rak analnog područja, rak želuca, gastrointestinalni karcinom, rak želuca, rak debelog crijeva, rak dvanaestpalčanog crijeva, kronična limfocitna leukemija, rak jednjaka, rak tankog crijeva, rak endokrinog sustava, rak štitne žlijezde, rak paratireoidnih žlijezda, nadbubrežne žlijezde, sarkom mekog tkiva, rak mokraćovoda, karcinom penisa, rak testisa, hepatocelularni karcinom, rak jetre, rak žučnog kanala, primarni ili sekundarni tumor središnjeg živčanog sustava, primarni ili sekundarni tumor mozga, Hodgkinova bolest, kronična ili akutna leukemija, kronična mijeloična leukemija, limfocitni limfom, limfoblastična leukemija, folikularni limfom, limfoidni maligni tumor T-stanica ili B-stanica, melanom, multipli mijelom, oralni karcinom,rak pluća ne-malih stanica, rak prostate, rak pluča malih stanica, raka bubrega i / ili uretera, karcinom bubrežnih stanica, karcinom bubrežne zdjelice,
neoplazam središnjeg živčanog sustava, primarni limfom središnjeg živčanog sustava, ne-Hodgkinov limfom, tumor kralježnične moždine, gliom moždanog stabla, adenom hipofize, adrenokortikalni tumor, rak žučnog mjehura, rak slezene, kolangiokarcinom, fibrosarkom, neuroblastom, retinoblastom i njihovih kombinacija.
30. Disperzija za uporabu u skladu s patentnim zahtjevom 27, naznačena time, da je bolest maligna limfoidna bolest.
31. Disperzija za uporabu u skladu s patentnim zahtjevom 30, naznačena time, da je limfoidni maligni tumor ne-Hodgkinov limfom, kronična limfoidna leukemija ili akutna limfocitna leukemija.
32. Disperzija za uporabu u skladu s patentnim zahtjevom 27, naznačena time, da navedeni postupak obuhvaća davanje navedene disperzije oralno u dozi od oko 50 do oko 1000 mg Spoja 1 ili njegove soli po danu u prosječnom intervalu tretmana od oko 3 sata do oko 7 dana.
33. Disperzija za uporabu u skladu s patentnim zahtjevom 27, naznačena time, da navedeni postupak obuhvaća davanje navedene disperzije oralno jednom dnevno u dozi od oko 200 do oko 400 mg ekvivalenta slobodne baze Spoja 1 na dan.
34. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da mu je sistemsko ime 4-(4-{[2-(4-klorfenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)N-({3-nitro-4-[(tetrahidro-2H-piran-4-ilmetil)-amino]fenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid hidroklorid u kristalnom obliku.
35. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da mu je sistemsko ime 4-(4-{[2-(4-klorfenil)-4,4-dimetilcikloheks-1-en-1-il]metil}piperazin-1-il)-N-({3-nitro-4-[(tetrahidro-2H-piran-4-ilmetil)-amino]fenil}sulfonil)-2-(1H-pirolo[2,3-b]piridin-5-iloksi)benzamid sulfata u kristalnom obliku.
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