HRP20170291T1 - Derivati ftalazina - Google Patents
Derivati ftalazina Download PDFInfo
- Publication number
- HRP20170291T1 HRP20170291T1 HRP20170291TT HRP20170291T HRP20170291T1 HR P20170291 T1 HRP20170291 T1 HR P20170291T1 HR P20170291T T HRP20170291T T HR P20170291TT HR P20170291 T HRP20170291 T HR P20170291T HR P20170291 T1 HRP20170291 T1 HR P20170291T1
- Authority
- HR
- Croatia
- Prior art keywords
- pharmaceutically acceptable
- stereoisomers
- stands
- denotes
- atoms
- Prior art date
Links
- LFSXCDWNBUNEEM-UHFFFAOYSA-N phthalazine Chemical class C1=NN=CC2=CC=CC=C21 LFSXCDWNBUNEEM-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 13
- 239000000203 mixture Substances 0.000 claims 10
- 239000012453 solvate Substances 0.000 claims 9
- 125000004432 carbon atom Chemical group C* 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 229940079593 drug Drugs 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 210000000481 breast Anatomy 0.000 claims 2
- 210000003169 central nervous system Anatomy 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 2
- 210000003800 pharynx Anatomy 0.000 claims 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010019695 Hepatic neoplasm Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 208000001738 Nervous System Trauma Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000012752 auxiliary agent Substances 0.000 claims 1
- 235000010290 biphenyl Nutrition 0.000 claims 1
- 239000004305 biphenyl Substances 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
- 201000011510 cancer Diseases 0.000 claims 1
- 201000007455 central nervous system cancer Diseases 0.000 claims 1
- 208000025997 central nervous system neoplasm Diseases 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 210000001508 eye Anatomy 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 239000004615 ingredient Substances 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 210000000867 larynx Anatomy 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 210000001165 lymph node Anatomy 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 210000000214 mouth Anatomy 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 210000003739 neck Anatomy 0.000 claims 1
- 210000000653 nervous system Anatomy 0.000 claims 1
- 208000028412 nervous system injury Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 210000000664 rectum Anatomy 0.000 claims 1
- 230000001850 reproductive effect Effects 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- 210000001550 testis Anatomy 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 210000003437 trachea Anatomy 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 210000004291 uterus Anatomy 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/30—Phthalazines
- C07D237/34—Phthalazines with nitrogen atoms directly attached to carbon atoms of the nitrogen-containing ring, e.g. hydrazine radicals
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (12)
1. Spojevi s formulom I
[image]
naznačeni time da
R1 označava H, Hal, CH3, OCH3 ili CH2OH,
X označava Ar ili Cyc,
Ar označava fenil, bifenil ili naftil, od kojih je svaki nesupstituiran ili jednostruko-, dvostruko- ili trostruko supstituiran s Hal, NO2, CN, A, [C(R2)2]pOR2, S(O)mR2, [C(R2)2]pN(R2)2, [C(R2)2]pCOOR2, [C(R2)2]pCON(R2)2, [C(R2)2]pSO2N(R2)2, NR2COR2, NR 2SO2R2 NR2CON(R2)2, NHCOOA, O[C(R2)2]nN(R2)2, CHO i/ili COA,
R2 označava H ili A,
A označava nerazgranati ili razgranati alkil s 1-10 C-atoma, pri čemu dva susjedna ugljikova atoma mogu tvoriti dvostruku vezu i/ili jedna ili dvije ne-susjedne CH- i/ili CH2- skupine mogu biti zamijenjene sa N-, O- i/ili S-atomima i pri čemu 1-7 H-atoma može biti zamijenjeno sa F, Cl i/ili OH,
Cyc označava cikloalkil s 3, 4, 5, 6 ili 7 C-atoma,
Hal označava F, Cl, Br ili I,
m označava 0, 1 ili 2,
n označava 1, 2 ili 3,
p označava 0, 1, 2, 3 ili 4,
i njihove farmaceutski prihvatljive soli, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima.
2. Spojevi prema zahtjevu 1 naznačeni time da
R1 označava H, Hal ili CH3,
i njihovi farmaceutski prihvatljivi solvati, soli, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima.
3. Spojevi prema zahtjevu 1 ili 2 naznačeni time da
Ar označava fenil, koji je nesupstituiran ili jednostruko-, dvostruko- ili trostruko supstituiran s Hal, NO2, CN, A i/ili [C(R2)2]pOR2,
i njihovi farmaceutski prihvatljivi solvati, soli, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima.
4. Spojevi prema jednom ili više od zahtjeva 1-3 naznačeni time da
A označava nerazgranati ili razgranati alkil s 1-6 C-atoma, pri čemu 1-5 H-atoma može biti zamijenjeno sa F,
i njihovi farmaceutski prihvatljivi solvati, soli, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima.
5. Spojevi prema zahtjevu 1, naznačeni time da
R1 označava H, Hal ili CH3,
X označava Ar ili Cyc,
Ar označava fenil, koji je nesupstituiran ili jednostruko-, dvostruko- ili trostruko supstituiran s Hal, NO2, CN, A i/ili [C(R2)2]pOR2,
R2 označava H ili A,
Cyc označava cikloalkil s 3, 4, 5, 6 ili 7 C-atoma,
A označava nerazgranati ili razgranati alkil s 1-6 C-atoma, pri čemu 1-5 H-atoma može biti zamijenjeno sa F,
Hal označava F, Cl, Br ili I,
p označava 0, 1, 2, 3 ili 4,
n označava 1, 2 ili 3,
i njihove farmaceutski prihvatljive soli, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima.
6. Spojevi prema zahtjevu 1, naznačeni time da se biraju iz skupine koju čine
[image]
njihovi farmaceutski prihvatljivi solvati, soli, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima.
7. Postupak za pripravu spojeva s formulom I prema zahtjevima 1-6 i njihovih farmaceutski prihvatljivih soli, solvata, tautomera i stereoizomera, naznačen time da
spoj s formulom II
[image]
u kojoj R1 ima značenja navedena u zahtjevu 1,
reagira
s spojem s formulom III
[image]
u kojoj X i n imaju značenja navedena u zahtjevu 1,
i L označava Cl, Br, I ili slobodnu ili reaktivno funkcionalno modificiranu OH skupinu,
i/ili
baza ili kiselina s formulom I se pretvara u jednu od njihovih soli.
8. Lijekovi naznačeni time da sadrže barem jedan spoj s formulom I prema zahtjevu 1 i/ili njihove farmaceutski prihvatljive soli, solvate, tautomere i stereoizomere, uključujući njihove smjese u svim omjerima, te proizvoljno farmaceutski prihvatljiv nosač, pomoćno sredstvo ili prijenosnik.
9. Spojevi s formulom I prema zahtjevu 1 i njihove farmaceutski prihvatljive soli, solvati, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima, naznačeni time da su za uporabu za liječenje i/ili sprječavanje raka, multiple skleroze, kardiovaskularnih bolesti, ozljede središnjeg živčanog sustava i različitih oblika upala.
10. Spojevi prema zahtjevu 9 naznačeni time da su za uporabu za liječenje i/ili sprječavanje bolesti koje su odabrane iz skupine koju čine rak glave, vrata, oka, usta, grla, jednjaka, dušnika, grkljana, ždrijela, grudi, kosti, pluća, debelog crijeva, rektuma, želuca, prostate, mokraćnog mjehura, maternice, vrata maternice, dojke, jajnika, testisa ili drugih reproduktivnih organa, kože, štitnjače, krvi, limfnih čvorova, bubrega, jetre, gušterače, mozga, središnjeg živčanog sustava, te solidni tumori i tumori nošeni krvlju.
11. Lijekovi naznačeni time da sadrže barem jedan spoj s formulom I prema zahtjevu 1 i/ili njihove farmaceutski prihvatljive soli, solvate i stereoizomere, uključujući njihove smjese u svim omjerima, te barem jedan dodatni aktivni sastojak lijeka.
12. Komplet (kit) naznačen time da sadrži odvojena pakiranja
(a) učinkovite količine spoja s formulom I prema zahtjevu 1 i/ili njihove farmaceutski prihvatljive soli, solvate, soli i stereoizomere, uključujući njihove smjese u svim omjerima, te
(b) učinkovite količine dodatnog aktivnog sastojka lijeka.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP13003205 | 2013-06-24 | ||
PCT/EP2014/001467 WO2014206524A1 (en) | 2013-06-24 | 2014-05-30 | Phthalazine derivatives |
EP14728832.8A EP3013804B1 (en) | 2013-06-24 | 2014-05-30 | Phthalazine derivatives |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20170291T1 true HRP20170291T1 (hr) | 2017-04-21 |
Family
ID=48698872
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20170291TT HRP20170291T1 (hr) | 2013-06-24 | 2017-02-21 | Derivati ftalazina |
Country Status (22)
Country | Link |
---|---|
US (1) | US9751842B2 (hr) |
EP (1) | EP3013804B1 (hr) |
JP (1) | JP6382964B2 (hr) |
KR (1) | KR20160023854A (hr) |
CN (1) | CN105339356B (hr) |
AR (1) | AR096652A1 (hr) |
AU (1) | AU2014301669B2 (hr) |
CA (1) | CA2916557C (hr) |
DK (1) | DK3013804T3 (hr) |
ES (1) | ES2623704T3 (hr) |
HK (1) | HK1221468A1 (hr) |
HR (1) | HRP20170291T1 (hr) |
IL (1) | IL243252A0 (hr) |
LT (1) | LT3013804T (hr) |
MX (1) | MX369393B (hr) |
PL (1) | PL3013804T3 (hr) |
PT (1) | PT3013804T (hr) |
RS (1) | RS55943B1 (hr) |
RU (1) | RU2663623C2 (hr) |
SG (1) | SG11201510584WA (hr) |
SI (1) | SI3013804T1 (hr) |
WO (1) | WO2014206524A1 (hr) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US10722484B2 (en) | 2016-03-09 | 2020-07-28 | K-Gen, Inc. | Methods of cancer treatment |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4466965A (en) | 1982-07-26 | 1984-08-21 | American Hospital Supply Corporation | Phthalazine compounds, compositions and use |
IT1296984B1 (it) | 1997-12-19 | 1999-08-03 | Zambon Spa | Derivati ftalazinici inibitori della fosfodiesterasi 4 |
CA2423279C (en) * | 2000-10-30 | 2011-07-05 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
DE102004023507A1 (de) * | 2004-05-10 | 2005-12-01 | Grünenthal GmbH | Substituierte Cyclohexylessigsäure-Derivate |
BRPI0512902A (pt) | 2004-06-30 | 2008-04-15 | Janssen Pharmaceutica Nv | derivados de ftalazina como inibidores de parp |
CA2593005A1 (en) * | 2005-01-03 | 2006-07-13 | Myriad Genetics Inc. | Pharmaceutical compounds as activators of caspases and inducers of apoptosis and the use thereof |
JP2009286773A (ja) * | 2008-03-14 | 2009-12-10 | Bayer Cropscience Ag | 殺虫性縮環式アリール類 |
-
2014
- 2014-05-30 RU RU2016102057A patent/RU2663623C2/ru not_active IP Right Cessation
- 2014-05-30 SI SI201430206A patent/SI3013804T1/sl unknown
- 2014-05-30 RS RS20170425A patent/RS55943B1/sr unknown
- 2014-05-30 MX MX2015016760A patent/MX369393B/es active IP Right Grant
- 2014-05-30 EP EP14728832.8A patent/EP3013804B1/en active Active
- 2014-05-30 JP JP2016522300A patent/JP6382964B2/ja not_active Expired - Fee Related
- 2014-05-30 CA CA2916557A patent/CA2916557C/en not_active Expired - Fee Related
- 2014-05-30 PL PL14728832T patent/PL3013804T3/pl unknown
- 2014-05-30 KR KR1020167001936A patent/KR20160023854A/ko not_active Application Discontinuation
- 2014-05-30 AU AU2014301669A patent/AU2014301669B2/en not_active Ceased
- 2014-05-30 CN CN201480036171.8A patent/CN105339356B/zh not_active Expired - Fee Related
- 2014-05-30 LT LTEP14728832.8T patent/LT3013804T/lt unknown
- 2014-05-30 ES ES14728832.8T patent/ES2623704T3/es active Active
- 2014-05-30 DK DK14728832.8T patent/DK3013804T3/en active
- 2014-05-30 SG SG11201510584WA patent/SG11201510584WA/en unknown
- 2014-05-30 PT PT147288328T patent/PT3013804T/pt unknown
- 2014-05-30 WO PCT/EP2014/001467 patent/WO2014206524A1/en active Application Filing
- 2014-05-30 US US14/392,145 patent/US9751842B2/en active Active
- 2014-06-19 AR ARP140102314A patent/AR096652A1/es unknown
-
2015
- 2015-12-21 IL IL243252A patent/IL243252A0/en active IP Right Grant
-
2016
- 2016-08-12 HK HK16109622.9A patent/HK1221468A1/zh not_active IP Right Cessation
-
2017
- 2017-02-21 HR HRP20170291TT patent/HRP20170291T1/hr unknown
Also Published As
Publication number | Publication date |
---|---|
AU2014301669A1 (en) | 2016-02-11 |
RU2016102057A3 (hr) | 2018-03-16 |
CN105339356A (zh) | 2016-02-17 |
HK1221468A1 (zh) | 2017-06-02 |
EP3013804A1 (en) | 2016-05-04 |
AU2014301669B2 (en) | 2018-03-01 |
CN105339356B (zh) | 2018-10-19 |
JP2016523272A (ja) | 2016-08-08 |
ES2623704T3 (es) | 2017-07-12 |
MX369393B (es) | 2019-11-07 |
RS55943B1 (sr) | 2017-09-29 |
US20160318876A1 (en) | 2016-11-03 |
WO2014206524A1 (en) | 2014-12-31 |
LT3013804T (lt) | 2017-04-10 |
CA2916557C (en) | 2021-08-03 |
DK3013804T3 (en) | 2017-04-10 |
RU2663623C2 (ru) | 2018-08-07 |
RU2016102057A (ru) | 2017-07-28 |
CA2916557A1 (en) | 2014-12-31 |
JP6382964B2 (ja) | 2018-08-29 |
SG11201510584WA (en) | 2016-01-28 |
US9751842B2 (en) | 2017-09-05 |
PT3013804T (pt) | 2017-05-08 |
IL243252A0 (en) | 2016-02-29 |
KR20160023854A (ko) | 2016-03-03 |
MX2015016760A (es) | 2016-04-13 |
SI3013804T1 (sl) | 2017-05-31 |
EP3013804B1 (en) | 2017-02-01 |
AR096652A1 (es) | 2016-01-27 |
PL3013804T3 (pl) | 2017-08-31 |
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