UA76512C2 - Dihydropteridinones, a method for producing thereof and use thereof as medicament - Google Patents

Dihydropteridinones, a method for producing thereof and use thereof as medicament Download PDF

Info

Publication number: UA76512C2
Authority: UA; Ukraine
Prior art keywords: group; hydrogen; optionally substituted; compound; residue selected
Prior art date: 2001-09-04

Application number

UA2004042514A

Other languages

English (en)

Ukrainian (uk)

Inventor

Juergen Quant

Original Assignee

Boehringer Ingelheim Pharma

Priority date (The priority date 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 date listed.)

2001-09-04

Filing date

2002-08-30

Publication date

2006-08-15

2002-08-30 Application filed by Boehringer Ingelheim Pharma filed Critical Boehringer Ingelheim Pharma

2006-08-15 Publication of UA76512C2 publication Critical patent/UA76512C2/uk

Links

239000003814 drug Substances 0.000 title abstract description 6
238000004519 manufacturing process Methods 0.000 title abstract description 3
150000001875 compounds Chemical class 0.000 claims description 100
239000001257 hydrogen Substances 0.000 claims description 51
229910052739 hydrogen Inorganic materials 0.000 claims description 51
239000000203 mixture Substances 0.000 claims description 47
-1 substituted Chemical class 0.000 claims description 34
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 29
239000013543 active substance Substances 0.000 claims description 28
125000000217 alkyl group Chemical group 0.000 claims description 25
125000001072 heteroaryl group Chemical group 0.000 claims description 20
150000002431 hydrogen Chemical group 0.000 claims description 19
238000000034 method Methods 0.000 claims description 19
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 19
150000003839 salts Chemical class 0.000 claims description 18
229910052736 halogen Inorganic materials 0.000 claims description 17
150000002367 halogens Chemical class 0.000 claims description 16
125000003118 aryl group Chemical group 0.000 claims description 14
239000002253 acid Substances 0.000 claims description 13
229920006395 saturated elastomer Polymers 0.000 claims description 12
125000000753 cycloalkyl group Chemical group 0.000 claims description 11
125000005842 heteroatom Chemical group 0.000 claims description 11
125000003342 alkenyl group Chemical group 0.000 claims description 10
HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 9
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125000003107 substituted aryl group Chemical group 0.000 claims description 6
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SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 1
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239000011737 fluorine Substances 0.000 description 15
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GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 8
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NGNBDVOYPDDBFK-UHFFFAOYSA-N 2-[2,4-di(pentan-2-yl)phenoxy]acetyl chloride Chemical compound CCCC(C)C1=CC=C(OCC(Cl)=O)C(C(C)CCC)=C1 NGNBDVOYPDDBFK-UHFFFAOYSA-N 0.000 description 7
125000000304 alkynyl group Chemical group 0.000 description 7
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210000004881 tumor cell Anatomy 0.000 description 7
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WGQKYBSKWIADBV-UHFFFAOYSA-N benzylamine Chemical compound NCC1=CC=CC=C1 WGQKYBSKWIADBV-UHFFFAOYSA-N 0.000 description 6
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208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 6
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XJMOSONTPMZWPB-UHFFFAOYSA-M propidium iodide Chemical compound [I-].[I-].C12=CC(N)=CC=C2C2=CC=C(N)C=C2[N+](CCC[N+](C)(CC)CC)=C1C1=CC=CC=C1 XJMOSONTPMZWPB-UHFFFAOYSA-M 0.000 description 6
239000000126 substance Substances 0.000 description 6
HXJUTPCZVOIRIF-UHFFFAOYSA-N sulfolane Chemical compound O=S1(=O)CCCC1 HXJUTPCZVOIRIF-UHFFFAOYSA-N 0.000 description 6
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125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 5
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239000003381 stabilizer Substances 0.000 description 1
230000000087 stabilizing effect Effects 0.000 description 1
238000010186 staining Methods 0.000 description 1
239000001119 stannous chloride Substances 0.000 description 1
235000011150 stannous chloride Nutrition 0.000 description 1
239000008117 stearic acid Substances 0.000 description 1
210000000130 stem cell Anatomy 0.000 description 1
238000007920 subcutaneous administration Methods 0.000 description 1
238000006467 substitution reaction Methods 0.000 description 1
150000008163 sugars Chemical class 0.000 description 1
239000006228 supernatant Substances 0.000 description 1
239000003765 sweetening agent Substances 0.000 description 1
238000001308 synthesis method Methods 0.000 description 1
239000003826 tablet Substances 0.000 description 1
238000003419 tautomerization reaction Methods 0.000 description 1
RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 description 1
125000000383 tetramethylene group Chemical group [H]C([H])([*:1])C([H])([H])C([H])([H])C([H])([H])[*:2] 0.000 description 1
150000003536 tetrazoles Chemical class 0.000 description 1
238000002560 therapeutic procedure Methods 0.000 description 1
VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical compound C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 description 1
239000002562 thickening agent Substances 0.000 description 1
229930192474 thiophene Natural products 0.000 description 1
239000011135 tin Substances 0.000 description 1
229910052718 tin Inorganic materials 0.000 description 1
239000010936 titanium Substances 0.000 description 1
229910052719 titanium Inorganic materials 0.000 description 1
230000007704 transition Effects 0.000 description 1
150000003852 triazoles Chemical class 0.000 description 1
QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 description 1
239000012588 trypsin Substances 0.000 description 1
229910052720 vanadium Inorganic materials 0.000 description 1
235000012141 vanillin Nutrition 0.000 description 1
MWOOGOJBHIARFG-UHFFFAOYSA-N vanillin Chemical compound COC1=CC(C=O)=CC=C1O MWOOGOJBHIARFG-UHFFFAOYSA-N 0.000 description 1
FGQOOHJZONJGDT-UHFFFAOYSA-N vanillin Natural products COC1=CC(O)=CC(C=O)=C1 FGQOOHJZONJGDT-UHFFFAOYSA-N 0.000 description 1
235000013311 vegetables Nutrition 0.000 description 1
210000003462 vein Anatomy 0.000 description 1
229960003048 vinblastine Drugs 0.000 description 1
JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 description 1
OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 description 1
229960004528 vincristine Drugs 0.000 description 1
OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 description 1
230000009385 viral infection Effects 0.000 description 1
230000003612 virological effect Effects 0.000 description 1
239000008215 water for injection Substances 0.000 description 1
239000000080 wetting agent Substances 0.000 description 1
230000029663 wound healing Effects 0.000 description 1
239000011701 zinc Substances 0.000 description 1
229910052725 zinc Inorganic materials 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- 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

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
General Health & Medical Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
Animal Behavior & Ethology (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Immunology (AREA)
Virology (AREA)
Oncology (AREA)
Communicable Diseases (AREA)
AIDS & HIV (AREA)
Molecular Biology (AREA)
Tropical Medicine & Parasitology (AREA)
Transplantation (AREA)
Pain & Pain Management (AREA)
Rheumatology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Plural Heterocyclic Compounds (AREA)
Hydrogenated Pyridines (AREA)

UA2004042514A 2001-09-04 2002-08-30 Dihydropteridinones, a method for producing thereof and use thereof as medicament UA76512C2 (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
DE10143272		2001-09-04
PCT/EP2002/009728 WO2003020722A1 (de)	2001-09-04	2002-08-30	Neue dihydropteridinone, verfahren zu deren herstellung und deren verwendung als arzneimittel

Publications (1)

Publication Number	Publication Date
UA76512C2 true UA76512C2 (en)	2006-08-15

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UA2004042514A UA76512C2 (en)	2001-09-04	2002-08-30	Dihydropteridinones, a method for producing thereof and use thereof as medicament

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EP (1)	EP1427730B1 (pt)
JP (1)	JP3876254B2 (pt)
KR (1)	KR100955589B1 (pt)
CN (1)	CN1551881A (pt)
AR (1)	AR036586A1 (pt)
AT (1)	ATE332898T1 (pt)
AU (1)	AU2002337047B2 (pt)
BR (1)	BRPI0212137A2 (pt)
CA (1)	CA2458699C (pt)
CO (1)	CO5560575A2 (pt)
CY (1)	CY1105337T1 (pt)
DE (1)	DE50207522D1 (pt)
DK (1)	DK1427730T3 (pt)
EA (1)	EA007062B1 (pt)
EC (1)	ECSP045003A (pt)
ES (1)	ES2268093T3 (pt)
HR (1)	HRP20040213A2 (pt)
HU (1)	HUP0401293A3 (pt)
IL (2)	IL160440A0 (pt)
MX (1)	MXPA04002067A (pt)
MY (1)	MY129751A (pt)
NO (1)	NO328804B1 (pt)
NZ (1)	NZ531928A (pt)
PL (1)	PL369740A1 (pt)
PT (1)	PT1427730E (pt)
RS (1)	RS51012B (pt)
UA (1)	UA76512C2 (pt)
UY (1)	UY27427A1 (pt)
WO (1)	WO2003020722A1 (pt)
ZA (1)	ZA200401365B (pt)

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AU2002337047B2 (en)	2008-01-10
ES2268093T3 (es)	2007-03-16
BRPI0212137A2 (pt)	2016-06-28
NO328804B1 (no)	2010-05-18
CO5560575A2 (es)	2005-09-30
MY129751A (en)	2007-04-30
ZA200401365B (en)	2005-05-27
ECSP045003A (es)	2004-04-28
CY1105337T1 (el)	2010-03-03
DE50207522D1 (de)	2006-08-24
PL369740A1 (en)	2005-05-02
DK1427730T3 (da)	2006-11-06
CA2458699A1 (en)	2003-03-13
UY27427A1 (es)	2003-03-31
NO20040680D0 (no)	2004-02-16
ATE332898T1 (de)	2006-08-15
MXPA04002067A (es)	2004-06-07
KR100955589B1 (ko)	2010-04-30
PT1427730E (pt)	2006-11-30
AU2002337047B8 (en)	2003-03-18
KR20040029465A (ko)	2004-04-06
JP3876254B2 (ja)	2007-01-31
HRP20040213A2 (en)	2005-02-28
NZ531928A (en)	2005-10-28
HUP0401293A3 (en)	2008-03-28
EP1427730B1 (de)	2006-07-12
WO2003020722A1 (de)	2003-03-13
NO20040680L (no)	2004-02-16
JP2005501904A (ja)	2005-01-20
HUP0401293A2 (hu)	2004-10-28
CA2458699C (en)	2010-10-19
IL160440A (en)	2009-09-01
YU27304A (sh)	2006-08-17
RS51012B (sr)	2010-10-31
EP1427730A1 (de)	2004-06-16
EA200400368A1 (ru)	2004-12-30
EA007062B1 (ru)	2006-06-30
CN1551881A (zh)	2004-12-01
AR036586A1 (es)	2004-09-22
IL160440A0 (en)	2004-07-25

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