SK8192003A3 - Pharmaceutical formulation containing pyrazolo[4,3-d]pyrimidines and antithrombotic agents, calcium-antagonists, prostaglandins or prostaglandin derivatives - Google Patents

Pharmaceutical formulation containing pyrazolo[4,3-d]pyrimidines and antithrombotic agents, calcium-antagonists, prostaglandins or prostaglandin derivatives Download PDF

Info

Publication number: SK8192003A3
Authority: SK; Slovakia
Prior art keywords: group; pharmaceutical composition; methyl; pyrazolo; propyl
Prior art date: 2000-12-19

Application number

SK819-2003A

Other languages

English (en)

Slovak (sk)

Inventor

Hans-Michael Eggenweiler

Volker Eiermann

Original Assignee

Merck Patent Gmbh

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.)

2000-12-19

Filing date

2001-11-28

Publication date

2003-10-07

2000-12-19 Priority claimed from DE10063224A external-priority patent/DE10063224A1/de

2000-12-21 Priority claimed from DE2000163882 external-priority patent/DE10063882A1/de

2000-12-23 Priority claimed from DE2000164993 external-priority patent/DE10064993A1/de

2001-11-28 Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh

2003-10-07 Publication of SK8192003A3 publication Critical patent/SK8192003A3/sk

Links

150000003180 prostaglandins Chemical class 0.000 title claims abstract description 73
229940127291 Calcium channel antagonist Drugs 0.000 title claims abstract description 42
239000003146 anticoagulant agent Chemical class 0.000 title claims abstract description 33
229960004676 antithrombotic agent Drugs 0.000 title claims abstract description 9
-1 calcium-antagonists Chemical class 0.000 title claims description 113
239000008194 pharmaceutical composition Substances 0.000 title claims description 59
229940094443 oxytocics prostaglandins Drugs 0.000 title description 5
APXRHPDHORGIEB-UHFFFAOYSA-N 1H-pyrazolo[4,3-d]pyrimidine Chemical class N1=CN=C2C=NNC2=C1 APXRHPDHORGIEB-UHFFFAOYSA-N 0.000 title description 2
150000001875 compounds Chemical group 0.000 claims abstract description 105
150000003839 salts Chemical class 0.000 claims abstract description 63
239000012453 solvate Substances 0.000 claims abstract description 48
239000000480 calcium channel blocker Substances 0.000 claims abstract description 32
239000003814 drug Substances 0.000 claims abstract description 14
206010019280 Heart failures Diseases 0.000 claims abstract description 13
206010007559 Cardiac failure congestive Diseases 0.000 claims abstract description 11
208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims abstract description 9
206010039163 Right ventricular failure Diseases 0.000 claims abstract description 9
208000002815 pulmonary hypertension Diseases 0.000 claims abstract description 7
208000023819 chronic asthma Diseases 0.000 claims abstract description 6
206010002383 Angina Pectoris Diseases 0.000 claims abstract description 5
206010028980 Neoplasm Diseases 0.000 claims abstract description 5
208000018262 Peripheral vascular disease Diseases 0.000 claims abstract description 5
208000001647 Renal Insufficiency Diseases 0.000 claims abstract description 5
208000019425 cirrhosis of liver Diseases 0.000 claims abstract description 5
208000002551 irritable bowel syndrome Diseases 0.000 claims abstract description 5
201000006370 kidney failure Diseases 0.000 claims abstract description 5
201000001320 Atherosclerosis Diseases 0.000 claims abstract description 4
208000010412 Glaucoma Diseases 0.000 claims abstract description 4
206010020772 Hypertension Diseases 0.000 claims abstract description 4
201000009961 allergic asthma Diseases 0.000 claims abstract description 4
208000006673 asthma Diseases 0.000 claims abstract description 4
206010006451 bronchitis Diseases 0.000 claims abstract description 4
206010039085 Rhinitis allergic Diseases 0.000 claims abstract description 3
201000010105 allergic rhinitis Diseases 0.000 claims abstract description 3
206010016654 Fibrosis Diseases 0.000 claims abstract 2
230000007882 cirrhosis Effects 0.000 claims abstract 2
210000004185 liver Anatomy 0.000 claims abstract 2
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 64
125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims description 62
GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical compound BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims description 50
125000000896 monocarboxylic acid group Chemical group 0.000 claims description 50
125000004432 carbon atom Chemical group C* 0.000 claims description 48
125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 42
239000000460 chlorine Substances 0.000 claims description 40
229910052760 oxygen Inorganic materials 0.000 claims description 39
229910052801 chlorine Inorganic materials 0.000 claims description 37
229910052731 fluorine Inorganic materials 0.000 claims description 35
229910052794 bromium Inorganic materials 0.000 claims description 32
229910052717 sulfur Inorganic materials 0.000 claims description 31
PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 29
230000002785 anti-thrombosis Effects 0.000 claims description 29
239000011737 fluorine Substances 0.000 claims description 29
125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 26
125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims description 25
239000001301 oxygen Substances 0.000 claims description 25
125000002947 alkylene group Chemical group 0.000 claims description 24
125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 24
125000000217 alkyl group Chemical group 0.000 claims description 23
229910052740 iodine Inorganic materials 0.000 claims description 23
125000004434 sulfur atom Chemical group 0.000 claims description 23
ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical group [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims description 22
229910052739 hydrogen Inorganic materials 0.000 claims description 22
QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 20
KZBUYRJDOAKODT-UHFFFAOYSA-N Chlorine Chemical compound ClCl KZBUYRJDOAKODT-UHFFFAOYSA-N 0.000 claims description 20
229910052799 carbon Inorganic materials 0.000 claims description 19
NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical compound CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 claims description 19
QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 18
FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Chemical compound CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 claims description 17
125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 16
125000000753 cycloalkyl group Chemical group 0.000 claims description 14
LIFZVJKHTQXNLW-UHFFFAOYSA-N 2-[[7-[(3-chloro-4-methoxyphenyl)methylamino]-1-methyl-3-propylpyrazolo[4,3-d]pyrimidin-5-yl]methoxy]acetic acid Chemical compound N1=C(COCC(O)=O)N=C2C(CCC)=NN(C)C2=C1NCC1=CC=C(OC)C(Cl)=C1 LIFZVJKHTQXNLW-UHFFFAOYSA-N 0.000 claims description 12
150000002169 ethanolamines Chemical class 0.000 claims description 12
239000001257 hydrogen Substances 0.000 claims description 12
125000004429 atom Chemical group 0.000 claims description 11
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HTTJABKRGRZYRN-UHFFFAOYSA-N Heparin Chemical class OC1C(NC(=O)C)C(O)OC(COS(O)(=O)=O)C1OC1C(OS(O)(=O)=O)C(O)C(OC2C(C(OS(O)(=O)=O)C(OC3C(C(O)C(O)C(O3)C(O)=O)OS(O)(=O)=O)C(CO)O2)NS(O)(=O)=O)C(C(O)=O)O1 HTTJABKRGRZYRN-UHFFFAOYSA-N 0.000 claims description 9
MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims description 8
206010020880 Hypertrophy Diseases 0.000 claims description 8
208000019693 Lung disease Diseases 0.000 claims description 8
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KAQKFAOMNZTLHT-VVUHWYTRSA-N epoprostenol Chemical compound O1C(=CCCCC(O)=O)C[C@@H]2[C@@H](/C=C/[C@@H](O)CCCCC)[C@H](O)C[C@@H]21 KAQKFAOMNZTLHT-VVUHWYTRSA-N 0.000 claims description 8
238000004519 manufacturing process Methods 0.000 claims description 7
239000005711 Benzoic acid Substances 0.000 claims description 6
WPYMKLBDIGXBTP-UHFFFAOYSA-N Benzoic acid Natural products OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims description 6
NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 6
235000010233 benzoic acid Nutrition 0.000 claims description 6
230000000747 cardiac effect Effects 0.000 claims description 6
HZAXFHJVJLSVMW-UHFFFAOYSA-N monoethanolamine hydrochloride Natural products NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 claims description 6
239000000546 pharmaceutical excipient Substances 0.000 claims description 6
GMVPRGQOIOIIMI-DWKJAMRDSA-N prostaglandin E1 Chemical compound CCCCC[C@H](O)\C=C\[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(O)=O GMVPRGQOIOIIMI-DWKJAMRDSA-N 0.000 claims description 6
239000011593 sulfur Substances 0.000 claims description 6
102000004190 Enzymes Human genes 0.000 claims description 5
108090000790 Enzymes Proteins 0.000 claims description 5
125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 5
229960001342 dinoprost Drugs 0.000 claims description 5
229940088598 enzyme Drugs 0.000 claims description 5
239000002590 phosphodiesterase V inhibitor Substances 0.000 claims description 5
PXGPLTODNUVGFL-YNNPMVKQSA-N prostaglandin F2alpha Chemical compound CCCCC[C@H](O)\C=C\[C@H]1[C@H](O)C[C@H](O)[C@@H]1C\C=C/CCCC(O)=O PXGPLTODNUVGFL-YNNPMVKQSA-N 0.000 claims description 5
GMVPRGQOIOIIMI-UHFFFAOYSA-N (8R,11R,12R,13E,15S)-11,15-Dihydroxy-9-oxo-13-prostenoic acid Natural products CCCCCC(O)C=CC1C(O)CC(=O)C1CCCCCCC(O)=O GMVPRGQOIOIIMI-UHFFFAOYSA-N 0.000 claims description 4
OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 4
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150000007657 benzothiazepines Chemical class 0.000 claims description 4
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FYBFDIIAPRHIQS-KKBLUXBBSA-N (Z)-7-[(1R,2R,3R,5S)-3,5-dihydroxy-2-[(E,3R)-3-hydroxy-4-thiophen-3-yloxybut-1-enyl]cyclopentyl]hept-5-enoic acid Chemical compound C([C@H](O)\C=C\[C@@H]1[C@H]([C@@H](O)C[C@H]1O)C\C=C/CCCC(O)=O)OC=1C=CSC=1 FYBFDIIAPRHIQS-KKBLUXBBSA-N 0.000 claims description 3
OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 3
239000005557 antagonist Substances 0.000 claims description 3
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229910052791 calcium Inorganic materials 0.000 claims description 3
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XEYBRNLFEZDVAW-ARSRFYASSA-N dinoprostone Chemical compound CCCCC[C@H](O)\C=C\[C@H]1[C@H](O)CC(=O)[C@@H]1C\C=C/CCCC(O)=O XEYBRNLFEZDVAW-ARSRFYASSA-N 0.000 claims description 3
229960001160 latanoprost Drugs 0.000 claims description 3
GGXICVAJURFBLW-CEYXHVGTSA-N latanoprost Chemical compound CC(C)OC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)CCC1=CC=CC=C1 GGXICVAJURFBLW-CEYXHVGTSA-N 0.000 claims description 3
XEYBRNLFEZDVAW-UHFFFAOYSA-N prostaglandin E2 Natural products CCCCCC(O)C=CC1C(O)CC(=O)C1CC=CCCCC(O)=O XEYBRNLFEZDVAW-UHFFFAOYSA-N 0.000 claims description 3
229940085239 selective calcium channel blockers with direct cardiac effects phenylalkylamine derivative Drugs 0.000 claims description 3
229950002099 tiaprost Drugs 0.000 claims description 3
HMJIYCCIJYRONP-UHFFFAOYSA-N (+-)-Isradipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OC(C)C)C1C1=CC=CC2=NON=C12 HMJIYCCIJYRONP-UHFFFAOYSA-N 0.000 claims description 2
PVHUJELLJLJGLN-INIZCTEOSA-N (S)-nitrendipine Chemical compound CCOC(=O)C1=C(C)NC(C)=C(C(=O)OC)[C@@H]1C1=CC=CC([N+]([O-])=O)=C1 PVHUJELLJLJGLN-INIZCTEOSA-N 0.000 claims description 2
SGTNSNPWRIOYBX-UHFFFAOYSA-N 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile Chemical compound C1=C(OC)C(OC)=CC=C1CCN(C)CCCC(C#N)(C(C)C)C1=CC=C(OC)C(OC)=C1 SGTNSNPWRIOYBX-UHFFFAOYSA-N 0.000 claims description 2
ZBIAKUMOEKILTF-UHFFFAOYSA-N 2-[4-[4,4-bis(4-fluorophenyl)butyl]-1-piperazinyl]-N-(2,6-dimethylphenyl)acetamide Chemical compound CC1=CC=CC(C)=C1NC(=O)CN1CCN(CCCC(C=2C=CC(F)=CC=2)C=2C=CC(F)=CC=2)CC1 ZBIAKUMOEKILTF-UHFFFAOYSA-N 0.000 claims description 2
NMKSAYKQLCHXDK-UHFFFAOYSA-N 3,3-diphenyl-N-(1-phenylethyl)-1-propanamine Chemical compound C=1C=CC=CC=1C(C)NCCC(C=1C=CC=CC=1)C1=CC=CC=C1 NMKSAYKQLCHXDK-UHFFFAOYSA-N 0.000 claims description 2
UIAGMCDKSXEBJQ-IBGZPJMESA-N 3-o-(2-methoxyethyl) 5-o-propan-2-yl (4s)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate Chemical compound COCCOC(=O)C1=C(C)NC(C)=C(C(=O)OC(C)C)[C@H]1C1=CC=CC([N+]([O-])=O)=C1 UIAGMCDKSXEBJQ-IBGZPJMESA-N 0.000 claims description 2
FSROZMKGWKKLCJ-UHFFFAOYSA-N 4-[7-(1,3-benzodioxol-5-ylmethylamino)-1-methyl-3-propylpyrazolo[4,3-d]pyrimidin-5-yl]butanoic acid Chemical compound C1=C2OCOC2=CC(CNC2=C3N(C)N=C(C3=NC(CCCC(O)=O)=N2)CCC)=C1 FSROZMKGWKKLCJ-UHFFFAOYSA-N 0.000 claims description 2
RZTAMFZIAATZDJ-HNNXBMFYSA-N 5-o-ethyl 3-o-methyl (4s)-4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate Chemical compound CCOC(=O)C1=C(C)NC(C)=C(C(=O)OC)[C@@H]1C1=CC=CC(Cl)=C1Cl RZTAMFZIAATZDJ-HNNXBMFYSA-N 0.000 claims description 2
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JYGLAHSAISAEAL-UHFFFAOYSA-N Diphenadione Chemical compound O=C1C2=CC=CC=C2C(=O)C1C(=O)C(C=1C=CC=CC=1)C1=CC=CC=C1 JYGLAHSAISAEAL-UHFFFAOYSA-N 0.000 claims description 2
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XQLWNAFCTODIRK-UHFFFAOYSA-N Gallopamil Chemical compound C1=C(OC)C(OC)=CC=C1CCN(C)CCCC(C#N)(C(C)C)C1=CC(OC)=C(OC)C(OC)=C1 XQLWNAFCTODIRK-UHFFFAOYSA-N 0.000 claims description 2
HBNPJJILLOYFJU-VMPREFPWSA-N Mibefradil Chemical group C1CC2=CC(F)=CC=C2[C@H](C(C)C)[C@@]1(OC(=O)COC)CCN(C)CCCC1=NC2=CC=CC=C2N1 HBNPJJILLOYFJU-VMPREFPWSA-N 0.000 claims description 2
ZBBHBTPTTSWHBA-UHFFFAOYSA-N Nicardipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OCCN(C)CC=2C=CC=CC=2)C1C1=CC=CC([N+]([O-])=O)=C1 ZBBHBTPTTSWHBA-UHFFFAOYSA-N 0.000 claims description 2
FAIIFDPAEUKBEP-UHFFFAOYSA-N Nilvadipine Chemical compound COC(=O)C1=C(C#N)NC(C)=C(C(=O)OC(C)C)C1C1=CC=CC([N+]([O-])=O)=C1 FAIIFDPAEUKBEP-UHFFFAOYSA-N 0.000 claims description 2
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108010010336 Platelet Membrane Glycoproteins Proteins 0.000 claims description 2
108010023197 Streptokinase Proteins 0.000 claims description 2
108090000373 Tissue Plasminogen Activator Proteins 0.000 claims description 2
102000003978 Tissue Plasminogen Activator Human genes 0.000 claims description 2
108090000435 Urokinase-type plasminogen activator Proteins 0.000 claims description 2
102000003990 Urokinase-type plasminogen activator Human genes 0.000 claims description 2
JNWFIPVDEINBAI-UHFFFAOYSA-N [5-hydroxy-4-[4-(1-methylindol-5-yl)-5-oxo-1H-1,2,4-triazol-3-yl]-2-propan-2-ylphenyl] dihydrogen phosphate Chemical compound C1=C(OP(O)(O)=O)C(C(C)C)=CC(C=2N(C(=O)NN=2)C=2C=C3C=CN(C)C3=CC=2)=C1O JNWFIPVDEINBAI-UHFFFAOYSA-N 0.000 claims description 2
229960002054 acenocoumarol Drugs 0.000 claims description 2
VABCILAOYCMVPS-UHFFFAOYSA-N acenocoumarol Chemical compound OC=1C2=CC=CC=C2OC(=O)C=1C(CC(=O)C)C1=CC=C([N+]([O-])=O)C=C1 VABCILAOYCMVPS-UHFFFAOYSA-N 0.000 claims description 2
229960003318 alteplase Drugs 0.000 claims description 2
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HTIQEAQVCYTUBX-UHFFFAOYSA-N amlodipine Chemical compound CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1Cl HTIQEAQVCYTUBX-UHFFFAOYSA-N 0.000 claims description 2
229960000983 anistreplase Drugs 0.000 claims description 2
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VXMOONUMYLCFJD-DHLKQENFSA-N barnidipine Chemical compound C1([C@@H]2C(=C(C)NC(C)=C2C(=O)OC)C(=O)O[C@@H]2CN(CC=3C=CC=CC=3)CC2)=CC=CC([N+]([O-])=O)=C1 VXMOONUMYLCFJD-DHLKQENFSA-N 0.000 claims description 2
229940085242 benzothiazepine derivative selective calcium channel blockers with direct cardiac effects Drugs 0.000 claims description 2
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UIEATEWHFDRYRU-UHFFFAOYSA-N bepridil Chemical compound C1CCCN1C(COCC(C)C)CN(C=1C=CC=CC=1)CC1=CC=CC=C1 UIEATEWHFDRYRU-UHFFFAOYSA-N 0.000 claims description 2
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GKTWGGQPFAXNFI-HNNXBMFYSA-N clopidogrel Chemical compound C1([C@H](N2CC=3C=CSC=3CC2)C(=O)OC)=CC=CC=C1Cl GKTWGGQPFAXNFI-HNNXBMFYSA-N 0.000 claims description 2
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HSUGRBWQSSZJOP-RTWAWAEBSA-N diltiazem Chemical group C1=CC(OC)=CC=C1[C@H]1[C@@H](OC(C)=O)C(=O)N(CCN(C)C)C2=CC=CC=C2S1 HSUGRBWQSSZJOP-RTWAWAEBSA-N 0.000 claims description 2
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229960000267 diphenadione Drugs 0.000 claims description 2
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- 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
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- A—HUMAN NECESSITIES
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- 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
- A61P37/08—Antiallergic agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- 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
- A61P9/08—Vasodilators for multiple indications
- 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
- 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
- A61P9/12—Antihypertensives

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Health & Medical Sciences (AREA)
Veterinary Medicine (AREA)
Pharmacology & Pharmacy (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Animal Behavior & Ethology (AREA)
Life Sciences & Earth Sciences (AREA)
Medicinal Chemistry (AREA)
Chemical Kinetics & Catalysis (AREA)
Organic Chemistry (AREA)
General Chemical & Material Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Engineering & Computer Science (AREA)
Epidemiology (AREA)
Pulmonology (AREA)
Cardiology (AREA)
Heart & Thoracic Surgery (AREA)
Ophthalmology & Optometry (AREA)
Urology & Nephrology (AREA)
Otolaryngology (AREA)
Hospice & Palliative Care (AREA)
Vascular Medicine (AREA)
Gastroenterology & Hepatology (AREA)
Immunology (AREA)
Toxicology (AREA)
Gynecology & Obstetrics (AREA)
Endocrinology (AREA)
Reproductive Health (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

SK819-2003A 2000-12-19 2001-11-28 Pharmaceutical formulation containing pyrazolo[4,3-d]pyrimidines and antithrombotic agents, calcium-antagonists, prostaglandins or prostaglandin derivatives SK8192003A3 (en)

Applications Claiming Priority (4)

Application Number	Priority Date	Filing Date	Title
DE10063224A DE10063224A1 (de)	2000-12-19	2000-12-19	Pharmazeutische Formulierung enthaltend Pyrazolo(4,3-d)pyrimidine und Antithrombotica
DE2000163882 DE10063882A1 (de)	2000-12-21	2000-12-21	Pharmazeutische Formulierung enthaltend Pyrazolo[4,3-d]pyrimidine und Calcium-Antagonisten
DE2000164993 DE10064993A1 (de)	2000-12-23	2000-12-23	Pharmazeutische Formulierung enthaltend Pyrazolo[4,3-d]pyrimidine und Prostaglandine oder Prostaglandinderivate
PCT/EP2001/013916 WO2002049651A1 (de)	2000-12-19	2001-11-28	Pharmazeutische formulierung enthaltend pyrazolo[4,3-d]pyrimidine und antithrombotica, calcium-antagonisten, prostaglandine oder prostaglandinderivate

Publications (1)

Publication Number	Publication Date
SK8192003A3 true SK8192003A3 (en)	2003-10-07

Family

ID=27214208

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
SK819-2003A SK8192003A3 (en)	2000-12-19	2001-11-28	Pharmaceutical formulation containing pyrazolo[4,3-d]pyrimidines and antithrombotic agents, calcium-antagonists, prostaglandins or prostaglandin derivatives

Country Status (16)

Country	Link
US (1)	US20040063730A1 (cs)
EP (1)	EP1343506A1 (cs)
JP (1)	JP2004516270A (cs)
KR (1)	KR20030059349A (cs)
CN (1)	CN1481244A (cs)
AR (1)	AR035676A1 (cs)
AU (1)	AU2002229573A1 (cs)
BR (1)	BR0115995A (cs)
CA (1)	CA2431077A1 (cs)
CZ (1)	CZ20031776A3 (cs)
HU (1)	HUP0303315A2 (cs)
MX (1)	MXPA03005393A (cs)
NO (1)	NO20032773D0 (cs)
PL (1)	PL362513A1 (cs)
SK (1)	SK8192003A3 (cs)
WO (1)	WO2002049651A1 (cs)

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ATE478872T1 (de) *	2002-03-28	2010-09-15	Ustav Ex Botan Av Cr V V I I O	Pyrazoloä4,3-düpyrimidine, verfahren zu ihrer herstellung und therapeutische anwendung
DE10229778A1 (de) *	2002-07-03	2004-01-29	Bayer Ag	Neue Verwendung von Imidazotriazinonen
FR2842809A1 (fr) *	2002-07-26	2004-01-30	Greenpharma Sas	NOUVELLES PYRAZOLO[1,5-a]-1,3,5-TRIAZINES SUBSTITUEES ET LEURS ANALOGUES, COMPOSITIONS PHARMACEUTIQUES LES CONTENANT, UTILISATION A TITRE DE MEDICAMENT ET PROCEDES POUR LEUR PREPARATION
KR100468352B1 (ko) *	2002-09-24	2005-01-27	한국과학기술연구원	신규 피라졸로피리미딘계 유도체, 그의 제조방법 및 이를 유효성분으로 하는 약학적 조성물
OA13050A (en)	2003-04-29	2006-11-10	Pfizer Ltd	5,7-diaminopyrazolo [4,3-D] pyrimidines useful in the treatment of hypertension.
EP1628663B1 (en) *	2003-05-15	2009-07-29	Roskamp Research llc	Method for producing medicaments for reducing amyloid deposition, amyloid neurotoxicity and microgliosis
US7572799B2 (en)	2003-11-24	2009-08-11	Pfizer Inc	Pyrazolo[4,3-d]pyrimidines as Phosphodiesterase Inhibitors
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CA2681582C (en) *	2007-03-30	2015-07-14	Amgen Inc.	Methods of treating bowel disorders
US20100093810A1 (en) *	2007-10-05	2010-04-15	Alzheimer's Institute Of America, Inc.	Pharmaceutical Compositions for Reducing Amyloid Deposition, Amyloid Neurotoxicity, and Microgliosis
NZ584729A (en) *	2007-10-05	2012-12-21	Alzheimer S Inst Of America Inc	Method for reducing amyloid deposition, amyloid neurotoxicity, and microgliosis with (-)-nilvadipine enantiomer
JP5764061B2 (ja) *	2008-08-13	2015-08-12	アクテリオンファーマシューティカルズリミテッドＡｃｔｅｌｉｏｎＰｈａｒｍａｃｅｕｔｉｃａｌｓＬｔｄ	マシテンタン含有治療用組成物
HK1243000A1 (zh) *	2015-01-28	2018-07-06	瑞采生技有限公司	用於增强PPARγ表现及核转位之化合物及其医疗用途
US20180072741A1 (en)	2016-09-09	2018-03-15	Incyte Corporation	Pyrazolopyrimidine compounds and uses thereof
CN115819417A (zh)	2016-09-09	2023-03-21	因赛特公司	作为hpk1调节剂的吡唑并吡啶衍生物及其用于治疗癌症的用途
WO2018049214A1 (en)	2016-09-09	2018-03-15	Incyte Corporation	Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer
WO2018152220A1 (en)	2017-02-15	2018-08-23	Incyte Corporation	Pyrazolopyridine compounds and uses thereof
MX2019012431A (es)	2017-04-21	2020-08-03	Ikena Oncology Inc	Inhibidores del receptor de hidrocarburos de arilo (ahr) de indol y usos de los mismos.
US10722495B2 (en)	2017-09-08	2020-07-28	Incyte Corporation	Cyanoindazole compounds and uses thereof
US10752635B2 (en)	2018-02-20	2020-08-25	Incyte Corporation	Indazole compounds and uses thereof
US10745388B2 (en)	2018-02-20	2020-08-18	Incyte Corporation	Indazole compounds and uses thereof
EP3755703B1 (en)	2018-02-20	2022-05-04	Incyte Corporation	N-(phenyl)-2-(phenyl)pyrimidine-4-carboxamide derivatives and related compounds as hpk1 inhibitors for treating cancer
US11299473B2 (en)	2018-04-13	2022-04-12	Incyte Corporation	Benzimidazole and indole compounds and uses thereof
US10899755B2 (en)	2018-08-08	2021-01-26	Incyte Corporation	Benzothiazole compounds and uses thereof
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BR112022002059A2 (pt)	2019-08-06	2022-06-07	Incyte Corp	Formas sólidas de um inibidor de hpk1
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2001
- 2001-11-28 EP EP01990452A patent/EP1343506A1/de not_active Withdrawn
- 2001-11-28 BR BR0115995-0A patent/BR0115995A/pt not_active Application Discontinuation
- 2001-11-28 CZ CZ20031776A patent/CZ20031776A3/cs unknown
- 2001-11-28 JP JP2002550991A patent/JP2004516270A/ja active Pending
- 2001-11-28 US US10/451,105 patent/US20040063730A1/en not_active Abandoned
- 2001-11-28 CA CA002431077A patent/CA2431077A1/en not_active Abandoned
- 2001-11-28 SK SK819-2003A patent/SK8192003A3/sk unknown
- 2001-11-28 HU HU0303315A patent/HUP0303315A2/hu unknown
- 2001-11-28 MX MXPA03005393A patent/MXPA03005393A/es not_active Application Discontinuation
- 2001-11-28 PL PL01362513A patent/PL362513A1/xx unknown
- 2001-11-28 AU AU2002229573A patent/AU2002229573A1/en not_active Abandoned
- 2001-11-28 CN CNA018209165A patent/CN1481244A/zh active Pending
- 2001-11-28 KR KR10-2003-7008078A patent/KR20030059349A/ko not_active Withdrawn
- 2001-11-28 WO PCT/EP2001/013916 patent/WO2002049651A1/de not_active Ceased
- 2001-12-19 AR ARP010105888A patent/AR035676A1/es unknown
2003
- 2003-06-18 NO NO20032773A patent/NO20032773D0/no unknown

Also Published As

Publication number	Publication date
NO20032773L (no)	2003-06-18
WO2002049651A1 (de)	2002-06-27
BR0115995A (pt)	2004-01-13
NO20032773D0 (no)	2003-06-18
US20040063730A1 (en)	2004-04-01
AU2002229573A1 (en)	2002-07-01
HUP0303315A2 (hu)	2004-01-28
EP1343506A1 (de)	2003-09-17
AR035676A1 (es)	2004-06-23
MXPA03005393A (es)	2003-09-25
CA2431077A1 (en)	2002-06-27
CN1481244A (zh)	2004-03-10
CZ20031776A3 (cs)	2003-09-17
PL362513A1 (en)	2004-11-02
JP2004516270A (ja)	2004-06-03
KR20030059349A (ko)	2003-07-07

Publication	Publication Date	Title
SK8192003A3 (en)	2003-10-07	Pharmaceutical formulation containing pyrazolo[4,3-d]pyrimidines and antithrombotic agents, calcium-antagonists, prostaglandins or prostaglandin derivatives
US20040034040A1 (en)	2004-02-19	Use of thienopyrimidines
KR20040041166A (ko)	2004-05-14	피리미딘 유도체
ES2247007T3 (es)	2006-03-01	Sulfamidotienopirimidinas para el empleo como inhibidores de la fosfodiesterasa.
US20040072846A1 (en)	2004-04-15	Pharmaceutical formulation containing thienopyrimidines and antithrombotics, calcium antagonists, prostaglandins or prostaglandin derivatives
CA2437085A1 (en)	2002-08-15	Pharmaceutical formulation comprising pyrazolo[4,3-d]pyrimidines and endothelin receptor antagonists or thienopyrimidines and endothelin receptor antagonists
US20040023990A1 (en)	2004-02-05	Use of pyrazolo[4,3-d]pyrimidines
US20040077664A1 (en)	2004-04-22	Pharmaceutical formulation comprising pyrazolo[4,3-d]pyrimidine and nitrates or thienopyrimidines and nitrates
SK8032003A3 (en)	2003-11-04	Pharmaceutical formulation containing thienopyrimidines and antithrombotics, calcium antagonists, prostaglandins or prostaglandin derivatives
DE10063223A1 (de)	2002-06-20	Pharmazeutische Formulierung enthaltend Thienopyrimidine und Antithrombotica (1)
ZA200305548B (en)	2005-01-26	Pharmaceutical formulation containing thienopyrimidines and antithrombotics calcium antagonists prostaglandins or prostaglandin derivatives (2)
DE10063224A1 (de)	2002-06-20	Pharmazeutische Formulierung enthaltend Pyrazolo(4,3-d)pyrimidine und Antithrombotica
ZA200305542B (en)	2005-01-26	Pharmaceutical formulation containing pyrazole [4,3-d]pymidines and antithrombotic agents calcium antagonists prostaglandins or prostaglandin derivatives
DE10063221A1 (de)	2002-06-20	Pharmazeutische Formulierung enthaltend Thienopyrimidine und Antithrombotica (2)
MXPA04003049A (es)	2004-07-05	Derivados de pirimidina.