ES2320922T3 - Uso de 4-piridilmetilftalazinas para el tratamiento de cancer renal. - Google Patents
Uso de 4-piridilmetilftalazinas para el tratamiento de cancer renal. Download PDFInfo
- Publication number
- ES2320922T3 ES2320922T3 ES06114903T ES06114903T ES2320922T3 ES 2320922 T3 ES2320922 T3 ES 2320922T3 ES 06114903 T ES06114903 T ES 06114903T ES 06114903 T ES06114903 T ES 06114903T ES 2320922 T3 ES2320922 T3 ES 2320922T3
- Authority
- ES
- Spain
- Prior art keywords
- day
- phthalazine
- pyridylmethyl
- chloroanilino
- dose
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired - Lifetime
Links
- 238000011282 treatment Methods 0.000 title claims abstract description 18
- 206010038389 Renal cancer Diseases 0.000 title claims abstract description 14
- 208000008839 Kidney Neoplasms Diseases 0.000 title description 4
- 201000010982 kidney cancer Diseases 0.000 title description 4
- WHOWNXIYXLWMGJ-UHFFFAOYSA-N 1-(pyridin-4-ylmethyl)phthalazine Chemical compound N=1N=CC2=CC=CC=C2C=1CC1=CC=NC=C1 WHOWNXIYXLWMGJ-UHFFFAOYSA-N 0.000 claims abstract description 15
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 14
- 208000006265 Renal cell carcinoma Diseases 0.000 claims abstract description 10
- 201000010174 renal carcinoma Diseases 0.000 claims abstract description 10
- 239000000825 pharmaceutical preparation Substances 0.000 claims abstract description 5
- YCOYDOIWSSHVCK-UHFFFAOYSA-N vatalanib Chemical group C1=CC(Cl)=CC=C1NC(C1=CC=CC=C11)=NN=C1CC1=CC=NC=C1 YCOYDOIWSSHVCK-UHFFFAOYSA-N 0.000 claims description 32
- 150000003839 salts Chemical class 0.000 claims description 13
- 230000006510 metastatic growth Effects 0.000 claims description 7
- 230000005764 inhibitory process Effects 0.000 claims description 4
- 206010050018 Renal cancer metastatic Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 description 27
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 13
- 201000010099 disease Diseases 0.000 description 12
- 201000011510 cancer Diseases 0.000 description 9
- 230000009467 reduction Effects 0.000 description 8
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 description 7
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 description 7
- 239000003814 drug Substances 0.000 description 6
- 238000013535 dynamic contrast enhanced MRI Methods 0.000 description 6
- 210000004185 liver Anatomy 0.000 description 5
- 230000001394 metastastic effect Effects 0.000 description 5
- 206010061289 metastatic neoplasm Diseases 0.000 description 5
- 238000002512 chemotherapy Methods 0.000 description 4
- 238000002595 magnetic resonance imaging Methods 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
- 230000000750 progressive effect Effects 0.000 description 4
- 201000009030 Carcinoma Diseases 0.000 description 3
- 206010027476 Metastases Diseases 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 230000010412 perfusion Effects 0.000 description 3
- 238000012546 transfer Methods 0.000 description 3
- 206010009944 Colon cancer Diseases 0.000 description 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 description 2
- 206010061818 Disease progression Diseases 0.000 description 2
- 206010021143 Hypoxia Diseases 0.000 description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 2
- 208000037844 advanced solid tumor Diseases 0.000 description 2
- 238000002648 combination therapy Methods 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 230000005750 disease progression Effects 0.000 description 2
- 239000012458 free base Substances 0.000 description 2
- 230000012010 growth Effects 0.000 description 2
- 230000001146 hypoxic effect Effects 0.000 description 2
- 230000003902 lesion Effects 0.000 description 2
- 201000005202 lung cancer Diseases 0.000 description 2
- 208000020816 lung neoplasm Diseases 0.000 description 2
- 230000009401 metastasis Effects 0.000 description 2
- 230000036470 plasma concentration Effects 0.000 description 2
- 230000001023 pro-angiogenic effect Effects 0.000 description 2
- 208000037821 progressive disease Diseases 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- 231100000419 toxicity Toxicity 0.000 description 2
- 230000001988 toxicity Effects 0.000 description 2
- 210000004881 tumor cell Anatomy 0.000 description 2
- 230000008728 vascular permeability Effects 0.000 description 2
- VVIAGPKUTFNRDU-UHFFFAOYSA-N 6S-folinic acid Natural products C1NC=2NC(N)=NC(=O)C=2N(C=O)C1CNC1=CC=C(C(=O)NC(CCC(O)=O)C(O)=O)C=C1 VVIAGPKUTFNRDU-UHFFFAOYSA-N 0.000 description 1
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 description 1
- MPJKWIXIYCLVCU-UHFFFAOYSA-N Folinic acid Natural products NC1=NC2=C(N(C=O)C(CNc3ccc(cc3)C(=O)NC(CCC(=O)O)CC(=O)O)CN2)C(=O)N1 MPJKWIXIYCLVCU-UHFFFAOYSA-N 0.000 description 1
- 206010024264 Lethargy Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 206010027540 Microcytosis Diseases 0.000 description 1
- 208000003788 Neoplasm Micrometastasis Diseases 0.000 description 1
- 206010060862 Prostate cancer Diseases 0.000 description 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 1
- 102000004278 Receptor Protein-Tyrosine Kinases Human genes 0.000 description 1
- 108090000873 Receptor Protein-Tyrosine Kinases Proteins 0.000 description 1
- 229940124639 Selective inhibitor Drugs 0.000 description 1
- 102000003929 Transaminases Human genes 0.000 description 1
- 108090000340 Transaminases Proteins 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 238000011226 adjuvant chemotherapy Methods 0.000 description 1
- 230000033115 angiogenesis Effects 0.000 description 1
- 239000004037 angiogenesis inhibitor Substances 0.000 description 1
- 239000000090 biomarker Substances 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 238000009104 chemotherapy regimen Methods 0.000 description 1
- 210000001072 colon Anatomy 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 230000002074 deregulated effect Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 229960002949 fluorouracil Drugs 0.000 description 1
- VVIAGPKUTFNRDU-ABLWVSNPSA-N folinic acid Chemical compound C1NC=2NC(N)=NC(=O)C=2N(C=O)C1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 VVIAGPKUTFNRDU-ABLWVSNPSA-N 0.000 description 1
- 235000008191 folinic acid Nutrition 0.000 description 1
- 239000011672 folinic acid Substances 0.000 description 1
- 230000009036 growth inhibition Effects 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 229960001691 leucovorin Drugs 0.000 description 1
- 208000019423 liver disease Diseases 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 230000001613 neoplastic effect Effects 0.000 description 1
- 231100000956 nontoxicity Toxicity 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 230000036961 partial effect Effects 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 238000009097 single-agent therapy Methods 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 238000012549 training Methods 0.000 description 1
- 230000001052 transient effect Effects 0.000 description 1
- 238000011269 treatment regimen Methods 0.000 description 1
- 230000004614 tumor growth Effects 0.000 description 1
- 231100000402 unacceptable toxicity Toxicity 0.000 description 1
- 239000002996 urinary tract agent Substances 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
Classifications
-
- 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
- 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
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/24—Heavy metals; Compounds thereof
- A61K33/243—Platinum; Compounds thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P35/04—Antineoplastic agents specific for metastasis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Inorganic Chemistry (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (8)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31869401P | 2001-09-12 | 2001-09-12 | |
| US33102501P | 2001-09-12 | 2001-09-12 | |
| US318694P | 2001-09-12 | ||
| US331025P | 2001-09-12 | ||
| US32204401P | 2001-09-14 | 2001-09-14 | |
| US322044P | 2001-09-14 | ||
| US38816302P | 2002-06-12 | 2002-06-12 | |
| US388163P | 2002-06-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2320922T3 true ES2320922T3 (es) | 2009-05-29 |
Family
ID=27502161
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES06114903T Expired - Lifetime ES2320922T3 (es) | 2001-09-12 | 2002-09-11 | Uso de 4-piridilmetilftalazinas para el tratamiento de cancer renal. |
| ES02779338T Expired - Lifetime ES2266590T3 (es) | 2001-09-12 | 2002-09-11 | Uso de una combinacion que comprende 4-pirilmetilftalazinas para el tratamiento de cancer. |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES02779338T Expired - Lifetime ES2266590T3 (es) | 2001-09-12 | 2002-09-11 | Uso de una combinacion que comprende 4-pirilmetilftalazinas para el tratamiento de cancer. |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US20040258770A1 (https=) |
| EP (1) | EP1427420B1 (https=) |
| JP (1) | JP2005502690A (https=) |
| KR (1) | KR20040029172A (https=) |
| CN (1) | CN1330308C (https=) |
| AT (2) | ATE421880T1 (https=) |
| AU (2) | AU2002342678B2 (https=) |
| BR (1) | BR0212446A (https=) |
| CA (1) | CA2457848A1 (https=) |
| CO (1) | CO5560545A2 (https=) |
| CY (1) | CY1105189T1 (https=) |
| DE (2) | DE60231068D1 (https=) |
| DK (1) | DK1427420T3 (https=) |
| ES (2) | ES2320922T3 (https=) |
| HR (1) | HRP20040241A2 (https=) |
| IL (1) | IL160382A0 (https=) |
| NO (1) | NO327358B1 (https=) |
| NZ (1) | NZ531484A (https=) |
| PL (1) | PL367349A1 (https=) |
| PT (1) | PT1427420E (https=) |
| RS (1) | RS16804A (https=) |
| WO (1) | WO2003022282A1 (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0223341D0 (en) * | 2002-10-08 | 2002-11-13 | Groningen Acad Ziekenhuis | Organic compounds |
| AU2003292888A1 (en) * | 2002-12-27 | 2004-07-22 | Schering Aktiengesellschaft | Pharmaceutical combinations of phthalazine vegf inhibitors and benzamide hdac inhibitors |
| EP1631278A4 (en) * | 2003-05-20 | 2006-09-20 | Aronex Pharmaceuticals Inc | COMBINATION SCHEMOTHERAPY WITH CAPECITABIN AND A LIPOSOMAL PLATINUM COMPLEX |
| BRPI0414698A (pt) * | 2003-09-23 | 2006-11-28 | Novartis Ag | combinação de um inibidor receptor de vegf com um agente quimioterapêutico |
| GB0610925D0 (en) * | 2006-06-02 | 2006-07-12 | Novartis Ag | Use of vascular endothelial growth factor receptor inhibitors for the treatment of cancer |
| KR101037292B1 (ko) * | 2010-09-03 | 2011-05-27 | (주)슈추어 | 신발 장식구 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996005176A1 (en) * | 1994-08-09 | 1996-02-22 | Eisai Co., Ltd. | Fused pyridazine compound |
| US6291455B1 (en) * | 1996-03-05 | 2001-09-18 | Zeneca Limited | 4-anilinoquinazoline derivatives |
| US6096904A (en) * | 1996-12-03 | 2000-08-01 | The Trustees Of The University Of Pennsylvania | Synthetic techniques and intermediates for polyhydroxy, dienyl lactone derivatives |
| CO4950519A1 (es) * | 1997-02-13 | 2000-09-01 | Novartis Ag | Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion |
-
2002
- 2002-09-11 DE DE60231068T patent/DE60231068D1/de not_active Expired - Lifetime
- 2002-09-11 JP JP2003526411A patent/JP2005502690A/ja active Pending
- 2002-09-11 WO PCT/EP2002/010194 patent/WO2003022282A1/en not_active Ceased
- 2002-09-11 NZ NZ531484A patent/NZ531484A/en not_active IP Right Cessation
- 2002-09-11 PL PL02367349A patent/PL367349A1/xx not_active Application Discontinuation
- 2002-09-11 CN CNB028178831A patent/CN1330308C/zh not_active Expired - Fee Related
- 2002-09-11 AU AU2002342678A patent/AU2002342678B2/en not_active Ceased
- 2002-09-11 AT AT06114903T patent/ATE421880T1/de not_active IP Right Cessation
- 2002-09-11 EP EP02779338A patent/EP1427420B1/en not_active Expired - Lifetime
- 2002-09-11 ES ES06114903T patent/ES2320922T3/es not_active Expired - Lifetime
- 2002-09-11 CA CA002457848A patent/CA2457848A1/en not_active Abandoned
- 2002-09-11 DE DE60212415T patent/DE60212415T2/de not_active Expired - Lifetime
- 2002-09-11 ES ES02779338T patent/ES2266590T3/es not_active Expired - Lifetime
- 2002-09-11 RS YUP-168/04A patent/RS16804A/sr unknown
- 2002-09-11 US US10/489,751 patent/US20040258770A1/en not_active Abandoned
- 2002-09-11 AT AT02779338T patent/ATE329597T1/de not_active IP Right Cessation
- 2002-09-11 HR HR20040241A patent/HRP20040241A2/hr not_active Application Discontinuation
- 2002-09-11 IL IL16038202A patent/IL160382A0/xx not_active IP Right Cessation
- 2002-09-11 KR KR10-2004-7003645A patent/KR20040029172A/ko not_active Abandoned
- 2002-09-11 DK DK02779338T patent/DK1427420T3/da active
- 2002-09-11 BR BR0212446-7A patent/BR0212446A/pt not_active IP Right Cessation
- 2002-09-11 PT PT02779338T patent/PT1427420E/pt unknown
-
2004
- 2004-02-27 CO CO04017661A patent/CO5560545A2/es active IP Right Grant
- 2004-03-05 NO NO20040973A patent/NO327358B1/no not_active IP Right Cessation
-
2006
- 2006-08-09 AU AU2006203428A patent/AU2006203428B2/en not_active Ceased
- 2006-08-31 CY CY20061101239T patent/CY1105189T1/el unknown
-
2009
- 2009-04-15 US US12/423,843 patent/US20090196871A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU2006203428B2 (en) | 2009-06-04 |
| IL160382A0 (en) | 2004-07-25 |
| AU2002342678B2 (en) | 2006-08-24 |
| DE60212415T2 (de) | 2006-11-23 |
| CY1105189T1 (el) | 2010-03-03 |
| DE60231068D1 (de) | 2009-03-19 |
| US20090196871A1 (en) | 2009-08-06 |
| EP1427420B1 (en) | 2006-06-14 |
| AU2006203428A1 (en) | 2006-08-31 |
| EP1427420A1 (en) | 2004-06-16 |
| KR20040029172A (ko) | 2004-04-03 |
| NO20040973L (no) | 2004-06-03 |
| ES2266590T3 (es) | 2007-03-01 |
| CA2457848A1 (en) | 2003-03-20 |
| CN1553803A (zh) | 2004-12-08 |
| PT1427420E (pt) | 2006-10-31 |
| HRP20040241A2 (en) | 2005-04-30 |
| WO2003022282A1 (en) | 2003-03-20 |
| ATE329597T1 (de) | 2006-07-15 |
| PL367349A1 (en) | 2005-02-21 |
| CN1330308C (zh) | 2007-08-08 |
| US20040258770A1 (en) | 2004-12-23 |
| DK1427420T3 (da) | 2006-10-02 |
| ATE421880T1 (de) | 2009-02-15 |
| NZ531484A (en) | 2007-02-23 |
| JP2005502690A (ja) | 2005-01-27 |
| DE60212415D1 (de) | 2006-07-27 |
| BR0212446A (pt) | 2004-08-17 |
| NO327358B1 (no) | 2009-06-15 |
| RS16804A (sr) | 2007-02-05 |
| CO5560545A2 (es) | 2005-09-30 |
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