HRP20100030T1 - Upotreba 1,2,3-supstituiranih indolizinskih derivata u liječenju bolesti povezanih s patološkom angiogenezom - Google Patents
Upotreba 1,2,3-supstituiranih indolizinskih derivata u liječenju bolesti povezanih s patološkom angiogenezom Download PDFInfo
- Publication number
- HRP20100030T1 HRP20100030T1 HR20100030T HRP20100030T HRP20100030T1 HR P20100030 T1 HRP20100030 T1 HR P20100030T1 HR 20100030 T HR20100030 T HR 20100030T HR P20100030 T HRP20100030 T HR P20100030T HR P20100030 T1 HRP20100030 T1 HR P20100030T1
- Authority
- HR
- Croatia
- Prior art keywords
- alk
- radical
- carbon atoms
- amino
- alkoxy
- Prior art date
Links
- 201000010099 disease Diseases 0.000 title claims abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims abstract 4
- 125000003406 indolizinyl group Chemical class C=1(C=CN2C=CC=CC12)* 0.000 title abstract 3
- 208000034038 Pathologic Neovascularization Diseases 0.000 title 1
- -1 NH 2 Chemical group 0.000 claims abstract 55
- 125000005843 halogen group Chemical group 0.000 claims abstract 8
- 150000003839 salts Chemical class 0.000 claims abstract 6
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 5
- 230000033115 angiogenesis Effects 0.000 claims abstract 3
- 239000003814 drug Substances 0.000 claims abstract 3
- 125000005842 heteroatom Chemical group 0.000 claims abstract 3
- 230000001575 pathological effect Effects 0.000 claims abstract 3
- 125000002947 alkylene group Chemical group 0.000 claims abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 42
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 14
- 150000003254 radicals Chemical class 0.000 claims 14
- ORTFAQDWJHRMNX-UHFFFAOYSA-M oxidooxomethyl Chemical compound [O-][C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-M 0.000 claims 6
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 claims 5
- SLRMQYXOBQWXCR-UHFFFAOYSA-N 2154-56-5 Chemical compound [CH2]C1=CC=CC=C1 SLRMQYXOBQWXCR-UHFFFAOYSA-N 0.000 claims 4
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 3
- TUJKJAMUKRIRHC-UHFFFAOYSA-N hydroxyl Chemical group [OH] TUJKJAMUKRIRHC-UHFFFAOYSA-N 0.000 claims 3
- 206010064930 age-related macular degeneration Diseases 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- BLNWTAHYTCHDJH-UHFFFAOYSA-O hydroxy(oxo)azanium Chemical compound O[NH+]=O BLNWTAHYTCHDJH-UHFFFAOYSA-O 0.000 claims 2
- 208000002780 macular degeneration Diseases 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 208000027496 Behcet disease Diseases 0.000 claims 1
- WZKSXHQDXQKIQJ-UHFFFAOYSA-N F[C](F)F Chemical compound F[C](F)F WZKSXHQDXQKIQJ-UHFFFAOYSA-N 0.000 claims 1
- 201000005485 Toxoplasmosis Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002478 indolizines Chemical class 0.000 claims 1
- 208000001491 myopia Diseases 0.000 claims 1
- 230000004379 myopia Effects 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 125000003545 alkoxy group Chemical group 0.000 abstract 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 4
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 2
- 210000003161 choroid Anatomy 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 102000018233 Fibroblast Growth Factor Human genes 0.000 abstract 1
- 108050007372 Fibroblast Growth Factor Proteins 0.000 abstract 1
- 230000001772 anti-angiogenic effect Effects 0.000 abstract 1
- 230000003110 anti-inflammatory effect Effects 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229940126864 fibroblast growth factor Drugs 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000002349 hydroxyamino group Chemical group [H]ON([H])[*] 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000010534 mechanism of action Effects 0.000 abstract 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
- A61K31/435—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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P31/10—Antimycotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Tropical Medicine & Parasitology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Ophthalmology & Optometry (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Communicable Diseases (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Indole Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
Upotreba 1,2,3-supstituiranih indolizinskih derivata sljedeće opće formule (I) ,u kojojR1 predstavlja hidroksilni radikal, nerazgranati ili razgranati alkoksi radikal s 1 do 5 atoma ugljika, karboksilni radikal, alkoksikarbonilni radikal s 2 do 6 atoma ugljika ili radikal formule• -NR5R6• -NH-SO2-Alk• -NH-SO2-Ph• -NH-CO-Ph• -N(Alk)-CO-Ph• -NH-CO-NH-Ph• -NH-CO-Alk• -NH-CO2-Alk• -O-(CH2)n-cAlk• -O-Alk-COOR7• -O-Alk-O-R8• -O-Alk-OH• -O-Alk-C(NH2):NOH• -O-Alk-NR5R6• -O-Alk-CN• -O-(CH2)n-Ph• -O-Alk-CO-NR5R6• -CO-NH-(CH2)m-COOR7• -CO-NH-Alkgdje• Alk predstavlja nerazgranati ili razgranati alkilni radikal ili alkilenski radikal s 1 do 5 atoma ugljika, • cAlk predstavlja cikloalkilni radikal s 3 do 6 atoma ugljika, • n predstavlja cijeli broj od 0 do 5, • m predstavlja cijeli broj od 1 do 5, • svaki od R5 i R6, koji su istovjetni ili različiti, predstavlja atom vodika, nerazgranati ili razgranati alkilni radikal s 1 do 5 atoma ugljika ili benzilni radikal, • R7 predstavlja atom vodika ili alkilni radikal s 1 do 5 atoma ugljika, • R8 predstavlja alkilni radikal s 1 do 5 atoma ugljika ili -CO-Alk radikal, • Ph predstavlja fenilni radikal, izborno supstituiran s jednim ili više atoma halogena, jednim ili više alkoksi radikala s 1 do 5 atoma ugljika, jednim ili više karboksilnih radikala ili jednim ili više alkoksikarbonilnih radikala s 2 do 6 atoma ugljika, R2 predstavlja atom vodika, alkilni radikal s 1 do 5 atoma ugljika, alkil-halogenidni radikal s 1 do 5 atoma ugljika i 3 do 5 atoma halogena, cikloalkilni radikal s 3 do 6 atoma ugljika ili fenilni radikal, izborno supstituiran s jednim ili više atoma halogena, jednim ili više alkoksi radikala s 1 do 5 atoma ugljika, jednim ili više karboksilnih radikala ili jednim ili više alkoksikarbonilnih radikala s 2 do 6 atoma ugljika, A predstavlja -CO-, -SO- ili -SO2- radikal, svaki od R3 i R4, koji su istovjetni ili različiti, predstavlja atom vodika, alkoksi radikal s 1 do 5 atoma ugljika, amino radikal, karboksilni radikal, alkoksikarbonilni radikal s 2 do 6 atoma ugljika, hidroksilni radikal, nitro radikal, hidroksiamino radikal, radikal formule• -Alk-COOR7• -NR5R6• -NH-Alk-COOR7• -NH-COO-Alk• -N(R11)-SO2-Alk-NR9R10• -N(R11)-SO2-Alk• -N(R11)-Alk-NR5R6• -N(R11)-CO-Alk-NR9R10• -N(R11)-CO-Alk• -N(R11)-CO-CF3• -NH-Alk-HetN• -O-Alk-NR9R10• -O-Alk-CO-NR5R6• -O-Alk-HetNgdje n, m, Alk, R5, R6 i R7 imaju značenje dano gore za R1; isvaki od R9 i R10, koji su istovjetni ili različiti, predstavlja atom vodika ili alkilni radikal s 1 do 5 atoma ugljika, R11 predstavlja atom vodika ili -Alk-COOR12 radikal, gdje R12 predstavlja atom vodika, alkilni radikal s 1 do 5 atoma ugljika ili benzilni radikal, HetN predstavlja 5- ili 6- člani heterocikl s najmanje jednim atomom dušika i izbor
Claims (4)
1. Upotreba 1,2,3-supstituiranih indolizinskih derivata sljedeće opće formule (I)
[image]
,
u kojoj
R1 predstavlja hidroksilni radikal, nerazgranati ili razgranati alkoksi radikal s 1 do 5 atoma ugljika, karboksilni radikal, alkoksikarbonilni radikal s 2 do 6 atoma ugljika ili radikal formule
• -NR5R6
• -NH-SO2-Alk
• -NH-SO2-Ph
• -NH-CO-Ph
• -N(Alk)-CO-Ph
• -NH-CO-NH-Ph
• -NH-CO-Alk
• -NH-CO2-Alk
• -O-(CH2)n-cAlk
• -O-Alk-COOR7
• -O-Alk-O-R8
• -O-Alk-OH
• -O-Alk-C(NH2):NOH
• -O-Alk-NR5R6
• -O-Alk-CN
• -O-(CH2)n-Ph
• -O-Alk-CO-NR5R6
• -CO-NH-(CH2)m-COOR7
• -CO-NH-Alk
gdje
• Alk predstavlja nerazgranati ili razgranati alkilni radikal ili alkilenski radikal s 1 do 5 atoma ugljika,
• cAlk predstavlja cikloalkilni radikal s 3 do 6 atoma ugljika,
• n predstavlja cijeli broj od 0 do 5,
• m predstavlja cijeli broj od 1 do 5,
• svaki od R5 i R6, koji su istovjetni ili različiti, predstavlja atom vodika, nerazgranati ili razgranati alkilni radikal s 1 do 5 atoma ugljika ili benzilni radikal,
• R7 predstavlja atom vodika ili alkilni radikal s 1 do 5 atoma ugljika,
• R8 predstavlja alkilni radikal s 1 do 5 atoma ugljika ili -CO-Alk radikal,
• Ph predstavlja fenilni radikal, izborno supstituiran s jednim ili više atoma halogena, jednim ili više alkoksi radikala s 1 do 5 atoma ugljika, jednim ili više karboksilnih radikala ili jednim ili više alkoksikarbonilnih radikala s 2 do 6 atoma ugljika,
R2 predstavlja atom vodika, alkilni radikal s 1 do 5 atoma ugljika, alkil-halogenidni radikal s 1 do 5 atoma ugljika i 3 do 5 atoma halogena, cikloalkilni radikal s 3 do 6 atoma ugljika ili fenilni radikal, izborno supstituiran s jednim ili više atoma halogena, jednim ili više alkoksi radikala s 1 do 5 atoma ugljika, jednim ili više karboksilnih radikala ili jednim ili više alkoksikarbonilnih radikala s 2 do 6 atoma ugljika,
A predstavlja -CO-, -SO- ili -SO2- radikal,
svaki od R3 i R4, koji su istovjetni ili različiti, predstavlja atom vodika, alkoksi radikal s 1 do 5 atoma ugljika, amino radikal, karboksilni radikal, alkoksikarbonilni radikal s 2 do 6 atoma ugljika, hidroksilni radikal, nitro radikal, hidroksiamino radikal, radikal formule
• -Alk-COOR7
• -NR5R6
• -NH-Alk-COOR7
• -NH-COO-Alk
• -N(R11)-SO2-Alk-NR9R10
• -N(R11)-SO2-Alk
• -N(R11)-Alk-NR5R6
• -N(R11)-CO-Alk-NR9R10
• -N(R11)-CO-Alk
• -N(R11)-CO-CF3
• -NH-Alk-HetN
• -O-Alk-NR9R10
• -O-Alk-CO-NR5R6
• -O-Alk-HetN
gdje n, m, Alk, R5, R6 i R7 imaju značenje dano gore za R1; i
svaki od R9 i R10, koji su istovjetni ili različiti, predstavlja atom vodika ili alkilni radikal s 1 do 5 atoma ugljika,
R11 predstavlja atom vodika ili -Alk-COOR12 radikal, gdje R12 predstavlja atom vodika, alkilni radikal s 1 do 5 atoma ugljika ili benzilni radikal,
HetN predstavlja 5- ili 6- člani heterocikl s najmanje jednim atomom dušika i izborno još jednim heteroatomom, kojeg se bira između dušika i kisika,
ili R3 i R4 zajedno tvore nezasićeni 5- ili 6- člani heterocikl, no uz uvjet da kada R3 predstavlja alkoksi radikal, a R4 predstavlja -O-Alk-NR9R10 radikal ili hidroksi radikal R1 ne predstavlja alkoksi radikal,
izborno u obliku jedne od njihovih farmaceutski prihvatljivih soli,
naznačena time što su navedeni derivati namijenjeni pripravi medikamenata za liječenje bolesti povezanih s patološkom koroidnom angiogenezom, koju se bira između staračkom degeneracijom makule (AMD), teškom miopijom, pseudoksantomom, pretpostavljenim histoplazmotičnim sindromom, toksoplazmozom, sarkoidozom i Behçetovom bolešću.
2. Upotreba, u skladu s patentnim zahtjevom 1, spojeva opće formule (I), naznačena time što
R1 predstavlja hidroksilni radikal, nerazgranati ili razgranati alkoksi radikal s 1 do 5 atoma ugljika, karboksilni radikal, alkoksikarbonilni radikal s 2 do 6 atoma ugljika ili radikal formule:
• -NR5R6
• -NH-SO2-Alk
• -NH-SO2-Ph
• -NH-CO-Ph
• -N(Alk)-CO-Ph
• -NH-CO-NH-Ph
• -NH-CO-Alk
• -NH-CO2-Alk
• -O-(CH2)n-cAlk
• -O-Alk-COOR7
• -O-Alk-O-R8
• -O-Alk-OH
• -O-Alk-NR5R6
• -O-Alk-CN
• -O-(CH2)n-Ph
• -O-Alk-CO-NR5R6
• -CO-NH-(CH2)m-COOR7
• -CO-NH-Alk
gdje
• Alk predstavlja nerazgranati ili razgranati alkilni radikal ili alkilenski radikal s 1 do 5 atoma ugljika,
• cAlk predstavlja cikloalkilni radikal s 3 do 6 atoma ugljika,
• n predstavlja cijeli broj od 0 do 5,
• m predstavlja cijeli broj od 1 do 5,
• svaki od R5 i R6, koji su istovjetni ili različiti, predstavlja atom vodika, nerazgranati ili razgranati alkilni radikal s 1 do 5 atoma ugljika ili benzilni radikal,
• R7 predstavlja atom vodika ili alkilni radikal s 1 do 5 atoma ugljika,
• R8 predstavlja alkilni radikal s 1 do 5 atoma ugljika ili -CO-Alk radikal,
• Ph predstavlja fenilni radikal, izborno supstituiran s jednim ili više atoma halogena, jednim ili više alkoksi radikala s 1 do 5 atoma ugljika, jednim ili više karboksilnih radikala ili jednim ili više alkoksikarbonilnih radikala s 2 do 6 atoma ugljika,
R2 predstavlja alkilni radikal s 1 do 5 atoma ugljika, trifluormetilni radikal, cikloalkilni radikal s 3 do 6 atoma ugljika ili fenilni radikal, izborno supstituiran s jednim ili više atoma halogena, jednim ili više alkoksi radikala s 1 do 5 atoma ugljika, jednim ili više karboksilnih radikala ili jednim ili više alkoksikarbonilnih radikala s 2 do 6 atoma ugljika,
A predstavlja -CO- ili -SO2- radikal,
svaki od R3 i R4, koji su istovjetni ili različiti, predstavlja atom vodika, alkoksi radikal s 1 do 5 atoma ugljika, amino radikal, karboksilni radikal, alkoksikarbonilni radikal s 2 do 6 atoma ugljika, nitro radikal, hidroksiamino radikal, radikal formule
• -Alk-COOR7
• -NR5R6
• -NH-Alk-COOR7
• -NH-COO-Alk
• -N(R11)-SO2-Alk-NR9R10
• -N(R11)-SO2-Alk
• -N(R11)-Alk-NR5R6
• -N(R11)-CO-Alk-NR9R10
• -N(R11)-CO-Alk
• -N(R11)-CO-CF3
• -NH-Alk-HetN
gdje n, m, Alk, R5, R6 i R7 imaju značenje dano gore za R1; i
svaki od R9 i R10, koji su istovjetni ili različiti, predstavlja atom vodika ili alkilni radikal s 1 do 5 atoma ugljika,
R11 predstavlja atom vodika ili -Alk-COOR12 radikal, gdje R12 predstavlja atom vodika, alkilni radikal s 1 do 5 atoma ugljika ili benzilni radikal,
HetN predstavlja 5- ili 6- člani heterocikl s najmanje jednim atomom dušika i izborno još jednim heteroatomom, kojeg se bira između dušika i kisika, izborno u obliku jedne od njihovih farmaceutski prihvatljivih soli.
3. Upotreba, u skladu s bilo kojim od patentnih zahtjeva 1 i 2, spojeva opće formule (I), naznačena time što
R1 predstavlja alkoksi radikal s 1 do 5 atoma ugljika, karboksilni radikal, -O-Alk-COOH radikal, gdje Alk predstavlja nerazgranati ili razgranati alkilenski radikal s 1 do 5 atoma ugljika, radikal formule -O-Alk-Ph, gdje Alk predstavlja alkilenski radikal s 1 do 5 atoma ugljika, a Ph predstavlja fenilni radikal, izborno supstituiran s jednim ili više atoma halogena ili jednim ili više alkoksi radikala s 1 do 5 atoma ugljika ili jednim ili više karboksilnih radikala, radikal formule -NH-CO-Ph, radikal formule -NH-SO2-Ph ili radikal formule -NH-CO-NH-Ph,
R2 predstavlja alkilni radikal s 1 do 5 atoma ugljika,
A predstavlja -CO- radikal,
svaki od R3 i R4, koji su različiti, predstavlja atom vodika, alkoksi radikal s 1 do 5 atoma ugljika, amino radikal, karboksilni radikal ili alkoksikarbonilni radikal s 2 do 6 atoma ugljika, izborno u obliku jedne od njihovih farmaceutski prihvatljivih soli.
4. Upotreba, u skladu s bilo kojim od patentnih zahtjeva 1 do 3, spojeva opće formule (I), naznačena time što se navedene spojeve bira između
– (4-amino-3-metoksifenil)(1-metoksi-2-metilindolizin-3-il)metanona
– 3-(4-amino-3-metoksibenzoil)-2-metilindolizin-1-ilkarboksilne kiseline
– 2-{[3-(4-amino-3-metoksibenzoil)-2-metilindolizin-1-il]oksi}octene kiseline
– (4-amino-3-metoksifenil){1-[(4-klorbenzil)oksi]-2-metilindolizin-3-il}metanona
– (4-amino-3-metoksifenil){1-[(3-metoksibenzil)oksi]-2-metilindolizin-3-il}metanona
– 4-({[3-(4-amino-3-metoksibenzoil)-2-metilindolizin-1-il]oksi}metil)benzojeve kiseline
– 3-(4-karboksibenzoil)-2-metilindolizin-1-ilkarboksilne kiseline
– metil-3-[(1-metoksi-2-metilindolizin-3-il)karbonil]benzoata
– 4-[(1-metoksi-2-metilindolizin-3-il)karbonil]benzojeve kiseline
– 2-amino-5-[(1-metoksi-2-metilindolizin-3-il)karbonil]benzojeve kiseline
– 2-amino-5-({1-[(3-metoksibenzoil)amino]-2-metilindolizin-3-il}karbonil)benzojeve kiseline
– 2-amino-5-({2-metil-1-[(3,4,5-trimetoksibenzoil)amino]indolizin-3-il}karbonil)benzojeve kiseline
– 2-amino-5-({1-{[(3-metoksifenil)sulfonil]amino}-2-metilindolizin-3-il}-karbonil)benzojeve kiseline,
izborno u obliku jedne od njihovih farmaceutski prihvatljivih soli.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR0401094A FR2865934B1 (fr) | 2004-02-05 | 2004-02-05 | Utilisation de derives d'indolizine 1,2,3 substitues, inhibiteurs des fgfs, pour la preparation de medicaments utiles pour le traitement de maladies liees a une angiogenese pathologique choroidienne |
PCT/FR2005/000253 WO2005082457A2 (fr) | 2004-02-05 | 2005-02-04 | Utilisation de derives d’indolizine 1,2,3 substitues pour le traitement de maladies liees à une angiogenese pathologique choroïdienne. |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20100030T1 true HRP20100030T1 (hr) | 2010-03-31 |
Family
ID=34778525
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HR20100030T HRP20100030T1 (hr) | 2004-02-05 | 2010-01-18 | Upotreba 1,2,3-supstituiranih indolizinskih derivata u liječenju bolesti povezanih s patološkom angiogenezom |
Country Status (21)
Country | Link |
---|---|
US (1) | US8034828B2 (hr) |
EP (1) | EP1713543B1 (hr) |
JP (1) | JP5268258B2 (hr) |
KR (1) | KR101199730B1 (hr) |
CN (1) | CN1917922B (hr) |
AT (1) | ATE448003T1 (hr) |
AU (1) | AU2005216671B2 (hr) |
BR (1) | BRPI0507509A (hr) |
CA (1) | CA2553895C (hr) |
CY (1) | CY1109669T1 (hr) |
DE (1) | DE602005017581D1 (hr) |
DK (1) | DK1713543T3 (hr) |
ES (1) | ES2335900T3 (hr) |
FR (1) | FR2865934B1 (hr) |
HK (1) | HK1101065A1 (hr) |
HR (1) | HRP20100030T1 (hr) |
IL (1) | IL177088A (hr) |
PL (1) | PL1713543T3 (hr) |
PT (1) | PT1713543E (hr) |
SI (1) | SI1713543T1 (hr) |
WO (1) | WO2005082457A2 (hr) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
JP2010505961A (ja) * | 2006-10-09 | 2010-02-25 | タケダ サン ディエゴ インコーポレイテッド | キナーゼ阻害剤 |
SG158147A1 (en) | 2006-10-09 | 2010-01-29 | Takeda Pharmaceutical | Kinase inhibitors |
EP2270043A1 (en) * | 2009-07-03 | 2011-01-05 | Sanofi-Aventis | Extracellular allosteric inhibitor binding domain from a tyrosine kinase receptor |
FR2962438B1 (fr) * | 2010-07-06 | 2012-08-17 | Sanofi Aventis | Derives d'indolizines, procedes de preparation et application en therapeutique |
FR2962437B1 (fr) | 2010-07-06 | 2012-08-17 | Sanofi Aventis | Derives d'imidazopyridine, leur procede de preparation et leur application en therapeutique |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2838123B1 (fr) * | 2002-04-04 | 2005-06-10 | Sanofi Synthelabo | Nouveaux derives d'indolozine-1,2,3 substituee, inhibiteurs selectifs du b-fgf |
-
2004
- 2004-02-05 FR FR0401094A patent/FR2865934B1/fr not_active Expired - Fee Related
-
2005
- 2005-02-04 CA CA2553895A patent/CA2553895C/fr not_active Expired - Fee Related
- 2005-02-04 AT AT05717556T patent/ATE448003T1/de active
- 2005-02-04 DK DK05717556.4T patent/DK1713543T3/da active
- 2005-02-04 CN CN2005800041509A patent/CN1917922B/zh not_active Expired - Fee Related
- 2005-02-04 PL PL05717556T patent/PL1713543T3/pl unknown
- 2005-02-04 DE DE602005017581T patent/DE602005017581D1/de active Active
- 2005-02-04 JP JP2006551884A patent/JP5268258B2/ja active Active
- 2005-02-04 EP EP05717556A patent/EP1713543B1/fr active Active
- 2005-02-04 SI SI200530900T patent/SI1713543T1/sl unknown
- 2005-02-04 WO PCT/FR2005/000253 patent/WO2005082457A2/fr active Application Filing
- 2005-02-04 PT PT05717556T patent/PT1713543E/pt unknown
- 2005-02-04 AU AU2005216671A patent/AU2005216671B2/en not_active Ceased
- 2005-02-04 BR BRPI0507509-2A patent/BRPI0507509A/pt not_active IP Right Cessation
- 2005-02-04 KR KR1020067017920A patent/KR101199730B1/ko not_active IP Right Cessation
- 2005-02-04 ES ES05717556T patent/ES2335900T3/es active Active
-
2006
- 2006-07-25 IL IL177088A patent/IL177088A/en not_active IP Right Cessation
-
2007
- 2007-08-13 HK HK07108749.0A patent/HK1101065A1/xx not_active IP Right Cessation
-
2008
- 2008-08-29 US US12/201,075 patent/US8034828B2/en active Active
-
2009
- 2009-12-09 CY CY20091101327T patent/CY1109669T1/el unknown
-
2010
- 2010-01-18 HR HR20100030T patent/HRP20100030T1/hr unknown
Also Published As
Publication number | Publication date |
---|---|
CY1109669T1 (el) | 2014-08-13 |
CN1917922B (zh) | 2013-06-12 |
FR2865934B1 (fr) | 2006-05-05 |
US8034828B2 (en) | 2011-10-11 |
US20090030034A1 (en) | 2009-01-29 |
JP2007520534A (ja) | 2007-07-26 |
KR101199730B1 (ko) | 2012-11-08 |
PL1713543T3 (pl) | 2010-04-30 |
DE602005017581D1 (de) | 2009-12-24 |
AU2005216671A1 (en) | 2005-09-09 |
ATE448003T1 (de) | 2009-11-15 |
CA2553895C (fr) | 2013-04-02 |
DK1713543T3 (da) | 2010-03-22 |
IL177088A (en) | 2010-12-30 |
AU2005216671B2 (en) | 2010-09-16 |
SI1713543T1 (sl) | 2010-03-31 |
PT1713543E (pt) | 2009-12-15 |
CA2553895A1 (fr) | 2005-09-09 |
WO2005082457A2 (fr) | 2005-09-09 |
BRPI0507509A (pt) | 2007-06-26 |
EP1713543B1 (fr) | 2009-11-11 |
CN1917922A (zh) | 2007-02-21 |
HK1101065A1 (hr) | 2007-10-05 |
KR20070034986A (ko) | 2007-03-29 |
IL177088A0 (en) | 2006-12-10 |
WO2005082457A3 (fr) | 2005-11-10 |
FR2865934A1 (fr) | 2005-08-12 |
JP5268258B2 (ja) | 2013-08-21 |
EP1713543A2 (fr) | 2006-10-25 |
ES2335900T3 (es) | 2010-04-06 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HRP20100030T1 (hr) | Upotreba 1,2,3-supstituiranih indolizinskih derivata u liječenju bolesti povezanih s patološkom angiogenezom | |
AU2010252451B2 (en) | 1-(substituted benzyl)-5-trifluoromethyl-2-(1H) pyridone compounds and their salts, their preparation methods and use thereof | |
RU2440997C2 (ru) | Производные циннамоил-пиперазина и их применение в качестве антагонистов par-1 | |
EP3570843A1 (en) | Fused heterocyclic compounds as selective bmp inhibitors | |
EA200970598A1 (ru) | Замещенные производные гетероарилпиридопиримидона | |
JP2020516591A (ja) | Morアゴニストおよびkorアゴニストを含有する医薬組成物、およびその用途 | |
CZ291095A3 (en) | £3-(4-phenylpiperazin-1-yl)propylamino, thio and oxy|-pyridine, pyrimidine and benzene derivatives as alpha1-adrenoreceptor antagonists | |
ES2371941T3 (es) | Solución antiinfecciosa que comprende un compuesto de tipo pirido (3,2,1-ij) benzoxadiazina. | |
AU2009220931B2 (en) | N-substitutedbenzenepropanamide or benzenepropenamide derivatives for use in the treatment of pain and inflammation | |
EP2750670A1 (en) | Pi3k inhibitor for use in the treatment of bone cancer or for preventing metastatic dissemination primary cancer cells into the bone | |
WO2010060940A2 (en) | Hsp90 inhibitors for therapeutic treatment | |
RU2007141412A (ru) | Пиридилдиметилсульфоновое производное | |
KR20100082359A (ko) | 신경병성 통증에 활성이 있는 약물 | |
EP1414432A2 (en) | Methods of use for novel sulfur containing organic nitrate compounds | |
RU2005119163A (ru) | Новые производные антагонисты рецептора витронектина, способ их получения, их применение в качестве лекарственного средства и фармацевтические композиции, их содержание | |
EA200501040A1 (ru) | Замещенные производные 1-пиперидин-3-ил-4-пиперидин-4-илпиперазина и их применение в качестве антагонистов нейрокинина | |
TW200509917A (en) | Use of growth hormone secretagogues for treatment of fibromyalgia | |
PT2125782E (pt) | Derivados ciclo-hexilamida de ácidos arilcarboxílicos | |
CZ287729B6 (en) | Aminoalkyl aminopyridine derivatives, process of their preparation and pharmaceutical preparation in which they are comprised | |
ATE522505T1 (de) | Benzensulfonamid-verbindungen zur behandlung von erkrankungen, die auf dopamin-d3- rezeptormodulation ansprechen | |
TW200418479A (en) | Pharmaceutical compositions for the treatment or prevention of visceral pains | |
JP2003192594A (ja) | 創傷治癒時の障害の治療剤または予防剤 | |
TH66267A (hr) | ||
AU2002349876A1 (en) | Methods of use for novel sulfur containing organic nitrate compounds |