HUP0004693A2 - PARP aktivitást gátló hatú oxoszubsztituált vegyületek, ezeket tartalmazó gyógyászati készítmények, valamint eljárás a vegyületek előállítására - Google Patents
PARP aktivitást gátló hatú oxoszubsztituált vegyületek, ezeket tartalmazó gyógyászati készítmények, valamint eljárás a vegyületek előállításáraInfo
- Publication number
- HUP0004693A2 HUP0004693A2 HU0004693A HUP0004693A HUP0004693A2 HU P0004693 A2 HUP0004693 A2 HU P0004693A2 HU 0004693 A HU0004693 A HU 0004693A HU P0004693 A HUP0004693 A HU P0004693A HU P0004693 A2 HUP0004693 A2 HU P0004693A2
- Authority
- HU
- Hungary
- Prior art keywords
- ring
- compounds
- atom
- hydrogen atom
- present
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 8
- 238000002360 preparation method Methods 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 2
- 101100462870 Drosophila melanogaster Parp gene Proteins 0.000 title 1
- 230000000694 effects Effects 0.000 title 1
- 230000002401 inhibitory effect Effects 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- -1 hydroxyl- Chemical group 0.000 abstract 11
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 3
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000002632 imidazolidinyl group Chemical group 0.000 abstract 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000006545 (C1-C9) alkyl group Chemical group 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 206010003246 arthritis Diseases 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 230000002349 favourable effect Effects 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 230000007721 medicinal effect Effects 0.000 abstract 1
- 239000002207 metabolite Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/06—Peri-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
- C07D217/24—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
- C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
- C07D221/04—Ortho- or peri-condensed ring systems
- C07D221/06—Ring systems of three rings
- C07D221/10—Aza-phenanthrenes
- C07D221/12—Phenanthridines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
- C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
- C07D221/04—Ortho- or peri-condensed ring systems
- C07D221/18—Ring systems of four or more rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/30—Phthalazines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/30—Phthalazines
- C07D237/32—Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/30—Phthalazines
- C07D237/34—Phthalazines with nitrogen atoms directly attached to carbon atoms of the nitrogen-containing ring, e.g. hydrazine radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/93—Sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D475/00—Heterocyclic compounds containing pteridine ring systems
- C07D475/02—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Abstract
A találmány tárgyát gyűrűtagként legalább egy nitrogénatomottartalmazó (I) általános képletű vegyületek, valamint ezekgyógyászatilag megfelelő bázisaddíciós sói vagy savaddíciós sói,hidrátjai, észterei, szolvátjai, előgyógyszerei, metabolitjai,sztereoizomerjei vagy ezek elegyei képezik; a találmány tárgyátképezik e vegyületeket tartalmazó gyógyászati készítmények is,valamint az (I) általános képletű vegyületek alkalmazása gyógyászatikészítmények előállítására; végül a találmány tárgyához tartozik az(I) általános képletű vegyületek előállítására szolgáló eljárás is. Atalálmány szerinti vegyületek kedvező gyógyászati hatássalrendelkeznek, így alkalmazhatók különböző neurológiairendellenességek, rák, diabetes, ízületi gyulladás és számos egyébbetegség kezelésére. Az (I) általános képletben a szubsztituensekjelentése igen sokféle, így X jelentése kettős kötéssel kapcsolódóoxigénatom vagy OH; R7 jelentése amennyiben jelen van, hidrogénatomvagy rövidszénláncú alkilcsoport; Y jelentése egy kondenzált mono-,bi- vagy triciklusos, karbociklusos vagy heterociklusos gyűrűképzéséhez szükséges atom, ahol mindegyik gyűrű külön-külön 5-6gyűrűtagból áll; és Z jelentése (i) -CHR2CHR3-, ahol az (I) általánosképletű vegyületben a gyűrűtagként jelenlévő nitrogénatomhozviszonyítva R2 a meta-helyzetben és R3 az ortohelyzetben van jelen, ésahol R2 és R3 jelentése egymástól függetlenül hidrogénatom, hidroxil-,amino-, dimetil-amino-, nitro-, piperidil-, piperazinil-,imidazolidinil-, alkil-, aril- vagy aralkicsoport; (ii) -CR6C=CR3-,ahol R6 a gyűrűtagként jelenlévő nitrogénhez viszonyítva meta-helyzetben található és R3 és R6 jelentése egymástól függetlenülhidrogénatom, rövidszénláncú alkil-, aril-, aralkilcsoport,halogénatom, hidroxil-, amino-, dimetil-amino-, piperidil-,piperazinil-, imidazolidinil-csoport, -NO2, -COOR7 vagy -NR7R8, aholR8 jelentése a többi csoporttól függetlenül hidrogénatom vagy 1-9szénatomos alkilcsoport vagy R6 és R3 jelentése együtt egy aromásgyűrűt képez, ahol mindegyik gyűrű 5-6 gyűrűtagból áll; (iii) -R2C=N-;(iv) -CR2(OH)-NR7-; (v) -C(O-NR7-; vagy (vi) -NR9-C(O)-CHR10-, aholR10, a gyűrűtagként jelenlévő nitrogénatomhoz viszonyítva orto-helyzetben van jelen, továbbá R9 és R10 jelentése egymástólfüggetlenül hidrogénatom, rövidszénláncú alkil-, aril-,aralkilcsoport, halogénatom, hidroxil-, piperidil-, piperazinil-imidazolidinil-csoport, -NO2, -COOR7 vagy -NR7R8, ahol R8 jelentéseegyéb csoportoktól függetlenül hidrogénatom vagy 1-9 szénatomosalkilcsoport vagy R9 és R10 együttes jelentése egy kondenzált gyűrű,ahol mindegyik gyűrű külön-külön 5-7 gyűrűtagból áll. Ó
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US92252097A | 1997-09-03 | 1997-09-03 | |
| US7950998A | 1998-05-15 | 1998-05-15 | |
| US09/145,180 US20020022636A1 (en) | 1997-09-03 | 1998-09-01 | Oxo-substituted compounds, process of making, and compositions and methods for inhibiting parp activity |
| PCT/US1998/018195 WO1999011624A1 (en) | 1997-09-03 | 1998-09-02 | Oxo-substituted compounds, process of making, and compositions and methods for inhibiting parp activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0004693A2 true HUP0004693A2 (hu) | 2001-10-28 |
| HUP0004693A3 HUP0004693A3 (en) | 2001-12-28 |
Family
ID=27373494
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0004693A HUP0004693A3 (en) | 1997-09-03 | 1998-09-02 | Oxo-substituted compounds inhibiting parp activity, pharmaceutical compositions containing them and process for preparation the compounds |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US20020022636A1 (hu) |
| EP (1) | EP1009739A2 (hu) |
| JP (1) | JP2002512637A (hu) |
| KR (1) | KR20010023909A (hu) |
| CN (1) | CN1278797A (hu) |
| AU (1) | AU9298698A (hu) |
| BR (1) | BR9812428A (hu) |
| CA (1) | CA2294118A1 (hu) |
| HU (1) | HUP0004693A3 (hu) |
| IL (1) | IL134847A0 (hu) |
| NO (1) | NO20001002L (hu) |
| PL (1) | PL339082A1 (hu) |
| TR (1) | TR200001557T2 (hu) |
| WO (1) | WO1999011624A1 (hu) |
Families Citing this family (82)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6291425B1 (en) * | 1999-09-01 | 2001-09-18 | Guilford Pharmaceuticals Inc. | Compounds, methods and pharmaceutical compositions for treating cellular damage, such as neural or cardiovascular tissue damage |
| CA2332279A1 (en) * | 1998-05-15 | 1999-11-25 | Jia-He Li | Carboxamide compounds, compositions, and methods for inhibiting parp activity |
| SI20691B (sl) | 1999-01-11 | 2008-10-31 | Agouron Pharma | Triciklični inhibitorji poli(ADP-riboza) polimeraz |
| AU3076700A (en) | 1999-01-26 | 2000-08-18 | Ono Pharmaceutical Co. Ltd. | 2h-phthalazin-1-one derivatives and drugs comprising these derivatives as the active ingredient |
| JP2001002572A (ja) * | 1999-04-19 | 2001-01-09 | Sankyo Co Ltd | ニューロトロフィン作用増強剤 |
| ECSP003637A (es) | 1999-08-31 | 2002-03-25 | Agouron Pharma | Inhibidores triciclicos de poli (adp-ribosa) polimerasas |
| US6277990B1 (en) | 1999-12-07 | 2001-08-21 | Inotek Corporation | Substituted phenanthridinones and methods of use thereof |
| US6476048B1 (en) | 1999-12-07 | 2002-11-05 | Inotek Pharamaceuticals Corporation | Substituted phenanthridinones and methods of use thereof |
| US6531464B1 (en) * | 1999-12-07 | 2003-03-11 | Inotek Pharmaceutical Corporation | Methods for the treatment of neurodegenerative disorders using substituted phenanthridinone derivatives |
| US6534651B2 (en) * | 2000-04-06 | 2003-03-18 | Inotek Pharmaceuticals Corp. | 7-Substituted isoindolinone inhibitors of inflammation and reperfusion injury and methods of use thereof |
| US7122679B2 (en) | 2000-05-09 | 2006-10-17 | Cephalon, Inc. | Multicyclic compounds and the use thereof |
| AU2001264595A1 (en) * | 2000-05-19 | 2001-12-03 | Guilford Pharmaceuticals Inc. | Sulfonamide and carbamide derivatives of 6(5h)phenanthridinones and their uses |
| CA2419838A1 (en) | 2000-08-31 | 2003-02-18 | Takeda Chemical Industries, Ltd. | Heart muscular cell apoptosis inhibitors and remedies/preventives for heart diseases |
| US7151102B2 (en) | 2000-10-30 | 2006-12-19 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| WO2002044183A2 (en) * | 2000-12-01 | 2002-06-06 | Guilford Pharmaceuticals Inc. | Benzoazepine and benzodiazepine derivatives and their use as parp inhibitors |
| CA2330350A1 (en) | 2000-12-05 | 2002-06-05 | Chemokine Therapeutics Corporation | Therapeutics for chemokine mediated diseases |
| WO2002045702A2 (en) * | 2000-12-05 | 2002-06-13 | Chemokine Therapeutics Corporation | Tricyclic therapeutics for chemokine mediated diseases |
| AUPR201600A0 (en) * | 2000-12-11 | 2001-01-11 | Fujisawa Pharmaceutical Co., Ltd. | Quinazolinone derivative |
| DE60218458T2 (de) | 2001-05-08 | 2007-11-15 | Kudos Pharmaceuticals Ltd. | Isochinolinon derivate als parp inhibitoren |
| AUPS019702A0 (en) * | 2002-01-29 | 2002-02-21 | Fujisawa Pharmaceutical Co., Ltd. | Condensed heterocyclic compounds |
| AUPS137402A0 (en) * | 2002-03-26 | 2002-05-09 | Fujisawa Pharmaceutical Co., Ltd. | Novel tricyclic compounds |
| US7196085B2 (en) | 2002-04-30 | 2007-03-27 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| MXPA05000983A (es) * | 2002-07-24 | 2005-08-18 | Kyorin Seiyaku Kk | Derivados de 4-(aril substituido)-5-hidroxiisoquinolinona. |
| PT1557414E (pt) * | 2002-10-01 | 2012-04-17 | Mitsubishi Tanabe Pharma Corp | Compostos de isoquinolina e sua utilização medicinal |
| EP2325224A1 (en) | 2002-10-30 | 2011-05-25 | Sumitomo Chemical Company, Limited | Aryl copolymer compounds and polymer light emitting devices made by using the same |
| US7501412B2 (en) | 2002-11-22 | 2009-03-10 | Mitsubishi Tanabe Pharma Corporation | Isoquinoline compounds and medicinal use thereof |
| US7449464B2 (en) | 2003-03-12 | 2008-11-11 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| GB0305681D0 (en) | 2003-03-12 | 2003-04-16 | Kudos Pharm Ltd | Phthalazinone derivatives |
| HU227948B1 (en) | 2003-04-30 | 2012-07-30 | Pecsi Tudomanyegyetem | Quinazoline derivatives and their use for the preparation of pharmaceutical compositions inhibiting parp enzyme |
| US20050008699A1 (en) * | 2003-07-11 | 2005-01-13 | Fred Wehling | Effervescent glucosamine composition |
| WO2005054201A1 (en) | 2003-11-20 | 2005-06-16 | Janssen Pharmaceutica N.V. | 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(adp-ribose) polymerase inhibitors |
| CN1890224B (zh) * | 2003-12-05 | 2011-06-08 | 詹森药业有限公司 | 用作聚(adp-核糖)聚合酶抑制剂的6-取代的2-喹啉酮和2-喹喔啉酮 |
| TW200536830A (en) | 2004-02-06 | 2005-11-16 | Chugai Pharmaceutical Co Ltd | 1-(2H)-isoquinolone derivative |
| DE102004028973A1 (de) | 2004-06-16 | 2006-01-05 | Sanofi-Aventis Deutschland Gmbh | Substituierte Tetrahydro-2H-isochinolin-1-on-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Medikament |
| TWI389897B (zh) | 2005-02-22 | 2013-03-21 | Chugai Pharmaceutical Co Ltd | 1- (2H) -isoquinolinone derivatives |
| GB0521373D0 (en) | 2005-10-20 | 2005-11-30 | Kudos Pharm Ltd | Pthalazinone derivatives |
| US9150628B2 (en) | 2005-11-14 | 2015-10-06 | Centre National De La Recherche Scientifique (Cnrs) | PARP inhibitors |
| AR059898A1 (es) * | 2006-03-15 | 2008-05-07 | Janssen Pharmaceutica Nv | Derivados de 3-ciano-piridona 1,4-disustituida y su uso como moduladores alostericos de los receptores mglur2 |
| DK2061765T3 (en) * | 2006-09-01 | 2015-01-26 | Senhwa Biosciences Inc | Serine-threonine protein kinase AND PARP-MODULATOR |
| UY30639A1 (es) | 2006-10-17 | 2008-05-31 | Kudos Pharm Ltd | Derivados sustituidos de 2h-ftalazin-1-ona, sus formas cristalinas, proceso de preparacion y aplicaciones |
| CN101616919B (zh) * | 2006-12-28 | 2012-10-10 | 雅培制药有限公司 | 聚（adp核糖）聚合酶抑制剂 |
| WO2008091555A2 (en) * | 2007-01-22 | 2008-07-31 | Gtx, Inc. | Nuclear receptor binding agents |
| US9604931B2 (en) | 2007-01-22 | 2017-03-28 | Gtx, Inc. | Nuclear receptor binding agents |
| CN101641339B (zh) | 2007-02-01 | 2013-07-17 | 雷斯韦洛吉克斯公司 | 用于预防和治疗心血管疾病的化合物 |
| TW200845978A (en) * | 2007-03-07 | 2008-12-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives |
| TW200900065A (en) | 2007-03-07 | 2009-01-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives |
| EP2134691B1 (en) | 2007-03-08 | 2012-01-25 | Janssen Pharmaceutica, N.V. | Quinolinone derivatives as parp and tank inhibitors |
| JP2010526825A (ja) * | 2007-05-10 | 2010-08-05 | エーエムアール テクノロジー インコーポレイテッド | アリール置換およびヘテロアリール置換テトラヒドロベンゾ−１，４−ジアゼピンならびにノルエピネフリン、ドーパミンおよびセロトニンの再取り込みを遮断するためのその使用 |
| TW200927731A (en) * | 2007-09-14 | 2009-07-01 | Ortho Mcneil Janssen Pharm | 1,3-disubstituted-4-phenyl-1H-pyridin-2-ones |
| CN101801951B (zh) | 2007-09-14 | 2013-11-13 | 杨森制药有限公司 | 1’,3’-二取代的-4-苯基-3,4,5,6-四氢-2h,1’h-[1,4’]二吡啶-2’-酮 |
| KR20100065191A (ko) | 2007-09-14 | 2010-06-15 | 오르토-맥닐-얀센 파마슈티칼스 인코포레이티드 | １,３-이치환된 ４-(아릴-ｘ-페닐)-１ｈ-피리딘-２-온 |
| AU2008299721A1 (en) | 2007-09-14 | 2009-03-19 | Astrazeneca Ab | Phthalazinone derivatives |
| PL2215075T3 (pl) * | 2007-10-26 | 2014-04-30 | Janssen Pharmaceutica Nv | Pochodne chinolinonu jako inhibitory PARP |
| ES2637794T3 (es) * | 2007-11-14 | 2017-10-17 | Janssen Pharmaceuticals, Inc. | Derivados de imidazo[1,2-A]piridina y su uso como moduladores alostéricos positivos de receptores MGLUR2 |
| UY31603A1 (es) | 2008-01-23 | 2009-08-31 | Derivados de ftalazinona | |
| RU2510396C2 (ru) | 2008-09-02 | 2014-03-27 | Янссен Фармасьютикалз, Инк. | 3-азабицикло[3.1.0]гексильные производные в качестве модуляторов метаботропных глутаматных рецепторов |
| HUE030800T2 (hu) | 2008-10-07 | 2017-05-29 | Astrazeneca Uk Ltd | 514 számú gyógyszerkészítmény |
| JP2012505257A (ja) * | 2008-10-13 | 2012-03-01 | バイオヴィスタ，インコーポレイテッド | 多発性硬化症治療のための組成物および方法 |
| BRPI0920354A2 (pt) | 2008-10-16 | 2017-06-27 | Addex Pharmaceuticals Sa | derivados de indol e benzomorfolina como moduladores de receptores de glutamato metabotrópicos |
| WO2010056038A2 (ko) * | 2008-11-11 | 2010-05-20 | 제일약품주식회사 | 신규한 트리시클릭 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 포함하는 약학적 조성물 |
| AU2009319387B2 (en) | 2008-11-28 | 2012-05-10 | Addex Pharma S.A. | Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors |
| EP2377871A4 (en) | 2008-11-28 | 2012-07-25 | Chugai Pharmaceutical Co Ltd | 1- (2H) -ISOCHINOLONDERIVAT |
| MX2021012876A (es) | 2009-03-18 | 2022-06-23 | Resverlogix Corp | Nuevos agentes anti-inflamatorios. |
| MY153913A (en) | 2009-05-12 | 2015-04-15 | Janssen Pharmaceuticals Inc | 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
| RS53075B (en) | 2009-05-12 | 2014-04-30 | Janssen Pharmaceuticals Inc. | 1,2,4-TRIAZOLO [4,3-A] PYRIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OR PREVENTION OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS |
| JP5707390B2 (ja) | 2009-05-12 | 2015-04-30 | ジャンセン ファーマシューティカルズ， インコーポレイテッド | １，２，４−トリアゾロ［４，３−ａ］ピリジン誘導体およびｍＧｌｕＲ２受容体の正のアロステリック調節因子としてのその使用 |
| EP2649069B1 (en) | 2010-11-08 | 2015-08-26 | Janssen Pharmaceuticals, Inc. | 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS |
| EP2661435B1 (en) | 2010-11-08 | 2015-08-19 | Janssen Pharmaceuticals, Inc. | 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS |
| EP2643320B1 (en) | 2010-11-08 | 2015-03-04 | Janssen Pharmaceuticals, Inc. | 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS |
| CN103781776A (zh) | 2011-07-13 | 2014-05-07 | 诺华股份有限公司 | 用作端锚聚合酶抑制剂的新的2-哌啶-1-基-乙酰胺化合物 |
| US9227982B2 (en) | 2011-07-13 | 2016-01-05 | Novartis Ag | 4-oxo-3,5,7,8-tetrahydro-4H-pyrano[4,3-d]pyrminidinyl compounds for use as tankyrase inhibitors |
| WO2013008217A1 (en) | 2011-07-13 | 2013-01-17 | Novartis Ag | 4 - piperidinyl compounds for use as tankyrase inhibitors |
| JO3368B1 (ar) | 2013-06-04 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2 |
| JO3367B1 (ar) | 2013-09-06 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2 |
| DK3431106T3 (da) | 2014-01-21 | 2021-03-15 | Janssen Pharmaceutica Nv | Kombinationer omfattende positive allosteriske modulatorer eller orthosteriske agonister af metabotrop glutamaterg subtype 2-receptor og anvendelse af disse |
| ES2860298T3 (es) | 2014-01-21 | 2021-10-04 | Janssen Pharmaceutica Nv | Combinaciones que comprenden moduladores alostéricos positivos del receptor glutamatérgico metabotrópico de subtipo 2 y su uso |
| US10111885B2 (en) | 2015-03-13 | 2018-10-30 | Resverlogix Corp. | Compositions and therapeutic methods for the treatment of complement-associated diseases |
| EP3263104A1 (en) * | 2016-07-01 | 2018-01-03 | N-Gene Research Laboratories Inc. | Use of bgp15 to stimulate mitochondrial fusion |
| US10874641B2 (en) | 2016-07-28 | 2020-12-29 | Mitobridge, Inc. | Methods of treating acute kidney injury |
| CN106798745A (zh) * | 2016-08-31 | 2017-06-06 | 四川省人民医院 | 一种用于治疗肿瘤疾病的药物 |
| MA46779A (fr) | 2016-11-02 | 2019-09-11 | Health Research Inc | Traitement combiné avec des conjugués anticorps-médicament et des inhibiteurs de parp |
| CN109293584B (zh) * | 2018-09-25 | 2021-11-26 | 暨南大学 | 靶向神经肽受体pac1-r的小分子别构调节化合物spam及其制备方法和用途 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US1880441A (en) * | 1932-10-04 | Etjbole m | ||
| US3291801A (en) * | 1963-05-23 | 1966-12-13 | Grace W R & Co | Novel octahydro-6(5)-phenanthridinones and preparation thereof |
| DE2355084A1 (de) * | 1972-11-06 | 1974-05-16 | Guidotti & C Spa Labor | Verbindungen mit magensaeuresekretionshemmender wirkung und verfahren zu deren herstellung |
| US3932643A (en) * | 1974-01-07 | 1976-01-13 | Pfizer Inc. | Phenanthridines and phenanthridinones as antiviral agents |
| SU514825A1 (ru) * | 1974-02-04 | 1976-05-25 | Химико-Фармацевтический Завод "Фармакон" | Способ получени хлоргидрата 1-фенил1-циклогексил-3-(1,-пиперидино) -пропанола-1 |
| GB9404485D0 (en) * | 1994-03-09 | 1994-04-20 | Cancer Res Campaign Tech | Benzamide analogues |
| US5589483A (en) * | 1994-12-21 | 1996-12-31 | Geron Corporation | Isoquinoline poly (ADP-ribose) polymerase inhibitors to treat skin diseases associated with cellular senescence |
-
1998
- 1998-09-01 US US09/145,180 patent/US20020022636A1/en not_active Abandoned
- 1998-09-02 AU AU92986/98A patent/AU9298698A/en not_active Abandoned
- 1998-09-02 KR KR1020007002595A patent/KR20010023909A/ko not_active Application Discontinuation
- 1998-09-02 EP EP98945833A patent/EP1009739A2/en not_active Withdrawn
- 1998-09-02 PL PL98339082A patent/PL339082A1/xx unknown
- 1998-09-02 WO PCT/US1998/018195 patent/WO1999011624A1/en not_active Application Discontinuation
- 1998-09-02 CA CA002294118A patent/CA2294118A1/en not_active Abandoned
- 1998-09-02 CN CN98810936A patent/CN1278797A/zh active Pending
- 1998-09-02 IL IL13484798A patent/IL134847A0/xx unknown
- 1998-09-02 BR BR9812428-5A patent/BR9812428A/pt not_active IP Right Cessation
- 1998-09-02 TR TR2000/01557T patent/TR200001557T2/xx unknown
- 1998-09-02 HU HU0004693A patent/HUP0004693A3/hu unknown
- 1998-09-02 JP JP51697799A patent/JP2002512637A/ja active Pending
-
2000
- 2000-02-28 NO NO20001002A patent/NO20001002L/no not_active Application Discontinuation
-
2002
- 2002-04-01 US US10/109,730 patent/US20030105102A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| TR200001557T2 (tr) | 2001-01-22 |
| JP2002512637A (ja) | 2002-04-23 |
| US20020022636A1 (en) | 2002-02-21 |
| BR9812428A (pt) | 2000-09-26 |
| NO20001002D0 (no) | 2000-02-28 |
| US20030105102A1 (en) | 2003-06-05 |
| IL134847A0 (en) | 2001-05-20 |
| CA2294118A1 (en) | 1999-03-11 |
| EP1009739A2 (en) | 2000-06-21 |
| WO1999011624A1 (en) | 1999-03-11 |
| AU9298698A (en) | 1999-03-22 |
| WO1999011624B1 (en) | 1999-04-22 |
| HUP0004693A3 (en) | 2001-12-28 |
| CN1278797A (zh) | 2001-01-03 |
| KR20010023909A (ko) | 2001-03-26 |
| NO20001002L (no) | 2000-04-27 |
| PL339082A1 (en) | 2000-12-04 |
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