DK2442644T3 - Opsin-bindende ligander, sammensætninger og fremgangsmåder til anvendelse - Google Patents

Opsin-bindende ligander, sammensætninger og fremgangsmåder til anvendelse Download PDF

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DK2442644T3
DK2442644T3 DK10789866.0T DK10789866T DK2442644T3 DK 2442644 T3 DK2442644 T3 DK 2442644T3 DK 10789866 T DK10789866 T DK 10789866T DK 2442644 T3 DK2442644 T3 DK 2442644T3
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trimethylcyclohex
opsin
acryloyl
enyl
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DK10789866.0T
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David S Garvey
Gregory J Larosa
Jeremy Robert Greenwood
Mark L Brewer
Tan Quach
Jamie B Cote
Judd Berman
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Bikam Pharmaceuticals Inc
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Claims (12)

1. Forbindelse med strukturen med formel I A-B-Q-V Formel I hvor A er:
B er -CH=CH-, -CH2-N(R22)- eller -CH2-CH2-, Q er -C(O)- eller -CH2-; V er
hvor b er 1 eller 2 og a er 1 eller 2; Y er NR22, N-Q-U, CR22R23, oxygen, S(0)„, N-C(S)-NR22R23; N-(C=N-CN)-NR22R23, N-(C=N-S02CH3)-NR22R23, C=NOR22, C=N-NR22R23 eller C-Q-U, n er 0, 1 eller 2; U er NR22R23, lavere alkyl, haloalkyl, OR22 eller hydrogen; X er hydrogen, alkyl eller -C^CR9; W er -OR22, -NR22R23, -N(R22)-C(0)-NR22R23, -0-C(0)-NR22R23, -N(R22)-C(S)-NR22R23, -0-C(S)-NR22R23, -S-C(0)-NR22R23, -N(R22)-(C=N-CN)-NR22R23, -N(R22)-(C=N-S02Me)-NR22R23, eller -C(0)N(R9)N(R14)(R16); hvor p er 0 eller 1; R14 og R16 er hver uafhængigt hydrogen, eller -CH3; R1 og R2 er uafhængigt -CHs eller -CH2CH3; R3 er hydrogen, -CH3 eller -CH2CH3; Ra, og Rb, er hver uafhængigt hydrogen, deutero eller -CH3; Rc, og Rd, er hver uafhængigt hydrogen, alkoxy, lavere alkyl eller alkenyl; R9 er hydrogen, eller -CH3; R22 og R23 er hver uafhængigt hydrogen; eller lavere alkyl; R24 og R25 er hver uafhængigt hydrogen eller -CH3; R26 er NR22R23 eller alkoxy; og hvor R1 og R2 taget sammen eller Ra og Rb taget sammen med det carbonatom til hvilket de er bundet er cyclopropyl; R24 og R25 taget sammen med det carbonatom til hvilket de er bundet er cyclopropyl: R24 og R25 taget sammen er oxo; herunder farmaceutisk acceptable salte, solvater og hydrater deraf; og hvor lavere alkyl er er en forgrenet eller ligekædet acyklisk alkylgruppe omfattende et til ti carbonatomer; haloalkyl er en lavere alkylgruppe, en alkenylgruppe, en alkynylgruppe, en brodannet cycloalkylgruppe, en cycloalkylgruppe til hvilke er vedhæftet én eller flere halogener; alkoxy er R50O-, hvor Rso er en alkylgruppe; alkyl er en ubrudt ikke-cyklisk kæde af carbonatomer der kan være forgrenede, uforgrenede, substituerede eller andre kemiske grupper såsom lavere alkyl, hydroxyl, ester, amidyl, oxo, carboxyl, carboxamido, halo, cyano, nitrat, nitrit, thionitrat, thionitrit, sulfhydryl og amino, eller usubstituerede; alkenyl er et forgrenet eller ligekædet C2-C10 carbonhydrid der kan omfatte én eller flere carbon-carbon-dobbeltbindinger; alkynyl er et umættet acyklisk C2-C10 carbonhydrid der kan indeholde én eller flere carbon-carbon-tredobbelte bindinger; cycloalkyl er er et mættet eller umættet cyklisk carbonhydrid omfattende fra 3 til 10 carbonatomer; heterocyklisk ring er en mættet eller umættet cyklisk eller polycyklisk carbonhydridgruppe med 2 til 12 carbonatomer hvor 1 til 4 carbonatomer er erstattet af ét eller flere nitrogen-, oxygen- og/eller svovlatomer.
2. Forbindelsen ifølge krav 1, hvor hver af R1, R2 og R3 er methyl, eller hvor hver af R24 er hydrogen, eller hvor Ra og Rb er hver uafhængigt hydrogen eller methyl, eller hvor Ra og Rb hver er methyl, eller hvor Rc og Rd hver er uafhængigt hydrogen eller lavere alkyl, eller hvor Rc og Rd hver er lavere alkyl eller hvor Rc og Rd hver er hydrogen; og hvor V er:
og hvor lavere alkyl er defineret i krav 1.
3. Forbindelsen ifølge krav 1, hvor V er:
eller hvor B er CH = CH, eller hvor Q er -C(O)-, eller hvor X er H, eller lavere alkyl eller -C=CR9, eller hvor X er H eller methyl, eller hvor Y er O eller N-C(0)-NR22R23; og hvor lavere alkyl er som defineret i krav 1.
4. Forbindelsen ifølge krav 1, hvor V er
og hvor Ra og Rb er hver uafhængigt hydrogen, deutero eller methyl, eller hvor Ra eller Rb hver er hydrogen, eller hvor Rc og Rd er hver uafhængigt hydrogen, alkoxy eller lavere alkyl, og hvor alkoxy og lavere alkyl er som defineret i krav 1.
5. Forbindelse ifølge krav 1, med strukturen
(E)-4-(3-(2,6,6-trimethylcyclohex-l-enyl)acryloyl)piperazin-l-carboxamid (forbindelse 33);
(S/E)-2-methyl-4-(3-(2,6,6-trimethylcyclohex-l-enyl)acryloyl)piperazin-l-carboxamid (forbindelse 52);
(E)-4-(3-(3,3-dideutero-2,6,6-trimethylcyclohex-l-en-l-yl)acryloyl)piperazin-l-carboxamid (forbindelse 63);
(±)-4-((E)-3-((l,6-ant/')-2,2,6-trimethylcyclohexyl)acryloyl)piperazin-l-carboxamid (forbindelse 71);
(-)-4-((E)-3-((lR, 6R)-2,2,6-trimethylcyclohexyl)acryloyl)piperazin-l-carboxamid (forbindelse 72);
(+)-4-((5)-3-((lS,6S)-2,2,6-trimethylcyclohexyl)acryloyl)piperazin-l-carboxamid (forbindelse 73); eller
4-(3-(( IR, 6S)-2,2,6-trimethylcyclohexyl)propanoyl)piperazin-l-carboxamid (forbindelse 80); herunder farmaceutisk acceptable salte, solvater og hydrater deraf.
6. Forbindelse ifølge krav 1, med strukturen
(E)-l-morpholino-3-(2,6,6-trimethylcyclohex-l-enyl)prop-2-en-l-on (forbindelse 6);
(E)-l-(l-(3-(2,6,6-trimethylcyclohex-l-enyl)acryloyl) pyrrolidin-3-yl)urinstof (forbindelse 50); eller
(E)-2-ethynyl-4-(3-(2,6,6-trimethylcyclohex-l-en-l-yl)acryloyl)piperazin-l-carboxamid (forbindelse 106); herunder farmaceutisk acceptable salte, solvater og hydrater deraf. 7
7. Forbindelse ifølge krav 1, med strukturen
(E)-4-(3-(2,6,6-trimethylcyclohex-l-enyl)acryloyl)-l,4-diazepan-l-carboxamid (forbindelse 13);
(E)-/V-isopropyl-4-(3-(2,6,6-trimethylcyclohex-l-enyl)acryloyl)piperazin-l-carboxamid (forbindelse 37);
(R,E)-2-methyl-4-(3-(2,6,6-trimethylcyclohex-l-enyl)acryloyl)piperazin-l-carboxamid (forbindelse 53); eller
A/J-((2,6,6-trimethylcyclohex-l-en-l-yl)methyl)piperazin-l ,4-dicarboxamid (forbindelse 55); herunder farmaceutisk acceptable salte, solvater og hydrater deraf.
8. Sammensætning til anvendelse i inhibering af dannelsen eller akkumulering af en toksisk visuel cyklusprodukttilstand i et individ med risiko derfor eller afficeret dermed, omfattende en effektiv mængde af forbindelse ifølge krav 1, 5, 6 eller 7.
9. Sammensætningen til anvendelse ifølge krav 8, hvor inhiberingen foregår i en celle.
10. Sammensætningen til anvendelse ifølge krav 8, hvor det visuelle cyklusprodukt er lipofuscin eller N-retinyliden-N-retinylethanolamin (A2E).
11. Sammensætning til anvendelse i behandling eller forebyggelse af en ophthalmisk tilstand i et individ med risiko derfor eller afficeret dermed, omfattende en effektiv mængde afen forbindelse ifølge krav 1, 5, 6 eller 7.
12. Sammensætningen til anvendelse ifølge krav 11, hvor den ophthalmiske tilstand er valgt fra gruppen bestående af våd- eller tør-alders-relateret makulær degeneration (ARMD), retinitis pigmentosa (RP), en retinal- eller makulær dystrofi, Stargardt's sygdom, Sorsby's dystrofi, autosomal dominant drusen, Best's dystrofi, peripherin mutation associeret med makulær dystrofi, dominant form af Stargart's sygdom, North Carolina makulær dystrofi, let toksicitet, normal synstabs-relateret aldring og normal tab af nattesyn relateret til aldring.
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Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2007277032A1 (en) * 2006-07-27 2008-01-31 University Of Florida Research Foundation, Inc. Opsin stabilizing compounds and methods of use
IN2012DN00352A (da) 2009-06-16 2015-08-21 Bikam Pharmaceuticals Inc
WO2012134971A2 (en) * 2011-03-25 2012-10-04 Bikam Pharmaceuticals, Inc. Opsin-binding ligands, compositions and methods of use
AU2012271728B2 (en) * 2011-06-14 2016-10-20 Bikam Pharmaceuticals, Inc. Opsin-binding ligands, compositions and methods of use
AU2012325341B2 (en) * 2011-10-19 2017-01-05 Bikam Pharmaceuticals, Inc. Opsin-binding ligands, compositions and methods of use
EP2785346A4 (en) * 2011-11-30 2015-04-29 Bikam Pharmaceuticals Inc OPSINBINDING LIGANDS, COMPOSITIONS THEREOF, AND METHOD OF USE THEREOF
AU2012346537A1 (en) * 2011-12-01 2014-07-17 Bikam Pharmaceuticals, Inc. Opsin-binding ligands, compositions and methods of use
US9447079B2 (en) 2013-03-14 2016-09-20 Epizyme, Inc. PRMT1 inhibitors and uses thereof
US9776972B2 (en) 2013-03-14 2017-10-03 Epizyme Inc. Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
US9023883B2 (en) 2013-03-14 2015-05-05 Epizyme, Inc. PRMT1 inhibitors and uses thereof
BR112015022785A2 (pt) 2013-03-14 2017-07-18 Epizyme Inc composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014153214A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyl transferase inhibtors and uses thereof
WO2014153235A2 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2015138934A1 (en) 2014-03-13 2015-09-17 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing cftr activity
AU2015229188A1 (en) 2014-03-13 2016-09-29 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing CFTR activity
WO2015196071A1 (en) 2014-06-19 2015-12-23 Proteostasis Therapeutics, Inc. Compounds, compositions and methods of increasing cftr activity
WO2016105468A1 (en) 2014-12-23 2016-06-30 Proteostasis Therapeutics, Inc. Derivatives of 3-heteroarylisoxazol-5-carboxylic amide useful for the treatment of inter alia cystic fibrosis
WO2016105484A1 (en) 2014-12-23 2016-06-30 Proteostasis Therapeutics, Inc. Derivatives of 5-(hetero)arylpyrazol-3-carboxylic amide or 1-(hetero)aryltriazol-4-carboxylic amide useful for the treatment of inter alia cystic fibrosis
MA41253A (fr) 2014-12-23 2017-10-31 Proteostasis Therapeutics Inc Composés, compositions et procédés pour augmenter l'activité du cftr
US10392378B2 (en) 2014-12-23 2019-08-27 Proteostasis Therapeutics, Inc. Derivatives of 5-phenyl- or 5-heteroarylathiazol-2-carboxylic amide useful for the treatment of inter alia cystic fibrosis
AU2016297886B2 (en) 2015-07-24 2020-12-10 Proteostasis Therapeutics, Inc. Compounds, compositions and methods of increasing CFTR activity
EP3359536B1 (en) 2015-10-06 2021-08-04 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for modulating cftr
AR108203A1 (es) 2016-04-07 2018-07-25 Proteostasis Therapeutics Inc Compuestos, composiciones y métodos para modular cftr (regulador de la conductancia transmembrana de la fibrosis quística)
US10899751B2 (en) 2016-06-21 2021-01-26 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing CFTR activity
JOP20190245A1 (ar) 2017-04-20 2019-10-15 Novartis Ag أنظمة توصيل إطلاق مستدام تتضمن روابط بلا أثر لنقطة الربط
SG11202003286YA (en) 2017-10-16 2020-05-28 Takasago Perfumery Co Ltd Cool-sensation imparter composition containing 2,2,6-trimethylcyclohexanecarboxylic acid derivative
TW202027794A (zh) 2018-10-03 2020-08-01 瑞士商諾華公司 血管生成素樣３多肽之持續遞送
EP4183449A1 (en) 2021-11-17 2023-05-24 Samsara Therapeutics Inc. Autophagy inducing compounds and uses thereof

Family Cites Families (109)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3022291A (en) * 1962-02-20 cuhno
US3416530A (en) 1966-03-02 1968-12-17 Richard A. Ness Eyeball medication dispensing tablet
US3854480A (en) 1969-04-01 1974-12-17 Alza Corp Drug-delivery system
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
US3850611A (en) * 1970-03-25 1974-11-26 Fujisawa Pharmaceutical Co Method for inhibiting plant growth with quaternary ammonium salts
US3828777A (en) 1971-11-08 1974-08-13 Alza Corp Microporous ocular device
BE802469A (fr) * 1972-07-20 1974-01-18 Wilkinson Sword Ltd Perfectionnements apportes et/ou relatifs a des composes exercant un effet refrigerant physiologique et compositions contenant ceux-ci
US3832253A (en) 1973-03-21 1974-08-27 Baxter Laboratories Inc Method of making an inflatable balloon catheter
US4014335A (en) 1975-04-21 1977-03-29 Alza Corporation Ocular drug delivery device
US4244890A (en) 1977-12-14 1981-01-13 Scm Corporation Cyclic terpenoid amines, their preparation and uses
US4263428A (en) 1978-03-24 1981-04-21 The Regents Of The University Of California Bis-anthracycline nucleic acid function inhibitors and improved method for administering the same
DE2830764A1 (de) 1978-07-13 1980-01-31 Basf Ag Acetanilide
US4300557A (en) 1980-01-07 1981-11-17 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Method for treating intraocular malignancies
DE3169595D1 (en) 1980-11-10 1985-05-02 Gersonde Klaus Method of preparing lipid vesicles by ultrasonic treatment, the use of this method and apparatus for its application
US4327725A (en) 1980-11-25 1982-05-04 Alza Corporation Osmotic device with hydrogel driving member
IE52535B1 (en) 1981-02-16 1987-12-09 Ici Plc Continuous release pharmaceutical compositions
US4485045A (en) 1981-07-06 1984-11-27 Research Corporation Synthetic phosphatidyl cholines useful in forming liposomes
EP0088046B1 (de) 1982-02-17 1987-12-09 Ciba-Geigy Ag Lipide in wässriger Phase
DE3218121A1 (de) 1982-05-14 1983-11-17 Leskovar, Peter, Dr.-Ing., 8000 München Arzneimittel zur tumorbehandlung
US4667014A (en) 1983-03-07 1987-05-19 Syntex (U.S.A.) Inc. Nonapeptide and decapeptide analogs of LHRH, useful as LHRH antagonists
EP0102324A3 (de) 1982-07-29 1984-11-07 Ciba-Geigy Ag Lipide und Tenside in wässriger Phase
US4452775A (en) 1982-12-03 1984-06-05 Syntex (U.S.A.) Inc. Cholesterol matrix delivery system for sustained release of macromolecules
CA1200416A (en) 1983-05-13 1986-02-11 Societe Des Produits Nestle S.A. Food process
US4544545A (en) 1983-06-20 1985-10-01 Trustees University Of Massachusetts Liposomes containing modified cholesterol for organ targeting
HUT35524A (en) 1983-08-02 1985-07-29 Hoechst Ag Process for preparing pharmaceutical compositions containing regulatory /regulative/ peptides providing for the retarded release of the active substance
EP0350973B1 (de) 1983-09-26 1997-11-05 Udo Dr. Ehrenfeld Mittel und Erzeugnis für die Diagnose und Therapie von Tumoren sowie zur Behandlung von Schwächen der zelligen und humoralen Immunabwehr
DE3474511D1 (en) 1983-11-01 1988-11-17 Terumo Corp Pharmaceutical composition containing urokinase
DE3576332D1 (de) 1984-09-12 1990-04-12 Firmenich & Cie Stickstoff-verbindungen, ihre herstellung und verwendung als ausgangsprodukte zur herstellung von decalinketonen.
US5147647A (en) 1986-10-02 1992-09-15 Sohrab Darougar Ocular insert for the fornix
US5322691A (en) 1986-10-02 1994-06-21 Sohrab Darougar Ocular insert with anchoring protrusions
US5075109A (en) 1986-10-24 1991-12-24 Southern Research Institute Method of potentiating an immune response
US4997652A (en) 1987-12-22 1991-03-05 Visionex Biodegradable ocular implants
US4853224A (en) 1987-12-22 1989-08-01 Visionex Biodegradable ocular implants
US4894388A (en) 1988-12-22 1990-01-16 Monsanto Company Glycosidase inhibitors and use thereof
DE3905050A1 (de) 1989-02-18 1990-08-30 Lohmann Therapie Syst Lts Therapeutisches system zur verzoegerten und gesteuerten transdermalen oder transmucosalen verabreichung von wirkstoffen (ii)
US4946450A (en) 1989-04-18 1990-08-07 Biosource Genetics Corporation Glucan/collagen therapeutic eye shields
US5043273A (en) 1989-08-17 1991-08-27 Monsanto Company Phosphorylated glycosidase inhibitor prodrugs
US5103008A (en) 1989-08-17 1992-04-07 Monsanto Company Compound, N-butyl-deoxynojirimycin-6-phosphate
US5164188A (en) 1989-11-22 1992-11-17 Visionex, Inc. Biodegradable ocular implants
JPH04167172A (ja) 1990-10-31 1992-06-15 Nec Corp ベクトルプロセッサ
US5290892A (en) 1990-11-07 1994-03-01 Nestle S.A. Flexible intraocular lenses made from high refractive index polymers
US5378475A (en) 1991-02-21 1995-01-03 University Of Kentucky Research Foundation Sustained release drug delivery devices
US5770592A (en) 1991-11-22 1998-06-23 Alcon Laboratories, Inc. Prevention and treatment of ocular neovascularization using angiostatic steroids
US5679666A (en) 1991-11-22 1997-10-21 Alcon Laboratories, Inc. Prevention and treatment of ocular neovascularization by treatment with angiostatic steroids
US5178635A (en) 1992-05-04 1993-01-12 Allergan, Inc. Method for determining amount of medication in an implantable device
FR2690846B1 (fr) 1992-05-05 1995-07-07 Aiache Jean Marc Forme galenique pour administration oculaire et procede de preparation.
US5672659A (en) 1993-01-06 1997-09-30 Kinerton Limited Ionic molecular conjugates of biodegradable polyesters and bioactive polypeptides
WO1995003009A1 (en) 1993-07-22 1995-02-02 Oculex Pharmaceuticals, Inc. Method of treatment of macular degeneration
US5443505A (en) 1993-11-15 1995-08-22 Oculex Pharmaceuticals, Inc. Biocompatible ocular implants
US5455351A (en) 1993-12-13 1995-10-03 Abbott Laboratories Retroviral protease inhibiting piperazine compounds
US5516522A (en) 1994-03-14 1996-05-14 Board Of Supervisors Of Louisiana State University Biodegradable porous device for long-term drug delivery with constant rate release and method of making the same
WO1995024929A2 (en) 1994-03-15 1995-09-21 Brown University Research Foundation Polymeric gene delivery system
US5710165A (en) 1994-07-06 1998-01-20 Synthelabo Use of polyamine antagonists for the treatment of glaucoma
US5844102A (en) 1994-07-07 1998-12-01 University Of Maryland Baltimore County Glycohydrolase inhibitors, their preparation and use thereof
US5595760A (en) 1994-09-02 1997-01-21 Delab Sustained release of peptides from pharmaceutical compositions
AUPM897594A0 (en) 1994-10-25 1994-11-17 Daratech Pty Ltd Controlled release container
WO1996014834A1 (en) 1994-11-10 1996-05-23 University Of Kentucky Research Foundation Implantable refillable controlled release device to deliver drugs directly to an internal portion of the body
US5725493A (en) 1994-12-12 1998-03-10 Avery; Robert Logan Intravitreal medicine delivery
US5869079A (en) 1995-06-02 1999-02-09 Oculex Pharmaceuticals, Inc. Formulation for controlled release of drugs by combining hydrophilic and hydrophobic agents
US5773019A (en) 1995-09-27 1998-06-30 The University Of Kentucky Research Foundation Implantable controlled release device to deliver drugs directly to an internal portion of the body
US5824073A (en) 1996-03-18 1998-10-20 Peyman; Gholam A. Macular indentor for use in the treatment of subretinal neovascular membranes
US5743274A (en) 1996-03-18 1998-04-28 Peyman; Gholam A. Macular bandage for use in the treatment of subretinal neovascular members
US6299895B1 (en) 1997-03-24 2001-10-09 Neurotech S.A. Device and method for treating ophthalmic diseases
US5904144A (en) 1996-03-22 1999-05-18 Cytotherapeutics, Inc. Method for treating ophthalmic diseases
JP2000509971A (ja) 1996-04-10 2000-08-08 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 化学的シャペローンを用いる遺伝的欠陥の修正
US6270954B1 (en) 1996-04-10 2001-08-07 The Regents Of The University Of California Correction of genetic defects using chemical chaperones
WO1998001121A1 (fr) * 1996-07-05 1998-01-15 Shionogi & Co., Ltd. Antagoniste des canaux calciques de type p/q
DE19638486A1 (de) 1996-09-20 1998-03-26 Basf Ag Hetaroylderivate
DE69827138T2 (de) 1997-08-11 2006-02-23 Allergan, Inc., Irvine Steriles Retinoid enthaltendes biodegradierbares Implantat mit verbesserter Biokompatibilität und Verfahren zu dessen Herstellung
US5902598A (en) 1997-08-28 1999-05-11 Control Delivery Systems, Inc. Sustained release drug delivery devices
US6146366A (en) 1998-11-03 2000-11-14 Ras Holding Corp Device for the treatment of macular degeneration and other eye disorders
US6492333B1 (en) 1999-04-09 2002-12-10 Osteoscreen, Inc. Treatment of myeloma bone disease with proteasomal and NF-κB activity inhibitors
US6562836B1 (en) 1999-05-24 2003-05-13 Queen's University Of Kingston Methods and compounds for inhibiting amyloid deposits
US6416777B1 (en) 1999-10-21 2002-07-09 Alcon Universal Ltd. Ophthalmic drug delivery device
US6331313B1 (en) 1999-10-22 2001-12-18 Oculex Pharmaceticals, Inc. Controlled-release biocompatible ocular drug delivery implant devices and methods
US7119091B2 (en) * 1999-12-03 2006-10-10 Ono Pharmaceutical Co., Ltd. Triazaspiro[5.5]undecane derivatives and pharmaceutical compositions comprising thereof, as an active ingredient
WO2001052830A2 (en) 2000-01-20 2001-07-26 Washington University METHODS TO TREAT α-1-ANTITRYPSIN DEFICIENCY
AU2001247848A1 (en) 2000-03-31 2001-10-15 Michigan State University Process for the preparation of 1,5-dideoxy-1,5-imino hexitols from oximes or imines
US6375972B1 (en) 2000-04-26 2002-04-23 Control Delivery Systems, Inc. Sustained release drug delivery devices, methods of use, and methods of manufacturing thereof
US6818203B2 (en) * 2000-08-11 2004-11-16 Schering Aktiengesellschaft Use of perfluoroalkyl-containing metal complexes as contrast media in MR-imaging for visualization of plaque, tumors and necroses
US6756058B2 (en) 2001-01-03 2004-06-29 Bausch & Lomb Incorporated Sustained release drug delivery devices with multiple agents
GB0118752D0 (en) 2001-08-01 2001-09-26 Pfizer Ltd Process for the production of quinazolines
JP2005511516A (ja) 2001-09-25 2005-04-28 スミスクライン ビーチャム コーポレーション 選択的ｒｘｒリガンド
US6976584B2 (en) 2002-06-26 2005-12-20 Bausch & Lomb Incorporated Package for surgical implant
US20040131648A1 (en) * 2002-10-24 2004-07-08 The Procter & Gamble Company Nuclear hormone receptor compounds, products and methods employing same
US20050048099A1 (en) 2003-01-09 2005-03-03 Allergan, Inc. Ocular implant made by a double extrusion process
PT2444102E (pt) 2003-01-31 2015-09-17 Sinai School Medicine Terapia combinada para o tratamento de distúrbios de deficiência proteica
EP2327400A3 (en) 2003-03-14 2011-10-19 University of Washington Retinoid Replacements and Opsin Agonists and Methods for the Use Thereof
WO2004108867A2 (en) 2003-06-02 2004-12-16 Flexitral, Inc. Cyclohexene carboamides and carbothioamides
CL2004001996A1 (es) 2003-08-08 2005-05-06 Eyetech Pharmaceuticals Inc Aptameros anti-vegf (factor de crecimiento endotelial vascular) con bloqueo nucleotidico 5'-5' o 3'-3' invertido, composicion que lo contiene, util para trastornos de neovascularizacion.
EP1727529B1 (en) 2004-03-17 2016-03-02 Lars Michael Larsen Prevention of retinopathy by inhibition of the visual cycle
SI1765322T1 (sl) 2004-06-18 2014-03-31 University Of Washington Intellectual Property And Technology Transfer 4311 Derivati retinala in postopki za njihovo uporabo za zdravljenje motenj vida
DK1768657T3 (da) 2004-06-23 2008-12-01 Sirion Therapeutics Inc Fremgangsmåder og sammensætninger til at behandle ophthalmiske tilstande med retinylderivater
JP2008515778A (ja) 2004-08-18 2008-05-15 シリオン セラピューティクス， インコーポレイテッド 眼の状態を１３−シス−レチニル誘導体で処置するための組み合わせ方法、組成物および治療
US20080275133A1 (en) 2004-09-30 2008-11-06 University Of Calfornia-San Francisco Local Administration of Retinoids to Treat Deficiencies in Dark Adaptation
MX2007006179A (es) 2004-11-23 2007-06-20 Ptc Therapeutics Inc Tetrahidrocarbazoles como agentes activos para inhibir la produccion del factor de crecimiento endotelial vascular por control de la traduccion.
US20080275134A1 (en) 2005-02-24 2008-11-06 University Of Washington Methods for Treatment of Retinal Degenerative Disease
GB0506133D0 (en) * 2005-03-24 2005-05-04 Sterix Ltd Compound
AU2006320578B2 (en) 2005-11-30 2013-01-31 Inotek Pharmaceuticals Corporation Purine derivatives and methods of use thereof
CA2657164A1 (en) 2006-07-27 2008-01-31 University Of Florida Research Foundation, Inc. Compositions and methods for treating or preventing ophthalmic light toxicity
WO2008013984A2 (en) 2006-07-27 2008-01-31 University Of Florida Research Foundation, Inc. Compositions and methods for treating or preventing ophthalmic disease
AU2007277032A1 (en) 2006-07-27 2008-01-31 University Of Florida Research Foundation, Inc. Opsin stabilizing compounds and methods of use
TWI446904B (zh) 2007-11-01 2014-08-01 Acucela Inc 用於治療眼科疾病及病症之胺衍生化合物
JP2011507910A (ja) * 2007-12-21 2011-03-10 ユニバーシティー オブ ロチェスター 真核生物の寿命を変更するための方法
WO2009116487A1 (ja) 2008-03-17 2009-09-24 住友化学株式会社 スルホン化合物及びその製造方法
CA2740952C (en) 2008-10-22 2015-12-29 Ian L. Scott Compounds for treating ophthalmic diseases and disorders
WO2010074746A1 (en) 2008-12-23 2010-07-01 Bikam Pharmaceuticals, Inc. Methods of use for opsin binding ligands
IN2012DN00352A (da) 2009-06-16 2015-08-21 Bikam Pharmaceuticals Inc
AU2012271728B2 (en) 2011-06-14 2016-10-20 Bikam Pharmaceuticals, Inc. Opsin-binding ligands, compositions and methods of use

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CA2767895A1 (en) 2010-12-23
ZA201200226B (en) 2013-06-26
EP2442644B1 (en) 2016-08-10
US9562022B2 (en) 2017-02-07
AU2010260535A1 (en) 2012-02-02
KR20120112351A (ko) 2012-10-11
ES2610429T3 (es) 2017-04-27
CA2767895C (en) 2017-12-12
HUE031705T2 (en) 2017-07-28
PL2442644T3 (pl) 2017-02-28
KR20180099944A (ko) 2018-09-05
HRP20161477T1 (hr) 2016-12-16
US20170037018A1 (en) 2017-02-09
EP2442644A4 (en) 2013-05-22
KR101726358B1 (ko) 2017-04-26
IN2012DN00352A (da) 2015-08-21
CN102480943A (zh) 2012-05-30
EP2442644A1 (en) 2012-04-25
SI2442644T1 (sl) 2017-01-31
WO2010147653A1 (en) 2010-12-23
EP3100723A1 (en) 2016-12-07
EA201270018A1 (ru) 2012-07-30
CY1118221T1 (el) 2017-06-28
KR101921288B1 (ko) 2018-11-22
SMT201600388B (it) 2017-03-08
PT2442644T (pt) 2016-11-09
EP3100723B1 (en) 2019-06-12
KR20170041282A (ko) 2017-04-14
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AU2010260535B2 (en) 2015-08-20
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