JP2014518212A5 - 化合物及び組成物 - Google Patents

化合物及び組成物 Download PDF

Info

Publication number
JP2014518212A5
JP2014518212A5 JP2014515939A JP2014515939A JP2014518212A5 JP 2014518212 A5 JP2014518212 A5 JP 2014518212A5 JP 2014515939 A JP2014515939 A JP 2014515939A JP 2014515939 A JP2014515939 A JP 2014515939A JP 2014518212 A5 JP2014518212 A5 JP 2014518212A5
Authority
JP
Japan
Prior art keywords
compound
compound according
hydrogen
methyl
independently
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.)
Granted
Application number
JP2014515939A
Other languages
English (en)
Other versions
JP6068457B2 (ja
JP2014518212A (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2012/042178 external-priority patent/WO2012174064A1/en
Publication of JP2014518212A publication Critical patent/JP2014518212A/ja
Publication of JP2014518212A5 publication Critical patent/JP2014518212A5/ja
Application granted granted Critical
Publication of JP6068457B2 publication Critical patent/JP6068457B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Claims (22)

  1. 式(1)の構造を有する化合物:
    Figure 2014518212
    Xは、1)C(R)(R)、又は2)酸素であり;
    Tは、1)CH、2)CHCH、又は3)存在せず;
    とRは、独立して、1)−CH、又は2)−CHCHであり;
    は、1)水素、2)−CH、又は3)−CHCHであり;
    は、1)水素、又は2)−CHであり;
    とRは、それぞれ独立して、1)水素、2)−CH、又は3)−CHCHであり;
    とRは、それぞれ独立して、1)水素、2)重陽子、3)ヒドロキシル、4)フルオロ、5)アルコキシ、6)低級アルキル、又は7)低級ハロアルキルであり;
    とRは、オキソ(=O)として統合してもよく、
    Bは、1)
    Figure 2014518212
    Figure 2014518212
    Figure 2014518212
    7)シクロアルキル、又は8)低級ハロアルキルであり;
    、R、R、R、及びRは、それぞれ独立して、1)水素、2)低級アルキル、3)低級ハロアルキル、4)ハロゲン、5)ニトロ、6)ヒドロキシ、7)アルコキシ、8)ニトリル、9)カルボキシアミド、10)アリールカルボニル、11)カルバモイル、12)アミジル、13)アミノ、14)アルキルカルボニル、15)ウレア、又は16)−C(NOH)NHであり;
    、R、及びRは、1)−CR、又は2)窒素であるが、R、R、及びRの少なくとも1つは窒素であり;
    Zは、1)酸素、又は2)硫黄である;
    並びに、これらの薬学的に許容される塩、溶媒和物、及び水和物。
  2. XがCRである請求項1に記載の化合物。
  3. とRがオキソ(=O)として統合した請求項2に記載の化合物。
  4. がヒドロキシルで、Rが水素である請求項2に記載の化合物。
  5. とRが、それぞれ独立してメチル又はエチルである請求項2に記載の化合物。
  6. とRが、それぞれメチルである請求項2に記載の化合物。
  7. が水素又はメチルである請求項2に記載の化合物。
  8. がメチルである請求項7に記載の化合物。
  9. とRの双方がメチルである請求項1に記載の化合物。
  10. がメチル又は水素である請求項1に記載の化合物。
  11. がメチルである請求項10に記載の化合物。
  12. TがCHである請求項1に記載の化合物。
  13. とRが独立して水素又はメチルである請求項1に記載の化合物。
  14. とRがそれぞれ水素である請求項13に記載の化合物。
  15. 薬学的に許容される担体中に請求項1に記載の化合物の治療的有効量を含む組成物
  16. 前記化合物が(4−(トリフルオロメチル)フェニル)((1R,6S)−2,2,6−トリメチルシクロヘキシル)メタノン(化合物16)である請求項1に記載の化合物
  17. 前記化合物が(4−(トリフルオロメトキシ)フェニル)((1R,6S)−2,2,6−トリメチルシクロヘキシル)メタノン(化合物29)である請求項1に記載の化合物
  18. 前記化合物が(S)−(4−(トリフルオロメチル)フェニル)((1R,6S)−2,2,6−トリメチルシクロヘキシル)メタノール(化合物15)である請求項1に記載の化合物
  19. 前記化合物が(3−フルオロ−4−(トリフルオロメチル)フェニル)((1R,6S)−2,2,6−トリメチルシクロヘキシル)メタノン(化合物74)である請求項1に記載の化合物
  20. 前記化合物が(4−フルオロフェニル)((1R,6S)−1,2,2,6−テトラメチルシクロヘキシル)メタノン(化合物62)である請求項1に記載の化合物
  21. 前記化合物が2−(トリフルオロメチル)−4−((1R,6S)−2,2,6−トリメチルシクロヘキサンカルボニル)ベンゾニトリル(化合物61)である請求項1に記載の化合物
  22. 前記化合物が2−フルオロ−4−((1R,6S)−2,2,6−トリメチルシクロヘキサンカルボニル)ベンゾニトリル(化合物45)である請求項1に記載の化合物
JP2014515939A 2011-06-14 2012-06-13 化合物及び組成物 Expired - Fee Related JP6068457B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201161520709P 2011-06-14 2011-06-14
US61/520,709 2011-06-14
US201161562689P 2011-11-22 2011-11-22
US61/562,689 2011-11-22
US201161564453P 2011-11-29 2011-11-29
US61/564,453 2011-11-29
PCT/US2012/042178 WO2012174064A1 (en) 2011-06-14 2012-06-13 Opsin-binding ligands, compositions and methods of use

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2016248210A Division JP2017081957A (ja) 2011-06-14 2016-12-21 化合物

Publications (3)

Publication Number Publication Date
JP2014518212A JP2014518212A (ja) 2014-07-28
JP2014518212A5 true JP2014518212A5 (ja) 2015-08-06
JP6068457B2 JP6068457B2 (ja) 2017-01-25

Family

ID=47357439

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2014515939A Expired - Fee Related JP6068457B2 (ja) 2011-06-14 2012-06-13 化合物及び組成物
JP2016248210A Pending JP2017081957A (ja) 2011-06-14 2016-12-21 化合物

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2016248210A Pending JP2017081957A (ja) 2011-06-14 2016-12-21 化合物

Country Status (10)

Country Link
US (3) US9133082B2 (ja)
EP (1) EP2720539B1 (ja)
JP (2) JP6068457B2 (ja)
CN (2) CN106431988A (ja)
AU (2) AU2012271728B2 (ja)
BR (1) BR112013032199A2 (ja)
CA (1) CA2838974A1 (ja)
EA (2) EA032666B1 (ja)
HK (1) HK1199793A1 (ja)
WO (1) WO2012174064A1 (ja)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IN2012DN00352A (ja) 2009-06-16 2015-08-21 Bikam Pharmaceuticals Inc
EA032666B1 (ru) * 2011-06-14 2019-06-28 Бикам Фармасьютикалз, Инк. Опсинсвязывающие лиганды и способы их применения
AU2012346214B2 (en) * 2011-11-30 2017-09-14 Bikam Pharmaceuticals, Inc. Opsin-binding ligands, compositions and methods of use
WO2013081642A1 (en) * 2011-12-01 2013-06-06 Bikam Pharmaceuticals, Inc. Opsin-binding ligands, compositions and methods of use
US11005042B2 (en) 2015-12-10 2021-05-11 Merck Patent Gmbh Formulations containing ketones comprising non-aromatic cycles
US20190169108A1 (en) 2016-08-04 2019-06-06 Basf Se 1-hydroxymethyl-1,2,2,6-tetramethyl-cyclohexane and derivatives thereof and their use as aroma chemicals
CN106928244B (zh) * 2017-02-07 2019-03-26 天津药明康德新药开发有限公司 一种2-氮-叔丁氧羰基-8-(羟甲基)-5-氧-螺[3.4]辛烷的制备方法

Family Cites Families (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US164188A (en) 1875-06-08 Improvement in car x c couplings
NL258405A (ja) * 1959-11-25 1900-01-01
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
US3828777A (en) 1971-11-08 1974-08-13 Alza Corp Microporous ocular device
US3832253A (en) 1973-03-21 1974-08-27 Baxter Laboratories Inc Method of making an inflatable balloon catheter
GB1456151A (en) * 1974-02-22 1976-11-17 Naarden International Nv Cycloaliphatic saturated and unsaturated ketones as flavour and odour agents
US4014335A (en) 1975-04-21 1977-03-29 Alza Corporation Ocular drug delivery device
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
US4292447A (en) * 1978-12-15 1981-09-29 International Flavors & Fragrances Inc. Process for hydrogenation of 2,6,6-trimethyl cyclohexene derivatives, products produced thereby and organoleptic uses of said products
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
EP0052322B1 (de) 1980-11-10 1985-03-27 Gersonde, Klaus, Prof. Dr. Verfahren zur Herstellung von Lipid-Vesikeln durch Ultraschallbehandlung, Anwendung des Verfahrens und Vorrichtung zur Durchführung des Verfahrens
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
ATE59966T1 (de) 1983-09-26 1991-02-15 Ehrenfeld Udo Mittel und erzeugnis fuer die diagnose und therapie von tumoren sowie zur behandlung von schwaechen der zelligen und humoralen immunabwehr.
US4615885A (en) 1983-11-01 1986-10-07 Terumo Kabushiki Kaisha Pharmaceutical composition containing urokinase
US5074661A (en) 1986-05-30 1991-12-24 Diffracto Ltd. Methods and apparatus for retroreflective surface inspection and distortion measurement
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
DE3738406A1 (de) * 1987-11-12 1989-05-24 Henkel Kgaa Sebosuppressive topische zubereitungen
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
US5103008A (en) 1989-08-17 1992-04-07 Monsanto Company Compound, N-butyl-deoxynojirimycin-6-phosphate
US5043273A (en) 1989-08-17 1991-08-27 Monsanto Company Phosphorylated glycosidase inhibitor prodrugs
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
US5679666A (en) 1991-11-22 1997-10-21 Alcon Laboratories, Inc. Prevention and treatment of ocular neovascularization by treatment with angiostatic steroids
US5770592A (en) 1991-11-22 1998-06-23 Alcon Laboratories, Inc. Prevention and treatment of ocular neovascularization using 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
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
EP0804249A2 (en) 1994-03-15 1997-11-05 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
JPH0873335A (ja) * 1994-09-06 1996-03-19 Pola Chem Ind Inc メラニン産生抑制剤及び皮膚外用剤
AUPM897594A0 (en) 1994-10-25 1994-11-17 Daratech Pty Ltd Controlled release container
AU708529B2 (en) 1994-11-10 1999-08-05 University Of Kentucky Research Foundation, The 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
US5743274A (en) 1996-03-18 1998-04-28 Peyman; Gholam A. Macular bandage for use in the treatment of subretinal neovascular members
US5824073A (en) 1996-03-18 1998-10-20 Peyman; Gholam A. Macular indentor for use in the treatment of subretinal neovascular membranes
US5904144A (en) 1996-03-22 1999-05-18 Cytotherapeutics, Inc. Method for treating ophthalmic diseases
US6299895B1 (en) 1997-03-24 2001-10-09 Neurotech S.A. Device and method for treating ophthalmic diseases
WO1999007418A2 (en) 1997-08-11 1999-02-18 Allergan Sales, Inc. Sterile bioerodible implant device with improved biocompatability and method
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
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
US6656912B2 (en) 2000-01-20 2003-12-02 Washington University In St. Louis Methods to treat α1-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
JP2001348353A (ja) * 2000-06-07 2001-12-18 Takasago Internatl Corp (1s,6r)−2,2,6−トリメチルシクロヘキシルメチルケトン及び/又は(1r,6s)−2,2,6−トリメチルシクロヘキシルメチルケトン、それらの製造方法並びにそれらを含有してなる香料組成物
JP2002114738A (ja) * 2000-10-10 2002-04-16 Takasago Internatl Corp 新規ケトン化合物とそれを用いたトリメチルシクロヘキサンカルボン酸類の製造法
WO2002053128A2 (en) 2001-01-03 2002-07-11 Bausch & Lomb Incorporated Sustained release drug delivery devices with multiple agents
US20050048099A1 (en) 2003-01-09 2005-03-03 Allergan, Inc. Ocular implant made by a double extrusion process
EP3326623A1 (en) 2003-03-14 2018-05-30 University of Washington Retinoid replacements and opsin agonists and methods for the use thereof
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.
US20050126448A1 (en) 2003-12-12 2005-06-16 David Bernstein Modular pallet
CA2657238A1 (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
AU2007277035A1 (en) 2006-07-27 2008-01-31 University Of Florida Research Foundation, Inc. Compositions and methods for treating or preventing ophthalmic light toxicity
JP4616237B2 (ja) 2006-11-07 2011-01-19 日本電信電話株式会社 シリコン化合物薄膜の形成方法
CA2704199C (en) * 2007-11-01 2016-01-19 Acucela Inc. Amine derivative compounds for treating ophthalmic diseases and disorders
CN101504399B (zh) * 2009-02-19 2011-12-07 北京化工大学 加氢尾油长直侧链环烷烃与烷基苯的定性定量分析方法
IN2012DN00352A (ja) 2009-06-16 2015-08-21 Bikam Pharmaceuticals Inc
EA032666B1 (ru) * 2011-06-14 2019-06-28 Бикам Фармасьютикалз, Инк. Опсинсвязывающие лиганды и способы их применения

Similar Documents

Publication Publication Date Title
JP2014518212A5 (ja) 化合物及び組成物
JP2013537203A5 (ja)
JP2014508811A5 (ja)
JP2008531599A5 (ja)
JP2017039755A5 (ja)
JP2011037901A5 (ja)
JP2011513305A5 (ja)
JP2014526549A5 (ja)
NZ590268A (en) 1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase
JP2011529054A5 (ja)
JP2014051526A5 (ja)
JP2012530705A5 (ja)
RU2011108281A (ru) Трипиридилкарбоксамидные антагонисты орексиновых рецепторов
JP2014530900A5 (ja)
JP2009501745A5 (ja)
JP2011519854A5 (ja)
JP2013536188A5 (ja)
DK2358680T3 (da) Faste former af n-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluormethyl)phenyl)-3-oxo-5-(trifluormethyl)-1,4-dihydroquinolin-3-carboxamid
JP2013513621A5 (ja)
RU2017120217A (ru) 2-амино-5,5-дифтор-6-(фторметил)-6-фенил-3,4,5,6-тетрагидпропиридины в качестве ингибиторов bace1
EA201000702A1 (ru) Некоторые производные 2-пиразинона и их применение в качестве ингибиторов нейтрофильной эластазы
RU2012132692A (ru) Новые ингибиторы s-нитрозоглутатионредуктазы
RU2017116196A (ru) 2-амино-6-(дифторметил)-5,5-дифтор-6-фенил-3,4,5,6-тетрагидропиридины как ингибиторы васе1
PE20080360A1 (es) Derivados 4-bencilftalazinona 2-sustituidos como antagonistas de histaminas h1 y h3
JP2017535559A5 (ja)