CN105362221A - 向眼部递送受体酪氨酸激酶抑制性(RTKi)化合物的药物组合物 - Google Patents
向眼部递送受体酪氨酸激酶抑制性(RTKi)化合物的药物组合物 Download PDFInfo
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- CN105362221A CN105362221A CN201510767618.5A CN201510767618A CN105362221A CN 105362221 A CN105362221 A CN 105362221A CN 201510767618 A CN201510767618 A CN 201510767618A CN 105362221 A CN105362221 A CN 105362221A
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- 239000002451 tumor necrosis factor inhibitor Substances 0.000 description 1
- 208000029257 vision disease Diseases 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
-
- 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
- A61P7/10—Antioedematous agents; Diuretics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2121/00—Preparations for use in therapy
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Ophthalmology & Optometry (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Dispersion Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US15698409P | 2009-03-03 | 2009-03-03 | |
| US61/156,984 | 2009-03-03 | ||
| CN2010800101411A CN102340993A (zh) | 2009-03-03 | 2010-03-03 | 向眼部递送受体酪氨酸激酶抑制性(RTKi)化合物的药物组合物 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2010800101411A Division CN102340993A (zh) | 2009-03-03 | 2010-03-03 | 向眼部递送受体酪氨酸激酶抑制性(RTKi)化合物的药物组合物 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105362221A true CN105362221A (zh) | 2016-03-02 |
Family
ID=42678477
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510767618.5A Pending CN105362221A (zh) | 2009-03-03 | 2010-03-03 | 向眼部递送受体酪氨酸激酶抑制性(RTKi)化合物的药物组合物 |
| CN2010800101411A Pending CN102340993A (zh) | 2009-03-03 | 2010-03-03 | 向眼部递送受体酪氨酸激酶抑制性(RTKi)化合物的药物组合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2010800101411A Pending CN102340993A (zh) | 2009-03-03 | 2010-03-03 | 向眼部递送受体酪氨酸激酶抑制性(RTKi)化合物的药物组合物 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20100226992A1 (https=) |
| EP (1) | EP2403342A4 (https=) |
| JP (1) | JP5583145B2 (https=) |
| KR (1) | KR20110123789A (https=) |
| CN (2) | CN105362221A (https=) |
| AU (1) | AU2010221438C1 (https=) |
| BR (1) | BRPI1008920A2 (https=) |
| CA (1) | CA2753837A1 (https=) |
| MX (1) | MX2011008680A (https=) |
| WO (1) | WO2010101971A1 (https=) |
| ZA (1) | ZA201105506B (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2007237096C1 (en) | 2006-04-07 | 2012-12-13 | EyePoint, Inc. | Antibodies that bind human protein tyrosine phosphatase beta (HPTPbeta) and uses thereof |
| US7622593B2 (en) | 2006-06-27 | 2009-11-24 | The Procter & Gamble Company | Human protein tyrosine phosphatase inhibitors and methods of use |
| TW201023912A (en) | 2008-12-05 | 2010-07-01 | Alcon Res Ltd | Pharmaceutical suspension |
| US8912236B2 (en) | 2009-03-03 | 2014-12-16 | Alcon Research, Ltd. | Pharmaceutical composition for delivery of receptor tyrosine kinase inhibiting (RTKi) compounds to the eye |
| MY160399A (en) | 2009-07-06 | 2017-03-15 | Aerpio Therapeutics Inc | Compounds, compositions, and methods for preventing metastasis of cancer cells |
| AU2012323856B2 (en) | 2011-10-13 | 2017-05-25 | EyePoint, Inc. | Methods for treating Vascular Leak Syndrome and cancer |
| KR20150000869A (ko) * | 2011-12-14 | 2015-01-05 | 애브비 인코포레이티드 | 키나제 억제제를 함유하는 조성물 |
| EP2825166A1 (en) * | 2012-03-12 | 2015-01-21 | Allergan, Inc. | Method of treating ophthalmic conditions with kinase inhibitors |
| US20150050277A1 (en) | 2013-03-15 | 2015-02-19 | Aerpio Therapeutics Inc. | Compositions and methods for treating ocular diseases |
| BR112016006153A2 (pt) | 2013-09-20 | 2017-08-01 | Santen Pharmaceutical Co Ltd | composição contendo polietileno glicol |
| EP3116503A4 (en) | 2014-03-14 | 2017-08-23 | Aerpio Therapeutics, Inc. | Hptp-beta inhibitors |
| ES2863601T3 (es) * | 2014-09-17 | 2021-10-11 | Panoptica Inc | Formulaciones oculares para administración de fármacos y protección del segmento anterior del ojo |
| WO2016197005A1 (en) * | 2015-06-05 | 2016-12-08 | Kato Pharmaceuticals, Inc. | Extended release urea compositions |
| TWI700085B (zh) * | 2015-06-22 | 2020-08-01 | 新源生物科技股份有限公司 | 酪胺酸激酶抑制劑之眼用調配物的用途 |
| ES2981607T3 (es) | 2015-09-23 | 2024-10-09 | Eyepoint Pharmaceuticals Inc | Activadores de Tie-2 para uso en el tratamiento de la presión intraocular |
| EP3962482A4 (en) | 2019-04-29 | 2023-01-11 | EyePoint Pharmaceuticals, Inc. | TIE 2 ACTIVATORS FACING THE SCHLEMM CHANNEL |
| EP4028015A4 (en) * | 2019-09-13 | 2023-11-15 | Aldeyra Therapeutics, Inc. | Ophthalmic formulations of methotrexate |
| AU2020354996B2 (en) | 2019-09-27 | 2022-12-01 | Virginia Commonwealth University | Compositions and methods for restoring or increasing tissue perfusion |
| CN116251186B (zh) * | 2021-12-09 | 2025-04-25 | 成都瑞沐生物医药科技有限公司 | 一种酪氨酸激酶抑制剂眼用制剂及其制备方法和用途 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070149593A1 (en) * | 2005-12-23 | 2007-06-28 | Alcon, Inc. | PHARMACEUTICAL FORMULATION FOR DELIVERY OF RECEPTOR TYROSINE KINASE INHIBITING (RTKi) COMPOUNDS TO THE EYE |
| WO2009014510A1 (en) * | 2007-07-20 | 2009-01-29 | Alcon, Inc. | Pharmaceutical formulation for delivery of receptor tyrosine kinase inhibiting (rtki) compounds to the eye |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3856919A (en) * | 1970-06-08 | 1974-12-24 | Burton Parsons Chemicals Inc | Ophthalmic solution |
| US3931319A (en) * | 1974-10-29 | 1976-01-06 | Millmaster Onyx Corporation | Capped polymers |
| US4027020A (en) * | 1974-10-29 | 1977-05-31 | Millmaster Onyx Corporation | Randomly terminated capped polymers |
| US4409205A (en) * | 1979-03-05 | 1983-10-11 | Cooper Laboratories, Inc. | Ophthalmic solution |
| US4407791A (en) * | 1981-09-28 | 1983-10-04 | Alcon Laboratories, Inc. | Ophthalmic solutions |
| US4525346A (en) * | 1981-09-28 | 1985-06-25 | Alcon Laboratories, Inc. | Aqueous antimicrobial ophthalmic solutions |
| US4727064A (en) * | 1984-04-25 | 1988-02-23 | The United States Of America As Represented By The Department Of Health And Human Services | Pharmaceutical preparations containing cyclodextrin derivatives |
| US4836986A (en) * | 1984-09-28 | 1989-06-06 | Bausch & Lomb Incorporated | Disinfecting and preserving systems and methods of use |
| US5002935A (en) * | 1987-12-30 | 1991-03-26 | University Of Florida | Improvements in redox systems for brain-targeted drug delivery |
| US5037647A (en) * | 1988-09-15 | 1991-08-06 | Alcon Laboratories, Inc. | Aqueous antimicrobial opthalmic solutions comprised of quaternary ammonium compound, citric acid, citrate and sodium chloride |
| US5461081A (en) * | 1989-09-28 | 1995-10-24 | Alcon Laboratories, Inc. | Topical ophthalmic pharmaceutical vehicles |
| US5932572A (en) * | 1992-02-21 | 1999-08-03 | Alcon Laboratories, Inc. | Topical anti-glaucoma compositions |
| US5300287A (en) * | 1992-11-04 | 1994-04-05 | Alcon Laboratories, Inc. | Polymeric antimicrobials and their use in pharmaceutical compositions |
| ES2141775T3 (es) * | 1993-04-16 | 2000-04-01 | Wakamoto Pharma Co Ltd | Composicion medicinal a base de agua termicamente gelificante reversible. |
| CA2226348A1 (en) * | 1996-05-07 | 1997-11-13 | Takashi Ikari | Ophthalmic preparations |
| CA2264290C (en) * | 1997-07-29 | 2005-11-29 | Alcon Laboratories, Inc. | Conditioning solutions for contact lens care |
| NZ517556A (en) * | 1999-09-06 | 2003-08-29 | Ono Pharmaceutical Co | N-[o-(p-pivaloyloxybenzenesulphonyl-amino)benzoyl]glycine as preventive and therapeutic agents for eye diseases |
| WO2001022936A1 (en) * | 1999-09-24 | 2001-04-05 | Alcon Universal Ltd. | Topical suspension formulations containing ciprofloxacin and dexamethasone |
| AU4511201A (en) * | 1999-12-03 | 2001-06-12 | Ista Pharmaceuticals, Inc | Compositions and methods for the induction and treatment of retinal detachments |
| WO2001087262A2 (en) * | 2000-05-15 | 2001-11-22 | Pharmacia Italia S.P.A. | Stabilized steroidal suspension |
| EP1318787A2 (en) * | 2000-07-26 | 2003-06-18 | Alcon Inc. | Pharmaceutical suspension compositions lacking a polymeric suspending agent |
| JP3450805B2 (ja) * | 2000-08-08 | 2003-09-29 | わかもと製薬株式会社 | 水性医薬組成物 |
| US20040256749A1 (en) * | 2000-12-22 | 2004-12-23 | Mahesh Chaubal | Process for production of essentially solvent-free small particles |
| US6743439B1 (en) * | 2001-06-27 | 2004-06-01 | Alcon, Inc. | Ophthalmic compositions containing copolymers of sulfonated styrene and maleic anhydride |
| RU2295346C2 (ru) * | 2001-09-21 | 2007-03-20 | Алькон, Инк. | Способ лечения инфекций среднего уха |
| US7001615B1 (en) * | 2001-12-07 | 2006-02-21 | Alcon, Inc. | Sustained release ophthalmic, otic and nasal suspension |
| WO2004000284A1 (en) * | 2002-06-21 | 2003-12-31 | Transform Pharmaceuticals, Inc. | Pharmaceutical compositions with improved dissolution |
| JP4810427B2 (ja) * | 2003-05-22 | 2011-11-09 | アボット・ラボラトリーズ | インダゾール、ベンズイソオキサゾールおよびベンズイソチアゾールキナーゼ阻害剤 |
| US20040235892A1 (en) * | 2003-05-22 | 2004-11-25 | Yujia Dai | Indazole and benzisoxazole kinase inhibitors |
| SI1755616T1 (sl) * | 2004-04-08 | 2014-04-30 | Eye Co Pty Ltd. | Zdravljenje eksudativne retinopatije z mineralkortikoidi |
| TWI358290B (en) * | 2004-12-02 | 2012-02-21 | Alcon Inc | Topical nepafenac formulations |
| TW200640443A (en) * | 2005-02-23 | 2006-12-01 | Alcon Inc | Methods for treating ocular angiogenesis, retinal edema, retinal ischemia, and diabetic retinopathy using selective RTK inhibitors |
| CA2607608A1 (en) * | 2005-05-10 | 2006-11-16 | Alcon, Inc. | Suspension formulations of nepafenac and other ophthalmic drugs for topical treatment of ophthalmic disorders |
| PL1906916T3 (pl) * | 2005-05-10 | 2009-02-27 | Alcon Inc | Zawiesina do oczu obejmująca lek okulistyczny, poloksaminę i glikolowy środek regulujący toniczność, zastosowanie wymienionej kompozycji do wytwarzania leku do leczenia zaburzeń wzroku |
| US20070149480A1 (en) * | 2005-12-23 | 2007-06-28 | Alcon, Inc. | PHARMACEUTICAL COMPOSITION FOR DELIVERY OF RECEPTOR TYROSINE KINASE INHIBITING (RTKi) COMPOUNDS TO THE EYE |
| US20070173538A1 (en) * | 2005-12-23 | 2007-07-26 | Alcon, Inc. | PHARMACEUTICAL FORMULATION FOR DELIVERY OF RECEPTOR TYROSINE KINASE INHIBITING (RTKi) COMPOUNDS TO THE EYE |
| US20070249546A1 (en) * | 2006-04-22 | 2007-10-25 | Sawaya Assad S | Ophthalmic and related aqueous solutions containing antifungal agents, uses therefor and methods for preparing them |
| TW201023912A (en) * | 2008-12-05 | 2010-07-01 | Alcon Res Ltd | Pharmaceutical suspension |
-
2010
- 2010-03-03 MX MX2011008680A patent/MX2011008680A/es active IP Right Grant
- 2010-03-03 CN CN201510767618.5A patent/CN105362221A/zh active Pending
- 2010-03-03 WO PCT/US2010/025998 patent/WO2010101971A1/en not_active Ceased
- 2010-03-03 CA CA2753837A patent/CA2753837A1/en not_active Abandoned
- 2010-03-03 AU AU2010221438A patent/AU2010221438C1/en not_active Ceased
- 2010-03-03 CN CN2010800101411A patent/CN102340993A/zh active Pending
- 2010-03-03 EP EP10749243.1A patent/EP2403342A4/en not_active Withdrawn
- 2010-03-03 US US12/716,385 patent/US20100226992A1/en not_active Abandoned
- 2010-03-03 BR BRPI1008920-9A patent/BRPI1008920A2/pt not_active IP Right Cessation
- 2010-03-03 KR KR1020117023002A patent/KR20110123789A/ko not_active Ceased
- 2010-03-03 JP JP2011553061A patent/JP5583145B2/ja not_active Expired - Fee Related
-
2011
- 2011-07-26 ZA ZA2011/05506A patent/ZA201105506B/en unknown
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070149593A1 (en) * | 2005-12-23 | 2007-06-28 | Alcon, Inc. | PHARMACEUTICAL FORMULATION FOR DELIVERY OF RECEPTOR TYROSINE KINASE INHIBITING (RTKi) COMPOUNDS TO THE EYE |
| WO2009014510A1 (en) * | 2007-07-20 | 2009-01-29 | Alcon, Inc. | Pharmaceutical formulation for delivery of receptor tyrosine kinase inhibiting (rtki) compounds to the eye |
Also Published As
| Publication number | Publication date |
|---|---|
| EP2403342A1 (en) | 2012-01-11 |
| WO2010101971A1 (en) | 2010-09-10 |
| JP5583145B2 (ja) | 2014-09-03 |
| AU2010221438B2 (en) | 2014-10-16 |
| MX2011008680A (es) | 2011-09-08 |
| ZA201105506B (en) | 2012-09-26 |
| JP2012519692A (ja) | 2012-08-30 |
| EP2403342A4 (en) | 2013-06-05 |
| AU2010221438C1 (en) | 2015-01-29 |
| CN102340993A (zh) | 2012-02-01 |
| AU2010221438A1 (en) | 2011-08-25 |
| BRPI1008920A2 (pt) | 2015-08-25 |
| CA2753837A1 (en) | 2010-09-10 |
| US20100226992A1 (en) | 2010-09-09 |
| KR20110123789A (ko) | 2011-11-15 |
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