RU2658015C2 - Ингибитор ассоциированного с функцией лимфоцитов антигена-1 (lfa-1), способы его получения и его полиморф - Google Patents

Ингибитор ассоциированного с функцией лимфоцитов антигена-1 (lfa-1), способы его получения и его полиморф Download PDF

Info

Publication number
RU2658015C2
RU2658015C2 RU2015102926A RU2015102926A RU2658015C2 RU 2658015 C2 RU2658015 C2 RU 2658015C2 RU 2015102926 A RU2015102926 A RU 2015102926A RU 2015102926 A RU2015102926 A RU 2015102926A RU 2658015 C2 RU2658015 C2 RU 2658015C2
Authority
RU
Russia
Prior art keywords
compound
formula
present
various embodiments
acetone
Prior art date
Application number
RU2015102926A
Other languages
English (en)
Russian (ru)
Other versions
RU2015102926A (ru
Inventor
Джеймс Роберт Зеллер
Срипати ВЕНКАТРАМАН
Элизабет К.А. БРОТ
Субашри ИЕР
Майкл ХОЛЛ
Original Assignee
Саркоуд Байосайенс Инк.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=49995472&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=RU2658015(C2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Саркоуд Байосайенс Инк. filed Critical Саркоуд Байосайенс Инк.
Publication of RU2015102926A publication Critical patent/RU2015102926A/ru
Application granted granted Critical
Publication of RU2658015C2 publication Critical patent/RU2658015C2/ru

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B63/00—Purification; Separation; Stabilisation; Use of additives

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
RU2015102926A 2012-07-25 2013-07-25 Ингибитор ассоциированного с функцией лимфоцитов антигена-1 (lfa-1), способы его получения и его полиморф RU2658015C2 (ru)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201261675663P 2012-07-25 2012-07-25
US61/675,663 2012-07-25
US201261680099P 2012-08-06 2012-08-06
US61/680,099 2012-08-06
US201261729294P 2012-11-21 2012-11-21
US61/729,294 2012-11-21
PCT/US2013/052044 WO2014018748A1 (en) 2012-07-25 2013-07-25 Lfa-1 inhibitor and polymorph thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
RU2018121523A Division RU2778771C2 (ru) 2012-07-25 2013-07-25 Ингибитор ассоциированного с функцией лимфоцитов антигена-1 (lfa-1), способы его получения и его полиморф

Publications (2)

Publication Number Publication Date
RU2015102926A RU2015102926A (ru) 2016-09-20
RU2658015C2 true RU2658015C2 (ru) 2018-06-19

Family

ID=49995472

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2015102926A RU2658015C2 (ru) 2012-07-25 2013-07-25 Ингибитор ассоциированного с функцией лимфоцитов антигена-1 (lfa-1), способы его получения и его полиморф

Country Status (14)

Country Link
US (4) US9085553B2 (enExample)
EP (3) EP4406950A3 (enExample)
JP (3) JP6607780B2 (enExample)
KR (2) KR102157608B1 (enExample)
CN (2) CN104797574B (enExample)
AU (5) AU2013295706A1 (enExample)
BR (1) BR112015001608B1 (enExample)
CA (1) CA2879982C (enExample)
HK (1) HK1210782A1 (enExample)
IN (1) IN2015DN00847A (enExample)
MX (2) MX2015001098A (enExample)
RU (1) RU2658015C2 (enExample)
SI (1) SI3715345T1 (enExample)
WO (1) WO2014018748A1 (enExample)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1881823T3 (en) * 2005-05-17 2015-03-02 Sarcode Bioscience Inc COMPOSITION AND PROCEDURES FOR TREATMENT OF EYE DISORDERS
EP3632444A3 (en) * 2008-04-15 2020-08-26 SARcode Bioscience Inc. Topical lfa-1 antagonists for use in localized treatment of immune related disorders
EP4406950A3 (en) * 2012-07-25 2025-04-23 Bausch + Lomb Ireland Limited Lfa-1 inhibitor and polymorph thereof
EP3197454B1 (en) * 2014-09-25 2021-01-06 Novartis AG Continuous flow carboxylation reaction
CA2973471A1 (en) 2015-01-12 2016-07-21 Kedalion Therapeutics, Inc. Micro-droplet delivery device and methods
WO2017152027A1 (en) 2016-03-04 2017-09-08 Rynerson James M Method of treating an eye disorder by inhibiting or disrupting bacterial biofilm formation
EP3492466B1 (en) * 2016-07-29 2022-06-01 Wuhan LL Science And Technology Development Co., Ltd. Oral solid preparation and use thereof
AU2017310520A1 (en) 2016-08-12 2019-03-21 Silk Technologies, Ltd. Silk-derived protein for treating inflammation
CN108084067B (zh) * 2016-11-22 2019-08-30 重庆圣华曦药业股份有限公司 一种立他司特中间体的制备方法
WO2018136618A2 (en) 2017-01-20 2018-07-26 Kedalion Therapeutics, Inc. Piezoelectric fluid dispenser
CN106947792A (zh) * 2017-03-07 2017-07-14 上海倍殊生物科技有限公司 一种间甲砜基‑l‑苯丙氨酸的制备方法
CA3068522A1 (en) * 2017-06-30 2019-01-03 Scinopharm Taiwan, Ltd. Process for preparing lifitegrast and intermediates thereof
EP3868754A1 (en) 2017-07-24 2021-08-25 Interquim, S.A. Process for preparing and purifying the lfa-1 antagonist lifitegrast
WO2019026014A1 (en) * 2017-08-03 2019-02-07 Dr. Reddy's Laboratories Limited METHODS FOR PREPARING LIFITEGRAST AND ITS INTERMEDIATES
WO2019053607A1 (en) * 2017-09-18 2019-03-21 Glenmark Pharmaceuticals Limited PROCESS FOR PREPARING LIFITEGRAST
BR112020006874A2 (pt) * 2017-10-10 2020-10-06 Mankind Pharma Ltd. processo inovador para a preparação de lifitegrast
WO2019097547A1 (en) * 2017-11-15 2019-05-23 Cipla Limited An improved process for the preparation of lifitegrast or salts thereof
WO2019096996A1 (en) 2017-11-17 2019-05-23 Medichem, S.A. A process to obtain a tetrahydroisoquinoline derivative
AU2018380433B2 (en) 2017-12-08 2024-10-10 Bausch + Lomb Ireland Limited Fluid delivery alignment system
KR20200105657A (ko) 2018-01-15 2020-09-08 코그니보티스 에이비 산업용 로봇 아암
US10435395B1 (en) 2018-03-30 2019-10-08 Scinopharm Taiwan, Ltd. Crystal forms of lifitegrast
US11345683B2 (en) * 2018-03-31 2022-05-31 Aurobindo Pharma Ltd Process for the preparation of lifitegrast
US12350194B1 (en) 2018-04-12 2025-07-08 Bausch + Lomb Ireland Limited Topical ocular delivery of fluids with controlled mass dosing and wireless communication
US20190314197A1 (en) 2018-04-12 2019-10-17 Kedalion Therapeutics, Inc. Topical Ocular Delivery Methods and Devices for Use in the Same
IT201800006337A1 (it) * 2018-06-14 2019-12-14 Procedimento per la preparazione di lifitegrast
AU2019297326B2 (en) 2018-07-03 2025-01-09 Bausch + Lomb Ireland Limited Topical ocular delivery devices and methods for using the same
CN111100118A (zh) * 2018-10-29 2020-05-05 重庆圣华曦药业股份有限公司 一种立他司特杂质及其制备方法
CN109384717A (zh) * 2018-10-29 2019-02-26 广安凯特制药有限公司 5,7-二氯-1,2,3,4-四氢异喹啉-6-甲酸盐酸盐水合物及其制备方法和用途
CN111285855A (zh) * 2018-12-07 2020-06-16 苏州旺山旺水生物医药有限公司 一种制备化合物Lifitegrast的方法
CN111471003B (zh) * 2019-01-24 2022-09-23 上海皓元医药股份有限公司 一种立他司特中间体的制备方法
US11679028B2 (en) 2019-03-06 2023-06-20 Novartis Ag Multi-dose ocular fluid delivery system
US12097145B2 (en) 2019-03-06 2024-09-24 Bausch + Lomb Ireland Limited Vented multi-dose ocular fluid delivery system
CN114025759A (zh) * 2019-04-18 2022-02-08 阿祖拉眼科有限公司 用于治疗眼病的化合物和方法
CN110256343A (zh) * 2019-05-28 2019-09-20 苏州芝宇生物科技有限公司 3,5-二氯-4-溴异喹啉衍生物及其制备方法和应用
CN112409256B (zh) * 2019-08-21 2024-04-02 山东福长药业有限公司 5,7-二氯四氢异喹啉缩醛胺类化合物、其制备方法与应用
CN111057003A (zh) * 2019-12-06 2020-04-24 广安凯特制药有限公司 一种立他司特中间体5,7-二氯-1,2,3,4-四氢异喹啉的合成方法
US11938057B2 (en) 2020-04-17 2024-03-26 Bausch + Lomb Ireland Limited Hydrodynamically actuated preservative free dispensing system
US12090087B2 (en) 2020-04-17 2024-09-17 Bausch + Lomb Ireland Limited Hydrodynamically actuated preservative free dispensing system having a collapsible liquid reservoir
US12290472B2 (en) 2020-04-17 2025-05-06 Bausch + Lomb Ireland Limited Hydrodynamically actuated preservative free dispensing system
EP4120974A4 (en) 2020-04-17 2024-05-22 Bausch + Lomb Ireland Limited Hydrodynamically actuated preservative free dispensing system
CN111205275A (zh) * 2020-04-22 2020-05-29 南京佰麦生物技术有限公司 立他司特晶型及其制备方法
CN112321506B (zh) * 2020-11-26 2021-12-24 江西天戌药业有限公司 一种5,7-二氯-1,2,3,4-四氢异喹啉的制备方法
CN112500343B (zh) * 2020-12-26 2023-04-07 山东金城柯瑞化学有限公司 5,7-二氯-1,2,3,4-四氢异喹啉盐酸盐的合成方法
CN112300139A (zh) * 2020-12-29 2021-02-02 南京佰麦生物技术有限公司 立他司特水合物晶型及其制备方法
US11459351B1 (en) 2021-04-05 2022-10-04 Azura Ophthalmics Ltd. Compounds and methods for the treatment of ocular disorders
CN119060022A (zh) * 2021-09-18 2024-12-03 浙江大学医学院附属第一医院 立他司特的制备方法及其中间体化合物
CN114524767B (zh) * 2022-03-11 2022-10-18 成都道合尔医药技术有限公司 立他司特中间体5,7-二氯-1,2,3,4-四氢异喹啉盐酸盐的合成方法
CN115784950B (zh) * 2022-12-08 2024-06-28 广东先强药业有限公司 一种立他司特中间体的制备方法
CN116239532B (zh) * 2022-12-19 2023-11-07 浙江博崤生物制药有限公司 一种二氯四氢异喹啉羧酸的中间体及其制备方法和应用
CN116462644B (zh) * 2023-05-06 2024-11-19 上海华默西医药科技有限公司 一种2-(呋喃-2-基亚甲基)-4-硝基丁酸酯化合物及其制备方法和应用
WO2025186765A1 (en) * 2024-03-08 2025-09-12 Olon S.P.A. Process for preparing lifitegrast
WO2025186758A1 (en) * 2024-03-08 2025-09-12 Olon S.P.A. Process for preparing lifitegrast

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5510495A (en) * 1994-09-19 1996-04-23 The Du Pont Merck Pharmaceutical Company Process for the isolation and purification of ester functionalized imidazole intermediates by selective hydrolysis
RU2005117343A (ru) * 2002-12-20 2006-01-27 Астразенека Аб (Se) Новые производные пиперидина в качестве модуляторов хемокинового рецептора ccr5
US20110015394A1 (en) * 2008-01-01 2011-01-20 Cipla Limited Method of Synthesis of Bosentan, Its Polymorphic Forms and Its Salts
US20110092707A1 (en) * 2009-10-21 2011-04-21 Sarcode Corporation Crystalline Pharmaceutical and Methods of Preparation and Use Thereof
US20120115858A1 (en) * 2005-04-28 2012-05-10 Wyeth Llc Polymorph Form II of Tanaproget

Family Cites Families (108)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
JPS5759843A (en) * 1980-09-30 1982-04-10 Neos Co Ltd Perfluoroalkyl ether amide derivative and its preparation
IE52535B1 (en) 1981-02-16 1987-12-09 Ici Plc Continuous release pharmaceutical compositions
US4713244A (en) 1985-08-16 1987-12-15 Bausch & Lomb Incorporated Sustained-release formulation containing an amino acid polymer with a lower alkyl (C1 -C4) polar solvent
US4931279A (en) 1985-08-16 1990-06-05 Bausch & Lomb Incorporated Sustained release formulation containing an ion-exchange resin
US4668506A (en) 1985-08-16 1987-05-26 Bausch & Lomb Incorporated Sustained-release formulation containing and amino acid polymer
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
GB2209937B (en) 1987-09-21 1991-07-03 Depiopharm S A Water insoluble polypeptides
ES2064327T3 (es) 1987-11-02 1995-02-01 Baylor College Medicine Uso de icam-1 o de sus derivados funcionales para el tratamiento de una inflamacion no especifica.
CA1338839C (en) 1988-01-29 1997-01-14 Yoshio Sasaki Controlled release formulation
DE3802996A1 (de) 1988-02-02 1989-08-10 Cassella Ag Verwendung von 2-oxo-pyrrolidin-1-acetamid zur bestimmung der glomerulaeren filtrationsrate beim menschen
US5424399A (en) 1988-06-28 1995-06-13 The Children's Medical Center Corporation Human CR3α/β heterodimers
DE68923048T2 (de) 1988-08-23 1995-11-16 Dana Farber Cancer Inst Inc Alpha-Subeinheit des LFA-1-Leukocyt-Adhäsions-Rezeptors.
ES2141076T3 (es) 1988-09-01 2000-03-16 Bayer Ag Proteina del receptor de rinovirus humano que inhibe la infectividad del virus.
HU218904B (hu) 1988-09-28 2000-12-28 Dana-Farber Cancer Institute Eljárás ICAM-1-et kódoló rekombináns DNS előállítására, ICAM-1-et kifejező sejtek vagy ezzel kapcsolatos betegségek diagnosztizálására és a specifikus védekező rendszer válaszából eredő gyulladások kezelésére szolgáló gyógyszerkészítmények előállítására
US5149780A (en) 1988-10-03 1992-09-22 The Scripps Research Institute Peptides and antibodies that inhibit integrin-ligand binding
WO1990010652A1 (en) 1989-03-09 1990-09-20 Dana Farber Cancer Institute Method of treating viral infections using lfa-1
AU5553290A (en) 1989-04-28 1990-11-29 Baylor College Of Medicine Dissemination of hiv-1 infected cells
CH679207A5 (enExample) 1989-07-28 1992-01-15 Debiopharm Sa
WO1991019511A1 (en) 1990-06-18 1991-12-26 The General Hospital Corporation CONTROLLING CELLULAR IMMUNE/INFLAMMATORY RESPONSES WITH β2 INTEGRINS
CA2046830C (en) 1990-07-19 1999-12-14 Patrick P. Deluca Drug delivery system involving inter-action between protein or polypeptide and hydrophobic biodegradable polymer
US5318965A (en) 1990-08-24 1994-06-07 Abbott Laboratories Quinobenzoxazine, antineoplastic agents
CA2090427A1 (en) 1990-08-27 1992-02-28 Cetus Oncology Corporation Cd18 peptide medicaments for the treatment of disease
JP2995860B2 (ja) 1990-11-27 1999-12-27 味の素株式会社 新規ペプチド
US5288854A (en) 1990-11-28 1994-02-22 Center For Blood Research, Inc. Functional derivatives of ICAM-1 which are substantially capable of binding to LFA-1 but are substantially incapable of binding to MAC-1
CH683149A5 (fr) 1991-07-22 1994-01-31 Debio Rech Pharma Sa Procédé pour la préparation de microsphères en matériau polymère biodégradable.
WO1993006865A1 (en) 1991-10-04 1993-04-15 The United States of America, represented by The Secretary, Department of Health & Human Services Treatment of ocular inflammation by blockage of cell adhesion molecules
GB9211268D0 (en) 1992-05-28 1992-07-15 Ici Plc Salts of basic peptides with carboxyterminated polyesters
US5298492A (en) 1992-08-04 1994-03-29 Schering Corporation Diamino acid derivatives as antihypertensives
ZA936128B (en) 1992-08-21 1995-02-20 Genentech Inc Method for treating a LFA-1 mediated disorder
WO1994011400A1 (en) 1992-11-18 1994-05-26 Helsinki University Licensing Ltd. Oy Peptides from human icam-2 and from human icam-1 and their analogs for use in therapy and diagnosis
US5672659A (en) 1993-01-06 1997-09-30 Kinerton Limited Ionic molecular conjugates of biodegradable polyesters and bioactive polypeptides
NZ261250A (en) 1993-01-06 1997-08-22 Kinerton Ltd Ionic conjugates of polypeptides
US5424289A (en) 1993-07-30 1995-06-13 Alza Corporation Solid formulations of therapeutic proteins for gastrointestinal delivery
US5397791A (en) 1993-08-09 1995-03-14 Merck & Co., Inc. Fibrinogen receptor antagonists
DE59409322D1 (de) 1993-12-03 2000-06-08 Hoffmann La Roche Essigsäurederivate als Arzneimittel
US5470953A (en) 1993-12-23 1995-11-28 Icos Corporation Human β2 integrin α subunit
WO1995028170A1 (en) 1994-04-19 1995-10-26 The University Of Kansas Icam-1/lfa-1 short-chain peptides and method of using same
US5849327A (en) 1994-07-29 1998-12-15 Advanced Polymer Systems, Inc. Delivery of drugs to the lower gastrointestinal tract
US5585359A (en) 1994-09-29 1996-12-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
EP0710657B1 (de) 1994-11-02 1998-08-26 MERCK PATENT GmbH Adhäsionsrezeptor-Antagonisten
US5612052A (en) 1995-04-13 1997-03-18 Poly-Med, Inc. Hydrogel-forming, self-solvating absorbable polyester copolymers, and methods for use thereof
US5747035A (en) 1995-04-14 1998-05-05 Genentech, Inc. Polypeptides with increased half-life for use in treating disorders involving the LFA-1 receptor
US5877224A (en) 1995-07-28 1999-03-02 Rutgers, The State University Of New Jersey Polymeric drug formulations
US5980945A (en) 1996-01-16 1999-11-09 Societe De Conseils De Recherches Et D'applications Scientifique S.A. Sustained release drug formulations
US5840332A (en) 1996-01-18 1998-11-24 Perio Products Ltd. Gastrointestinal drug delivery system
CA2250981C (en) 1996-04-23 2002-07-02 Kinerton Limited Acidic polylactic polymers
HRP970493A2 (en) 1996-09-23 1998-08-31 Wienman E. Phlips Oral delayed immediate release medical formulation and method for preparing the same
CA2217134A1 (en) 1996-10-09 1998-04-09 Sumitomo Pharmaceuticals Co., Ltd. Sustained release formulation
IL129344A0 (en) 1996-11-27 2000-02-17 Du Pont Pharm Co Novel integrin receptor antagonists
US5968895A (en) 1996-12-11 1999-10-19 Praecis Pharmaceuticals, Inc. Pharmaceutical formulations for sustained drug delivery
US5893985A (en) 1997-03-14 1999-04-13 The Lincoln Electric Company Plasma arc torch
AR012443A1 (es) 1997-04-16 2000-10-18 Uriach & Cia Sa J Nuevas carboxamidas como inhibidores de la agregacion plaquetaria, procedimiento para su preparacion, composiciones farmaceuticas que loscontienen y uso de los mismos en la manufactura de medicamentos
HUP0101587A3 (en) 1998-03-27 2003-03-28 Genentech Inc Antagonists for treatment of cd11/cd18 adhesion receptor mediated disorders
US6331640B1 (en) 1998-10-13 2001-12-18 Hoffmann-La Roche Inc. Diaminopropionic acid derivatives
US7097851B1 (en) 1998-11-27 2006-08-29 Kanji Takada Oral formulation for gastrointestinal drug delivery
IT1304152B1 (it) 1998-12-10 2001-03-08 Mediolanum Farmaceutici Srl Composizioni comprendenti un peptide ed acido polilattico-glicolicoatte alla preparazione di impianti sottocutanei aventi un prolungato
US6670321B1 (en) 1998-12-30 2003-12-30 The Children's Medical Center Corporation Prevention and treatment for retinal ischemia and edema
WO2000040262A1 (en) 1999-01-05 2000-07-13 The Flinders University Of South Australia Novel agents and methods for treatment and diagnosis of ocular disorders
AU2847200A (en) 1999-01-27 2000-08-18 G.D. Searle & Co. Novel hydroxyamidino carboxylate derivatives useful as nitric oxide synthase inhibitors
EP1028114A1 (en) 1999-02-13 2000-08-16 Aventis Pharma Deutschland GmbH Novel guanidine derivatives as inhibitors of cell adhesion
JP4928668B2 (ja) 1999-03-31 2012-05-09 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 制御放出製剤中の前糊化澱粉
AU1186401A (en) 1999-06-23 2001-01-22 Sedum Laboratories, Inc. Ionically formulated biomolecule microcarriers
DE60006250T2 (de) 1999-08-18 2004-07-29 Société de Conseils de Recherches et d'Applications Scientifiques S.A.S. Formulierung zur verzögerten freisetzung von peptiden
ECSP003707A (es) 1999-10-13 2002-05-23 Novartis Ag Diazepanes
US6294522B1 (en) 1999-12-03 2001-09-25 Cv Therapeutics, Inc. N6 heterocyclic 8-modified adenosine derivatives
US6605597B1 (en) 1999-12-03 2003-08-12 Cv Therapeutics, Inc. Partial or full A1agonists-N-6 heterocyclic 5′-thio substituted adenosine derivatives
AU768324B2 (en) 1999-12-14 2003-12-11 Genentech Inc. TNF-alpha antagonist and LFA-1 antagonist for treating LFA-1 or TNF-alpha mediated disorder
CA2396037A1 (en) 1999-12-31 2001-07-12 Rutgers, The State University Pharmaceutical formulation for regulating the timed release of biologically active compounds based on a polymer matrix
AU775905B2 (en) 1999-12-31 2004-08-19 Rutgers, The State University Pharmaceutical formulation composed of a polymer blend and an active compound for time-controlled release
US7521061B2 (en) 1999-12-31 2009-04-21 Rutgers, The State University Of New Jersey Pharmaceutical formulation for regulating the timed release of biologically active compounds based on a polymer matrix
US20030064105A1 (en) 2000-08-25 2003-04-03 Myung-Jin Kim Lipophilic-coated microparticle containing a protein drug and formulation comprising same
US6515124B2 (en) 2000-02-09 2003-02-04 Hoffman-La Roche Inc. Dehydroamino acids
JP2003532703A (ja) 2000-05-05 2003-11-05 ソシエテ・ド・コンセイユ・ド・ルシエルシエ・エ・ダアツプリカーション・シヤンテイフイツク・（エス．セー．エール．アー．エス） 新規アミノ酸誘導体及びその医薬としての使用
GB0011817D0 (en) 2000-05-16 2000-07-05 Pharmacia & Upjohn Spa Antagonists of integrin receptors
AU2001268718B2 (en) 2000-06-29 2006-01-05 Abbott Laboratories Aryl phenylheterocyclyl sulfide derivatives and their use as cell adhesion-inhibiting anti-inflammatory and immune-suppressive agents
JP2002030052A (ja) * 2000-07-18 2002-01-29 Tosoh Corp ヒドロキシアミノカルボン酸、その用途、及びその製造法
AU2001290272A1 (en) * 2000-09-27 2002-04-08 Asahi Glass Company, Limited Process for producing acyl fluoride and carboxylic acid salt
AR030817A1 (es) 2000-10-02 2003-09-03 Novartis Ag Derivados de diazacicloalcanodiona
GB0025208D0 (en) 2000-10-13 2000-11-29 Euro Celtique Sa Delayed release pharmaceutical formulations
US6653478B2 (en) 2000-10-27 2003-11-25 Ortho-Mcneil Pharmaceutical, Inc. Substituted benzimidazol-2-ones as vasopressin receptor antagonists and neuropeptide Y modulators
DE10055857A1 (de) 2000-11-10 2002-08-22 Creative Peptides Sweden Ab Dj Neue pharmazeutische Depotformulierung
GB0028367D0 (en) 2000-11-21 2001-01-03 Celltech Chiroscience Ltd Chemical compounds
KR20030051882A (ko) 2000-11-28 2003-06-25 제넨테크, 인크. Ｌｆａ-1 대항제 화합물
WO2002050080A1 (en) 2000-12-19 2002-06-27 Boehringer Ingelheim Pharmaceuticals, Inc. Small molecules useful in the treatment of inflammatory disease
CA2435415A1 (en) 2001-01-26 2002-08-01 Debio Recherche Pharmaceutique S.A. Microparticles of biodegradable polymer encapsulating a biologically active substance
ES2275808T3 (es) 2001-02-06 2007-06-16 Pfizer Products Inc. Composiciones farmaceuticas para el tratamiento de trastornos del snc y otros trastornos.
AU2002322478A1 (en) 2001-03-02 2002-12-16 Medimmune, Inc. Methods of administering/dosing cd2 antagonists for the prevention and treatment of autoimmune disorders or inflammatory disorders
US20020176841A1 (en) 2001-03-19 2002-11-28 Praecis Pharmaceuticals Inc. Pharmaceutical formulations for sustained release
US6872382B1 (en) 2001-05-21 2005-03-29 Alcon, Inc. Use of selective PDE IV inhibitors to treat dry eye disorders
ES2296926T3 (es) 2001-06-06 2008-05-01 Aventis Pharma Limited Tetrahidroisoquinolinas sustituidas para usar en el tratamiento de enfermedades inflamatorias.
KR20040066177A (ko) 2001-12-19 2004-07-23 알자 코포레이션 친수성 거대분자의 경구 생체이용률을 증가시키기 위한제형 및 투여 형태
RU2004129577A (ru) 2002-03-04 2005-04-10 Сосьете Де Консей Де Решерш Э Д`Аппликасьон (Fr) Лекарственные композиции с замедленным высвобождением, содержащие пептид-носитель
CA2497977A1 (en) 2002-09-20 2004-04-01 Alcon, Inc. Use of cytokine synthesis inhibitors for the treatment of dry eye disorders
US7785578B2 (en) 2002-10-11 2010-08-31 Aciont, Inc. Non-invasive ocular drug delivery
US7544699B2 (en) 2003-08-08 2009-06-09 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions, and methods of use
US7459472B2 (en) 2003-08-08 2008-12-02 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions, and methods of use
WO2005042710A1 (en) 2003-10-28 2005-05-12 The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Use of statin to kill ebv-transformed b cells
US7314938B2 (en) 2003-11-05 2008-01-01 Sunesis Pharmaceuticals, Inc. Modulators of cellular adhesion
GT200500139A (es) 2004-06-08 2005-07-25 Metodo para la preparacion de acidos hidroxamicos
DK1881823T3 (en) 2005-05-17 2015-03-02 Sarcode Bioscience Inc COMPOSITION AND PROCEDURES FOR TREATMENT OF EYE DISORDERS
WO2007057919A2 (en) * 2005-10-25 2007-05-24 Alembic Limited An improved process for preparation of (s)-n-(1-carboxy-2-methyl-prop-1-yl)-n-pentanoyl-n-[2'-(1h-tetrazol-5-yl)biphenyl-4-ylmethyl]-amine
JP4193895B2 (ja) 2006-10-12 2008-12-10 横河電機株式会社 欠陥検査装置
CN101873797A (zh) 2007-10-19 2010-10-27 萨可德公司 用于治疗糖尿病性视网膜病的组合物和方法
US8080562B2 (en) 2008-04-15 2011-12-20 Sarcode Bioscience Inc. Crystalline pharmaceutical and methods of preparation and use thereof
EP4406950A3 (en) 2012-07-25 2025-04-23 Bausch + Lomb Ireland Limited Lfa-1 inhibitor and polymorph thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5510495A (en) * 1994-09-19 1996-04-23 The Du Pont Merck Pharmaceutical Company Process for the isolation and purification of ester functionalized imidazole intermediates by selective hydrolysis
RU2005117343A (ru) * 2002-12-20 2006-01-27 Астразенека Аб (Se) Новые производные пиперидина в качестве модуляторов хемокинового рецептора ccr5
US20120115858A1 (en) * 2005-04-28 2012-05-10 Wyeth Llc Polymorph Form II of Tanaproget
US20110015394A1 (en) * 2008-01-01 2011-01-20 Cipla Limited Method of Synthesis of Bosentan, Its Polymorphic Forms and Its Salts
US20110092707A1 (en) * 2009-10-21 2011-04-21 Sarcode Corporation Crystalline Pharmaceutical and Methods of Preparation and Use Thereof

Also Published As

Publication number Publication date
EP4406950A2 (en) 2024-07-31
EP3715345B8 (en) 2024-05-29
US20150336939A1 (en) 2015-11-26
RU2018121523A3 (enExample) 2022-02-25
KR20150067129A (ko) 2015-06-17
US10214517B2 (en) 2019-02-26
EP2877465A4 (en) 2016-05-11
JP2015523398A (ja) 2015-08-13
HK1210782A1 (en) 2016-05-06
EP4406950A3 (en) 2025-04-23
KR102157608B1 (ko) 2020-09-18
WO2014018748A1 (en) 2014-01-30
BR112015001608A2 (pt) 2017-07-04
EP3715345B1 (en) 2024-04-10
CA2879982C (en) 2020-09-01
RU2015102926A (ru) 2016-09-20
AU2023204287A1 (en) 2023-07-27
AU2017265071B2 (en) 2019-08-22
CN110922393A (zh) 2020-03-27
US20140031387A1 (en) 2014-01-30
AU2023204287B2 (en) 2025-08-21
AU2017265071A1 (en) 2017-12-14
CN104797574B (zh) 2019-11-22
JP6607780B2 (ja) 2019-11-20
AU2013295706A1 (en) 2015-02-19
RU2018121523A (ru) 2019-12-13
HK1210145A1 (en) 2016-04-15
JP2020128433A (ja) 2020-08-27
US20180118726A1 (en) 2018-05-03
US20190382389A1 (en) 2019-12-19
MX2015001098A (es) 2015-09-25
US9708303B2 (en) 2017-07-18
CA2879982A1 (en) 2014-01-30
EP2877465A1 (en) 2015-06-03
CN104797574A (zh) 2015-07-22
SI3715345T1 (sl) 2024-07-31
MX2020001602A (es) 2020-07-13
AU2019210525B2 (en) 2020-12-17
AU2020281063A1 (en) 2021-01-07
EP3715345A3 (en) 2020-11-11
JP7008750B2 (ja) 2022-01-25
EP3715345A2 (en) 2020-09-30
AU2019210525A1 (en) 2019-08-15
IN2015DN00847A (enExample) 2015-06-12
US9085553B2 (en) 2015-07-21
US10906892B2 (en) 2021-02-02
JP2018162313A (ja) 2018-10-18
KR20200108932A (ko) 2020-09-21
BR112015001608B1 (pt) 2022-08-23

Similar Documents

Publication Publication Date Title
RU2658015C2 (ru) Ингибитор ассоциированного с функцией лимфоцитов антигена-1 (lfa-1), способы его получения и его полиморф
EP0474561A1 (fr) Arylalkylamines, procédé pour leur préparation et compositions pharmaceutiques les contenant
EP3481200B1 (en) Processes for the preparation of 4-alkoxy-3-(acyl or alkyl)oxypicolinamides
WO2017108960A1 (en) Method for producing monomethyl fumarate compounds
JP2013540779A (ja) ２−シリロキシ−ピロールを使用する３−（（ピロール−２−イル）メチレン）−２−ピロロンの調製方法
RU2778771C2 (ru) Ингибитор ассоциированного с функцией лимфоцитов антигена-1 (lfa-1), способы его получения и его полиморф
HK1210145B (zh) Lfa-1抑制剂及其多晶型物
EP3210975A1 (en) Cocrystals of lorcaserin
RU2444516C2 (ru) Способ синтеза производных имидазоламинокислот и родственных соединений
EP0859773A1 (en) Phenol derivatives with pharmaceutical activity
SK8862002A3 (en) Non peptide tachykinin receptor antagonists
JP2006188505A (ja) インドール類の製造方法および製造中間体

Legal Events

Date Code Title Description
PC41 Official registration of the transfer of exclusive right

Effective date: 20200907