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MX2020001602A - Inhibidor del antigeno-1 asociado a la funcion del linfocito (lfa-1) y polimorfo del mismo. - Google Patents

Inhibidor del antigeno-1 asociado a la funcion del linfocito (lfa-1) y polimorfo del mismo.

Info

Publication number
MX2020001602A
MX2020001602A MX2020001602A MX2020001602A MX2020001602A MX 2020001602 A MX2020001602 A MX 2020001602A MX 2020001602 A MX2020001602 A MX 2020001602A MX 2020001602 A MX2020001602 A MX 2020001602A MX 2020001602 A MX2020001602 A MX 2020001602A
Authority
MX
Mexico
Prior art keywords
lfa
polymorph
inhibitor
disclosed
intermediates
Prior art date
Application number
MX2020001602A
Other languages
English (en)
Inventor
Michael Hall
James Robert Zeller
Subashree Iyer
Sripathy Venkatraman
Elisabeth C A Brot
Original Assignee
Novartis Ag
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=MX2020001602(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of MX2020001602A publication Critical patent/MX2020001602A/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic 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
    • C07D407/02Heterocyclic 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
    • C07D407/06Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B63/00Purification; Separation; Stabilisation; Use of additives

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (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)

Abstract

La presente invención se refiere a métodos de preparación y purificación de un compuesto, intermediarios del mismo, un polimorfo del mismo, y compuestos relacionados. También se describen las formulaciones y usos de las mismas en el tratamiento de enfermedades mediadas por LFA-1.
MX2020001602A 2012-07-25 2015-01-23 Inhibidor del antigeno-1 asociado a la funcion del linfocito (lfa-1) y polimorfo del mismo. MX2020001602A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261675663P 2012-07-25 2012-07-25
US201261680099P 2012-08-06 2012-08-06
US201261729294P 2012-11-21 2012-11-21

Publications (1)

Publication Number Publication Date
MX2020001602A true MX2020001602A (es) 2020-07-13

Family

ID=49995472

Family Applications (2)

Application Number Title Priority Date Filing Date
MX2015001098A MX2015001098A (es) 2012-07-25 2013-07-25 Inhibidor del antigeno-1 asociado a la funcion del linfocito (lfa-1) y polimorfo del mismo.
MX2020001602A MX2020001602A (es) 2012-07-25 2015-01-23 Inhibidor del antigeno-1 asociado a la funcion del linfocito (lfa-1) y polimorfo del mismo.

Family Applications Before (1)

Application Number Title Priority Date Filing Date
MX2015001098A MX2015001098A (es) 2012-07-25 2013-07-25 Inhibidor del antigeno-1 asociado a la funcion del linfocito (lfa-1) y polimorfo del mismo.

Country Status (14)

Country Link
US (4) US9085553B2 (es)
EP (3) EP3715345B8 (es)
JP (3) JP6607780B2 (es)
KR (2) KR20200108932A (es)
CN (2) CN110922393A (es)
AU (5) AU2013295706A1 (es)
BR (1) BR112015001608B1 (es)
CA (1) CA2879982C (es)
HK (1) HK1210782A1 (es)
IN (1) IN2015DN00847A (es)
MX (2) MX2015001098A (es)
RU (1) RU2658015C2 (es)
SI (1) SI3715345T1 (es)
WO (1) WO2014018748A1 (es)

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1881823E (pt) * 2005-05-17 2015-03-02 Sarcode Bioscience Inc Composições e métodos para o tratamento de transtornos oculares
CN102056485A (zh) * 2008-04-15 2011-05-11 萨可德公司 用于局部治疗免疫相关疾病的局部lfa-1拮抗剂
CA2879982C (en) 2012-07-25 2020-09-01 Sarcode Bioscience Inc. Lfa-1 inhibitor and polymorph thereof
CA2960392A1 (en) * 2014-09-25 2016-03-31 Sarcode Bioscience Inc. Process to prepare 5,7-dichloro-3,4-dihydro-1h-isoquinolin-6-carboxylic acid using a continuous flow carboxylation reaction
EP3244851B1 (en) 2015-01-12 2024-10-16 Bausch + Lomb Ireland Limited Micro-droplet delivery device
JP2019507193A (ja) 2016-03-04 2019-03-14 ジェームズ・エム・ライナーソン 細菌のバイオフィルム形成を阻止又は妨害することによって眼障害を治療する方法
US11013736B2 (en) * 2016-07-29 2021-05-25 Wuhan Ll Science And Technology Development Co., Ltd. Oral solid preparation and use thereof
EP3496662A4 (en) 2016-08-12 2019-10-30 Silk Technologies Ltd. SILICONE PROTEIN FOR THE TREATMENT OF IGNITION
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
KR102412086B1 (ko) 2017-01-20 2022-06-22 켄달리온 테라퓨틱스 인코포레이티드 압전 유체 분배기
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
CN110944996A (zh) * 2017-07-24 2020-03-31 因特奎姆私人控股公司 制备和纯化lfa-1拮抗剂立他司特的方法
US20200369652A1 (en) * 2017-08-03 2020-11-26 Dr. Reddy's Laboratories Limited Processes for preparation of lifitegrast and intermediates thereof
WO2019053607A1 (en) * 2017-09-18 2019-03-21 Glenmark Pharmaceuticals Limited PROCESS FOR PREPARING LIFITEGRAST
KR102716461B1 (ko) * 2017-10-10 2024-10-11 맨카인드 파마 리미티드 리피테그라스트의 신규 제조 방법
WO2019097547A1 (en) * 2017-11-15 2019-05-23 Cipla Limited An improved process for the preparation of lifitegrast or salts thereof
US11001574B2 (en) 2017-11-17 2021-05-11 Medichem S.A. Process to obtain a tetrahydroisoquinoline derivative
CA3083219A1 (en) 2017-12-08 2019-06-13 Reynaldo Quintana Fluid delivery alignment system
TWI844041B (zh) 2018-01-15 2024-06-01 瑞典商寇格尼博迪克斯有限公司 工業機器人手臂
US10435395B1 (en) 2018-03-30 2019-10-08 Scinopharm Taiwan, Ltd. Crystal forms of lifitegrast
WO2019186520A1 (en) * 2018-03-31 2019-10-03 Aurobindo Pharma Limited A process for the preparation of lifitegrast
US20190314198A1 (en) 2018-04-12 2019-10-17 Kedalion Therapeutics, Inc. Topical Ocular Delivery Methods and Devices for Use in the Same
US12350194B1 (en) 2018-04-12 2025-07-08 Bausch + Lomb Ireland Limited Topical ocular delivery of fluids with controlled mass dosing and wireless communication
IT201800006337A1 (it) * 2018-06-14 2019-12-14 Procedimento per la preparazione di lifitegrast
JP2021529598A (ja) 2018-07-03 2021-11-04 ケダリオン セラピューティックス,インコーポレイテッド 局所眼内送達装置及びこれを使用した方法
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
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
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
US12097145B2 (en) 2019-03-06 2024-09-24 Bausch + Lomb Ireland Limited Vented multi-dose ocular fluid delivery system
US11679028B2 (en) 2019-03-06 2023-06-20 Novartis Ag Multi-dose ocular fluid delivery system
JP7700045B2 (ja) 2019-04-18 2025-06-30 アズーラ オフサルミックス エルティーディー. 眼障害を処置するための化合物および方法
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
US12496218B1 (en) 2019-11-12 2025-12-16 Bausch + Lomb Ireland Limited Fractionated topical ocular drug delivery methods and devices for use in the same
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
US12290472B2 (en) 2020-04-17 2025-05-06 Bausch + Lomb Ireland Limited Hydrodynamically actuated preservative free dispensing system
EP4120973A4 (en) 2020-04-17 2024-04-17 Bausch + Lomb Ireland Limited Hydrodynamically actuated preservative free dispensing system having a collapsible liquid reservoir
IL297215A (en) 2020-04-17 2022-12-01 Kedallon Therapeutics Inc A hydrodynamically activated preservative free distribution system
US11938057B2 (en) 2020-04-17 2024-03-26 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
CN116063286A (zh) * 2021-10-29 2023-05-05 威智医药有限公司 一种立他司特及其中间体的制备方法
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
WO2025186758A1 (en) * 2024-03-08 2025-09-12 Olon S.P.A. Process for preparing lifitegrast
WO2025186765A1 (en) * 2024-03-08 2025-09-12 Olon S.P.A. Process for preparing lifitegrast

Family Cites Families (113)

* 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
US4931279A (en) 1985-08-16 1990-06-05 Bausch & Lomb Incorporated Sustained release formulation containing an ion-exchange resin
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
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
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
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.
ATE90570T1 (de) 1988-01-29 1993-07-15 Sumitomo Pharma Verbesserte formulierungen mit kontrollierter abgabe.
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
EP0362526B1 (en) 1988-08-23 1995-06-14 Dana Farber Cancer Institute The Alpha-subunit of the LFA-1 leukocyte adhesion receptor
DE68929096T2 (de) 1988-09-01 2000-05-11 Bayer Corp., Pittsburgh Menschliches Rhinovirusrezeptorprotein, das die Virusinfektionsanfälligkeit hemmt
JP2976381B2 (ja) 1988-09-28 1999-11-10 ダナ ファーバー キャンサー インスティテュート 細胞間粘着分子およびその結合性リガンド
US5149780A (en) 1988-10-03 1992-09-22 The Scripps Research Institute Peptides and antibodies that inhibit integrin-ligand binding
EP0462184A4 (en) 1989-03-09 1992-01-08 Dana Farber Cancer Institute Method of treating viral infections using lfa-1
ZA903223B (en) 1989-04-28 1991-02-27 Baylor College Medicine Dissemination of hiv-1 infected cells
CH679207A5 (es) 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
JPH06500555A (ja) 1990-08-27 1994-01-20 カイロン コーポレイション 病気の処置のためのペプチドの薬物
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.
JP3679112B2 (ja) 1991-10-04 2005-08-03 アメリカ合衆国 細胞接着分子の遮断による眼の炎症の治療
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
DK0656789T3 (da) 1992-08-21 1998-08-24 Genentech Inc Fremgangsmåde til behandling af en LFA-1-medieretforstyrrelse.
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
EP0678018B1 (en) 1993-01-06 2003-04-09 Kinerton Limited Ionic molecular conjugates of biodegradable polyesters and bioactive polypeptides
US5672659A (en) 1993-01-06 1997-09-30 Kinerton Limited Ionic molecular conjugates of biodegradable polyesters and bioactive 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
ES2147210T3 (es) 1993-12-03 2000-09-01 Hoffmann La Roche Derivados de acido acetico como medicamentos.
US5470953A (en) 1993-12-23 1995-11-28 Icos Corporation Human β2 integrin α subunit
CA2188287A1 (en) 1994-04-19 1995-10-26 Stephen Benedict 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
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
US5585359A (en) 1994-09-29 1996-12-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
ATE170179T1 (de) 1994-11-02 1998-09-15 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
JP3155013B2 (ja) 1996-04-23 2001-04-09 キナートン・リミテッド 酸性ポリ乳酸ポリマー
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
ES2270475T3 (es) 1996-11-27 2007-04-01 Bristol-Myers Squibb Pharma Company Nuevos antagonistas de receptores de integrina.
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
EP1063982B1 (en) 1998-03-27 2007-02-14 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
ID29085A (id) 1998-11-27 2001-07-26 Kanji Takada Suatu formulasi oral untuk penghantaran obat gastrointestinal
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
DK1140170T3 (da) 1999-01-05 2006-10-23 Univ Southern Australia Antistoffragmenter til topisk behandling af öjensygdomme
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
EE05022B1 (et) 1999-03-31 2008-06-16 Janssen Pharmaceutica N.V. Eelthelatineeritud tärklise kasutamine hüdrofiilses kontrollitud vabanemisega preparaadis ja hüdrofiilne kontrollitud vabanemisega preparaat
US6645525B1 (en) 1999-06-23 2003-11-11 Sedum Laboratories, Inc. Ionically formulated biomolecule microcarriers
KR20020031407A (ko) 1999-08-18 2002-05-01 다푸르 가브리에 펩타이드의 서방형 제제
ECSP003707A (es) 1999-10-13 2002-05-23 Novartis Ag Diazepanes
US6605597B1 (en) 1999-12-03 2003-08-12 Cv Therapeutics, Inc. Partial or full A1agonists-N-6 heterocyclic 5′-thio substituted adenosine derivatives
US6294522B1 (en) 1999-12-03 2001-09-25 Cv Therapeutics, Inc. N6 heterocyclic 8-modified adenosine derivatives
ES2311483T3 (es) 1999-12-14 2009-02-16 Genentech, Inc. Anatagonista del tnf-alfa y antagonista del lfa-1 para el tratamiento de la artritis reumatoide.
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
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
JP4917726B2 (ja) 1999-12-31 2012-04-18 ルトガーズ、ザ ステイト ユニバーシティ オブ ニュージャージー ポリマー混合物および活性化合物からなる徐放用医薬製剤
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
EP1296943A1 (fr) 2000-05-05 2003-04-02 Societe De Conseils De Recherches Et D'applications Scientifiques S.A. (S.C.R.A.S.) Derives d'aminoacides et leur application a titre de medicaments
GB0011817D0 (en) 2000-05-16 2000-07-05 Pharmacia & Upjohn Spa Antagonists of integrin receptors
CA2414461A1 (en) 2000-06-29 2002-01-10 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
CN1466562A (zh) * 2000-09-27 2004-01-07 ������������ʽ���� 酰氟类和羧酸盐类的制备方法
PE20020420A1 (es) 2000-10-02 2002-06-27 Novartis Ag Derivados de diazacicloalcanodiona como antagonistas del antigeno asociado a la funcion del linfocito-1 (lfa-1)
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
CA2429353A1 (en) 2000-11-28 2002-08-01 Genentech, Inc. Lfa-1 antagonist compounds
US20030008848A1 (en) 2000-12-19 2003-01-09 Fleck Roman Wolfgang 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
EP1231212B1 (en) 2001-02-06 2006-12-20 Pfizer Products Inc. Pharmaceutical compositions for the treatment of disorders of the CNS and other disorders
WO2002069904A2 (en) 2001-03-02 2002-09-12 Medimmune, Inc. Cd2 antagonists for treatment of autoimmune or inflammatory disease
WO2002074247A2 (en) 2001-03-19 2002-09-26 Praecis Pharmaceuticals Incorporated 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.
HUP0402451A3 (en) 2001-12-19 2008-04-28 Alza Corp Formulation and dosage form for increasing oral bioavailability of hydrophilic macromolecules
AU2003224649B2 (en) 2002-03-04 2006-09-07 Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. Sustained release drug formulations containing a carrier peptide
PL374700A1 (pl) 2002-09-20 2005-10-31 Alcon, Inc. Zastosowanie inhibitorów syntezy cytokiny do leczenia zespołu suchego oka
US7785578B2 (en) 2002-10-11 2010-08-31 Aciont, Inc. Non-invasive ocular drug delivery
RU2005117343A (ru) * 2002-12-20 2006-01-27 Астразенека Аб (Se) Новые производные пиперидина в качестве модуляторов хемокинового рецептора ccr5
AU2004263508A1 (en) 2003-08-08 2005-02-17 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions, and methods of use
US7501538B2 (en) 2003-08-08 2009-03-10 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
EP1682537B1 (en) 2003-11-05 2012-03-28 SARcode Bioscience Inc. Modulators of cellular adhesion
GT200500139A (es) 2004-06-08 2005-07-25 Metodo para la preparacion de acidos hidroxamicos
MX2007013469A (es) * 2005-04-28 2008-01-22 Wyeth Corp Forma ii polimorfa de tanaproget.
PT1881823E (pt) 2005-05-17 2015-03-02 Sarcode Bioscience Inc Composições e métodos para o tratamento de transtornos oculares
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
MX2010004281A (es) 2007-10-19 2010-09-10 Sarcode Corp Composiciones y metodos para el tratamiento de la retinopatia diabetica.
US8481730B2 (en) * 2008-01-01 2013-07-09 Cipla Limited Method of synthesis of Bosentan, its polymorphic forms and its salts
US8080562B2 (en) 2008-04-15 2011-12-20 Sarcode Bioscience Inc. Crystalline pharmaceutical and methods of preparation and use thereof
WO2011050175A1 (en) * 2009-10-21 2011-04-28 Sarcode Corporation Crystalline pharmaceutical and methods of preparation and use thereof
CA2879982C (en) 2012-07-25 2020-09-01 Sarcode Bioscience Inc. Lfa-1 inhibitor and polymorph thereof

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