AU2017257185B9 - Phospholipase A2 inhibitors for immediate treatment of venom toxicity that causes hemolysis, cerebral edema, and acute kidney injury - Google Patents

Phospholipase A2 inhibitors for immediate treatment of venom toxicity that causes hemolysis, cerebral edema, and acute kidney injury Download PDF

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Publication number
AU2017257185B9
AU2017257185B9 AU2017257185A AU2017257185A AU2017257185B9 AU 2017257185 B9 AU2017257185 B9 AU 2017257185B9 AU 2017257185 A AU2017257185 A AU 2017257185A AU 2017257185 A AU2017257185 A AU 2017257185A AU 2017257185 B9 AU2017257185 B9 AU 2017257185B9
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Prior art keywords
pla2
inhibitor
venom
varespladib
administered
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AU2017257185A
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AU2017257185A1 (en
AU2017257185B8 (en
AU2017257185B2 (en
Inventor
Matthew R. Lewin
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Ophirex Inc
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Ophirex Inc
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Publication of AU2017257185B9 publication Critical patent/AU2017257185B9/en
Publication of AU2017257185B8 publication Critical patent/AU2017257185B8/en
Priority to AU2023233187A priority Critical patent/AU2023233187A1/en
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    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/4045Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/192Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • A61K31/366Lactones having six-membered rings, e.g. delta-lactones
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/405Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • A61P39/02Antidotes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Toxicology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
AU2017257185A 2016-04-29 2017-05-01 Phospholipase A2 inhibitors for immediate treatment of venom toxicity that causes hemolysis, cerebral edema, and acute kidney injury Active AU2017257185B8 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2023233187A AU2023233187A1 (en) 2016-04-29 2023-09-22 Phospholipase A2 inhibitors for immediate treatment of venom toxicity that causes hemolysis, cerebral edema, and acute kidney injury

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201662329611P 2016-04-29 2016-04-29
US62/329,611 2016-04-29
US201662340075P 2016-05-23 2016-05-23
US62/340,075 2016-05-23
US201662423693P 2016-11-17 2016-11-17
US62/423,693 2016-11-17
PCT/US2017/030436 WO2017190141A1 (en) 2016-04-29 2017-05-01 Pla2 and hmg-coa inhibitors for treatment of pathological conditions causing hemolysis, cerebral edema, and acute kidney injury

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2023233187A Division AU2023233187A1 (en) 2016-04-29 2023-09-22 Phospholipase A2 inhibitors for immediate treatment of venom toxicity that causes hemolysis, cerebral edema, and acute kidney injury

Publications (4)

Publication Number Publication Date
AU2017257185A1 AU2017257185A1 (en) 2018-11-22
AU2017257185B2 AU2017257185B2 (en) 2023-06-22
AU2017257185B9 true AU2017257185B9 (en) 2023-07-06
AU2017257185B8 AU2017257185B8 (en) 2023-07-06

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AU2017257185A Active AU2017257185B8 (en) 2016-04-29 2017-05-01 Phospholipase A2 inhibitors for immediate treatment of venom toxicity that causes hemolysis, cerebral edema, and acute kidney injury
AU2023233187A Pending AU2023233187A1 (en) 2016-04-29 2023-09-22 Phospholipase A2 inhibitors for immediate treatment of venom toxicity that causes hemolysis, cerebral edema, and acute kidney injury

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Country Status (9)

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US (2) US12383531B2 (enExample)
EP (1) EP3448378B1 (enExample)
JP (2) JP7542935B2 (enExample)
KR (2) KR102723249B1 (enExample)
CN (2) CN109562098B (enExample)
AU (2) AU2017257185B8 (enExample)
IL (2) IL262620B2 (enExample)
MX (2) MX391165B (enExample)
WO (1) WO2017190141A1 (enExample)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7542935B2 (ja) 2016-04-29 2024-09-02 オフィレックス インコーポレイテッド 溶血、脳浮腫および急性腎障害を引き起こす病態の治療のためのpla2およびhmg-coa阻害剤
WO2023086343A1 (en) * 2021-11-09 2023-05-19 Ophirex, Inc. Compositions and dosage forms for topical and transdermal delivery of actives and methods of use

Citations (2)

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US20080096963A1 (en) * 2004-07-21 2008-04-24 Cerep Use Of A Fatty Acid For Preparing A Topical Composition For Allaying Inflammatory Reaction Due To Vennemous Hymenoptera Strings
WO2016081826A2 (en) * 2014-11-21 2016-05-26 Ophirex, Inc Envenomation therapies and related pharmaceutical compositions, systems and kits

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IL84252A (en) 1987-10-23 1994-02-27 Yissum Res Dev Co Phospholipase inhibiting compositions
SI0675110T1 (en) * 1994-04-01 2002-12-31 Eli Lilly And Company 1H-Indole-3-glyoxylamide sPLA2 inhibitors
DE69716619T2 (de) * 1996-08-28 2003-06-26 The Procter & Gamble Company, Cincinnati Phosphinsäureamide als matrix metalloprotease inhibitoren
AUPP076797A0 (en) * 1997-12-05 1998-01-08 Active (Pla) R&D Pty Ltd Phospholipase inhibitor
GB2365769A (en) * 2000-08-18 2002-02-27 Secr Defence Skin preparations containing silicon
US8106019B2 (en) * 2002-11-15 2012-01-31 Philadelphia Health & Education Corporation CHEC-7 a novel sPLA2 inhibitor
AU2004270261B2 (en) * 2003-09-09 2008-12-04 University Of Florida Research Foundation, Inc. Polyamine-metal chelator conjugates
JP2008538586A (ja) 2005-04-21 2008-10-30 グレン エー. ゴールドスタイン, 酸化ストレスに関連する疾患および病気の処置のためのn−アセチルシステインアミド(nacアミド)
US20100204249A1 (en) * 2009-01-08 2010-08-12 Colin Hislop Secretory phospholipase a2 (spla2) inhibitor and niacin drug compositions and methods for treating cardiovascular disease and dyslipidemia
US20110269786A1 (en) * 2010-04-30 2011-11-03 Colin Hislop Treatment of major adverse cardiac events and acute coronary syndrome in diabetic patients using secretory phospholipase a2 (spla2) inhibitor or spla2 inhibitor combination therapies
AU2013312240A1 (en) * 2012-09-10 2015-03-19 Ophirex Inc. Administration of acetylcholinesterase inhibitors to mitigate neurotoxin-induced paralysis and residual neuromuscular blockade
US20140087003A1 (en) * 2012-09-21 2014-03-27 Ignacio Cisneros Method for treating venomous bites and stings
US10786483B2 (en) * 2016-03-04 2020-09-29 Hk Pharma Tumescent contravenom drug delivery
JP7542935B2 (ja) 2016-04-29 2024-09-02 オフィレックス インコーポレイテッド 溶血、脳浮腫および急性腎障害を引き起こす病態の治療のためのpla2およびhmg-coa阻害剤

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US20080096963A1 (en) * 2004-07-21 2008-04-24 Cerep Use Of A Fatty Acid For Preparing A Topical Composition For Allaying Inflammatory Reaction Due To Vennemous Hymenoptera Strings
WO2016081826A2 (en) * 2014-11-21 2016-05-26 Ophirex, Inc Envenomation therapies and related pharmaceutical compositions, systems and kits

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Also Published As

Publication number Publication date
MX2018013084A (es) 2019-03-06
CN109562098A (zh) 2019-04-02
US20250120949A1 (en) 2025-04-17
JP2022177020A (ja) 2022-11-30
JP7542935B2 (ja) 2024-09-02
MX2022003739A (es) 2022-05-02
AU2023233187A1 (en) 2023-10-12
KR20230049762A (ko) 2023-04-13
CN116585306A (zh) 2023-08-15
US12383531B2 (en) 2025-08-12
WO2017190141A1 (en) 2017-11-02
AU2017257185A1 (en) 2018-11-22
KR102723249B1 (ko) 2024-10-28
JP2019514935A (ja) 2019-06-06
EP3448378C0 (en) 2024-04-17
EP3448378A1 (en) 2019-03-06
IL262620A (en) 2018-12-31
EP3448378B1 (en) 2024-04-17
CN109562098B (zh) 2023-04-21
MX391165B (es) 2025-03-21
AU2017257185B8 (en) 2023-07-06
IL262620B1 (en) 2023-10-01
IL307232B1 (en) 2025-12-01
BR112018072162A2 (pt) 2019-02-12
IL262620B2 (en) 2024-02-01
CA3022013A1 (en) 2017-11-02
CN116585306B (zh) 2025-06-20
US20210220332A1 (en) 2021-07-22
IL307232A (en) 2023-11-01
EP3448378A4 (en) 2020-04-08
AU2017257185B2 (en) 2023-06-22
KR20190005898A (ko) 2019-01-16

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DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE INVENTION TITLE TO READ PLA2 INHIBITORS FOR IMMEDIATE TREATMENT OF HYMENOPTERA ENVENOMATION, ITS COMPLICATIONS AND PATHOLOGICAL CONDITIONS CAUSING HEMOLYSIS, KIDNEY DAMAGE, OR CEREBRAL EDEMA

SREP Specification republished
TH Corrigenda

Free format text: IN VOL 57 , NO 24 , PAGE(S) 3548 UNDER THE HEADING APPLICATIONS ACCEPTED - NAME INDEX UNDER THE NAME OPHIREX, INC., APPLICATION NO. 2017257185, UNDER INID (54) CORRECT THE TITLE TO READ PHOSPHOLIPASE A2 INHIBITORS FOR IMMEDIATE TREATMENT OF VENOM TOXICITY THAT CAUSES HEMOLYSIS, CEREBRAL EDEMA, AND ACUTE KIDNEY INJURY

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