AU2016338916B2 - Enhancing beta cell replication and/or survival - Google Patents

Enhancing beta cell replication and/or survival Download PDF

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Publication number
AU2016338916B2
AU2016338916B2 AU2016338916A AU2016338916A AU2016338916B2 AU 2016338916 B2 AU2016338916 B2 AU 2016338916B2 AU 2016338916 A AU2016338916 A AU 2016338916A AU 2016338916 A AU2016338916 A AU 2016338916A AU 2016338916 B2 AU2016338916 B2 AU 2016338916B2
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Australia
Prior art keywords
gaba
pam
activating ligand
receptor activating
replication
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AU2016338916A
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AU2016338916A1 (en
Inventor
Daniel L. Kaufman
Jide Tian
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University of California San Diego UCSD
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University of California Berkeley
University of California San Diego UCSD
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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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A61K31/515Barbituric acids; Derivatives thereof, e.g. sodium pentobarbital
    • 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
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • 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
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/55171,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (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)
AU2016338916A 2015-10-14 2016-10-12 Enhancing beta cell replication and/or survival Active AU2016338916B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2022202004A AU2022202004B2 (en) 2015-10-14 2022-03-23 Enhancing beta cell replication and/or survival

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562241566P 2015-10-14 2015-10-14
US62/241,566 2015-10-14
US201662279908P 2016-01-18 2016-01-18
US62/279,908 2016-01-18
PCT/US2016/056528 WO2017066240A1 (en) 2015-10-14 2016-10-12 Enhancing beta cell replication and/or survival

Related Child Applications (1)

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AU2022202004A Division AU2022202004B2 (en) 2015-10-14 2022-03-23 Enhancing beta cell replication and/or survival

Publications (2)

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AU2016338916A1 AU2016338916A1 (en) 2018-05-31
AU2016338916B2 true AU2016338916B2 (en) 2021-12-23

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AU2022202004A Active AU2022202004B2 (en) 2015-10-14 2022-03-23 Enhancing beta cell replication and/or survival

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Country Status (7)

Country Link
US (1) US20180235916A1 (enExample)
EP (1) EP3362069A4 (enExample)
JP (2) JP6957455B2 (enExample)
KR (1) KR20180054796A (enExample)
CN (1) CN108697712A (enExample)
AU (2) AU2016338916B2 (enExample)
WO (1) WO2017066240A1 (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2806877B2 (en) 2012-01-23 2025-01-29 Sage Therapeutics, Inc. Neuroactive steroid formulations comprising a complex of allopregnanolone and sulfobutyl ether beta-cyclodextrin
BR112015003747A2 (pt) 2012-08-21 2017-07-04 Sage Therapeutics Inc métodos de tratamento de epilepsia ou estado de mal epiléptico
EP2925327B1 (en) 2012-11-30 2024-01-10 The Regents of The University of California Allopregnanolone for treating, reducing or mitigating symptoms of post-partum depression
JOP20200195A1 (ar) 2014-09-08 2017-06-16 Sage Therapeutics Inc سترويدات وتركيبات نشطة عصبياً، واستخداماتها
CN113616661A (zh) 2016-03-08 2021-11-09 萨奇治疗股份有限公司 神经活性类固醇、其组合物及用途
CA3104810A1 (en) * 2017-06-23 2018-12-27 The Regents Of The University Of California Enhancing gaba's ability to modulate immune responses
EP3866777A4 (en) * 2018-10-18 2022-07-20 The Regents of the University of California COMBINATION THERAPIES FOR THE TREATMENT OF INFLAMMATORY DISEASES
CN115361944A (zh) * 2020-01-10 2022-11-18 均衡生物制药私人有限责任公司 用阿维菌素治疗神经病症
US20250375429A1 (en) * 2024-05-29 2025-12-11 Smarter Not Harder, Inc. Obligate pairing of orthosteric and non-orthosteric gaba ligands in pharmaceutical formulations

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012050907A2 (en) * 2010-09-28 2012-04-19 The Regents Of The University Of California Gaba agonists in the treatment of disorders associated with metabolic syndrome and gaba combinations in treatment or prophylaxis of type i diabetes
WO2014048788A1 (en) * 2012-09-27 2014-04-03 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for producing a population of pancreatic beta-cells
WO2015140081A1 (en) * 2014-03-18 2015-09-24 Algiax Pharmaceuticals Gmbh 2-cyano-3-cyclopropyl-3-hydroxy-n-aryl-thioacrylamide derivatives

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU3503300A (en) * 1999-02-24 2000-09-14 Regents Of The University Of California, The Gaba receptors mediate inhibition of t cell responses

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012050907A2 (en) * 2010-09-28 2012-04-19 The Regents Of The University Of California Gaba agonists in the treatment of disorders associated with metabolic syndrome and gaba combinations in treatment or prophylaxis of type i diabetes
WO2014048788A1 (en) * 2012-09-27 2014-04-03 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for producing a population of pancreatic beta-cells
WO2015140081A1 (en) * 2014-03-18 2015-09-24 Algiax Pharmaceuticals Gmbh 2-cyano-3-cyclopropyl-3-hydroxy-n-aryl-thioacrylamide derivatives

Non-Patent Citations (9)

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Title
CHWEH A Y ET AL, "Effect of GABA agonists on the neurotoxicity and anticonvulsant activity of benzodiazepines", LIFE SCIENCES, PERGAMON PRESS, OXFORD, GB, vol. 36, no. 8, (1985-02-25), pages 737 - 744, (1985-02-25) *
DAVIES L P ET AL, "Substituted imidazo[1,2-b]pyridazines", BIOCHEMICAL PHARMACOLOGY, ELSEVIER, US, vol. 44, no. 8, ISSN 0006-2952, (1992-10-20), pages 1555 - 1561, (1992-10-20) *
E S El-Denshary ET AL, "Effects of tetracycline and diazepam on insulin secretion and adenylyl cyclase activity of isolated rat islets of Langerhans.", Diabete Metab. 1977 Mar;3(1):3-6., (1977-01-01), pages 3 - 6, *
J. TIAN ET AL, "-Aminobutyric Acid Regulates Both the Survival and Replication of Human -Cells", DIABETES, US, (2013-08-30), vol. 62, no. 11, doi:10.2337/db13-0931, ISSN 0012-1797, pages 3760 - 3765 *
JIDE TIAN ET AL, "Clinically applicable GABA receptor positive allosteric modulators promote ß-cell replication", SCIENTIFIC REPORTS, (2017-03-23), vol. 7, no. 1, doi:10.1038/s41598-017-00515-y *
PAUL SM, "Alcohol-sensitive GABA receptors and alcohol antagonists", 2006-05-22, (2006-05-22) *
RAMIREZ G ET AL, "Gabaergic modulation of acetylcholine release in cholinergic synaptosomes from Torpedo marmorata electric organ", NEUROSCIENCE, NEW YORK, NY, US, vol. 30, no. 1, (1989-01-01), pages 251 - 255. *
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Also Published As

Publication number Publication date
CN108697712A (zh) 2018-10-23
EP3362069A1 (en) 2018-08-22
US20180235916A1 (en) 2018-08-23
EP3362069A4 (en) 2019-10-02
JP6957455B2 (ja) 2021-11-02
AU2016338916A1 (en) 2018-05-31
AU2022202004B2 (en) 2024-09-19
JP2022008902A (ja) 2022-01-14
JP2018530581A (ja) 2018-10-18
WO2017066240A1 (en) 2017-04-20
AU2022202004A1 (en) 2022-04-14
KR20180054796A (ko) 2018-05-24

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