AU2015260906B2 - Crystalline form of 6-((4R)-4-methyl-1,2-dioxido-1,2,6-thiadiazinan-2-yl)isoquinoline-1-carbonitrile - Google Patents

Crystalline form of 6-((4R)-4-methyl-1,2-dioxido-1,2,6-thiadiazinan-2-yl)isoquinoline-1-carbonitrile Download PDF

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Publication number
AU2015260906B2
AU2015260906B2 AU2015260906A AU2015260906A AU2015260906B2 AU 2015260906 B2 AU2015260906 B2 AU 2015260906B2 AU 2015260906 A AU2015260906 A AU 2015260906A AU 2015260906 A AU2015260906 A AU 2015260906A AU 2015260906 B2 AU2015260906 B2 AU 2015260906B2
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Prior art keywords
thiadiazinan
dioxido
isoquinoline
methyl
crystalline form
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Ceased
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AU2015260906A
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AU2015260906A1 (en
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Eugene Lvovich Piatnitski Chekler
Roberta Louise Dorow
Jeffrey Braden SPERRY
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Pfizer Inc
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Pfizer Inc
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    • 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
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/549—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
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    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
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    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
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    • A61P3/04—Anorexiants; Antiobesity agents
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    • A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
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    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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

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  • Health & Medical Sciences (AREA)
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  • Pregnancy & Childbirth (AREA)
  • Immunology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2015260906A 2014-05-15 2015-05-01 Crystalline form of 6-((4R)-4-methyl-1,2-dioxido-1,2,6-thiadiazinan-2-yl)isoquinoline-1-carbonitrile Ceased AU2015260906B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201461993693P 2014-05-15 2014-05-15
US61/993,693 2014-05-15
US201562138037P 2015-03-25 2015-03-25
US62/138,037 2015-03-25
PCT/IB2015/053194 WO2015173684A1 (en) 2014-05-15 2015-05-01 Crystalline form of 6-[(4r)-4-methyl-1,2-dioxido-1,2,6-thiadiazinan-2-yl]isoquinoline-1-carbonitrile

Publications (2)

Publication Number Publication Date
AU2015260906A1 AU2015260906A1 (en) 2016-10-20
AU2015260906B2 true AU2015260906B2 (en) 2017-08-31

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AU2015260906A Ceased AU2015260906B2 (en) 2014-05-15 2015-05-01 Crystalline form of 6-((4R)-4-methyl-1,2-dioxido-1,2,6-thiadiazinan-2-yl)isoquinoline-1-carbonitrile

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Country Link
US (1) US9920043B2 (enExample)
EP (1) EP3143019B1 (enExample)
JP (1) JP6523782B2 (enExample)
KR (1) KR101817889B1 (enExample)
CN (1) CN106459025B (enExample)
AU (1) AU2015260906B2 (enExample)
CA (1) CA2891398C (enExample)
CY (1) CY1123826T1 (enExample)
DK (1) DK3143019T3 (enExample)
ES (1) ES2845639T3 (enExample)
HU (1) HUE052692T2 (enExample)
IL (1) IL248918A0 (enExample)
MX (1) MX371014B (enExample)
PL (1) PL3143019T3 (enExample)
PT (1) PT3143019T (enExample)
RU (1) RU2698194C2 (enExample)
SG (1) SG11201608320QA (enExample)
SI (1) SI3143019T1 (enExample)
TW (1) TWI553007B (enExample)
WO (1) WO2015173684A1 (enExample)
ZA (1) ZA201606796B (enExample)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2864079T3 (es) * 2014-05-30 2021-10-13 Pfizer Derivados de carbonitrilo como moduladores selectivos del receptor de andrógenos
WO2023275715A1 (en) * 2021-06-30 2023-01-05 Pfizer Inc. Metabolites of selective androgen receptor modulators

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005018573A2 (en) * 2003-08-22 2005-03-03 Ligand Pharmaceuticals Incorporated 6-cycloamino-2-quinolinone derivatives as androgen receptor modulator compounds
WO2009082437A2 (en) * 2007-12-21 2009-07-02 Ligand Pharmaceuticals Incorporated Selective androgen receptor modulators (sarms) and uses thereof

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0089139A2 (en) 1982-03-16 1983-09-21 Beecham Group Plc Antibiotics, their preparation and use
US4489075A (en) * 1982-05-15 1984-12-18 Pfizer Inc. Cyclic sulfonamidoalkyl substituted 4-piperidinoquinazoline cardiac stimulants
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
GB9518953D0 (en) 1995-09-15 1995-11-15 Pfizer Ltd Pharmaceutical formulations
WO2000035298A1 (en) 1996-11-27 2000-06-22 Wm. Wrigley Jr. Company Chewing gum containing medicament active agents
GB9711643D0 (en) 1997-06-05 1997-07-30 Janssen Pharmaceutica Nv Glass thermoplastic systems
WO2004110978A2 (en) 2003-06-10 2004-12-23 Smithkline Beecham Corporation 1-aminonaphthalenes as modulators of androgen, glucocorticoid, mineralocorticoid and progesterone receptors
MY176727A (en) * 2012-12-03 2020-08-20 Pfizer Selective androgen receptor modulators

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005018573A2 (en) * 2003-08-22 2005-03-03 Ligand Pharmaceuticals Incorporated 6-cycloamino-2-quinolinone derivatives as androgen receptor modulator compounds
WO2009082437A2 (en) * 2007-12-21 2009-07-02 Ligand Pharmaceuticals Incorporated Selective androgen receptor modulators (sarms) and uses thereof

Also Published As

Publication number Publication date
CA2891398A1 (en) 2015-11-15
EP3143019B1 (en) 2020-12-16
PL3143019T3 (pl) 2021-03-22
HUE052692T2 (hu) 2021-05-28
EP3143019A1 (en) 2017-03-22
JP2015218166A (ja) 2015-12-07
TW201546069A (zh) 2015-12-16
AU2015260906A1 (en) 2016-10-20
DK3143019T3 (da) 2021-01-04
MX371014B (es) 2020-01-10
RU2698194C2 (ru) 2019-08-23
CN106459025B (zh) 2019-05-28
RU2016144671A (ru) 2018-06-15
PT3143019T (pt) 2021-01-28
SG11201608320QA (en) 2016-11-29
KR20160144478A (ko) 2016-12-16
US20170073338A1 (en) 2017-03-16
CY1123826T1 (el) 2022-05-27
KR101817889B1 (ko) 2018-01-11
CA2891398C (en) 2019-09-24
WO2015173684A1 (en) 2015-11-19
US9920043B2 (en) 2018-03-20
TWI553007B (zh) 2016-10-11
CN106459025A (zh) 2017-02-22
IL248918A0 (en) 2017-01-31
MX2016014999A (es) 2017-04-11
JP6523782B2 (ja) 2019-06-05
RU2016144671A3 (enExample) 2018-06-15
SI3143019T1 (sl) 2021-03-31
ZA201606796B (en) 2018-04-25
ES2845639T3 (es) 2021-07-27

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