SG11201810976TA - Pharmaceutical salts of n-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide and crystalline forms thereof - Google Patents

Pharmaceutical salts of n-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide and crystalline forms thereof

Info

Publication number
SG11201810976TA
SG11201810976TA SG11201810976TA SG11201810976TA SG11201810976TA SG 11201810976T A SG11201810976T A SG 11201810976TA SG 11201810976T A SG11201810976T A SG 11201810976TA SG 11201810976T A SG11201810976T A SG 11201810976TA SG 11201810976T A SG11201810976T A SG 11201810976TA
Authority
SG
Singapore
Prior art keywords
international
pyrimidin
acrylamide
dimethylamino
ethoxy
Prior art date
Application number
SG11201810976TA
Inventor
Michael Greco
Michael Costanzo
Michael Green
Jirong Peng
Victoria Wilde
Don Zhang
Original Assignee
Beta Pharma Inc
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
Application filed by Beta Pharma Inc filed Critical Beta Pharma Inc
Publication of SG11201810976TA publication Critical patent/SG11201810976TA/en

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Classifications

    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/265—Citric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 21 December 2017 (21.12.2017) WIP0 I PCT Iiiimmoimiolollmolomm oimIE (10) International Publication Number WO 2017/218892 Al (51) International Patent Classification: A61K 31/506 (2006.01) C07D 403/04 (2006.01) (21) International Application Number: PCT/US2017/037872 (22) International Filing Date: Published: — with international search report (Art. 21(3)) 16 June 2017 (16.06.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/351,749 17 June 2016 (17.06.2016) US (71) Applicant: BETA PHARMA, INC. [US/US]; 1000 N. West Street, Suite 1200, Wilmington, DE 19801 (US). (72) Inventors: GRECO, Michael, Nicholas; 1634 Clearbrook Road, Lansdale, PA 19446 (US). COSTANZO, Michael, John; 14 Breckenridge Drive, Warminster, PA 18974 (US). GREEN, Michael, Alan; 1184 Dewalt Drive, Easton, PA 18040 (US). PENG, Jirong; 11019 North Kensington Dr., Mequon, WI 53097 (US). WILDE, Victoria, Lynn; 50 Pine Street, Apt. 41, Montclair, NJ 07042 (US). ZHANG, Don; 9 Kensington Court, Princeton, NJ 08540 (US). (74) Agent: LIU, Wansheng Jerry et al.; Fox Rothschild LLP, 997 Lenox Drive, Building 3, Lawrenceville, NJ 08648-2311 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. = (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, 1-1 KM, ML, MR, NE, SN, TD, TG). co co (54) Title: PHARMACEUTICAL SALTS OF N-(2-(2-(DIMETHYLAMINO)ETHOXY)-4-METHOXY-544-(1-METHYL-1H-IN- DOL-3-YL)PYRIMIDIN-2-YL)AMINO)PHENYL)ACRYLAMIDE AND CRYSTALLINE FORMS THEREOF (57) : Crystalline forms of N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-54(4-(1-methyl-1H- indo1-3-yl)pyrimidin-2- © yl)amino)phenyl)acrylamide (1) and its pharmaceutically acceptable salts and compositions thereof useful for the treatment or preven- tion of diseases or medical conditions mediated through mutated forms of epidermal growth factor receptor (EGFR), such as various 0 cancers, are disclosed.
SG11201810976TA 2016-06-17 2017-06-16 Pharmaceutical salts of n-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide and crystalline forms thereof SG11201810976TA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662351749P 2016-06-17 2016-06-17
PCT/US2017/037872 WO2017218892A1 (en) 2016-06-17 2017-06-16 Pharmaceutical salts of n-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide and crystalline forms thereof

Publications (1)

Publication Number Publication Date
SG11201810976TA true SG11201810976TA (en) 2019-01-30

Family

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Family Applications (1)

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SG11201810976TA SG11201810976TA (en) 2016-06-17 2017-06-16 Pharmaceutical salts of n-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide and crystalline forms thereof

Country Status (17)

Country Link
US (1) US10844045B2 (en)
EP (1) EP3471730B1 (en)
JP (1) JP6928964B2 (en)
KR (1) KR20190018494A (en)
CN (1) CN109937043A (en)
AU (1) AU2017285448B2 (en)
BR (1) BR112018075823A2 (en)
CA (1) CA3027732A1 (en)
CO (1) CO2018013416A2 (en)
EA (1) EA201892661A1 (en)
IL (1) IL263619A (en)
MX (1) MX2018015508A (en)
PH (1) PH12018502668A1 (en)
SG (1) SG11201810976TA (en)
TW (1) TW201800404A (en)
WO (1) WO2017218892A1 (en)
ZA (1) ZA201808234B (en)

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KR20200016969A (en) 2017-06-16 2020-02-17 베타 파마, 인크. N- (2- (2- (dimethylamino) ethoxy) -4-methoxy-5-((4- (1-methyl-1H-indol-3-yl) pyrimidin-2-yl) amino) phenyl Pharmaceutical Formulation of Acrylamide and Its Salts
CN110898026A (en) * 2019-12-11 2020-03-24 倍而达药业（苏州）有限公司 Pharmaceutical composition containing BPI-7711 and preparation method thereof
CN111100117B (en) * 2019-12-18 2021-02-19 上海倍而达药业有限公司 Crystal form A of aminopyrimidine compound mesylate and preparation method and application thereof

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EA029488B1 (en) * 2011-07-27 2018-04-30 Астразенека Аб 2-(2,4,5-substituted-anilino)pyrimidine derivatives as egfr modulators useful for treating cancer
DE102011115849B3 (en) 2011-10-13 2012-05-10 Thomas Magnete Gmbh Metering pump for use as electromagnetically driven reciprocating pump in e.g. truck, has metallic mold in damper whose bias is adjusted by rotation of socket relative to outlet or by rotation of atomization device relative to socket
AU2015277786B2 (en) 2014-06-19 2019-04-18 Takeda Pharmaceutical Company Limited Heteroaryl compounds for kinase inhibition
CN105315285B (en) * 2014-07-25 2017-12-08 上海海雁医药科技有限公司 2,4 2 substitution 7H pyrrolo-es [2,3 d] pyrimidine derivatives, its preparation method and purposes pharmaceutically
CN113121575A (en) * 2014-08-25 2021-07-16 四川海思科制药有限公司 (substituted phenyl) (substituted pyrimidine) amino derivative and preparation method and pharmaceutical application thereof
JP6456086B2 (en) * 2014-09-25 2019-01-23 キヤノン株式会社 Projection type image display apparatus and control method thereof, projector and control method thereof
CN105085489B (en) 2014-11-05 2019-03-01 益方生物科技（上海）有限公司 Pyrimidine or pyridine compounds and their, preparation method and medical usage
WO2016092841A1 (en) 2014-12-10 2016-06-16 王子ホールディングス株式会社 Absorbent article
TWI618704B (en) * 2014-12-11 2018-03-21 貝達醫藥公司 Substituted 2-anilinopyrimidine derivatives as egfr modulators
CN104961731A (en) * 2015-02-05 2015-10-07 苏州晶云药物科技有限公司 Phosphate of epidermal growth factor receptor inhibitor, and crystal form and preparation method thereof
CN104910049B (en) * 2015-06-16 2016-06-29 苏州明锐医药科技有限公司 AZD9291 intermediate and preparation method thereof
EP3454860A4 (en) 2016-05-11 2020-01-15 Beta Pharma, Inc. 2-anilinopyrimidine derivatives as therapeutic agents for treatment of brain cancers

Also Published As

Publication number Publication date
IL263619A (en) 2019-01-31
EP3471730A4 (en) 2019-11-27
CO2018013416A2 (en) 2019-01-18
CA3027732A1 (en) 2017-12-21
EP3471730B1 (en) 2021-10-20
PH12018502668A1 (en) 2019-10-07
MX2018015508A (en) 2019-04-11
EP3471730A1 (en) 2019-04-24
AU2017285448A1 (en) 2019-01-03
CN109937043A (en) 2019-06-25
KR20190018494A (en) 2019-02-22
ZA201808234B (en) 2019-11-27
EA201892661A1 (en) 2019-07-31
WO2017218892A1 (en) 2017-12-21
JP6928964B2 (en) 2021-09-01
JP2019518062A (en) 2019-06-27
AU2017285448B2 (en) 2021-02-04
US20190233399A1 (en) 2019-08-01
US10844045B2 (en) 2020-11-24
BR112018075823A2 (en) 2019-03-26
TW201800404A (en) 2018-01-01

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