SG10201504735QA - Novel polymorphic forms of 3-(1-{3-[5-(1-methyl-piperidin-4ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride salt and processes of manufacturing thereof - Google Patents

Novel polymorphic forms of 3-(1-{3-[5-(1-methyl-piperidin-4ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride salt and processes of manufacturing thereof

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Publication number
SG10201504735QA
SG10201504735QA SG10201504735QA SG10201504735QA SG10201504735QA SG 10201504735Q A SG10201504735Q A SG 10201504735QA SG 10201504735Q A SG10201504735Q A SG 10201504735QA SG 10201504735Q A SG10201504735Q A SG 10201504735QA SG 10201504735Q A SG10201504735Q A SG 10201504735QA
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SG
Singapore
Prior art keywords
4ylmethoxy
pyridazin
pyrimidin
piperidin
dihydro
Prior art date
Application number
SG10201504735QA
Inventor
Axel Becker
Clemens Kuehn
Christoph Saal
Oliver Schadt
Dieter Dorsch
Heinz-Hermann Bokel
Frank Stieber
Christina Donini
Original Assignee
Merck Patent Gmbh
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Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of SG10201504735QA publication Critical patent/SG10201504735QA/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
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    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
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    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P5/00Drugs for disorders of the endocrine system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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 linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
SG10201504735QA 2009-01-08 2009-12-04 Novel polymorphic forms of 3-(1-{3-[5-(1-methyl-piperidin-4ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride salt and processes of manufacturing thereof SG10201504735QA (en)

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EP09000140 2009-01-08

Publications (1)

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SG10201504735QA true SG10201504735QA (en) 2015-07-30

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SG2011048576A SG172831A1 (en) 2009-01-08 2009-12-04 Novel polymorphic forms of 3-(1-{3-[5-(1-methyl-piperidin-4ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride salt and processes of manufacturing thereof
SG10201504735QA SG10201504735QA (en) 2009-01-08 2009-12-04 Novel polymorphic forms of 3-(1-{3-[5-(1-methyl-piperidin-4ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride salt and processes of manufacturing thereof

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US (3) US8710058B2 (en)
EP (1) EP2373640B1 (en)
JP (2) JP5719781B2 (en)
KR (2) KR101730791B1 (en)
CN (1) CN102272121B (en)
AR (1) AR074996A1 (en)
AU (1) AU2009336839B2 (en)
BR (1) BRPI0922642B8 (en)
CA (4) CA3097370A1 (en)
CL (1) CL2011001356A1 (en)
CO (1) CO6400191A2 (en)
CY (1) CY1115631T1 (en)
DK (1) DK2373640T3 (en)
EA (1) EA019342B1 (en)
EC (1) ECSP11011248A (en)
ES (1) ES2522629T3 (en)
HK (1) HK1164856A1 (en)
HR (1) HRP20140908T1 (en)
IL (1) IL213829A0 (en)
MX (3) MX363852B (en)
MY (1) MY160017A (en)
NZ (1) NZ594404A (en)
PE (2) PE20141317A1 (en)
PL (1) PL2373640T3 (en)
PT (1) PT2373640E (en)
SG (2) SG172831A1 (en)
SI (1) SI2373640T1 (en)
SM (1) SMT201400161B (en)
TW (1) TWI475997B (en)
UA (1) UA106220C2 (en)
WO (1) WO2010078897A1 (en)
ZA (1) ZA201105782B (en)

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BR112014022266A2 (en) * 2012-03-19 2021-09-08 Merck Patent Gmbh COMBINATION OF A 6-OXO-1,6-DI-HYDRO-PYRIDAZINE DERIVATIVE HAVING ANTI-CANCER ACTIVITY WITH OTHER ANTI-TUMOR COMPOUNDS
SG11201503214YA (en) * 2012-11-02 2015-05-28 Merck Patent Gmbh A 6-oxo-1,6-dihydro-pyridazine derivative for the use for the treatment of hepatocellular carcinoma (hcc)
RU2016132401A (en) * 2014-01-07 2018-02-13 Мерк Патент Гмбх 6-OXO-1, 6-DIHYDRO-PYRIDAZINE DERIVATIVE FOR USE FOR TREATMENT OF RENAL CELL CANCER (RCC)
UA120108C2 (en) 2014-12-12 2019-10-10 Мерк Патент Гмбх Combination of a 6-oxo-1,6-dihydro-pyridazine derivative having anti-cancer activity with an egfr inhibitor
CA2981627C (en) 2015-04-03 2024-02-20 Suixiong Cai Solid pharmaceutical formulation of parp inhibitors and the use thereof
WO2016192831A1 (en) 2015-05-29 2016-12-08 Merck Patent Gmbh Compositions of anions and cations with pharmacological activity
KR20180092096A (en) 2017-02-08 2018-08-17 에이비온 주식회사 Novel Polymorphic Forms of Triazolopyrazine Derivatives and Processes of Manufacturing Thereof
ES2962679T3 (en) 2018-04-26 2024-03-20 Fujian Akeylink Biotechnology Co Ltd Crystalline form of the c-MET inhibitor and its salt form and method of preparation thereof
WO2021005077A1 (en) * 2019-07-10 2021-01-14 Merck Patent Gmbh Pharmaceutical preparation
WO2022063869A2 (en) 2020-09-24 2022-03-31 Merck Patent Gmbh Compounds for the treatment of viral infections
KR102489160B1 (en) 2021-05-26 2023-01-18 주식회사 이노큐어테라퓨틱스 Derivatives of Piperidinedione
WO2022250350A1 (en) 2021-05-26 2022-12-01 주식회사 이노큐어테라퓨틱스 Piperidinedione derivative
CA3222061A1 (en) 2021-06-04 2022-12-08 Merck Patent Gmbh Compounds for the treatment of glioblastoma
CN114394957B (en) * 2021-12-24 2023-05-09 武汉九州钰民医药科技有限公司 Preparation method of MET inhibitor terpotinib hydrochloride
KR20230155324A (en) 2022-05-03 2023-11-10 주식회사 이노큐어테라퓨틱스 Derivatives of Piperidinedione
CN116768868B (en) * 2023-08-15 2023-12-08 云南省药物研究所 Pyridazinone thio derivative and preparation method and application thereof

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CA3014648A1 (en) 2010-07-15
KR20170047408A (en) 2017-05-04
US20150148351A1 (en) 2015-05-28
US8710058B2 (en) 2014-04-29
TW201029655A (en) 2010-08-16
CN102272121A (en) 2011-12-07
BRPI0922642A2 (en) 2016-01-05
BRPI0922642B1 (en) 2020-09-29
EA019342B1 (en) 2014-02-28
JP2015038148A (en) 2015-02-26
US9308205B2 (en) 2016-04-12
SG172831A1 (en) 2011-08-29
UA106220C2 (en) 2014-08-11
US20110269767A1 (en) 2011-11-03
US20140200221A1 (en) 2014-07-17
IL213829A0 (en) 2011-07-31
CA2749012A1 (en) 2010-07-15
JP5719781B2 (en) 2015-05-20
AU2009336839A8 (en) 2011-09-08
HRP20140908T1 (en) 2014-11-07
MX350894B (en) 2017-09-22
MX2011007322A (en) 2011-07-29
CO6400191A2 (en) 2012-03-15
ES2522629T3 (en) 2014-11-17
TWI475997B (en) 2015-03-11
WO2010078897A1 (en) 2010-07-15
CA3014648C (en) 2021-06-01
AU2009336839B2 (en) 2015-12-24
CN102272121B (en) 2014-12-10
NZ594404A (en) 2013-04-26
PT2373640E (en) 2014-09-30
JP5860126B2 (en) 2016-02-16
EP2373640A1 (en) 2011-10-12
BRPI0922642B8 (en) 2021-05-25
MX363852B (en) 2019-04-05
CL2011001356A1 (en) 2011-09-30
ZA201105782B (en) 2012-04-25
EA201101039A1 (en) 2012-02-28
AU2009336839A1 (en) 2011-08-25
CA2749012C (en) 2017-01-31
HK1164856A1 (en) 2012-09-28
DK2373640T3 (en) 2014-10-06
KR101829595B1 (en) 2018-02-14
AR074996A1 (en) 2011-03-02
JP2012514609A (en) 2012-06-28
PL2373640T3 (en) 2014-12-31
SI2373640T1 (en) 2014-11-28
ECSP11011248A (en) 2011-10-31
CA2949515C (en) 2018-10-23
PE20141317A1 (en) 2014-09-26
CY1115631T1 (en) 2017-01-04
PE20120474A1 (en) 2012-05-04
MY160017A (en) 2017-02-15
KR20110111472A (en) 2011-10-11
CA3097370A1 (en) 2010-07-15
MX363848B (en) 2019-04-05
US9289427B2 (en) 2016-03-22
KR101730791B1 (en) 2017-04-27
CA2949515A1 (en) 2010-07-15
EP2373640B1 (en) 2014-07-30
SMT201400161B (en) 2015-01-15

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