PH26286A - Injection containing 3-benzoyloxy-1,3,5(10)-estratrienes-17-[4-äp-(bis(2-chloroethyl)-amino)-phenylü-butanoyloxy] acetate as an active ingredient - Google Patents

Injection containing 3-benzoyloxy-1,3,5(10)-estratrienes-17-[4-äp-(bis(2-chloroethyl)-amino)-phenylü-butanoyloxy] acetate as an active ingredient Download PDF

Info

Publication number: PH26286A
Authority: PH; Philippines
Prior art keywords: chloroethyl; benzoyloxy; amino; bis; cancer
Prior art date: 1987-07-22

Application number

PH37238A

Other languages

English (en)

Inventor

Kiro Asano

Humio Tamura

Satoshi Mitsuhashi

Kenji Bannai

Hisayuki Wada

Original Assignee

Kureha Chemical Ind Co Ltd

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.)

1987-07-22

Filing date

1988-07-18

Publication date

1992-04-10

1988-07-18 Application filed by Kureha Chemical Ind Co Ltd filed Critical Kureha Chemical Ind Co Ltd

1992-04-10 Publication of PH26286A publication Critical patent/PH26286A/en

Links

239000004480 active ingredient Substances 0.000 title claims description 10
239000007924 injection Substances 0.000 title description 28
238000002347 injection Methods 0.000 title description 28
QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 title 1
206010028980 Neoplasm Diseases 0.000 claims description 14
240000001090 Papaver somniferum Species 0.000 claims description 10
235000008753 Papaver somniferum Nutrition 0.000 claims description 10
235000014113 dietary fatty acids Nutrition 0.000 claims description 10
229930195729 fatty acid Natural products 0.000 claims description 10
239000000194 fatty acid Substances 0.000 claims description 10
150000004665 fatty acids Chemical class 0.000 claims description 10
201000011510 cancer Diseases 0.000 claims description 9
150000002148 esters Chemical class 0.000 claims description 9
-1 bis(2-chloroethyl)amino Chemical group 0.000 claims description 8
238000000034 method Methods 0.000 claims description 5
239000000203 mixture Substances 0.000 claims description 5
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 5
230000026045 iodination Effects 0.000 claims description 4
238000006192 iodination reaction Methods 0.000 claims description 4
125000004494 ethyl ester group Chemical group 0.000 claims description 3
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 3
239000007972 injectable composition Substances 0.000 claims 3
239000003921 oil Substances 0.000 description 10
235000019198 oils Nutrition 0.000 description 10
210000004027 cell Anatomy 0.000 description 9
210000001519 tissue Anatomy 0.000 description 9
241000700159 Rattus Species 0.000 description 8
AOJJSUZBOXZQNB-TZSSRYMLSA-N doxorubicine Natural products O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 description 7
230000000694 effects Effects 0.000 description 7
239000002246 antineoplastic agent Substances 0.000 description 6
239000000243 solution Substances 0.000 description 6
229940009456 adriamycin Drugs 0.000 description 4
230000000259 anti-tumor effect Effects 0.000 description 4
230000002440 hepatic effect Effects 0.000 description 4
239000002904 solvent Substances 0.000 description 4
238000012360 testing method Methods 0.000 description 4
RXDLEJFWURUGLT-UHFFFAOYSA-N 2-butanoyloxyacetic acid Chemical compound CCCC(=O)OCC(O)=O RXDLEJFWURUGLT-UHFFFAOYSA-N 0.000 description 3
102100036475 Alanine aminotransferase 1 Human genes 0.000 description 3
108010082126 Alanine transaminase Proteins 0.000 description 3
WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical group OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 3
WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 3
239000003814 drug Substances 0.000 description 3
238000001727 in vivo Methods 0.000 description 3
VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 description 2
201000000274 Carcinosarcoma Diseases 0.000 description 2
206010058467 Lung neoplasm malignant Diseases 0.000 description 2
208000000453 Skin Neoplasms Diseases 0.000 description 2
229940100198 alkylating agent Drugs 0.000 description 2
239000002168 alkylating agent Substances 0.000 description 2
JCKYGMPEJWAADB-UHFFFAOYSA-N chlorambucil Chemical compound OC(=O)CCCC1=CC=C(N(CCCl)CCCl)C=C1 JCKYGMPEJWAADB-UHFFFAOYSA-N 0.000 description 2
229960004630 chlorambucil Drugs 0.000 description 2
229960005309 estradiol Drugs 0.000 description 2
229930182833 estradiol Natural products 0.000 description 2
201000007270 liver cancer Diseases 0.000 description 2
208000014018 liver neoplasm Diseases 0.000 description 2
201000005202 lung cancer Diseases 0.000 description 2
208000020816 lung neoplasm Diseases 0.000 description 2
239000008159 sesame oil Substances 0.000 description 2
235000011803 sesame oil Nutrition 0.000 description 2
201000000849 skin cancer Diseases 0.000 description 2
239000007787 solid Substances 0.000 description 2
125000001340 2-chloroethyl group Chemical group [H]C([H])(Cl)C([H])([H])* 0.000 description 1
206010006187 Breast cancer Diseases 0.000 description 1
208000026310 Breast neoplasm Diseases 0.000 description 1
206010009944 Colon cancer Diseases 0.000 description 1
108090000790 Enzymes Proteins 0.000 description 1
102000004190 Enzymes Human genes 0.000 description 1
208000000461 Esophageal Neoplasms Diseases 0.000 description 1
108010085330 Estradiol Receptors Proteins 0.000 description 1
102100038595 Estrogen receptor Human genes 0.000 description 1
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
206010020843 Hyperthermia Diseases 0.000 description 1
208000008839 Kidney Neoplasms Diseases 0.000 description 1
241001465754 Metazoa Species 0.000 description 1
229930192392 Mitomycin Natural products 0.000 description 1
NWIBSHFKIJFRCO-WUDYKRTCSA-N Mytomycin Chemical compound C1N2C(C(C(C)=C(N)C3=O)=O)=C3[C@@H](COC(N)=O)[C@@]2(OC)[C@@H]2[C@H]1N2 NWIBSHFKIJFRCO-WUDYKRTCSA-N 0.000 description 1
241000283973 Oryctolagus cuniculus Species 0.000 description 1
206010033128 Ovarian cancer Diseases 0.000 description 1
206010061535 Ovarian neoplasm Diseases 0.000 description 1
206010060862 Prostate cancer Diseases 0.000 description 1
208000000236 Prostatic Neoplasms Diseases 0.000 description 1
206010038389 Renal cancer Diseases 0.000 description 1
FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
208000005718 Stomach Neoplasms Diseases 0.000 description 1
208000024770 Thyroid neoplasm Diseases 0.000 description 1
108090000340 Transaminases Proteins 0.000 description 1
208000002495 Uterine Neoplasms Diseases 0.000 description 1
230000007059 acute toxicity Effects 0.000 description 1
231100000403 acute toxicity Toxicity 0.000 description 1
125000005907 alkyl ester group Chemical group 0.000 description 1
230000001093 anti-cancer Effects 0.000 description 1
235000019445 benzyl alcohol Nutrition 0.000 description 1
230000015572 biosynthetic process Effects 0.000 description 1
239000008280 blood Substances 0.000 description 1
210000004369 blood Anatomy 0.000 description 1
230000017531 blood circulation Effects 0.000 description 1
201000005200 bronchus cancer Diseases 0.000 description 1
208000029742 colonic neoplasm Diseases 0.000 description 1
238000002591 computed tomography Methods 0.000 description 1
238000000354 decomposition reaction Methods 0.000 description 1
238000003745 diagnosis Methods 0.000 description 1
230000001804 emulsifying effect Effects 0.000 description 1
201000004101 esophageal cancer Diseases 0.000 description 1
230000029142 excretion Effects 0.000 description 1
230000003631 expected effect Effects 0.000 description 1
210000003608 fece Anatomy 0.000 description 1
210000001105 femoral artery Anatomy 0.000 description 1
206010017758 gastric cancer Diseases 0.000 description 1
210000001035 gastrointestinal tract Anatomy 0.000 description 1
210000002767 hepatic artery Anatomy 0.000 description 1
125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
230000036031 hyperthermia Effects 0.000 description 1
239000004615 ingredient Substances 0.000 description 1
210000000936 intestine Anatomy 0.000 description 1
PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 description 1
201000010982 kidney cancer Diseases 0.000 description 1
238000004811 liquid chromatography Methods 0.000 description 1
210000004185 liver Anatomy 0.000 description 1
210000002751 lymph Anatomy 0.000 description 1
229960004857 mitomycin Drugs 0.000 description 1
230000002093 peripheral effect Effects 0.000 description 1
WSDQIHATCCOMLH-UHFFFAOYSA-N phenyl n-(3,5-dichlorophenyl)carbamate Chemical compound ClC1=CC(Cl)=CC(NC(=O)OC=2C=CC=CC=2)=C1 WSDQIHATCCOMLH-UHFFFAOYSA-N 0.000 description 1
239000002504 physiological saline solution Substances 0.000 description 1
XZNXVSDNACTASG-RZNNTOFGSA-M sodium;3,5-diacetamido-2,4,6-triiodobenzoate;3,5-diacetamido-2,4,6-triiodobenzoic acid;(2r,3r,4r,5s)-6-(methylamino)hexane-1,2,3,4,5-pentol Chemical compound [Na+].CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.CC(=O)NC1=C(I)C(NC(C)=O)=C(I)C(C(O)=O)=C1I.CC(=O)NC1=C(I)C(NC(C)=O)=C(I)C(C([O-])=O)=C1I XZNXVSDNACTASG-RZNNTOFGSA-M 0.000 description 1
238000001179 sorption measurement Methods 0.000 description 1
201000011549 stomach cancer Diseases 0.000 description 1
230000004083 survival effect Effects 0.000 description 1
230000002195 synergetic effect Effects 0.000 description 1
238000003786 synthesis reaction Methods 0.000 description 1
230000001225 therapeutic effect Effects 0.000 description 1
201000002510 thyroid cancer Diseases 0.000 description 1
102000014898 transaminase activity proteins Human genes 0.000 description 1
210000004881 tumor cell Anatomy 0.000 description 1
206010046766 uterine cancer Diseases 0.000 description 1

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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Public Health (AREA)
Medicinal Chemistry (AREA)
Veterinary Medicine (AREA)
General Health & Medical Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Animal Behavior & Ethology (AREA)
Epidemiology (AREA)
Oil, Petroleum & Natural Gas (AREA)
Dermatology (AREA)
Chemical Kinetics & Catalysis (AREA)
Organic Chemistry (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicinal Preparation (AREA)
Steroid Compounds (AREA)

PH37238A 1987-07-22 1988-07-18 Injection containing 3-benzoyloxy-1,3,5(10)-estratrienes-17-[4-äp-(bis(2-chloroethyl)-amino)-phenylü-butanoyloxy] acetate as an active ingredient PH26286A (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
JP62182842A JPH0794377B2 (ja)	1987-07-22	1987-07-22	エストラジオール誘導体を含有する注射剤

Publications (1)

Publication Number	Publication Date
PH26286A true PH26286A (en)	1992-04-10

Family

ID=16125411

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
PH37238A PH26286A (en)	1987-07-22	1988-07-18	Injection containing 3-benzoyloxy-1,3,5(10)-estratrienes-17-[4-äp-(bis(2-chloroethyl)-amino)-phenylü-butanoyloxy] acetate as an active ingredient

Country Status (8)

Country	Link
US (1)	US4921849A (de)
EP (1)	EP0300749B1 (de)
JP (1)	JPH0794377B2 (de)
KR (1)	KR900006983B1 (de)
CA (1)	CA1315682C (de)
DE (1)	DE3887401T2 (de)
PH (1)	PH26286A (de)
ZA (1)	ZA885227B (de)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
JP2520074B2 (ja) *	1992-06-11	1996-07-31	呉羽化学工業株式会社	新規なエストラジオ―ル誘導体−クロラムブチル結合体、その製造方法、及び医薬製剤
JPH07101977A (ja) *	1993-10-05	1995-04-18	Kureha Chem Ind Co Ltd	ホルモン作用を軽減した新規なエストラジオール誘導体及びその増殖因子阻害剤
CN107400587B (zh)	2016-05-18	2021-06-25	Lg电子株式会社	啤酒酿造装置

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4261910A (en) *	1978-08-14	1981-04-14	Kureha Kagaku Kogyo Kabushiki Kaisha	Process for the preparation of Chlorambucil derivatives
JPS5810397B2 (ja) *	1978-12-08	1983-02-25	呉羽化学工業株式会社	新規なエストラジオ−ル誘導体とその製造方法及び抗腫瘍剤
JPS56110700A (en) *	1980-02-08	1981-09-01	Kureha Chem Ind Co Ltd	Estradiol-17alphaderivative and ist antitumor agent
JPS58124714A (ja) *	1982-01-20	1983-07-25	Yamanouchi Pharmaceut Co Ltd	抗腫瘍物質の油性組成物
US4578391A (en) *	1982-01-20	1986-03-25	Yamanouchi Pharmaceutical Co., Ltd.	Oily compositions of antitumor drugs
JPS61189215A (ja) *	1985-02-18	1986-08-22	Teijin Ltd	５−フルオロ−２′−デオキシウリジンエステル類の油状医薬組成物
JPH0621072B2 (ja) *	1986-11-12	1994-03-23	呉羽化学工業株式会社	エストラジオ−ル誘導体よりなる免疫調節剤

1987
- 1987-07-22 JP JP62182842A patent/JPH0794377B2/ja not_active Expired - Lifetime
1988
- 1988-07-18 US US07/220,596 patent/US4921849A/en not_active Expired - Fee Related
- 1988-07-18 PH PH37238A patent/PH26286A/en unknown
- 1988-07-19 ZA ZA885227A patent/ZA885227B/xx unknown
- 1988-07-20 EP EP88306627A patent/EP0300749B1/de not_active Expired - Lifetime
- 1988-07-20 DE DE88306627T patent/DE3887401T2/de not_active Expired - Fee Related
- 1988-07-21 CA CA000572642A patent/CA1315682C/en not_active Expired - Fee Related
- 1988-07-22 KR KR1019880009321A patent/KR900006983B1/ko not_active Expired

Also Published As

Publication number	Publication date
JPH0794377B2 (ja)	1995-10-11
DE3887401T2 (de)	1994-05-11
KR890001565A (ko)	1989-03-27
DE3887401D1 (de)	1994-03-10
KR900006983B1 (ko)	1990-09-25
EP0300749B1 (de)	1994-01-26
AU592708B2 (en)	1990-01-18
EP0300749A2 (de)	1989-01-25
US4921849A (en)	1990-05-01
EP0300749A3 (en)	1990-01-31
AU1971088A (en)	1989-01-27
JPS6426595A (en)	1989-01-27
CA1315682C (en)	1993-04-06
ZA885227B (en)	1989-03-29

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