JP2000501073A - １−アリールスルホニル、アリール（チオ）カルボニルピリダジノ誘導体及び製造法 - Google Patents

１−アリールスルホニル、アリール（チオ）カルボニルピリダジノ誘導体及び製造法

Info

Publication number: JP2000501073A
Authority: JP; Japan
Prior art keywords: diazo; hexahydro; hexahydrophenanthrene; benzo; cyclohepta
Prior art date: 1995-11-06
Legal status (The legal status 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 status listed.): Ceased

Application number

JP9518177A

Other languages

English (en)

Japanese (ja)

Inventor

コームス，ドナルド・ダブリユー

Original Assignee

オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド

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.)

1995-11-06

Filing date

1996-10-10

Publication date

2000-02-02

1996-10-10 Application filed by オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド filed Critical オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド

2000-02-02 Publication of JP2000501073A publication Critical patent/JP2000501073A/ja

Status Ceased legal-status Critical Current

Links

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208000001132 Osteoporosis Diseases 0.000 claims abstract description 6
230000009245 menopause Effects 0.000 claims abstract description 5
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WQKHERPPDYPMNX-UHFFFAOYSA-N 6-chloro-3,4-dihydro-2h-naphthalen-1-one Chemical compound O=C1CCCC2=CC(Cl)=CC=C21 WQKHERPPDYPMNX-UHFFFAOYSA-N 0.000 description 1
ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 description 1
DIYWCGZFCFYCIE-UHFFFAOYSA-N 8-bromo-3,4-dihydro-2h-naphthalen-1-one Chemical compound C1CCC(=O)C2=C1C=CC=C2Br DIYWCGZFCFYCIE-UHFFFAOYSA-N 0.000 description 1
241001156002 Anthonomus pomorum Species 0.000 description 1
241000255925 Diptera Species 0.000 description 1
KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 1
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 1
YBIMKXARZPMCJM-UHFFFAOYSA-N Ic1ccc(cc1)[S](=O)=O Chemical group Ic1ccc(cc1)[S](=O)=O YBIMKXARZPMCJM-UHFFFAOYSA-N 0.000 description 1
102000004877 Insulin Human genes 0.000 description 1
108090001061 Insulin Proteins 0.000 description 1
WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 description 1
FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
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239000012979 RPMI medium Substances 0.000 description 1
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PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 1
229920002472 Starch Polymers 0.000 description 1
229930006000 Sucrose Natural products 0.000 description 1
CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
ATJFFYVFTNAWJD-UHFFFAOYSA-N Tin Chemical compound [Sn] ATJFFYVFTNAWJD-UHFFFAOYSA-N 0.000 description 1
DJLIDEBGUUAVAX-UHFFFAOYSA-K [Al](I)(I)I.[Li] Chemical compound [Al](I)(I)I.[Li] DJLIDEBGUUAVAX-UHFFFAOYSA-K 0.000 description 1
230000010933 acylation Effects 0.000 description 1
238000005917 acylation reaction Methods 0.000 description 1
239000000556 agonist Substances 0.000 description 1
125000003545 alkoxy group Chemical group 0.000 description 1
XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
229910052782 aluminium Inorganic materials 0.000 description 1
239000005557 antagonist Substances 0.000 description 1
FIVPIPIDMRVLAY-UHFFFAOYSA-N aspergillin Natural products C1C2=CC=CC(O)C2N2C1(SS1)C(=O)N(C)C1(CO)C2=O FIVPIPIDMRVLAY-UHFFFAOYSA-N 0.000 description 1
238000003556 assay Methods 0.000 description 1
239000012298 atmosphere Substances 0.000 description 1
SLUNEGLMXGHOLY-UHFFFAOYSA-N benzene;hexane Chemical compound CCCCCC.C1=CC=CC=C1 SLUNEGLMXGHOLY-UHFFFAOYSA-N 0.000 description 1
239000011230 binding agent Substances 0.000 description 1
230000004071 biological effect Effects 0.000 description 1
239000008280 blood Substances 0.000 description 1
210000004369 blood Anatomy 0.000 description 1
238000009835 boiling Methods 0.000 description 1
230000031709 bromination Effects 0.000 description 1
238000005893 bromination reaction Methods 0.000 description 1
201000011510 cancer Diseases 0.000 description 1
125000001309 chloro group Chemical group Cl* 0.000 description 1
239000003086 colorant Substances 0.000 description 1
238000012875 competitive assay Methods 0.000 description 1
238000013329 compounding Methods 0.000 description 1
239000003433 contraceptive agent Substances 0.000 description 1
230000002254 contraceptive effect Effects 0.000 description 1
238000002425 crystallisation Methods 0.000 description 1
230000008025 crystallization Effects 0.000 description 1
230000001351 cycling effect Effects 0.000 description 1
CGZZMOTZOONQIA-UHFFFAOYSA-N cycloheptanone Chemical compound O=C1CCCCCC1 CGZZMOTZOONQIA-UHFFFAOYSA-N 0.000 description 1
230000001086 cytosolic effect Effects 0.000 description 1
125000000950 dibromo group Chemical group Br* 0.000 description 1
229940117389 dichlorobenzene Drugs 0.000 description 1
239000003085 diluting agent Substances 0.000 description 1
239000007884 disintegrant Substances 0.000 description 1
239000003814 drug Substances 0.000 description 1
238000001035 drying Methods 0.000 description 1
239000012259 ether extract Substances 0.000 description 1
AEOCXXJPGCBFJA-UHFFFAOYSA-N ethionamide Chemical compound CCC1=CC(C(N)=S)=CC=N1 AEOCXXJPGCBFJA-UHFFFAOYSA-N 0.000 description 1
238000001704 evaporation Methods 0.000 description 1
238000000605 extraction Methods 0.000 description 1
239000012467 final product Substances 0.000 description 1
239000000796 flavoring agent Substances 0.000 description 1
235000019634 flavors Nutrition 0.000 description 1
239000011737 fluorine Substances 0.000 description 1
229910052731 fluorine Inorganic materials 0.000 description 1
239000012737 fresh medium Substances 0.000 description 1
239000007789 gas Substances 0.000 description 1
239000000499 gel Substances 0.000 description 1
150000002334 glycols Chemical class 0.000 description 1
239000003979 granulating agent Substances 0.000 description 1
125000005843 halogen group Chemical group 0.000 description 1
230000002140 halogenating effect Effects 0.000 description 1
230000026030 halogenation Effects 0.000 description 1
238000005658 halogenation reaction Methods 0.000 description 1
230000020169 heat generation Effects 0.000 description 1
238000010438 heat treatment Methods 0.000 description 1
LELOWRISYMNNSU-UHFFFAOYSA-N hydrogen cyanide Chemical compound N#C LELOWRISYMNNSU-UHFFFAOYSA-N 0.000 description 1
239000004615 ingredient Substances 0.000 description 1
229940125396 insulin Drugs 0.000 description 1
239000011872 intimate mixture Substances 0.000 description 1
239000011630 iodine Substances 0.000 description 1
229910052740 iodine Inorganic materials 0.000 description 1
125000002346 iodo group Chemical group I* 0.000 description 1
150000002500 ions Chemical class 0.000 description 1
125000000468 ketone group Chemical group 0.000 description 1
229910052744 lithium Inorganic materials 0.000 description 1
239000000314 lubricant Substances 0.000 description 1
239000011777 magnesium Substances 0.000 description 1
229910052749 magnesium Inorganic materials 0.000 description 1
239000000463 material Substances 0.000 description 1
238000005259 measurement Methods 0.000 description 1
230000003278 mimic effect Effects 0.000 description 1
239000004570 mortar (masonry) Substances 0.000 description 1
229960004719 nandrolone Drugs 0.000 description 1
229910052757 nitrogen Inorganic materials 0.000 description 1
239000006186 oral dosage form Substances 0.000 description 1
229910052760 oxygen Inorganic materials 0.000 description 1
238000007911 parenteral administration Methods 0.000 description 1
230000003334 potential effect Effects 0.000 description 1
JWMFYGXQPXQEEM-WZBAXQLOSA-N pregnane Chemical compound C1CC2CCCC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](CC)[C@@]1(C)CC2 JWMFYGXQPXQEEM-WZBAXQLOSA-N 0.000 description 1
230000002335 preservative effect Effects 0.000 description 1
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239000000186 progesterone Substances 0.000 description 1
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Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/06—Antiabortive agents; Labour repressants
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/18—Feminine contraceptives
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/36—Benzo-cinnolines

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Animal Behavior & Ethology (AREA)
Pharmacology & Pharmacy (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Endocrinology (AREA)
Physical Education & Sports Medicine (AREA)
Reproductive Health (AREA)
Rheumatology (AREA)
Gynecology & Obstetrics (AREA)
Orthopedic Medicine & Surgery (AREA)
Pregnancy & Childbirth (AREA)
Diabetes (AREA)
Epidemiology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

JP9518177A 1995-11-06 1996-10-10 １−アリールスルホニル、アリール（チオ）カルボニルピリダジノ誘導体及び製造法 Ceased JP2000501073A (ja)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
US790095P	1995-11-06	1995-11-06
US60/007,900		1995-11-06
PCT/US1996/016227 WO1997017332A1 (en)	1995-11-06	1996-10-10	1-arylsulphonyl, aryl(thio)carbonyl pyridazino derivatives and methods of preparation

Publications (1)

Publication Number	Publication Date
JP2000501073A true JP2000501073A (ja)	2000-02-02

Family

ID=21728709

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
JP9518177A Ceased JP2000501073A (ja)	1995-11-06	1996-10-10	１−アリールスルホニル、アリール（チオ）カルボニルピリダジノ誘導体及び製造法

Country Status (17)

Country	Link
JP (1)	JP2000501073A (zh)
KR (1)	KR100360614B1 (zh)
CN (1)	CN1110485C (zh)
AU (1)	AU704507B2 (zh)
BR (1)	BR9611407A (zh)
CZ (1)	CZ286789B6 (zh)
HU (1)	HU225162B1 (zh)
IL (1)	IL124320A (zh)
MX (1)	MX9803605A (zh)
NO (1)	NO310460B1 (zh)
NZ (1)	NZ319979A (zh)
PL (1)	PL185618B1 (zh)
RU (1)	RU2175969C2 (zh)
TW (1)	TW460467B (zh)
UA (1)	UA48989C2 (zh)
WO (1)	WO1997017332A1 (zh)
ZA (1)	ZA969298B (zh)

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4816467A (en) *	1987-01-09	1989-03-28	Farmitalia Carlo Erba S.R.L	Heteroaryl 3-oxo-propanenitrile derivatives, pharmaceutical compositions and use
ATE92476T1 (de) *	1987-11-02	1993-08-15	Yoshitomi Pharmaceutical	Kondensierte pyridazin-verbindungen und deren verwendung als arzneimittel.
CA2116448A1 (en) *	1991-08-27	1993-03-04	Tohru Nakao	Fused pyridazine compound and pharmaceutical use thereof

1996
- 1996-10-10 HU HU0201305A patent/HU225162B1/hu not_active IP Right Cessation
- 1996-10-10 RU RU98110813/04A patent/RU2175969C2/ru not_active IP Right Cessation
- 1996-10-10 BR BR9611407-0A patent/BR9611407A/pt not_active Application Discontinuation
- 1996-10-10 CN CN96199481A patent/CN1110485C/zh not_active Expired - Fee Related
- 1996-10-10 JP JP9518177A patent/JP2000501073A/ja not_active Ceased
- 1996-10-10 WO PCT/US1996/016227 patent/WO1997017332A1/en not_active Ceased
- 1996-10-10 PL PL96326669A patent/PL185618B1/pl not_active IP Right Cessation
- 1996-10-10 UA UA98052267A patent/UA48989C2/uk unknown
- 1996-10-10 CZ CZ19981380A patent/CZ286789B6/cs not_active IP Right Cessation
- 1996-10-10 KR KR10-1998-0703345A patent/KR100360614B1/ko not_active Expired - Fee Related
- 1996-10-10 AU AU72637/96A patent/AU704507B2/en not_active Ceased
- 1996-10-10 NZ NZ319979A patent/NZ319979A/xx unknown
- 1996-10-10 IL IL12432096A patent/IL124320A/en not_active IP Right Cessation
- 1996-11-05 ZA ZA9609298A patent/ZA969298B/xx unknown
- 1996-11-25 TW TW085114479A patent/TW460467B/zh not_active IP Right Cessation
1998
- 1998-05-05 NO NO19982030A patent/NO310460B1/no unknown
- 1998-05-06 MX MX9803605A patent/MX9803605A/es not_active IP Right Cessation

Also Published As

Publication number	Publication date
ZA969298B (en)	1998-05-05
IL124320A0 (en)	1998-12-06
NO310460B1 (no)	2001-07-09
KR19990067340A (ko)	1999-08-16
CZ138098A3 (cs)	1998-09-16
HU225162B1 (en)	2006-07-28
UA48989C2 (uk)	2002-09-16
CZ286789B6 (en)	2000-07-12
HUP0201305A3 (en)	2003-02-28
CN1110485C (zh)	2003-06-04
NO982030D0 (no)	1998-05-05
PL185618B1 (pl)	2003-06-30
AU704507B2 (en)	1999-04-22
RU2175969C2 (ru)	2001-11-20
PL326669A1 (en)	1998-10-12
WO1997017332A1 (en)	1997-05-15
IL124320A (en)	2001-10-31
NO982030L (no)	1998-06-23
HUP0201305A2 (hu)	2002-12-28
CN1207091A (zh)	1999-02-03
NZ319979A (en)	1999-11-29
MX9803605A (es)	1998-09-30
TW460467B (en)	2001-10-21
KR100360614B1 (ko)	2003-06-02
BR9611407A (pt)	1999-12-28
AU7263796A (en)	1997-05-29

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A02

Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20080304