SI20637A - Aril- in heterociklil-substituirani pirimidinski derivati kot antikoagulanti - Google Patents

Aril- in heterociklil-substituirani pirimidinski derivati kot antikoagulanti Download PDF

Info

Publication number: SI20637A
Authority: SI; Slovenia
Prior art keywords: alkyl; aryl; aralkyl; optionally substituted; halo
Prior art date: 1998-12-04

Application number

SI9920090A

Other languages

English (en)

Slovenian (sl)

Inventor

David D. Davey

Gary B. Phillips

Original Assignee

Berlex Laboratories, 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.)

1998-12-04

Filing date

1999-12-03

Publication date

2002-02-28

1999-12-03 Application filed by Berlex Laboratories, Inc. filed Critical Berlex Laboratories, Inc.

2002-02-28 Publication of SI20637A publication Critical patent/SI20637A/sl

Links

125000003118 aryl group Chemical group 0.000 title claims abstract description 142
125000000623 heterocyclic group Chemical group 0.000 title claims abstract description 17
239000003146 anticoagulant agent Substances 0.000 title abstract description 12
229940127219 anticoagulant drug Drugs 0.000 title abstract description 12
229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 title abstract description 4
150000003230 pyrimidines Chemical class 0.000 title abstract description 4
150000001875 compounds Chemical class 0.000 claims abstract description 255
-1 nitro, ureido, guanidino Chemical group 0.000 claims description 224
125000003710 aryl alkyl group Chemical group 0.000 claims description 160
125000000217 alkyl group Chemical group 0.000 claims description 148
125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 84
125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 83
125000003545 alkoxy group Chemical group 0.000 claims description 77
150000001412 amines Chemical class 0.000 claims description 73
125000001188 haloalkyl group Chemical group 0.000 claims description 73
125000005265 dialkylamine group Chemical group 0.000 claims description 71
125000004473 dialkylaminocarbonyl group Chemical group 0.000 claims description 50
125000004356 hydroxy functional group Chemical group O* 0.000 claims description 43
239000001257 hydrogen Substances 0.000 claims description 42
229910052739 hydrogen Inorganic materials 0.000 claims description 42
150000003839 salts Chemical class 0.000 claims description 40
150000002431 hydrogen Chemical class 0.000 claims description 27
239000000203 mixture Substances 0.000 claims description 22
201000010099 disease Diseases 0.000 claims description 19
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 19
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 15
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 11
WKTCFPZPRJPZID-UHFFFAOYSA-N 4-hydroxy-3-[6-[3-(1-methyl-4,5-dihydroimidazol-2-yl)phenoxy]-2-phenylpyrimidin-4-yl]oxybenzenecarboximidamide Chemical compound CN1CCN=C1C1=CC=CC(OC=2N=C(N=C(OC=3C(=CC=C(C=3)C(N)=N)O)C=2)C=2C=CC=CC=2)=C1 WKTCFPZPRJPZID-UHFFFAOYSA-N 0.000 claims description 9
230000001732 thrombotic effect Effects 0.000 claims description 9
239000008194 pharmaceutical composition Substances 0.000 claims description 8
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XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims description 7
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 6
125000002947 alkylene group Chemical group 0.000 claims description 5
125000001118 alkylidene group Chemical group 0.000 claims description 5
125000004663 dialkyl amino group Chemical group 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 4
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 4
OOLQXIIIKBZNTF-UHFFFAOYSA-N 4-hydroxy-3-[2-[3-(1-methyl-4,5-dihydroimidazol-2-yl)phenoxy]-6-phenylpyrimidin-4-yl]oxybenzenecarboximidamide Chemical compound CN1CCN=C1C1=CC=CC(OC=2N=C(C=C(OC=3C(=CC=C(C=3)C(N)=N)O)N=2)C=2C=CC=CC=2)=C1 OOLQXIIIKBZNTF-UHFFFAOYSA-N 0.000 claims description 3
239000003814 drug Substances 0.000 claims description 3
125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 3
239000003513 alkali Substances 0.000 claims description 2
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DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 6
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GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Chemical class OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 5
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MXXWOMGUGJBKIW-YPCIICBESA-N piperine Chemical compound C=1C=C2OCOC2=CC=1/C=C/C=C/C(=O)N1CCCCC1 MXXWOMGUGJBKIW-YPCIICBESA-N 0.000 description 5
229940075559 piperine Drugs 0.000 description 5
WVWHRXVVAYXKDE-UHFFFAOYSA-N piperine Natural products O=C(C=CC=Cc1ccc2OCOc2c1)C3CCCCN3 WVWHRXVVAYXKDE-UHFFFAOYSA-N 0.000 description 5
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Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/14—Heterocyclic 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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
- 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
- C07D403/14—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 three or more hetero rings

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Diabetes (AREA)
Hematology (AREA)
Oncology (AREA)
Vascular Medicine (AREA)
Obesity (AREA)
Heart & Thoracic Surgery (AREA)
Urology & Nephrology (AREA)
Communicable Diseases (AREA)
Emergency Medicine (AREA)
Endocrinology (AREA)
Cardiology (AREA)
Pulmonology (AREA)
Epidemiology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Separation Of Suspended Particles By Flocculating Agents (AREA)
Agricultural Chemicals And Associated Chemicals (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)

SI9920090A 1998-12-04 1999-12-03 Aril- in heterociklil-substituirani pirimidinski derivati kot antikoagulanti SI20637A (sl)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US09/205,498 US6127376A (en)	1998-12-04	1998-12-04	Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants
PCT/US1999/028537 WO2000033844A1 (en)	1998-12-04	1999-12-03	Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants

Publications (1)

Publication Number	Publication Date
SI20637A true SI20637A (sl)	2002-02-28

Family

ID=22762435

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
SI9920090A SI20637A (sl)	1998-12-04	1999-12-03	Aril- in heterociklil-substituirani pirimidinski derivati kot antikoagulanti

Country Status (26)

Country	Link
US (2)	US6127376A (pt)
EP (1)	EP1135131A4 (pt)
JP (1)	JP2002531506A (pt)
KR (1)	KR20010093799A (pt)
CN (1)	CN1329491A (pt)
AU (1)	AU760370B2 (pt)
BG (1)	BG105557A (pt)
BR (1)	BR9915938A (pt)
CA (1)	CA2354040A1 (pt)
CZ (1)	CZ20011932A3 (pt)
EE (1)	EE200100298A (pt)
HR (1)	HRP20010499A2 (pt)
HU (1)	HUP0104508A3 (pt)
IL (2)	IL143347A0 (pt)
LT (1)	LT4912B (pt)
LV (1)	LV12783B (pt)
MX (1)	MXPA01005656A (pt)
NO (1)	NO20012701L (pt)
NZ (1)	NZ512104A (pt)
PL (1)	PL348034A1 (pt)
RO (1)	RO120971B1 (pt)
RU (1)	RU2001118466A (pt)
SI (1)	SI20637A (pt)
SK (1)	SK7632001A3 (pt)
WO (1)	WO2000033844A1 (pt)
ZA (1)	ZA200104235B (pt)

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1998
- 1998-12-04 US US09/205,498 patent/US6127376A/en not_active Expired - Fee Related
1999
- 1999-12-03 HR HR20010499A patent/HRP20010499A2/hr not_active Application Discontinuation
- 1999-12-03 HU HU0104508A patent/HUP0104508A3/hu unknown
- 1999-12-03 BR BR9915938-4A patent/BR9915938A/pt not_active IP Right Cessation
- 1999-12-03 AU AU31075/00A patent/AU760370B2/en not_active Ceased
- 1999-12-03 RO ROA200100606A patent/RO120971B1/ro unknown
- 1999-12-03 MX MXPA01005656A patent/MXPA01005656A/es not_active IP Right Cessation
- 1999-12-03 NZ NZ512104A patent/NZ512104A/en unknown
- 1999-12-03 EP EP99965087A patent/EP1135131A4/en not_active Withdrawn
- 1999-12-03 RU RU2001118466/14A patent/RU2001118466A/ru not_active Application Discontinuation
- 1999-12-03 JP JP2000586336A patent/JP2002531506A/ja active Pending
- 1999-12-03 IL IL14334799A patent/IL143347A0/xx active IP Right Grant
- 1999-12-03 EE EEP200100298A patent/EE200100298A/xx unknown
- 1999-12-03 CZ CZ20011932A patent/CZ20011932A3/cs unknown
- 1999-12-03 WO PCT/US1999/028537 patent/WO2000033844A1/en not_active Ceased
- 1999-12-03 PL PL99348034A patent/PL348034A1/xx not_active Application Discontinuation
- 1999-12-03 SK SK763-2001A patent/SK7632001A3/sk unknown
- 1999-12-03 CA CA002354040A patent/CA2354040A1/en not_active Abandoned
- 1999-12-03 KR KR1020017006934A patent/KR20010093799A/ko not_active Withdrawn
- 1999-12-03 CN CN99814024A patent/CN1329491A/zh active Pending
- 1999-12-03 SI SI9920090A patent/SI20637A/sl not_active IP Right Cessation
2000
- 2000-03-30 US US09/539,812 patent/US6372751B1/en not_active Expired - Fee Related
2001
- 2001-05-23 ZA ZA200104235A patent/ZA200104235B/en unknown
- 2001-05-24 IL IL143347A patent/IL143347A/en not_active IP Right Cessation
- 2001-06-01 BG BG105557A patent/BG105557A/xx unknown
- 2001-06-01 NO NO20012701A patent/NO20012701L/no not_active Application Discontinuation
- 2001-06-12 LT LT2001061A patent/LT4912B/lt not_active IP Right Cessation
- 2001-07-04 LV LVP-01-100A patent/LV12783B/xx unknown

Also Published As

Publication number	Publication date
BR9915938A (pt)	2001-08-21
LV12783B (en)	2002-10-20
KR20010093799A (ko)	2001-10-29
PL348034A1 (en)	2002-05-06
US6127376A (en)	2000-10-03
CN1329491A (zh)	2002-01-02
CA2354040A1 (en)	2000-06-15
EP1135131A1 (en)	2001-09-26
US6372751B1 (en)	2002-04-16
HUP0104508A3 (en)	2002-07-29
HRP20010499A2 (en)	2003-04-30
JP2002531506A (ja)	2002-09-24
BG105557A (en)	2001-12-29
IL143347A0 (en)	2002-04-21
LT2001061A (en)	2001-12-27
NZ512104A (en)	2003-10-31
ZA200104235B (en)	2002-08-23
EE200100298A (et)	2002-12-16
AU760370B2 (en)	2003-05-15
IL143347A (en)	2006-12-10
NO20012701D0 (no)	2001-06-01
EP1135131A4 (en)	2002-01-02
HUP0104508A2 (hu)	2002-05-29
LT4912B (lt)	2002-04-25
SK7632001A3 (en)	2001-12-03
WO2000033844A1 (en)	2000-06-15
NO20012701L (no)	2001-07-25
MXPA01005656A (es)	2002-04-24
RU2001118466A (ru)	2003-04-20
AU3107500A (en)	2000-06-26
RO120971B1 (ro)	2006-10-30
LV12783A (en)	2002-01-20
CZ20011932A3 (cs)	2001-10-17

Legal Events

Date	Code	Title	Description
2005-01-10	IF	Valid on the event date
2005-10-31	KO00	Lapse of patent	Effective date: 20050830

Publication	Publication Date	Title
SI20637A (sl)	2002-02-28	Aril- in heterociklil-substituirani pirimidinski derivati kot antikoagulanti
US5846970A (en)	1998-12-08	Bicyclic pyrimidine derivatives and their use as anti-coagulants
US6495574B2 (en)	2002-12-17	Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants
US6221886B1 (en)	2001-04-24	Thio acid derived monocyclic N-heterocyclics as anticoagulants
EP0929547B1 (en)	2002-11-27	Benzamidine derivatives substituted by cyclic amino acid or cycl ic hydroxy acid derivatives and their use as anti-coagulants
US5994375A (en)	1999-11-30	Benzamidine derivatives substituted by amino acid and hydroxy acid derivatives and their use as anti-coagulants
HUP9902308A2 (en)	2000-07-28	Anti-coagulant purine derivatives, medicaments containing them and method for producing them
SI20815A (sl)	2002-08-31	Derivati benzenamina kot antikoagulanti