HRP20010499A2 - Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants - Google Patents
Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants Download PDFInfo
- Publication number
- HRP20010499A2 HRP20010499A2 HR20010499A HRP20010499A HRP20010499A2 HR P20010499 A2 HRP20010499 A2 HR P20010499A2 HR 20010499 A HR20010499 A HR 20010499A HR P20010499 A HRP20010499 A HR P20010499A HR P20010499 A2 HRP20010499 A2 HR P20010499A2
- Authority
- HR
- Croatia
- Prior art keywords
- alkyl
- aryl
- optionally substituted
- halo
- nitro
- Prior art date
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- 125000003118 aryl group Chemical group 0.000 title claims description 126
- 125000000623 heterocyclic group Chemical group 0.000 title claims description 12
- 239000003146 anticoagulant agent Substances 0.000 title description 12
- 229940127219 anticoagulant drug Drugs 0.000 title description 12
- 229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 title description 2
- 150000003230 pyrimidines Chemical class 0.000 title description 2
- -1 nitro, ureido, guanidino Chemical group 0.000 claims description 291
- 239000000126 substance Substances 0.000 claims description 242
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 141
- 125000000217 alkyl group Chemical group 0.000 claims description 133
- 125000001188 haloalkyl group Chemical group 0.000 claims description 79
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 69
- 125000004473 dialkylaminocarbonyl group Chemical group 0.000 claims description 69
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 68
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 68
- 125000003545 alkoxy group Chemical group 0.000 claims description 65
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 57
- 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 41
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- 238000000034 method Methods 0.000 claims description 30
- 150000002431 hydrogen Chemical group 0.000 claims description 27
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- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 description 1
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- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
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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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Communicable Diseases (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Endocrinology (AREA)
- Obesity (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)
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 |
|---|---|
| HRP20010499A2 true HRP20010499A2 (en) | 2003-04-30 |
Family
ID=22762435
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20010499A HRP20010499A2 (en) | 1998-12-04 | 2001-07-04 | Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US6127376A (lt) |
| EP (1) | EP1135131A4 (lt) |
| JP (1) | JP2002531506A (lt) |
| KR (1) | KR20010093799A (lt) |
| CN (1) | CN1329491A (lt) |
| AU (1) | AU760370B2 (lt) |
| BG (1) | BG105557A (lt) |
| BR (1) | BR9915938A (lt) |
| CA (1) | CA2354040A1 (lt) |
| CZ (1) | CZ20011932A3 (lt) |
| EE (1) | EE200100298A (lt) |
| HR (1) | HRP20010499A2 (lt) |
| HU (1) | HUP0104508A3 (lt) |
| IL (2) | IL143347A0 (lt) |
| LT (1) | LT4912B (lt) |
| LV (1) | LV12783B (lt) |
| MX (1) | MXPA01005656A (lt) |
| NO (1) | NO20012701L (lt) |
| NZ (1) | NZ512104A (lt) |
| PL (1) | PL348034A1 (lt) |
| RO (1) | RO120971B1 (lt) |
| RU (1) | RU2001118466A (lt) |
| SI (1) | SI20637A (lt) |
| SK (1) | SK7632001A3 (lt) |
| WO (1) | WO2000033844A1 (lt) |
| ZA (1) | ZA200104235B (lt) |
Families Citing this family (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996028427A1 (en) | 1995-03-10 | 1996-09-19 | Berlex Laboratories, Inc. | Benzamidine derivatives their preparation and their use as anti-coagulants |
| US6686364B2 (en) | 1997-12-08 | 2004-02-03 | Berlex Laboratories, Inc. | Benzamidine derivatives and their use as anti-coagulants |
| US6262088B1 (en) | 1998-11-19 | 2001-07-17 | Berlex Laboratories, Inc. | Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants |
| US6350761B1 (en) | 1999-07-30 | 2002-02-26 | Berlex Laboratories, Inc. | Benzenamine derivatives as anti-coagulants |
| US7129242B2 (en) | 2000-12-06 | 2006-10-31 | Signal Pharmaceuticals, Llc | Anilinopyrimidine derivatives as JNK pathway inhibitors and compositions and methods related thereto |
| US7122544B2 (en) | 2000-12-06 | 2006-10-17 | Signal Pharmaceuticals, Llc | Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto |
| TWI329105B (en) * | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| AU2003217961B2 (en) | 2002-03-08 | 2008-02-28 | Signal Pharmaceuticals, Llc | Combination therapy for treating, preventing or managing proliferative disorders and cancers |
| GB0206215D0 (en) | 2002-03-15 | 2002-05-01 | Novartis Ag | Organic compounds |
| DE60330466D1 (de) | 2002-07-29 | 2010-01-21 | Rigel Pharmaceuticals Inc | VERFAHREN ZUR BEHANDLUNG ODER PRuVENTION VON AUTOIMMUNKRANKHEITEN MIT 2,4-PYRIMIDINDIAMIN-VERBINDUNGEN |
| BR0313255A (pt) * | 2002-08-08 | 2005-07-12 | Amgen Inc | Composto, composição farmacêutica, uso de um composto e métodos de fabricar um medicamento e de preparar um composto |
| PT1569912E (pt) | 2002-12-03 | 2015-09-15 | Pharmacyclics Llc | Derivados 2-(2-hidroxibifenil-3-il)-1h-benzoimidazole-5- carboxamidina como inibidores do fator viia |
| NZ545270A (en) | 2003-07-30 | 2010-04-30 | Rigel Pharmaceuticals Inc | 2,4-Pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases |
| WO2005047268A2 (en) * | 2003-11-10 | 2005-05-26 | X-Ceptor Therapeutics, Inc. | Substituted pyrimidine compositions and methods of use |
| ES2380550T3 (es) * | 2004-11-24 | 2012-05-16 | Rigel Pharmaceuticals, Inc. | Compuestos de espiro-2,4-pirimidindiamina y sus usos |
| EP2161275A1 (en) | 2005-01-19 | 2010-03-10 | Rigel Pharmaceuticals, Inc. | Prodrugs of 2,4-pyrimidinediamine compounds and their uses |
| US20060270694A1 (en) * | 2005-05-03 | 2006-11-30 | Rigel Pharmaceuticals, Inc. | JAK kinase inhibitors and their uses |
| US8367682B2 (en) * | 2006-07-21 | 2013-02-05 | Novartis Ag | Pyrimidine derivatives and their use as pesticides |
| NZ589315A (en) | 2008-04-16 | 2012-11-30 | Portola Pharm Inc | 2,6-diamino-pyrimidin-5-yl-carboxamides as Spleen tryosine kinase (syk) or Janus kinase (JAK) inhibitors |
| US8138339B2 (en) | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| EP2300013B1 (en) | 2008-05-21 | 2017-09-06 | Ariad Pharmaceuticals, Inc. | Phosphorous derivatives as kinase inhibitors |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| JP2011526299A (ja) | 2008-06-27 | 2011-10-06 | アビラ セラピューティクス， インコーポレイテッド | ヘテロアリール化合物およびそれらの使用 |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US8932842B2 (en) | 2009-02-11 | 2015-01-13 | Northwestern University | Aminopyridine dimer compounds, compositions and related methods for neuronal nitric oxide synthase inhibition |
| US8278084B2 (en) | 2009-02-11 | 2012-10-02 | Northwestern University | Aminopyridine dimer compounds, compositions and related methods for neuronal nitric oxide synthase inhibition |
| CA2760794C (en) | 2009-05-05 | 2017-07-25 | Dana Farber Cancer Institute | Egfr inhibitors and methods of treating disorders |
| AU2011289604C1 (en) | 2010-08-10 | 2016-04-21 | Celgene Avilomics Research, Inc. | Besylate salt of a BTK inhibitor |
| EP2635285B1 (en) | 2010-11-01 | 2017-05-03 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| NZ609957A (en) | 2010-11-01 | 2015-08-28 | Celgene Avilomics Res Inc | Heterocyclic compounds and uses thereof |
| WO2012064706A1 (en) | 2010-11-10 | 2012-05-18 | Avila Therapeutics, Inc. | Mutant-selective egfr inhibitors and uses thereof |
| JP5999177B2 (ja) | 2011-05-04 | 2016-09-28 | アリアド・ファーマシューティカルズ・インコーポレイテッド | Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物 |
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| BR112014022789B1 (pt) | 2012-03-15 | 2022-04-19 | Celgene Car Llc | Formas sólidas de um inibidor de quinase de receptor do fator de crescimento epidérmico, composição farmacêutica e usos do mesmo |
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1998
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1999
- 1999-12-03 AU AU31075/00A patent/AU760370B2/en not_active Ceased
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- 1999-12-03 HU HU0104508A patent/HUP0104508A3/hu unknown
- 1999-12-03 NZ NZ512104A patent/NZ512104A/en unknown
- 1999-12-03 EP EP99965087A patent/EP1135131A4/en not_active Withdrawn
- 1999-12-03 JP JP2000586336A patent/JP2002531506A/ja active Pending
- 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 EE EEP200100298A patent/EE200100298A/xx unknown
- 1999-12-03 KR KR1020017006934A patent/KR20010093799A/ko not_active Application Discontinuation
- 1999-12-03 CA CA002354040A patent/CA2354040A1/en not_active Abandoned
- 1999-12-03 CN CN99814024A patent/CN1329491A/zh active Pending
- 1999-12-03 PL PL99348034A patent/PL348034A1/xx not_active Application Discontinuation
- 1999-12-03 RU RU2001118466/14A patent/RU2001118466A/ru not_active Application Discontinuation
- 1999-12-03 BR BR9915938-4A patent/BR9915938A/pt not_active IP Right Cessation
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- 1999-12-03 WO PCT/US1999/028537 patent/WO2000033844A1/en not_active Application Discontinuation
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2000
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2001
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- 2001-06-12 LT LT2001061A patent/LT4912B/lt not_active IP Right Cessation
- 2001-07-04 HR HR20010499A patent/HRP20010499A2/hr not_active Application Discontinuation
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Also Published As
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| BR9915938A (pt) | 2001-08-21 |
| EE200100298A (et) | 2002-12-16 |
| US6127376A (en) | 2000-10-03 |
| NO20012701D0 (no) | 2001-06-01 |
| CN1329491A (zh) | 2002-01-02 |
| SK7632001A3 (en) | 2001-12-03 |
| KR20010093799A (ko) | 2001-10-29 |
| PL348034A1 (en) | 2002-05-06 |
| LT2001061A (lt) | 2001-12-27 |
| US6372751B1 (en) | 2002-04-16 |
| CZ20011932A3 (cs) | 2001-10-17 |
| HUP0104508A2 (hu) | 2002-05-29 |
| JP2002531506A (ja) | 2002-09-24 |
| RO120971B1 (ro) | 2006-10-30 |
| IL143347A0 (en) | 2002-04-21 |
| WO2000033844A1 (en) | 2000-06-15 |
| SI20637A (sl) | 2002-02-28 |
| AU3107500A (en) | 2000-06-26 |
| BG105557A (en) | 2001-12-29 |
| NO20012701L (no) | 2001-07-25 |
| EP1135131A4 (en) | 2002-01-02 |
| NZ512104A (en) | 2003-10-31 |
| LV12783B (en) | 2002-10-20 |
| HUP0104508A3 (en) | 2002-07-29 |
| ZA200104235B (en) | 2002-08-23 |
| EP1135131A1 (en) | 2001-09-26 |
| IL143347A (en) | 2006-12-10 |
| MXPA01005656A (es) | 2002-04-24 |
| RU2001118466A (ru) | 2003-04-20 |
| AU760370B2 (en) | 2003-05-15 |
| LV12783A (en) | 2002-01-20 |
| CA2354040A1 (en) | 2000-06-15 |
| LT4912B (lt) | 2002-04-25 |
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