JP2003513066A5 - - Google Patents
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- Publication number
- JP2003513066A5 JP2003513066A5 JP2001534764A JP2001534764A JP2003513066A5 JP 2003513066 A5 JP2003513066 A5 JP 2003513066A5 JP 2001534764 A JP2001534764 A JP 2001534764A JP 2001534764 A JP2001534764 A JP 2001534764A JP 2003513066 A5 JP2003513066 A5 JP 2003513066A5
- Authority
- JP
- Japan
- Prior art keywords
- groups
- alkyl
- different
- formula
- aryl
- Prior art date
- 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.)
- Granted
Links
- 125000004432 carbon atom Chemical group C* 0.000 description 9
- 150000001875 compounds Chemical class 0.000 description 9
- 150000003839 salts Chemical class 0.000 description 9
- 125000004433 nitrogen atom Chemical group N* 0.000 description 8
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 description 7
- 125000001424 substituent group Chemical group 0.000 description 7
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 7
- 125000003118 aryl group Chemical group 0.000 description 6
- 229910052739 hydrogen Inorganic materials 0.000 description 6
- 239000001257 hydrogen Substances 0.000 description 6
- 239000000203 mixture Substances 0.000 description 6
- 229910052757 nitrogen Inorganic materials 0.000 description 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 5
- 125000000217 alkyl group Chemical group 0.000 description 5
- 229910052736 halogen Inorganic materials 0.000 description 5
- 150000002367 halogens Chemical class 0.000 description 5
- 125000005842 heteroatom Chemical group 0.000 description 5
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 description 4
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 4
- 125000002950 monocyclic group Chemical group 0.000 description 4
- -1 nitro, hydroxy Chemical group 0.000 description 4
- 125000005915 C6-C14 aryl group Chemical group 0.000 description 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 3
- 229910052799 carbon Inorganic materials 0.000 description 3
- 125000000623 heterocyclic group Chemical group 0.000 description 3
- 150000002431 hydrogen Chemical class 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 3
- 229920006395 saturated elastomer Polymers 0.000 description 3
- 229910052717 sulfur Inorganic materials 0.000 description 3
- 239000011593 sulfur Substances 0.000 description 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 description 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 2
- 125000001072 heteroaryl group Chemical group 0.000 description 2
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 description 2
- 230000000269 nucleophilic effect Effects 0.000 description 2
- 229910052760 oxygen Inorganic materials 0.000 description 2
- 239000001301 oxygen Substances 0.000 description 2
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 description 1
- 0 *C(C(CN(C(NI)=NI)I)N)=O Chemical compound *C(C(CN(C(NI)=NI)I)N)=O 0.000 description 1
- 108010054265 Factor VIIa Proteins 0.000 description 1
- 108010074860 Factor Xa Proteins 0.000 description 1
- 208000001435 Thromboembolism Diseases 0.000 description 1
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 description 1
- 125000002619 bicyclic group Chemical group 0.000 description 1
- 230000035602 clotting Effects 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 229940012414 factor viia Drugs 0.000 description 1
- 125000000524 functional group Chemical group 0.000 description 1
- 125000005843 halogen group Chemical group 0.000 description 1
- 230000028709 inflammatory response Effects 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 208000037803 restenosis Diseases 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- 208000019553 vascular disease Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP99121623.5 | 1999-10-30 | ||
| EP99121623A EP1095933A1 (en) | 1999-10-30 | 1999-10-30 | Novel N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them |
| PCT/EP2000/010395 WO2001032611A1 (en) | 1999-10-30 | 2000-10-21 | N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2003513066A JP2003513066A (ja) | 2003-04-08 |
| JP2003513066A5 true JP2003513066A5 (enExample) | 2007-12-06 |
| JP4658430B2 JP4658430B2 (ja) | 2011-03-23 |
Family
ID=8239305
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001534764A Expired - Fee Related JP4658430B2 (ja) | 1999-10-30 | 2000-10-21 | Ｎ−グアニジノアルキルアミド、その製造、その使用およびそれを含む医薬調製物 |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | US6472562B1 (enExample) |
| EP (2) | EP1095933A1 (enExample) |
| JP (1) | JP4658430B2 (enExample) |
| KR (1) | KR100981593B1 (enExample) |
| CN (1) | CN1249026C (enExample) |
| AR (1) | AR026257A1 (enExample) |
| AT (1) | ATE264837T1 (enExample) |
| AU (1) | AU776797B2 (enExample) |
| BR (1) | BR0015186A (enExample) |
| CA (1) | CA2389412C (enExample) |
| CZ (1) | CZ301855B6 (enExample) |
| DE (1) | DE60010113T2 (enExample) |
| DK (1) | DK1228039T3 (enExample) |
| EE (1) | EE05168B1 (enExample) |
| ES (1) | ES2220553T3 (enExample) |
| HR (1) | HRP20020372B1 (enExample) |
| HU (1) | HUP0203627A3 (enExample) |
| IL (2) | IL149209A0 (enExample) |
| ME (1) | MEP54708A (enExample) |
| MX (1) | MXPA02003805A (enExample) |
| NO (1) | NO328016B1 (enExample) |
| NZ (1) | NZ518607A (enExample) |
| PL (1) | PL203859B1 (enExample) |
| PT (1) | PT1228039E (enExample) |
| RS (1) | RS50471B (enExample) |
| RU (1) | RU2253651C2 (enExample) |
| SI (1) | SI1228039T1 (enExample) |
| SK (1) | SK286856B6 (enExample) |
| TR (1) | TR200201181T2 (enExample) |
| WO (1) | WO2001032611A1 (enExample) |
| ZA (1) | ZA200203294B (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1644401E (pt) * | 2003-07-04 | 2011-06-06 | Lonza Ag | Acesso melhorado para síntese em fase suportada |
| KR102069498B1 (ko) | 2007-09-28 | 2020-01-23 | 포톨라 파마슈티컬스, 인코포레이티드 | 인자 Ｘａ 저해제에 대한 안티도트 및 그것을 사용하는 방법 |
| US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| BRPI0906473A8 (pt) | 2008-01-04 | 2016-02-10 | Intellikine Inc | Certas entidades químicas, composições e métodos |
| RU2377990C1 (ru) * | 2008-07-23 | 2010-01-10 | Федеральное Государственное Образовательное Учреждение Высшего Профессионального Образования "Южный Федеральный Университет" | Антитромботическое средство, влияющее на регуляцию функциональной активности тромбоцитов |
| CA2743496C (en) | 2008-11-14 | 2018-03-27 | Portola Pharmaceuticals, Inc. | Antidotes for factor xa inhibitors and methods of using the same in combination with blood coagulating agents |
| PL3604510T3 (pl) | 2009-03-30 | 2025-07-28 | Alexion Pharmaceuticals, Inc. | Antidota na inhibitory czynnika xa i sposoby ich stosowania |
| EP2453910B1 (en) | 2009-07-15 | 2016-08-31 | Portola Pharmaceuticals, Inc. | Unit dose formulation of antidote for factor xa inhibitors for use in preventing bleeding |
| EP3238722B1 (en) | 2011-01-10 | 2019-03-13 | Infinity Pharmaceuticals, Inc. | Solid forms of isoquinolinones |
| US8828998B2 (en) | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
| RU2702908C2 (ru) | 2012-11-01 | 2019-10-14 | Инфинити Фармасьютикалз, Инк. | Лечение злокачественных опухолей с использованием модуляторов изоформ pi3-киназы |
| WO2015160975A2 (en) | 2014-04-16 | 2015-10-22 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| EP3474856B1 (en) | 2016-06-24 | 2022-09-14 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| CN110357800B (zh) * | 2018-04-09 | 2022-07-26 | 青岛海生洋润生物科技有限公司 | 脯氨酸衍生物及其在制备治疗心脑血管疾病药物中的应用 |
| CN121221582A (zh) * | 2021-05-10 | 2025-12-30 | 中国海洋大学 | 一种苯酰胍衍生物在用于制备预防和治疗神经系统疾病或心血管系统疾病的药物中的应用 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU206372B (en) * | 1990-09-03 | 1992-10-28 | Richter Gedeon Vegyeszet | Process for producing new oligopeptides which selectively inhibit proliferation of haemopoietic cells and pharmaceutical compositions comprising same |
| US5506134A (en) | 1990-10-22 | 1996-04-09 | Corvas International, Inc. | Hypridoma and monoclonal antibody which inhibits blood coagulation tissue factor/factor VIIa complex |
| US5833982A (en) | 1991-02-28 | 1998-11-10 | Zymogenetics, Inc. | Modified factor VII |
| US5788965A (en) | 1991-02-28 | 1998-08-04 | Novo Nordisk A/S | Modified factor VII |
| US5371072A (en) * | 1992-10-16 | 1994-12-06 | Corvas International, Inc. | Asp-Pro-Arg α-keto-amide enzyme inhibitors |
| DE4326465A1 (de) * | 1993-01-20 | 1995-02-09 | Thomae Gmbh Dr K | Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung |
| WO1994017635A1 (en) | 1993-01-20 | 1994-08-04 | Peter John Alexandrovics | A line monitoring system |
| NZ263084A (en) * | 1993-03-12 | 1997-08-22 | Arris Pharm Corp | Dipeptide derivatives, treatment of immunomediated inflammatory disorders |
| ZA953361B (en) | 1994-04-26 | 1996-01-12 | Selectide Corp | Factor Xa inhibitors |
| NZ296210A (en) * | 1994-12-02 | 1998-05-27 | Yamanouchi Pharma Co Ltd | Amidinonaphthyl derivatives to inhibit activated blood coagulation factor x |
| US6342504B1 (en) * | 1994-12-13 | 2002-01-29 | Corvas International, Inc. | Aromatic heterocyclic derivatives as enzyme inhibitors |
| EP1020434A4 (en) * | 1997-08-27 | 2000-11-15 | Kissei Pharmaceutical | 3-AMIDINOANILINE DERIVATIVES, INHIBITORS OF THE ACTIVATED BLOOD COINTENANCE FACTOR X AND INTERMEDIATE PRODUCTS FOR PRODUCING BOTH |
| SE9703414D0 (sv) * | 1997-09-23 | 1997-09-23 | Astra Ab | New compounds |
| BR9814340B1 (pt) | 1997-12-24 | 2010-07-13 | compostos derivados de indol, processo para a preparação dos mesmo e composição farmacêutica. | |
| WO1999037643A1 (en) * | 1998-01-26 | 1999-07-29 | Yamanouchi Pharmaceutical Co., Ltd. | Novel benzene-fused heterocyclic derivatives or salts thereof |
| EP0987274A1 (en) | 1998-09-15 | 2000-03-22 | Hoechst Marion Roussel Deutschland GmbH | Factor VIIa Inhibitors |
| US6348482B1 (en) * | 1999-05-05 | 2002-02-19 | Merck & Co., Inc. | Catechols as antimicrobial agents |
-
1999
- 1999-10-30 EP EP99121623A patent/EP1095933A1/en not_active Withdrawn
-
2000
- 2000-10-21 SK SK578-2002A patent/SK286856B6/sk not_active IP Right Cessation
- 2000-10-21 CZ CZ20021489A patent/CZ301855B6/cs not_active IP Right Cessation
- 2000-10-21 NZ NZ518607A patent/NZ518607A/en not_active IP Right Cessation
- 2000-10-21 ES ES00971396T patent/ES2220553T3/es not_active Expired - Lifetime
- 2000-10-21 DK DK00971396T patent/DK1228039T3/da active
- 2000-10-21 CA CA002389412A patent/CA2389412C/en not_active Expired - Fee Related
- 2000-10-21 ME MEP-547/08A patent/MEP54708A/xx unknown
- 2000-10-21 RU RU2002114041/04A patent/RU2253651C2/ru not_active IP Right Cessation
- 2000-10-21 HR HR20020372A patent/HRP20020372B1/xx not_active IP Right Cessation
- 2000-10-21 BR BR0015186-6A patent/BR0015186A/pt active Search and Examination
- 2000-10-21 CN CNB008151407A patent/CN1249026C/zh not_active Expired - Fee Related
- 2000-10-21 AU AU10265/01A patent/AU776797B2/en not_active Ceased
- 2000-10-21 KR KR1020027005515A patent/KR100981593B1/ko not_active Expired - Fee Related
- 2000-10-21 PT PT00971396T patent/PT1228039E/pt unknown
- 2000-10-21 AT AT00971396T patent/ATE264837T1/de active
- 2000-10-21 JP JP2001534764A patent/JP4658430B2/ja not_active Expired - Fee Related
- 2000-10-21 MX MXPA02003805A patent/MXPA02003805A/es active IP Right Grant
- 2000-10-21 WO PCT/EP2000/010395 patent/WO2001032611A1/en not_active Ceased
- 2000-10-21 IL IL14920900A patent/IL149209A0/xx active IP Right Grant
- 2000-10-21 EE EEP200200199A patent/EE05168B1/xx not_active IP Right Cessation
- 2000-10-21 PL PL354808A patent/PL203859B1/pl not_active IP Right Cessation
- 2000-10-21 TR TR2002/01181T patent/TR200201181T2/xx unknown
- 2000-10-21 RS YUP-297/02A patent/RS50471B/sr unknown
- 2000-10-21 DE DE60010113T patent/DE60010113T2/de not_active Expired - Lifetime
- 2000-10-21 SI SI200030422T patent/SI1228039T1/xx unknown
- 2000-10-21 EP EP00971396A patent/EP1228039B1/en not_active Expired - Lifetime
- 2000-10-21 HU HU0203627A patent/HUP0203627A3/hu unknown
- 2000-10-26 AR ARP000105647A patent/AR026257A1/es active IP Right Grant
- 2000-10-27 US US09/697,188 patent/US6472562B1/en not_active Expired - Lifetime
-
2002
- 2002-04-18 IL IL149209A patent/IL149209A/en not_active IP Right Cessation
- 2002-04-25 ZA ZA200203294A patent/ZA200203294B/xx unknown
- 2002-04-29 NO NO20022022A patent/NO328016B1/no not_active IP Right Cessation
- 2002-08-26 US US10/227,222 patent/US6664393B2/en not_active Expired - Lifetime
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