JP2010511641A5 - - Google Patents
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- Publication number
- JP2010511641A5 JP2010511641A5 JP2009539631A JP2009539631A JP2010511641A5 JP 2010511641 A5 JP2010511641 A5 JP 2010511641A5 JP 2009539631 A JP2009539631 A JP 2009539631A JP 2009539631 A JP2009539631 A JP 2009539631A JP 2010511641 A5 JP2010511641 A5 JP 2010511641A5
- Authority
- JP
- Japan
- Prior art keywords
- alkylene
- alkyl
- phenyl
- substituted
- independently
- 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
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 71
- -1 amino, carboxyl Chemical group 0.000 claims 71
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 38
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 32
- 229910052736 halogen Inorganic materials 0.000 claims 26
- 150000002367 halogens Chemical class 0.000 claims 26
- 125000000753 cycloalkyl group Chemical group 0.000 claims 15
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 14
- 125000002947 alkylene group Chemical group 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 6
- 125000002619 bicyclic group Chemical group 0.000 claims 6
- BVCRERJDOOBZOH-UHFFFAOYSA-N bicyclo[2.2.1]heptanyl Chemical group C1C[C+]2CC[C-]1C2 BVCRERJDOOBZOH-UHFFFAOYSA-N 0.000 claims 5
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 5
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 5
- 125000006413 ring segment Chemical group 0.000 claims 5
- 229940124530 sulfonamide Drugs 0.000 claims 5
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 4
- 229960002684 aminocaproic acid Drugs 0.000 claims 4
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 4
- 125000005508 decahydronaphthalenyl group Chemical group 0.000 claims 4
- 239000011737 fluorine Substances 0.000 claims 4
- 229910052731 fluorine Inorganic materials 0.000 claims 4
- 125000002950 monocyclic group Chemical group 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 125000003072 pyrazolidinyl group Chemical group 0.000 claims 4
- 229920006395 saturated elastomer Polymers 0.000 claims 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 3
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 3
- 125000004122 cyclic group Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 239000001301 oxygen Substances 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 150000003463 sulfur Chemical class 0.000 claims 3
- 125000001544 thienyl group Chemical group 0.000 claims 3
- NGERQMAWGVKQNJ-UHFFFAOYSA-N 4-azabicyclo[3.2.2]nonane Chemical compound C1CC2CCC1NCC2 NGERQMAWGVKQNJ-UHFFFAOYSA-N 0.000 claims 2
- SNZSSCZJMVIOCR-UHFFFAOYSA-N 7-azabicyclo[2.2.1]heptane Chemical compound C1CC2CCC1N2 SNZSSCZJMVIOCR-UHFFFAOYSA-N 0.000 claims 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-N Propionic acid Substances CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 2
- 230000029936 alkylation Effects 0.000 claims 2
- 238000005804 alkylation reaction Methods 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- NNBZCPXTIHJBJL-UHFFFAOYSA-N decalin Chemical compound C1CCCC2CCCCC21 NNBZCPXTIHJBJL-UHFFFAOYSA-N 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000004502 1,2,3-oxadiazolyl group Chemical group 0.000 claims 1
- 125000004511 1,2,3-thiadiazolyl group Chemical group 0.000 claims 1
- 125000001399 1,2,3-triazolyl group Chemical group N1N=NC(=C1)* 0.000 claims 1
- 125000004504 1,2,4-oxadiazolyl group Chemical group 0.000 claims 1
- 125000001376 1,2,4-triazolyl group Chemical group N1N=C(N=C1)* 0.000 claims 1
- 125000004506 1,2,5-oxadiazolyl group Chemical group 0.000 claims 1
- 125000001781 1,3,4-oxadiazolyl group Chemical group 0.000 claims 1
- 125000004520 1,3,4-thiadiazolyl group Chemical group 0.000 claims 1
- 125000005955 1H-indazolyl group Chemical group 0.000 claims 1
- JKTCBAGSMQIFNL-UHFFFAOYSA-N 2,3-dihydrofuran Chemical compound C1CC=CO1 JKTCBAGSMQIFNL-UHFFFAOYSA-N 0.000 claims 1
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000005915 C6-C14 aryl group Chemical group 0.000 claims 1
- NQPDZGIKBAWPEJ-UHFFFAOYSA-N Valeric acid Natural products CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 125000000641 acridinyl group Chemical group C1(=CC=CC2=NC3=CC=CC=C3C=C12)* 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 125000002785 azepinyl group Chemical group 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 125000004069 aziridinyl group Chemical group 0.000 claims 1
- 125000004604 benzisothiazolyl group Chemical group S1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000000609 carbazolyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3NC12)* 0.000 claims 1
- 125000004623 carbolinyl group Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000003016 chromanyl group Chemical group O1C(CCC2=CC=CC=C12)* 0.000 claims 1
- 125000004230 chromenyl group Chemical group O1C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims 1
- UKJLNMAFNRKWGR-UHFFFAOYSA-N cyclohexatrienamine Chemical group NC1=CC=C=C[CH]1 UKJLNMAFNRKWGR-UHFFFAOYSA-N 0.000 claims 1
- 125000004856 decahydroquinolinyl group Chemical group N1(CCCC2CCCCC12)* 0.000 claims 1
- 125000005509 dibenzothiophenyl group Chemical group 0.000 claims 1
- 125000004852 dihydrofuranyl group Chemical group O1C(CC=C1)* 0.000 claims 1
- 125000000532 dioxanyl group Chemical group 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000003838 furazanyl group Chemical group 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000002632 imidazolidinyl group Chemical group 0.000 claims 1
- 125000002636 imidazolinyl group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 1
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 125000001977 isobenzofuranyl group Chemical group C=1(OC=C2C=CC=CC12)* 0.000 claims 1
- 125000003384 isochromanyl group Chemical group C1(OCCC2=CC=CC=C12)* 0.000 claims 1
- 125000005438 isoindazolyl group Chemical group 0.000 claims 1
- 125000004594 isoindolinyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 claims 1
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 125000004628 isothiazolidinyl group Chemical group S1N(CCC1)* 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000003965 isoxazolidinyl group Chemical group 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 1
- 125000004930 octahydroisoquinolinyl group Chemical group C1(NCCC2CCCC=C12)* 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229940127557 pharmaceutical product Drugs 0.000 claims 1
- 125000004934 phenanthridinyl group Chemical group C1(=CC=CC2=NC=C3C=CC=CC3=C12)* 0.000 claims 1
- 125000004625 phenanthrolinyl group Chemical group N1=C(C=CC2=CC=C3C=CC=NC3=C12)* 0.000 claims 1
- 125000001791 phenazinyl group Chemical group C1(=CC=CC2=NC3=CC=CC=C3N=C12)* 0.000 claims 1
- 125000001484 phenothiazinyl group Chemical group C1(=CC=CC=2SC3=CC=CC=C3NC12)* 0.000 claims 1
- 125000004932 phenoxathinyl group Chemical group 0.000 claims 1
- 125000001644 phenoxazinyl group Chemical group C1(=CC=CC=2OC3=CC=CC=C3NC12)* 0.000 claims 1
- UYWQUFXKFGHYNT-UHFFFAOYSA-N phenylmethyl ester of formic acid Natural products O=COCC1=CC=CC=C1 UYWQUFXKFGHYNT-UHFFFAOYSA-N 0.000 claims 1
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 125000001042 pteridinyl group Chemical group N1=C(N=CC2=NC=CN=C12)* 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000001422 pyrrolinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims 1
- 125000004853 tetrahydropyridinyl group Chemical group N1(CCCC=C1)* 0.000 claims 1
- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- DBDCNCCRPKTRSD-UHFFFAOYSA-N thieno[3,2-b]pyridine Chemical compound C1=CC=C2SC=CC2=N1 DBDCNCCRPKTRSD-UHFFFAOYSA-N 0.000 claims 1
- 229940125670 thienopyridine Drugs 0.000 claims 1
- 239000002175 thienopyridine Substances 0.000 claims 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
- 125000001834 xanthenyl group Chemical group C1=CC=CC=2OC3=CC=CC=C3C(C12)* 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102006057413 | 2006-12-06 | ||
| DE102006057413.3 | 2006-12-06 | ||
| PCT/EP2007/010101 WO2008067909A2 (de) | 2006-12-06 | 2007-11-22 | Harnstoff- und sulfamidderivate als inhibitoren von tafia |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010511641A JP2010511641A (ja) | 2010-04-15 |
| JP2010511641A5 true JP2010511641A5 (cg-RX-API-DMAC7.html) | 2010-12-16 |
| JP5396279B2 JP5396279B2 (ja) | 2014-01-22 |
Family
ID=39384480
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009539631A Expired - Fee Related JP5396279B2 (ja) | 2006-12-06 | 2007-11-22 | ＴＡＦＩａ阻害剤としての尿素及びスルファミド誘導体 |
Country Status (27)
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2494390T3 (es) | 2008-06-06 | 2014-09-15 | Sanofi | Derivados macrocíclicos de urea y de sulfamida como inhibidores de TAFIa |
| AU2009263076B2 (en) | 2008-06-23 | 2012-07-26 | Astrazeneca Ab | New heterocyclic carboxamides for use as thrombin inhibitors |
| US8354444B2 (en) | 2008-09-18 | 2013-01-15 | Hoffmann-La Roche Inc. | Substituted pyrrolidine-2-carboxamides |
| AU2009310841A1 (en) * | 2008-10-29 | 2010-05-06 | Taisho Pharmaceutical Co., Ltd. | Compounds having TAFIa inhibitory activity |
| EP3027611B1 (en) * | 2013-06-10 | 2017-07-26 | Sanofi | Macrocyclic urea derivatives as inhibitors of tafi a, their preparation and their use as pharmaceuticals |
| CN104529859B (zh) * | 2015-01-13 | 2016-08-17 | 佛山市赛维斯医药科技有限公司 | 含苯胺和二烯氟代金刚烷结构的化合物、其制备方法和用途 |
| RU2687254C1 (ru) * | 2018-10-03 | 2019-05-08 | Федеральное государственное бюджетное учреждение науки Новосибирский институт органической химии им. Н.Н. Ворожцова Сибирского отделения Российской академии наук (НИОХ СО РАН) | N-гетероциклические производные борниламина в качестве ингибиторов ортопоксвирусов |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU667995B2 (en) * | 1993-02-15 | 1996-04-18 | Bayer Aktiengesellschaft | New pseudopeptides having an antiviral action |
| TW394760B (en) * | 1993-09-07 | 2000-06-21 | Hoffmann La Roche | Novel Carboxamides, process for their preparation and pharmaceutical composition containing the same |
| CA2298601A1 (en) * | 1997-08-28 | 1999-03-11 | Pharmacia & Upjohn Company | Inhibitors of protein tyrosine phosphatase |
| US6482921B1 (en) * | 1999-01-28 | 2002-11-19 | Essential Therapeutics, Inc. | Uridyl peptide antibiotic (UPA) derivatives, their synthesis and use |
| WO2000056725A1 (en) * | 1999-03-19 | 2000-09-28 | Du Pont Pharmaceuticals Company | N-adamant-1-yl-n'-[4-chlorobenzothiazol-2-yl] urea useful in the treatment of inflammation and as an anticancer radiosensitizing agent |
| US6359129B1 (en) * | 2000-08-15 | 2002-03-19 | University Of Kansas | Amino acid-derived, 7-membered cyclic sulfamides and methods of synthesizing the same |
| ATE447557T1 (de) * | 2000-08-17 | 2009-11-15 | Pfizer Ltd | Substitutuierte imidazole als tafia inhibitoren |
| DE102004020186A1 (de) * | 2004-04-22 | 2005-11-17 | Aventis Pharma Deutschland Gmbh | Heterocyclylessigsäuren als Inhibitoren von TAFla |
| CA2583089A1 (en) * | 2004-10-05 | 2006-04-20 | Bayer Schering Pharma Aktiengesellschaft | Tafi inhibitors and their use to treat pulmonary fibrosis |
-
2007
- 2007-11-22 AU AU2007327959A patent/AU2007327959B2/en not_active Ceased
- 2007-11-22 ES ES07856207.1T patent/ES2537093T3/es active Active
- 2007-11-22 WO PCT/EP2007/010101 patent/WO2008067909A2/de not_active Ceased
- 2007-11-22 CN CN2007800435586A patent/CN101553219B/zh not_active Expired - Fee Related
- 2007-11-22 JP JP2009539631A patent/JP5396279B2/ja not_active Expired - Fee Related
- 2007-11-22 RU RU2009125534/15A patent/RU2459619C2/ru not_active IP Right Cessation
- 2007-11-22 SI SI200731653T patent/SI2104497T1/sl unknown
- 2007-11-22 EP EP07856207.1A patent/EP2104497B1/de active Active
- 2007-11-22 NZ NZ577312A patent/NZ577312A/en not_active IP Right Cessation
- 2007-11-22 CA CA2671861A patent/CA2671861C/en not_active Expired - Fee Related
- 2007-11-22 PL PL07856207T patent/PL2104497T3/pl unknown
- 2007-11-22 DK DK07856207.1T patent/DK2104497T3/en active
- 2007-11-22 HR HRP20150514TT patent/HRP20150514T1/hr unknown
- 2007-11-22 PT PT78562071T patent/PT2104497E/pt unknown
- 2007-11-22 MX MX2009005516A patent/MX2009005516A/es active IP Right Grant
- 2007-11-22 KR KR1020097011740A patent/KR20090087044A/ko not_active Abandoned
- 2007-11-22 BR BRPI0720241-5A patent/BRPI0720241A2/pt not_active IP Right Cessation
- 2007-12-04 CL CL200703494A patent/CL2007003494A1/es unknown
- 2007-12-04 AR ARP070105408A patent/AR064119A1/es unknown
- 2007-12-04 PE PE2007001712A patent/PE20081349A1/es not_active Application Discontinuation
- 2007-12-04 TW TW096145997A patent/TWI399203B/zh not_active IP Right Cessation
-
2009
- 2009-05-04 ZA ZA2009/03040A patent/ZA200903040B/en unknown
- 2009-06-03 CO CO09057335A patent/CO6180422A2/es active IP Right Grant
- 2009-06-03 MA MA31948A patent/MA30968B1/fr unknown
- 2009-06-08 US US12/480,348 patent/US8389764B2/en not_active Expired - Fee Related
- 2009-06-10 NO NO20092246A patent/NO20092246L/no not_active Application Discontinuation
-
2015
- 2015-05-15 CY CY20151100436T patent/CY1116384T1/el unknown
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