ZA200503811B - Method of treatment of transplant rejection - Google Patents
Method of treatment of transplant rejection Download PDFInfo
- Publication number
- ZA200503811B ZA200503811B ZA200503811A ZA200503811A ZA200503811B ZA 200503811 B ZA200503811 B ZA 200503811B ZA 200503811 A ZA200503811 A ZA 200503811A ZA 200503811 A ZA200503811 A ZA 200503811A ZA 200503811 B ZA200503811 B ZA 200503811B
- Authority
- ZA
- South Africa
- Prior art keywords
- alkyl
- amino
- alkoxy
- methyl
- alkylamino
- Prior art date
Links
- 206010052779 Transplant rejections Diseases 0.000 title claims description 10
- 238000000034 method Methods 0.000 title description 44
- 125000000217 alkyl group Chemical group 0.000 claims description 331
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 104
- 150000001875 compounds Chemical class 0.000 claims description 92
- -1 hydroxy, amino Chemical group 0.000 claims description 89
- 125000003545 alkoxy group Chemical group 0.000 claims description 73
- 125000003282 alkyl amino group Chemical group 0.000 claims description 71
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 67
- 229910052684 Cerium Inorganic materials 0.000 claims description 66
- 125000004442 acylamino group Chemical group 0.000 claims description 60
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 56
- 125000002252 acyl group Chemical group 0.000 claims description 52
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 52
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical group [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 37
- 229910052805 deuterium Inorganic materials 0.000 claims description 37
- 125000003342 alkenyl group Chemical group 0.000 claims description 35
- 125000000304 alkynyl group Chemical group 0.000 claims description 35
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 35
- 229910052739 hydrogen Inorganic materials 0.000 claims description 35
- 239000001257 hydrogen Substances 0.000 claims description 35
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 33
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 31
- 150000003839 salts Chemical class 0.000 claims description 31
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 30
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 30
- 125000003118 aryl group Chemical group 0.000 claims description 29
- 125000004423 acyloxy group Chemical group 0.000 claims description 27
- 229910052792 caesium Inorganic materials 0.000 claims description 27
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 26
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims description 22
- 125000001072 heteroaryl group Chemical group 0.000 claims description 20
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 claims description 19
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 15
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 13
- 239000002253 acid Substances 0.000 claims description 11
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims description 11
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims description 9
- 241000124008 Mammalia Species 0.000 claims description 9
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 9
- 239000001301 oxygen Substances 0.000 claims description 9
- 229910052760 oxygen Inorganic materials 0.000 claims description 9
- 229910052799 carbon Inorganic materials 0.000 claims description 8
- 150000002431 hydrogen Chemical class 0.000 claims description 8
- 125000004657 aryl sulfonyl amino group Chemical group 0.000 claims description 7
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- 210000000056 organ Anatomy 0.000 claims description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 claims description 6
- 125000004043 oxo group Chemical group O=* 0.000 claims description 6
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 3
- MTRMACOHLXKTOY-PWSUYJOCSA-N 3,3,3-trifluoro-1-[(3r,4r)-4-methyl-3-[methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]propan-1-one Chemical compound C[C@@H]1CCN(C(=O)CC(F)(F)F)C[C@@H]1N(C)C1=NC=NC2=C1C=CN2 MTRMACOHLXKTOY-PWSUYJOCSA-N 0.000 claims description 2
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- KLCACFBGIDQWHE-UHFFFAOYSA-N 1-[3-[(5-chloro-7h-pyrrolo[2,3-d]pyrimidin-4-yl)methylamino]-4-methylpiperidin-1-yl]propan-1-one Chemical compound C1N(C(=O)CC)CCC(C)C1NCC1=NC=NC2=C1C(Cl)=CN2 KLCACFBGIDQWHE-UHFFFAOYSA-N 0.000 claims 1
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Classifications
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42978402P | 2002-11-26 | 2002-11-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200503811B true ZA200503811B (en) | 2006-07-26 |
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| US (1) | US7250420B2 (zh) |
| EP (1) | EP1572213A1 (zh) |
| JP (1) | JP2006509000A (zh) |
| KR (1) | KR20050086784A (zh) |
| CN (1) | CN1717236A (zh) |
| AU (1) | AU2003276591A1 (zh) |
| BR (1) | BR0316487A (zh) |
| CA (1) | CA2507392A1 (zh) |
| MX (1) | MXPA05005576A (zh) |
| MY (1) | MY137250A (zh) |
| NZ (1) | NZ539901A (zh) |
| PL (1) | PL378246A1 (zh) |
| TW (1) | TW200418482A (zh) |
| WO (1) | WO2004047843A1 (zh) |
| ZA (1) | ZA200503811B (zh) |
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-
2003
- 2003-11-17 EP EP03811831A patent/EP1572213A1/en not_active Withdrawn
- 2003-11-17 CA CA002507392A patent/CA2507392A1/en not_active Abandoned
- 2003-11-17 KR KR1020057009377A patent/KR20050086784A/ko not_active Application Discontinuation
- 2003-11-17 JP JP2004554807A patent/JP2006509000A/ja not_active Withdrawn
- 2003-11-17 CN CNA2003801042374A patent/CN1717236A/zh active Pending
- 2003-11-17 MX MXPA05005576A patent/MXPA05005576A/es unknown
- 2003-11-17 AU AU2003276591A patent/AU2003276591A1/en not_active Abandoned
- 2003-11-17 NZ NZ539901A patent/NZ539901A/en unknown
- 2003-11-17 PL PL378246A patent/PL378246A1/pl not_active Application Discontinuation
- 2003-11-17 WO PCT/IB2003/005229 patent/WO2004047843A1/en not_active Application Discontinuation
- 2003-11-17 BR BR0316487-0A patent/BR0316487A/pt not_active IP Right Cessation
- 2003-11-20 TW TW092132613A patent/TW200418482A/zh unknown
- 2003-11-21 MY MYPI20034496A patent/MY137250A/en unknown
- 2003-11-24 US US10/720,600 patent/US7250420B2/en not_active Expired - Fee Related
-
2005
- 2005-05-11 ZA ZA200503811A patent/ZA200503811B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2006509000A (ja) | 2006-03-16 |
| CN1717236A (zh) | 2006-01-04 |
| MY137250A (en) | 2009-01-30 |
| US7250420B2 (en) | 2007-07-31 |
| AU2003276591A1 (en) | 2004-06-18 |
| TW200418482A (en) | 2004-10-01 |
| EP1572213A1 (en) | 2005-09-14 |
| PL378246A1 (pl) | 2006-03-20 |
| US20040116449A1 (en) | 2004-06-17 |
| BR0316487A (pt) | 2005-10-11 |
| NZ539901A (en) | 2007-09-28 |
| WO2004047843A1 (en) | 2004-06-10 |
| KR20050086784A (ko) | 2005-08-30 |
| CA2507392A1 (en) | 2004-06-10 |
| MXPA05005576A (es) | 2005-07-27 |
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