HRP950034A2 - Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family - Google Patents
Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family Download PDFInfo
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- HRP950034A2 HRP950034A2 HR08/358,351A HRP950034A HRP950034A2 HR P950034 A2 HRP950034 A2 HR P950034A2 HR P950034 A HRP950034 A HR P950034A HR P950034 A2 HRP950034 A2 HR P950034A2
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- 102000001301 EGF receptor Human genes 0.000 title claims description 25
- 108060006698 EGF receptor Proteins 0.000 title claims description 23
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 title claims description 12
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 title claims description 12
- 230000002401 inhibitory effect Effects 0.000 title claims description 7
- 125000002619 bicyclic group Chemical group 0.000 title 1
- 125000004432 carbon atom Chemical group C* 0.000 claims description 618
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 309
- -1 -O-C(O)-R) Chemical group 0.000 claims description 271
- 229910052757 nitrogen Inorganic materials 0.000 claims description 209
- 125000003118 aryl group Chemical group 0.000 claims description 185
- 125000000217 alkyl group Chemical group 0.000 claims description 175
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 172
- 239000000203 mixture Substances 0.000 claims description 137
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 119
- 229910052799 carbon Inorganic materials 0.000 claims description 116
- 125000003545 alkoxy group Chemical group 0.000 claims description 98
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 98
- 238000000034 method Methods 0.000 claims description 98
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 98
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 90
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 72
- 150000001875 compounds Chemical class 0.000 claims description 54
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 52
- 238000002360 preparation method Methods 0.000 claims description 48
- 229910052717 sulfur Inorganic materials 0.000 claims description 45
- 125000001424 substituent group Chemical group 0.000 claims description 43
- OAKJQQAXSVQMHS-UHFFFAOYSA-N hydrazine group Chemical group NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims description 40
- 101800003838 Epidermal growth factor Proteins 0.000 claims description 38
- 229940116977 epidermal growth factor Drugs 0.000 claims description 38
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
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- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
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US08/358,351 US5654307A (en) | 1994-01-25 | 1994-12-23 | Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family |
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US (5) | US6084095A (no) |
EP (1) | EP0742717A1 (no) |
JP (1) | JPH09508127A (no) |
CN (2) | CN1493291A (no) |
AU (1) | AU686334B2 (no) |
BG (1) | BG63245B1 (no) |
CA (1) | CA2177372A1 (no) |
CZ (1) | CZ197096A3 (no) |
FI (3) | FI114213B (no) |
GE (1) | GEP20012376B (no) |
HR (1) | HRP950034A2 (no) |
HU (1) | HU221741B1 (no) |
IL (1) | IL112249A (no) |
MD (1) | MD1632G2 (no) |
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NZ (1) | NZ281011A (no) |
PL (1) | PL179132B1 (no) |
RO (1) | RO117257B1 (no) |
SK (1) | SK89496A3 (no) |
TJ (1) | TJ381B (no) |
WO (1) | WO1995019774A1 (no) |
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- 1995-01-23 AU AU17314/95A patent/AU686334B2/en not_active Ceased
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- 1995-01-23 EP EP95909316A patent/EP0742717A1/en not_active Withdrawn
- 1995-01-23 JP JP7519732A patent/JPH09508127A/ja not_active Ceased
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