JP2011510078A5 - - Google Patents
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- Publication number
- JP2011510078A5 JP2011510078A5 JP2010544354A JP2010544354A JP2011510078A5 JP 2011510078 A5 JP2011510078 A5 JP 2011510078A5 JP 2010544354 A JP2010544354 A JP 2010544354A JP 2010544354 A JP2010544354 A JP 2010544354A JP 2011510078 A5 JP2011510078 A5 JP 2011510078A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- moiety
- hydrogen
- formula
- group
- 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
- 229910052739 hydrogen Inorganic materials 0.000 claims description 62
- 239000001257 hydrogen Substances 0.000 claims description 62
- 150000001875 compounds Chemical class 0.000 claims description 52
- 125000004432 carbon atom Chemical group C* 0.000 claims description 46
- 125000000217 alkyl group Chemical group 0.000 claims description 35
- 150000002431 hydrogen Chemical class 0.000 claims description 32
- 239000003446 ligand Substances 0.000 claims description 32
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 30
- -1 4-methyl-piperazinyl Chemical group 0.000 claims description 30
- 229910052799 carbon Inorganic materials 0.000 claims description 30
- 125000002252 acyl group Chemical group 0.000 claims description 28
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 26
- 229910052736 halogen Inorganic materials 0.000 claims description 24
- 150000002367 halogens Chemical group 0.000 claims description 24
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 24
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 22
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims description 18
- 125000004429 atom Chemical group 0.000 claims description 18
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 18
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 16
- 125000001424 substituent group Chemical group 0.000 claims description 16
- 125000003118 aryl group Chemical group 0.000 claims description 14
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 13
- 239000011737 fluorine Substances 0.000 claims description 13
- 229910052731 fluorine Inorganic materials 0.000 claims description 13
- 125000003545 alkoxy group Chemical group 0.000 claims description 12
- 229910052757 nitrogen Inorganic materials 0.000 claims description 10
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 8
- 239000004721 Polyphenylene oxide Chemical group 0.000 claims description 8
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims description 8
- 125000005907 alkyl ester group Chemical group 0.000 claims description 8
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims description 8
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 8
- 150000003857 carboxamides Chemical class 0.000 claims description 8
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims description 8
- 239000000539 dimer Substances 0.000 claims description 8
- 125000002541 furyl group Chemical group 0.000 claims description 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 8
- 150000002825 nitriles Chemical class 0.000 claims description 8
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 8
- 125000003386 piperidinyl group Chemical group 0.000 claims description 8
- 229920000570 polyether Chemical group 0.000 claims description 8
- 125000004076 pyridyl group Chemical group 0.000 claims description 8
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 8
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 8
- 229940124530 sulfonamide Drugs 0.000 claims description 8
- 150000003456 sulfonamides Chemical class 0.000 claims description 8
- 150000003457 sulfones Chemical class 0.000 claims description 8
- 150000003462 sulfoxides Chemical class 0.000 claims description 8
- 125000000335 thiazolyl group Chemical group 0.000 claims description 8
- 125000001544 thienyl group Chemical group 0.000 claims description 8
- 150000003568 thioethers Chemical class 0.000 claims description 8
- PNLQPWWBHXMFCA-UHFFFAOYSA-N 2-chloroprop-1-ene Chemical compound CC(Cl)=C PNLQPWWBHXMFCA-UHFFFAOYSA-N 0.000 claims description 6
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims description 6
- 125000005097 aminocarbonylalkyl group Chemical group 0.000 claims description 6
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 6
- 229920000233 poly(alkylene oxides) Polymers 0.000 claims description 6
- 125000006850 spacer group Chemical group 0.000 claims description 6
- 125000005864 sulfonamidyl group Chemical group 0.000 claims description 6
- 239000000203 mixture Substances 0.000 claims description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 5
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims description 4
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 4
- 239000000178 monomer Substances 0.000 claims description 4
- 238000000034 method Methods 0.000 claims description 3
- STFJMSUXVNOEQX-UHFFFAOYSA-N 4-[(4-benzylpiperazin-1-yl)-(3-hydroxyphenyl)methyl]-n,n-diethylbenzamide Chemical compound C1=CC(C(=O)N(CC)CC)=CC=C1C(C=1C=C(O)C=CC=1)N1CCN(CC=2C=CC=CC=2)CC1 STFJMSUXVNOEQX-UHFFFAOYSA-N 0.000 claims description 2
- LBLDMHBSVIVJPM-YZIHRLCOSA-N 4-[(R)-[(2S,5R)-2,5-dimethyl-4-prop-2-enyl-1-piperazinyl]-(3-hydroxyphenyl)methyl]-N,N-diethylbenzamide Chemical compound C1=CC(C(=O)N(CC)CC)=CC=C1[C@H](C=1C=C(O)C=CC=1)N1[C@@H](C)CN(CC=C)[C@H](C)C1 LBLDMHBSVIVJPM-YZIHRLCOSA-N 0.000 claims description 2
- PNOKAHOIMXUBTH-STSQHVNTSA-N 4-[(s)-[(2s,5r)-2,5-dimethylpiperazin-1-yl]-(3-hydroxyphenyl)methyl]-n,n-diethylbenzamide Chemical compound C1=CC(C(=O)N(CC)CC)=CC=C1[C@@H](C=1C=C(O)C=CC=1)N1[C@@H](C)CN[C@H](C)C1 PNOKAHOIMXUBTH-STSQHVNTSA-N 0.000 claims description 2
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 2
- 230000008878 coupling Effects 0.000 claims description 2
- 238000010168 coupling process Methods 0.000 claims description 2
- 238000005859 coupling reaction Methods 0.000 claims description 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N diethylenediamine Natural products C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims description 2
- 239000002552 dosage form Substances 0.000 claims description 2
- 150000002148 esters Chemical class 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 150000002222 fluorine compounds Chemical class 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 description 6
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 description 4
- 125000000000 cycloalkoxy group Chemical group 0.000 description 4
- 125000002768 hydroxyalkyl group Chemical group 0.000 description 4
- 125000004183 alkoxy alkyl group Chemical group 0.000 description 3
- 125000004966 cyanoalkyl group Chemical group 0.000 description 3
- 238000002560 therapeutic procedure Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US6233008P | 2008-01-25 | 2008-01-25 | |
| US61/062,330 | 2008-01-25 | ||
| PCT/US2009/000475 WO2009094209A1 (en) | 2008-01-25 | 2009-01-22 | Oligomer-diarylpiperazine conjugates |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011510078A JP2011510078A (ja) | 2011-03-31 |
| JP2011510078A5 true JP2011510078A5 (https=) | 2012-12-27 |
| JP5693967B2 JP5693967B2 (ja) | 2015-04-01 |
Family
ID=40589565
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010544354A Expired - Fee Related JP5693967B2 (ja) | 2008-01-25 | 2009-01-22 | オリゴマー−ジアリールピペラジンコンジュゲート |
Country Status (4)
| Country | Link |
|---|---|
| US (3) | US8685979B2 (https=) |
| EP (1) | EP2249872B1 (https=) |
| JP (1) | JP5693967B2 (https=) |
| WO (1) | WO2009094209A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10512644B2 (en) | 2007-03-12 | 2019-12-24 | Inheris Pharmaceuticals, Inc. | Oligomer-opioid agonist conjugates |
| US8173666B2 (en) | 2007-03-12 | 2012-05-08 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
| WO2009058387A2 (en) | 2007-11-02 | 2009-05-07 | Nektar Therapeutics Al, Corporation | Oligomer-nitroimidazole anti-infective conjugates |
| US8685979B2 (en) | 2008-01-25 | 2014-04-01 | Nektar Therapeutics | Oligomer-diarylpiperazine conjugates |
| KR101660996B1 (ko) * | 2008-09-16 | 2016-09-28 | 넥타르 테라퓨틱스 | 남용에 대한 낮은 잠재성을 갖는 페길화 오피오이드 |
| US20130023553A1 (en) * | 2010-01-12 | 2013-01-24 | Nektar Therapeutics | Pegylated opioids with low potential for abuse and side effects |
| US9226970B2 (en) | 2010-02-22 | 2016-01-05 | Nektar Therapeutics | Oligomer modified diaromatic substituted compounds |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB817231A (en) | 1956-01-27 | 1959-07-29 | Henri Morren | New derivatives of n-mono-benzhydryl-piperazine and process for the preparation thereof |
| US5574159A (en) * | 1992-02-03 | 1996-11-12 | Delta Pharmaceuticals, Inc. | Opioid compounds and methods for making therefor |
| GB9202238D0 (en) * | 1992-02-03 | 1992-03-18 | Wellcome Found | Compounds |
| US5672662A (en) | 1995-07-07 | 1997-09-30 | Shearwater Polymers, Inc. | Poly(ethylene glycol) and related polymers monosubstituted with propionic or butanoic acids and functional derivatives thereof for biotechnical applications |
| US6835802B2 (en) | 2001-06-04 | 2004-12-28 | Nobex Corporation | Methods of synthesizing substantially monodispersed mixtures of polymers having polyethylene glycol moieties |
| EP2905033B1 (en) * | 2003-12-16 | 2020-09-02 | Nektar Therapeutics | Monodisperse PEGylated naloxol compositions |
| JP2010521465A (ja) * | 2007-03-12 | 2010-06-24 | ネクター セラピューティックス | 複合体のデノボ合成 |
| KR101561707B1 (ko) | 2007-03-12 | 2015-10-19 | 넥타르 테라퓨틱스 | 올리고머―항히스타민제 컨주게이트 |
| US8173666B2 (en) * | 2007-03-12 | 2012-05-08 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
| US8685979B2 (en) | 2008-01-25 | 2014-04-01 | Nektar Therapeutics | Oligomer-diarylpiperazine conjugates |
-
2009
- 2009-01-22 US US12/864,481 patent/US8685979B2/en active Active
- 2009-01-22 WO PCT/US2009/000475 patent/WO2009094209A1/en not_active Ceased
- 2009-01-22 EP EP09704271.7A patent/EP2249872B1/en active Active
- 2009-01-22 JP JP2010544354A patent/JP5693967B2/ja not_active Expired - Fee Related
-
2014
- 2014-02-07 US US14/175,410 patent/US9061026B2/en not_active Expired - Fee Related
-
2015
- 2015-06-03 US US14/729,578 patent/US9314463B2/en not_active Expired - Fee Related
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