MX2010008697A - Tratamiento de enfermedades de la vejiga con un activador de tlr7. - Google Patents
Tratamiento de enfermedades de la vejiga con un activador de tlr7.Info
- Publication number
- MX2010008697A MX2010008697A MX2010008697A MX2010008697A MX2010008697A MX 2010008697 A MX2010008697 A MX 2010008697A MX 2010008697 A MX2010008697 A MX 2010008697A MX 2010008697 A MX2010008697 A MX 2010008697A MX 2010008697 A MX2010008697 A MX 2010008697A
- Authority
- MX
- Mexico
- Prior art keywords
- carbon atoms
- alkyl
- substituted
- group
- acid
- Prior art date
Links
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- -1 imidazoquinolinamine compound Chemical class 0.000 claims description 120
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- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 100
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- 150000001875 compounds Chemical class 0.000 claims description 62
- 125000001424 substituent group Chemical group 0.000 claims description 54
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- 239000000203 mixture Substances 0.000 claims description 48
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- 125000000623 heterocyclic group Chemical group 0.000 claims description 32
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- DOUYETYNHWVLEO-UHFFFAOYSA-N imiquimod Chemical compound C1=CC=CC2=C3N(CC(C)C)C=NC3=C(N)N=C21 DOUYETYNHWVLEO-UHFFFAOYSA-N 0.000 claims description 18
- 229960002751 imiquimod Drugs 0.000 claims description 17
- 125000003107 substituted aryl group Chemical group 0.000 claims description 17
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- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims description 7
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims description 7
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims description 7
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 7
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- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims description 7
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 7
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- BXNMTOQRYBFHNZ-UHFFFAOYSA-N resiquimod Chemical compound C1=CC=CC2=C(N(C(COCC)=N3)CC(C)(C)O)C3=C(N)N=C21 BXNMTOQRYBFHNZ-UHFFFAOYSA-N 0.000 claims description 7
- 229910052701 rubidium Inorganic materials 0.000 claims description 7
- 239000004094 surface-active agent Substances 0.000 claims description 7
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 7
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- 229910052760 oxygen Inorganic materials 0.000 claims description 5
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 4
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- 125000004429 atom Chemical group 0.000 claims description 4
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- HVBSAKJJOYLTQU-UHFFFAOYSA-N 4-aminobenzenesulfonic acid Chemical compound NC1=CC=C(S(O)(=O)=O)C=C1 HVBSAKJJOYLTQU-UHFFFAOYSA-N 0.000 claims 6
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- 230000000699 topical effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- FGMPLJWBKKVCDB-UHFFFAOYSA-N trans-L-hydroxy-proline Natural products ON1CCCC1C(O)=O FGMPLJWBKKVCDB-UHFFFAOYSA-N 0.000 description 1
- 229960002622 triacetin Drugs 0.000 description 1
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical group [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 description 1
- 201000008827 tuberculosis Diseases 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 230000005909 tumor killing Effects 0.000 description 1
- 230000003827 upregulation Effects 0.000 description 1
- 210000003708 urethra Anatomy 0.000 description 1
- 210000003741 urothelium Anatomy 0.000 description 1
- 238000001291 vacuum drying Methods 0.000 description 1
- 125000003774 valeryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0034—Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Urology & Nephrology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Gynecology & Obstetrics (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US2699908P | 2008-02-07 | 2008-02-07 | |
| PCT/US2009/000771 WO2009099650A2 (en) | 2008-02-07 | 2009-02-06 | Treatment of bladder diseases with a tlr7 activator |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2010008697A true MX2010008697A (es) | 2010-12-07 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2010008697A MX2010008697A (es) | 2008-02-07 | 2009-02-06 | Tratamiento de enfermedades de la vejiga con un activador de tlr7. |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20090202626A1 (enExample) |
| EP (1) | EP2259788A4 (enExample) |
| JP (2) | JP2011511073A (enExample) |
| KR (1) | KR20100137449A (enExample) |
| CN (1) | CN102088974A (enExample) |
| AU (1) | AU2009210655B2 (enExample) |
| BR (1) | BRPI0907907A2 (enExample) |
| CA (1) | CA2713438A1 (enExample) |
| EA (1) | EA201001264A1 (enExample) |
| IL (1) | IL207246A0 (enExample) |
| MX (1) | MX2010008697A (enExample) |
| WO (1) | WO2009099650A2 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12295950B2 (en) | 2017-06-23 | 2025-05-13 | Birdie Biopharmaceuticals, Inc. | Pharmaceutical compositions |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2577514T3 (es) | 2005-08-22 | 2016-07-15 | The Regents Of The University Of California | Antagonistas de TLR |
| WO2007142755A2 (en) | 2006-05-31 | 2007-12-13 | The Regents Of The University Of California | Purine analogs |
| EA019151B1 (ru) | 2007-02-07 | 2014-01-30 | Дзе Регентс Оф Дзе Юниверсити Оф Калифорния | Конъюгаты синтетических агонистов tlr и их применение |
| WO2010020590A1 (en) * | 2008-08-20 | 2010-02-25 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for predicting the response to anti-cancer treatment with an agonist of tlr7 or an agonist of tlr8 |
| WO2010088924A1 (en) * | 2009-02-06 | 2010-08-12 | Telormedix Sa | Pharmaceutical compositions comprising imidazoquinolin(amines) and derivatives thereof suitable for local administration |
| KR20110117705A (ko) | 2009-02-11 | 2011-10-27 | 더 리전트 오브 더 유니버시티 오브 캘리포니아 | 톨-유사 수용체 조정제 및 질병의 치료 |
| WO2012038058A1 (en) | 2010-09-21 | 2012-03-29 | Telormedix Sa | Treatment of conditions by toll-like receptor modulators |
| KR101250419B1 (ko) | 2010-12-16 | 2013-04-05 | 강원대학교산학협력단 | Tlr 작동제를 포함하는 유방암 방사선 치료 보조제 |
| EA027792B1 (ru) | 2011-04-08 | 2017-09-29 | Янссен Сайенсиз Айрлэнд Юси | Производные пиримидина для лечения вирусных инфекций |
| CN104066733A (zh) | 2011-11-09 | 2014-09-24 | 爱尔兰詹森研发公司 | 用于治疗病毒感染的嘌呤衍生物 |
| EA033907B1 (ru) * | 2012-02-08 | 2019-12-09 | Янссен Сайенсиз Айрленд Юси | Производные пиперидино-пиримидина, фармацевтическая композиция и их применение |
| SG11201408542VA (en) | 2012-07-13 | 2015-02-27 | Janssen Sciences Ireland Uc | Macrocyclic purines for the treatment of viral infections |
| CN103566377A (zh) | 2012-07-18 | 2014-02-12 | 上海博笛生物科技有限公司 | 癌症的靶向免疫治疗 |
| KR102280595B1 (ko) | 2012-10-10 | 2021-07-22 | 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 | 바이러스 감염 및 다른 질환 치료를 위한 피롤로[3,2-d]피리미딘 유도체 |
| CN105051018B (zh) | 2012-11-16 | 2019-09-20 | 爱尔兰詹森科学公司 | 用于治疗病毒性感染的杂环的经取代的2-氨基-喹唑啉衍生物 |
| CN105189468B (zh) | 2013-02-21 | 2018-10-30 | 爱尔兰詹森科学公司 | 用于治疗病毒性感染的2-氨基嘧啶衍生物 |
| MX366481B (es) | 2013-03-29 | 2019-07-09 | Janssen Sciences Ireland Uc | Deaza-purinonas macrociclicas para el tratamiento de infecciones virales. |
| DK3004074T3 (da) | 2013-05-24 | 2018-01-29 | Janssen Sciences Ireland Uc | Pyridonderivater til behandling af virusinfektioner og yderligere sygdomme |
| NO3030563T3 (enExample) | 2013-06-27 | 2018-01-06 | ||
| MX368625B (es) | 2013-07-30 | 2019-10-08 | Janssen Sciences Ireland Uc | Derivados de tieno[3,2-d]pirimidinas para el tratamiento de infecciones virales. |
| WO2015104030A1 (en) * | 2014-01-10 | 2015-07-16 | Telormedix Sa | Pharmaceutical compositions comprising imiquimod for use in the treatment of carcinoma in situ of the bladder |
| CN105899537A (zh) | 2014-01-10 | 2016-08-24 | 博笛生物科技(北京)有限公司 | 靶向表达egfr的肿瘤的化合物和组合物 |
| EP3091978B1 (en) * | 2014-01-10 | 2021-08-18 | Urogen Pharma Ltd. | Pharmaceutical compositions comprising imiquimod for use in the treatment of carcinoma in situ of the bladder |
| EP4001311B1 (en) | 2014-07-09 | 2025-11-05 | Birdie Biopharmaceuticals Inc. | Anti-pd-l1/pd-1 combinations for treating tumors |
| CN112546238A (zh) | 2014-09-01 | 2021-03-26 | 博笛生物科技有限公司 | 用于治疗肿瘤的抗-pd-l1结合物 |
| KR101729236B1 (ko) * | 2015-06-01 | 2017-04-21 | (주)노터스생명과학 | Tlr7 항진제를 포함하는 비만 또는 간질환 예방 및 치료용 약학 조성물 |
| CN115350279A (zh) | 2016-01-07 | 2022-11-18 | 博笛生物科技有限公司 | 用于治疗肿瘤的抗-her2组合 |
| CN106943596A (zh) | 2016-01-07 | 2017-07-14 | 博笛生物科技(北京)有限公司 | 用于治疗肿瘤的抗-cd20组合 |
| CN106943597A (zh) | 2016-01-07 | 2017-07-14 | 博笛生物科技(北京)有限公司 | 用于治疗肿瘤的抗-egfr组合 |
| US11697851B2 (en) | 2016-05-24 | 2023-07-11 | The Regents Of The University Of California | Early ovarian cancer detection diagnostic test based on mRNA isoforms |
| CA3027471A1 (en) | 2016-07-01 | 2018-01-04 | Janssen Sciences Ireland Unlimited Company | Dihydropyranopyrimidines for the treatment of viral infections |
| CN109790154B (zh) | 2016-09-29 | 2023-06-23 | 爱尔兰詹森科学公司 | 用于治疗病毒感染和另外的疾病的嘧啶前药 |
| CN108794467A (zh) | 2017-04-27 | 2018-11-13 | 博笛生物科技有限公司 | 2-氨基-喹啉衍生物 |
| TW201945003A (zh) | 2018-03-01 | 2019-12-01 | 愛爾蘭商健生科學愛爾蘭無限公司 | 2,4-二胺基喹唑啉衍生物及其醫學用途 |
| CA3140207C (en) | 2019-06-13 | 2025-05-13 | Hollister Inc | REUSABLE URINARY CATHETER-TYPE PRODUCTS |
| WO2020263859A1 (en) | 2019-06-25 | 2020-12-30 | Hollister Incorporated | Reusable urinary catheter products |
| CN112778372B (zh) * | 2019-11-11 | 2025-09-23 | 苏州泽璟生物制药股份有限公司 | 咪唑并喹啉取代磷酸酯类激动剂及其制备方法和应用 |
Family Cites Families (68)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL73534A (en) * | 1983-11-18 | 1990-12-23 | Riker Laboratories Inc | 1h-imidazo(4,5-c)quinoline-4-amines,their preparation and pharmaceutical compositions containing certain such compounds |
| US4938949A (en) * | 1988-09-12 | 1990-07-03 | University Of New York | Treatment of damaged bone marrow and dosage units therefor |
| US5238944A (en) * | 1988-12-15 | 1993-08-24 | Riker Laboratories, Inc. | Topical formulations and transdermal delivery systems containing 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine |
| US5736553A (en) * | 1988-12-15 | 1998-04-07 | Riker Laboratories, Inc. | Topical formulations and transdermal delivery systems containing 1-isobutyl-1H-imidazo 4,5-C!quinolin-4-amine |
| US4929624A (en) * | 1989-03-23 | 1990-05-29 | Minnesota Mining And Manufacturing Company | Olefinic 1H-imidazo(4,5-c)quinolin-4-amines |
| US5037986A (en) * | 1989-03-23 | 1991-08-06 | Minnesota Mining And Manufacturing Company | Olefinic 1H-imidazo[4,5-c]quinolin-4-amines |
| NZ232740A (en) * | 1989-04-20 | 1992-06-25 | Riker Laboratories Inc | Solution for parenteral administration comprising a 1h-imidazo(4,5-c) quinolin-4-amine derivative, an acid and a tonicity adjuster |
| CA2093132C (en) * | 1990-10-05 | 2002-02-26 | John F. Gerster | Process for the preparation of imidazo[4,5-c]quinolin-4-amines |
| US5175296A (en) * | 1991-03-01 | 1992-12-29 | Minnesota Mining And Manufacturing Company | Imidazo[4,5-c]quinolin-4-amines and processes for their preparation |
| IL105325A (en) * | 1992-04-16 | 1996-11-14 | Minnesota Mining & Mfg | Immunogen/vaccine adjuvant composition |
| US5395937A (en) * | 1993-01-29 | 1995-03-07 | Minnesota Mining And Manufacturing Company | Process for preparing quinoline amines |
| US5648516A (en) * | 1994-07-20 | 1997-07-15 | Minnesota Mining And Manufacturing Company | Fused cycloalkylimidazopyridines |
| US5352784A (en) * | 1993-07-15 | 1994-10-04 | Minnesota Mining And Manufacturing Company | Fused cycloalkylimidazopyridines |
| US5525606A (en) * | 1994-08-01 | 1996-06-11 | The United States Of America As Represented By The Department Of Health And Human Services | Substituted 06-benzylguanines and 6(4)-benzyloxypyrimidines |
| DE19505168A1 (de) * | 1995-02-16 | 1996-08-22 | Boehringer Mannheim Gmbh | Spezifische Lipidkonjugate von Nucleosid-Diphosphonaten und deren Verwendung als Arzneimittel |
| US5624677A (en) * | 1995-06-13 | 1997-04-29 | Pentech Pharmaceuticals, Inc. | Controlled release of drugs delivered by sublingual or buccal administration |
| US5693811A (en) * | 1996-06-21 | 1997-12-02 | Minnesota Mining And Manufacturing Company | Process for preparing tetrahdroimidazoquinolinamines |
| US5741908A (en) * | 1996-06-21 | 1998-04-21 | Minnesota Mining And Manufacturing Company | Process for reparing imidazoquinolinamines |
| DE19637209B4 (de) * | 1996-09-12 | 2006-12-14 | Siemens Ag | Verfahren zum Steuern des Antriebsstrangs eines Kraftfahrzeugs und integrierte Antriebsstrangsteuerung |
| HUP9904665A3 (en) * | 1996-10-25 | 2000-11-28 | Minnesota Mining And Mfg Co Sa | Immune response modifier compounds for treatment of th2 mediated and related diseases |
| WO1999024432A1 (fr) * | 1997-11-12 | 1999-05-20 | Mitsubishi Chemical Corporation | Derives de purine et medicament les renfermant en tant qu'ingredient actif |
| CA2311742C (en) * | 1997-11-28 | 2009-06-16 | Sumitomo Pharmaceuticals Co., Ltd. | 6-amino-9-benzyl-8-hydroxypurine derivatives |
| US7001609B1 (en) * | 1998-10-02 | 2006-02-21 | Regents Of The University Of Minnesota | Mucosal originated drug delivery systems and animal applications |
| NZ512628A (en) * | 1999-01-08 | 2004-03-26 | 3M Innovative Properties Co | Formulations and methods for treatment of mucosal associated conditions with an immune response modifier |
| US6486168B1 (en) * | 1999-01-08 | 2002-11-26 | 3M Innovative Properties Company | Formulations and methods for treatment of mucosal associated conditions with an immune response modifier |
| US20020058674A1 (en) * | 1999-01-08 | 2002-05-16 | Hedenstrom John C. | Systems and methods for treating a mucosal surface |
| CZ27399A3 (cs) * | 1999-01-26 | 2000-08-16 | Ústav Experimentální Botaniky Av Čr | Substituované dusíkaté heterocyklické deriváty, způsob jejich přípravy, tyto deriváty pro použití jako léčiva, farmaceutická kompozice a kombinovaný farmaceutický přípravek tyto deriváty obsahující a použití těchto derivátů pro výrobu léčiv |
| EP1244668B1 (en) * | 2000-01-07 | 2006-04-05 | Universitaire Instelling Antwerpen | Purine derivatives, process for their preparation and use thereof |
| US6533645B2 (en) * | 2000-01-18 | 2003-03-18 | Applied Materials, Inc. | Substrate polishing article |
| US6733764B2 (en) * | 2000-06-14 | 2004-05-11 | Alain Martin | Immunostimulator anti-cancer compounds and methods for their use in the treatment of cancer |
| CA2419244A1 (en) * | 2000-09-15 | 2002-03-21 | Virco Bvba | System and method for optimizing drug therapy for the treatment of diseases |
| AU2002211602A1 (en) * | 2000-10-11 | 2002-04-22 | Johns Hopkins University | Polymer controlled delivery of a therapeutic agent |
| US20020127224A1 (en) * | 2001-03-02 | 2002-09-12 | James Chen | Use of photoluminescent nanoparticles for photodynamic therapy |
| ES2278016T3 (es) * | 2001-04-09 | 2007-08-01 | Novartis Vaccines And Diagnostics, Inc. | Compuestos guanidino como agonistas del receptor de melanocortina 4 (mc4-r). |
| DE60228229D1 (de) * | 2001-04-17 | 2008-09-25 | Dainippon Sumitomo Pharma Co | Neue adeninderivate |
| ATE307132T1 (de) * | 2001-06-29 | 2005-11-15 | Cv Therapeutics Inc | Purin derivate als a2b adenosin rezeptor antagonisten |
| US7241890B2 (en) * | 2001-10-30 | 2007-07-10 | Conforma Therapeutics Corporation | Purine analogs having HSP90-inhibiting activity |
| NZ539064A (en) * | 2002-09-27 | 2007-09-28 | Dainippon Sumitomo Pharma Co | Novel adenine compound and use thereof |
| EP1608384A2 (en) * | 2003-01-28 | 2005-12-28 | Shanghai Sunway Biotech Co Ltd | Therapy for primary and metastatic cancers |
| US20040265351A1 (en) * | 2003-04-10 | 2004-12-30 | Miller Richard L. | Methods and compositions for enhancing immune response |
| US20050004144A1 (en) * | 2003-04-14 | 2005-01-06 | Regents Of The University Of California | Combined use of IMPDH inhibitors with toll-like receptor agonists |
| US20050059613A1 (en) * | 2003-07-08 | 2005-03-17 | Bahram Memarzadeh | Compositions and methods for the enhanced uptake of therapeutic agents through the bladder epithelium |
| US20070161582A1 (en) * | 2003-08-08 | 2007-07-12 | Dusan Mijikovic | Pharmaceutical compositions and methods for metabolic modulation |
| WO2005025583A2 (en) * | 2003-09-05 | 2005-03-24 | Anadys Pharmaceuticals, Inc. | Tlr7 ligands for the treatment of hepatitis c |
| EP2145888A1 (en) * | 2003-09-18 | 2010-01-20 | Conforma Therapeutics Corporation | Deazapurine derivatives as HSP90-Inhibitors |
| FR2863890B1 (fr) * | 2003-12-19 | 2006-03-24 | Aventis Pasteur | Composition immunostimulante |
| CN101031287A (zh) * | 2004-03-02 | 2007-09-05 | 麻省理工学院 | 纳米细胞药物递送系统 |
| TWI392678B (zh) * | 2004-03-26 | 2013-04-11 | Dainippon Sumitomo Pharma Co | 9-取代-8-氧基腺嘌呤化合物 |
| CA2587676A1 (en) * | 2004-11-19 | 2006-05-26 | Institut Gustave Roussy | Improved treatment of cancer by double-stranded rna |
| WO2006065234A1 (en) * | 2004-12-10 | 2006-06-22 | University Of Pittsburgh | Use of lipid and hydrogel vehicles for treatment and drug delivery |
| US20070292418A1 (en) * | 2005-04-26 | 2007-12-20 | Eisai Co., Ltd. | Compositions and methods for immunotherapy |
| ES2577514T3 (es) * | 2005-08-22 | 2016-07-15 | The Regents Of The University Of California | Antagonistas de TLR |
| JPWO2007034817A1 (ja) * | 2005-09-22 | 2009-03-26 | 大日本住友製薬株式会社 | 新規アデニン化合物 |
| WO2007034917A1 (ja) * | 2005-09-22 | 2007-03-29 | Dainippon Sumitomo Pharma Co., Ltd. | 新規なアデニン化合物 |
| US20070100146A1 (en) * | 2005-11-03 | 2007-05-03 | Trevor Dzwiniel | Process for the preparation of imidazo[4,5-c]-quinolin-4-amines |
| WO2007142755A2 (en) * | 2006-05-31 | 2007-12-13 | The Regents Of The University Of California | Purine analogs |
| AU2007269557B2 (en) * | 2006-07-07 | 2013-11-07 | Gilead Sciences, Inc. | Modulators of toll-like receptor 7 |
| US7902187B2 (en) * | 2006-10-04 | 2011-03-08 | Wyeth Llc | 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression |
| TW200831104A (en) * | 2006-10-04 | 2008-08-01 | Pharmacopeia Inc | 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression |
| EA019151B1 (ru) * | 2007-02-07 | 2014-01-30 | Дзе Регентс Оф Дзе Юниверсити Оф Калифорния | Конъюгаты синтетических агонистов tlr и их применение |
| ES2541434T3 (es) * | 2007-06-29 | 2015-07-20 | Gilead Sciences, Inc. | Derivados de purina y su uso como moduladores del receptor de tipo Toll 7 |
| WO2009052310A1 (en) * | 2007-10-16 | 2009-04-23 | Cv Therapeutics, Inc | A3 adenosine receptor antagonists |
| KR20110117705A (ko) * | 2009-02-11 | 2011-10-27 | 더 리전트 오브 더 유니버시티 오브 캘리포니아 | 톨-유사 수용체 조정제 및 질병의 치료 |
| US8507507B2 (en) * | 2009-10-22 | 2013-08-13 | Gilead Sciences, Inc. | Modulators of toll-like receptors |
| EP2563401A1 (en) * | 2010-04-30 | 2013-03-06 | Telormedix SA | Methods for inducing an immune response |
| CA2797315C (en) * | 2010-04-30 | 2018-09-11 | Telormedix Sa | Phospholipid drug analogs |
| CN105999275A (zh) * | 2010-09-01 | 2016-10-12 | 诺华有限公司 | 免疫增强剂吸附不溶性金属离子 |
| WO2012038058A1 (en) * | 2010-09-21 | 2012-03-29 | Telormedix Sa | Treatment of conditions by toll-like receptor modulators |
-
2009
- 2009-02-06 EP EP20090709019 patent/EP2259788A4/en not_active Withdrawn
- 2009-02-06 MX MX2010008697A patent/MX2010008697A/es active IP Right Grant
- 2009-02-06 EA EA201001264A patent/EA201001264A1/ru unknown
- 2009-02-06 JP JP2010545884A patent/JP2011511073A/ja active Pending
- 2009-02-06 KR KR1020107019944A patent/KR20100137449A/ko not_active Ceased
- 2009-02-06 CN CN2009801124117A patent/CN102088974A/zh active Pending
- 2009-02-06 US US12/367,172 patent/US20090202626A1/en not_active Abandoned
- 2009-02-06 AU AU2009210655A patent/AU2009210655B2/en not_active Ceased
- 2009-02-06 CA CA2713438A patent/CA2713438A1/en not_active Abandoned
- 2009-02-06 BR BRPI0907907-6A patent/BRPI0907907A2/pt not_active IP Right Cessation
- 2009-02-06 WO PCT/US2009/000771 patent/WO2009099650A2/en not_active Ceased
-
2010
- 2010-07-27 IL IL207246A patent/IL207246A0/en unknown
-
2014
- 2014-04-08 JP JP2014079326A patent/JP2014129425A/ja active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12295950B2 (en) | 2017-06-23 | 2025-05-13 | Birdie Biopharmaceuticals, Inc. | Pharmaceutical compositions |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2009099650A2 (en) | 2009-08-13 |
| EP2259788A4 (en) | 2011-03-16 |
| WO2009099650A3 (en) | 2009-10-22 |
| CN102088974A (zh) | 2011-06-08 |
| AU2009210655B2 (en) | 2013-08-15 |
| KR20100137449A (ko) | 2010-12-30 |
| BRPI0907907A2 (pt) | 2015-07-28 |
| IL207246A0 (en) | 2010-12-30 |
| JP2014129425A (ja) | 2014-07-10 |
| US20090202626A1 (en) | 2009-08-13 |
| JP2011511073A (ja) | 2011-04-07 |
| EA201001264A1 (ru) | 2011-04-29 |
| EP2259788A2 (en) | 2010-12-15 |
| WO2009099650A4 (en) | 2010-01-14 |
| CA2713438A1 (en) | 2009-08-13 |
| AU2009210655A1 (en) | 2009-08-13 |
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