WO2005009944A1 - Prodrugs of 9-aminomethyl tetracycline compounds - Google Patents

Prodrugs of 9-aminomethyl tetracycline compounds Download PDF

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Publication number
WO2005009944A1
WO2005009944A1 PCT/US2004/020305 US2004020305W WO2005009944A1 WO 2005009944 A1 WO2005009944 A1 WO 2005009944A1 US 2004020305 W US2004020305 W US 2004020305W WO 2005009944 A1 WO2005009944 A1 WO 2005009944A1
Authority
WO
WIPO (PCT)
Prior art keywords
compound
tefracycline
tetracycline
alkyl
formula
Prior art date
Application number
PCT/US2004/020305
Other languages
English (en)
French (fr)
Inventor
Kwasi Ohemeng
Victor Amoo
Oak Kim
Todd Bowser
Haregewein Assefa
Beena Bhatia
Joel Berniac
Jackson Chen
Mark Grier
Laura Honeyman
Jingwen Pan
Rachid Mechiche
Original Assignee
Paratek Pharmaceuticals, Inc.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Paratek Pharmaceuticals, Inc. filed Critical Paratek Pharmaceuticals, Inc.
Priority to EP04756044A priority Critical patent/EP1656341A1/en
Priority to CA2531732A priority patent/CA2531732C/en
Priority to JP2006518681A priority patent/JP4738333B2/ja
Priority to AU2004259661A priority patent/AU2004259661B2/en
Publication of WO2005009944A1 publication Critical patent/WO2005009944A1/en
Priority to IL173022A priority patent/IL173022A/en
Priority to IL212689A priority patent/IL212689A0/en
Priority to IL216089A priority patent/IL216089A0/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
    • C07C237/26—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/40—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings
    • C07C271/42—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/54—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/30—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by halogen atoms, or by nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/40—Ortho- or ortho- and peri-condensed systems containing four condensed rings
    • C07C2603/42—Ortho- or ortho- and peri-condensed systems containing four condensed rings containing only six-membered rings
    • C07C2603/44—Naphthacenes; Hydrogenated naphthacenes
    • C07C2603/46—1,4,4a,5,5a,6,11,12a- Octahydronaphthacenes, e.g. tetracyclines

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  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
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  • Pulmonology (AREA)
  • Dermatology (AREA)
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PCT/US2004/020305 2003-07-09 2004-06-25 Prodrugs of 9-aminomethyl tetracycline compounds WO2005009944A1 (en)

Priority Applications (7)

Application Number Priority Date Filing Date Title
EP04756044A EP1656341A1 (en) 2003-07-09 2004-06-25 Prodrugs of 9-aminomethyl tetracycline compounds
CA2531732A CA2531732C (en) 2003-07-09 2004-06-25 Prodrugs of 9-aminomethyl tetracycline compounds
JP2006518681A JP4738333B2 (ja) 2003-07-09 2004-06-25 ９−アミノメチルテトラサイクリン化合物のプロドラッグ
AU2004259661A AU2004259661B2 (en) 2003-07-09 2004-06-25 Prodrugs of 9-aminomethyl tetracycline compounds
IL173022A IL173022A (en) 2003-07-09 2006-01-08 Tetracycline compounds, a method of treating a tetracycline responsive state in a non-human subject, a pharmaceutical composition and use thereof for the preparation of a medicament
IL212689A IL212689A0 (en) 2003-07-09 2011-05-04 Prodrugs of 9 - aminomethyl tetracycline compounds
IL216089A IL216089A0 (en) 2003-07-09 2011-11-01 Prodrugs of 9-aminomethyl tetracycline compounds

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US48601703P 2003-07-09 2003-07-09
US60/486,017 2003-07-09
US52528703P 2003-11-25 2003-11-25
US60/525,287 2003-11-25
US53012303P 2003-12-16 2003-12-16
US60/530,123 2003-12-16
US56615004P 2004-04-27 2004-04-27
US60/566,150 2004-04-27

Publications (1)

Publication Number Publication Date
WO2005009944A1 true WO2005009944A1 (en) 2005-02-03

Family

ID=34109096

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2004/020305 WO2005009944A1 (en) 2003-07-09 2004-06-25 Prodrugs of 9-aminomethyl tetracycline compounds

Country Status (7)

Country Link
US (1) US20050137174A1 (US20050137174A1-20050623-C00027.png)
EP (2) EP2292590A3 (US20050137174A1-20050623-C00027.png)
JP (3) JP4738333B2 (US20050137174A1-20050623-C00027.png)
AU (1) AU2004259661B2 (US20050137174A1-20050623-C00027.png)
CA (1) CA2531732C (US20050137174A1-20050623-C00027.png)
IL (3) IL173022A (US20050137174A1-20050623-C00027.png)
WO (1) WO2005009944A1 (US20050137174A1-20050623-C00027.png)

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7534766B2 (en) 2004-11-05 2009-05-19 Wyeth Glucuronide metabolites and epimers thereof of tigecycline
JP2009524675A (ja) * 2006-01-24 2009-07-02 パラテック ファーマシューティカルズ インコーポレイテッド テトラサイクリンの経口バイオアベイラビリティーを増加する方法
JP2010138182A (ja) * 2007-04-27 2010-06-24 Paratek Pharmaceuticals Inc アミノアルキルテトラサイクリン化合物の合成方法および精製方法
JP2010532759A (ja) * 2007-07-06 2010-10-14 パラテック ファーマシューティカルズ インコーポレイテッド 置換テトラサイクリン化合物を合成するための方法
EP2287150A3 (en) * 2004-10-25 2011-10-19 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
JP2014221820A (ja) * 2008-03-28 2014-11-27 パラテック ファーマシューティカルズ インコーポレイテッド テトラサイクリン化合物の経口製剤および注射可能な製剤
EP3045449A1 (en) * 2006-12-21 2016-07-20 Paratek Pharmaceuticals, Inc. Tetracycline derivatives for the treatment of bacterial, viral and parasitic infections
US10954250B2 (en) 2011-12-15 2021-03-23 Alkermes Pharma Ireland Limited Prodrugs of secondary amine compounds

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8106225B2 (en) * 1999-09-14 2012-01-31 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
EP2327686A3 (en) * 1999-09-14 2012-08-22 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
EP1263442A1 (en) * 2000-01-24 2002-12-11 Trustees Of Tufts College TETRACYCLINE COMPOUNDS FOR TREATMENT OF i CRYPTOSPORIDIUM PARVUM /i RELATED DISORDERS
JP2004505012A (ja) * 2000-03-31 2004-02-19 トラスティーズ・オブ・タフツ・カレッジ ７−および９−カルバメート、尿素、チオ尿素、チオカルバメート、およびヘテロアリール−アミノ置換テトラサイクリン化合物
EP1286954B1 (en) * 2000-05-15 2004-04-14 Paratek Pharmaceuticals, Inc. 7-substituted fused ring tetracycline compounds
WO2001098236A2 (en) * 2000-06-16 2001-12-27 Trustees Of Tufts College 7-phenyl-substituted tetracycline compounds
US7094806B2 (en) 2000-07-07 2006-08-22 Trustees Of Tufts College 7, 8 and 9-substituted tetracycline compounds
MXPA03000055A (es) 2000-07-07 2003-07-14 Tufts College Compuestos de monociclina sustituidos en posicion 9..
WO2002072506A2 (en) * 2001-03-13 2002-09-19 Paratek Pharmaceuticals, Inc. 7-pyrollyl tetracycline compounds and methods of use thereof
US7553828B2 (en) 2001-03-13 2009-06-30 Paratek Pharmaceuticals, Inc. 9-aminomethyl substituted minocycline compounds
EP1381372A2 (en) 2001-03-14 2004-01-21 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds as synergistic antifungal agents
US8088820B2 (en) * 2001-04-24 2012-01-03 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for the treatment of malaria
US20060194773A1 (en) * 2001-07-13 2006-08-31 Paratek Pharmaceuticals, Inc. Tetracyline compounds having target therapeutic activities
WO2003055441A2 (en) * 2001-08-02 2003-07-10 Paratek Pharmaceuticals, Inc. Medicaments
EP2311799A1 (en) * 2002-01-08 2011-04-20 Paratek Pharmaceuticals, Inc. 4-dedimethylamino tetracycline compounds
IL163931A0 (en) * 2002-03-08 2005-12-18 Paratek Pharm Innc Amino-methyl substituted tetracyline compounds
CN1653037A (zh) 2002-03-21 2005-08-10 帕拉特克药品公司 取代的四环素化合物
EA012136B1 (ru) * 2002-07-12 2009-08-28 Пэрэтек Фамэсьютикэлс, Инк. Замещенные соединения тетрациклина, фармацевтическая композиция и способ лечения чувствительного к тетрациклину состояния у субъекта
JP4686189B2 (ja) 2002-10-24 2011-05-18 パラテック ファーマシューティカルズ インコーポレイテッド Ｒｎａを調節するための置換テトラサイクリン化合物の使用方法
AU2004259659B2 (en) 2003-07-09 2011-11-03 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
US20060287283A1 (en) * 2003-07-09 2006-12-21 Paratek Pharmaceuticals, Inc. Prodrugs of 9-aminomethyl tetracycline compounds
TWI261038B (en) * 2004-08-11 2006-09-01 Bo-Cheng Chen Bicycle gear-shifting handgrip
EP2301916A3 (en) 2004-10-25 2011-09-28 Paratek Pharmaceuticals, Inc. 4-aminotetracyclines and methods of use thereof
AU2006210406C1 (en) * 2005-02-04 2013-03-07 Paratek Pharmaceuticals, Inc. 11a, 12-derivatives of tetracycline compounds
US8440646B1 (en) 2006-10-11 2013-05-14 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for treatment of Bacillus anthracis infections
RU2483072C2 (ru) 2007-11-29 2013-05-27 Актелион Фармасьютиклз Лтд Производные фосфоновой кислоты и их применение в качестве антагонистов рецептора p2y12
KR20100126469A (ko) * 2008-03-05 2010-12-01 파라테크 파마슈티컬스, 인크. 미노사이클린 화합물 및 이들의 사용 방법
TW201014818A (en) * 2008-06-24 2010-04-16 Teva Pharma Processes for preparing prodrugs of gabapentin and intermediates thereof
US20130053381A1 (en) * 2010-05-20 2013-02-28 Novartis Ag 2,4-dioxo-1,4-dihydro-2h-quinazolin-3-yl-sulfonamide derivatives
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