Piperidine-Based Drug Discovery

Front Cover -- Piperidine-Based Drug Discovery -- Copyright Page -- Contents -- 1. Introduction -- 1.1 The Scope of the Material Under Consideration -- 1.2 General Methods of the Synthesis of Piperidine Compounds -- Nucleophilic Substitution Reactions -- Intermolecular Michael Reactions -- Catalyzed Hydroamination Reactions -- Aza-Diels-Alder Reactions -- Intramolecular Ene Reactions -- Ring-Closing Metathesis Reactions -- Synthesis of Piperidin-4-Ones -- The Synthesis of 2,2,6,6-Tetramethyl-4-Oxopiperidine -- Petrenko-Kritschenko Reaction for the Synthesis of 2,6-Disubstituted Piperidin-4-Ones -- Synthesis of Piperidin-4-Ones by Dieckmann Condensation -- Synthesis of Piperidin-4-Ones by Miscellaneous Methods -- Nucleophilic Addition Reactions to the Carbonyl Group of Piperidin-4-Ones -- Nucleophilic Substitution Reactions Involving [alpha]-Carbon of Piperidin-4-Ones -- Piperidin-3-Ones -- Piperidin-2-Ones -- 4-Cyano-4-Phenylpiperidines -- References -- 2. 1-Substituted Piperidines -- 2.1 Derivatives of 1-Phenyl-3-(Piperidin-1-yl)Propan-1-ol -- Trihexyphenidyl (2226) -- Biperiden (1329) -- Pridinol (157) -- Cycrimine (82) -- 2.2 Derivatives of 1-Phenyl-4-(Piperidin-1-yl)Butan-1-ol -- Diphenidol (323) -- Pirmenol (234) -- 2.3 Derivatives of 2-(Piperidin-1-yl)Ethan-1-ol and 3-(Piperidin-1-yl)Propan-1-ol -- Cloperastine (199) -- Benproperine (140) -- Pipazethate (98) -- Raloxifene (7685) -- Flavoxate (452) -- Piperocaine (266) -- 2.4 Derivatives of 3-(Piperidin-1-yl)Propane-1,2-Diol and 3-(Piperidin-1-yl)Propane-1,1-Diol -- Diperodon (147) -- Pipoxolan (25) -- 2.5 Derivatives of 1-Phenyl-3-(Piperidin-1-yl)Propan-1-One -- Dyclonine (584) -- 2.6 Derivatives of 2,2-Diphenyl-4-(Piperidin-1-yl)Butanamide -- Fenpiverinium Bromide (83) -- References -- 3. 2-Substituted and 1,2-Disubstituted Piperidines -- 3.1 Methylphenidate (11968) -- 3.2 Perhexiline (1216)

3.3 Pipradrol (259) -- 3.4 Mefloquine (5370) -- 3.5 Mepivacaine (4176) -- 3.6 Ropivacaine (6847) -- 3.7 Bupivacaine (21293) and Levobupivacaine (1976) -- 3.8 Flecainide (3638) -- 3.9 Encainide (682) -- 3.10 Thioridazine (6558) -- 3.11 Rimiterol (219) -- 3.12 Lobeline (1914) -- 3.13 Argatroban (2627) -- 3.14 Ascomycin (752), Pimecrolimus (1645), Tacrolimus (32436), Sirolimus (22468), Everolimus (8972), and Temsirolimus (2859) -- References -- 4. 3-Substituted and 1,3-Disubstituted Piperidines -- 4.1 Methixene (92) -- 4.2 Tipepidine (132) -- 4.3 Timepidium (83) -- 4.4 Tiagabine (2008) -- 4.5 Piperidolate (72) -- 4.6 Mepenzolate (137) -- 4.7 Pipenzolate (109) -- 4.8 Benidipine (927) -- 4.9 Paroxetine (12203) and Femoxetine (270) -- 4.10 Troxipide (110) -- 4.11 Linagliptin (1133) -- 4.12 Tofacitinib (1130) -- References -- 5. 4-Substituted and 1,4-Disubstituted Piperidines -- 5.1 4-Piperidinols and Their Derivatives -- Periciazine (112) -- Diphenylpyraline (453) -- Ebastine (990) -- Bepotastine (236) -- Lamifiban (257) -- Eucatropine (90) -- Propiverine (664) -- Pentapiperide (22) -- 5.2 4-Phenylpiperidin-4-ols and Their Derivatives -- Haloperidol (41140) -- Bromperidol (515) -- Moperone (218) -- Trifluperidol (613) -- Penfluridol (633) -- Loperamide (3756) -- Alpha-Prodine (502) -- 5.3 Derivatives of 4-Phenylpiperidine-4-Carboxylic Acids -- Pethidine (11164) -- Phenoperidine (506) -- Diphenoxylate (878) -- Levocabastine (854) -- 5.4 Derivatives of (4-Phenylpiperidin-4-yl)Ketones -- Ketobemidone (722) -- Ketanserin (9597) -- 5.5 Derivatives of 4-Phenylpiperidine-4-Carboxamide -- Metopimazine (188) -- Pipamazine (110) -- 5.6 Derivatives of Piperidin-4-Amines -- Indoramin (700) -- Clebopride (419) -- Cinitapride (115) -- Prucalopride (537) -- Lomitapide (241) -- Cisapride (3766) -- Astemizole (2283) -- 5.7 Derivatives of 4-Anylinopiperidines

Fentanyl (31404) -- Carfentanil (614) -- Remifentanil (8289) -- Sufentanil (5866) -- Alfentanil (4090) -- Lorcainide (358) -- 5.8 Derivatives of 4-(N, N-Disubstituted)-Piperidines -- Bamipine (189) and Thenalidine (79) -- Mizolastine (573) -- Sabeluzole (123) -- Lubeluzole (198) -- 5.9 Derivatives of 4-(Dialkylamino)Piperidine-4-Carboxamide -- Pipamperone (438) -- Piritramide (704) -- Carpipramine (144) -- Clocarpramine (72) -- 5.10 Alvimopan (396) -- References -- 6. Piperidin-4-Ylidene Substituted Tricyclic Compounds -- 6.1 Cyproheptadine (6511) -- 6.2 Azatadine (395) -- 6.3 Loratadine (3853) and Desloratadine (1609) -- 6.4 Rupatadine (368) -- 6.5 Ketotifen (3522) -- 6.6 Pizotifen (623) -- 6.7 Alcaftadine (74) -- 6.8 Ritanserin (2840) -- References -- 7. Piperidine-Based Nonfused Biheterocycles With C-N and C-C Coupling -- 7.1 Piperidine-Based Nonfused Biheterocycles With C-N Coupling -- Droperidol (4475) -- Benperidol (1114) -- Timiperone (108) -- Pimozide (5441) -- Zaldaride (39) -- Domperidone (5565) -- Bezitramide (204) -- Benzpiperylon (30) and Piperylon (1) -- 7.2 Piperidine-Based Nonfused Biheterocycles With C-C Coupling -- Risperidone (15970) -- Paliperidone (1968) -- Iloperidone (595) -- Naratriptan (903) -- Sertindole (1242) -- References -- 8. Piperidine-Based Fused Biheterocycles -- 8.1 Thienopyridine Derivatives -- Ticlopidine (12218) -- Clopidogrel (20379) -- Prasugrel (3208) -- 8.2 [gamma]-Carbolines -- Mebhydrolin (74) -- Gevotroline (14) and Carvotroline (12) -- 8.3 5,6,7,8-Tetrahydropyrido[4,3-c]pyridazines -- Endralazine (114) -- Phenindamine (413) -- References -- 9. Piperidine-Based Spiro-Fused Biheterocycles -- 9.1 Spiperone (8015) -- Fluspirilene (493) -- Mosapramine (101) -- Fenspiride (188) -- Clospirazine (7) -- Pazinaclone (43) -- References -- 10. Classes of Piperidine-Based Drugs -- 10.1 Piperidine-Based Analgesics

4-Phenylpiperidines -- 4-Phenylpiperidine-4-Carboxylic Acid Derivatives -- 4-Phenylpiperidin-4-yl Propionates -- 1-(4-Phenylpiperidin-4-yl)Propan-1-Ones -- 4-Anilidopiperidines -- Miscellanous Analgesic Piperidine Derivatives -- 10.2 Piperidine-Based Antipsychotics -- Butyrophenones -- Diphenylbutylpiperidines -- Benzisoxazoles -- Phenothiazines -- Dibenzazepines -- Tetrahydro-[gamma]-Carbolines and 3-(Piperidin-4-yl)-1H-Indoles -- 10.3 Piperidine-Based Antihistamine Drugs -- Piperidin-4-Ylidene Diaryl[a, d][7]Annulenes -- 4-(Benzhydryloxy)Piperidines -- Miscellanous Antihistamine Piperidine Derivatives -- 10.4 Piperidine-Based Anticholinergic Drugs -- Muscarinic Receptor Antagonists -- 10.5 Piperidine-Based Local Anesthetics -- Aminoamide-Type Local Anesthetics -- Amino Ester-Type Local Anesthetics -- 10.6 Piperidine-Based Antithrombotic Drugs -- Antiplatelet Drugs -- Anticoagulant Drugs -- 10.7 Piperidine-Based Antiarrhythmic Drugs -- 10.8 Piperidine-Based Antihypertensive Drugs -- 10.9 Piperidine-Based Drugs for Treating Respiratory System Diseases -- Cough Suppressants -- 10.10 Piperidine-Based Antidepressants -- Selective Serotonin Reuptake Inhibitors -- Norepinephrine-Dopamine Reuptake Inhibitors -- 10.11 Piperidine-Based Antiparkinsonian drugs -- 10.12 Piperidine-Based Hypolipidemic and Antihyperlipidemic Drugs -- 10.13 Piperidine-Based Adrenergic (Sympathomimetic) Drugs -- 10.14 Piperidine-Based Central Nervous System Stimulants -- 10.15 Piperidine-Based Selective Estrogen Receptor Modulators -- 10.16 Piperidine-Based Antianginal Drugs -- 10.17 Piperidine-Based Drugs for Treating Protozoan Infections -- 10.18 Piperidine-Based Antimigraine Drugs -- 10.19 Piperidine-Based Nootropic and Neuroprotective Drugs -- 10.20 Piperidine-Based Antiemetics -- 10.21 Piperidine-Based Antidiarrheal and Prokinetic Drugs -- Antidiarrheals -- Prokinetics

10.22 Piperidine-Based Gastric Antisecretory Drugs -- 10.23 Piperidine-Based Hypoglycemic Drugs -- 10.24 Piperidine-Based Drugs Used in the Treatment of Rheumatoid Arthritis -- 10.25 Piperidine-Based Nicotinic Cholinomimetics -- 10.26 Piperidine-Based Immunosuppresant Drugs -- 10.27 Conclusion -- Index-Trade Names -- Index-Substance Classes -- Back Cover